Nitrogen Attached Directly Or Indirectly To The Bicyclo Ring System By Nonionic Bonding Patents (Class 549/55)
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Publication number: 20030171413Abstract: Compounds of formula (1) are described, wherein q is zero or the integer 1, 2 or 3; R which when present may be attached to any available carbon or nitrogen atom of the bicyclic heteroaromatic ring of formula (1) is an atom or group -L3(Alk3)wL4(R8)u; X is an O atom or a S(O)m atom or group in which m is zero or the integer 1 or 2 or an NR group; Y is a N atom or a CR1a group in which R1a is a group R or a group R1; R1 which may he on any available carbon atom of the bicyclic heteroaromatic ring of formula (1) is a hydrogen atom or a group -Alk1L1CyAlk2L2D; provided that at least one but not both of R1 and R1a is the group -Alk1L1CyAlk2L2D. The compounds are potent inhibitors of the interaction between CCR-3 and it chemokine ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders in which inhibition of this interaction can have a beneficial effect.Type: ApplicationFiled: April 10, 2003Publication date: September 11, 2003Inventors: David Alan Owen, Alan Findlay Haughan, Duncan Batty, Alistair George Draffan, Hannah Jayne Kendall, Sarah Louise Mellor
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Publication number: 20030158194Abstract: The subject invention pertains to novel compounds (and salts thereof), and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns methods of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. This results in an improved safety profile. The new compounds have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The compounds also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.Type: ApplicationFiled: December 10, 2002Publication date: August 21, 2003Inventor: Pascal Druzgala
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Publication number: 20030153604Abstract: This invention is directed to an (aminoiminomethyl or aminomethyl)benzoheteroaryl compound of formula I which is useful for inhibiting the activity of Factor Xa by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.Type: ApplicationFiled: February 24, 2003Publication date: August 14, 2003Applicant: Aventis Pharmaceuticals Inc.Inventors: William P. Dankulich, Daniel G. McGarry, Christopher Burns, Timothy F. Gallagher, Francis A. Volz
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Publication number: 20030149030Abstract: A compound of the formula 1Type: ApplicationFiled: December 10, 2002Publication date: August 7, 2003Inventors: Alexander Alanine, Alexander Flohr
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Publication number: 20030139457Abstract: The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a hedgehog agonist, such as the compounds depicted in FIGS. 32 and 33. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal ptc pathway or agonizing smoothened or hedgehog activity.Type: ApplicationFiled: September 17, 2002Publication date: July 24, 2003Applicant: Curis, Inc.Inventors: Anthony David Baxter, Edward Andrew Boyd, Maria Frank-Kamenetsky, Oivin Guicherit, Jeffery Porter, Stephen Price, Lee Rubin, John Harry Alexander Stibbard
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Patent number: 6566373Abstract: The invention relates to 3-hydroxy-and 3-keto-cyclohetero-substituted leucine compounds that are inhibitors of cysteine proteases, particularly cathepsin K, and are useful in the treatment of diseases in which inhibition of bone loss is a factor. The 3-hydroxy-or 3-keto-moiety is bonded to a tetrahydrothiophene, tetrahydrothiopyran, tetrahydrofuran or tetrahydropyran ring.Type: GrantFiled: July 30, 2001Date of Patent: May 20, 2003Assignees: SmithKline Beecham Corporation, SmithKline Beecham p.l.c.Inventors: Andrew D Gribble, Ashley Edward Fenwick, Robert W Marquis, Daniel F Veber, Jason Witherington
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Publication number: 20030083359Abstract: Compounds of formula (I) 1Type: ApplicationFiled: May 10, 2002Publication date: May 1, 2003Inventors: Chih-Hung Lee, Richard J. Perner, Daniel P. Larson, John R. Koenig, Arthur R. Gomtsyan, Guo Zhu Zheng, Stanley DiDomenico, Andrew O. Stewart, Erol K. Bayburt
