Cyano Or -c(=x)-, Wherein X Is Chalcogen, Attached Directly Or Indirectly To The Oxazole Ring By Nonionic Bonding Patents (Class 548/236)
  • Patent number: 6096688
    Abstract: 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: Grant
    Filed: December 22, 1997
    Date of Patent: August 1, 2000
    Assignee: American Cyanamid Company
    Inventors: Trevor Newton, Isabel Waldeck
  • Patent number: 6096747
    Type: Grant
    Filed: May 28, 1996
    Date of Patent: August 1, 2000
    Assignee: Celltech Therapeutics Limited
    Inventors: Nigel Robert Arnold Beeley, Thomas Andrew Millican
  • Patent number: 6051588
    Abstract: 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: Grant
    Filed: April 19, 1995
    Date of Patent: April 18, 2000
    Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
  • Patent number: 6043265
    Abstract: 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: Grant
    Filed: January 27, 1998
    Date of Patent: March 28, 2000
    Assignee: Bristol-Myers Squibb Co.
    Inventors: Natesan Murugesan, Joel C. Barrish, Zhengxiang Gu, Richard A. Morrison
  • Patent number: 6043282
    Abstract: 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: Grant
    Filed: July 29, 1998
    Date of Patent: March 28, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: 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
  • Patent number: 6025375
    Abstract: 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: Grant
    Filed: June 5, 1998
    Date of Patent: February 15, 2000
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Kiyoshi Taniguchi, Masanobu Nagano, Kouji Hattori, Kazunori Tsubaki, Osamu Okitsu, Seiichiro Tabuchi
  • Patent number: 6008219
    Abstract: 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: Grant
    Filed: October 29, 1997
    Date of Patent: December 28, 1999
    Assignee: SmithKline Beech p.l.c.
    Inventors: Geoffrey Stemp, Christopher Norbert Johnson
  • Patent number: 5994381
    Abstract: 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: Grant
    Filed: August 19, 1996
    Date of Patent: November 30, 1999
    Assignee: Japan Tobacco, Inc.
    Inventors: Junichi Haruta, Hiromasa Hashimoto, Mutsuyoshi Matsushita
  • Patent number: 5985911
    Abstract: 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: Grant
    Filed: December 17, 1997
    Date of Patent: November 16, 1999
    Assignee: Abbott Laboratories
    Inventors: 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
  • Patent number: 5985919
    Abstract: (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: Grant
    Filed: October 30, 1997
    Date of Patent: November 16, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Thomas Grote, Reinhard Kirstgen, Bernd Muller, Hubert Sauter, Albrecht Harreus, Hartmann Konig, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Franz Rohl
  • Patent number: 5977149
    Abstract: 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: Grant
    Filed: January 14, 1998
    Date of Patent: November 2, 1999
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Richard James Brown, King-Mo Sun, Deborah Ann Frasier
  • Patent number: 5965740
    Abstract: 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: Grant
    Filed: February 20, 1998
    Date of Patent: October 12, 1999
    Assignee: Shionogi & Co., Ltd.
    Inventors: Hiroyuki Kai, Akira Takase, Toshikazu Ohtsuka
  • Patent number: 5965558
    Abstract: 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: Grant
    Filed: October 29, 1997
    Date of Patent: October 12, 1999
    Assignee: Ontogen Corporation
    Inventors: Adnan Mjalli, Sepehr Sarshar, Xiaodong Cao, Farid Bakir
  • Patent number: 5942535
    Abstract: 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: Grant
    Filed: March 28, 1997
    Date of Patent: August 24, 1999
    Assignee: Merckle GmbH
    Inventors: Stefan Laufer, Hans Gunther Striegel, Gerd Dannhardt
  • Patent number: 5935973
    Abstract: 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: Grant
    Filed: January 5, 1998
    Date of Patent: August 10, 1999
    Assignee: Knoll Aktiengesellschaft
    Inventors: Alan Martin Birch, David John Heal, Frank Kerrigan, Keith Frank Martin, Patricia Lesley Needham, Bruce Jeremy Sargent
  • Patent number: 5925631
    Abstract: 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: Grant
    Filed: August 3, 1998
    Date of Patent: July 20, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Cameron Black, Greg Hughes, Erich Grimm, Serge Leger, Petpiboon Prasit, Zhaoyin Wang
  • Patent number: 5922881
    Abstract: The invention relates to novel heterocyclic imino derivatives, several processes for their preparation and their use for controlling pests.
