The Hetero Ring Is Substituted Patents (Class 514/465)
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Publication number: 20020077347Abstract: Compounds of formula (I) 1Type: ApplicationFiled: August 23, 2001Publication date: June 20, 2002Inventors: Gang Liu, Zhonghua Pei
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Patent number: 6407100Abstract: The invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.Type: GrantFiled: September 1, 1993Date of Patent: June 18, 2002Assignee: Bayer AktiengesellschaftInventors: Hans Peter Isenring, Bettina Weiss
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Patent number: 6399628Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: March 12, 1999Date of Patent: June 4, 2002Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: James E. Audia, Beverly K. Folmer, Varghese John, Lee H. Latimer, Jeffrey S. Nissen, Jon K. Reel, Eugene D. Thorsett, Celia A. Whitesitt
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Patent number: 6391916Abstract: Novel C3-substituted cyclodeca-1,5-diynes can be prepared through novel synthetic procedures using starting (E)-C3-substituted-4-(aryl- or heteroarylmethylidene)cyclodeca-1,5-diynes reagents. Both the C3-substituted cyclodeca-1,5-diyn-3-enes and the starting reagents have improved thermal stability compared to unsubstituted counterparts.Type: GrantFiled: July 21, 2000Date of Patent: May 21, 2002Assignee: The Hong Kong University of Science and TechnologyInventors: Wei-Min Dai, Anxin Wu, Yuk Ha Lee, Wataru Hamaguchi, Sei-ichi Nishimoto, Ling Zhou, Atsushi Ishii
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Patent number: 6376513Abstract: The present invention relates to a novel drug method for relieving pain and promoting the removal of calculi in urolithiasis which contains an active ingredient having stimulating effects on both &bgr;2- and &bgr;3-adrenoceptors and exerting a potent relaxing effect on human ureteral smooth muscle.Type: GrantFiled: November 24, 1999Date of Patent: April 23, 2002Assignee: Kissei Pharmaceuticals Co., Ltd.Inventors: Masuo Akahane, Yoshitaka Tomiyama
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Patent number: 6376535Abstract: The present invention relates to oxygen-containing heterocyclic compounds represented by the following formula (I): wherein m represents an integer of 0 to 4; R1, R2, R3 and R4 independently represent a hydrogen atom, substituted or unsubstituted lower alkyl, etc.; R5 represents substituted or unsubstituted lower alkoxy etc.; R6 represents a hydrogen atom etc.; and Y represents the following formula (II): wherein R9 represents cyano etc., R10 represents a hydrogen atom etc., R11 represents carboxy etc., and R12 represents a hydrogen atom etc.; and the like; or pharmaceutically acceptable salts thereof.Type: GrantFiled: March 1, 2001Date of Patent: April 23, 2002Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Ohshima, Koji Yanagawa, Haruhiko Manabe, Ichiro Miki, Yoshiaki Masuda
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Patent number: 6369099Abstract: A method of modifying or altering the structure of a 1&agr;-hydroxylated vitamin D compound to increase its biological activity by altering the conformational equilibrium of the A-ring to favor a chair conformation that presents the 1&agr;-hydroxyl in the axial orientation. This is accomplished by either locking the A-ring chair conformation in a geometry having an axially orientated 1&agr;-hydroxyl, or by the addition of one or more substituents to the A-ring which interact with other substituents in the molecule or on the A-ring to provide a driving force to the A-ring to adopt a chair conformation which presents the 1&agr;-hydroxyl in the axial orientation.Type: GrantFiled: April 20, 2000Date of Patent: April 9, 2002Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Rafal R. Sicinski
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Publication number: 20020037922Abstract: This invention provides O-&agr;-acyloxyalkyl ethers of the venlafaxine metabolite 4-[2-(Dimethylamino-1-(1-hydroxycyclohexyl)ethyl]phenol, represented by Formula (I): 1Type: ApplicationFiled: November 21, 2001Publication date: March 28, 2002Applicant: American Home Products CorporationInventors: John P. Yardley, Magid A. Abou-Gharbia, John W. Ullrich
