The Hetero Ring Is Substituted Patents (Class 514/465)
  • Patent number: 5880147
    Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 is alkyl; R.sup.2a, R.sup.2b, R.sup.2c and R.sup.2d are the same or different and each is hydrogen, optionally substituted alkyl, --(C.dbd.O)--B.sup.1 (wherein B.sup.1 is hydrogen or alkyl), nitro, --NR.sup.c R.sup.d (wherein R.sup.c is hydrogen or alkyl and Rd is alkyl), hydroxy, protected hydroxy group, alkoxy, cyano, alkylthio, alkylsulfinyl, alkylsulfonyl or halogen;R.sup.3 is alkyl; R.sup.4 is a group of the formula (II) ##STR2## wherein A.sup.1 is a single bond, alkylene or alkenylene; R.sup.5a and R.sup.5b are the same or different and each is hydrogen, alkyl or --A.sup.4 R.sup.5.sub.c wherein A is a single bond, alkylene or alkenylene and R.sup.5.sub.c is alkoxy; and n is 0, and pharmaceutically acceptable salts thereof. Such compounds have valuable inhibitory activity against acyl-CoA (cholesterol acyl transferase).
    Type: Grant
    Filed: September 18, 1996
    Date of Patent: March 9, 1999
    Assignee: Sankyo Company, Limited
    Inventors: Akira Yoshida, Kozo Oda, Takashi Kasai, Kousei Shimada, Hiroshi Kogen, Ichiro Hayakawa, Sadao Ishihara, Teiichiro Koga, Eiichi Kitazawa, Taro Tokui
  • Patent number: 5877191
    Abstract: The present invention is directed to certain novel compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.11, R.sup.12, R.sup.13, m, n and the dashed lines are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.
    Type: Grant
    Filed: October 22, 1997
    Date of Patent: March 2, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Charles G. Caldwell, Yuan-Ching Chiang, Conrad Dorn, Paul Finke, Jeffrey Hale, Malcolm Maccoss, Sander Mills, Albert Robichaud
  • Patent number: 5849747
    Abstract: The present invention relates to a compound of the formula (I): ##STR1## wherein Ar.sup.1, Ar.sup.2, Ar.sup.3 and Ar.sup.4 represent an aryl group or a heteroaromatic ring group; A represents a hydrocarbon group which may be substituted; X and Y represent an oxygen atom, a sulfur atom, a carbonyl group or a group of the formula --CHR.sup.a -- (wherein R.sup.a is a hydrogen atom or a lower alkyl group) or --NR.sup.b -- (wherein R.sup.b is a hydrogen atom or a lower alkyl group), or X and Y together represent a vinylene group or an ethynylene group; R.sup.1, R.sup.2, R.sup.3, R.sup.8 and R.sup.9 represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a lower alkoxy group; R.sup.4 and R.sup.
    Type: Grant
    Filed: March 15, 1996
    Date of Patent: December 15, 1998
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Yoshikazu Iwasawa, Tetsuya Aoyama, Kumiko Kawakami, Sachie Arai, Toshihiko Satoh, Yoshiaki Monden
  • Patent number: 5811438
    Abstract: The compounds of the present invention are of the formula (I): A--X--(CH.sub.2).sub.n --Y--(CH.sub.3).sub.m --Z wherein: A is an non-steroidal anti-inflammatory agent (NSAIA); A--X is an ester or amide linkage derived from the carboxylic acid moiety of the NSAIA, wherein X is O or NR; R is H, C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.6 cycloalkyl; Y, if present, is O, NR, C(R).sub.2, CH(OH) or S(O).sub.n' ; n is 2 to 4 and m is 1 to 4 when Y is O, NR, or S(O).sub.n' ; n is 0 to 4 and m is 0 to 4 when Y is C(R).sub.2 or is not present; n is 1 to 4 and m is 0 to 4 when Y is CH(OH); n' is 0 to 2; and Z is (a), (b), (c), (d) or (e) wherein: R' and R.sup.3 are H, C(O)R, C(O)N(R).sub.2, PO.sub.3.sup.-, or SO.sub.3.sup.- ; R" is H or C.sub.1 -C.sub.6 alkyl; and R' and R.sup.3 together may form a ring having structure: (1) or (2); and provided that when Z is (e), X is not O. The compounds of the present invention also include pharmaceutically acceptable salts of the compounds of formula (I).
    Type: Grant
    Filed: June 4, 1997
    Date of Patent: September 22, 1998
    Assignee: Alcon Laboratories, Inc.
