Cyano Or -c(=x)-, Wherein X Is Chalcogen, Attached Directly Or Indirectly To The Oxazole Ring By Nonionic Bonding Patents (Class 548/236)
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Patent number: 6096688Abstract: The novel compounds of formula I: wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and Ar have the meaning given in claim 1, and herbicidal compositions containing such compounds as active ingredients.Type: GrantFiled: December 22, 1997Date of Patent: August 1, 2000Assignee: American Cyanamid CompanyInventors: Trevor Newton, Isabel Waldeck
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Patent number: 6096747Type: GrantFiled: May 28, 1996Date of Patent: August 1, 2000Assignee: Celltech Therapeutics LimitedInventors: Nigel Robert Arnold Beeley, Thomas Andrew Millican
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Patent number: 6051588Abstract: A compound comprising a non-steroidal antiinflammatory agent to which is directly or indirectly linked an NO group, a pharmaceutical composition including the compounds and methods of treatment of pain and/or inflammation using the compounds and compositions are disclosed. Also disclosed is a composition comprising a non-steroidal antiinflammatory agent and a compound that donates, transfers or releases nitric oxide.Type: GrantFiled: April 19, 1995Date of Patent: April 18, 2000Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
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Patent number: 6043265Abstract: The compounds N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-bi phenyl]-2-yl]methyl]-N,3,3-trimethylbutanamide and N-(4,5-dimethyl-3-isoxazolyl)-2'-[(3,3-dimethyl-2-oxo-1-pyrrolidinyl)methy l]-4'-(2-oxazolyl)[1,1'-biphenyl]-2-sulfonamide, and salts thereof, useful as endothelin antagonists.Type: GrantFiled: January 27, 1998Date of Patent: March 28, 2000Assignee: Bristol-Myers Squibb Co.Inventors: Natesan Murugesan, Joel C. Barrish, Zhengxiang Gu, Richard A. Morrison
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Patent number: 6043282Abstract: Azinooxime ethers of the formula I ##STR1## (X=NOCH.sub.3, CHOCH.sub.3, CHCH.sub.3 ; Y=O, NZ, where Z=H, alkyl; R.sup.1 =H, alkyl; R.sup.2 =cyano, nitro, trifluoromethyl, halogen, alkyl, alkoxy; m=0, 1, 2, it being possible for the radicals R.sup.2 to be different if m=2; R.sup.3 =H, cyano, alkyl, haloalkyl, alkoxy, cycloalkyl; R.sup.4, R.sup.5, R.sup.6 =indepedently of one another H, unsubst. or subst. alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl), and their salts, processes and intermediates for their preparation and their use for controlling harmful fungi and animal pests.Type: GrantFiled: July 29, 1998Date of Patent: March 28, 2000Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Hubert Sauter, Klaus Oberdorf, Wassilios Grammenos, Thomas Grote, Reinhard Kirstgen, Bernd Muller, Ruth Muller, Franz Rohl, Eberhard Ammermann, Volker Harries, Gisela Lorenz, Siegfried Strathmann
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Patent number: 6025375Abstract: Heterocyclic compounds of the formula: ##STR1## whereinR.sup.1 is carboxy or protected carboxy,R.sup.2 is aryl which may have suitable substituent(s),R.sup.3 is aryl which may have suitable substituent(s),A.sup.1 is lower alkylene,A.sup.2 is bond or lower alkylene and-Q- is ##STR2## etc., and pharmaceutically acceptable salts thereof which are useful as a medicament.Type: GrantFiled: June 5, 1998Date of Patent: February 15, 2000Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Masanobu Nagano, Kouji Hattori, Kazunori Tsubaki, Osamu Okitsu, Seiichiro Tabuchi
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Patent number: 6008219Abstract: This invention relates to compounds of formula (I) ##STR1## which are useful as modulators of D.sub.3 receptors, in particular as antipsychotic agents.Type: GrantFiled: October 29, 1997Date of Patent: December 28, 1999Assignee: SmithKline Beech p.l.c.Inventors: Geoffrey Stemp, Christopher Norbert Johnson
