v17n99 pct 2nd - intellectual property officeonlineservices.ipophil.gov.ph/patgazette/ipas... ·...

Intellectual Property Center, 28 Upper McKinley Rd. McKinley Hill Town Center, Fort Bonifacio, Taguig City 1634 Philippines

Tel. No. 238-6300 Website: http://www.ipophil.gov.ph e-mail: [email protected]

Volume 17 Number 99 Date Released: September 3, 2014

Invention Granted Under R.A. 8293 (PCT)

1 INVENTIONS

[19] INTELLECTUAL PROPERTY PHILIPPINES 45] Issued Date: 20 June 2014 [12] INVENTION GRANT

[21] Registration Number: 1/2008/501356 Document Code: B1

[22] Date Filed: 06/06/2008

[54] Title: THERAPEUTIC AGENT FOR INFLAMMATORY BOWEL DISEASE CONTAINING AS ACTIVE INGREDIENT 2-AMINO-1,3-PROPANEDIOL DERIVATIVE, OR METHOD FOR TREATING INFLAMMATORY BOWEL DISEASE

[71] Proprietors(s): KYORIN PHARMACEUTICAL CO., LTD. [JP]

[72] Inventor(s): RYOTARO KOJIMA[JO]: KOICHI NAKAMURA[JP]: TOKUTAROU YASUE[JP]

[73] Assignee(s): KYORIN PHARMACEUTICAL CO., LTD. [JP]

[74] Attorney / Agent: E.B. ASTUDILLO & ASSOCIATES

[30] Priority Data: 2006-027883 06/02/2006 JP

[51] International Class 8: A 61K 31/137, 45/00, A 61P 1/00, 1/04

[57] Abstract:

A novel therapeutic and prophylactic agent for inflammatory bowel diseases and a method for treating inflammatory bowel diseases. The agent comprises a 2-amino-1,3-propanediol derivative, e.g. 2-amino-2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl-1,3-propanediol hydrochloride) represented by the chemical formula (1) or a pharmaceutically acceptable salt or hydrate thereof.

The agent is useful in the treatment or prevention of Crohn's disease, Crohn's disease in large intestine, intestinal Behcet's disease, ulcerative colitis, bleeding rectal ulcer and pouchitis.

Representative Drawing(s): NONE

[56] Reference(s) Cited and/or Considered: WO 2003029205 GB 2400318 WO 2005105146 KOHNO, Y. ET. AL. CAROLIN, D. ET. AL.

No. of Claims: 5






[22] Date Filed: 08/08/2008

[54] Title: TRANSGENIC BRINJAL (SOLANUM MELONGENA) COMPRISING EE-1 EVENT

[71] Proprietors(s): MAHARASHTRA HYBRID SEEDS COMPANY LIMITED (MAHYCO) [IN]

[72] Inventor(s): CHAR, BHARAT, RAGHUNATH[IN]: GHANDI, RATNAPAL, POPATLAL[IN]

[73] Assignee(s): MAHARASHTRA HYBRID SEEDS COMPANY LIMITED (MAHYCO) [IN]

[74] Attorney / Agent: SALUDO FERNANDEZ AND AQUINO (SAFA LAW)

[30] Priority Data: 368/DEL/2006, 10/02/2006 IN

[51] International Class 8: A 01H 5/08, C 12N 15/82, C 12Q 1/68

[57] Abstract:

The present invention relates to an insect resistant transgenic brinjal plant, plant cell, seed and progeny thereof comprising a specific event EE-I. Further, the invention provides the DNA sequence of the region flanking the insertion locus of the brinjal plant EE-I event. It also relates to a process of detecting the presence or absence of specific brinjal plant EE-I event. The invention also provides a diagnostic method for distinguishing the said specific brinjal plant EE-I elite event in transgenic brinjal plants. The invention further provides a kit for identifying the transgenic plants comprising the elite event EE-I.


[56] Reference(s) Cited and/or Considered: NONE

No. of Claims: 10






[22] Date Filed: 17/10/2008

[54] Title: METHOD OF RECOVERING USEFUL MATERIALS FROM SCRAP OF RARE EARTH-IRON-BORON MAGNET

[71] Proprietors(s): SANTOKU CORPORATION [JP]

[72] Inventor(s): KANEKO, AKIHITO[JP]: OHRAI, HIROSHI[JP]

[73] Assignee(s): SANTOKU CORPORATION [JP]

[74] Attorney / Agent: SAPALO VELEZ BUNDANG & BULILAN LAW OFFICES

[30] Priority Data: 2006-113462 17/04/2006 JP

[51] International Class 8: C 22B 1/04, 5/04, 59/00, 61/00, 7/00, 7/04, C 22C 38/00, 38/10, H 01F 41/00, 41/02

[57] Abstract:

The invention provides a method for recovering useful materials from rare earth-iron-boron based magnet scrap that allows efficient recovery of iron and boron as ferroboron and rare earth elements as oxide, from rare earth-iron-boron based magnet scrap. The method includes the steps of oxidizing rare earth-iron-boron based magnet scrap in an oxygen-containing atmosphere, preparing a mixture for thermit reaction containing the oxidized magnet scrap and aluminum and/ or an aluminum alloy, effecting thermit reaction of the mixture for thermit reaction for generating ferroboron and slag, and separating the ferroboron obtained through the thermit reaction from the slag.


[56] Reference(s) Cited and/or Considered: JPH05132321 A 05/28/1993 FUREDERITSUKU EI SHIYUMITSUTO, ET. AL. JPS61157646 A 07/17/1986 TANAKA MITSUNOBU

No. of Claims: 6






[22] Date Filed: 29/10/2008

[54] Title: HLA ALLELES ASSOCIATED WITH ADVERSE DRUG REACTIONS AND METHODS FOR DETECTING SUCH

[71] Proprietors(s): ACADEMIA SINICA [TW] and PHARMIGENE INC. [TW]

[72] Inventor(s): CHEN, YUAN-TSONG[US]: HUNG, SHUEN LU[TW]: SHEN, CHIH-LUNG[TW]: CHANG, CHI-FENG[TW]: LIN, HSIN-YU[TW]: CHEN, WEI-HSUAN[TW]

[73] Assignee(s): ACADEMIA SINICA [TW] and PHARMIGENE INC. [TW]

[74] Attorney / Agent: CRUZ MARCELO & TENEFRANCIA

[30] Priority Data: 60/800,121 11/05/2006 US

[51] International Class 8: C 12Q 1/68

[57] Abstract:

This invention relates to a method of determining the presence of certain HLA alleles, such as HLA-B*1502 or HLA-B*5801, and a kit for carrying out this method. Also disclosed is a method for assessing whether a patient is at risk for developing adverse drug reactions (e.g., Stevens-Johnson syndrome, toxic epidermal necrolysis, or hypersensitivity syndrome) based on the presence or absence of a genetic marker (e.g., HLA-B*1502, HLA-B*5801, or HLA-B*4601).

