Polycyclo Ring System Is Tricyclo-carbocyclic Patents (Class 514/325)
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Publication number: 20080261985Abstract: This invention describes novel tricyclic-bis-enone derivatives (TBEs), such as TBE-31, TBE-34, TBE-45 and water-soluble TBEs. The methods of preparing these compounds are also disclosed. The inventors demonstrate the ability of these new TBEs to inhibit proliferation of human myeloma cells, inhibit the induction of iNOS in cells stimulated with interferon-?, induce heme oxygenase-1 (HO-1), induce CD11b expression—a leukemia differentiation marker, inhibit proliferation of leukemia cells, induce apoptosis in human lung cancer, and induce apoptosis in other cancerous cells. The TBEs of this invention are expected to be useful agents for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.Type: ApplicationFiled: November 16, 2007Publication date: October 23, 2008Inventors: Tadashi Honda, Chitra Sundararajan, Gordon W. Gribble, Michael B. Sporn, Karen T. Liby
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Publication number: 20080261873Abstract: Disclosed are methods of treating a disorder of the stomach, intestine or duodenum in a human subject. The method includes administering to the subject, a pharmaceutical composition comprising a compound that increases gastrointestinal motility (e.g., by modulating myenteric nerve activity) and/or induces the secretion or production of growth hormone.Type: ApplicationFiled: August 18, 2005Publication date: October 23, 2008Applicant: ELIXIR PHARMACEUTICALS, INC.Inventor: Bard J. Geesaman
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Publication number: 20080253985Abstract: The invention provides methods and compositions for treating hyperlipidemia and disorders associated with hyperlipidemia in a mammal. Compositions useful in the practice of the invention include a microsomal triglyceride transport protein inhibitor (“MTPI”) and at least two other cholesterol lowering drugs selected from the group consisting of a cholesterol absorption inhibitor (“CAI”), a HMG-CoA reductase inhibitor, a bile acid sequestrant, a fibric acid derivative, niacin, and squalene synthetase inhibitor.Type: ApplicationFiled: October 18, 2006Publication date: October 16, 2008Inventor: Gerald L. Wisler
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Patent number: 7432284Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Pagets disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.Type: GrantFiled: September 15, 2003Date of Patent: October 7, 2008Assignee: Merck & Co., Inc.Inventors: Dann LeRoy Parker, Robert R. Wilkening, Dongfang Meng, Ronald W. Ratcliffe
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Publication number: 20080207530Abstract: The invention provides a method for the treatment of COPD and/or gastrointestinal disease conditions ameliorated by histamine management in a subject, comprising administering to the subject an effective amount of a histidine decarboxylase inhibitor.Type: ApplicationFiled: February 12, 2008Publication date: August 28, 2008Inventors: Michalis Nicolaou, Emile Loria, Gaetan Terrasse, Yves Trehin
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Publication number: 20080207593Abstract: A once daily formulation containing the combination of a non-sedating or selective antihistamine (Loratadine) with a sedating or non-selective antihistamine (Chlorpheniramine) administered at bed-time has demonstrated greater efficacy in relieving allergic symptoms than Loratadine alone.Type: ApplicationFiled: August 20, 2007Publication date: August 28, 2008Inventors: Michael Heffernan, Jane C. Hirsh, Roman V. Rariy
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Publication number: 20080194631Abstract: The invention relates to the use of a molecule, alone or in combination, chosen from the group of molecules having a simultaneous antagonist action on the alpha1-noradrenergic, glutamatergic NMDA and serotoninergic 5HT2 receptors, for the preparation of a medicament intended for treating pathologies of the central nervous system.Type: ApplicationFiled: July 26, 2005Publication date: August 14, 2008Applicants: Key OBS, GreenpharmaInventors: Fabrice Trovero, Philippe Bernard