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Publication number: 20030078422Abstract: Process for the preparation of benzo-fused heterocycles of general formula I: 1Type: ApplicationFiled: October 9, 2002Publication date: April 24, 2003Inventors: Frank-Hardi Wartenberg, Thomas Koppe, Walter Wetzel, Markus Wydra, Achim Benz
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Publication number: 20030069233Abstract: Novel sulphonamide derivatives having CNS activity, processes for their preparation and their use as medicaments.Type: ApplicationFiled: May 29, 2002Publication date: April 10, 2003Applicant: SmithKline Beecham p.l.c.Inventors: Steven Mark Bromidge, Francis David King, Paul Adrian Wyman
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Publication number: 20030045569Abstract: This invention relates to a series of difluoromethylene aromatic ethers of the formula 1Type: ApplicationFiled: August 15, 2002Publication date: March 6, 2003Applicant: Pfizer Inc.Inventor: John Adams Lowe
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Patent number: 6514967Abstract: The invention relates to compounds of the following general formula (I): in which: R1 and R2 represent a hydrogen atom, or form a ring, especially a benzene ring, R3 represents a hydrogen atom or an alkyl group, especially a methyl group, X and Y, independently of one another, represent a carbon atom, or a heteroatom such as a sulphur atom S, or a group with the formula (a) in which R4 and R5 represent a hydrogen atom or a methyl group, or R4 and R5 form a heterocycle, and their use for the preparation of a drug intended for the treatment of pathologies associated with abnormally high concentrations of extracellular glutamate.Type: GrantFiled: December 16, 1999Date of Patent: February 4, 2003Assignee: Centre National de la Recherche ScientifiqueInventors: Jean-Marc Kamenka, Isoline Caubere, Gerard Barbanel
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Publication number: 20030018062Abstract: The present invention provides hydroxamate compounds which are deacetylase inhibitors. The compounds are suitable for pharmaceutical compositions having anti-proliferative properties.Type: ApplicationFiled: August 31, 2001Publication date: January 23, 2003Inventors: Stacy W. Remiszewski, Kenneth W. Bair, Richard W. Versace, Lawrence B. Perez, Michael A. Green, Lidia C. Sambucetti, Sushil Sharma
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Publication number: 20020156281Abstract: The present invention provides compounds having the Formula I 1Type: ApplicationFiled: December 12, 2001Publication date: October 24, 2002Inventors: Richard John Booth, Helen Tsenwhei Lee, Jason Keith Pontrello, Randy Ranjee Ramharack, Bruce David Roth
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Patent number: 6433005Abstract: This invention relates to compounds, which are generally anti-inflammatory and analgesic compounds, and which are represented by Formula I: wherein A is a —CH2—, —C(O)—, —O—, —S—, —S(O)—, or —S(O)2— and the other substituents are as defined in the specification; or prodrugs, individual isomers, mixtures of isomers, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.Type: GrantFiled: December 3, 2001Date of Patent: August 13, 2002Assignee: Syntex (U.S.A.) LLCInventors: Kevin L. McLaren, David Bernard Smith, Jahari Laurant Tracy
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Patent number: 6423717Abstract: Novel sulphonamide derivatives having CNS activity, processes for their preparation and their use as medicaments are disclosed.Type: GrantFiled: August 21, 2000Date of Patent: July 23, 2002Assignee: SmithKline Beecham p.l.c.Inventors: Steven Mark Bromidge, Francis David King, Paul Adrian Wyman