Representative Drawing(s):


No. of Claims: 16






[22] Date Filed: 28/11/2008

[54] Title: PHARMACEUTICAL COMPOSITIONS FOR SUSTAINED RELEASE OF PHENYLEPHRINE

[71] Proprietors(s): MERCK SHARP & DOHME CORP. [US]

[72] Inventor(s): SERGIO R. ULLOA[MX]: LUIS JAVIER JUAREZ VARGAS[MX]: JOSE DE JESUS, MATEO VILLACAMPA RAMOS[MX]

[73] Assignee(s): MERCK SHARP & DOHME CORP. [US]

[74] Attorney / Agent: HECHANOVA & CO., INC.

[30] Priority Data: 60/810,019 01/06/2006 US

[51] International Class 8: A 61K 31/137, 31/4545, 9/20, 9/28

[57] Abstract:

The invention discloses a pharmaceutical composition comprising phenylephrine in a sustained-release formulation alone or in combination with another active such as an antihistamine, an analgesic, an antipyretic or a non-steroidal anti-inflammatory agent or a mixture of two or more other actives. In a preferred embodiment, the composition comprises a solid dosage form with hydroxypropyl methylcellulose and carboxymethyl cellulose sodium as a matrix for sustained release of phenylephrine. Phenylephrine is released over a prolonged period of time by the solid dosage form essentially independent of pH.



No. of Claims: 14






[22] Date Filed: 20/02/2009

[54] Title: METHOD OF REDUCING NEURONAL CELL DAMAGE

[71] Proprietors(s): THE UNIVERSITY OF MONTANA, [US]

[72] Inventor(s): THOMAS FREDERICK RAU[US]: DAVID J. POULSEN[US]

[73] Assignee(s): THE UNIVERSITY OF MONTANA, [US]

[74] Attorney / Agent: SYCIP SALAZAR HERNANDEZ AND GATMAITAN

[30] Priority Data: 60/839,974 23/08/2006 US

[51] International Class 8: A 61K 31/445

[57] Abstract:

The present invention is directed to a method of reducing the occurrence of neuronal cell damage, including death, caused by transient cerebral hypoxia and/or ischemia. The method comprises the steps of: diagnosing a subject having a transient cerebral hypoxic and/or ischemic condition; and within 16 hours after onset of the condition, administering to the subject a neuroprotective amount of a pharmaceutical agent. The pharmaceutical agent is preferably selected from the group consisting of: a central nervous system stimulant (CNSS), monoamine neurotransmitter, monoamine oxidase inhibitor (MAOI), tricyclic antidepressant (TCA), or a combination thereof. Preferred agents include amphetamines, methamphetamine, methylphenidate, methylenedioxymethamphetamine, or a combination thereof.



No. of Claims: 17






[22] Date Filed: 05/05/2009

[54] Title: AZAADAMANTANE DERIVATIVES AND METHODS OF USE

[71] Proprietors(s): ABBVIE BAHAMAS LTD. [BS]

[72] Inventor(s):

MICHAEL SCHRIMPF[US]: DIANA NERSESIAN[US]: WILLAIM BUNNELLE[US]: KEVIN SIPPY[US]: MARC SCANIO[US]: RODGER HENRY[US]: PAUL BRACKMEYER[US]: JIANGUO JI[US]: CHIH-HUNG LEE[US]: TAO LI[US]: SHUANG CHEN[US]: LEI SHI[US]: GEOFF, G.Z. ZHANG[US]

[73] Assignee(s): ABBVIE BAHAMAS LTD. [BS]


[30] Priority Data: 11/953,257 05/11/2007 US; 60/856,992 06/11/2006 US and 60/908,143 26/03/2007 US

[51] International Class 8: A 61K 31/395, 31/439, 31/444, 31/496, 31/497, 31/501, 31/506, A 61P 15/08, 17/02, 19/02, 25/00, 25/04, 25/14, 25/18, 25/28, 25/34, 29/00, 3/10, 43/00, 9/00, 9/10, C 07D 451/14, 471/18

[57] Abstract:

The invention relates to compounds that are azaadamantane derivatives, particularly ether- or amine-substituted azaadamantane derivatives and salts and prodrugs thereof, compositions comprising such compounds, methods of using such compounds and compositions, processes for preparing such compounds, and intermediates obtained during such processes.


[56] Reference(s) Cited and/or Considered: BUNNELLE W H ET. AL.: "NEURONAL NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS AS POTENTIAL

ANALGESICS" EXPERT OPINION ON THERAPEUTIC PATENTS, ASHLEY PUBLICATIONS, GB, VOL. 13, NO. 7, 1 JULY 2003, PAGES 1003-1021

BUNNELLE W.H., DART M. J. AND SCHRIMPF M. R.: "DESIGN OF LIGANDS FOR THE NICOTINIC

ACETYLCHOLINE RECEPTORS: THE QUEST FOR SELECTIVITY" CURRENT TOPICS IN MEDICINAL CHEMISTRY, VOL. 4, 2004 - 2004 pages 299-334

WO 99/51601 A (REYNOLDS TOBACCO CO R [US]) 14 OCTOBER 1999 WO 99/51602 A (REYNOLDS TOBACCO CO R [US]) 14 OCTOBER 1999 US 5260303 A (SEARLE & CO [US]) 9 NOVEMBER 1993

No. of Claims: 72






[22] Date Filed: 12/05/2009

[54] Title: LIQUID ANTI-RABIES ANTIBODY FORMULATIONS

[71] Proprietors(s): CRUCELL HOLLAND B.V., [NL]

[72] Inventor(s): ALEXANDER BERTHOLD HENDRIK BAKKER[NL]: WILLEM EGBERT MARISSEN[NL]

[73] Assignee(s): CRUCELL HOLLAND B.V., [NL]

[74] Attorney / Agent: BUCOY POBLADOR & ASSOCIATES

[30] Priority Data: 06125400.9 05/12/2006 EP and 60/872,892 05/12/2006 US

[51] International Class 8: A 61K 9/00, C 07K 16/00

[57] Abstract:

The present invention provides pharmaceutical antibody formulations, in particular liquid pharmaceutical formulations comprising anti-rabies virus antibodies. The formulations can be used in the post exposure prophylaxis of rabies.