    Inventors: Mark R. Hellberg, Gustav Graff, Daniel A. Gamache, Jon C. Nixon, William H. Garner
  • Patent number: 5801197
    Abstract: This invention relates to the method of using specially formulated neurotrophic pipecolic acid derivative compounds having an affinity for FKBP-type immunophilins as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity to stimulate or promote neuronal growth or regeneration.
    Type: Grant
    Filed: May 13, 1996
    Date of Patent: September 1, 1998
    Assignee: GPI Nil Holdings, Inc.
    Inventors: Joseph P. Steiner, Gregory S. Hamilton
  • Patent number: 5780592
    Abstract: A composition comprising lipoproteins and a compound of the formula I ##STR1## stereoisomeric form or salt thereof, suitable for the treatment of immunological disorders, cancer or in transplantation.
    Type: Grant
    Filed: December 10, 1996
    Date of Patent: July 14, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Stefan Mullner, Axel Hofmann, Karin Saar, Hans-Ulrich Schorlemmer, Robert Bartlett
  • Patent number: 5756510
    Abstract: A range of 3-oxybenzamide compounds and related quinazolinone compounds are disclosed which can act as potent inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase or PARP enzyme (EC 2.4.2.30), and which thereby can provide useful therapeutic compounds for use in conjunction with DNA-damaging cytotoxic drugs or radiotherapy to potentiate the effects of the latter. The compounds disclosed include 3-benzyloxybenzamides, 3-oxybenzamides in which a chain of 5 or more methylene groups terminate in a halogen atom or in a purin-9-yl moiety, certain benzoxazole-4-carboxamide compounds and certain quinazolinone compounds. In formula X and Y together may form a bride --X--Y-- that represents the grouping (a), (b) or (c )wherein R.sup.5 is H, alkyl, aryl or aralkyl.
    Type: Grant
    Filed: August 30, 1996
    Date of Patent: May 26, 1998
    Assignee: Newcastle University Ventures Limited
    Inventors: Roger John Griffin, Alan Hilary Calvert, Nicola Jane Curtin, David Richard Newell, Bernard Thomas Golding
  • Patent number: 5731352
    Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which A, R.sub.1, R'.sub.1, R.sub.2, R.sub.3 and n are as defined in the description, and medicinal product containing the same useful for treating a mammal afflicted with a disorder of the melatoninergic system.
    Type: Grant
    Filed: May 30, 1996
    Date of Patent: March 24, 1998
    Assignee: Adir Et Compagnie
    Inventors: Daniel Lesieur, Veronique Leclerc, Patrick Depreux, Philippe Delagrange, Pierre Renard
  • Patent number: 5726165
    Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, or solvate thereof, wherein,R.sup.o represents an aryl group, optionally substituted;X represents O or S;R.sup.1 and R.sup.1a each independently represents hydrogen or an alkyl group;R.sup.2 represents OCH.sub.2 CO.sub.2 H, or an ester or amide thereof, or R.sup.2 represents a moiety of formula (b): ##STR2## wherein R.sup.4 represent hydrogen, alkyl, hydroxyalkyl, arylalkyl, aralkyloxyalkyl or cycloalkyl and R.sup.5 represent hydroxy, alkoxy, arylalkyloxy, hydroxyalkyloxy, alkoxyalkyloxy, arylalkoxyalkyloxy, cycloalkyloxy, hydrogen, alkyl, substituted alkyl, cycloalkyl, aryl, arylalkyl, arylalkyloxyalkyl or R.sup.5 together with OR.sup.4 represents O(CH.sub.2).sub.n O wherein n is 2, 3 or 4; andR.sup.3 represents hydrogen, halogen, alkyl or alkoxy or R.sup.3 together with R.sup.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: March 10, 1998
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Lee James Beeley, Mervyn Thompson, David Kenneth Dean, Nikesh Rasiklal Kotecha, John Michael Berge, Robert William Ward
  • Patent number: 5726195
    Abstract: Certain novel aminoacyl adenylate mimics are described. An exemplary compound of this invention is ?S-(R*,R*)!-3,6-anhydro-1,2-dideoxy-1-?5-?4-?(5-nitro-2-thienyl)ethynyl!ph enyl!-2H-tetrazol-2-yl!-D-allo-heptitol 7-(2-amino-3-methyl-1-oxopentyl)sulfamate. These compounds inhibit isoleucyl-tRNA synthetases and are useful as antimicrobial and antiparasitic agents.
    Type: Grant
    Filed: July 16, 1996
    Date of Patent: March 10, 1998
    Assignee: Cubist Pharmaceuticals, Inc.
