Abstract: This invention relates to a process for the preparation of compounds of the formula: wherein R1 is C1-C6alkyl and the C1-C6alkyl moiety is straight or branched.
Abstract: Derivatives of C2-substituted indan-1-ol compounds of formula I: its physiologically acceptable salts, and its physiologically functional derivatives for the prophylaxis or treatment of obesity are disclosed herein. Compositions comprising the same, methods for preparing the instant compounds, and methods for reducing weight in mammals and for the prophylaxis or treatment of obesity are also described.
Type:
Grant
Filed:
October 27, 2003
Date of Patent:
July 19, 2005
Assignee:
Aventis Pharma Deutschland GmbH.
Inventors:
Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
Abstract: This invention relates to novel compounds of the formula:
wherein
R1 is H or C1-C6alkyl and the C1-C6alkyl moiety is straight or branched;
R2 and R3 are each independently C1-C6alkyl and the C1-C6alkyl moiety is straight or branched; X is Cl, Br or I; or stereoisomers thereof.
Abstract: This invention relates to novel piperidine derivatives of formula (I) and a process for the preparation thereof.
wherein
R1 is H or C1-C6alkyl wherein the C1-C6alkyl moiety is straight or branched;
R2 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; or
stereoisomers or pharmaceutically acceptable acid addition salt thereof.
Abstract: This invention relates to novel compounds of formula:
wherein
R1 is H or C1-C6alkyl and the C1-C6alkyl moiety is straight or branched;
R2 and R3 are each independently C1-C6alkyl and the C1-C6alkyl moiety is straight or branched; or stereoisomers or pharmaceutically acceptable acid addition salt thereof.
Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Type:
Grant
Filed:
April 19, 2000
Date of Patent:
July 16, 2002
Assignee:
Aventis Pharmaceuticals Inc.
Inventors:
Joseph T. Strupczewski, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
Abstract: The invention related to 4-aza-17&bgr;-(cyclopropoxy)-androst-5&agr;-androstan-3-one, 4-aza-17&bgr;-(cyclopropylamino)-androst-4-en-3-one and related compounds and to compositions incorporating these compounds, as well as the inhibition of C17-20 lyase, 5&agr;-reductase and C17&agr;-hydroxylase and to the use of these compounds in the treatment of androgen and estrogen mediated disorders, including benign prostatic hyperplasia, androgen mediated prostate cancer, estrogen mediated breast cancer and to DHT-mediated disorders such as acne. Disorders relating to the oversynthesis of cortisol, for example, Cushing's Syndrome, are also included. The treatment of androgen-dependent disorders also includes a combination therapy with known androgen-receptor antagonists, such as flutamide.
Type:
Grant
Filed:
February 11, 1997
Date of Patent:
April 2, 2002
Assignee:
Aventis Pharmaceuticals Inc.
Inventors:
James R. Pribish, Cynthia A. Gates, Philip M. Weintraub
Abstract: The present invention relates to novel substituted N-methyl-N-(4-(piperidin-1-yl)-2-(aryl)butyl)benzamide derivatives of the formula
stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonists. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.
Type:
Grant
Filed:
June 9, 1999
Date of Patent:
October 2, 2001
Assignee:
Aventis Pharmaceuticals Inc.
Inventors:
George P. Maynard, John M. Kane, Larry D. Bratton, Elizabeth M. Kudlacz
Abstract: The present invention provides novel compounds such as certain aryloxy indanamines which are useful as anti-depressants and as inhibitors of synaptic norepinephrine and serotonin uptake. The present invention also provides an improvement in the treatment of depression which comprises inhibiting synaptic serotonin and epinepherine uptake.