No. of Claims: 18






[22] Date Filed: 22/05/2009

[54] Title: COMPOUNDS MODULATING CFMS AND/OR C-KIT ACTIVITY AND USES THEREFOR

[71] Proprietors(s): PLEXXIKON, INC. [US]

[72] Inventor(s): CHAO ZHANG[US]: JIAZHONG ZHANG[US]: PRABHA N. IBRAHIM[US]: DEAN R. ARTIS[US]: RYAN BREMER[US]: GUOXIAN WU[US]: HONGYAO ZHU[US]: MARIKA NESPI[US]

[73] Assignee(s): PLEXXIKON, INC. [US]

[74] Attorney / Agent: AGCAOILI ASSOCIATES

[30] Priority Data: 60/860,749 22/11/2006 US

[51] International Class 8:

A 61K 31/437, 31/444, 31/497, 31/501, 31/506, 31/5377, A 61P 1/04, 11/00, 11/02, 11/06, 13/12, 15/08, 19/02, 19/08, 19/10, 25/00, 25/04, 25/16, 25/28, 29/00, 3/04, 3/10, 35/00, 35/02, 35/04, 37/02, 37/06, 37/08, 43/00, 5/50, 7/00, 9/10, C 07D 471/04

[57] Abstract:

Compounds active on the receptor protein tyrosine kinases c-kit and/or c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or conditions and/or c-fms-mediated diseases or conditions, and methods for the use thereof.


[56] Reference(s) Cited and/or Considered: WO 2005/062795 A 07/14/2005 PLEXXIKON INC. [US]; IBRAHIM PRABHA [US] WO 2006/009755 A 01/26/2006 PLEXXIKON INC. [US]; IBRAHIM PRABHA [US]; HURT CLARENCE R [US] WO 2006/009797 A 01/26/2006 PLEXXIKON INC. [US]; IBRAHIM PRABHA [US]; HURT CLARENCE R [US]

No. of Claims: 103






[22] Date Filed: 28/05/2009

[54] Title: COMPOSITIONS AND METHODS FOR TREATING A NEOPLASM

[71] Proprietors(s): GENENTECH, INC., [US]

[72] Inventor(s): ROBERT D. MASS[US]: GREGORY D. PLOWMAN[US]

[73] Assignee(s): GENENTECH, INC., [US]

[74] Attorney / Agent: HECHANOVA AND CO. INC.

[30] Priority Data: 60/874,460 11/12/2006 US

[51] International Class 8: A 61K 39/395, A 61P 35/00

[57] Abstract:

The present invention relates to compositions and methods for treating neoplasms, including refractory or relapsed neoplasms, using VEGF antagonists. Furthermore, the present invention provides therapy regimens for treating those diseases.



No. of Claims: 16






[22] Date Filed: 24/06/2009

[54] Title: HLA-A* 1101-RESTRICTED WT1 PEPTIDE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

[71] Proprietors(s): INTERNATIONAL INSTITUTE OF CANCER IMMUNOLOGY, INC., [JP]

[72] Inventor(s): HARUO SUGIYAMA[JP]

[73] Assignee(s): INTERNATIONAL INSTITUTE OF CANCER IMMUNOLOGY, INC., [JP]


[30] Priority Data: 2006-355356 28/12/2006 JP

[51] International Class 8: A 61K 31/7088, 38/00, 48/00, A 61P 35/00, 35/02, C 07K 14/82, C 12N 15/12, 5/06, C 12Q 1/02, G 01N 33/574

[57] Abstract:

The present invention relates to an HLA-A*1101-restricted WT1 peptide, specifically, a peptide comprising an amino acid sequence consisting of 9 contiguous amino acids from a WT1 protein, wherein the peptide has an ability to bind to an HLA-A* 1101 molecule, and has an ability to induce a CTL. The present invention also relates to a peptide dimer having an ability to bind to an HLA-A8 1101 molecule and having an ability to induce a CTL, in which two peptide monomers each comprising an amino acid sequence consisting of 9 contiguous amino acids from a WT1 protein and comprising at least one cysteine residue are bound to each other through a disulfide bond. Furthermore, the present invention relates to a polynucleotide encoding the peptide, a pharmaceutical composition for the treatment and/or prevention of a cancer comprising the same and the like.



No. of Claims: 13






[22] Date Filed: 20/08/2009

[54] Title: ARMOR UNIT

[71] Proprietors(s): UNITED STATES GOVERNMENT [US]

[72] Inventor(s): STEPHEN COLLINSWORTH[US]: JEFFREY MELBY[US]

[73] Assignee(s): UNITED STATES GOVERNMENT [US]

[74] Attorney / Agent: SAPALO VELEZ BUNDANG & BULILAN

[30] Priority Data: 60/898,412 31/01/2007 US

[51] International Class 8: E 02B 3/12

[57] Abstract:

Armor units for rubble mound structures including breakwaters, revetments, groins, jetties, and the like. Embodiments are appropriate for ocean, river, lake and reservoir structure armoring, to prevent erosion from damaging hydrodynamic forces resulting from waves and water currents, and the like. An embodiment includes a central rectangular section, three "half H-shaped" appendages, two identical frusta (end members), and a flat bottom with two extrusions, nominally smaller than other appendages and frusta. An embodiment is symmetric about two perpendicularly intersecting vertical planes extending through the centroid of the unit. The three half H-shaped members are connected to outer parts of a side defined as the top and the two longitudinal sides of the central section. The three half H-shaped members and the two end members comprise four-sided frusta that taper from a base at the central rectangular section to four-sided distal ends. For select embodiments, the frusta are generally symmetric.