    Inventors: Jason M. Hill, Guixue Yu, Youe-Kong Shue, Thomas M. Zydowsky, Julius Rebek
  • Patent number: 5719183
    Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: February 17, 1998
    Assignee: SmithKline Beecham Corporation
    Inventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
  • Patent number: 5719182
    Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.
    Type: Grant
    Filed: May 16, 1995
    Date of Patent: February 17, 1998
    Assignee: SmithKline Beecham Corporation
    Inventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
  • Patent number: 5716985
    Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.
    Type: Grant
    Filed: May 23, 1995
    Date of Patent: February 10, 1998
    Assignee: SmithKline Beecham Corporation
    Inventors: John Duncan Elliott, Maria Amparo Lago
  • Patent number: 5691373
    Abstract: Novel nonpeptide antagonists of endothelin I are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, myocardial ischemia, cerebral vasospasm, cerebral ischemia, cerebral infarction, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, stroke, benign prosthatic hyperplasia (BPH), and diabetes.
    Type: Grant
    Filed: February 6, 1995
    Date of Patent: November 25, 1997
    Assignee: Warner-Lambert Company
    Inventors: Kent Alan Berryman, Annette Marian Doherty, Jeremy John Edmunds, William Chester Patt, Mark Stephen Plummer, Joseph Thomas Repine
  • Patent number: 5681842
    Abstract: The present invention provides a compound of the formula: ##STR1## such compounds are useful for inhibiting prostaglandin synthesis. Pharmaceutical compositions and methods for inhibiting prostaglandin synthesis are also disclosed.
    Type: Grant
    Filed: November 8, 1996
    Date of Patent: October 28, 1997
    Assignee: Abbott Laboratories
    Inventors: Joseph F. Dellaria, Todd H. Gane
  • Patent number: 5654332
    Abstract: The present invention relates to methods and pharmaceutical compositions for stimulating the growth of neurites in nerve cells. The compositions comprise a neurotrophic amount of a compound which binds to the FK-506 binding protein (FKBP) and a neurotrophic factor, such as nerve growth factor NGF. The methods comprise treating nerve cells with the above-described compositions or compositions comprising the FKBP binding compound without a neurotrophic factor. The methods of this invention can be used to promote repair of neuronal damage caused by disease or physical trauma.
    Type: Grant
    Filed: June 8, 1995
    Date of Patent: August 5, 1997
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventor: David M. Armistead
  • Patent number: 5646147
    Abstract: Acaricidal, insecticidal and nematicidal substituted (hetero)arylalkyl ketone oxime O-ethers, processes for their preparation, agents containing them, and their use as pesticides.The invention relates to compounds of the formula ##STR1## in which Ar.sup.1 and Ar.sup.2 are aryl or heteroaryl, each of which is optionally substituted, and R is an optionally substituted aliphatic or alicyclic radical, to processes for their preparation, and to agents containing these compounds, and to their use for controlling animal pests.
    Type: Grant
    Filed: April 20, 1994
    Date of Patent: July 8, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Birgit Kuhn, Gerhard Salbeck, deceased, Uwe Doller, Stefan Schnatterer, Hans-Herbert Schubert, Werner Knauf, Anna Waltersdorfer, Manfred Kern
  • Patent number: 5633248
    Abstract: A compound of the formula: ##STR1## wherein Ar.sup.1 and Ar.sup.2 independently represent an optionally substituted aromatic group; P and Q independently represent a divalent aliphatic hydrocarbon group having at least 2 carbon atoms and optionally having either oxygen or sulfur in the carbon chain; R.sup.1 and R.sup.3 independently represent --CO--R, --CONH--R (R represents a hydrocarbon group or a heterocyclic group) or a hydrocarbon group; R.sup.2 and R.sup.4 independently represent hydrogen or an alkyl group; R.sup.2 and R.sup.4 independently represent hydrogen or an alkyl group; R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4, taken together with the adjacent nitrogen atom, may form a nitrogen-containing heterocyclic group; and j represents 0 or 1, or a salt thereof, has excellent GnRH-receptor antagonizing activity and is useful as a prophylactic and therapeutic agent for hormone-dependent and other diseases.
    Type: Grant
    Filed: November 21, 1995
    Date of Patent: May 27, 1997
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Kaneyoshi Kato, Yoshihiro Sugiura, Koichi Kato
  • Patent number: 5631248
    Abstract: Two-component pharmaceutical compositions for topical application to the human or animal body comprising two miscible liquid phases having different lipophilicities and a drug dissolved in at least one liquid phase, each phase comprising at least one topically acceptable non-aqueous and non-volatile solvent.
