Cyano Attached Indirectly To The Piperidine Ring By Nonionic Bonding Patents (Class 546/230)
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Publication number: 20030203898Abstract: 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: ApplicationFiled: March 11, 2003Publication date: October 30, 2003Inventors: Helmut Haning, Gunter Schmidt, Josef Pernerstorfer, Hilmar Bischoff, Carsten Schmeck, Verena Vohringen, Michael Woltering, Axel Kretschmer, Christiane Faeste
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Publication number: 20030203935Abstract: Intermediates represented by the following formula: 1Type: ApplicationFiled: March 24, 2003Publication date: October 30, 2003Applicant: TEIJIN LIMITEDInventors: Tomohisa Nakada, Takayuki Hara, Yasunobu Takano
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Publication number: 20030203919Abstract: Dipeptide nitrile Cathepsin K inhibitors of formula I, and pharmaceutically acceptable salts or esters thereof 1Type: ApplicationFiled: April 9, 2003Publication date: October 30, 2003Inventor: Martin Missbach
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Patent number: 6605623Abstract: 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: GrantFiled: June 21, 2000Date of Patent: August 12, 2003Assignee: Bristol-Myers Squibb Pharma Co.Inventors: Soo S. Ko, George V. DeLucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
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Publication number: 20030144322Abstract: The invention provides a compound of formula (I): 1Type: ApplicationFiled: October 23, 2002Publication date: July 31, 2003Inventors: Alan P. Kozikowski, Gian Luca Araldi
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Patent number: 6562965Abstract: 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: GrantFiled: July 6, 2000Date of Patent: May 13, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Jiacheng Zhou, Lynette May Oh, Philip Ma
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Publication number: 20030078428Abstract: 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: ApplicationFiled: June 4, 2002Publication date: April 24, 2003Inventors: Stephen Douglas Barrett, Alexander James Bridges, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Haile Tecle
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Patent number: 6552022Abstract: 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: GrantFiled: May 15, 2001Date of Patent: April 22, 2003Assignee: SmithKline Beecham CorporationInventor: Alain Claude-Marie Daugan
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Patent number: 6538137Abstract: 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: GrantFiled: November 7, 2001Date of Patent: March 25, 2003Assignee: Teijin LimitedInventors: Tomohisa Nakada, Takayuki Hara, Yasunobu Takano
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Publication number: 20020198214Abstract: The invention is directed to inhibition of p38-&agr; kinase using compounds of the formula 1Type: ApplicationFiled: November 20, 2001Publication date: December 26, 2002Inventors: Babu Mavunkel, Sundeep Dugar, Gregory Luedtke, Xuefei Tan, Glenn McEnroe
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Patent number: 6486180Abstract: 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: GrantFiled: December 17, 1999Date of Patent: November 26, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Soo S. Ko, Cheryl McArdle Clark, George V. DeLucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
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Publication number: 20020151566Abstract: PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs.Type: ApplicationFiled: January 22, 2002Publication date: October 17, 2002Applicant: 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
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Patent number: 6458812Abstract: 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: GrantFiled: December 17, 2001Date of Patent: October 1, 2002Assignee: Schering CorporationInventors: Brian A. McKittrick, Guihua Guo, Zhaoning Zhu, Yuanzan Ye
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Patent number: 6441001Abstract: 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: GrantFiled: December 17, 1999Date of Patent: August 27, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Paul S. Watson, Soo S. Ko, George V. Delucca, Joseph B. Santella, III, Dean A. Wacker, John V. Duncia
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Publication number: 20020099214Abstract: There is provided a compound of formula I, 1Type: ApplicationFiled: March 27, 2002Publication date: July 25, 2002Applicant: Pfizer Inc.Inventors: Stephen Paul Gibson, Ivan Tommasini, David Morris Gethin, Richard Edward Armer
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Patent number: 6365626Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.Type: GrantFiled: December 7, 2000Date of Patent: April 2, 2002Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Yaguo Zheng, Sutapa Ghosh