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Publication number: 20080161279Abstract: The invention is directed to methods for treating and/or controlling obesity in a patient. The methods involve combination therapies using a microsomal triglyceride transfer protein (MTP) inhibitor (for example, AEGR-733 and implitapide) and a cholesterol absorption inhibitor (CAI) (for example, ezetimibe).Type: ApplicationFiled: December 21, 2007Publication date: July 3, 2008Inventor: Gerald L. Wisler
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Publication number: 20080153761Abstract: Compositions for protection against SVFS induced by niacin, a carcinoid, mesenteric fraction, serotonin, post-menopause, alcohol or monosodium glutamate, comprising a flavonoid compound of the structure 2-phenyl-4H-1-benzopyran or 2-phenyl-4-keto-1-benzopyran or glycosides thereof, administered alone or together with an anti-superficial vasodilation dose of one or more of a non-bovine sulfated proteoglycan, a D-hexosamine sulfate, a serotonin inhibitor, willow bark extract and an olive kernel extract. As much as 100% protection against niacin flush can be achieved by luteolin and quercetin alone. A composition for treating cardiovascular disease with niacin, but without eliciting the SVFS effects of niacin, has also been invented.Type: ApplicationFiled: December 10, 2007Publication date: June 26, 2008Inventor: Theoharis C. Theoharides
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Publication number: 20080119516Abstract: It was an object of the present invention to provide novel compounds that are suitable in particular as active substances in medicaments, preferably in medicaments for the regulation of neuropeptide Y receptors, particularly preferably of neuropeptide Y5 (NPY5) receptor, for the regulation of food ingestion (food intake), preferably for the prophylaxis and/or treatment of disorders of food ingestion, such as obesity, anorexia, cachexia, bulimia or type II (non insulin dependent) diabetes, for the prophylaxis and/or treatment of disorders of the peripheral nervous system, disorders of the central nervous system, anxiety, depression, cognitive disorders, preferably memory disorders, cardiovascular diseases, pain, epilepsy, arthritis, hypertensive syndrom, inflammatory diseases, immune diseases and other NPY5 mediated disorders in animals and mammals, including man. Said object was achieved by providing 1,4-disubstituted piperidine compounds of general formula (I) wherein the substituents are defined in claim 1.Type: ApplicationFiled: July 29, 2004Publication date: May 22, 2008Applicant: LABORATORIOS DEL DR. ESTEVE S.A.Inventors: Antoni Torrens Jover, Josep Mas Prio, Alberto Dordal Zueras, Maria Angeles Fisas Escasany
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Patent number: 7375117Abstract: The present invention relates to polypeptides, and nucleic acids DNA encoding these polypeptides, capable of eliciting an immune reaction against cancer, methods for generating T lymphocytes capable of recognizing and destroying tumor cells, and pharmaceutical compositions for the treatment, prophylaxis or diagnosis of cancer.Type: GrantFiled: March 29, 2006Date of Patent: May 20, 2008Assignee: GemVax ASInventors: Gustav Gaudernack, Stein Sæøe-Larssen, Mona Møller, Jon Amund Eriksen
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Patent number: 7351720Abstract: The present application describes modulators of chemokine receptor activity of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis, including methods of preparing and intermediates thereof.Type: GrantFiled: June 10, 2004Date of Patent: April 1, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Soo S. Ko, George V. Delucca
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Patent number: 7326696Abstract: Aminomethyl substituted tetracycline compounds, pharmaceutical compositions, and methods of use thereof are discussed.Type: GrantFiled: December 15, 2003Date of Patent: February 5, 2008Assignee: Paratek Pharmaceuticals, Inc.Inventors: Mark L. Nelson, Kwasi Ohemeng, Roger Frechette, Paul Abato, Victor Amoo, Haregewein Assefa, Joel Berniac, Beena Bhatia, Todd Bowser, Jackson Chen, Laura Honeyman, Mohamed Y. Ismail, Oak Kim, Rachid Mechiche, N. Laxma Reddy, Atul K. Verma, Peter Viski, Tadeusz Warchol, Ivan Yanachkov