    Type: Grant
    Filed: October 7, 1994
    Date of Patent: May 20, 1997
    Assignee: SmithKline Beecham plc
    Inventors: Adrian F. Davis, Jennifer J. Gordon
  • Patent number: 5612371
    Abstract: New amino acid derivatives, processes for their preparation and their therapeutic application.Amino acid derivatives corresponding to the general formulae ##STR1## These derivatives may be used as medicaments which exhibit an enkephalinase-inhibitory activity.
    Type: Grant
    Filed: July 18, 1994
    Date of Patent: March 18, 1997
    Assignee: Societe Civile Bioproject
    Inventors: Denis Danvy, Thierry Monteil, Christophe Lusson, Jean-Charles Schwartz, Claude Gros, Nadine Noel, Jeanne-Marie Lecomte, Pierre Duhamel, Lucette Duhamel
  • Patent number: 5607966
    Abstract: Compounds having anti-inflammatory and anti-oxidant activity are disclosed. The compounds are useful in preventing and treating inflammatory disorders through several mechanisms. Methods of treatment employing these properties of the compounds and corresponding pharmaceutical compositions are disclosed.
    Type: Grant
    Filed: December 23, 1994
    Date of Patent: March 4, 1997
    Assignee: Alcon Laboratories, Inc.
    Inventors: Mark R. Hellberg, Gustav Graff
  • Patent number: 5597843
    Abstract: The present invention provides a method of reducing a wasting condition, which can occur due to a pathology or to a particular physiologic or metabolic state in a subject, by administering to the subject a substituted 1,3-benzodioxole.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: January 28, 1997
    Assignee: Houghten Pharmaceuticals
    Inventors: Beverly E. Girten, Ronald R. Tuttle
  • Patent number: 5567728
    Abstract: Use of a compound selected from the group consisting of 3,5-diiodo-4-(2-N, N-diethylaminoethoxy)phenyl-(2-butylbenzofur-3-yl)methanol hydrochloride (001), 2-methyl-3-(3,5-diiodo-4-(2-N,N-diethylaminoethoxy)-benzoyl)benzofuran hydrochloride (003), 2-n-butyl-3-(3,5-diiodo-4-carboxymethoxybenzoyl)benzofuran (005), 2-methyl-3-(3,5-diiodo-4-hydroxy-benzoyl)benzofuran (011), 2-methyl-3-(3,5-diiodo-4-carboxymethoxybenzyl)benzofuran (015), 4'-hydroxy-3'-iodo-3,5-diiodo-4-(2-N,N-diethylaminoethoxy)benzophenon hydrochloride (024), 2-butyl-3-(3-iodo-4-hydroxy-benzoyl)benzofuran (029), 4'4'-dihydroxy-3'3,5-triiododiphenylmethan (032), which compound is a 3,5,3'-triiodothyronine (T-3) receptor ligand, for the preparation of a medicament for the therapeutic or prophylactic treatment of a disorder which depends on the expression of T-3 regulated genes, and pharmaceutical preparations comprising said compounds, are disclosed.
    Type: Grant
    Filed: February 25, 1994
    Date of Patent: October 22, 1996
    Assignee: Karobio Aktiebolag
    Inventors: Ulf Norinder, Jurgen Bajorath, Jay F. Stearns
  • Patent number: 5565485
    Abstract: Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, inflammatory diseases including Raynaud's disease and asthma.
    Type: Grant
    Filed: August 22, 1994
    Date of Patent: October 15, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Scott W. Bagley, Theodore P. Broten, Prasun K. Chakravarty, Daljit S. Dhanoa, Kenneth J. Fitch, William J. Greenlee, Nancy J. Kevin, Douglas J. Pettibone, Ralph A. Rivero, Thomas F. Walsh, David L. Williams, Jr., Richard B. Toupence, Jay M. Matthews
  • Patent number: 5563171
    Abstract: Substituted 5-2-((2-aryl-2-hydroxyethyl)amino)propyl)-1,3-benzodioxoles having the structural formula: ##STR1## wherein R4, R5, R6, R7, and R8 are as hereinafter defined, are .beta.3-adrenergic agonists useful in the treatment of elevated intraocular pressure and glaucoma.
