4868192 pharmaceutical compositions and methods using certain 4h-pyrano (3,2-g) quinoline compounds

2
New Patents v is prepared by reacting a solution of an alkali metal salt of 5-chloro-7-iodo-8- hydroxyquinoline with a solution containing an excess of an inorganic or organic zinc salt or a zinc complex having a lower stability constant than that of the complex of formula (I) and separating the product precipitated. 4868177 their preparation. In the general formula (I) See Patentfor Chemical Structure (I) R l, R2, R3, R4 and R5 are the same or different and stand for hydrogen or halogen, or a trihalomethyl, CI-4 alkyl or CI-4 alkoxy group; R6 means hydrogen or a C1-4 alkyl group; and n is 2 or 3. The com- pounds of the general formula (I) are useful for treating diseases arising from a decrease in the dopamine level, i.e. from a hypofunction of the dopaminergic system, and have low toxicity. 1,2,3,4-TETRAHYDRO-I 9- ACRIDINEDIAMINES, PHARMACEUTICAL COMPOSITIONS AND USE Gregory M Shutske, Kevin Kapples assigned to Hoechst-Roussel Pharmaceuticals Inc 4868191 ALKALOID COMPOUNDS, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM There are disclosed compounds having the for- mula See Patentfor Chemical Structure (I) where n is I, 2 or 3; X is hydrogen, loweralkyl, ioweralkoxy, halogen, hydroxy, nitro or trifluoromethyl R1 and R2 are each indepen- dently hydrogen, lower alkyl or arylloweralkyl, but both may not be arylloweralkyl simul- taneously; R3 and R4 are each independently hydrogen, lower alkyl, arylloweraikyl, formyl or lower alkylcarbonyl, or alternatively the group - NR3R4 taken as a whole constitutes See Patent for Chemical Structure See Patent for Tabular Presentation See Patent for Tabular Presentation stereo isomers thereof and pharmaceutically ac- ceptable acid addition salts thereof, which are useful for the treatment of various memory dysfunctions characterized by decreased cholinergic function, such as Alzheimer's dis- ease. Shige Komoto, Y A Gunawardana, Konakadai, FL, Japan assigned to Harbor Branch Oceanographic Institution Inc Novel alkaloid compounds that are derivatives of methaniminoetheno(d, e)acridine are derived from marine sponges of the genus Dercitus. These compounds and pharmaceutical composi- tions containing therapeutic effective amounts thereof are useful as antitumor and immuno- modulatory medications. 4868192 PHARMACEUTICAL COMPOSITIONS AND METHODS USING CERTAIN 4H-PYRANO (3,2-G) QUINOLINE COMPOUNDS 4868184 BENZHYDRYLPIPERAZINES PHARMACEUTICAL COMPOSITIONS THEREOF AND METHOD OF USE Edith Toth, Bela Kiss, Jozse Torley, Eva Palosi, Istvan Hajdu, Laszlo Gro Dora Szporny, Erz- sebet Lapis, Istvan Laszlovszky, Budapest, Hungary assigned to Richter Gedeon Vegyeszeti Gyar The invention relates to novel benzhydryl- piperazine derivatives of the general formula (I) and the acid addition and quaternary am- monium salts thereof, pharmaceutical compositions containing them and a process for Joseph W Totten, Kenneth A Waiters, Old Woodhouse, United Kingdom assigned to Fisons pie A pharmaceutical composition comprising, as active ingredient, 9-ethyl-6, 9-dihydro-4,6- dioxo- i 0-propyl-4H-pyrano(3,2-g)quinoline- 2,8-dicarbo xylic acid or a pharmaceutically acceptable derivative thereofin admixture with a pharmaceutical acceptable adjuvant or excip- ient, the composition being suitable for topical administration to a patient's skin but not suitable for administration orally or to the patient's eye. Also described are methods of treatment of various dermatological disorders comprising topical administration to the skin of a patient suffering from such a disorder of a therapeutically effective quantity of 9-ethyl-6, 9- dihydro-4,6-dioxo-10-propyl-4H-pyrano 3,2-g

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Page 1: 4868192 Pharmaceutical compositions and methods using certain 4H-pyrano (3,2-g) quinoline compounds

N e w Patents v

is prepared by reacting a solution of an alkali metal salt of 5-chloro-7-iodo-8- hydroxyquinoline with a solution containing an excess of an inorganic or organic zinc salt or a zinc complex having a lower stability constant than that of the complex of formula (I) and separating the product precipitated.