Abstract: The present invention provides 4-nitro-.DELTA..sup.4 -3-ketosteroids, their use as steroid C.sub.17-20 lyase and 5.alpha.-reductase inhibitors and to a novel process for preparing a compound of the formula: ##STR1## comprising sequentially: a) reacting a starting compound of the formula ##STR2## with an effective amount of a strong base at an elevated or suitable temperature for a time sufficient to create the corresponding thermodynamic dienolate, followed by addition of a neutral nitrating agent to produce the 4-nitrosteroid; and then;b) reacting the 4-nitrosteroid with a suitable reducing agent.
Type:
Grant
Filed:
February 24, 1999
Date of Patent:
November 23, 1999
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Philip M. Weintraub, Michael R. Angelastro, Cynthia A. Gates, Gary Alan Flynn, Timothy Thomas Curran, Chi-Hsin Richard King
Abstract: The invention discloses 3-ketosteroids of the following formula used to inhibit steroid C.sub.17-20 lyase: ##STR1## wherein R is OH, C.sub.1 -C.sub.6 alkanoyl, C.sub.1 -C.sub.6 alkanoyloxy, C.sub.1 -C.sub.4 alkanol, COCH.sub.2 OH, CO.sub.2 H, CONR.sub.7 R.sub.8, cyclopropyloxy, cyclopropylamino, acetylthioalkane, 2,2-dimethyldioxolan4-yl, 1,2-dihydroxyethyl and C.sub.1-4 alkylthiol;R.sub.1 is hydrogen, hydroxy or C.sub.1-6 alkyl;R and R.sub.1 together may indicate .dbd.O, that is an oxygen double bonded to the 17 carbon;R.sub.2, R.sub.3, and R.sub.4 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.5 and R.sub.6 are each independently hydrogen or OH;R.sub.5 and R.sub.6 together may indicate .dbd.O, that is an oxygen double bonded to the 11 carbon;R.sub.7 is hydrogen or C.sub.1 -C.sub.8 alkyl;R.sub.8 is C.sub.1 -C.sub.8 alkyl; andwith the proviso that, when R is OH, then R.sub.1 is hydrogen; andwith the proviso that, when R.sub.5 is OH, then R.sub.6 is hydrogen.
Type:
Grant
Filed:
January 22, 1998
Date of Patent:
October 12, 1999
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Philip M. Weintraub, Michael R. Angelastro, Cynthia A. Gates, Timothy Thomas Curran, Gary Alan Flynn, Chi-Hsin Richard King
Abstract: The present invention relates to novel N-methyl-N-(4-(4-(1H-benzimidazol-2-yl)?1,4!diazepan-1-yl)-2-(aryl)butyl)b enzamide derivatives of the formula: ##STR1## stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonists. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.
Type:
Grant
Filed:
March 6, 1998
Date of Patent:
August 3, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
George D. Maynard, John M. Kane, Christopher R. Dalton, Braulio Santiago, Elizabeth M. Kudlacz, Larry D. Bratton
Abstract: The present invention relates to novel substituted N-methyl-N-(4-(4-(1H-benzimidazol-2-yl-amino)piperidin-1-yl)-2-(aryl)butyl )benzamide derivatives of the formula: ##STR1## stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonists. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.
Type:
Grant
Filed:
January 6, 1997
Date of Patent:
July 13, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
George Daniel Maynard, John Michael Kane, Braulio Santiago, Elizabeth Mary Kudlacz, Larry Don Bratton, Christopher Robin Dalton
Abstract: The present invention provides novel compounds such as certain aryloxy indanamines which are useful as anti-depressants and as inhibitors of synaptic norepinephrine and serotonin uptake. The present invention also provides an improvement in the treatment of depression which comprises inhibiting synaptic serotonin and epinepherine uptake.