    Type: Grant
    Filed: November 5, 1993
    Date of Patent: October 8, 1996
    Assignee: American Cyanamid Company
    Inventors: Romulus K. Brazzell, Bernard Dubnick
  • Patent number: 5527822
    Abstract: A method of treatment of a mammal, including humans, suffering from traumatic brain injury, which comprises administering to the sufferer a therapeutically effective amount of a butyrolactone derivative.
    Type: Grant
    Filed: December 29, 1993
    Date of Patent: June 18, 1996
    Assignee: Forest Laboratories, Inc.
    Inventor: Stuart L. Scheiner
  • Patent number: 5516797
    Abstract: This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamase) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.
    Type: Grant
    Filed: April 11, 1994
    Date of Patent: May 14, 1996
    Assignee: Vertex Pharmaceuticals, Incorporated
    Inventors: David M. Armistead, Joshua S. Boger, Harold V. Meyers, Jeffrey O. Saunders, Roger D. Tung
  • Patent number: 5496848
    Abstract: The reaction of 2,2-difluorobenzo-1,3-dioxole with (a) an alkali metal or an alkali metal compound and then (b) a compound R.sup.1 -Z.sup.1 in which Z.sup.1 is a leaving group, or with an aldehyde produces compounds of formula I ##STR1## wherein R.sup.1 is --OH, --SH, --CHO, --CN, --COOH, --B(OH).sub.2, --COX, with X being Cl or Br, or is --COOR.sup.2, --SIR.sup.2.sub.3 or --B(OR.sup.2).sub.2, with R.sup.2 being a C.sub.1 -C.sub.12 alcohol moiety without the hydroxy group, wherein R.sup.1 is further --C.sub.n H.sub.2n COOR.sup.2, with n being an integer from 1 to 4, or linear or branched C.sub.1 -C.sub.12 hydroxyalkyl which is unsubstituted or is substituted by --F, --CN, C.sub.1 -C.sub.6 alkoxy, phenyl, fluorophenyl, C.sub.1 -C.sub.4 alkoxy-phenyl, C.sub.1 -C.sub.4 alkylthio-phenyl, C.sub.1 -C.sub.4 alkyl-phenyl, C.sub.1 -C.sub.4 fluoroalkyl-phenyl, nitrophenyl or by cyanophenyl, or wherein R.sup.1 is a benzyl alcohol which is unsubstituted or is substituted by F, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.
    Type: Grant
    Filed: May 12, 1995
    Date of Patent: March 5, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Peter Ackermann, Hans-Ruedi Ka/ nel, Bruno Schaub
  • Patent number: 5489587
    Abstract: The present invention provides methods for inhibiting bone loss comprising administering to a mammal in need of treatment of a bone loss inhibiting amount of a compound of formula I ##STR1## wherein R is hydrogen or methyl;R.sup.1 and R.sup.2 each are methyl or ethyl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached represent a saturated heterocyclic group; andX is bromo, chloro, fluoro, or hydrogen; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 20, 1995
    Date of Patent: February 6, 1996
    Assignee: Eli Lilly and Company
    Inventor: Steven A. Fontana
  • Patent number: 5488064
    Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof where A is phenyl, naphthyl or dihydro- or tetrahydronaphthyl optionally substituted on the aromatic ring by one to three substituents independently selected from halogen, cyano, trifluoromethyl, nitro, alkoxy, alkylsulfonyl, alkyl, cycloalkyl, aryl or a hydrogen bond donor; B is a bond or an oxygen atom and R.sup.1 to R.sup.4 are as defined herein. These compounds are beta 3 adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity and gastrointestinal diseases.
    Type: Grant
    Filed: May 2, 1994
    Date of Patent: January 30, 1996
    Assignee: Bristol-Myers Squibb Company
    Inventor: Philip M. Sher
  • Patent number: 5482971
    Abstract: This invention is concerned with novel compounds of formula I: ##STR1## which are selective beta.sub.3 -adrenergic agents.
    Type: Grant
    Filed: October 1, 1993
    Date of Patent: January 9, 1996
    Assignee: American Cyanamid Company
    Inventors: Joseph W. Epstein, Gary H. Birnberg, Feng L. Qing
  • Patent number: 5480871
    Abstract: Compounds of the formula: ##STR1## are useful for treating conditions modulated by .alpha..sub.1 -adrenergic receptors.
    Type: Grant
    Filed: May 12, 1995
    Date of Patent: January 2, 1996
    Assignee: Chiron Corporation
    Inventors: David C. Spellmeyer, Walter H. Moos, Eric J. Martin, Ronald N. Zuckermann, Gregory Stauber
  • Patent number: 5480908
    Abstract: The invention is antiobesity/antidiabetes beta-3 agonists of the formula: ##STR1## wherein Ar, X, R.sub.2, R.sub.3, Y and n are as defined in the specification.