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Publication number: 20080027107Abstract: Anthraquinone compounds of the general formula (I) or a salt thereof (Formula I) in which R1 to R4 are each selected from the group consisting of H, C1-4 alkyl, X1, —NHR0N (Rs)2 in which R° is a C1l12 alkanediyl and each R5 is H or optionally substituted C14 alkyl, and a group of formula (11) in which at least one of R6,R7 and R8 is selected from X2 , and X2 substituted C1-4 alkyl and any others are H or C14 alkyl; R9 is selected from H, C14 alkyl, X2 and X2 substituted C1-4 alkyl; m is 0 or 1; n is 1 or 2; X1 is a halogen atom, a hydroxyl group, a C1.6 alkoxyl group, an aryloxy group or an acyloxy group; and X2 is a halogen atom, a hydroxyl group, a C16 alkoxyl group, an aryloxy group or an acyloxy group; provided that at least one of R1 to R4 is a group of formula (II). The N-oxides are useful prodrugs which are selectively bioreduced in hypoxic tumours to the corresponding cyclic amine derivatives.Type: ApplicationFiled: December 22, 2004Publication date: January 31, 2008Inventors: Laurence Hylton Patterson, Klaus Pors, Paul Henry Teesdale-Spittle
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Patent number: 7314875Abstract: The present invention provides compounds of the structure: wherein the constituent members are defined herein, including pharmaceutical compositions thereof and methods of treating diseases therewith.Type: GrantFiled: April 12, 2005Date of Patent: January 1, 2008Assignee: Cephalon, Inc.Inventors: Edward R. Bacon, Sankar Chatterjee, Derek Dunn, John A. Gruner, Rabindranath Tripathy
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Patent number: 7312222Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: March 25, 2004Date of Patent: December 25, 2007Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Soo S. Ko, George V. Delucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
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Patent number: 7189757Abstract: The invention is directed to compositions used for treating Central Nervous System (CNS) disorders. In addition, the invention provides convenient methods of treatment of a CNS disorder. Furthermore, the invention provides methods of treating sleep disorders using compositions that remain active for a discrete period of time to reduce side effects. More specifically, the invention is directed to the compositions and use of derivatized, e.g., ester or carboxylic acid derivatized, antihistamine antagonists for the treatment of sleep disorders.Type: GrantFiled: October 16, 2002Date of Patent: March 13, 2007Assignee: Hypnion, Inc.Inventors: Dale M. Edgar, David G. Hangauer, Harry Jefferson Leighton, Emmanuel J. M. Mignot
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Patent number: 7053071Abstract: The present invention provides compounds that are inducers or inhibitors of apoptosis or apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical compositions and methods for treating mammals with leukemia or other forms of cancer or for treating disease conditions caused by apoptosis of cells.Type: GrantFiled: December 2, 2002Date of Patent: May 30, 2006Assignee: The Burnham InstituteInventors: Marcia Dawson, Joseph A. Fontana, Xiao-kun Zhang, Mark Leid, Ling Jong, Peter D. Hobbs
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Patent number: 6908934Abstract: Compounds of Formula I and the pharmaceutically acceptable salts and esters thereof, wherein Z is selected from the group consisting of: (a) Formula Ia ?and (b) Formula Ib are novel LXR agonists and are useful in the treatment of dyslipidemic conditions particularly depressed levels of HDL cholesterol.Type: GrantFiled: May 30, 2002Date of Patent: June 21, 2005Assignee: Merck & Co., Inc.Inventors: Alan D. Adams, Aileen Bouffard, James F. Dropinski, Clare E. Gutteridge, A. Brian Jones, Weiguo Lui, John George Ondeyka, Ali Shiafee, Sheo Bux Singh
