Cyano Attached Indirectly To The Piperidine Ring By Nonionic Bonding Patents (Class 546/230)
  • Publication number: 20030203898
    Abstract: The invention relates to novel diphenylmethane derivatives, processes for their preparation and their use in medicaments, in particular for the indications of arteriosclerosis and hypercholesterolaemia.
    Type: Application
    Filed: March 11, 2003
    Publication date: October 30, 2003
    Inventors: Helmut Haning, Gunter Schmidt, Josef Pernerstorfer, Hilmar Bischoff, Carsten Schmeck, Verena Vohringen, Michael Woltering, Axel Kretschmer, Christiane Faeste
  • Publication number: 20030203935
    Abstract: Intermediates represented by the following formula: 1
    Type: Application
    Filed: March 24, 2003
    Publication date: October 30, 2003
    Applicant: TEIJIN LIMITED
    Inventors: Tomohisa Nakada, Takayuki Hara, Yasunobu Takano
  • Publication number: 20030203919
    Abstract: Dipeptide nitrile Cathepsin K inhibitors of formula I, and pharmaceutically acceptable salts or esters thereof 1
    Type: Application
    Filed: April 9, 2003
    Publication date: October 30, 2003
    Inventor: Martin Missbach
  • Patent number: 6605623
    Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
    Type: Grant
    Filed: June 21, 2000
    Date of Patent: August 12, 2003
    Assignee: Bristol-Myers Squibb Pharma Co.
    Inventors: Soo S. Ko, George V. DeLucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
  • Publication number: 20030144322
    Abstract: The invention provides a compound of formula (I): 1
    Type: Application
    Filed: October 23, 2002
    Publication date: July 31, 2003
    Inventors: Alan P. Kozikowski, Gian Luca Araldi
  • Patent number: 6562965
    Abstract: The present invention relates to processes for the production of &agr;-aryl-&bgr;-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) receptor antagonists.
    Type: Grant
    Filed: July 6, 2000
    Date of Patent: May 13, 2003
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Jiacheng Zhou, Lynette May Oh, Philip Ma
  • Publication number: 20030078428
    Abstract: Phenylamino benzhydroxamic acid derivatives of formula (I) where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as psoriasis and restenosis.
    Type: Application
    Filed: June 4, 2002
    Publication date: April 24, 2003
    Inventors: Stephen Douglas Barrett, Alexander James Bridges, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Haile Tecle
  • Patent number: 6552022
    Abstract: The invention relates to therapeutic benzamide compounds of formula (I) wherein A, X, Z, R1, Y, R2, R3, are as defined herein, and physiologically acceptable salts, solvates or derivatives thereof. The present invention also provides pharmaceutical compositions, processes for the preparation of compounds of formula (I) and their use in the treatment of conditions mediated by ApoB-100 regulation.
    Type: Grant
    Filed: May 15, 2001
    Date of Patent: April 22, 2003
    Assignee: SmithKline Beecham Corporation
    Inventor: Alain Claude-Marie Daugan
  • Patent number: 6538137
    Abstract: Intermediates represented by the following formula: (wherein R1 is a hydrogen atom, an alkyl group, an aryl group, an aralkyl group or the like; X is a carboxyl group, an alkoxycarbonyl group, an aryloxycarbonyl group, an aralkoxycarbonyl group, a formyl group, —CH2—Y, —CHZ1Z2, —CH(OR4)OR5 or the like), in the synthesis of biphenylamidine derivatives to be used as inhibitors for an activated blood coagulation factor X, and a process for preparing the same.
    Type: Grant
    Filed: November 7, 2001
    Date of Patent: March 25, 2003
    Assignee: Teijin Limited
    Inventors: Tomohisa Nakada, Takayuki Hara, Yasunobu Takano
  • Publication number: 20020198214
    Abstract: The invention is directed to inhibition of p38-&agr; kinase using compounds of the formula 1
    Type: Application
    Filed: November 20, 2001
    Publication date: December 26, 2002
    Inventors: Babu Mavunkel, Sundeep Dugar, Gregory Luedtke, Xuefei Tan, Glenn McEnroe
  • Patent number: 6486180
    Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
    Type: Grant
    Filed: December 17, 1999
    Date of Patent: November 26, 2002
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Soo S. Ko, Cheryl McArdle Clark, George V. DeLucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
  • Publication number: 20020151566
    Abstract: PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs.