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Patent number: 5994381Abstract: A heterocyclic aromatic oxazole compound of the formula (I) ##STR1## wherein Z is an oxygen atom; one of R and R.sub.1 is a group of the formula ##STR2## wherein R.sub.3 is lower alkyl, amino or lower alkylamino, and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are the same or different and each is hydrogen atom, halogen atom, lower alkyl, lower alkoxy, trifluoromethyl, hydroxy or amino, provided that at least one of R.sub.4, R.sub.5, R.sub.6 and R.sub.7 is not hydrogen atom, and the other is an optionally substituted cycloalkyl, an optionally substituted heterocyclic group or an optionally substituted aryl; and R.sub.2 is a lower alkyl or a halogenated lower alkyl, and a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 19, 1996Date of Patent: November 30, 1999Assignee: Japan Tobacco, Inc.Inventors: Junichi Haruta, Hiromasa Hashimoto, Mutsuyoshi Matsushita
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Patent number: 5985911Abstract: C-terminal compounds of formula ##STR1## are potent inhibitors of matrix metalloproteinase and are useful in the treatment of diseases in which matrix metalloproteinase play a role. Also disclosed are matrix metalloproteinase inhibiting compositions and a method of inhibiting matrix metalloproteinase in a mammal.Type: GrantFiled: December 17, 1997Date of Patent: November 16, 1999Assignee: Abbott LaboratoriesInventors: Steven K. Davidsen, Alan S. Florjancic, George S. Sheppard, Jamie R. Giesler, Lianhong Xu, Yan Guo, Michael L. Curtin, Michael R. Michaelides, Carol K. Wada, James H. Holms
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Patent number: 5985919Abstract: (Het)aryloxy-, -thio- and -aminocrotonates of the formula I ##STR1## where the substituents have the following meanings: U is oxygen, sulfur or amino;V is oxygen, sulfur, amino or alkylamino;X, Y and Z independently of one another are .dbd.N-- or .dbd.CR.sup.3 --;R.sup.1 and R.sup.2 independently of one another are alkyl;R.sup.3 is hydrogen, cyano, nitro, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio and haloalkylthio; andR.sup.4 is an organic radical which is bonded to the skeleton directly or via an oxy, mercapto, amino, carboxyl or carbonylamino group,process for their preparation, and their use.Type: GrantFiled: October 30, 1997Date of Patent: November 16, 1999Assignee: BASF AktiengesellschaftInventors: Thomas Grote, Reinhard Kirstgen, Bernd Muller, Hubert Sauter, Albrecht Harreus, Hartmann Konig, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Franz Rohl
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Patent number: 5977149Abstract: Cyclic amides of Formula (I) which are useful as fungicides wherein: A is O; S; N; NR.sup.5 ;or CR.sup.14--, G is C or N; W is O or S; X is OR.sup.1, S(O).sub.m R.sup.1 or halogen; R.sup.1, R.sup.2, and R.sup.5 are independently, in part, C.sub.1 -C.sub.6 alkyl; Y is, in part, --O--; --S(O).sub.n --,--CHR.sup.6 O--; or --CHR.sup.6 O--N.dbd.C(R.sup.7)--; Z is, in part, optionally substituted cycloalkyl, phenyl, pyridinyl, pyrimidinyl, or naphthyl; and R.sup.3, R.sup.4, R.sup.6, R.sup.7, R.sup.14, m, and n are defined in the disclosure, are disclosed.Type: GrantFiled: January 14, 1998Date of Patent: November 2, 1999Assignee: E. I. du Pont de Nemours and CompanyInventors: Richard James Brown, King-Mo Sun, Deborah Ann Frasier
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Patent number: 5965740Abstract: A compound represented by the formula (I): ##STR1## wherein R.sup.1 is an optionally substituted heterocyclic group; R.sup.2 is optionally substituted aryl or heterocyclic group; R.sup.3 is hydrogen, alkyl, alkenyl, or alkynyl; R.sup.4 is hydrogen, alkyl, alkoxy, halogen, nitro, cyano, or halogenated alkyl; M is oxygen, S(O).sub.i wherein i is 0, 1, or 2, NR.sup.5 wherein R.sup.5 is hydrogen, alkyl, or acyl, --Q--N.dbd.C(R.sup.6)--, --B--C(R.sup.8).dbd.N--, --CH.dbd.N--N.dbd.C(R.sup.9)--, or --CH.dbd.N--A--(CR.sup.10 R.sup.11)m--; and n is 0, 1, or 2, an intermediate for producing the same and an agrochemical composition containing the same as an active ingredient.Type: GrantFiled: February 20, 1998Date of Patent: October 12, 1999Assignee: Shionogi & Co., Ltd.Inventors: Hiroyuki Kai, Akira Takase, Toshikazu Ohtsuka