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Patent number: 6355634Abstract: The invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.Type: GrantFiled: June 7, 1995Date of Patent: March 12, 2002Assignee: Bayer AktiengesellschaftInventors: Hans Peter Isenring, Bettina Weiss
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Patent number: 6353014Abstract: A method of treating glaucoma or ocular hypertension in a patient, which comprises administering to the patient a pharmaceutically effective amount of a compound of formula I:Type: GrantFiled: June 2, 1999Date of Patent: March 5, 2002Assignee: Alcon Laboratories, Inc.Inventors: Verney L. Sallee, Mark R. Hellberg, Peter G. Klimko
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Patent number: 6344570Abstract: Compounds of formula (II) where R1 is in the para or meta position and is (A); R2 and R3 are each independently selected from hydrogen, nitro, C1-6alkyl, C3-6cycloalkyl, C2-6alkenyl, C2-6alkynyl, C1-4alkoxyl, C1-6alkylamino, C1-6dialkylamino, C1-6akylC1-4alkoxyl, C1-6alkylaminoC1-6alkyl, amino, cyano, halogeno, trifluoromethyl, —CO2R12 and —CONR12R13, where R12 and R13 are independently selected from hydrogen or C1-6alkyl, or R2 and R3 together with the phenyl to which they are attached form a 9 or 10 membered bicyclic ring system; R4 is C1-4alkyl; R5 is selected from hydrogen and C1-4alkyl; R6 is selected from C1-6alkyl, C1-4alkyl(C4-6)cycloalkyl, C1-6alkyl(C1-6)alkoxyl, C1-6alkylS(C1-6)alkyl, C1-4alkylsulphonyl(C1-4)alkyl; (B) where q is an integer from 1 to 6 and R14 is halogeno; R7 is selected from C1-6alkyl, C1-8alkoxylcarbonyl, C2-6alkenyl, 1,3-benzodioxol-5-yl and aryl each optionally substituted by one or more substituents selected from C1-4alkoxy, C1-6alkyl, cyano, halogType: GrantFiled: July 11, 2000Date of Patent: February 5, 2002Assignee: AstraZeneca UK LimitedInventors: David R Brittain, Craig Johnstone
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Publication number: 20020013363Abstract: A phytomicrobicidal composition comprising such an amount of at least two active ingredient components that a synergistic effect is achieved, together with a suitable carrier material, wherein component I is a compound of the formula I 1Type: ApplicationFiled: August 13, 2001Publication date: January 31, 2002Inventors: Gertrude Knauf-Beiter, Ronald Zeun
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Publication number: 20020013344Abstract: 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: ApplicationFiled: October 31, 1995Publication date: January 31, 2002Inventors: JOSEPH P. STEINER, GREGORY S. HAMILTON
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Patent number: 6342497Abstract: This invention relates to compounds of the formula and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1 and R2 are as defined herein. The compounds of formula 1 are antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1.Type: GrantFiled: September 7, 1999Date of Patent: January 29, 2002Assignee: Pfizer IncInventor: Robert Gerald Linde, II
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Patent number: 6335358Abstract: Compounds related to lactacystin and lactacystin &bgr;-lactone, pharmaceutical compositions containing the compounds, and methods of use.Type: GrantFiled: April 12, 1995Date of Patent: January 1, 2002Assignee: President and Fellows of Harvard CollegeInventors: Gabriel Fenteany, Timothy F. Jamison, Stuart L. Schreiber, Robert F. Standaert
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Patent number: 6329419Abstract: This invention relates to an insecticidal and miticidal composition which contains as active ingredients chlorfenapyr [4-bromo-2-(chlorophenyl)-1-(ethoxymethyl)-5-(trifluoromethyl)pyrrole-3-carbonitrile] in combination with asynergistic amount of at least one of a carbamate-type insecticidal compound.Type: GrantFiled: June 1, 1999Date of Patent: December 11, 2001Assignee: American Cyanamid Co.Inventor: Toshiki Fukuchi