    Type: Application
    Filed: January 22, 2002
    Publication date: October 17, 2002
    Applicant: MEMORY PHARMACEUTICALS CORP.
    Inventors: Richard A. Schumacher, William F. Brubaker, Michael De Vivo, Hans-Jurgen Ernst Hess, Allen Hopper, Ashok Tehim, Ruiping Liu, Axel Unterbeck
  • Patent number: 6458812
    Abstract: Amide derivatives of 1,4 di-substituted piperidine compounds of the formula: or a pharmaceutically acceptable salt, ester or solvate thereof, wherein R1 is optionally substituted cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or heteroaryl; R2 is H, alkyl, or optionally substituted cycloalkyl, cycloalkylalkyl, heterocycloalkyl, bridged cycloalkyl, or bridged heterocycloalkyl; R3 is alkyl or —CH2OH; and R4 is H or alkyl; are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed.
    Type: Grant
    Filed: December 17, 2001
    Date of Patent: October 1, 2002
    Assignee: Schering Corporation
    Inventors: Brian A. McKittrick, Guihua Guo, Zhaoning Zhu, Yuanzan Ye
  • Patent number: 6441001
    Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
    Type: Grant
    Filed: December 17, 1999
    Date of Patent: August 27, 2002
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Paul S. Watson, Soo S. Ko, George V. Delucca, Joseph B. Santella, III, Dean A. Wacker, John V. Duncia
  • Publication number: 20020099214
    Abstract: There is provided a compound of formula I, 1
    Type: Application
    Filed: March 27, 2002
    Publication date: July 25, 2002
    Applicant: Pfizer Inc.
    Inventors: Stephen Paul Gibson, Ivan Tommasini, David Morris Gethin, Richard Edward Armer
  • Patent number: 6365626
    Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.
    Type: Grant
    Filed: December 7, 2000
    Date of Patent: April 2, 2002
    Assignee: Parker Hughes Institute
    Inventors: Fatih M. Uckun, Yaguo Zheng, Sutapa Ghosh
  • Patent number: 6358979
    Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R3, R4, R5, R6, R7, R8, X, n, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
    Type: Grant
    Filed: June 8, 2000
    Date of Patent: March 19, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Paul E. Finke, Kerry A. Hilfiker, Malcolm MacCoss, Kevin T. Chapman, Jennifer L. Loebach, Sander G. Mills, Ravi N. Guthikonda, Shrenik K. Shah, Dooseop Kim, Dong-Ming Shen, Bryan Oates
  • Patent number: 6313097
    Abstract: Compounds of the formula (I) wherein A, R, R1, R2, X1, X2, X3, and Y are as defined herein, and the tautomers and the pharmaceutically acceptable salts thereof, including pharmaceutical compositions containing these compounds, and their use in the selective antagonization of calcitonin gene-related peptide (CGRP) and in the treatment or prophylaxis of migraine or cluster headaches, non-insulin-dependent diabetes mellitus, inflammation, allergic rhinitis, asthma, morphine tolerance, menopausal hot flashes, and diseases characterized by excessive vasodilatation and consequent reduction in blood-flow.
    Type: Grant
    Filed: March 10, 2000
    Date of Patent: November 6, 2001
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Wolfgang Eberlein, Klaus Rudolf, Wolfhard Engel, Henri Doods, Gerhard Hallermayer
  • Patent number: 6303652
    Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.
    Type: Grant
    Filed: March 19, 1999
    Date of Patent: October 16, 2001
    Assignee: Hughes Institute
    Inventors: Fatih M. Uckun, Yaguo Zheng, Sutapa Ghosh
  • Patent number: 6303637
    Abstract: The present invention relates to a class of heterocyclic compounds of Formula I that are useful as potassium channel inhibitors to treat autoimmune disorders, cardiac arrhythmias, and the like.