    Type: Grant
    Filed: November 27, 1996
    Date of Patent: July 13, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Lutz Assmann, Thomas Seitz, Ralf Tiemann, Heinz-Wilhelm Dehne, Klaus Stenzel
  • Patent number: 5917048
    Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning described in the specification, have retinoid-like biological activity.
    Type: Grant
    Filed: March 19, 1997
    Date of Patent: June 29, 1999
    Assignee: Allergan Sales Inc.
    Inventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
  • Patent number: 5910594
    Abstract: 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: Grant
    Filed: January 20, 1998
    Date of Patent: June 8, 1999
    Assignee: Roche Vitamins Inc.
    Inventors: Klaus Behringer, Werner Bonrath, Horst Pauling
  • Patent number: 5892052
    Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.
    Type: Grant
    Filed: April 6, 1995
    Date of Patent: April 6, 1999
    Assignee: Abbott Labortories
    Inventors: Dale J. Kempf, Daniel W. Norbeck, Hing Leung Sham, Chen Zhao
  • Patent number: 5889058
    Abstract: 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: Grant
    Filed: November 3, 1994
    Date of Patent: March 30, 1999
    Assignee: Celltech Limited
    Inventors: John Robert Porter, Thomas Andrew Millican, John Richard Morphy, Nigel Robert Arnold Beeley
  • Patent number: 5888941
    Abstract: 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: Grant
    Filed: March 31, 1997
    Date of Patent: March 30, 1999
    Assignee: J. Uriach & Cia. S.A.
    Inventors: Javier Bartroli, Enric Turmo, Manuel Anguita
  • Patent number: 5856506
    Abstract: 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: Grant
    Filed: August 22, 1997
    Date of Patent: January 5, 1999
    Assignee: University of Pittsburgh
    Inventors: John S. Lazo, Robert L. Rice, April Cunningham, Peter Wipf
  • Patent number: 5849911
    Abstract: 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: Grant
    Filed: April 9, 1997
    Date of Patent: December 15, 1998
    Assignee: Novartis Finance Corporation
    Inventors: Alexander Fassler, Guido Bold, Hans-Georg Capraro, Marc Lang, Satish Chandra Khanna
  • Patent number: 5849921
    Abstract: 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: Grant
    Filed: June 2, 1995
    Date of Patent: December 15, 1998
    Assignee: Astra Aktiebolag
    Inventors: Robin Bernad Boar, Alan John Cross, Duncan Alastair Gray, Richard Alfred Green
  • Patent number: 5846906
    Abstract: 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: Grant
    Filed: July 30, 1997
    Date of Patent: December 8, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: 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
  • Patent number: 5846990
    Abstract: 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: Grant
    Filed: February 13, 1997
    Date of Patent: December 8, 1998
    Assignee: Bristol-Myers Squibb Co.
    Inventors: Natesan Murugesan, Joel C. Barrish, Steven H. Spergel
  • Patent number: 5846907
    Abstract: 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: Grant
    Filed: July 30, 1997
    Date of Patent: December 8, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: 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
  • Patent number: 5837702
    Abstract: 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: Grant
    Filed: August 30, 1994
    Date of Patent: November 17, 1998
    Assignee: Bristol-Myers Squibb Co.