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Patent number: 6319515Abstract: The present invention relates to an isosorbide dinitrate-containing patch, in which an adhesive layer comprising an adhesive composition is formed on a flexible support, and the adhesive composition consists of an acrylic-based adhesive (A), a polyvinyl acetate-based adhesive (B), a plasticizing component (C) and isosorbide dinitrate (D), and satisfies the following weight ratios (1) through (3) of each of the components: (1) A:B=70:30 to 10:90, (2) the weight ratio of the component C based on the adhesive composition is 10 to 40% by weight, and (3) the weight ratio of the component D based on the adhesive composition is 20 to 35% by weight. Provided is a patch excellent in percutaneous absorption, handleability, resistance to skin irritation, sustained release, adhesivity, etc.Type: GrantFiled: September 8, 1998Date of Patent: November 20, 2001Assignee: Teijin LimitedInventors: Osafumi Hidaka, Satoshi Murakami, Yoshifusa Tachimori, Michisuke Ohe
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Patent number: 6313122Abstract: This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: March 20, 2000Date of Patent: November 6, 2001Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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Patent number: 6310080Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically inhibiting retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: December 1, 1999Date of Patent: October 30, 2001Assignee: G. D. Searle & Co.Inventors: Daniel P Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L. Brown, Joseph J. McDonald
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Patent number: 6288071Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.Type: GrantFiled: December 10, 1998Date of Patent: September 11, 2001Assignee: Bayer AktiengesellschaftInventors: Henry Szczepanski, Martin Zeller, Ottmar Franz Hüter
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Patent number: 6274600Abstract: Compounds are useful for enhancing synaptic responses mediated by AMPA receptors are disclosed, as are methods for the preparation thereof and methods for their use for treatment of subjects suffering from impaired nervous or intellectual functioning due to deficiencies in the number of excitatory synapses or in the number of AMPA receptors. The invention compounds can also be used for the treatment of non-impaired subjects for enhancing performance in sensory-motor and cognitive tasks which depend on brain networks utilizing AMPA receptors and for improving memory encoding.Type: GrantFiled: April 5, 1999Date of Patent: August 14, 2001Assignee: The Regents of the University of CaliforniaInventors: Gary S. Lynch, Gary A. Rogers
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Patent number: 6274604Abstract: A tachykinin antagonist is useful, alone or in conjunction with other agents, for altering circadian rhythmicity and alleviating circadian rhythm disorders and for enhancing and improving the quality of sleep.Type: GrantFiled: May 5, 1999Date of Patent: August 14, 2001Assignee: Merck & Co., Inc.Inventor: Carl Mendel
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Patent number: 6242637Abstract: The invention relates to compounds of the formula in which: A is a divalent radical selected from: A1) —O—CO— A2) —CH2—O—CO— A3) —O—CH2—CO— A4) —O—CH2—CH2— A5) —N(R1)—CO— A6) —N(R1)—CO—CO— A7) —N(R1)—CH2—CH2— A8) —O—CH2— in which: R1 is a hydrogen or a (C1-C4)-alkyl; and Am is a nitrogen-containing heterocycle.Type: GrantFiled: October 20, 1998Date of Patent: June 5, 2001Assignee: Sanofi-SynthelaboInventors: Xavier Emonds-Alt, Isabelle Grossriether, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck
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Patent number: 6242480Abstract: Compounds having ant-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 composition are disclosed.Type: GrantFiled: May 24, 1999Date of Patent: June 5, 2001Assignee: Alcon Laboratories, Inc.Inventors: John M. Yanni, Gustav Graff
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Patent number: 6214870Abstract: The present invention relates to dioxocyclopentyl hydroxamide derivatives of the formula wherein X, Z and Q are as defined in the specification, and to pharmaceutical compositions and methods of treatment thereof.Type: GrantFiled: March 28, 2000Date of Patent: April 10, 2001Assignee: Pfizer IncInventors: Kim F. McClure, Ralph P. Robinson