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Patent number: 6894059Abstract: The present invention provides 1,4 substituted piperazines, 1,4 substituted piperidines, and 1-substituted, 4-alkylidenyl piperidines compounds. The compounds of the invention are dual acting molecules having both leukotriene inhibition properties as well as antihistaminergic properties. The compounds of the invention are useful for treating conditions in which there is likely to be a histamine and/or leukotriene component. These conditions include preferably asthma, seasonal and perennial allergic rhinitis, sinusitus, conjunctivitis, food allergy, scombroid poisoning, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, chronic obsructive pulmonary disease, thrombotic disease and otitis media. Also provided are methods of treating asthma and rhinitis by administering an effective asthma and rhinitis-relieving amount of the compounds to a subject in need thereof.Type: GrantFiled: March 23, 2000Date of Patent: May 17, 2005Assignee: UCB S.A.Inventors: Ralph Scannell, Pierre Chatelain, Anna Toy-Palmer, Edmund Differding, James Ellis, Marie-Agnes Lassoie, Michelle Young, Xiong Cai, Sajjat Hussoin, Gurmit Grewal, Timothy Lewis
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Patent number: 6803378Abstract: Novel diketoacid compounds of Formula I are provided which are useful as HIV integrase inhibitors and for the treatment of AIDS or ARC.Type: GrantFiled: September 25, 2002Date of Patent: October 12, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Michael A. Walker, Timothy D. Johnson, Nicholas A. Meanwell, Jacque Banville
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Patent number: 6800636Abstract: Disclosed are compounds of the formula: wherein R8 represents a cyclic moiety to which is bound an imodazolylalkyl group; R9 represents a carbamate, urea, amide or sulfonamide group; and the remaining substituents are as defined herein. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.Type: GrantFiled: December 20, 2001Date of Patent: October 5, 2004Assignee: Schering CorporationInventors: Timothy Guzi, Dinanath F. Rane, Alan K. Mallams, Alan B. Cooper, Ronald J. Doll, Viyyoor M. Girijavallabhan, Arthur G. Taveras, Corey Strickland, Joseph M. Kelly, Jianping Chao
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Publication number: 20040180884Abstract: The present invention discloses a dibenzocycloheptene compound represented by the formula (I): 1Type: ApplicationFiled: December 23, 2003Publication date: September 16, 2004Inventors: Yoshiaki Kuroki, Hitoshi Ueno, Tetsushi Katsube, Tetsuo Kawaguchi, Eiji Okanari, Ichiro Tanaka, Masayuki Tanaka, Masahiko Hagihara
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Patent number: 6790980Abstract: The present invention is directed to methods and compositions for treating upper respiratory indications, such as the treatment, management or mitigation of cough, cold, cold-like symtoms, symtoms related to upper respiratory infections, influenza symptoms and allergic rhinitis, perennial rhinitis, nasal and Eustachian tube congestion in an animal by administration of tannate compositions comprising single agent formulations or combinations of at least one or more agents into a single administrative dose.Type: GrantFiled: October 2, 2002Date of Patent: September 14, 2004Assignee: First Horizon Pharmaceutical CorporationInventor: Balaji Venkataraman
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Patent number: 6767915Abstract: Certain novel 4-substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: January 27, 2003Date of Patent: July 27, 2004Assignee: Merck & Co., Inc.Inventors: Raman K. Bakshi, Khaled J. Barakat, Yingjie Lai, Ravi P. Nargund, Brenda L. Palucki, Min K. Park, Iyassu K. Sebhat, Zhixiong Ye, Arthur A. Patchett
