4710498 pyridyloxy derivatives

1
PATENT ABSTRACTS 257 4710498 PYRIDYLOXY DERIVATIVES Fujio Nohara, Tomoak Fujinawa, Takaoka, Japan assigned to Ikeda Mohando Co Ltd Pyridyloxy derivatives represented by the gene- ral formula: See Patent for Chemical Structure (1) wherein the substituted group Z is either one of the following groups: See Patent for Chemical Structure See Patent for Tabular Presentation NHHNGNORI2, NHNRI5NRI3RI4, or NO See Patent for Tabular Presentation were pre- pared. These derivatives exert antagonism against Histamine H2-receptors and hence are efficacious for the treatments of digestive ulcers. 4710499 NEW DERIVATIVES OF PYRIDAZINE ACTIVE ON THE CENTRAL NERVOUS SYSTEM Camille G Wermuth, ,lean-Pierre Chambon, Strasbourg, France assigned to Sanofi The present invention relates to derivatives of pyridazine of formula: See Patent for Chemical Structure (I) in which R1 is alkyl or a phenyl group and R2 is H or RI and R2 form, with the carbon atoms to which they are attached, a ben- zene cycle, R3 is H or phenyl and R4 is See Pa- tent for Chemical Structure in which R5 is H or CH3 and R6 is H, OH, OR or OCOR; it also relates to a process for preparing the products of formula (I) and to the drugs containing at least one of said products. 4710500 I-(4'-FLUOROPHENYL)-3,5- SUBSTITUTED INDOLES USEFUL IN THE TREATMENT OF PSYCHIC DISORDERS AND PHARMACEUTICAL COMPOSITIONS THEREOF degree of undesired side effects. Moreover, the invention relates to methods for the preparation of said indole derivatives, pharmaceutical com- positions containing same, and methods for the treatment of psychic disorders, especially psychoses, by administering a therapeutically ac- tive amount of one of said derivatives to a living animal body, including human beings. The novel indole derivatives of the present invention are represented by the following formula: See Patent for Chemical Structure I wherein R is phenyl, op- tionally substituted with halogen, lower alkyl or trifluoromethyl, or a hetero aromatic group, such as 2-thienyl, 3-tbienyl, 2-furoyl, 3-furoyl, 2- thiazol, 2-oxazol, 2-imidazole, 2-pyridyl, 3- pyridyl or 4-pyridyl; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy, cyano, nitro, lower alkylthio, trifluoromethyl, lower alkylsul- fonyl, amino, lower alkylamino or lower di- alkylamino; A is nitrogen or carbon, and the dotted line indicates-when A is carbon-an op- tional bond; R2 is hydrogen, cycloalkyl, lower alkyl or lower alkenyl, optionally substituted with one or two hydroxy groups, any hydroxy group present being optionally esterified with an aliphatic carboxylic acid radical having from two to twenty-four carbon atoms inclusive, or R2 is the group See Patent for Chemical Struc- ture wherein n is an integer of 2-6; X is oxygen or sulfur, or )C double bondX may constitute the group )CH double bond when Y is double bondN- or double bondCH-; Y is oxygen, sulfur, CH2 or N R3, where R3 is hydrogen or lower alkyl, lower alkenyl or a cycloalkylmethyl group, said cycloalkyl having from three to six carbon atoms inclusive; Z is -(CH2)m-, m being 2 or 3, or Z is -CH double bondCH- or 1,2-phenylene op- tionally substituted with halogen or trifluoromethyl, or Z is -CO(or S)CH2-; U is nitrogen or carbon, provided that when R1 is chloro, A is nitrogen and R2 is methyl or cyclo- hexyl, R may not be phenyl; as well as their pharmaceutically acceptable acid addition salts. 4710501 CIRCULATION ACTIVE PYRIMIDINYL- DIHYDROPYRIDINES .lens K Perregaard, Oelstykke, Denmark as- signed to H Lundbeck A/S The present invention relates to novel indole derivatives which have interesting pharma- codynamic effects indicating pronounced ac- tivity in the treatment of psychic disorders, especially psychoses and, at the same time, a low Gerhard Franckowiak, Martin Bechem, Rainer Gross, Michael Kayser, Matthias Schramm, Gunter Thomas, Wuppertal, Federal Republic Of Germany assigned to Bayer Aktiengesel- lschaft Novel compounds of the formula See Patent for Chemical Structure in which R2 is hydrogen or a

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PATENT ABSTRACTS 257

4710498

P Y R I D Y L O X Y D E R I V A T I V E S

Fujio Nohara, Tomoak Fujinawa, Takaoka, Japan assigned to Ikeda Mohando Co Ltd

Pyridyloxy derivatives represented by the gene- ral formula: See Patent for Chemical Structure (1) wherein the substituted group Z is either one of the following groups: See Patent for Chemical Structure See Patent for Tabular Presentation NHHNGNORI2, NHNRI5NRI3RI4, or NO See Patent for Tabular Presentation were pre- pared. These derivatives exert antagonism against Histamine H2-receptors and hence are efficacious for the treatments of digestive ulcers.