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Patent number: 5965558Abstract: Y--X--C(R').dbd.C(R")COOR"'(A1)The present invention relates to novel protein tyrosine phosphatase modulating compounds having the general structure shown in Formula (A1), to methods for their preparation, to compositions comprising the compounds, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phosphotyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryoic cells, whole animals and human beings. R' and R" are independently selected from the group consisting of hydrogen, halo, cyano, nitro, trihalomethyl, alkyl, arylalkyl. R"' is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, arylalkyl. X is aryl. Y is selected from hydrogen or ##STR1## wherein (*) indicates a potential point of attachment to X.Type: GrantFiled: October 29, 1997Date of Patent: October 12, 1999Assignee: Ontogen CorporationInventors: Adnan Mjalli, Sepehr Sarshar, Xiaodong Cao, Farid Bakir
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Patent number: 5942535Abstract: The present invention relates to heterocyclic compounds of the formula ##STR1## in which R.sup.1 -R.sup.7, B, a and X have the meanings recited in the specification. These compounds are usable in the treatment of diseases of the rheumatoid group and for the prevention of allergically induced diseases.Type: GrantFiled: March 28, 1997Date of Patent: August 24, 1999Assignee: Merckle GmbHInventors: Stefan Laufer, Hans Gunther Striegel, Gerd Dannhardt
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Patent number: 5935973Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R.sub.1 is an optional substituent; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents CO.HET, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.Type: GrantFiled: January 5, 1998Date of Patent: August 10, 1999Assignee: Knoll AktiengesellschaftInventors: Alan Martin Birch, David John Heal, Frank Kerrigan, Keith Frank Martin, Patricia Lesley Needham, Bruce Jeremy Sargent
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Patent number: 5925631Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: August 3, 1998Date of Patent: July 20, 1999Assignee: Merck & Co., Inc.Inventors: Cameron Black, Greg Hughes, Erich Grimm, Serge Leger, Petpiboon Prasit, Zhaoyin Wang
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Patent number: 5922881Abstract: The invention relates to novel heterocyclic imino derivatives, several processes for their preparation and their use for controlling pests.Type: GrantFiled: November 27, 1996Date of Patent: July 13, 1999Assignee: Bayer AktiengesellschaftInventors: Lutz Assmann, Thomas Seitz, Ralf Tiemann, Heinz-Wilhelm Dehne, Klaus Stenzel
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Patent number: 5917048Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning described in the specification, have retinoid-like biological activity.Type: GrantFiled: March 19, 1997Date of Patent: June 29, 1999Assignee: Allergan Sales Inc.Inventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
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Patent number: 5910594Abstract: A process for the manufacture of a 5-cyano-4-lower alkyl-oxazole by the dehydration of a 5-carbamoyl-4-lower alkyl-oxazole is disclosed. The reaction is carried out by dehydrating the oxazole with silicon tetrachloride in the presence of an amine in an aprotic organic solvent. 5-Carbamoyl-4-methyl-oxazole may be dehydrated by the process in accordance with the invention to obtain 5-cyano-4-methyl-oxazole, which is a valuable intermediate in the synthesis of pyridoxine.Type: GrantFiled: January 20, 1998Date of Patent: June 8, 1999Assignee: Roche Vitamins Inc.Inventors: Klaus Behringer, Werner Bonrath, Horst Pauling
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Patent number: 5892052Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.Type: GrantFiled: April 6, 1995Date of Patent: April 6, 1999Assignee: Abbott LabortoriesInventors: Dale J. Kempf, Daniel W. Norbeck, Hing Leung Sham, Chen Zhao