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Patent number: 6214869Abstract: There is provided a novel series of cis cyclopropane compounds of Formula I wherein R1, R2, R3, R4, X, Y, Z and m are as defined herein which bind to the human melatonin receptor and therefore are useful as melatonergic agents.Type: GrantFiled: May 25, 1999Date of Patent: April 10, 2001Assignee: Bristol-Myers SquibbInventors: Jie Chen, Pierre Dextraze, Marco Dodier, Katherine S. Takaki
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Patent number: 6214859Abstract: Ethylamine derivatives of the formula (I): (wherein R1 is hydrogen, hydroxyl, lower alkoxy or halogen; R2 is alkyl having 2 to 5 carbon atoms; R3 is hydrogen, alkyl having 2 to 5 carbon atoms, alkylcarbonyl having 2 to 5 carbon atoms, aryl having 6 to 10 carbon atoms or arylalkyl having 7 to 11 carbon atoms; the ring is a bicyclic compound which consists of at least one benzene ring and may comprise a saturated or unsaturated five- or six-membered ring which may or may not have heteroatoms, providing that when the ring is indole or 1,3-benzodioxole, R2 and R3 do not constitute, at the same time, two carbon atoms members, and when R3 is hydrogen, the ring is a bicyclic compound which is not indole, benzothiophene or benzodioxole and R2 is alkyl having 3 to 5 carbon atoms and pharmaceutically acceptable acid addition salts thereof. These compounds are promising as psychotropic drugs, antidepressants, drugs for Parkinson's disease and/or drugs for Alzeimer's disease.Type: GrantFiled: July 12, 1999Date of Patent: April 10, 2001Assignee: Fujimoto Brothers Co., Ltd.Inventors: Fumio Yoneda, Joseph Knoll, Hironori Ode, Masatoshi Sakae, Masanori Katurada, Toshiaki Moto, Takashi Ando, Seiichiro Shimazu, Kazue Takahata, Michitaro Fujimoto
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Patent number: 6211228Abstract: Novel compounds, compositions and methods effective for the prevention and treatment of mast-cell mediated inflammatory disorders are described. The compounds, compositions and methods are effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis, as well as other types of immunomediated inflammatory disorders, such as rheumatoid arthritis, conjunctivitis and inflammatory bowel disease, various dermatological conditions, as well as certain viral conditions. The compounds comprise potent and selective inhibitors of the mast cell protease tryptase. The compositions for treating these conditions include oral, inhalant, topical and parenteral preparations as well as devices comprising such preparations.Type: GrantFiled: March 29, 1999Date of Patent: April 3, 2001Assignee: Axys Pharmaceuticals, IncInventors: Ken Duane Rice, Jeffrey Mark Dener, Anthony Robert Gangloff, Elaine Yee-Lin Kuo
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Patent number: 6187799Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.Type: GrantFiled: May 22, 1998Date of Patent: February 13, 2001Assignees: Onyx Pharmaceuticals, Bayer CorporationInventors: Jill E Wood, Hanno Wild, Daniel H Rogers, John Lyons, Michael Katz, Yolanda Caringal, Robert Dally, Wendy Lee, Roger A. Smith, Cheri Blum
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Patent number: 6162810Abstract: A new family of inadone and tetralone tubulin-binding compounds (TBs) is disclosed. Unlike classical TBs, which inhibit mitosis among affected dividing cells, the TBs of the invention possess two unique properties: (1) they induce apoptosis among stationary phase (non-dividing) malignant cells, yet do not impair the viability of normal nonproliferating cells; and, (2) they affect cells which have acquired MDR more powerfully than they affect cells without MDR. Thus, the TBs of the invention provide means to target malignant cells for chemotherapy, even after previous therapies have failed, without affecting normal cells and tissues in the host.Type: GrantFiled: September 4, 1998Date of Patent: December 19, 2000Assignee: The Regents of the University of CaliforniaInventors: Dennis A. Carson, Hsien C. Shih, Howard B. Cottam, Lorenzo Leoni