[56] Reference(s) Cited and/or Considered: US 2002/0114669 A1 08/2009 YANG

No. of Claims: 18






[22] Date Filed: 14/09/2009

[54] Title: DOMINANT GENE SUPPRESSION TRANSGENES AND METHODS OF USING SAME

[71] Proprietors(s): PIONEER HI-BRED INTERNATIONAL, INC, [US]

[72] Inventor(s): ANDREW M. CIGAN[US]: HOWARD P. HERSHEY[US]: TIM W. FOX[US]

[73] Assignee(s): PIONEER HI-BRED INTERNATIONAL, INC, [US]


[30] Priority Data: 11/685,956 14/03/2007 US

[51] International Class 8: C 12N 15/82

[57] Abstract:

Pairs of plants are provided in which complementing constructs result in suppression of a parental phenotype in the progeny. Methods to generate and maintain such plants, and methods of use of said plants, are provided, including use of parental plants to produce sterile plants for hybrid seed production. Also provided are regulatory elements for pollen-preferred expression of linked polynucleotides. Also provided are methods for identifying gene function, methods for testing allelic variants, and methods for repressing transmission of transgenes.



No. of Claims: 3






[22] Date Filed: 02/10/2009

[54] Title: BENZAMIDE COMPOUNDS AND APPLICATIONS THEREOF

[71] Proprietors(s): SHENYANG RESEARCH INSTITUTE OF CHEMICAL INDUSTRY CO., LTD., [CN] and SINOCHEM CORPORATION, [CN]

[72] Inventor(s): BIN LI[CN]: DONG XIANG[CN]: BAOSHAN CHAI[CN]: JING YUAN[CN]: HUIBIN YANG[CN]: HONG ZHANG[CN]: HONGFEI WU[CN]: HAIBO YU[CN]

[73] Assignee(s): SHENYANG RESEARCH INSTITUTE OF CHEMICAL INDUSTRY CO., LTD., [CN] and SINOCHEM CORPORATION, [CN]

[74] Attorney / Agent: VERALAW (DEL ROSARIO RABOCA ET.AL.)

[30] Priority Data: 200710011176.7 30/04/2007 CN and 200810057102.1 30/01/2008 CN

[51] International Class 8: A 01N 43/56, A 01P 3/00, 7/04, C 07D 231/14, 231/16, 401/04

[57] Abstract:

Novel benzamide compounds and intermediate compounds thereof, as shown by formula I and II respectively, wherein the definition of each substituent see the description. Compounds with formula I has excellent insecticidal and fungicidal activities and can be used to control insect pest and diseases.



No. of Claims: 9






[22] Date Filed: 02/10/2009

[54] Title: 5,6-DIHYDRO-1H-PYRIDIN-2-ONE COMPOUNDS

[71] Proprietors(s): ANADYS PHARMACEUTICALS, INC. [US]

[72] Inventor(s):

CHINH VIET TRAN[US]: FRANK RUEBSAM[US]: DOUGLAS ERIC MURPHY[US]: PETER DRAGOVICH[US]: YUEFEN ZHOU[US]: LIJIAN CHEN[US]: DAVID KUCERA[US]: FRITZ BLATTER[CH]: MARTIN VIERTELHAUS[DE]

[73] Assignee(s): ANADYS PHARMACEUTICALS, INC. [US]

[74] Attorney / Agent: PLATON MARTINEZ FLOREZ SAN PEDRO AND LEANO LAW OFFICES

[30] Priority Data: 60/907,478 03/04/2007 US

[51] International Class 8: A 61K 31/5415, 31/549, 45/00, A 61P 31/14, C 07D 417/04, 417/14, 491/08, 513/04

[57] Abstract: The invention is directed to 5,6-dihydro-lH-pyridin-2-one compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.


[56] Reference(s) Cited and/or Considered: US 2005/0075331 A1 04/07/2005 PRATT, ET. AL.

No. of Claims: 120






[22] Date Filed: 10/12/2009

[54] Title: PYRIDAZINONE DERIVATIVES

[71] Proprietors(s): MERCK PATENT GMBH, [DE]

[72] Inventor(s): DIETER DORSCH[DE]: FRANK STIEBER[DE]: OLIVER SCHADT[DE]: ANDREE BLAUKAT[DE]

[73] Assignee(s): MERCK PATENT GMBH, [DE]

[74] Attorney / Agent: BUCOY POBLADOR & ASSOCIATES

[30] Priority Data: 10 2007 032 507.1 12/07/2007 DE

[51] International Class 8: A 61K 31/501, 31/506, 31/5355, 31/5377, 31/55, A 61P 35/00, 35/02, 43/00, C 07D 403/14, 413/10, 413/14, 417/10

[57] Abstract:

Compounds of the formula (I)

in which R1, R2, R3, R4, R4' are each as defined in claim (1) are inhibitors of tyrosine kinases, especially of Met kinase, and can be used, inter alia, for treatment of tumours.



No. of Claims: 311






[22] Date Filed: 15/01/2010

[54] Title: PURIFICATION OF PEGYLATED POLYPEPTIDES

[71] Proprietors(s): F. HOFFMANN -LA ROCHE AG, [CH]

[72] Inventor(s): JOSEF BURG[DE]: KLAUS REICHERT[DE]: AXEL SCHROTH[DE]: HARTMUT SCHURIG[DE]: AXEL WESSNER[DE]

[73] Assignee(s): F. HOFFMANN -LA ROCHE AG, [CH]


[30] Priority Data: 07013959.7 17/01/2007 EP

[51] International Class 8: A 61K 38/18, 47/48, C 07K 1/18

[57] Abstract:

The current invention comprises a method for the purification of mono-PEGylated erythropoietin comprising two cation exchange chromatography steps wherein the same type of cation exchange material is used in both cation exchange chromatography steps and a method for producing a mono-PEGylated erythropoietin in substantially homogeneous form.