Abstract: The invention discloses 3-ketosteroids of the following formula used to inhibit steroid 5.alpha.-reductase: ##STR1## wherein R is OH, C.sub.1 -C.sub.6 alkanoyl, C.sub.1 -C.sub.6 alkanoyloxy, C.sub.1 -C.sub.4 alkanol, COCH.sub.2 OH, CO.sub.2 H, CONR.sub.7 R.sub.8, cyclopropoxy, acetylthioalkane, cyclopylamino, 2-2-dimethyldioxolan-4-yl, 1,2-dihydroxyethyl and C.sub.1-4 alkanethiol;R.sub.1 is hydrogen, hydroxy or C.sub.1-6 alkyl;R.sub.1 and R.sub.2 together may indicate .dbd.O, that is an oxygen double bonded to the 17 carbon;R.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen or C.sub.1-6 alkyl;R.sub.5 and R.sub.6 are each independently hydrogen or OH;R.sub.5 and R.sub.6 together may indicate .dbd.O, that is an oxygen double bonded to the 11 carbon;R.sub.7 is hydrogen or C.sub.1-8 alkyl;R.sub.8 is C.sub.1-8 alkyl; andwith the proviso that, when R is OH, then R.sub.1 is hydrogen; and with the proviso that, when R.sub.5 is OH, then R.sub.6 is hydrogen.
Type:
Grant
Filed:
November 14, 1997
Date of Patent:
February 9, 1999
Assignee:
Merrell Pharmaceuticals, Inc.
Inventors:
Timothy Thomas Curran, Chi-Hsin Richard King, Gary Alan Flynn, Philip M. Weintraub, Michael R. Angelastro, Cynthia A. Gates
Abstract: This invention relates to compounds of the formula ##STR1## wherein X is halogen, hydroxy, (C.sub.1 -C.sub.6)alkoxy, amino or trifluoromethyl; andY is --CN or --NR.sup.1 R.sup.2 ;wherel is an integer of 0, 1 or 2;m is an integer of 0, 1 or 2;n is an integer of 2, 3 or 4, except when Y is CN, in which case n can also be 1;R.sup.1 is hydrogen, (C.sub.1 -C.sub.6)alkyl or (C.sub.1 -C.sub.6)alkylcarbonyl;R.sup.2 is hydrogen, (C.sub.1 -C.sub.10)alkylcarbonyl, (C.sub.3 -C.sub.12)cycloalkylcarbonyl, hydroxy-(C.sub.1 -C.sub.6)alkylcarbonyl, phenylcarbonyl, thienylcarbonyl or benzothienylcarbonyl;orR.sub.1 and R.sup.2 together with nitrogen atom to which they are attached form the ring ##STR2## where A is C.dbd.O or CH.sub.2 ;andB is C.dbd.O, CHOH, CH.sub.2 or CH.sub.2 CH.sub.2 ; andZ is halogen, hydroxy, (C.sub.1 -C.sub.6)alkoxy, amino or trifluoromethyl p is 0 or 1; and pharmaceutically acceptable acid addition salts thereof, pharmaceutical compositions thereof and their use for the treatment of psychoses.
Type:
Grant
Filed:
June 6, 1997
Date of Patent:
September 1, 1998
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Nicholas Joseph Hrib, John Gerard Jurcak, Abdul E. Mutlib
Abstract: A compound selected from the following formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, m and n are as defined in the specification having antipsychotic activity.
Type:
Grant
Filed:
October 9, 1996
Date of Patent:
September 1, 1998
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Nicholas Joseph Hrib, John Gerard Jurcak
Abstract: This invention relates to a method of treating a patient in need of relief from convulsions which comprises administering to such a patient a convulsion-alleviating amount of a compound of the formula ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, m and n are as defined within.
Type:
Grant
Filed:
July 8, 1996
Date of Patent:
July 7, 1998
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Francis Parker Huger, Craig Paul Smith, Sathapana Kongsamut, Lei Tang
Abstract: This invention relates to silylated aromatic fluoroketones possessing acetylcholinesterase-inhibiting properties and to their use in the treatment of Alzheimer disease and senile dementia.
Type:
Grant
Filed:
January 31, 1995
Date of Patent:
December 2, 1997
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Daniel Schirlin, Jean-Noel Collard, Jean-Marie Hornsperger, Prakash R. Keshary