The Hetero Ring Is Substituted Patents (Class 514/465)
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Patent number: 5880147Abstract: 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: GrantFiled: September 18, 1996Date of Patent: March 9, 1999Assignee: Sankyo Company, LimitedInventors: Akira Yoshida, Kozo Oda, Takashi Kasai, Kousei Shimada, Hiroshi Kogen, Ichiro Hayakawa, Sadao Ishihara, Teiichiro Koga, Eiichi Kitazawa, Taro Tokui
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Patent number: 5877191Abstract: 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: GrantFiled: October 22, 1997Date of Patent: March 2, 1999Assignee: Merck & Co., Inc.Inventors: Charles G. Caldwell, Yuan-Ching Chiang, Conrad Dorn, Paul Finke, Jeffrey Hale, Malcolm Maccoss, Sander Mills, Albert Robichaud
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Patent number: 5849747Abstract: 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: GrantFiled: March 15, 1996Date of Patent: December 15, 1998Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshikazu Iwasawa, Tetsuya Aoyama, Kumiko Kawakami, Sachie Arai, Toshihiko Satoh, Yoshiaki Monden
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Patent number: 5811438Abstract: 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: GrantFiled: June 4, 1997Date of Patent: September 22, 1998Assignee: Alcon Laboratories, Inc.Inventors: Mark R. Hellberg, Gustav Graff, Daniel A. Gamache, Jon C. Nixon, William H. Garner
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Patent number: 5801197Abstract: 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: GrantFiled: May 13, 1996Date of Patent: September 1, 1998Assignee: GPI Nil Holdings, Inc.Inventors: Joseph P. Steiner, Gregory S. Hamilton
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Patent number: 5780592Abstract: 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: GrantFiled: December 10, 1996Date of Patent: July 14, 1998Assignee: Hoechst AktiengesellschaftInventors: Stefan Mullner, Axel Hofmann, Karin Saar, Hans-Ulrich Schorlemmer, Robert Bartlett
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Patent number: 5756510Abstract: 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: GrantFiled: August 30, 1996Date of Patent: May 26, 1998Assignee: Newcastle University Ventures LimitedInventors: Roger John Griffin, Alan Hilary Calvert, Nicola Jane Curtin, David Richard Newell, Bernard Thomas Golding
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Patent number: 5731352Abstract: 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: GrantFiled: May 30, 1996Date of Patent: March 24, 1998Assignee: Adir Et CompagnieInventors: Daniel Lesieur, Veronique Leclerc, Patrick Depreux, Philippe Delagrange, Pierre Renard
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Patent number: 5726165Abstract: 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: GrantFiled: June 5, 1995Date of Patent: March 10, 1998Assignee: SmithKline Beecham p.l.c.Inventors: Lee James Beeley, Mervyn Thompson, David Kenneth Dean, Nikesh Rasiklal Kotecha, John Michael Berge, Robert William Ward
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Patent number: 5726195Abstract: 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: GrantFiled: July 16, 1996Date of Patent: March 10, 1998Assignee: Cubist Pharmaceuticals, Inc.Inventors: Jason M. Hill, Guixue Yu, Youe-Kong Shue, Thomas M. Zydowsky, Julius Rebek
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Patent number: 5719183Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: June 2, 1995Date of Patent: February 17, 1998Assignee: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
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Patent number: 5719182Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: May 16, 1995Date of Patent: February 17, 1998Assignee: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
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Patent number: 5716985Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: May 23, 1995Date of Patent: February 10, 1998Assignee: SmithKline Beecham CorporationInventors: John Duncan Elliott, Maria Amparo Lago
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Patent number: 5691373Abstract: 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: GrantFiled: February 6, 1995Date of Patent: November 25, 1997Assignee: Warner-Lambert CompanyInventors: Kent Alan Berryman, Annette Marian Doherty, Jeremy John Edmunds, William Chester Patt, Mark Stephen Plummer, Joseph Thomas Repine
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Patent number: 5681842Abstract: 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: GrantFiled: November 8, 1996Date of Patent: October 28, 1997Assignee: Abbott LaboratoriesInventors: Joseph F. Dellaria, Todd H. Gane
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Patent number: 5654332Abstract: 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: GrantFiled: June 8, 1995Date of Patent: August 5, 1997Assignee: Vertex Pharmaceuticals IncorporatedInventor: David M. Armistead
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Patent number: 5646147Abstract: 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: GrantFiled: April 20, 1994Date of Patent: July 8, 1997Assignee: Hoechst AktiengesellschaftInventors: Birgit Kuhn, Gerhard Salbeck, deceased, Uwe Doller, Stefan Schnatterer, Hans-Herbert Schubert, Werner Knauf, Anna Waltersdorfer, Manfred Kern