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Publication number: 20040142972Abstract: The invention is directed to compositions used for treating Central Nervous System (CNS) disorders. In addition, the invention provides convenient methods of treatment of a CNS disorder. Furthermore, the invention provides methods of treating sleep disorders using compositions that remain active for a discrete period of time to reduce side effects. More specifically, the invention is directed to the compositions and use of derivatized, e.g., ester or carboxylic acid derivatized, antihistamine antagonists for the treatment of sleep disorders.Type: ApplicationFiled: December 4, 2003Publication date: July 22, 2004Applicant: Hypnion, Inc.Inventors: Dale M. Edgar, David G. Hangauer, Harry Jefferson Leighton, Emmanuel J.M. Mignot
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Publication number: 20040110793Abstract: Novel heterocyclo compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: April 16, 2003Publication date: June 10, 2004Inventors: John Lloyd, Yoon T. Jeon, Heather Finlay, Lin Yan, Michael F. Gross, Serge Beaudoin
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Publication number: 20040102482Abstract: A compound of formula (I) wherein R and R2 together with the nitrogen atom to which they are attached form pyrrolidinyl or piperidinyl, R1 is a group of formula (II) R3 and R′3 are hydrogen, deuterium or halogen, R4, R5 and R10 are independently of each other hydrogen or alkyl, R6, R7 and R8 are hydrogen or deuterium; R9 is amino, alkyl, aryl, heterocyclyl or mercapto; and, if X is oxygen, R9 is additionally hydrogen; R′10 is alkyl, X is sulphur, oxygen, NR10, or N+(R′10)2; Y is sulphur or oxygen, and m is 0, 1 or 2; with the proviso that, when R and R2 together with the nitrogen atom to which they are attached form piperidinyl, m is O, Y is S and Y is attached in position 3 of said piperidine ring, that group of formula (I) which is attached to the piperidine ring via the residue Y is either in the (S)-configuration or in the (R)-configuration, preferably in the (S) -configuration which is e.g. useful as antimicrobial, antibacterial.Type: ApplicationFiled: March 10, 2003Publication date: May 27, 2004Inventors: Gerd Ascher, Heinz Berner, Johannes Hildebrandt
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Patent number: 6727242Abstract: The present invention relates generally to pharmacological methods for the prevention of amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess serotonin-related pharmacological activity.Type: GrantFiled: December 14, 2001Date of Patent: April 27, 2004Assignee: The Board of Trustees of the University of IllinoisInventors: Miodrag Radulovacki, David W. Carley
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Patent number: 6673815Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is CH or N and, A, E, M, G, X2, X3, X4, R1, R2, R2a, R2b, R2c, R3, Y, x, m, and n are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.Type: GrantFiled: November 6, 2002Date of Patent: January 6, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Pratik Devasthale, Yoon T. Jeon
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Publication number: 20030236262Abstract: Certain novel 4-substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: ApplicationFiled: January 27, 2003Publication date: December 25, 2003Inventors: Raman K Bakshi, Khaled J Barakat, Yingjie Lai, Ravi P Nargund, Brenda L Palucki, Min K Park, Iyassu K Sebhat, Zhixiong Ye, Arthur A Patchett
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Publication number: 20030232786Abstract: Novel tricyclic-bis-enone derivatives (TBEs) as well as the process for the preparation of such TBEs are provided. Also provided are methods for prevention and/or treatment of cancer, Alzheimer's disease, Parkinson's disease, multiple sclerosis, amyotropic lateral sclerosis, rheumatoid arthritis, inflammatory bowel disease, and all other diseases whose pathogenesis is believed to involve excessive production of either nitric oxide (NO) or prostaglandins or the overexpression of iNOS or COX-2 genes or gene products. Further, methods for the synthesis of the TBE compounds of the invention utilize cheap commercially available reagents and are highly cost effective and amenable to scale-up. Additional high efficiency synthetic methods that utilize novel intermediates as well as the synthesis of these intermediates are also provided. Furthermore, the invention also provides methods for designing novel and water-soluble TBEs.Type: ApplicationFiled: January 15, 2003Publication date: December 18, 2003Inventors: Tadashi Honda, Frank G. Favaloro, Gordon W. Gribble, Michael B. Sporn, Nanjoo Suh