    Type: Grant
    Filed: October 21, 1999
    Date of Patent: October 16, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Jianming Bao, Andrew Kotliar, Frank Kayser, William H. Parsons, Kathleen M. Rupprecht, Christopher F. Claiborne, David A. Claremon, Nigel Liverton, Wayne J. Thompson
  • Patent number: 6294575
    Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.
    Type: Grant
    Filed: October 16, 2000
    Date of Patent: September 25, 2001
    Assignee: Parker Hughes Institute
    Inventors: Fatih M. Uckun, Yaguo Zheng, Sutapa Ghosh
  • Patent number: 6231786
    Abstract: In the fluorinated azoles of the formula (I) R1(—A1)a—T—(A2—)b(M—A3—)cR2   (I) the symbols and indices have -the following meanings: T is undirected and is 4-fluorothiazole-2,5-diyl, 5-fluorothiazole-2,4-diyl, 4-fluorooxazole-2,5-diyl, 5-fluorooxazole-2,4-diyl or 4-fluoroisoxazole-2,5-diyl; R1 and R2 are identical or different and are hydrogen or a straight-chain or branched C1-20-alkyl or C2-20-alkenyl radical (with or without asymmetrical carbon atoms); A1, A2 and A3 are identical or different and are, for example, phenylene-1,4-diyl or cyclohexane-1,4-diyl; M is undirected and is —OC(═O)—, —OCH2—, —CH2CH2—, —OC(═O)CH2CH2—, —OCH2CH2CH2—, —C≡C—, —CH2CH2CH2CH2— or a single bond; a, b and c, independently of one another, are 0 or 1, with the proviso that the sum a+b+c is 1 or 2.
    Type: Grant
    Filed: January 18, 2000
    Date of Patent: May 15, 2001
    Assignee: Clariant GmbH
    Inventors: Rainer Wingen, Barbara Hornung, Ayako Ogawa, Wolfgang Schmidt
  • Patent number: 6221898
    Abstract: There is provided compounds of formula I, wherein R1, R2, R3, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
    Type: Grant
    Filed: August 29, 1997
    Date of Patent: April 24, 2001
    Assignee: Astra Aktiebolag
    Inventor: Thomas Antonsson
  • Patent number: 6160010
    Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.
    Type: Grant
    Filed: July 22, 1999
    Date of Patent: December 12, 2000
    Assignee: Parker Hughes Institute
    Inventors: Fatih M. Uckun, Yaguo Zheng, Sutapa Ghosh
  • Patent number: 6143896
    Abstract: A process for the alkylation of compounds of the formula II ##STR1## where the reaction with the alkylating agent is carried out in the presence of a base and a trialkylamine and/or trialkylphosphine.
    Type: Grant
    Filed: December 16, 1998
    Date of Patent: November 7, 2000
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Gerhard Korb, Hans-Wolfram Flemming, Rudolf Lehnert
  • Patent number: 6124323
    Abstract: Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 4-substituted piperidine analogs are selective active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, psychosis, anxiety, migraine headaches, glaucoma, CMV retinitis, aminoglycoside antibiotics-induced hearing loss, convulsions, chronic pain, opioid tolerance or withdrawal, urinary incontinence or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described.
    Type: Grant
    Filed: September 16, 1998
    Date of Patent: September 26, 2000
    Assignees: Warner-Lambert Company, Cocensys, Incorporated
    Inventors: Christopher F. Bigge, Po-Wai Yuen, Sui Xiong Cai, Eckard Weber, Richard Woodward, Nancy C. Lan, Zhang-Lin Zhou, John F. W. Keana, Anthony P. Guzikowski
  • Patent number: 6107508
    Abstract: The present invention relates to processes for the production of .alpha.-aryl-.beta.-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) receptor antagonists.
    Type: Grant
    Filed: March 31, 1999
    Date of Patent: August 22, 2000
    Assignee: Dupont Pharmaceuticals Company
    Inventors: Jiacheng Zhou, Lynette May Oh, Philip Ma
  • Patent number: 6008220
    Abstract: Aromatic keto-acid compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, arthrities, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes.