4710499

N E W D E R I V A T I V E S O F P Y R I D A Z I N E A C T I V E O N T H E C E N T R A L N E R V O U S S Y S T E M

Camille G Wermuth, ,lean-Pierre Chambon, Strasbourg, France assigned to Sanofi

The present invention relates to derivatives of pyridazine of formula: See Patent for Chemical Structure (I) in which R1 is alkyl or a phenyl group and R2 is H or RI and R2 form, with the carbon atoms to which they are attached, a ben- zene cycle, R3 is H or phenyl and R4 is See Pa- tent for Chemical Structure in which R5 is H or CH3 and R6 is H, OH, OR or OCOR; it also relates to a process for preparing the products of formula (I) and to the drugs containing at least one of said products.

4710500

I - ( 4 ' - F L U O R O P H E N Y L ) - 3 , 5 - S U B S T I T U T E D I N D O L E S U S E F U L

IN T H E T R E A T M E N T O F PSYCHIC D I S O R D E R S A N D

P H A R M A C E U T I C A L C O M P O S I T I O N S T H E R E O F

degree of undesired side effects. Moreover, the invention relates to methods for the preparation of said indole derivatives, pharmaceutical com- positions containing same, and methods for the treatment of psychic disorders, especially psychoses, by administering a therapeutically ac- tive amount of one of said derivatives to a living animal body, including human beings. The novel indole derivatives of the present invention are represented by the following formula: See Patent for Chemical Structure I wherein R is phenyl, op- tionally substituted with halogen, lower alkyl or trifluoromethyl, or a hetero aromatic group, such as 2-thienyl, 3-tbienyl, 2-furoyl, 3-furoyl, 2- thiazol, 2-oxazol, 2-imidazole, 2-pyridyl, 3- pyridyl or 4-pyridyl; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy, cyano, nitro, lower alkylthio, trifluoromethyl, lower alkylsul- fonyl, amino, lower alkylamino or lower di- alkylamino; A is nitrogen or carbon, and the dotted line indicates-when A is carbon-an op- tional bond; R2 is hydrogen, cycloalkyl, lower alkyl or lower alkenyl, optionally substituted with one or two hydroxy groups, any hydroxy group present being optionally esterified with an aliphatic carboxylic acid radical having from two to twenty-four carbon atoms inclusive, or R2 is the group See Patent for Chemical Struc- ture wherein n is an integer of 2-6; X is oxygen or sulfur, or )C double bondX may constitute the group )CH double bond when Y is double bondN- or double bondCH-; Y is oxygen, sulfur, CH2 or N R3, where R3 is hydrogen or lower alkyl, lower alkenyl or a cycloalkylmethyl group, said cycloalkyl having from three to six carbon atoms inclusive; Z is -(CH2)m-, m being 2 or 3, or Z is -CH double bondCH- or 1,2-phenylene op- tionally substituted with halogen or trifluoromethyl, or Z is -CO(or S)CH2-; U is nitrogen or carbon, provided that when R1 is chloro, A is nitrogen and R2 is methyl or cyclo- hexyl, R may not be phenyl; as well as their pharmaceutically acceptable acid addition salts.

4710501

C I R C U L A T I O N A C T I V E P Y R I M I D I N Y L -

D I H Y D R O P Y R I D I N E S

.lens K Perregaard, Oelstykke, Denmark as- signed to H Lundbeck A/S

The present invention relates to novel indole derivatives which have interesting pharma- codynamic effects indicating pronounced ac- tivity in the treatment of psychic disorders, especially psychoses and, at the same time, a low

Gerhard Franckowiak, Martin Bechem, Rainer Gross, Michael Kayser, Matthias Schramm, Gunter Thomas, Wuppertal, Federal Republic Of Germany assigned to Bayer Aktiengesel- lschaft

Novel compounds of the formula See Patent for Chemical Structure in which R2 is hydrogen or a