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Patent number: 5633248Abstract: 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: GrantFiled: November 21, 1995Date of Patent: May 27, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Kaneyoshi Kato, Yoshihiro Sugiura, Koichi Kato
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Patent number: 5631248Abstract: 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: GrantFiled: October 7, 1994Date of Patent: May 20, 1997Assignee: SmithKline Beecham plcInventors: Adrian F. Davis, Jennifer J. Gordon
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Patent number: 5612371Abstract: 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: GrantFiled: July 18, 1994Date of Patent: March 18, 1997Assignee: Societe Civile BioprojectInventors: Denis Danvy, Thierry Monteil, Christophe Lusson, Jean-Charles Schwartz, Claude Gros, Nadine Noel, Jeanne-Marie Lecomte, Pierre Duhamel, Lucette Duhamel
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Patent number: 5607966Abstract: 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: GrantFiled: December 23, 1994Date of Patent: March 4, 1997Assignee: Alcon Laboratories, Inc.Inventors: Mark R. Hellberg, Gustav Graff
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Patent number: 5597843Abstract: 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: GrantFiled: June 7, 1995Date of Patent: January 28, 1997Assignee: Houghten PharmaceuticalsInventors: Beverly E. Girten, Ronald R. Tuttle
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Patent number: 5567728Abstract: 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: GrantFiled: February 25, 1994Date of Patent: October 22, 1996Assignee: Karobio AktiebolagInventors: Ulf Norinder, Jurgen Bajorath, Jay F. Stearns
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Patent number: 5565485Abstract: 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: GrantFiled: August 22, 1994Date of Patent: October 15, 1996Assignee: 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
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Patent number: 5563171Abstract: 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: GrantFiled: November 5, 1993Date of Patent: October 8, 1996Assignee: American Cyanamid CompanyInventors: Romulus K. Brazzell, Bernard Dubnick
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Patent number: 5527822Abstract: 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: GrantFiled: December 29, 1993Date of Patent: June 18, 1996Assignee: Forest Laboratories, Inc.Inventor: Stuart L. Scheiner
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Patent number: 5516797Abstract: 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: GrantFiled: April 11, 1994Date of Patent: May 14, 1996Assignee: Vertex Pharmaceuticals, IncorporatedInventors: David M. Armistead, Joshua S. Boger, Harold V. Meyers, Jeffrey O. Saunders, Roger D. Tung
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Patent number: 5496848Abstract: 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: GrantFiled: May 12, 1995Date of Patent: March 5, 1996Assignee: Ciba-Geigy CorporationInventors: Peter Ackermann, Hans-Ruedi Ka/ nel, Bruno Schaub
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Patent number: 5489587Abstract: 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: GrantFiled: January 20, 1995Date of Patent: February 6, 1996Assignee: Eli Lilly and CompanyInventor: Steven A. Fontana
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Patent number: 5488064Abstract: 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: GrantFiled: May 2, 1994Date of Patent: January 30, 1996Assignee: Bristol-Myers Squibb CompanyInventor: Philip M. Sher
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Patent number: 5482971Abstract: This invention is concerned with novel compounds of formula I: ##STR1## which are selective beta.sub.3 -adrenergic agents.Type: GrantFiled: October 1, 1993Date of Patent: January 9, 1996Assignee: American Cyanamid CompanyInventors: Joseph W. Epstein, Gary H. Birnberg, Feng L. Qing
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Patent number: 5480871Abstract: Compounds of the formula: ##STR1## are useful for treating conditions modulated by .alpha..sub.1 -adrenergic receptors.Type: GrantFiled: May 12, 1995Date of Patent: January 2, 1996Assignee: Chiron CorporationInventors: David C. Spellmeyer, Walter H. Moos, Eric J. Martin, Ronald N. Zuckermann, Gregory Stauber
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Patent number: 5480908Abstract: 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: GrantFiled: December 13, 1993Date of Patent: January 2, 1996Assignee: American Cyanamid CompanyInventors: Joseph W. Epstein, Gary H. Birnberg, Minu D. Dutia, Thomas H. Claus, Elwood E. Largis
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Patent number: 5475024Abstract: 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: GrantFiled: October 14, 1993Date of Patent: December 12, 1995Assignee: 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