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Patent number: 6358979Abstract: 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: GrantFiled: June 8, 2000Date of Patent: March 19, 2002Assignee: 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
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Patent number: 6313097Abstract: 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: GrantFiled: March 10, 2000Date of Patent: November 6, 2001Assignee: Boehringer Ingelheim Pharma KGInventors: Wolfgang Eberlein, Klaus Rudolf, Wolfhard Engel, Henri Doods, Gerhard Hallermayer
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Patent number: 6303652Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.Type: GrantFiled: March 19, 1999Date of Patent: October 16, 2001Assignee: Hughes InstituteInventors: Fatih M. Uckun, Yaguo Zheng, Sutapa Ghosh
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Patent number: 6303637Abstract: 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: GrantFiled: October 21, 1999Date of Patent: October 16, 2001Assignee: 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
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Patent number: 6294575Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.Type: GrantFiled: October 16, 2000Date of Patent: September 25, 2001Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Yaguo Zheng, Sutapa Ghosh
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Patent number: 6231786Abstract: 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: GrantFiled: January 18, 2000Date of Patent: May 15, 2001Assignee: Clariant GmbHInventors: Rainer Wingen, Barbara Hornung, Ayako Ogawa, Wolfgang Schmidt
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Patent number: 6221898Abstract: 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: GrantFiled: August 29, 1997Date of Patent: April 24, 2001Assignee: Astra AktiebolagInventor: Thomas Antonsson
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Patent number: 6160010Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.Type: GrantFiled: July 22, 1999Date of Patent: December 12, 2000Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Yaguo Zheng, Sutapa Ghosh
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Patent number: 6143896Abstract: 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: GrantFiled: December 16, 1998Date of Patent: November 7, 2000Assignee: Aventis Pharma Deutschland GmbHInventors: Gerhard Korb, Hans-Wolfram Flemming, Rudolf Lehnert
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Patent number: 6124323Abstract: 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: GrantFiled: September 16, 1998Date of Patent: September 26, 2000Assignees: Warner-Lambert Company, Cocensys, IncorporatedInventors: 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
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Patent number: 6107508Abstract: 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: GrantFiled: March 31, 1999Date of Patent: August 22, 2000Assignee: Dupont Pharmaceuticals CompanyInventors: Jiacheng Zhou, Lynette May Oh, Philip Ma
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Patent number: 6008220Abstract: 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: GrantFiled: June 8, 1998Date of Patent: December 28, 1999Assignee: Warner Lambert CompanyInventors: Donald Hupe, Linda Lea Johnson, Daniel Fred Ortwine, Claude Forsey Purchase, Jr., Andrew David White, Qi-Zhuang Ye
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Patent number: 6008358Abstract: 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: GrantFiled: April 29, 1998Date of Patent: December 28, 1999Assignee: Takasago International CorporationInventors: Takenobu Nishikawa, Nobuo Seido
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Patent number: 6002009Abstract: 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: GrantFiled: January 14, 1998Date of Patent: December 14, 1999Assignee: Boehringer Ingelheim Italia, S.p.A.Inventors: Enzo Cereda, Maura Bignotti, Vincenzo Martino, Giovanni Battista Schiavi, Angelo Sagrada
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Patent number: 5977141Abstract: 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: GrantFiled: May 13, 1998Date of Patent: November 2, 1999Assignee: Warner-Lambert CompanyInventors: Daniel F. Ortwine, Claude F. Purchase, Jr., Andrew D. White
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Patent number: 5932594Abstract: 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: GrantFiled: April 24, 1995Date of Patent: August 3, 1999Assignee: Pfizer, Inc.Inventors: Peter Edward Cross, Alexander Roderick MacKenzie
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Patent number: 5922763Abstract: 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: GrantFiled: November 26, 1997Date of Patent: July 13, 1999Assignee: Dr. Karl Thomae GmbHInventors: Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Gunter Linz, Thomas Muller, Wolfgang Eisert, Johannes Weisenberger