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Patent number: 5889058Abstract: Methods of use for compounds of formula (I) are described wherein R represent a --CONHOH, carboxyl (--CO.sub.2 H) or esterified carboxyl group; R.sup.1 represents a hydrogen atom or an optionally substituted alkyl, alkenyl, aryl, aralkyl, heteroaralkyl or heteroarylthioalkyl group; R.sup.2 represents an optionally substituted phenylethyl, phenylpropyl or phenylbutyl group; R.sup.3 represents a hydrogen atom or an alkyl group; R.sup.4 represents a hydrogen atom or an alkyl group; R.sup.5 represents an optionally substituted alkyl or alkenyl group optionally interrupted by one or more --O-- or --S-- atoms or --N(R.sup.7)-- groups (where R.sup.7 is a hydrogen atom or a C.sub.1-6 alkyl group); X represents an amino (--NH.sub.2), or substituted amino, hydroxyl or substituted hydroxyl group; and the salts, solvates and hydrates thereof.Type: GrantFiled: November 3, 1994Date of Patent: March 30, 1999Assignee: Celltech LimitedInventors: John Robert Porter, Thomas Andrew Millican, John Richard Morphy, Nigel Robert Arnold Beeley
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Patent number: 5888941Abstract: Compounds of general formula I and their salts and solvates are antifungal agents and as such are useful in the treatment of various fungal infections. Pharmaceutical compositions including these compounds and processes for their preparation are also provided.Type: GrantFiled: March 31, 1997Date of Patent: March 30, 1999Assignee: J. Uriach & Cia. S.A.Inventors: Javier Bartroli, Enric Turmo, Manuel Anguita
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Patent number: 5856506Abstract: The present invention is directed to compounds having the formula: ##STR1## The invention further provides a method of making the compounds. The compounds are useful as inhibitors of protein phosphatases, for example PP1, PP2A, PP3, CDC25A and CDC25B. The invention is further directed to a method of inhibiting a protein phosphatase, a method of inhibiting cell proliferation, and pharmaceutical compositions comprising the subject compounds.Type: GrantFiled: August 22, 1997Date of Patent: January 5, 1999Assignee: University of PittsburghInventors: John S. Lazo, Robert L. Rice, April Cunningham, Peter Wipf
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Patent number: 5849911Abstract: There are described compounds of formula I*, ##STR1## wherein R.sub.1 is lower alkoxycarbonyl,R.sub.2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl,R.sub.3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C.sub.4 -C.sub.8 cycloalkyl,R.sub.4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, sulfinyl (--SO--) and sulfonyl (--SO.sub.2 --) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl,R.sub.5, independently of R.sub.2, has one of the meanings mentioned for R.sub.2, andR.sub.6, independently of R.sub.1, is lower alkoxycarbonyl,or salts thereof, provided that at least one salt-forming group is present.The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS.Type: GrantFiled: April 9, 1997Date of Patent: December 15, 1998Assignee: Novartis Finance CorporationInventors: Alexander Fassler, Guido Bold, Hans-Georg Capraro, Marc Lang, Satish Chandra Khanna
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Patent number: 5849921Abstract: Angiotensin-II antagonists of the formula ##STR1## wherein R.sub.1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R.sub.2 is, inter alia, optionally substituted benzimidazol-2-yl, 5,6,7,8-tetrahydro-imidazo?1,2-a!pyridin-2-yl, butanesultam-1-yl, imidazol-4-yl, and tetrahydobenzimidazol-2-yl; R.sub.3 is, inter alia, lower alkyl; and, R.sub.4 is an acidic group, such as carboxyl or tetrazolyl. An exemplary compound is: 4'-?(2-ethyl-4-methyl-6-(5,6,7,8-tetrahydroimidazo?1,2-a!pyridin-2-yl)-ben zimidazol-1-yl)-methyl!-biphenyl-2-carboxylic acid.Type: GrantFiled: June 2, 1995Date of Patent: December 15, 1998Assignee: Astra AktiebolagInventors: Robin Bernad Boar, Alan John Cross, Duncan Alastair Gray, Richard Alfred Green