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Patent number: 6399788Abstract: A process for preparing a compound having PGD2 antagonism represented by the formula (I), or a pharmaceutically acceptable salt or hydrate thereof, which process comprises reacting an amino alcohol of the formula (II) or its salt with a compound of the formula (III) or its reactive derivative, oxidizing the product with halo oxoacid in the presence of 2,2,6,6-tetramethylpiperidine-1-oxyls, reacting the product with an ylide under the conditions for Wittig reaction, and optionally deprotecting the product.Type: GrantFiled: September 29, 2000Date of Patent: June 4, 2002Assignee: Shionogi & Co., Ltd.Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu, Tetsuo Okada, Makoto Kakinuma
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Patent number: 6316487Abstract: The subject invention pertains to novel compounds, and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns a method of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. The new compounds can have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The product can also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.Type: GrantFiled: October 6, 2000Date of Patent: November 13, 2001Assignee: Aryx TherapeuticsInventors: Pascal Druzgala, Peter G. Milner
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Patent number: 6310074Abstract: The invention relates to compound of formula (I): A—G1—Cy—G2—Cy′—G3—B (I) wherein: A represents a grouping NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3, B represents a grouping NR1C(Q)R2, NR1C(Q)NR2R3, C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3, G1 and G3 represent an optionally substituted alkylene chain, Cy and Cy′, which are different, represent a ring structure or G2 represents a chain and medicinal products containing the same are useful in treating or in preventing melatoninergic disorders.Type: GrantFiled: May 18, 2000Date of Patent: October 30, 2001Assignee: Adir et CompagnieInventors: Patrick Depreux, Said Yous, Gwenael Cheve, Gérald Guillaumet, Marie-Claude Viaud, Carlos Larraya, Caroline Bennejean, Philippe Delagrange, Pierre Renard, Carole Descamps-Francois
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Patent number: 6291513Abstract: The fungicidal compound 4,5-dimethyl-N-2-propenyl-2-(trimethylsilyl)-3-thiophenecarboxamide (Formula (I)) has shown superior and unexpected control of the growth of the soil-borne fungus Gaeumannomyces graminis (Gg). The present invention provides a novel compound for synthesizing the compound of Formula (I) which uses the compound 4-hydroxy-4,5-dimethyl-2-trimethylsilanyl-dihydrothiophene-3-carboxylic acid allylamide (Formula (II)) as well as novel compounds of synthesizing the allylamide. In addition, Formula (II) itself has unexpectedly been found to provide control of Gg.Type: GrantFiled: July 5, 2000Date of Patent: September 18, 2001Assignee: Monsanto companyInventors: Wendell G. Phillips, Michael K. Mao, Chun Ma, Thomas L. Fevig
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Patent number: 6288107Abstract: Novel sulfatase inhibitor/estrogen receptor blocker compounds useful in the treatment of estrogen dependent illnesses are disclosed. The compounds generally comprise a sulfamate moiety and an aromatic, estrogen receptor blocker moiety. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of an estrogen-dependent disease are also disclosed.Type: GrantFiled: March 24, 2000Date of Patent: September 11, 2001Assignee: Duquesne University of the Holy GhostInventors: Pui-Kai Li, Kyle W. Selcer
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Patent number: 6281240Abstract: This invention provides methods of treating secretory diarrhea or cystic fibrosis in a mammal which comprises administering to a mammal in need thereof an effective amount of diarylsulfonylurea. This invention also describes specific diarylsulfonylureas for use in treating secretory diarrhea or cystic fibrosis.Type: GrantFiled: January 31, 2000Date of Patent: August 28, 2001Assignee: Eli Lilly and CompanyInventor: Bruce D Schultz