    Type: Grant
    Filed: June 8, 1998
    Date of Patent: December 28, 1999
    Assignee: Warner Lambert Company
    Inventors: Donald Hupe, Linda Lea Johnson, Daniel Fred Ortwine, Claude Forsey Purchase, Jr., Andrew David White, Qi-Zhuang Ye
  • Patent number: 6008358
    Abstract: Disclosed is a process for economic, safe and simple production of a 2-phenyl-2-(2'-piperidinylidene)acetate derivative at a reduced number of steps in a high yield, which comprises allowing 2,3,4,5-Tetrahydro-6-methoxypyridine and a benzyl cyanide derivative represented by the following general formula (2): wherein R.sup.1 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a halogen atom or an amino group, to undergo condensation reaction in the presence of an organic base such as 1,8-diazabicyclo[5.4.0]-7-undecene or a transition metal complex as a catalyst to produce a 2-phenyl-2-(2'-piperidinylidene)acetonitrile derivative represented by the following general formula (4): ##STR1## wherein R.sup.1 is as defined above; and the wavy line indicates a geometrical isomer, and then reacting with an alcohol in the presence of hydrogen chloride.
    Type: Grant
    Filed: April 29, 1998
    Date of Patent: December 28, 1999
    Assignee: Takasago International Corporation
    Inventors: Takenobu Nishikawa, Nobuo Seido
  • Patent number: 6002009
    Abstract: Pharmacologically active novel esters and amides of di-substituted 1,4 piperidine as 5-HT.sub.4 antagonists of formula (I) ##STR1## wherein A, X, Y and R have the meanings specified in the description, and a process for their preparation, are disclosed.
    Type: Grant
    Filed: January 14, 1998
    Date of Patent: December 14, 1999
    Assignee: Boehringer Ingelheim Italia, S.p.A.
    Inventors: Enzo Cereda, Maura Bignotti, Vincenzo Martino, Giovanni Battista Schiavi, Angelo Sagrada
  • Patent number: 5977141
    Abstract: Sulfonamide compounds are described which are inhibitors of matrix metalloproteinases, particularly stromelysin-1 and gelatinase A (72 kD gelatinase). Also described are methods for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes using the compounds.
    Type: Grant
    Filed: May 13, 1998
    Date of Patent: November 2, 1999
    Assignee: Warner-Lambert Company
    Inventors: Daniel F. Ortwine, Claude F. Purchase, Jr., Andrew D. White
  • Patent number: 5932594
    Abstract: A compound of the formula: or a pharmaceutically acceptable salt thereof,wherein Y is a direct link, --(CH.sub.2 --, --(CH.sub.2).sub.2 --, --CH.sub.2 O-- or CH.sub.2 S--; R is --CN or --CONH.sub.2 ;and R.sup.1 is a group of the formula: ##STR1## where R.sup.2 and R.sup.3 are each independently H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, --(CH.sub.2).sub.n OH, halo, trifluoromethyl, cyano, --(CH.sub.2).sub.n NR.sup.4 R.sup.5, --CO(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.4 alkyl), --CH(OH) (C.sub.1 -C.sub.4 alkyl), --C(OH) (C.sub.1 -C.sub.4 alkyl).sub.2, --SO.sub.2 NH.sub.2, --(CH.sub.2).sub.n CONR.sup.4 R.sup.5 or --(CH.sub.2).sub.n COO(C.sub.1 -C.sub.4 alkyl; R.sub.4 and R.sup.5 are each independently H or C.sub.1 -C.sub.4 alkyl; n is 0, 1 or 2;and "Het" is pyridyl, pyrazinyl or thienyl.The compounds are muscarinic receptor antagonists usedful in the treatment of diseases associated with the altered motility and/or tone of smooth muscle, especially irritable bowel syndrome.
    Type: Grant
    Filed: April 24, 1995
    Date of Patent: August 3, 1999
    Assignee: Pfizer, Inc.
    Inventors: Peter Edward Cross, Alexander Roderick MacKenzie
  • Patent number: 5922763
    Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.
    Type: Grant
    Filed: November 26, 1997
    Date of Patent: July 13, 1999
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Gunter Linz, Thomas Muller, Wolfgang Eisert, Johannes Weisenberger
  • Patent number: 5792769
    Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 --R.sup.4, R.sup.7 --R.sup.8, R.sup.a, R.sup.b, R.sup.c, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.