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Patent number: 6150404Abstract: The phenoxybenzyl moiety of conventional pyrethroids is a major site of oxidative metabolism in resistant tobacco budworms, Heliothis virescens (F.). This group was replaced with several P450 monooxygenase-inhibiting or oxidatively blocked groups. Several isomers were tested as insecticides or synergists for insecticides against tobacco budworms that were insecticide-susceptible or that expressed metabolic resistance to cypermethrin. Several compounds with insecticidal and synergistic activities were found. Activity was dependent on both geometric and stereochemical configurations. These compounds may be used in diagnosing the mechanism of resistance in field strains with acquired resistance to pyrethroids. Knowledge of the mechanism underlying acquired insecticide resistance helps farmers to control emerging resistant strains.Type: GrantFiled: December 16, 1998Date of Patent: November 21, 2000Assignee: Board of Supervisors of Louisiana State University and Agricultural and Mechanical CollegeInventors: James A. Ottea, Guomin Shan
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Patent number: 6133263Abstract: Novel nonpeptide endothelin antagonists with ether-linked groups are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating atherosclerosis, restenosis, Raynaud's phenomenon, mild or severe congestive heart failure, cerebral ischemia, cerebral infarction, embolic stroke, cerebral vasospasm, subarachnoid hemorrhage, hemorrhagic stroke, diabetes, gastric ulceration and mucosal damage, ischemnic bowel disease, Chrohn's disease, essential or malignant hypertension, pulmonary hypertension, pulmonary hypertension after bypass, acute respiratory distress syndrome, chronic obstructive pulmonary diseases, male penile erectile dysfunction, cancer, especially malignant hemangicendothelioma or prostate cancer, myocardial infarction or ischemia, acute or chronic renal failure, renal ischemia, radiocontrast-induced nepbrotoxicity, endotoxic, septic, hemorrhagic shock, angina, preeclampsia, asthma, arhythmias, benign prostatic hyperplasia, and elevated levType: GrantFiled: August 3, 1998Date of Patent: October 17, 2000Assignee: Warner-Lambert CompanyInventors: Xue-Min Cheng, Annette Marian Doherty, William Chester Patt, Joseph Thomas Repine
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Patent number: 6103708Abstract: This invention provides compounds of Formula I having the structure: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, W, X, Y, and Z are as defined in the specification, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.Type: GrantFiled: May 10, 1999Date of Patent: August 15, 2000Assignee: American Home Products CorporationInventors: Paul J. Dollings, Robert E. McDevitt, Folake O. Adebayo
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Patent number: 6087389Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: June 18, 1998Date of Patent: July 11, 2000Assignee: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
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Patent number: 6066649Abstract: The invention relates to a drug, which contains one or more inhibitors for the cGMP-stimulated phosphodiesterase (PDE II) together with conventional substrates and/or diluents. Preferably the drug contains erythro-9-(2-hydroxy-3-nonyl)-adenine or 2-o-propoxyphenyl-8-azapurine-6-one, optionally together with one or more activators of guanyl cyclase. The invention also relates to the application of inhibitors of cGMP-stimulated phosphodiesterase (PDE II) for the control and prophylaxis of cardiovascular diseases and for the manufacture of drugs for cardiovascular diseases. Preferably erythro-9-(2-hydroxy-3-nonyl)-adenine or 2-o-propoxyphenyl-8-azapurine-6-one is used, optionally together with one or more activators of guanyl cyclase.Type: GrantFiled: February 28, 1995Date of Patent: May 23, 2000Assignee: Thomas PodzuweitInventor: Thomas Podzuweit