    Type: Grant
    Filed: December 13, 1993
    Date of Patent: January 2, 1996
    Assignee: American Cyanamid Company
    Inventors: Joseph W. Epstein, Gary H. Birnberg, Minu D. Dutia, Thomas H. Claus, Elwood E. Largis
  • Patent number: 5475024
    Abstract: A new benzodioxole derivative has a substituent in the phenyl ring which is a carboxyalkylthioalkyl or the like and is effective to treat a liver disease.
    Type: Grant
    Filed: October 14, 1993
    Date of Patent: December 12, 1995
    Assignee: Eisai Co., Ltd.
    Inventors: Yoshitake Ogata, Makoto Ikeda, Seiichiro Nomoto, Makoto Okita, Naoyuki Shimomura, Toshihiko Kaneko, Takashi Yamanaka, Ieharu Hishinuma, Junichi Nagakawa, Kazuo Hirota, Kaname Miyamoto, Toru Horie, Tsuneo Wakabayashi
  • Patent number: 5447916
    Abstract: Compounds of the formula: ##STR1## are useful for treating conditions modulated by .alpha..sub.1 -adrenergic receptors.
    Type: Grant
    Filed: July 30, 1993
    Date of Patent: September 5, 1995
    Assignee: Chiron Corporation
    Inventors: David C. Spellmeyer, Walter H. Moos, Eric J. Martin, Ronald N. Zuckermann, Gregory Stauber
  • Patent number: 5428060
    Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. 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 and in preventing the formation of atherosclerotic plaques.
    Type: Grant
    Filed: August 27, 1992
    Date of Patent: June 27, 1995
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Yves Ducharme, John W. Gillard, Rejean Fortin, Daniel Dube, Yves Girard, Pierre Hamel, Daniel Delorme
  • Patent number: 5385931
    Abstract: The invention relates to new sulphonamide derivatives of benzo-cyclic or benzo-heterocyclic acids and their derivatives of general formula I ##STR1## in which: R represents a straight-chain or branched lower alkyl radical having 1 to 9 C;a phenyl radical which is unsubstituted or substituted by one or more groups:straight-chain or branched lower alkyl having 1 to 4 C, halogeno, alkoxy, nitro, amino, dialkylamino or CF.sub.3 ;a substituted or unsubstituted naphthalene;a thiophenyl radical;R.sub.1 represents a hydrogen or a straight-chain or branched lower alkyl or a benzyl;R.sub.2 represents a hydrogen, a straight-chain or branched lower alkyl group, a substituted or unsubstituted phenyl group or an aralkyl group;R.sub.3 represents a hydrogen or a straight-chain or branched lower alkyl (1 to 6 C);--X-- represents a divalent functional radical chosen from the following: --CH.sub.2 --; ##STR2## where R.sub.
    Type: Grant
    Filed: December 28, 1990
    Date of Patent: January 31, 1995
    Assignee: Pierre Fabre Medicament
    Inventors: Dennis Bigg, Alain Duflos, Jean-Pierre Rieu
  • Patent number: 5378727
    Abstract: Novel substituted heterocyclic derivatives are provided which inhibit platelet aggregation. This invention also pertains to pharmaceutical compositions and methods of using such derivatives.
    Type: Grant
    Filed: July 19, 1993
    Date of Patent: January 3, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Philippe R. Bovy, Joseph G. Rico, Thomas E. Rogers, Foe S. Tjoeng, Jeffery A. Zablocki
  • Patent number: 5373020
    Abstract: The present invention discloses substituted 1,3-benzodioxoles which possess anti-diabetic and/or anti-hyperglycemic and/or anti-obesity properties in humans and other animals.