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Patent number: 5447916Abstract: Compounds of the formula: ##STR1## are useful for treating conditions modulated by .alpha..sub.1 -adrenergic receptors.Type: GrantFiled: July 30, 1993Date of Patent: September 5, 1995Assignee: Chiron CorporationInventors: David C. Spellmeyer, Walter H. Moos, Eric J. Martin, Ronald N. Zuckermann, Gregory Stauber
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Patent number: 5428060Abstract: 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: GrantFiled: August 27, 1992Date of Patent: June 27, 1995Assignee: Merck Frosst Canada, Inc.Inventors: Yves Ducharme, John W. Gillard, Rejean Fortin, Daniel Dube, Yves Girard, Pierre Hamel, Daniel Delorme
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Patent number: 5385931Abstract: 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: GrantFiled: December 28, 1990Date of Patent: January 31, 1995Assignee: Pierre Fabre MedicamentInventors: Dennis Bigg, Alain Duflos, Jean-Pierre Rieu
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Patent number: 5378727Abstract: Novel substituted heterocyclic derivatives are provided which inhibit platelet aggregation. This invention also pertains to pharmaceutical compositions and methods of using such derivatives.Type: GrantFiled: July 19, 1993Date of Patent: January 3, 1995Assignee: G. D. Searle & Co.Inventors: Philippe R. Bovy, Joseph G. Rico, Thomas E. Rogers, Foe S. Tjoeng, Jeffery A. Zablocki
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Patent number: 5373020Abstract: 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: GrantFiled: June 3, 1993Date of Patent: December 13, 1994Assignee: American Cyanamid CompanyInventors: Jonathan D. Bloom, Thomas H. Claus, Vern G. DeVries, Jo A. Dolan, Minu D. Dutia
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Patent number: 5326785Abstract: 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: GrantFiled: March 31, 1993Date of Patent: July 5, 1994Assignee: Suntory LimitedInventors: Hidetsura Cho, Mie Tamaoka, Seiitsu Murota, Ikuo Morita
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Patent number: 5308865Abstract: 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: GrantFiled: January 6, 1993Date of Patent: May 3, 1994Assignee: Roussel UclafInventors: Robert R. Bartlett, David P. Kay, Elizabeth A. Kuo, Rudolf Schleyerbach, Wilfried Schwab
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Patent number: 5296507Abstract: 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: GrantFiled: January 6, 1993Date of Patent: March 22, 1994Assignee: H.Lundbeck A/SInventors: Yoshiaki Tanaka, Naomi Kobayashi, Tadashi Kurimoto, Yugo Ikeda
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Patent number: 5274000Abstract: 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: GrantFiled: April 21, 1992Date of Patent: December 28, 1993Assignee: Kotobuki Seiyaku Company LimitedInventors: Tsuyoshi Tomiyama, Akira Tomiyama, Koichi Kubota
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Patent number: 5252601Abstract: The present invention relates to novel 2-mercaptomethylene-tetrahydronaphthalene derivatives which are useful as enkephalinase inhibitors.Type: GrantFiled: April 3, 1992Date of Patent: October 12, 1993Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Gary A. Flynn, Douglas W. Beight
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Patent number: 5250558Abstract: Substituted triazolinone, triazolinethione, and triazolinimine compounds of formula (I) are as neurotensin II antagonists.Type: GrantFiled: January 28, 1992Date of Patent: October 5, 1993Assignee: Merck & Co., Inc.Inventors: Prasun K. Chakravarty, Richard W. Ransom
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Patent number: 5202351Abstract: 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: GrantFiled: January 22, 1991Date of Patent: April 13, 1993Assignee: Mitsubishi Kasei CorporationInventors: Tetsuo Sekiya, Shinya Inoue, Chiaki Hyodo, Hiromi Okushima, Kohei Umezu, Kazuo Suzuki
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Patent number: 5162367Abstract: 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: GrantFiled: October 23, 1989Date of Patent: November 10, 1992Assignee: The Wellcome Foundation LimitedInventors: Robert J. Blade, John E. Robinson
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Patent number: 5106867Abstract: 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: GrantFiled: April 5, 1991Date of Patent: April 21, 1992Assignee: American Cyanamid CompanyInventors: Jonathan D. Bloom, Thomas H. Claus, Vern G. DeVries, Jo A. Dolan, Minu D. Dutia
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Patent number: 5106407Abstract: 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: GrantFiled: December 4, 1989Date of Patent: April 21, 1992Assignee: The Dow Chemical CompanyInventors: Attila G. Relenyi, Gerald F. Koser, Richard W. Walter, Jr., William J. Kruper, Jr., Ravi B. Shankar, Anthony P. Zelinko
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Patent number: 5102906Abstract: 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: GrantFiled: October 31, 1990Date of Patent: April 7, 1992Assignee: Mitsui Toatsu Chemicals, IncorporatedInventors: Shigenobu Nakayama, Fumiaki Ikeda