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Patent number: 6040339Abstract: 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 or various other organic groups; R.sup.3 is alkyl; R.sup.4 is a group of formula (II), (III), (IV), (V), (VI), (VII), (VIII) or (IX): ##STR2## wherein: A.sup.1 is a single bond, alkylene or alkenylene; A.sup.2 is or alkenylene; A.sup.3 is a single bond, alkyleneor alkenylene; R.sup.5a and R.sup.5b are the same or different and each is hydrogen, alkyl or various other groups; R.sup.6 is alkyl or phenyl; R.sup.7 is hydrogen or alkyl; R.sup.8 is alkyl or various other groups; and n is 0 and pharmaceutically acceptable salts thereof have valuable inhibitory activity against acyl-CoA: cholesterol acyl transferase.Type: GrantFiled: May 28, 1998Date of Patent: March 21, 2000Assignee: 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: 6037365Abstract: This invention provides a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutical compositions of such compounds and a method of treatment to inhibit aggregation of platelets.Type: GrantFiled: September 25, 1998Date of Patent: March 14, 2000Assignee: G.D. Searle & Co.Inventors: Philippe Roger Bovy, Joseph Gerace Rico, Thomas Edward Rogers
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Patent number: 6037370Abstract: 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: March 14, 2000Assignee: Vertex Pharmaceuticals IncorporatedInventor: David M. Armistead
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Patent number: 6034105Abstract: A tachykinin antagonist is useful, alone or in conjunction with other agents, for altering circadian rhythmicity and alleviating circadian rhythm disorders and for enhancing and improving the quality of sleep.Type: GrantFiled: December 18, 1998Date of Patent: March 7, 2000Assignee: Merck & Co., Inc.Inventor: Carl M. Mendel
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Patent number: 6017956Abstract: 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 25, 1998Date of Patent: January 25, 2000Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshikazu Iwasawa, Tetsuya Aoyama, Kumiko Kawakami, Sachie Arai, Toshihiko Satoh, Yoshiaki Monden
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Patent number: 6017952Abstract: This invention relates to derivatives of furan and thiophene, their composition, process of making and method of use as endothelin receptor antagonists.Type: GrantFiled: February 2, 1998Date of Patent: January 25, 2000Assignee: SmithKline Beecham CorporationInventors: John Duncan Elliott, Aiming Gao, Jia-Ning Xiang
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Patent number: 6017916Abstract: 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: January 22, 1997Date of Patent: January 25, 2000Assignee: 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: 6013244Abstract: Compounds of the pregnane series are described having general formula (I) or their solvates in which R.sub.1 individually represents --OC(.dbd.O)C.sub.1-6 alkyl; R.sub.2 individually represents hydrogen, methyl (which may be in the .alpha. or .beta. configuration) or methylene; or R.sub.1 and R.sub.2 together represent formula (a) where R.sub.5 and R.sub.6 are the same or different and each represents hydrogen or C.sub.1-6 alkyl; R.sub.3 and R.sub.4 are the same or different and each represents hydrogen or halogen; and represents a single or a double bond. Compounds of formula (I) and their solvates are useful as anti-inflammatory or anti-allergic agents.Type: GrantFiled: June 24, 1998Date of Patent: January 11, 2000Assignee: Glaxo Wellcome Inc.Inventors: Keith Biggadike, Rosanne Mary Farrell
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Patent number: 5998408Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.Type: GrantFiled: October 8, 1997Date of Patent: December 7, 1999Assignee: Merck & Co., Inc.Inventors: Robert K. Baker, Frank Kayser, Jianming Bao, Andrew Kotliar, William H. Parsons, Kathleen M. Rupprecht