    Type: Grant
    Filed: June 3, 1993
    Date of Patent: December 13, 1994
    Assignee: American Cyanamid Company
    Inventors: Jonathan D. Bloom, Thomas H. Claus, Vern G. DeVries, Jo A. Dolan, Minu D. Dutia
  • Patent number: 5326785
    Abstract: Described are caffeic acid derivatives represented by the following formula: ##STR1## wherein either one of R.sup.1 and R.sup.2 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, a group --CO.sub.2 R.sup.4, or a group --CONR.sup.5 R.sup.6, R.sup.4, R.sup.5 and R.sup.6 being either a hydrogen atom or a particular group, and the other is the group --CO.sub.2 R.sup.4 or the group --CONR.sup.5 R.sup.6, or R.sup.1 and R.sup.2 are coupled together to represent a 5-membered ring so formed, Y represents a particular group or atom, X represents a substituted or unsubstituted C.sub.6 -C.sub.10 aryl, C.sub.7 -C.sub.12 aralkyl, heterocyclic or heterocyclic ring-alkyl group, m and n stand for particular integers, and R.sup.3 represents a hydrogen atom, a hydroxyl group, a group --OCO.sub.2 R.sup.7, R.sup.7 being a hydrogen atom or a particular group, or a group --OCONR.sup.8 R.sup.9, R.sup.8 representing a C.sub.1 -C.sub.6 alkyl group and R.sup.9 representing a hydrogen atom or a C.sub.1 -C.sub.
    Type: Grant
    Filed: March 31, 1993
    Date of Patent: July 5, 1994
    Assignee: Suntory Limited
    Inventors: Hidetsura Cho, Mie Tamaoka, Seiitsu Murota, Ikuo Morita
  • Patent number: 5308865
    Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of ##STR2## R.sub.13, R.sub.14 and R.sub.15 are individually selected from the group consisting of hydrogen, halogen and alkyl of 1 to 3 carbon atoms, n is an integer from 1 to 3, R.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.3, R.sub.4 R.sub.5, R.sub.6 and R.sub.7 are individually selected from the group consisting of hydrogen, halogen, --NO.sub.2, --CN, alkyl, alkylthio and alkoxy of 1 to 6 carbon atoms, alkylcarbonyl of 2 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, ##STR3## m is 0, 1, 2 or 3, n is 1, 2 or 3; Hal, Hal.sub.1, Hal.sub.2 and Hal.sub.3 are individually halogen and ##STR4## R.sub.8, R.sub.9, R.sub.10, R.sub.11 and R.sub.12 are individually any of the groups defined above for R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 or R.sub.4 and R.sub.5 together form --O--CH.sub.
    Type: Grant
    Filed: January 6, 1993
    Date of Patent: May 3, 1994
    Assignee: Roussel Uclaf
    Inventors: Robert R. Bartlett, David P. Kay, Elizabeth A. Kuo, Rudolf Schleyerbach, Wilfried Schwab
  • Patent number: 5296507
    Abstract: A method for the treatment of dementia and cerebrovascular disorders and for inhibiting platelet aggregation in patients in need thereof comprising the step of administering a therapeutically effective amount of a 1-[3-(dimethylamino)propyl]-1-phenylphthalane of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each are selected from the group consisting of halogen, trifluoromethyl, cyano and R--CO--, wherein R is an alkyl radical, or a pharmaceutically-acceptable acid addition salt thereof, is described.
    Type: Grant
    Filed: January 6, 1993
    Date of Patent: March 22, 1994
    Assignee: H.Lundbeck A/S
    Inventors: Yoshiaki Tanaka, Naomi Kobayashi, Tadashi Kurimoto, Yugo Ikeda
  • Patent number: 5274000
    Abstract: A new series of benzofuran and benzothiophene derivatives are disclosed. These compounds have a structure which can be obtained by substituting the third position of 2-lower alkyl-benzofuran or 2-lower alkyl-benzothiophene with a substituted benzene derivative, itaconic acid derivative or a substituted phenoxymethyl tetrazole derivative. They are useful as diuretics without side effects of elevating serum uric acid levels and can be used in the treatment of hyperuricemia.
    Type: Grant
    Filed: April 21, 1992
    Date of Patent: December 28, 1993
    Assignee: Kotobuki Seiyaku Company Limited
    Inventors: Tsuyoshi Tomiyama, Akira Tomiyama, Koichi Kubota
  • Patent number: 5252601
    Abstract: The present invention relates to novel 2-mercaptomethylene-tetrahydronaphthalene derivatives which are useful as enkephalinase inhibitors.
    Type: Grant
    Filed: April 3, 1992
    Date of Patent: October 12, 1993
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Gary A. Flynn, Douglas W. Beight
  • Patent number: 5250558
    Abstract: Substituted triazolinone, triazolinethione, and triazolinimine compounds of formula (I) are as neurotensin II antagonists.