    Type: Grant
    Filed: August 15, 1996
    Date of Patent: August 11, 1998
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Tianbao Lu, Carl R. Illig, Bruce E. Tomczuk, Richard M. Soll, Nalin L. Subasinghe, Roger F. Bone
  • Patent number: 5777123
    Abstract: The invention provides a process for regioselective substitution of trifluorobenzoate/trifluorobenzonitrile to afford the difluorobenzoate/difluorobenzonitrile in good yields. The resulting difluorobenzoate/difluorobenzonitrile can again be regioselectively substituted with a second nucleophile to give monofluorobenzoate/monofluorobenzonitrile also in good yields. This process is particularly useful for forming key intermediates in the synthesis of oxytocin antagonist compounds.
    Type: Grant
    Filed: February 27, 1997
    Date of Patent: July 7, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Joseph E. Lynch, Yao-Jun Shi, Kenneth M. Wells
  • Patent number: 5767151
    Abstract: The present invention relates to novel 3,3-(disubstituted)-cyclohexan-1-ylidene acetate dimers of Formula (I): ##STR1## and related compounds, pharmaceutical compositions containing these compounds, and their use in treating allergic and inflammateory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).
    Type: Grant
    Filed: June 23, 1997
    Date of Patent: June 16, 1998
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Joseph M. Karpinski
  • Patent number: 5763638
    Abstract: A process for the preparation of nitriles of formula ##STR1## wherein X is CH or N, and R.sub.1 and R.sub.2 are each independently of the other hydrogen, chloro, bromo, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylamino, CN, phenyl, phenoxy, dimethylamino, piperidyl, morpholinyl or pyrrolidyl, or R.sub.1 and R.sub.2 together form a fused benzene ring, by reacting an aldehyde of formula ##STR2## with hydroxylaminosulfate in the presence of a tertiary amine base of formula ##STR3## wherein R.sub.3 and R.sub.4 are each independently of the other hydrogen, methyl or ethyl, R.sub.5 is branched C.sub.3 -C.sub.5 alkyl or phenyl, and R.sub.6 and R.sub.7 are methyl or ethyl,in the temperature range from 100.degree. to 160.degree. C., while distilling the released water of reaction off concomittantly at a pressure in the range of 0.02 to 1.5 bar, with subsequent removal of the ammonium salts, and isolating the nitrile so obtained by customary methods.
    Type: Grant
    Filed: February 4, 1997
    Date of Patent: June 9, 1998
    Assignee: Ciba Specialty Chemicals Corporation
    Inventor: Richard Breitschuh
  • Patent number: 5736559
    Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.
    Type: Grant
    Filed: August 1, 1996
    Date of Patent: April 7, 1998
    Assignee: Karl Thomae GmbH
    Inventors: Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Gunter Linz, Thomas Muller, Wolfgang Eisert, Johannes Weisenberger
  • Patent number: 5733756
    Abstract: Novel lactams and processes for the preparation of chiral compounds having utility as intermediates in the synthesis of compounds with Central Nervous System stimulant activity.
    Type: Grant
    Filed: January 5, 1996
    Date of Patent: March 31, 1998
    Assignee: Celgene Corporation
    Inventors: Andrew L. Zeitlin, David I. Stirling
  • Patent number: 5663352
    Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts and prodrugs thereof, wherein X represents a propylene or propenylene chain optionally substituted by one or more of R.sup.4, R.sup.5, R.sup.6 and R.sup.7 ; m is 2, 3 or 4; n is 0, 1 or 2 when m is 2 or 3, and n is 0 or 1 when m is 4; R.sup.1 represents optionally substituted phenyl; R.sup.2 represents optionally substituted phenyl, heteroaryl, benzhydryl or benzyl; R.sup.3 represents H, COR.sup.9, CO.sub.2 R.sup.10, COCONR.sup.10 R.sup.11, COCO.sub.2 R.sup.10, SO.sub.2 R.sup.15, CONR.sup.10 SO.sub.2 R.sup.15, C.sub.1-6 alkyl optionally substituted by a group selected from (CO.sub.2 R.sup.10, CONR.sup.10 R.sup.11, hydroxy, cyano, COR.sup.9, NR.sup.10 R.sup.11, C(NOH)NR.sup.10 R.sup.11, CONHphenyl(C.sub.1-4 alkyl), COCO.sub.2 R.sup.10, COCONR.sup.10 R.sup.11, SO.sub.2 R.sup.15, CONR.sup.10 SO.sub.2 R.sup.15 and optionally substituted phenyl), Y--R.sup.8 or CO--Z--(CH.sub.2).sub.q --R.sup.12 ; R.sup.4 and R.sup.