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Patent number: 5968921Abstract: FK506 and geldanamycin promote nerve regeneration by a common mechanism that involves the binding of these compounds to polypeptide components of steroid receptor complexes other than the steroid hormone binding portion of the complex (FKBP52 and hsp90, respectively). These and other agents cause hsp90 dissociation from steroid receptor complexes or block association of hsp90 with steroid receptor complexes.Type: GrantFiled: October 24, 1997Date of Patent: October 19, 1999Assignee: Orgegon Health Sciences UniversityInventor: Bruce G. Gold
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Patent number: 5955491Abstract: The present invention provides a cathepsin L inhibitor containing a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an arylalkyl, heterocyclic-alkyl or lower alkyl group which may be substituted; R.sup.2 and R.sup.3 independently are a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.4 is an alkanoyl, sulfonyl, carbonyloxy, carbamoyl or thiocarbamoyl group which may be substituted; X is formula: --CHO or --CH.sub.2 OB (wherein B is a hydrogen atom or a protecting group of hydroxyl group); m and n independently are an integer of 0 or 1; provided that R.sup.4 is an alkanoyl group substituted by aryl, a sulfonyl group substituted by aryl having more than 9 carbon atoms or by lower alkyl, or a carbamoyl or thiocarbamoyl group which may be substituted when R.sup.1 is an unsubstituted lower alkyl, arylalkyl on methylthioethyl group, R.sup.2 and R.sup.3 independently are a lower alkyl or arylalkyl, X is --CHO, m is 1 and n is 0 or 1, or a salt thereof.Type: GrantFiled: June 27, 1995Date of Patent: September 21, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Yukio Fujisawa, Tsuneo Yasuma, Junji Mizoguchi, Masakuni Kori, Masayuki Takizawa
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Patent number: 5952386Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.Type: GrantFiled: September 24, 1997Date of Patent: September 14, 1999Assignee: Sumitomo Chemical Company, LimitedInventors: Sanshiro Matsuo, Taro Hirose, Keiichi Izumi, Masaya Suzuki, Noriyasu Sakamoto, Kazunori Tsushima, Shigeru Saito, Hirotaka Takano
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Patent number: 5925673Abstract: Methods for treating inflammnatory pathologies are disclosed. Particularly, the methods utilize pharmaceutical compositions containing certain compounds having an anti-inflanumatory and anti-oxidant moiety covalently linked by thiol or sulfoxide or sulfone bond. The compounds are useflil in preventing and treating inflammatory disorders through several mechanisms.Type: GrantFiled: December 19, 1997Date of Patent: July 20, 1999Assignee: Alcon Laboratories, Inc.Inventors: Mark R. Hellberg, Abdelmoula Namil, Jon C. Nixon
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Patent number: 5919786Abstract: 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 25, 1998Date of Patent: July 6, 1999Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshikazu Iwasawa, Tetsuya Aoyama, Kumiko Kawakami, Sachie Arai, Toshihiko Satoh, Yoshiaki Monden
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Patent number: 5914339Abstract: The present invention provides new compounds having anti-diabetic and/or antihyperglycemia and/or anti-obesity activity, as well as pharmaceutical compositions and methods of treatment utilizing the compounds and processes for making the compounds, the compounds having the formula (II): ##STR1## wherein: R.sub.1 and R.sub.6 are independently hydrogen, C.sub.1 to C.sub.6 alkyl, trifluoromethyl, cyano, C.sub.1 to C.sub.6 alkoxy, or halogen;R.sub.2 is hydrogen or C.sub.1 to C.sub.6 trialkylsilyl;R.sub.3 is hydrogen or C.sub.1 to C.sub.6 alkoxycarbonyl;or R.sub.2 and R.sub.3 are joined to form a ring: ##STR2## wherein R' is hydrogen, C.sub.1 to C.sub.6 alkyl, or aryl; R.sub.4 and R.sub.5 are independently hydrogen or C.sub.1 to C.sub.6 alkyl;R.sub.7 and R.sub.8 are independently OR.sub.9 or NR.sub.10 R.sub.11 ;R.sub.9 is hydrogen, C.sub.1 to C.sub.12 alkyl, C.sub.1 to C.sub.12 cycloalkyl, C.sub.1 to C.sub.12 silylalkyl, aryl, arylalkyl, alkoxyalkyl, heteroaryl, --CHR.sub.12 COOR.sub.13, --CHR.sub.12 C(O)R.sub.Type: GrantFiled: May 9, 1997Date of Patent: June 22, 1999Assignee: American Home Products CorporationInventors: Fuk-Wah Sum, Adam M. Gilbert, George T. Grosu, Michael S. Malamas, Aranapakam M. Venkatesan, Gerardo D. Francisco