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Publication number: 20030220347Abstract: The present invention provides 1,4 substituted piperazines, 1,4 substituted piperidines, and 1-substituted,4-alkylidenyl piperidines compounds. The compounds of the invention are dual acting molecules having both leukotriene inhibition properties as well as antihistaminergic properties. The compounds of the invention are useful for treating conditions in which there is likely to be a histamine and/or leukotriene component. These conditions include preferably asthma, seasonal and perennial allergic rhinitis, sinusitus, conjunctivitis, food allergy, scombroid poisoning, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, chronic obstructive pulmonary disease, thrombotic disease and otitis media. Also provided are methods of treating asthma and rhinitis by administering an effective asthma and rhinitis-relieving amount of the compounds to a subject in need thereof.Type: ApplicationFiled: September 12, 2002Publication date: November 27, 2003Applicant: UCB S.A.Inventors: Ralph Scannell, Pierre Chatelain, Anna Toy-Palmer, Edmond Differding, James Ellis, Marie-Agnes Lassoie, Michelle Young, Xiong Cai, Sajjat Hussoin, Gurmit Grewal, Timothy Lewis
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Publication number: 20030207881Abstract: The use of a compound of formula (I): wherein R1, R2, R3, R4, R5 and R6 are independently selected from hydrogen, alkyl, aryl and non-aromatic heterocyclic groups, or each of one or more pair(s) of the substituent groups R1 to R6 may together form a 3, 4, 5, 6, 7 or 8-membered ring containing 0, 1 or 2 heteroatom(s); R7 is selected from alkyl, aryl and non-aromatic heterocyclic groups, and R8 is selected from hydrogen, halogen, alkyl, aryl and non-aromatic heterocyclic groups; and pharmaceutically acceptable salts and prodrugs thereof, in the manufacture of a medicament for use in the treatment of a condition generally associated with abnormalities in glutamatergic transmission; novel compounds of formula (1) per se and for use in therapy.Type: ApplicationFiled: March 31, 2003Publication date: November 6, 2003Inventors: Michael Frederick Snape, Roger John Gillespie, Claire Elizabeth Dawson, Steven Michael McAteer, Suneel Gaur
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Publication number: 20030195173Abstract: The invention related to colchinol derivatives of the formula (I): Wherein: R1, R2 and R3 are each independently hydroxy, phosphoryloxy (—OPO3H2), C1-4alkoxy or an in vivo hydrolysable ester of hydroxy, with the proviso that at least 2 of R1, R2 and R3 are C1-4alkoxy; A is —CO—, —C(O)O—, —CON(R8)— (wherein R8 is hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl, aminoC1-3alkyl or hydroxyC1-3alkyl); a is an integer from 1 to 4 inclusive; Ra and Rb are independently selected from hydrogen, hydroxy and amino; B is —O—, —CO—, N(R9)CO—, —CON(R9)—, —N(R9)C(O)O—, —N(R9)CON(R10)—, —N(R9)SO2—, —SO2N(R9)— or a direct single blond (wherein R9 and R10 are independently selected from hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl,aminoC1-3alkyl and hydroxyC1-3alkyl); b is O or an integer from 1 to 4 inclusive, (provided that when bis O, B is a single direct bond); D is carboxy, sulpho, tetrazolyl, imidazolyType: ApplicationFiled: January 7, 2003Publication date: October 16, 2003Inventor: Jean Claude Arnould
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Patent number: 6620782Abstract: The present invention is directed to novel 2-aminobenzamide thereof, represented by the general Formula I: where R1-R3, X, and A—D are defined herein. The present invention also relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.Type: GrantFiled: March 16, 2000Date of Patent: September 16, 2003Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Yan Wang