[56] Reference(s) Cited and/or Considered: WO 2007/039436 A 04/12/2007 HOFFMANN LA ROCHE, CH WO 01/87329 A1 11/22/2001 HOFFMANN LA ROCHE, CH WO 2004/009627 A 01/29/2004 CANGENE CORP, CA EP 1 064 951 A2 01/03/2001 HOFFMANN LA ROCHE, CH WO 2004/012773 A 02/12/2004 HOFFMANN LA ROCHE, CH

No. of Claims: 29






[22] Date Filed: 19/01/2010

[54] Title: METHODS FOR PRODUCING ARIPIPRAZOLE SUSPENSION AND FREEZE-DRIED FORMULATION

[71] Proprietors(s): OTSUKA PHARMACEUTICAL CO., LTD., [JP]

[72] Inventor(s): TAKAKUNI MATSUDA[JP]: JUNICHI HATANAKA[JP]: SHOGO HIRAOKA[JP]

[73] Assignee(s): OTSUKA PHARMACEUTICAL CO., LTD., [JP]

[74] Attorney / Agent: E.B. ASTUDILLO AND ASSOCIATES

[30] Priority Data: 2007-200088 31/07/2007 JP

[51] International Class 8: A 61K 31/496, 47/32, 47/38, 9/10, 9/19

[57] Abstract:

Disclosed are a method for producing an aripiprazole suspension, wherein the aripiprazole has a mean particle size of 1 to 10 ?m, the method comprising the steps of: (a) combining bulk aripiprazole and a vehicle to form a primary suspension; (b) subjecting the primary suspension to first pulverization using e.g., a high shear pulverizing machine, a dispersion machine that applies shear force to a material to be processed, a colloid mill, an ultrasonic dispersion machine, or a high-pressure jet type emulsifying dispersion machine to form a secondary suspension; and (c) subjecting the secondary suspension to second pulverization using e.g., a high-pressure jet type emulsifying dispersion machine to form a sterile final suspension; and a method for producing a freeze-dried formulation from the aripiprazole suspension.



No. of Claims: 39






[22] Date Filed: 17/02/2010

[54] Title:

IDENTIFICATION OF HUMAN T2R RECEPTORS THAT RESPOND TO BITTER COMPOUNDS THAT ELICIT THE BITTER TASTE IN COMPOSITIONS, AND THE USE THEREOF IN ASSAYS TO IDENTIFY COMPOUNDS THAT INHIBIT (BLOCK) BITTER TASTE IN COMPOSITIONS AND USE THEREOF

[71] Proprietors(s): SENOMYX, INC., [US]

[72] Inventor(s):

XIAODONG LI[US]: ANDREW PATRON[US]: CATHERINE TACHDJIAN[US]: HONG XU[US]: QING LI[US]: ALEXEY PRONIN[US]: GUY SERVANT[US]: LAN ZHANG[US]: THOMAS BRADY[US]: VINCENT DARMOHUSODO[US]: MELISSA ARELLANO[US]: VICTOR SELCHAU[US]: BRETT WEYLAN CHING[US]: DONALD KARANEWSKY[US]: PAUL BRUST[US]: JING LING[US]: WEN ZHAO[US]: CHAD PRIEST[US]

[73] Assignee(s): SENOMYX, INC., [US]


[30] Priority Data: 60/957,129 21/08/2007 US and 61/047,187 23/04/2008 US

[51] International Class 8: G 01N 33/53

[57] Abstract:

The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in e.g. coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g. coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.



No. of Claims: 163






[22] Date Filed: 19/02/2010

[54] Title: NOVEL HERBICIDES

[71] Proprietors(s): SYNGENTA LIMITED, [GB]

[72] Inventor(s): JOHN BENJAMIN TAYLOR[GB]: STEPHANE ANDRE MARIE JEANMART[GB]: CHRISTOPHER JOHN MATHEWS[GB]: MELLONEY TYTE[GB]: STEVEN CHRISTOPHER SMITH[GB]

[73] Assignee(s): SYNGENTA LIMITED, [GB]


[30] Priority Data: 0717082.2 03/09/2007 GB

[51] International Class 8: C 07D 493/08

[57] Abstract:

Compounds of formula (I) wherein the substituents are as defined in claim 1, are suitable for use as herbicides.



No. of Claims: 13






[22] Date Filed: 15/03/2010

[54] Title: IMPROVED ANTIBODY MOLECULES

[71] Proprietors(s): CHUGAI SEIYAKU KABUSHIKI KAISHA, [JP]

[72] Inventor(s):

TOMOYUKI IGAWA[JP]: SHINYA ISHII[JP]: ATSUHIKO MAEDA[JP]: MIKA SAKURAI[JP]: TETSUO KOJIMA[JP]: TATSUHIKO TACHIBANA[JP]: HIROTAKE SHIRAIWA[JP]: HIROYUKI TSUNODA[JP]: YOSHINOBU HIGUCHI[JP]

[73] Assignee(s): CHUGAI SEIYAKU KABUSHIKI KAISHA, [JP]

[74] Attorney / Agent: SAPALO VELEZ BUNDANG & BULILAN LAW OFFICES

[30] Priority Data: 2008-248213 26/09/2008 JP; 2009-060806 13/03/2009 JP and 2009-067925 19/03/2009 JP

[51] International Class 8: A 61K 39/395, A 61P 1/04, 1/16, 11/00, 11/06, 13/12, 15/08, 17/00, 17/06, 19/02, 19/10, 21/00, 25/00, 27/02, 29/00, 3/10, 35/00, 37/02, 37/08, 7/06, 7/08, 9/00, 9/10, C 07K 16/28, C 12N 1/15, 1/19, 1/21, 15/09, 5/10, C 12P 21/08

[57] Abstract:

The present invention provides pharmaceutical compositions comprising second-generation molecules that are superior than TOCILIZUMAB, by altering the amino acid sequences of the variable and constant regions of TOCILIZUMAB, which is a humanized anti-IL-6 receptor IgG1 antibody, to enhance the antigen-neutralizing ability and increase the pharmacokinetics, so that the therapeutic effect is exerted with a less frequency of administration, and the immunogenicity, safety and physicochemical properties (stability and homogeneity) are improved. The present invention also provides methods for producing these pharmaceutical compositions. The present inventors have successfully generated second-generation molecules that are superior to TOCILIZUMAB by appropriately combining amino acid sequence alterations in the CDR domains, variable regions, and constant regions.



No. of Claims: 11






[22] Date Filed: 07/04/2010

[54] Title: NOVEL PATIENT SUBGROUPS FOR THROMBOLYSIS

[71] Proprietors(s): H.LUNDBECK A/S [DK]

[72] Inventor(s): ALICE EBEL[DE]: YASIR ALAA SHAFEEK AL-RAWI[AE]: MARIOLA SOHNGEN[DE]

[73] Assignee(s): H.LUNDBECK A/S [DK]

[74] Attorney / Agent: BARANDA & ASSOCIATES

[30] Priority Data: 07020401.1 18/10/2009 EP

[51] International Class 8: A 61K 38/49, A 61P 9/10

[57] Abstract: A method for treating a stroke patient with thrombolysis, whereas prior treatment the patient is diagnosed in particular for exhibiting cerebral tissue at risk, a cerebral artery occlusion and/or an absolute "mismatch volume".