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Patent number: 5846906Abstract: Herbicidally active phenyldiketone compounds of the formula I ##STR1## in which the substituents have the following meanings: L and M are hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, C.sub.1 -C.sub.4 -alkoxy, it being possible for these groups to be unsubstituted or substituted by one to five halogen atoms or C.sub.1 -C.sub.4 -alkoxy, or halogen, cyano, nitro, a group --(Y).sub.n --S(O).sub.m R.sup.7 or a group --(Y).sub.n --CO--R.sup.8,Z is a 5- or 6-membered heterocyclic saturated or unsaturated radical which has one to three hetero atoms selected from the group consisting of oxygen, sulfur or nitrogen and which is unsubstituted or substituted by halogen, cyano, nitro, a group --CO--R.sup.8, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkylthio, di-C.sub.1 -C.sub.Type: GrantFiled: July 30, 1997Date of Patent: December 8, 1998Assignee: BASF AktiengesellschaftInventors: Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Stefan Engel, Martina Otten, Marcus Vossen, Peter Plath, Harald Rang, Albrecht Harreus, Hartmann Konig, Helmut Walter, Karl-Otto Westphalen, Ulf Misslitz
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Patent number: 5846990Abstract: Compounds of the formula ##STR1## inhibit the activity of endothelin. The symbols are defined as follows: R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each directly bonded to a ring carbon and are each independently(a) hydrogen;(b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z.sup.1, Z.sup.2 and Z.sup.3 ;(c) halo;(d) hydroxyl;(e) cyano;(f) nitro;(g) --C(O)H or --C(O)R.sup.5 ;(h) --CO.sub.2 H or --CO.sub.2 R.sup.5 ;(i) --Z.sup.4 --NR.sup.6 R.sup.7 ;(j) --Z.sup.4 --N(R.sup.10)--Z.sup.5 --NR.sup.8 R.sup.9 ; or(k) R.sup.3 and R.sup.4 together may also be alkylene or alkenylene, either of which may be substituted with Z.sup.1, Z.sup.2 and Z.sup.3, completing a 4- to 8-membered saturated, unsaturated or aromatic ring together with the carbon atoms to which they are attached;and the remaining symbols are as defined in the specification.Type: GrantFiled: February 13, 1997Date of Patent: December 8, 1998Assignee: Bristol-Myers Squibb Co.Inventors: Natesan Murugesan, Joel C. Barrish, Steven H. Spergel
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Patent number: 5846907Abstract: Pyrazol-4-ylbenzoyl compounds of the formula I ##STR1## where Z is a 5- or 6-membered heterocyclic saturated or unsaturated radical, Q is a pyrazole ring and L and M are as defined in the specification, their use as herbicidal compounds and to processes for preparing the compounds.Type: GrantFiled: July 30, 1997Date of Patent: December 8, 1998Assignee: BASF AktiengesellschaftInventors: Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Stefan Engel, Martina Otten, Marcus Vossen, Peter Plath, Harald Rang, Albrecht Harreus, Hartmann Konig, Helmut Walter, Karl-Otto Westphalen, Ulf Misslizt
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Patent number: 5837702Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is alkyl, Y is a single bond, --CH.sub.2 --, --C(O)--, --O--, --S-- or --N(R.sup.8)-- where R.sup.8 is hydrogen, alkyl, haloalkyl, aryl, arylalkyl, cycloalkyl or (cycloalkyl)alkyl, and R.sup.1 to R.sup.7 are as defined herein. These compounds have potassium channel activating activity and are useful, therefore for example, as cardiovascular agents.Type: GrantFiled: August 30, 1994Date of Patent: November 17, 1998Assignee: Bristol-Myers Squibb Co.Inventors: George C. Rovnyak, Karnail S. Atwal, Dinos P. Santafianos, Charles Z. Ding
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Patent number: 5834468Abstract: This invention relates to substituted and unsubstituted ???(aryl- and heteroaryl-) alkyl-, alkyloxy-, alkylthio-, oxo-, thio-, and alkylamino!- heteroaryl and aryl!- alkylamino-, aminoalkyl-, alkyloxy-, and alkylthio!- aryl and heteroaryl compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are useful as antagonists of the pain enhancing effects of E-type prostaglandins, to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods for treating pain comprising the administration of such compounds.Type: GrantFiled: July 2, 1996Date of Patent: November 10, 1998Assignee: Zeneca LimitedInventors: Gloria Anne Breault, John Oldfield, Howard Tucker, Peter Warner