    Inventors: George C. Rovnyak, Karnail S. Atwal, Dinos P. Santafianos, Charles Z. Ding
  • Patent number: 5834468
    Abstract: 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: Grant
    Filed: July 2, 1996
    Date of Patent: November 10, 1998
    Assignee: Zeneca Limited
    Inventors: Gloria Anne Breault, John Oldfield, Howard Tucker, Peter Warner
  • Patent number: 5827860
    Abstract: Compounds of the Formula I: ##STR1## useful in the treatment of thrombin and trypsin related disorders.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 27, 1998
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Michael J. Costanzo, Bruce E. Maryanoff
  • Patent number: 5827868
    Abstract: 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: Grant
    Filed: October 7, 1991
    Date of Patent: October 27, 1998
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Raj N. Misra, Jagabandhu Das, Steven E. Hall, Wen-Ching Han, Philip M. Sher, Philip D. Stein
  • Patent number: 5827866
    Abstract: Compounds of the Formula I: ##STR1## useful in the treatment of thrombin and trypsin related disorders.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 27, 1998
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Michael J. Costanzo, Bruce E. Maryanoff
  • Patent number: 5817827
    Abstract: 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: Grant
    Filed: October 22, 1996
    Date of Patent: October 6, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Werner Bonrath, Horst Pauling
  • Patent number: 5807876
    Abstract: 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: Grant
    Filed: April 23, 1996
    Date of Patent: September 15, 1998
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David M. Armistead, Michael C. Badia, Guy W. Bemis, Randy S. Bethiel, Catharine A. Frank, Perry M. Novak, Steven M. Ronkin, Jeffrey O. Saunders
  • Patent number: 5808101
    Abstract: 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: Grant
    Filed: November 21, 1997
    Date of Patent: September 15, 1998
    Assignee: Allergan
    Inventors: Robert M. Burk, David F. Woodward
  • Patent number: 5801246
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: September 1, 1998
    Assignee: Pharmacia & Upjohn Company
    Inventors: Michael R. Barbachyn, Steven J. Brickner
  • Patent number: 5780647
    Abstract: 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: Grant
    Filed: February 25, 1997
    Date of Patent: July 14, 1998
    Assignee: Allergan
    Inventors: Vidyasagar Vuligonda, Roshantha A. Chandraratna
  • Patent number: 5770615
    Abstract: 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: Grant
    Filed: March 28, 1997
    Date of Patent: June 23, 1998
    Assignee: Bristol-Myers Squibb Company
    Inventors: 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
  • 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: 5750543
    Abstract: 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: Grant
    Filed: February 1, 1996
    Date of Patent: May 12, 1998
    Assignee: The Procter & Gamble Company
    Inventors: Laurence Ichih Wu, John Michael Janusz
  • Patent number: 5750706
    Abstract: 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: Grant
    Filed: September 3, 1996
    Date of Patent: May 12, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Pierre Barbier, Isabelle Huber, Fernand Schneider, Josef Stadlwieser, Sven Taylor
  • Patent number: 5733882
    Abstract: 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: Grant
    Filed: February 28, 1995
    Date of Patent: March 31, 1998
    Assignee: SmithKline Beecham Corporation
    Inventors: Thomas Joseph Carr, Peter Lawrence DeMarsh, Geoffrey Bainbridge Dreyer, Ashley Edward Fenwick
  • Patent number: 5733648
    Abstract: 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: Grant
    Filed: February 23, 1996
    Date of Patent: March 31, 1998
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Ernest L. Thurber, Eric G. Larson, Alan R. Kirk, Gregg D. Dahlke
  • Patent number: 5728720
    Abstract: 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: Grant
    Filed: August 25, 1995
    Date of Patent: March 17, 1998
    Assignee: Japan Tobacco Inc.
    Inventor: Hisashi Shinkai
  • Patent number: 5718845
    Abstract: Nonlinear optical compounds which contain a heteroaromatic ring and may further comprise a tricyanovinyl group attached to the heteroaromatic ring.
    Type: Grant
    Filed: January 18, 1995
    Date of Patent: February 17, 1998
    Assignee: Enichem S.p.A.
    Inventors: Kevin J. Drost, Pushkara Rao Varanasi, Kwan-Yue Alex Jen, Michael Anthony Drzewinski
  • Patent number: 5710288
    Abstract: 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: Grant
    Filed: May 3, 1996
    Date of Patent: January 20, 1998
    Assignee: Allergan
    Inventors: Robert M. Burk, David F. Woodward
  • Patent number: 5709935
    Abstract: 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: Grant
    Filed: February 23, 1996
    Date of Patent: January 20, 1998
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Ernest L. Thurber, Eric G. Larson, Alan R. Kirk, Gregg D. Dahlke
  • Patent number: 5691374
    Abstract: 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: Grant
    Filed: May 18, 1995
    Date of Patent: November 25, 1997
    Assignee: Merck Frosst Canada Inc.
    Inventors: Cameron Black, Erich Grimm, Zhaoyin Wang, Serge Leger
  • Patent number: 5686471
    Abstract: 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: Grant
    Filed: February 1, 1996
    Date of Patent: November 11, 1997
    Assignee: The Procter & Gamble Company
    Inventors: Zhuoliang Chen, John Michael Janusz