4868177

their preparation. In the general formula (I) See Patent for Chemical Structure (I) R l, R2, R3, R4 and R5 are the same or different and stand for hydrogen or halogen, or a trihalomethyl, CI-4 alkyl or CI-4 alkoxy group; R6 means hydrogen or a C1-4 alkyl group; and n is 2 or 3. The com- pounds of the general formula (I) are useful for treating diseases arising from a decrease in the dopamine level, i.e. from a hypofunction of the dopaminergic system, and have low toxicity.

1,2,3,4-TETRAHYDRO-I 9- ACRIDINEDIAMINES, PHARMACEUTICAL

COMPOSITIONS AND USE

Gregory M Shutske, Kevin Kapples assigned to Hoechst-Roussel Pharmaceuticals Inc

4868191

ALKALOID COMPOUNDS, AND PHARMACEUTICAL

COMPOSITIONS CONTAINING THEM

There are disclosed compounds having the for- mula See Patent for Chemical Structure (I) where n is I, 2 or 3; X is hydrogen, loweralkyl, ioweralkoxy, halogen, hydroxy, nitro or trifluoromethyl R1 and R2 are each indepen- dently hydrogen, lower alkyl or arylloweralkyl, but both may not be arylloweralkyl simul- taneously; R3 and R4 are each independently hydrogen, lower alkyl, arylloweraikyl, formyl or lower alkylcarbonyl, or alternatively the group - NR3R4 taken as a whole constitutes See Patent for Chemical Structure See Patent for Tabular Presentation See Patent for Tabular Presentation stereo isomers thereof and pharmaceutically ac- ceptable acid addition salts thereof, which are useful for the treatment of various memory dysfunctions characterized by decreased cholinergic function, such as Alzheimer's dis- ease.

Shige Komoto, Y A Gunawardana, Konakadai, FL, Japan assigned to Harbor Branch Oceanographic Institution Inc

Novel alkaloid compounds that are derivatives of methaniminoetheno(d, e)acridine are derived from marine sponges of the genus Dercitus. These compounds and pharmaceutical composi- tions containing therapeutic effective amounts thereof are useful as antitumor and immuno- modulatory medications.

4868192

PHARMACEUTICAL COMPOSITIONS AND METHODS

USING CERTAIN 4H-PYRANO (3,2-G) QUINOLINE COMPOUNDS

4868184

BENZHYDRYLPIPERAZINES PHARMACEUTICAL

COMPOSITIONS THEREOF AND METHOD OF USE

Edith Toth, Bela Kiss, Jozse Torley, Eva Palosi, Istvan Hajdu, Laszlo Gro Dora Szporny, Erz- sebet Lapis, Istvan Laszlovszky, Budapest, Hungary assigned to Richter Gedeon Vegyeszeti Gyar

The invention relates to novel benzhydryl- piperazine derivatives of the general formula (I) and the acid addition and quaternary am- monium salts thereof, pharmaceutical compositions containing them and a process for

Joseph W Totten, Kenneth A Waiters, Old Woodhouse, United Kingdom assigned to Fisons pie

A pharmaceutical composition comprising, as active ingredient, 9-ethyl-6, 9-dihydro-4,6- dioxo- i 0-propyl-4H-pyrano(3,2-g)quinoline- 2,8-dicarbo xylic acid or a pharmaceutically acceptable derivative thereofin admixture with a pharmaceutical acceptable adjuvant or excip- ient, the composition being suitable for topical administration to a patient's skin but not suitable for administration orally or to the patient's eye. Also described are methods of treatment of various dermatological disorders comprising topical administration to the skin of a patient suffering from such a disorder of a therapeutically effective quantity of 9-ethyl-6, 9- dihydro-4,6-dioxo-10-propyl-4H-pyrano 3,2-g

Page 2: 4868192 Pharmaceutical compositions and methods using certain 4H-pyrano (3,2-g) quinoline compounds

vi New Patents

quinoline-2,8-dicarbo xylic acid or a pharma- ceutically acceptable derivative thereof.