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Patent number: 5792769Abstract: 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: GrantFiled: August 15, 1996Date of Patent: August 11, 1998Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Carl R. Illig, Bruce E. Tomczuk, Richard M. Soll, Nalin L. Subasinghe, Roger F. Bone
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Patent number: 5777123Abstract: 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: GrantFiled: February 27, 1997Date of Patent: July 7, 1998Assignee: Merck & Co., Inc.Inventors: Joseph E. Lynch, Yao-Jun Shi, Kenneth M. Wells
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Patent number: 5767151Abstract: 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: GrantFiled: June 23, 1997Date of Patent: June 16, 1998Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Joseph M. Karpinski
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Patent number: 5763638Abstract: 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: GrantFiled: February 4, 1997Date of Patent: June 9, 1998Assignee: Ciba Specialty Chemicals CorporationInventor: Richard Breitschuh
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Patent number: 5736559Abstract: 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: GrantFiled: August 1, 1996Date of Patent: April 7, 1998Assignee: Karl Thomae GmbHInventors: Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Gunter Linz, Thomas Muller, Wolfgang Eisert, Johannes Weisenberger
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Patent number: 5733756Abstract: 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: GrantFiled: January 5, 1996Date of Patent: March 31, 1998Assignee: Celgene CorporationInventors: Andrew L. Zeitlin, David I. Stirling
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Patent number: 5663352Abstract: 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: GrantFiled: January 19, 1996Date of Patent: September 2, 1997Assignee: Merck Sharp & Dohme LimitedInventors: Angus Murray MacLeod, Kevin John Merchant, Graeme Irvine Stevenson
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Patent number: 5646149Abstract: 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: GrantFiled: June 7, 1995Date of Patent: July 8, 1997Assignee: Alcon Laboratories, Inc.Inventors: Mark R. Hellberg, George Barnes, Robert J. Collier, Jr.
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Patent number: 5646144Abstract: 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: GrantFiled: June 7, 1995Date of Patent: July 8, 1997Assignee: Ciba-Geigy CorporationInventors: Walter Schilling, Silvio Ofner, Siem J. Veenstra
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Patent number: 5597825Abstract: 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: GrantFiled: May 16, 1994Date of Patent: January 28, 1997Assignee: Dr. Karl Thomae GmbHInventors: Frank Himmelsbach, Helmut Pieper, Volkhard Austel, G unter Linz, Thomas M uller, Wolfgang Eisert, Johannes Weisenberger
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Patent number: 5563168Abstract: 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: GrantFiled: June 16, 1995Date of Patent: October 8, 1996Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
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Patent number: 5506227Abstract: 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: GrantFiled: April 13, 1992Date of Patent: April 9, 1996Assignee: Merck Frosst Canada, Inc.Inventors: Robert Zamboni, Daniel Guay, Jacques-Yves Gauthier
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Patent number: 5466813Abstract: 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: GrantFiled: July 20, 1993Date of Patent: November 14, 1995Assignee: Eastman Kodak CompanyInventors: Donald R. Diehl, Margaret J. Helber, Hugh Williamson
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Patent number: 5462947Abstract: 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: GrantFiled: October 12, 1993Date of Patent: October 31, 1995Assignee: The Upjohn CompanyInventors: 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
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Patent number: 5432284Abstract: 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: GrantFiled: September 8, 1993Date of Patent: July 11, 1995Assignee: 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
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Patent number: 5401869Abstract: 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: GrantFiled: January 21, 1994Date of Patent: March 28, 1995Assignee: Bayer AktiengesellschaftInventors: Helmut Kraus, Nikolaus Muller, Gerhard Marzolph, Bernhard Beitzke
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Patent number: 5364864Abstract: 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: GrantFiled: May 26, 1992Date of Patent: November 15, 1994Assignee: Pierre Fabre MedicamentInventors: Denis Bigg, Jean-Louis Vidaluc, Francis Calmel