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Patent number: 6265428Abstract: Methods, compositions, and compounds for modulating the activity of an endothelin peptide are provided. The methods use compositions that contain compounds of formula (1): where X and Y are selected from groups that include O, S, and NH; and Ar1, Ar2 and Ar3 are independently selected from substituted or unsubstituted groups that include 5 to 6 membered aryl groups and heteroaryl groups that contain one or two heteroatom(s). The methods are effected by contacting endothelin receptors with one or more of the compounds or with compositions containing one or more of the compounds prior to, simultaneously with, or subsequent to contacting the receptors with an endothelin peptide.Type: GrantFiled: June 8, 1999Date of Patent: July 24, 2001Assignee: Texas Biotechnology CorporationInventors: Ming Fai Chan, Vitukudi Narayanaiyengar Balaji, Rosario Silvestre Castillo, Adam Kois, Bore Gowda Raju, Chengde Wu
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Patent number: 6235768Abstract: Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof.Type: GrantFiled: May 10, 1999Date of Patent: May 22, 2001Assignee: Shionogi & Co., Ltd.Inventors: Fumihiko Wantanabe, Hiroshige Tsuzuki, Mitsuaki Ohtani
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Patent number: 6225336Abstract: This invention provides novel compounds which are dual antagonistic to TXA2 and PGD2 receptors and the pharmaceutical compositions containing them. They are useful for treating, for example, systemic mastocytosis and disorder of systemic mast cell activation as well as tracheal contraction, asthma, allergic rhinitis, allergic conjunctivitis, urticaria, ischemic reperfusion injury, and inflammation. In detail, this invention provides a compound of the foumula (I): pharmaceutically acceptable salt thereof, or hydrate thereof.Type: GrantFiled: February 14, 2000Date of Patent: May 1, 2001Assignee: Shionogi & Co., Ltd.Inventor: Tsunetoshi Honma
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Patent number: 6217642Abstract: A method and composition for protection against fouling of objects which come into contact with sea water or brackish water comprising a benzothiophene-2-carbomide S,S-dioxide as the essential component are described.Type: GrantFiled: March 11, 1998Date of Patent: April 17, 2001Assignee: Bayer AktiengesellschaftInventors: Franz Kunisch, Martin Kugler, Heinrich Schrage, Hans-Ludwig Elbe
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Patent number: 6204380Abstract: Carboxylic acid ester derivatives of formula (1): wherein R is C1-C6 alkyl, R2 and R3 are independently hydrogen or C1-C3 alkyl, and Q is optionally substituted phenyl, can be easily converted by ring closing into pyridazin-3-one derivatives of formula (7): The carboxylic acids of formula (1) can be produced by reacting hydrazone compounds of formula (5): wherein R3 and Q are as defined above, with malonic acid monoester derivatives of formula (6): wherein R and R2 are as defined above, in the presence of a base.Type: GrantFiled: April 21, 1999Date of Patent: March 20, 2001Assignee: Sumitomo Chemical Company, LimitedInventor: Takashi Furukawa
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Patent number: 6130240Abstract: Described is a novel compound and method, useful for treatment of cardiac arrhythmias, especially useful in patients with congestive heart failure (CHF). A process for synthesizing the novel compound is also described.Type: GrantFiled: December 14, 1998Date of Patent: October 10, 2000Assignee: Aryx Therapeutics, Inc.Inventor: Pascal Druzgala
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Patent number: 6100292Abstract: This invention relates to ketones represented by the following formula ##STR1## and to drugs in which such a ketone or pharmacologically acceptable salt thereof is an effective component.The ketones of the present invention encourage the production of platelets, red blood cells, white blood cells and the like, and can be used to prevent or treat cytopaenia brought about by cancer chemotherapy, radiotherapy, bone marrow transplantation and drug therapy, or by immunological abnormality or anaemia, and the like.Type: GrantFiled: May 25, 1999Date of Patent: August 8, 2000Assignee: Toray Industries, Inc.Inventors: Tsuyoshi Matsumoto, Hideki Kawai, Kiyoshi Okano, Katsuyuki Mori, Yasumoto Adachi