    Type: Grant
    Filed: January 19, 1996
    Date of Patent: September 2, 1997
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Angus Murray MacLeod, Kevin John Merchant, Graeme Irvine Stevenson
  • Patent number: 5646149
    Abstract: Compounds having both calcium antagonist and antioxidant activity are disclosed. The compounds are useful in preventing or alleviating damage to tissues at the cellular level. Methods of treatment which employ these properties of the compounds and corresponding pharmaceutical compositions are also disclosed.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 8, 1997
    Assignee: Alcon Laboratories, Inc.
    Inventors: Mark R. Hellberg, George Barnes, Robert J. Collier, Jr.
  • Patent number: 5646144
    Abstract: 1-Acylpiperidine compound of the formula I ##STR1## in which R.sub.1 is an optionally substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl, heteroarylalkanoyl, aralkoxycarbonyl or arylcarbamoyl radical or the acyl radical of an .alpha.-amino acid which is optionally N-substituted by lower alkanoyl or carbamoyl-lower-alkanoyl, R.sub.2 is cycloalkyl or an optionally substituted aryl or heteroaryl radical, R.sub.3 is hydrogen, alkyl, carbamoyl or an alkanoyl or alkenoyl radical which is optionally substituted by carboxyl or esterified or amidated carboxyl, R.sub.4 is an optionally substituted aryl or optionally partially hydrogenated heteroaryl radical, X.sub.1 is methylene, ethylene, a direct linkage, an optionally ketalized carbonyl group or an optionally etherified hydroxymethylene group, X.sub.2 is alkylene, carbonyl or a direct linkage, and X.sub.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 8, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Walter Schilling, Silvio Ofner, Siem J. Veenstra
  • Patent number: 5597825
    Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.
    Type: Grant
    Filed: May 16, 1994
    Date of Patent: January 28, 1997
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Frank Himmelsbach, Helmut Pieper, Volkhard Austel, G unter Linz, Thomas M uller, Wolfgang Eisert, Johannes Weisenberger
  • Patent number: 5563168
    Abstract: O-Benzyloxime ethers of the formula I ##STR1## where 5 X is substituted or unsubstituted CH.sub.2, NOalkylY isO, S, NR.sup.5R.sup.1, R.sup.2, R.sup.5 are H, alkylZ.sup.1, Z.sup.2 are H, halogen, methyl, methoxy, cyanoR.sup.3, R.sup.4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl,N(R.sup.6).sub.2, where R.sup.6 is H, alkyl, substituted or unsubstituted phenyl,--CO--N(R.sup.7).sub.2, where R.sup.
    Type: Grant
    Filed: June 16, 1995
    Date of Patent: October 8, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
  • Patent number: 5506227
    Abstract: Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.
    Type: Grant
    Filed: April 13, 1992
    Date of Patent: April 9, 1996
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Robert Zamboni, Daniel Guay, Jacques-Yves Gauthier
  • Patent number: 5466813
    Abstract: Imine dyes useful in photographic materials have the formula ##STR1## wherein R.sup.1, E.sup.1, E.sup.2, L.sup.1, L.sup.2, L.sup.3,D and m are defined as in the specification.Solid particle dispersions of dyes of formula (I) that contain at least one base-ionizable functional group such as carboxy, sulfonamido, or sulfamoyl are useful as filter dyes in photographic elements.