No. of Claims: 12






[22] Date Filed: 29/04/2010

[54] Title: IMPROVED NOGO-A BINDING MOLECULES AND PHARMACEUTICAL USE THEREOF

[71] Proprietors(s): NOVARTIS AG, [CH] and UNIVERSITY OF ZURICH, [CH]

[72] Inventor(s): CARMEN BARSKE[DE]: ANIS KHURSO MIR[FR]: ALESSANDRA VITALITI[CH]: STEFAN FRENTZEL[DE]: MARTIN SCHWAB[CH]

[73] Assignee(s): NOVARTIS AG, [CH] and UNIVERSITY OF ZURICH, [CH]


[30] Priority Data: 07119847.7, 02/11/2007 EP and 61/001,741, 02/11/2007 US

[51] International Class 8: A 61K 39/395, A 61P 11/06, 25/00, 25/16, 25/28, C 07K 16/22

[57] Abstract:

The present invention provides a binding molecule which is capable of binding to the human NogoA polypeptide or human NiG with a dissociation constant < 1000nM, a polynucleotide encoding such binding molecule; an expression vector comprising said polynucleotide; an expression system comprising a polynucleotide capable of producing a binding molecule; an isolated host cell which comprises an expression system as defined above; the use of such binding molecule as a pharmaceutical, especially in the treatment of a disease of the peripheral (PNS) and central (CNS) nervous system; a pharmaceutical composition comprising said binding molecule; and a method of treatment of a disease of the peripheral (PNS) and/or central (CNS) nervous system.


[56] Reference(s) Cited and/or Considered: WO 2005/028508 A 03/31/2005 NOVARTIS AG ET. AL. WO 2004/052932 A 06/24/2004 NOVARTIS, ET. AL. WO 2007/068750 A 06/21/2007 GLAXO GRP LTD ET. AL. WO 2007/003421 A 01/11/2007 GLAXO GRP LTD WO 2005/061544 A 07/07/2005 GLAXO GRP LTD WIESSNES C. ET. AL.: Anti-Nogo-A Antibody Infusion 24 Hours After Experimental Stroke..."J. Cerebral Bld

Flow and Metabolism, Raven Press, NY, vol. 23, no. 2, February 2003, pp. 154-165, XP008047583 LIEBSCHIER TOMAS ET. AL.: "Nogo-A antibody improves regeneration and locomotion of spinal cord-

injured rats" ANNALS NEURO, vol. 58, no. 5, November 2005, pp. 706-719, XP002473061




FREUND PATRICK, ET. AL.: "Anti-Nogo-A antibody treatment enhances sprouting of corticospinal axons

rostral to a unilateral cervical spinal cord lesion in adult macaque monkey"J. Comparative Neuro, vol. 502, no. 4, June 1, 2007, pp. 644-659 XP002473062

WEINMANN, ET. AL.: "Intrathecally infused antibodies against Nogo-A penetrate the CNS and downregulate

the endogenous neurite growth inhibitor Nogo-A"MOLECULAR AND CELLULAR NEUROSCI, San Diego, US, vol. 32, no. 12, May 2006, pp. 161-173, XP005502160

No. of Claims: 12






[22] Date Filed: 03/08/2010

[54] Title: ALPHA 5-BETA 1 ANTIBODIES AND THEIR USES

[71] Proprietors(s): BRISTOL-MYERS SQUIBB COMPANY [US] and PFIZER INC. [US]

[72] Inventor(s):

STEVEN LEE BENDER[US]: GERALD FRIES CASPERSON[US]: DANA DAN HU-LOWE[US]: XIN JIANG[US]: GANG, LI[US]: MICHAEL AIDAN NORTH[US]: JIANYING WANG[US]: GRANT WICKMAN[GB]: PETER BRAMS[US]: HAICHUN HUANG[US]: BRIGITTE DEVAUX[US]: HAIBIN CHEN[US]: DAWN TANAMACHI[US]: KRISTOPHER TOY[US]: LAN YANG[US]: TIM SPROUL[US]: MARK YAMANAKA[US]

[73] Assignee(s): BRISTOL-MYERS SQUIBB COMPANY [US] and PFIZER INC. [US]



[51] International Class 8: A 61K 39/395, A 61P 35/00, C 07K 16/28

[57] Abstract:

The present disclosure provides isolated monoclonal antibodies, particularly human monoclonal antibodies, or antigen binding portions thereof that specifically bind to integrin a5ß1 with high affinity. Nucleic acid molecules encoding the antibodies of the disclosure, expression vectors, host cells and methods for expressing the antibodies of the disclosure are also provided. Immunoconjugates, bispecific ,olecules and pharmaceutical compositions comprising the antibodies or antigen binding portions thereof are also provided. The disclosure also provides methods for treating various ccancers using the anti-a5ß1 antibodies or antigen binding portions thereof described herein.



No. of Claims: 18






[22] Date Filed: 18/08/2010

[54] Title: COMPOUNDS THAT ARE ERK INHIBITORS

[71] Proprietors(s): MERCK SHARP & DOHME CORP. [US]

[72] Inventor(s):

ALAN B. COOPER[US]: YANG NAN[US]: YOUNGQI DENG[US]: GERALD W . SHIPPS JR.[US]: NENG YANG SHIH[US]: HUGH Y. ZHU[US]: JOSEPH M. KELLY[US]: SUBRAHMANYAM GUDIPATI[US]: RONALD DOLL[US]: MEHUL F. PATEL[US]: JAGDISH A. DESAI[US]: JAMES J-S WANG[US]: SUNIL PALIWAL[US]: HON-CHUNG TSUI[US]: SOBHANA, BABU BOGA[US]: ABDUL-BASIT ALHASSAN[US]: XIAOLEI GAO[US]: LIANG ZHU[US]: XIN YAO[US]

[73] Assignee(s): MERCK SHARP & DOHME CORP. [US]


[30] Priority Data: 61/030,407 21/02/2008 US

[51] International Class 8: A 61K 31/435, C 07D 403/14

[57] Abstract:

Disclosed are the ERK inhibitors of formula 1.0:

and the pharmaceutically acceptable salts, and solvates thereof. Q is a tetrahydopyridinyl ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.