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Patent number: 6075151Abstract: The invention provides benzothiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions, including hyperlipidemia, and other cardiovascular pathologies.Type: GrantFiled: August 24, 1998Date of Patent: June 13, 2000Assignee: Eli Lilly and CompanyInventors: Kenneth Lee Hauser, Alan David Palkowitz, Kenneth Jeff Thrasher
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Patent number: 6048875Abstract: A compound of formula (I): ##STR1## wherein: X represents oxygen, sulphur, or NR.sub.3 wherein R.sub.3 is as defined in the description,Y represents oxygen, sulphur, NR.sub.3, or may a single bond when X represents NR.sub.3,Z represents nitrogen, carbon, or CH,A represents a single bond, alkylene (optionally substituted), arylene, cycloalkylene, heterocycle, or --SO.sub.2 --R.sub.4 -- wherein R.sub.4 is as defined in the description,W represents hydroxy, alkoxy, aryloxy, arylalkoxy, cycloalkyloxy, heterocycle bonded to oxygen, amino, or hydroxyamino,Ra, Rb, Rc, Rd, which may be the same or different, each independently of the others are as defined in the description,R.sub.1 represents aryl substituted by one to five identical or different substituents, each independently of the others,R.sub.Type: GrantFiled: April 26, 1999Date of Patent: April 11, 2000Assignee: Adir et CompagnieInventors: Guillaume De Manteuil, Christine Lila, Tony Verbeuren, Alain Rupin
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Patent number: 6011045Abstract: The present invention relates to compounds of the formula IA--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: December 22, 1997Date of Patent: January 4, 2000Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Jochen Knolle, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
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Patent number: 5990145Abstract: The present invention relates to compounds of the formula I,A--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: December 22, 1997Date of Patent: November 23, 1999Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Karlheinz Scheunemann, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
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Patent number: 5989451Abstract: This invention provides chiral thioindigo compounds for doping smectic liquid crystal hosts, wherein the compounds modulate a chiral bulk property of an induced chiral smectic liquid crystal phase upon irradiation at a wavelength in the visible range. Modulation of the chiral bulk property is effected by reversible trans-cis photoisomerization of the compound upon irradiation. The compounds maintain their rod-like shape in both isomeric forms, and hence do not destabilize the chiral smectic liquid crystal phase. Compounds according to the invention are useful in optical devices such as optical switches, displays, and memory.Type: GrantFiled: February 6, 1998Date of Patent: November 23, 1999Assignee: Queen's University at KingstonInventors: Robert P. Lemieux, Liviu Dinescu
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Patent number: 5942546Abstract: A compound of the formula: ##STR1## wherein X is arylene, heteroarylene, fused arylene, fused heteroarylene, or deleted; Y is sulfonyl, --O--, or deleted; R.sub.1 is aryl, heteroaryl, fused aryl, or fused heteroaryl; R.sub.2 is H, lower alkyl, lower alkoxy, halo, nitro, cyano, haloalkyl, hydroxyl, carboxyl, amido, amino, or aminoalkyl; or a salt thereof are disclosed. Also disclosed are a pharmaceutical composition which contains an excipient and an effective amount of a compound of the above formula and a method of treating cancer which involves the administration of an effective amount of such a compound to a patient in need thereof.Type: GrantFiled: November 20, 1997Date of Patent: August 24, 1999Assignee: Development Center for BiotechnologyInventors: Ji-Wang Chern, Yu-Ling Leu, Shan-Shue Wang, Chin-Fen Lee, Shih-Chung Hsu
