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5175284 Tricyclic thienothiopyrans as pharmaceutical intermediates
New Patents
5175157 CYCLIC AMINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS AND METHODS FOR PREPARING THEM Manfred Psiorz, Joachim Heider, Andreas Bomhard, Manfred Reiffen, Norbert Hauel, Klaus Noll, Berthold Narr, Christia Lillie, Walter Kobinger, Jurgen Dammgen, Biberach, Federal Republic Of Germany assigned to Boehringer Ingelheim GmbH Disclosed are new cyclic amine derivatives of the formula I See Patent for Chemical Structure (I) wherein the substituents are defined in the specification. These compounds are useful as for treating sinus tachycardia.
5175158 CONDENSED DIAZEPINONES, PROCESSES FOR PREPARING THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS Wolfgan Eberlein, Wolfhard Engel, Gunter Trummlitz, Gerhard Mihm, Norbert Mayer, Henri Doods, Biberach, Federal Republic Of Germany assigned to Dr Karl Thomae GmbH New diazepinones of formula I See Patent for Chemical Structure (I) wherein the substituents are defined herein, which compounds exhibit favorable effects on heart rate and in view of the absence of inhibitory effects on gastric acid secretion and salivation and the absence of mydriatic effects, are suitable as vagal pacemakers for the treatment of bradycardia and bradyarrhythmia in human andveterinary medicine.
iii
S(CH2)nOCOOH (II) wherein R1 is hydrogen, nitro, amino, halogen or C 1-4 alkyl; R2 is hydrogen, nitro, amino, halogen, C1-4 alkyl, C1-4 haloalkyl, acyl, C2-5 alkoxycarbonyl, C1-4 alkoxy-C1-4 alkyl, aryloxy-C1-4 alkyl, acyloxyC1-4 alkyl, hydroxy-C1-4 alkyl, acyloxy-C2-5 alkanoyl, C1-4 alkoxy-C2-5 alkanoyl, hydroxyC2-5 alkanoyl, aryloxy-C2-5 alkanoyl or C2-5 haloalkanoyl; R3 is hydrogen, C1-8 alkyl, hydroxy-C1-4 alkyl, C2-5 alkanoyloxy-C1-4 alkyl, aryl, aryl-C1-4 alkyl, heteroaryl, heteroaryl-C1-4 alkyl or aryl, aryl-CI-4 alkyl, heteroaryl or heteroaryl-CI-4 alkyl substituted by at least one substituent selected from the group consisting of halogen, hydroxy, amino, nitro, cyano, C1-4 alkyl, CI-4 alkoxy, C2-5 alkanoylamino, C1-4 haloalkyl, acyloxy, C2-5 • alkoxycarbonyl and carboxyl on the aromatic ring; m is 0, 1 or 2, n is 1 or 2; the bond represented by--is a single bond or a double bond. Thiophene compounds (I) are useful as antianxiety drugs, hypnotics, antiepileptic drugs or nootropics. Thiophene compounds (II) are useful as intermediates for said thiophene compounds (I).
5175281 PHARMACEUTICALLY ACTIVE PYRIMIDINYLPIPERAZINYL STERIOIDS John M McCall, Donald E Ayer, E Jonatha Jacobsen, Frederick VanDoornik, John R Palmer, Harold A Karnes assigned to The Upjohn Company Disclosed are Delta9(ll)-steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C17-side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), Delta 16-steroids (Ilia and IIIb), reduced Aring steroids (IV), Deltal7(20)-steroids (Va and Vb) and Delta9(1 l)-steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.