    Type: Grant
    Filed: July 20, 1993
    Date of Patent: November 14, 1995
    Assignee: Eastman Kodak Company
    Inventors: Donald R. Diehl, Margaret J. Helber, Hugh Williamson
  • Patent number: 5462947
    Abstract: A compound of Formula I ##STR1## or a pharmaceutically acceptable salt thereof wherein n is 1 or 2; R.sup.1 and R.sup.2 are independently H (provided only one is H at the same time), --OH, CN, CH.sub.2 CN, 2-- or 4--CF.sub.3, CH.sub.2 CF.sub.3, CH.sub.2 CHF.sub.2, CH.dbd.CF.sub.2, (CH.sub.2).sub.2 CF.sub.3, ethenyl, 2-propenyl, OSO.sub.2 CH.sub.3, OSO.sub.2 CF.sub.3, SSO.sub.2 CF.sub.3, COR, COOR, CON(R).sub.2, SO.sub.x CH.sub.3 (where, x is 0-2), SO.sub.x CF.sub.3, O(CH.sub.2).sub.x CF.sub.3, SO.sub.2 N(R).sub.2, CH.dbd.NOR, COCOOR, COCOON(R).sub.2, C.sub.1-8 alkyls, C.sub.3-8 cycloalkyls, CH.sub.2 OR, CH.sub.2 (R).sub.2, NRSO.sub.2 CF.sub.3, NO.sub.2, halogen, a phenyl at positions 2, 3 or 4, thienyl, furyl, pyrrole, oxazole, thiazole, N-pyrroline, triazole, tetrazole or pyridine; R.sup.3 is hydrogen, CF.sub.3, CH.sub.2 CF.sub.3, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.4 -C.sub.9 cycloalkyl-methyl, C.sub. 2 -C.sub.8 alkenyl, C.sub.2 -C.sub.
    Type: Grant
    Filed: October 12, 1993
    Date of Patent: October 31, 1995
    Assignee: The Upjohn Company
    Inventors: Kjell A. I. Svensson, Hakan V. Wikstrom, Per A. E. Carlsson, Anna M. P. Boije, R. Nicholas Waters, Clas A. Sonesson, Nils P. Stjernlof, Bengt R. Andersson, Lars O. Hansson
  • Patent number: 5432284
    Abstract: The present invention relates to a novel process for the preparation of heterocyclic alkylamide derivatives having the following formula: ##STR1## and the pharmaceutically acceptable acid addition salt thereof wherein X represents halo, alkyl having 1 to 6 carbon atoms, hydrido, trifluoromethyl, phenyl, or lower alkoxy having 1 to 6 carbon atoms; Y represents the group --CN or --CONH.sub.2 ; R.sub.2 represents alkyl having 1 to 6 carbon atoms; R.sub.
    Type: Grant
    Filed: September 8, 1993
    Date of Patent: July 11, 1995
    Assignee: G. D. Searle & Co.
    Inventors: John H. Dygos, Thomas R. Kowar, Kathleen T. McLaughlin, Gatis Plume, Michael L. Prunier, Richard J. Salzmann, Mike G. Scaros, Joseph J. Wieczorek
  • Patent number: 5401869
    Abstract: Aminomethylene compounds of the formula ##STR1## may advantageously be prepared by reacting C--H-acidic compounds of the formula ##STR2## with formamide acetals of the formula ##STR3## in which the radicals R.sup.1 to R.sup.6 have the meaning given in the description,if the process is carried out in the presence of a secondary amine of the formula ##STR4## in which R.sup.7 and R.sup.8 have the meaning given in the description.
    Type: Grant
    Filed: January 21, 1994
    Date of Patent: March 28, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Helmut Kraus, Nikolaus Muller, Gerhard Marzolph, Bernhard Beitzke
  • Patent number: 5364864
    Abstract: 1,4-disubstituted piperidines of formula 1: ##STR1## as well as the therapeutically acceptable salts of these molecules. The invention also relates to the application in therapy of the compounds of the general formula 1.
    Type: Grant
    Filed: May 26, 1992
    Date of Patent: November 15, 1994
    Assignee: Pierre Fabre Medicament
    Inventors: Denis Bigg, Jean-Louis Vidaluc, Francis Calmel