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Patent number: 5863936Abstract: Methods and compositions for treating cancer and other diseases in which inhibition of telomerase activity can ameliorate disease symptoms or prevent or treat the disease relate to compounds characterized by the following structure: ##STR1## and their pharmaceutically acceptable salts. Y is selected from the group consisting of oxygen, sulfur, sulfonyl, sulfinyl, and --NR.sub.7 --. R.sub.1 is --TR.sub.8, where T is --C(X.sub.1)-- or --SO.sub.2 --, and R.sub.8 is selected from the group consisting of --OR.sub.9, --NHNHSO.sub.2 R.sub.9, --NHNHC(X.sub.2)OR.sub.9, --NR.sub.9 R.sub.10, --NHNHC(X.sub.2)NR.sub.9 R.sub.10, --NHCR.sub.9 R.sub.10 C(X.sub.2)NR.sub.11 R.sub.12, --NHC(X.sub.2)NR.sub.9 R.sub.10, and the piperazinyl moiety shown below: ##STR2## where n is 0 or 1, and Q.sub.n, for n=1, is --SO.sub.2 --, --C(X.sub.2)-- or --C(X.sub.2)NR.sub.10 --. R.sub.2 -R.sub.Type: GrantFiled: October 27, 1995Date of Patent: January 26, 1999Assignee: Geron CorporationInventors: Federico C.A. Gaeta, Adam A. Galan, Elaine C. Stracker
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Patent number: 5843997Abstract: The present invention provides novel compounds that affect excitatory amino acid receptors and are useful in the treatment of neurological disorders. This invention also provides synthetic methods for the preparation of the novel compounds.Type: GrantFiled: April 2, 1996Date of Patent: December 1, 1998Assignee: Eli Lilly and CompanyInventors: Lawrence J. Heinz, William H.W. Lunn, Darryle Darwin Schoepp
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Process for preparing benzoic acid derivative intermediates and benzothiophene pharmaceutical agents
Patent number: 5750688Abstract: Novel processes are provided for producing compounds of formula II ##STR1## wherein R.sup.1 and R.sup.2 each are independently C.sub.1 -C.sub.4 alkyl, or combine to form piperidinyl, pyrrolidinyl, methylpyrrolidinyl, dimethylpyrrolidinyl, morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino;R.sup.3 and R.sup.4 each are H or a hydroxy protecting group; andn is 2 or 3;or a pharmaceutically acceptable salt thereof by reacting a haloalkylamine with a phenolic ester in the presence of an alkylacetate solvent and a base.Type: GrantFiled: April 9, 1996Date of Patent: May 12, 1998Assignee: Eli Lilly and CompanyInventors: Douglas P. Kjell, Fred M. Perry -
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: 5684033Abstract: This invention provides a novel series of non-peptidyl compounds which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these novel compounds.Type: GrantFiled: June 5, 1995Date of Patent: November 4, 1997Assignee: Eli Lilly and CompanyInventors: Sung Y. Cho, Thomas A. Crowell, Bruce D. Gitter, Philip A. Hipskind, J. Jeffry Howbert, Joseph H. Krushinski, Jr., Karen L. Lobb, Brian S. Muehl, James A. Nixon
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Patent number: 5663375Abstract: Pharmaceutical compounds of the formula ##STR1## in which n is 0, 1 or 2 and R.sup.1 is attached at any of the positions 7, 8, 9 or 10, and each R.sup.1 is halo, carboxy, trifluoromethyl, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, hydroxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkoxy, nitrogen-containing heterocyclyl, nitro, trifluoromethoxy, --COOR.sup.5 where R.sup.5 is an ester group, --COR.sup.6, --CONR.sup.6 R.sup.7 or --NR.sup.6 R.sup.7 where R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl;R.sup.2 is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R.sup.2 is furanyl optionally substituted with C.sub.1-4 alkyl;R.sup.3 is nitrile, carboxy, --COOR.sup.8 where R.sup.8 is an ester group, or --CONR.sup.9 R.sup.10 where R.sup.9 and R.sup.10 are each hydrogen or C.sub.1-4 alkyl; andR.sup.4 is --NR.sup.11 R.sup.12, --NR.sup.11 COR.sup.Type: GrantFiled: August 22, 1994Date of Patent: September 2, 1997Assignees: Eli Lilly and Company, Lilly Industries LimitedInventors: Michael Brunavs, Colin Peter Dell, Peter Thaddeus Gallagher, William Martin Owton, Colin William Smith