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Patent number: 6599921Abstract: Novel non-steroidal estrogen receptor ligands and methods of synthesis are disclosed. The novel molecules are intended for use in therapeutic preparations for the treatment of estrogen receptor related disease states. The compounds specified are tetra-cyclic derivatives and have been shown to be antiproliferative against human estrogen-dependent cancer cells and to have good binding affinity for the estrogen receptor.Type: GrantFiled: August 21, 2001Date of Patent: July 29, 2003Assignee: NanoDesign, Inc.Inventors: Jonathan Martin Schmidt, Julie Mercure, Jeffry Lawrence Lowell, Stefan Kwiatkowski, Krzysztof Pupek, Shuguang Zhu, John Whelan, Natalie Lazarowych
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Publication number: 20030130272Abstract: Use of compound of Formula (I): at least one of R1, R2, R5 and R6 is a group —AB and the others are independently selected from hydrogen, hydroxy, alkoxy or acyloxy, a group —AB a group -amino-(R7)nX—Y wherein R7 is a divalent organic radical and n is 0 or 1; R3 and R4are independently oxo, hydroxy or hydrogen; the or each A is independently a spacer group of formula -amino-(R7)n—X— which is bonded to the anthracene ring via the amino group nitrogen and to B via —X—, X is independently selected from O, NH and C(O); B is an amino acid residue or a peptide group or isostere thereof and Y is hydrogen or a capping group, or a physiologically acceptable derivative of such compound for the manufacture of a medicament for the treatment of cancers or microbial infections having cells exhibiting topoisomerase I activity characterised in that the group -amino-(R7)n—X— incorporates an optionally substituted heterocyclic ring directly attached to the anthroquinone rinType: ApplicationFiled: July 15, 2002Publication date: July 10, 2003Inventors: David John Mincher, Agnes Turnbull, Graeme Gillies Kay
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Publication number: 20030125357Abstract: Compounds of Formula I 1Type: ApplicationFiled: May 30, 2002Publication date: July 3, 2003Inventors: Alan D. Adams, Aileen Bouffard, James F. Dropinski, Clare E. Gutteridge, A. Brian Jones, Weiguo Lui, John George Ondeyka, Ali Shiafee, Sheo Bux Singh
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Patent number: 6569849Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula wherein X, Y, Z, A, R1, R2, r and s are as defined in the detailed part of the present description or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to secretion and circulation of insulin antagonising peptides.Type: GrantFiled: October 3, 1997Date of Patent: May 27, 2003Assignee: Novo Nordisk A/SInventors: Tine Krogh Jorgensen, Rolf Hohlweg, Peter Madsen, Knud Erik Andersen, Svend Treppendahl, Uffe Bang Olsen, Zdenek Polivka, Alexandra Silhankova, Karel Sindelar, Vladimir Valenta, Tomas Kalisz
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Patent number: 6548504Abstract: The present invention therefore provides, in a first aspect, a compound of formula (I) or a salt thereof: in which the group D is selected from a group of formula (A), (B) or (C) below: in which P is a monocyclic, bicyclic or tricyclic alicyclic ring containing up to 20 carbon atoms in the ring(s); A is a single bond, a C1-6alkylene or a C2-6alkenylene group; R1 is halogen, C1-6alkyl optionally substituted by one or more fluorine atoms, C3-6cycloalkyl, C1-6alkoxy, OCF3, hydroxy, hydroxyC1-6alkyl, hydroxyC1-6alkoxy, C1-6alkoxyC1-6alkoxy, C1-6alkanoyl, amino, alkylamino or dialkylamino, SR11 where R11 is hydrogen or C1-6alkyl or R1 is aryl, arylC1-6alkyl, a bicyclic heterocyclic ring or is a 5 to 7-membered heterocyclic ring each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulfur; n is 0, 1, 2 or 3; and R2 is hydrogen, C1-6alkyl, aryl, arylC1-6alkyl or C3-6cycloalkyl; or in which Ra is an alkyl group containing 1 to 20 carbon atoms oType: GrantFiled: July 19, 2000Date of Patent: April 15, 2003Assignee: SmithKline Beecham p.l.c.Inventors: Steven Mark Bromidge, Stephen Frederick Moss
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Publication number: 20030040520Abstract: Disclosed are compounds of the formula: 1Type: ApplicationFiled: December 20, 2001Publication date: February 27, 2003Inventors: Timothy Guzi, Dinanath F. Rane, Alan K. Mallams, Alan B. Cooper, Ronald J. Doll, Viyyoor M. Girijavallabhan, Arthur G. Taveras, Corey Strickland, Joseph M. Kelly, Jianping Chao