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Patent number: 5827860Abstract: Compounds of the Formula I: ##STR1## useful in the treatment of thrombin and trypsin related disorders.Type: GrantFiled: June 7, 1995Date of Patent: October 27, 1998Assignee: Ortho Pharmaceutical CorporationInventors: Michael J. Costanzo, Bruce E. Maryanoff
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Patent number: 5827868Abstract: Thromboxane receptor antagonist activity is exhibited by compounds of the formula ##STR1## wherein: V is --(CH.sub.2).sub.m --, --O--, or ##STR2## but if V is --O--or ##STR3## R.sup.3 and R.sup.4 must complete an aromatic ring; W is --(CH.sub.2).sub.2 --, --CH.dbd.CH-- or phenylene;X is a single bond, --CH.dbd.CH--, --(CH.sub.2).sub.n --, or --O--(CH.sub.2).sub.n --; or X is branched alkylene or --O--branched alkylene wherein W is linked to Y through a chain n carbon atoms long;Y is --CO.sub.2 H, --CO.sub.2 alkyl, --CO.sub.2 alkali metal, --CH.sub.2 OH, --CONHSO.sub.2 R.sup.5, --CONHR.sup.6, or --CH.sub.2 -5-tetrazolyl;Z is O or NH;R.sup.3 and R.sup.4 are each independently hydrogen or alkyl or R.sup.3 and R.sup.4 together complete a ring optionally substituted through a ring carbon with a halo, lower alkyl, phenyl, halo (lower alkyl), halophenyl, oxo or hydroxyl group; and the remaining symbols are as defined in the specification.Type: GrantFiled: October 7, 1991Date of Patent: October 27, 1998Assignee: E. R. Squibb & Sons, Inc.Inventors: Raj N. Misra, Jagabandhu Das, Steven E. Hall, Wen-Ching Han, Philip M. Sher, Philip D. Stein
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Patent number: 5827866Abstract: Compounds of the Formula I: ##STR1## useful in the treatment of thrombin and trypsin related disorders.Type: GrantFiled: June 7, 1995Date of Patent: October 27, 1998Assignee: Ortho Pharmaceutical CorporationInventors: Michael J. Costanzo, Bruce E. Maryanoff
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Patent number: 5817827Abstract: The present invention relates to a process for the dehydration of amides to nitrites which comprises carrying out the dehydration in the presence of an adduct of sulphur trioxide and an amine as the dehydrating reagent in a basic reaction mixture. Thereby, for example, aliphatic, aromatic and heteroaromatic amides are dehydrated to the corresponding nitrites, such as 5-carbamoyl-4-methyl-oxazole to 5-cyano-4-methyl-oxazole, a valuable intermediate in the synthesis of pyridoxine.Type: GrantFiled: October 22, 1996Date of Patent: October 6, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Werner Bonrath, Horst Pauling
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Patent number: 5807876Abstract: The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as agents for immunosuppression. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.Type: GrantFiled: April 23, 1996Date of Patent: September 15, 1998Assignee: Vertex Pharmaceuticals IncorporatedInventors: David M. Armistead, Michael C. Badia, Guy W. Bemis, Randy S. Bethiel, Catharine A. Frank, Perry M. Novak, Steven M. Ronkin, Jeffrey O. Saunders
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Patent number: 5808101Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification, are capable of lowering intraocular pressure in the eye of a mammal.Type: GrantFiled: November 21, 1997Date of Patent: September 15, 1998Assignee: AllerganInventors: Robert M. Burk, David F. Woodward
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Patent number: 5801246Abstract: The present invention discloses novel substituted aryl- and heteroarylphenyloxazolidinones which are useful as anti-bacterial agents. More specifically, the substituted aryl- and heteroarylphenyloxazolidinones of the invention are characterized by oxazolidinones having an aryl or heteroaryl group at the p-position of the 3-phenyl ring and additional substitutions at the m-position(s) of the 3-phenyl ring. A compound representative of this new class of oxazolidinones is (.+-.)-5-(acetamidomethyl)-3-?4-(3-pyridyl)-3,5-difluorophenyl!-2-oxazolid inone.Type: GrantFiled: June 6, 1995Date of Patent: September 1, 1998Assignee: Pharmacia & Upjohn CompanyInventors: Michael R. Barbachyn, Steven J. Brickner