No. of Claims: 62






[22] Date Filed: 23/11/2010

[54] Title: SALTS AND POLYMORPHS OF A TETRACYCLINE COMPOUND

[71] Proprietors(s): PARATEK PHARMACEUTICALS, INC. [US]

[72] Inventor(s): RAYMOND CVETOVICH[US]: TADEUSZ WARCHOL[US]

[73] Assignee(s): PARATEK PHARMACEUTICALS, INC. [US]

[74] Attorney / Agent: CASTILLO LAMAN TAN PANTALEON & SAN JOSE LAW OFFICES

[30] Priority Data: 61/128,712 23/05/2008 US

[51] International Class 8: A 01N 37/18

[57] Abstract:

Crystalline forms, including salts and polymorphs, of a compound useful in the treatment of tetracycline compound-responsive states are provided herein. The crystalline compounds are useful for the treatment or prevention of conditions and disorders such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds in general.



No. of Claims: 17






[22] Date Filed: 17/12/2010

[54] Title: LAUNDRY COMPOSITION

[71] Proprietors(s): THE PROCTER & GAMBLE COMPANY [US]

[72] Inventor(s): LANT, NEIL JOSEPH[GB]

[73] Assignee(s): THE PROCTER & GAMBLE COMPANY [US]

[74] Attorney / Agent: SANTOS PILAPIL AND ASSOCIATES

[30] Priority Data: 08158707.3 20/06/2008 EP

[51] International Class 8: C 11D 3/22

[57] Abstract:

Laundry treatment composition comprising a substituted cellulose having a degree of substitution, DS, of from 0.01 to 0.99 and a specific degree of blockiness, DB, such that either DS+DB is of at least 1or DB+2DS-DS2 is of at least 1.20, and a laundry adjunct ingredient.



No. of Claims: 8






[22] Date Filed: 29/12/2010

[54] Title: IMPROVEMENTS RELATING TO FABRIC CONDITIONERS

[71] Proprietors(s): UNILEVER N.V. [NL]

[72] Inventor(s): JEREMY ROBERT WESTWELL[GB]: JANE HOWARD[GB]: JANICE ELAINE WRIGHT[NL]: ROBERT ALLAN HUNTER[GB]

[73] Assignee(s): UNILEVER N.V. [NL]

[74] Attorney / Agent: OSCAR M. MANAHAN, ESQ.

[30] Priority Data: 08161377.0 29/07/2008 EP

[51] International Class 8: C 11D 1/38, 1/72, 3/04

[57] Abstract:

A composition comprising: i) encapsulated perfume components, ii) a fabric softening active, iii) a stabilising active selected from the group consisting of from 0.05 to 0.2 wt% by the total weight of the composition of water soluble cationic quaternary ammonium compound (s), from 0.65 to 1.5 wt % by the total weight of the composition of non-ionic surfactant (s) and mixtures thereof, and iv) from 0.005 to 0.1 wt% by the total weight of the composition of salt, wherein the encapsulates comprise a capsule wall having surface weak acid groups or moieties, allows the formulation of stable fabric conditioning compositions.



No. of Claims: 17






[22] Date Filed: 11/02/2011

[54] Title: CMET INHIBITORS

[71] Proprietors(s): TAKEDA PHARMACEUTICAL COMPANY LIMITED [JP]

[72] Inventor(s):

JEROME C. BRESSI[US]: SHAOSONG CHU[US]: PHILIP ERICKSON[US]: MALLAREDDY KOMANDLA[US]: LILY KWOK[US]: JOHN D. LAWSON[US]: JEFFREY A. STAFFORD[US]: MICHAEL B. WALLACE[US]: ZHIYUAN ZHANG[US]: SANJIB DAS[US]

[73] Assignee(s): TAKEDA PHARMACEUTICAL COMPANY LIMITED [JP]

[74] Attorney / Agent: Ortega, Bacorro Odulio, Calma & Carbonell

[30] Priority Data: 61/088,959 14/08/2008 US; 61/117,910 25/11/2008 US and 61/161,007 17/03/2009 US

[51] International Class 8: A 61K 31/437, A 61P 35/00, C 07D 471/04, 487/04, 519/00

[57] Abstract:

Compounds of the following formula are provided for use with cMET:

wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.



No. of Claims: 110






[22] Date Filed: 02/03/2011

[54] Title: PICOLINAMIDE DERIVATIVES AS KINASE INHIBITORS

[71] Proprietors(s): NOVARTIS AG [CH]

[72] Inventor(s): MATTHEW T. BURGER[US]: WOOSEOK HAN[US]: JIONG LAN[US]: GISELE NISHIGUCHI[US]

[73] Assignee(s): NOVARTIS AG [CH]



[51] International Class 8: A 61K 31/444, A 61P 35/00, C 07D 401/12, 401/14

[57] Abstract:

New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.



No. of Claims: 171






[22] Date Filed: 25/03/2011

[54] Title: 7-PIPERIDINOALKYL-3, 4-DIHYDROQUINOLONE DERIVATIVE

[71] Proprietors(s): TAISHO PHARMACEUTICAL CO., LTD. [JP]

[72] Inventor(s): KOSUKE KANUMA[JP]: NAOKI MIYAKOSHI[JP]: MADOKA KAWAMURA[JP]: TSUYOSHI SHIBATA[JP]

[73] Assignee(s): TAISHO PHARMACEUTICAL CO., LTD. [JP]

[74] Attorney / Agent: A.Q. ANCHETA AND PARTNERS

[30] Priority Data: 2008-257072 02/10/2008 JP

[51] International Class 8: A 61K 31/4709, A 61P 1/14, 15/10, 25/00, 25/02, 25/08, 25/18, 25/20, 25/22, 25/24, 25/28, 25/36, 3/04, 3/06, 3/10, 43/00, 9/10, 9/12, C 07D 401/06, 401/14

[57] Abstract:

To provide a novel compound, a pharmaceutically acceptable salt or a hydrate thereof useful for preventing or treating for depression, anxiety disorders (such as generalized anxiety disorder, posttraumatic stress disorder, panic disorder, obsessive-compulsive disorder or social anxiety disorder), attention deficit disorder, mania, manic-depressive illness, schizophrenia, mood disorders, stress, sleep disorders, attacks, memory impairment, cognitive impairment, dementia, amnesia, delirium, obesity, eating disorder, appetite disorder, hyperphagia, bulimia, cibophobia, diabetes, cardiovascular diseases, hypertension, dyslipidemia, myocardial infarction, movement disorder (such as Parkinson's disease, epilepsy, convulsion or tremor), drug abuse, drug addiction or sexual dysfunction, based on a melanin-concentrating hormone receptor (MCH receptor) antagonistic action. SOLUTION A compound, a pharmaceutically acceptable salt or a hydrate thereof represented by the formula (I).