5175162 THIOPHENE COMPOUNDS AND THEIR PHARMACEUTICAL USES Tohru Nakao, Yasuto Morimoto, Shuzo Takehara, Hiroshi Tanaka, Oita, Japan assigned to Yoshitiomi Pharmaceutical Industries Ltd Thiophene compounds of the formula: See Patent for Chemical Structure (I) and R2SR 1(O)mGP 24/3--R
5175284 TRICYCLIC THIENOTHIOPYRANS AS PHARMACEUTICAL INTERMEDIATES John J Baldwin, Gerald S Ponticello, Kenneth Shepard, Theresa M Williams assigned to Merck & Co Inc
5175157 CYCLIC AMINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS AND METHODS FOR PREPARING THEM Manfred Psiorz, Joachim Heider, Andreas Bomhard, Manfred Reiffen, Norbert Hauel, Klaus Noll, Berthold Narr, Christia Lillie, Walter Kobinger, Jurgen Dammgen, Biberach, Federal Republic Of Germany assigned to Boehringer Ingelheim GmbH Disclosed are new cyclic amine derivatives of the formula I See Patent for Chemical Structure (I) wherein the substituents are defined in the specification. These compounds are useful as for treating sinus tachycardia.
5175158 CONDENSED DIAZEPINONES, PROCESSES FOR PREPARING THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS Wolfgan Eberlein, Wolfhard Engel, Gunter Trummlitz, Gerhard Mihm, Norbert Mayer, Henri Doods, Biberach, Federal Republic Of Germany assigned to Dr Karl Thomae GmbH New diazepinones of formula I See Patent for Chemical Structure (I) wherein the substituents are defined herein, which compounds exhibit favorable effects on heart rate and in view of the absence of inhibitory effects on gastric acid secretion and salivation and the absence of mydriatic effects, are suitable as vagal pacemakers for the treatment of bradycardia and bradyarrhythmia in human andveterinary medicine.
iii
S(CH2)nOCOOH (II) wherein R1 is hydrogen, nitro, amino, halogen or C 1-4 alkyl; R2 is hydrogen, nitro, amino, halogen, C1-4 alkyl, C1-4 haloalkyl, acyl, C2-5 alkoxycarbonyl, C1-4 alkoxy-C1-4 alkyl, aryloxy-C1-4 alkyl, acyloxyC1-4 alkyl, hydroxy-C1-4 alkyl, acyloxy-C2-5 alkanoyl, C1-4 alkoxy-C2-5 alkanoyl, hydroxyC2-5 alkanoyl, aryloxy-C2-5 alkanoyl or C2-5 haloalkanoyl; R3 is hydrogen, C1-8 alkyl, hydroxy-C1-4 alkyl, C2-5 alkanoyloxy-C1-4 alkyl, aryl, aryl-C1-4 alkyl, heteroaryl, heteroaryl-C1-4 alkyl or aryl, aryl-CI-4 alkyl, heteroaryl or heteroaryl-CI-4 alkyl substituted by at least one substituent selected from the group consisting of halogen, hydroxy, amino, nitro, cyano, C1-4 alkyl, CI-4 alkoxy, C2-5 alkanoylamino, C1-4 haloalkyl, acyloxy, C2-5 • alkoxycarbonyl and carboxyl on the aromatic ring; m is 0, 1 or 2, n is 1 or 2; the bond represented by--is a single bond or a double bond. Thiophene compounds (I) are useful as antianxiety drugs, hypnotics, antiepileptic drugs or nootropics. Thiophene compounds (II) are useful as intermediates for said thiophene compounds (I).
5175281 PHARMACEUTICALLY ACTIVE PYRIMIDINYLPIPERAZINYL STERIOIDS John M McCall, Donald E Ayer, E Jonatha Jacobsen, Frederick VanDoornik, John R Palmer, Harold A Karnes assigned to The Upjohn Company Disclosed are Delta9(ll)-steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C17-side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), Delta 16-steroids (Ilia and IIIb), reduced Aring steroids (IV), Deltal7(20)-steroids (Va and Vb) and Delta9(1 l)-steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.
5175162 THIOPHENE COMPOUNDS AND THEIR PHARMACEUTICAL USES Tohru Nakao, Yasuto Morimoto, Shuzo Takehara, Hiroshi Tanaka, Oita, Japan assigned to Yoshitiomi Pharmaceutical Industries Ltd Thiophene compounds of the formula: See Patent for Chemical Structure (I) and R2SR 1(O)mGP 24/3--R
5175284 TRICYCLIC THIENOTHIOPYRANS AS PHARMACEUTICAL INTERMEDIATES John J Baldwin, Gerald S Ponticello, Kenneth Shepard, Theresa M Williams assigned to Merck & Co Inc