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Patent number: 5780647Abstract: Compounds of Formula 1 ##STR1## wherein Z is selected from the group consisting of the radicals shown in Formula 2 and in Formula 3, ##STR2## Y is cycloalkyl or cycloalkenyl of 3 to 8 carbons optionally substituted with one or two R.sub.4 groups, or Y is selected from phenyl, pyridyl, thienyl, furyl, pyrrolyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, and imidazolyl, said groups being optionally substituted with one or two R.sub.4 groups, the divalent Y radical being substituted by the Z and --CR.sub.1 .dbd.CR.sub.1 --CR.sub.1 .dbd.CR.sub.1 groups on adjacent carbons; X is S, O, or NR.sub.5 ; n is 1 or 2; R.sub.1 and R.sub.2 independently are H, lower alkyl or fluoroalkyl; R.sub.3 is hydrogen, lower alkyl, Cl or Br; R.sub.4 is lower alkyl, fluoroalkyl or halogen; R.sub.5 is H or lower alkyl, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.Type: GrantFiled: February 25, 1997Date of Patent: July 14, 1998Assignee: AllerganInventors: Vidyasagar Vuligonda, Roshantha A. Chandraratna
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Patent number: 5770615Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof. These compounds are beta three adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity and gastrointestinal diseases.Type: GrantFiled: March 28, 1997Date of Patent: June 23, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. W. Cheng, Gregory S. Bisacchi, Ashvinikumar V. Gavai, Kathleen M. Poss, Denis E. Ryono, Philip M. Sher, Chong-qing Sun, William N. Washburn
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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: 5750543Abstract: A compound having the structure: ##STR1## wherein (a) n is from 1 to about 3;(b) X is selected from the group consisting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen;(e) W is O or S; and(f) Het is a heteroaryl group comprising one or more rings each ring containing from about 5 to about 6 atoms other than hydrogen and wherein the group contains at least one heteroatom selected from O, N, or S.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.Type: GrantFiled: February 1, 1996Date of Patent: May 12, 1998Assignee: The Procter & Gamble CompanyInventors: Laurence Ichih Wu, John Michael Janusz
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Patent number: 5750706Abstract: The compounds of formula I ##STR1## wherein R.sup.1 -R.sup.9, R.sup.15, A, X, Y, Z and n have the meaning given in the specification are active as protein kinase inhibitors and can be used as medicaments, particularly for the treatment of inflammatory skin disorders and alopecia.Type: GrantFiled: September 3, 1996Date of Patent: May 12, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Pierre Barbier, Isabelle Huber, Fernand Schneider, Josef Stadlwieser, Sven Taylor
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Patent number: 5733882Abstract: The present invention provides compounds, more particularly dipeptide analogs, which bind to retroviral proteases. These compounds are inhibitors of retroviral proteases and are useful for treating diseases related to infection by retroviruses.Type: GrantFiled: February 28, 1995Date of Patent: March 31, 1998Assignee: SmithKline Beecham CorporationInventors: Thomas Joseph Carr, Peter Lawrence DeMarsh, Geoffrey Bainbridge Dreyer, Ashley Edward Fenwick
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Patent number: 5733648Abstract: Organic compounds having at least one ethylenically-unsaturated group are described, the organic compounds being suitable for use in coatable compositions as reactive diluents; compounds of the invention preferably have a divalent organic linking moiety devoid of reactive groups other than optional ethylenically-unsaturated groups, and a polar organic moiety and are particularly adept in solubilizing aminoplast resins having radiation-curable pendant groups.Type: GrantFiled: February 23, 1996Date of Patent: March 31, 1998Assignee: Minnesota Mining and Manufacturing CompanyInventors: Ernest L. Thurber, Eric G. Larson, Alan R. Kirk, Gregg D. Dahlke