    Type: Grant
    Filed: January 28, 1992
    Date of Patent: October 5, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Prasun K. Chakravarty, Richard W. Ransom
  • Patent number: 5202351
    Abstract: A novel 1-phenylalkyl-3-phenylurea derivative represented by the following formula (I): ##STR1## wherein R.sup.1 and R.sup.5 represent independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.5 alkoxyl or halo; R.sup.2 represents hydrogen or C.sub.1 -C.sub.15 alkyl; R.sup.3 represents C.sub.1 -C.sub.15 alkyl or R.sup.3 represents together with R.sup.2 C.sub.2 -C.sub.9 alkylene; R.sup.4 and R.sup.5 represent independently C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxyl or halo; X represents oxygen or sulfur; Y represents --O--(CH.sub.2).sub.l --O-- wherein l is an integer of 1 to 3 or --(CH.sub.2).sub.p -- wherein p is an integer of 3 to 5; m is 0 or an integer of 1 to 5; and n is 0 or an integer of 1 to 3, is provided. The 1-phenylalkyl-3-phenylurea derivative (I) have the action of reducing cholesterol in blood by ACAT inhibition, and therefore, useful for treating hyperlipemia and atherosclerosis.
    Type: Grant
    Filed: January 22, 1991
    Date of Patent: April 13, 1993
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Tetsuo Sekiya, Shinya Inoue, Chiaki Hyodo, Hiromi Okushima, Kohei Umezu, Kazuo Suzuki
  • Patent number: 5162367
    Abstract: Insecticidal and acaricidal compounds of FormulaAR(CH.sub.2).sub.x O(CH.sub.2).sub.m A(CH.sub.2).sub.n (CE.sup.1 =CE.sup.2).sub.a (CE.sup.3 =CE.sup.4)CONR.sup.1 R.sup.2 (I)whereinAr is phenyl or naphthyl, in either case optionally substituted by one or more of optionally substituted C.sub.1-6 alkyl, optionally substituted C.sub.1-6 -alkylthio or C.sub.1-6 alkylthiooxy, halogen or optionally substituted C.sub.1-6 alkoxy,x=0 or 1m=1 to 7n=1 to 7A=CH.sub.2 or oxygena=0 or 1R.sup.1 and R.sup.2 are independently selected from hydrogen, C.sub.1-6 alkyl and C.sub.3-6 cycloalkyl (either of which may be substituted by one or more of halo, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, CF.sub.2-6 alkoxy, C.sub.2-6 alkynyl, dioxalanyl and C.sub.3-6 cycloalkyl)E.sup.1, E.sup.2, E.sup.3 and E.sup.4 are independently selected from hydrogen, C.sub.1-4 alkyl, optionally substituted by halo, and nitrile, provided that at least one of E.sup.1, E.sup.2, E.sup.3 and E.sup.
    Type: Grant
    Filed: October 23, 1989
    Date of Patent: November 10, 1992
    Assignee: The Wellcome Foundation Limited
    Inventors: Robert J. Blade, John E. Robinson
  • Patent number: 5106867
    Abstract: The present invention discloses substituted 1,3-benzodioxoles which possess anti-diabetic and/or anti-hyperglycemic and/or anti-obesity properties in humans and other animals.
    Type: Grant
    Filed: April 5, 1991
    Date of Patent: April 21, 1992
    Assignee: American Cyanamid Company
    Inventors: Jonathan D. Bloom, Thomas H. Claus, Vern G. DeVries, Jo A. Dolan, Minu D. Dutia
  • Patent number: 5106407
    Abstract: The present invention discloses the antimicrobial utility of certain iodonium ylide compounds. The particular iodonium ylide compounds are phenyl iodonium ylides having an ortho substituent that stabilizes the positive charge on the polyvalent iodine by a nonbonded electrostatic interaction. The polyvalent iodine is further stabilized by a cyclic 1,3-dicarbonyl anion.
    Type: Grant
    Filed: December 4, 1989
    Date of Patent: April 21, 1992
    Assignee: The Dow Chemical Company
    Inventors: Attila G. Relenyi, Gerald F. Koser, Richard W. Walter, Jr., William J. Kruper, Jr., Ravi B. Shankar, Anthony P. Zelinko
  • Patent number: 5102906
    Abstract: Catechol derivatives which relate to the production of nerve growth factor in particular tissues of brain are disclosed.Methods for the synthesis, data on the physiological activity, and data on the toxicity of these derivatives as well as examples of preparation for their administration are also disclosed.The disclosed derivatives provide preventive and remedial effect for regressive disorders in the central nervous system including senile dementia of Alzheimer type.
    Type: Grant
    Filed: October 31, 1990
    Date of Patent: April 7, 1992
    Assignee: Mitsui Toatsu Chemicals, Incorporated
    Inventors: Shigenobu Nakayama, Fumiaki Ikeda