4731383 aminoguanidine compounds, their compositions and pharmaceutical uses

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New Patents iii 4731364 4731374 DIHYDROBENZO(B)THIOPHENES AND PHARMACEUTICAL COMPOSITIONS THEREOF USEFUL AS ANTIFUNGALS Dinanath Rane, Russell Pike assigned to Schering Corporation 2-Alkyl-, 2-alkenyl- and 2-alkynyl-2, 3-dihydro- 2-(1H-azolyl(C1-C2)alkyl)benzo(b)thiophenes especially 2-alkyl-, 2-alkenyl- and 2-alkynyl-2, 3- dihydro-3-hydroxy-2-(1 H- 1 -imidazolylmethyl)- 4-,5-,6- and 7-halobenzo(b)thiophenes and related derivatives having antifungal activity are disclosed. Pharmaceutical compositions com- prising compounds of the invention and their use in treating fungal infections in susceptible hosts such as humans are also disclosed. 4731370 PYRIDYL ESTER CONTAINING 1,4-DIHYDROPYRIDINE DERIVATIVES AND SALTS THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME Isao Watanabe, Kaishu Momonoi, Toru Hiraiwa, Satoshi Ono, Joji Nakano, Katsuyuk Nagumo, Hiroyasu Takagi, Toyama, Japan as- signed to Toyama Chemical Co Ltd This invention relates to a novel 1,4- dihydropyridine derivative of the formula See Patent for Chemical Structure wherein R2 is pyridyl, or a salt thereof. These compounds have a vasodilating activity and a platelet aggregation inhibiting activity. Also disclosed are pharma- ceutical compositions containing the same. TETRAHYDRO-BENZTHIAZOLES, THE PREPARATION THEREOF AND THEIR USE AS INTERMEDIATE PRODUCTS OR AS PHARMACEUTICALS Gerhart Griss, Rudolf Hurnaus, Walter Kobinger, Ludwig Pichler, Rudolf Bauer, Joachim Mierau, Dieter Hinzen, Gunter Schingnitz, late of Biberach: Federal Republic Of Germany assigned to Dr Karl Thomae GmbH This invention relates to new tetra- hydrobenzthiazoles of general formula See Pa- tent for Chemical Structure (I) wherein R1 represents a hydrogen atom, an alkyl group, an alkenyl or alkynylk group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nuclei may each be sub- stituted by 1 or 2 halogen atoms, R2 represents a hydrogen atom or an alkyl group, R3 represents a hydrogen atom, an alkyl group a cycloalkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the phenyl nucleus may be substituted by flurorine, chlorine or bromine atoms, R4 represents a hydrogen atom, an alkyl group, an alkyl or alkenyl group, or R3 and R4 together with the nitrogen atom between them represent a pyrrolidino, piperidino, hexamethyleneimino or morpholino group, the enantiomers and the acid addition salts thereof. The compounds of gene- ral formula I above in which one of the groups R1 or R3 or both groups R1 and R3 represent an acyl group are valuable intermediate products for preparing the other compounds of general formula I which have valuable pharmacological properties. The new compounds may be pre- pared using methods known per se. 4731383 AMINOGUANIDINE COMPOUNDS, THEIR COMPOSITIONS AND PHARMACEUTICAL USES Istvan Erczi, Jeno Marosfalvi, Gyorg Rabloczky, Andras Varro, nee Kurthy Maria Kuhar, Istvan Elekes, Laszl Szatmary, Laszl Jas- zlits, Budapest, Hungary assigned to Biogal Gyogyszergyar

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Page 1: 4731383 Aminoguanidine compounds, their compositions and pharmaceutical uses

New Patents iii

4731364 4731374

D I H Y D R O B E N Z O ( B ) T H I O P H E N E 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 U S E F U L A S A N T I F U N G A L S

Dinanath Rane, Russell Pike assigned to Schering Corporation

2-Alkyl-, 2-alkenyl- and 2-alkynyl-2, 3-dihydro- 2-(1H-azolyl(C1-C2)alkyl)benzo(b)thiophenes especially 2-alkyl-, 2-alkenyl- and 2-alkynyl-2, 3- dihydro-3-hydroxy-2-(1 H- 1 -imidazolylmethyl)- 4-,5-,6- and 7-halobenzo(b)thiophenes and related derivatives having antifungal activity are disclosed. Pharmaceutical compositions com- prising compounds of the invention and their use in treating fungal infections in susceptible hosts such as humans are also disclosed.

4731370

P Y R I D Y L E S T E R C O N T A I N I N G 1,4-DIHYDROPYRIDINE

D E R I V A T I V E S A N D S A L T S T H E R E O F 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 C O N T A I N I N G

T H E S A M E

Isao Watanabe, Kaishu Momonoi, Toru Hiraiwa, Satoshi Ono, Joji Nakano, Katsuyuk Nagumo, Hiroyasu Takagi, Toyama, Japan as- signed to Toyama Chemical Co Ltd

This invention relates to a novel 1,4- dihydropyridine derivative of the formula See Patent for Chemical Structure wherein R2 is pyridyl, or a salt thereof. These compounds have a vasodilating activity and a platelet aggregation inhibiting activity. Also disclosed are pharma- ceutical compositions containing the same.

TETRAHYDRO-BENZTHIAZOLES, T H E P R E P A R A T I O N T H E R E O F

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

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

Gerhart Griss, Rudolf Hurnaus, Walter Kobinger, Ludwig Pichler, Rudolf Bauer, Joachim Mierau, Dieter Hinzen, Gunter Schingnitz, late of Biberach: Federal Republic Of Germany assigned to Dr Karl Thomae GmbH

This invention relates to new tetra- hydrobenzthiazoles of general formula See Pa- tent for Chemical Structure (I) wherein R1 represents a hydrogen atom, an alkyl group, an alkenyl or alkynylk group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nuclei may each be sub- stituted by 1 or 2 halogen atoms, R2 represents a hydrogen atom or an alkyl group, R3 represents a hydrogen atom, an alkyl group a cycloalkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the phenyl nucleus may be substituted by flurorine, chlorine or bromine atoms, R4 represents a hydrogen atom, an alkyl group, an alkyl or alkenyl group, or R3 and R4 together with the nitrogen atom between them represent a pyrrolidino, piperidino, hexamethyleneimino or morpholino group, the enantiomers and the acid addition salts thereof. The compounds of gene- ral formula I above in which one of the groups R1 or R3 or both groups R1 and R3 represent an acyl group are valuable intermediate products for preparing the other compounds of general formula I which have valuable pharmacological properties. The new compounds may be pre- pared using methods known per se.

4731383

A M I N O G U A N I D I N E C O M P O U N D S , T H E I R C O M P O S I T I O N S A N D

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

Istvan Erczi, Jeno Marosfalvi, Gyorg Rabloczky, Andras Varro, nee Kurthy Maria Kuhar, Istvan Elekes, Laszl Szatmary, Laszl Jas- zlits, Budapest, Hungary assigned to Biogal Gyogyszergyar