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Patent number: 5635527Abstract: A novel carboxylic acid compound having a condensed ring, which is represented by the formula (I) ##STR1## wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition thereof and pharmaceutical use thereof. The novel carboxylic acid compound having a condensed ring and pharmacologically acceptable salt thereof of the present invention have superior GPIIb/IIIa antagonism in mammals inclusive of human; can be administered orally; have long life in blood and low toxicity; and show less side-effects. Accordingly, they are extremely useful for the prophylaxis and treatment of thrombotic diseases and other diseases.Type: GrantFiled: February 6, 1996Date of Patent: June 3, 1997Assignee: The Green Cross CorporationInventors: Shinichiro Ono, Tomohiro Yoshida, Atsuyuki Ashimori, Keigo Kosaka, Takehiro Okada, Kazuhiro Maeda, Masahiro Eda, Fumio Mori, Yoshihisa Inoue, Hajime Ebisu, Teruaki Imada, Ruriko Ikegawa, Feng Wang, Norifumi Nakamura
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Patent number: 5607624Abstract: A process for the preparation of compounds of formula I ##STR1## wherein the general symbols are as defined in claim 1, which comprises reacting a compound of formula III ##STR2## wherein the general symbols are as defined in claim 1, with a compound of formula IV[H].sub.n --R.sub.1 (IV).Type: GrantFiled: September 12, 1994Date of Patent: March 4, 1997Assignee: Ciba-Geigy CorporationInventors: Peter Nesvadba, Samuel Evans, Ralf Schmitt
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Patent number: 5569772Abstract: The present invention is directed to a new process for the synthesis of 2-aryl benzo[b]thiophenes, and to novel intermediates therefor.Type: GrantFiled: June 7, 1995Date of Patent: October 29, 1996Assignee: Eli Lilly and CompanyInventors: David W. Hoard, Wayne D. Luke
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Patent number: 5565488Abstract: The inventive Oxalylamino-benzofuran- and benzothienyl-derivatives are prepared by reacting the appropriate amino substituted benzofuranes and benzothiophenes with oxalic acid derivatives. The inventive compounds are suitable for the prevention and treatment of acute and chronic inflammatory processes, particularly of the airways.Type: GrantFiled: May 23, 1995Date of Patent: October 15, 1996Assignee: Bayer AktiengesellschaftInventors: Gabriele Braunlich, Rudiger Fischer, Mazen Es-Sayed, Rudolf Hanko, Stephen Tudhope, Graham Sturton, Trevor Abram, Wendy J. McDonald-Gibson, Mary F. Fitzgerald
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Patent number: 5508431Abstract: The subject of the invention is 4-hydroxyphenylthio derivatives of general formula: ##STR1## in which: R.sub.1 and R.sub.2, which are identical or different, each represent hydrogen, a methyl or ethyl radical or a halogen atom,R represents a (C.sub.1 -C.sub.6) alkyl, (C.sub.3 -C.sub.6) cycloalkyl or phenyl radical,R.sub.3 represents hydrogen or a halogen atom,X represents --O--, --S-- or --NR.sub.4 -- in which R.sub.4 represents hydrogen or a (C.sub.1 -C.sub.4) alkyl group, useful as synthetic intermediates, especially for the preparation of aminoalkoxyphenylsulphonyl derivatives which are pharmaceutically active compounds.Type: GrantFiled: September 8, 1994Date of Patent: April 16, 1996Assignee: Elf SanofiInventors: Jean Gubin, Henri Inion