4868195

4868200

NOVEL ENOLAMIDES, PHARMACEUTICAL

COMPOSITIONS AND METHODS OF USE THEREOF FOR ACTIVITY

AS MODULATORS OF THE ARACHIDONIC ACID CASCADE

NOVEL ENOLAMIDES, PHARMACEUTICAL

COMPOSITIONS AND METHODS OF USE THEREOF FOR ACTIVITY

AS MODULATORS OF THE ARACHIDONIC ACID CASCADE

Mary E Carethers, Wiaczeslaw Cetenko, David T Connor, Elizabeth Johnson, John S Kiely, Charles Schwender, Jagadish C Sircar, Roderick Sorenson, Paul C Unangst, Robert F Bruns as- signed to Warner-Lambert Company

Mary E Carethers, Wiaczeslaw A Cetenko, David T Connor, Elizabeth A Johnson, John S Kiely, Charles F Schwender, Jagadish Sircar, Roderick J Sorenson, Paul C Unangst, Robert F Bruns assigned to Warner-Lambert Company

The present invention relates to novel enolamide type compounds, pharmaceutical compositions, and methods of use thereof, useful in the treat- ment of diseases in which products of lipoxy- genase enzyme activity or the action of leukotrienes contribute to the pathological con- dition.

The present invention relates to novel enolamide type compounds, pharmaceutical compositions, and methods of use thereof, useful in the treat- ment of diseases in which products of lipoxy- genase enzyme activity or the action of ieukotrienes contribute to the pathological con- dition.

4868203

BACTERIAL SUBSTANCE AND PHARMACEUTICAL

COMPOSITION THEREOF

Ryuz Ueno, Ryuj Ueno, Hirosh Kita, Ichie Kato, Akihiko Tabata, Takashi Hironaka, Nishinomiya, Japan assigned to Kabushikikaisha Ueno Seiyaku Oyo Kenkyujo

4868199

NOVEL ENOLAMIDES, PHARMACEUTICAL

COMPOSITIONS AND METHODS OF USE THEREOF FOR ACTIVITY

AS MODULATORS OF THE ARACHIDONIC ACID CASCADE

Mary E Carethers, Wiaczeslaw A Cetenko, David T Connor, Elizabeth A Johnson, John S Kiely, Charles F Schwender, Jagadish Sircar, Roderick J Sorenson, Paul C Unangst, Robert F Bruns assigned to Warner-Lambert Company

The present invention relates to novel enolamide type compounds, pharmaceutical compositions, and methods of use thereof, useful in the treat- ment of diseases in which products of lipoxy- genase enzyme activity or the action of leukotrienes contribute to the pathological con- dition.

A bacterial substance UFC-N 11 of the formula: See Patent for Chemical Structure See Patent for Tabular Presentation

4868205

NOVEL ENOLAMIDES, PHARMACEUTICAL

COMPOSITIONS AND METHODS OF USE THEREOF FOR ACTIVITY

AS MODULATORS OF THE ARACHIDONIC ACID CASCADE

Mary Carethers, Wiaczeslaw A Cetenko, David T Connor, Elizabeth A Johnson, John S Kiely, Charles F Schwender, Jagadish Sircar, Roderick J Sorenson, Paul C Unangst, Robert F Bruns as- signed to Warner-Lambert Company

The present invention relates to novel enolamide type compounds, pharmaceutical compositions,