[56] Reference(s) Cited and/or Considered: US 2005/209274 A1 (COLLINS C.A., US) 22 September 2005 IYENGAR, R.R. ET. AL.: "An evaluation of 3, 4-methylenedioxy phenyl replacements in the aminopiperidine

chromone class of MCHr1 antagonists", BIO ORG. MED. CHEM. LETT., vol. 17, no. 4, 2007, pages 874-878 WO 2008/044632 A1 (TAISHO PHARM CO LTD, JP) 17 April 2008 KIM N ET. AL.: "Identification of substituted 4-aminopiperidines and 3aminopyrrolidines" vol. 16, no. 20, 15

October 2006, pages 5445-5450

No. of Claims: 42






[22] Date Filed: 25/03/2011

[54] Title: PROCESS FOR THE PRODUCTION OF THE ACTINOBACILLUS PLEUROPNEUMONIAE TOXINS APXI OR APCIII IN A LIQUID CULTURE MEDIUM UNDER SUPPLY OF AIR ENRICHED IN CARBON DIOXIDE

[71] Proprietors(s): INTERVET INTERNATIONAL B.V. [NL]

[72] Inventor(s): CHRISTIAN THEODOOR GERARDUS SMITS[NL]: SIMEN-JAN SLAGMAN[NL]

[73] Assignee(s): INTERVET INTERNATIONAL B.V. [NL]


[30] Priority Data: 08105880.2 27/11/2008 EP and 61/118,766 01/12/2008 US

[51] International Class 8: C 12P 21/02

[57] Abstract:

The current invention peratins to a method to produce RTX-toxins Apx1 or Apx111 by culturing Actinobacillus pleuropneumoniae bacteria in a liquid culturing medium that supports growth of the bacteria, characterised in that air is passed through the medium, wherein the air has a carbon dioxide content above normal atmospheric level to increase RTX-toxin production during the production phase of the RTX-toxins.



No. of Claims: 18






[22] Date Filed: 20/04/2011

[54] Title: SALTS OF ISOBUTYRIC ACID (1 R*, 2R*, 4R*)-2-(2-{[3-(4,7-DIMETHOXY-1-BENZOIMIDAZOL-2-YL)-PROPYL]-METHYL-AMINO}-ETHYL)-5-PHENYL-BICYCLO [2.2.2] OCT-5-EN-2-YL- ESTER

[71] Proprietors(s): ACTELION PHARMACEUTICALS LTD [CH]

[72] Inventor(s): KURT HILPERT[CH]: MARKUS VON RAUMER[CH]: STEFAN ABELE[CH]: STÉPHANIE COMBES[CH]: JACQUES-ALEXIS FUNEL[CH]: FRANCIS HUBLER[CH]: Dorte RENNEBERG[CH]: KATHARINA REICHENBAECHER[CH]

[73] Assignee(s): ACTELION PHARMACEUTICALS LTD [CH]


[30] Priority Data: PCT/IB2008/054351 22/10/2008 IB

[51] International Class 8: A 61K 31/4184, A 61P 9/00, C 07D 235/14

[57] Abstract:

The invention relates to crystalline salts of isobutyric acid (1R*,2R*,4R*)-2-(2-{[3-(4,7-dimethoxy-1H-benzoimidazol-2-yl)-propyl]-methyl-amino}-ethyl)-5-phenyl-bicyclo[2.2.2]oct-5-en-2-yl ester, processes for the preparation thereof, pharmaceutical compositions containing said crystalline salts, and their use as medicaments, especially as calcium channel blockers.



No. of Claims: 13






[22] Date Filed: 14/06/2011

[54] Title: CYCLIC CARBODIIMIDE COMPOUND

[71] Proprietors(s): TEIJIN LIMITED [JP]

[72] Inventor(s): SHOJI, SHINICHIRO[JP]: SUZUKI, HIROTAKA[JP]

[73] Assignee(s): TEIJIN LIMITED [JP]

[74] Attorney / Agent: CARAG JAMORA SOMERA & VILLAREAL LAW OFFICES

[30] Priority Data: 2008-318533 15/12/2008 JP

[51] International Class 8: C 07D 273/08, 498/10, C 08G 85/00

[57] Abstract:

A cyclic carbodiimide compound which is useful as an end-sealing agent for polymer compounds. The cyclic carbodiimide compound is represented by the following formula (i):

(in the above formula, X is a divalent group or a tetravalent group represented by the following formula (i-4). When X is divalent, q is 0 and when X is tetravalent, q is 1. Ar 1 to Ar 4 are each independently an aromatic group. They may be substituted by an alkyl group having 1 to 6 carbon atoms or phenyl group.)



No. of Claims: 12






[22] Date Filed: 08/11/2011

[54] Title: FLUORINATED AMINOTRIAZOLE DERIVATIVES

[71] Proprietors(s): ACTELION PHARMACEUTICALS LTD [CH]

[72] Inventor(s): BUR, DANIEL[CH]: CORMINBOEUF, OLIVIER[CH]: CREN, SYLVAINE[CH]: GRISOSTOMI, CORINNA[CH]: LEROY, XAVIER[CH]: RICHARD-BILDSTEIN, SYLVIA[CH]

[73] Assignee(s): ACTELION PHARMACEUTICALS LTD [CH]


[30] Priority Data: /IB2009/052445 09/06/2009 IB

[51] International Class 8: A 61K 31/4192, A 61P 9/00, C 07D 413/14, 417/14

[57] Abstract:

The invention relates to fluorinated aminotriazole derivatives of formula (I),

wherein A, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds.



No. of Claims: 50

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