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Patent number: 5498630Abstract: A method of controlling Take-All disease of plants by applying a fungicide of the formula ##STR1## wherein Z1 and Z2 are C and are part of an aromatic ring which is benzothiophene; andA is selected from --C(X)-amine wherein the amine is an unsubstituted, monosubstituted or disubstituted amino radical, --C(O)--SR.sub.3, --NH--C(X)R.sub.4, and --C(.dbd.NR.sub.3)--XR.sub.7 ;B is --W.sub.m --Q(R.sub.2).sub.3 or selected from O-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R.sub.4 ;Q is C, Si, Ge, or Sn;W is --C(R.sub.3).sub.p H.sub.(2-p) --; or when Q is C, W is selected from --C(R.sub.3).sub.p H(.sub.2-p), --N(R.sub.3).sub.m H(.sub.1-m)--, --S(O)p--, and --O--;X is 0 or S;n is 0, 1, 2, or 3;m is 0 or 1;p is 0, 1, or 2;each R and R.sub.2 is independently defined herein;R.sub.3 is C.sub.1 -C.sub.4 alkyl;R.sub.4 is C.sub.1 -C.sub.4 alkyl, haloalkyl, alkoxy, alkylthio, alkylamino, or dialkylamino; andR.sub.7 is C.sub.1 -C.sub.Type: GrantFiled: November 16, 1994Date of Patent: March 12, 1996Assignee: Monsanto CompanyInventors: Dennis P. Phillion, Diane S. Braccolino, Matthew J. Graneto, Wendell G. Phillips, Karey A. Van Sant, Daniel M. Walker, Sai C. Wong
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Patent number: 5451596Abstract: This invention relates to a class of novel polycyclic compounds containing a cycloalkyl ring having substituted thereon a primary amine and which is further linked or bridged to two mono- and/or bicyclic rings and which reduces levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.Type: GrantFiled: December 29, 1992Date of Patent: September 19, 1995Assignee: Rhone Poulenc Rorer Pharmaceuticals Inc.Inventors: John W. Ullrich, Terence J. Kiesow, Kent W. Neuenschwander, Keith S. Learn, William P. Dankulich, Anthony C. Scotese
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Patent number: RE37087Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I in which R1, R2, R3, R4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.Type: GrantFiled: June 20, 1991Date of Patent: March 6, 2001Assignee: Schering AktiengesellschaftInventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles
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Patent number: RE35279Abstract: The present invention relates to novel hydantoin derivatives, processes for producing said hydantoin derivatives, pharmaceutical compositions containing at least one of said hydantoin derivatives as aldose reductase inhibitors and novel intermediate compounds in the synthesis of said hydantoin derivatives.The present invention is based on the selection of a hydantoin which is bonded by a sulfonyl group to various substituents at the 1-position of the hydantoin skeleton.The compounds of the present invention have a strong inhibitory activity against aldose reductase. These compounds are extremely useful for the treatment and/or prevention of various forms of diabetic complications based on the accumulation of polyol metabolites.Type: GrantFiled: February 17, 1994Date of Patent: June 18, 1996Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Ei Mochida, Kimihiro Murakami, Kazuo Kato, Katsuaki Kato, Jun Okuda, Ichitomo Miwa
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Patent number: RE36562Abstract: A method of controlling Take-All disease of plants by applying a fungicide of the formula ##STR1## wherein Z.sub.1 and Z.sub.2 are C and are part of an aromatic ring which is .[.benzothiophene.]..Iadd.thiophene.Iaddend.; andA is .[.selected from.]. --C(X)-amine .[.wherein the amine is an unsubstituted, monosubstituted or disubstituted amino radical.]..Iadd.wherein the amine is a monosubstituted or a disubstituted amine, wherein one of the substituents has a cyclic moiety, said cyclic moiety which is chosen from the group consisting of thienyl, furanyl, and a non-heterocyclic substituent, wherein when the amine is disubstituted, the second substituent is a non-cyclic substituent.Iaddend., --C(O)--SR.sub.3, --NH--C(X)R.sub.4, .[.and.]. .Iadd.or .Iaddend.--C(.dbd.NR.sub.3)--XR.sub.7 ;B is --W.sub.m --Q(R.sub.2).sub.3 or selected from .[.O-tolyl.]..Iadd.o-tolyl.Iaddend., 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R.sub.4 ;Q is C, Si, Ge, or Sn;W is --C(R.sub.3).sub.p H.Type: GrantFiled: March 11, 1998Date of Patent: February 8, 2000Assignee: Monsanto CompanyInventors: Dennis P. Phillion, Diane S. Braccolino, Matthew J. Graneto, Wendell G. Phillips, Karey A. Van Sant, Daniel M. Walker, Sai C. Wong