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Patent number: 5728720Abstract: Novel isoxazolidinedione derivatives of the formula (I) ##STR1## wherein R is an optionally substituted aromatic hydrocarbon, an optionally substituted alicyclic hydrocarbon, an optionally substituted heterocyclic group, an optionally substituted condensed heterocyclic group or a group of the formula ##STR2## R.sub.4 is a hydrogen atom, a lower alkyl or a hydroxy; R.sub.5 is a lower alkyl optionally substituted by hydroxy; and P and Q are each a hydrogen atom or P and Q together form a bond, and pharmaceutically acceptable salts thereof. Said novel isoxazolidinedione derivatives and pharmaceutically acceptable salts thereof have superior hypoglycemic and hypolipidemic actions and are useful for the treatment of diabetes and the complications thereof, as well as therapeutic agents for related diseases such as hyperlipidemia.Type: GrantFiled: August 25, 1995Date of Patent: March 17, 1998Assignee: Japan Tobacco Inc.Inventor: Hisashi Shinkai
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Patent number: 5718845Abstract: Nonlinear optical compounds which contain a heteroaromatic ring and may further comprise a tricyanovinyl group attached to the heteroaromatic ring.Type: GrantFiled: January 18, 1995Date of Patent: February 17, 1998Assignee: Enichem S.p.A.Inventors: Kevin J. Drost, Pushkara Rao Varanasi, Kwan-Yue Alex Jen, Michael Anthony Drzewinski
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Patent number: 5710288Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification, are capable of lowering intraocular pressure in the eye of a mammal.Type: GrantFiled: May 3, 1996Date of Patent: January 20, 1998Assignee: AllerganInventors: Robert M. Burk, David F. Woodward
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Patent number: 5709935Abstract: Organic compounds having at least one ethylenically-unsaturated group are described, the organic compounds being suitable for use in coatable compositions as reactive diluents; compounds of the invention preferably have a divalent organic linking moiety devoid of reactive groups other than optional ethylenically-unsaturated groups, and a polar organic moiety and are particularly adept in solubilizing aminoplast resins having radiation-curable pendant groups.Type: GrantFiled: February 23, 1996Date of Patent: January 20, 1998Assignee: Minnesota Mining and Manufacturing CompanyInventors: Ernest L. Thurber, Eric G. Larson, Alan R. Kirk, Gregg D. Dahlke
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Patent number: 5691374Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: May 18, 1995Date of Patent: November 25, 1997Assignee: Merck Frosst Canada Inc.Inventors: Cameron Black, Erich Grimm, Zhaoyin Wang, Serge Leger
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Patent number: 5686471Abstract: A compound having the structure: ##STR1## wherein (a) n is from about 1 to about 3;(b) X is selected from the group consisiting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl or aralkyl having from 1 to about 3 carbon atoms; or the Y's are bonded together to form an alkanyl ring having from 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen;(e) R.sub.1 and R.sub.2 are each independently hydrogen or straight, branched or cyclic alkyl, unsubstituted or substituted, carboxyl, carboxamido, alkoxycarbonyl or alkylcarbonyl; and(f) Het is a heteroaryl group comprising one or more rings containing from about 5 to about 8 atoms in the rings and wherein at least one ring has at least one heteroatom selected from O, N, or S,pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.Type: GrantFiled: February 1, 1996Date of Patent: November 11, 1997Assignee: The Procter & Gamble CompanyInventors: Zhuoliang Chen, John Michael Janusz