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Patent number: 6509492Abstract: The present invention is directed to methods and compositions for treating upper respiratory indications, such as the treatment, management or mitigation of cough, cold, cold-like symptoms, symptoms related to upper respiratory infections, influenza symptoms and allergic rhinitis, perennial rhinnitis, nasal and Eustachian tube congestion in an animal by administration of tannate compositions comprising combinations of at least one or more agents into a single administrative dose.Type: GrantFiled: September 14, 2001Date of Patent: January 21, 2003Assignee: First Horizon Pharmaceutical CorporationInventor: Balaji Venkataraman
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Publication number: 20030013704Abstract: 1Type: ApplicationFiled: June 12, 2002Publication date: January 16, 2003Inventors: Lilian Alcaraz, Moya Caffrey, Mark Furber, Timothy Luker, Michael Mortimore, Austen Pimm, Philip Thorne, Paul Willis
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Patent number: 6492355Abstract: The invention provides compounds of general formula in which m, A, R1 and Ar have the meanings defined in the specification; a process for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.Type: GrantFiled: June 1, 2000Date of Patent: December 10, 2002Assignee: AstraZeneca ABInventors: Lilian Alcaraz, Mark Furber, Michael P. Mortimore
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Publication number: 20020173500Abstract: Substituted heterocyclo-norbornylaminoderivatives having: a) an exo-configuration nitrogen and an endo-fused five-membered ring or six-membered ring of the formula (I) or b) an exo-configuration nitrogen and an exo-fused five-membered ring or six-membered ring of the formula (Ia), 1Type: ApplicationFiled: December 18, 2001Publication date: November 21, 2002Inventors: Uwe Heinelt, Hans-Jochen Lang, Klaus Wirth, Hans-Willi Jansen
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Publication number: 20020147195Abstract: The present invention relates to a novel serotonin antagonist and an anti-platelet agent, more particularly, a serotonin antagonist and an anti-platelet agent which potently and specifically inhibit the serotonin 2 receptor with low adverse side effect.Type: ApplicationFiled: March 21, 2002Publication date: October 10, 2002Applicant: AJINOMOTO CO., INC.Inventors: Shingo Makino, Harumi Arisaka, Hiroshi Yamamoto, Masataka Shoji, Ryota Yoshimoto
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Patent number: 6451801Abstract: The present invention provides 1,4 substituted piperazines, 1,4 substituted piperidines, and 1-substituted, 4-alkylidenyl peperidines compounds. The compounds of the invention are dual acting molecules having both leukotriene inhibition properties as well as antihistaminergic properties. The compounds of the invention are useful for treating conditions in which there is likely to be a histamine and/or leukotriene component. These conditions include preferable asthma, seasonal and perennial allergic rhinitis, sinusitus, conjunctivitis, food allergy, scombroid poisoning, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, chronic obstructive pulmonary disease, thrombotic disease and otitis media. Also provided are methods of treating asthma and rhinitis by administering an effective asthma and rhinitis-relieving amount of the compounds to a subject in need thereof.Type: GrantFiled: March 24, 2000Date of Patent: September 17, 2002Assignee: UCB, S.A.Inventors: Ralph Scannell, Pierre Chatelain, Anna Toy-Palmer, Edmond Differding, James Ellis, Marie-Agnes Lassoie, Xiong Cai, Sajjat Hussoin, Gurmit Grewal, Timothy Lewis
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Patent number: 6444821Abstract: Monohydrate and trihydrate crystals of N-(2-(4-(5H-dibenzo[a,d]cyclohepten-5-ylidene)-piperidino) ethyl)-1-formyl-4-piperidinecarboxamide hydrochloride having excellent stability.Type: GrantFiled: February 6, 2001Date of Patent: September 3, 2002Assignee: Ajinomoto Co., Inc.Inventors: Akiko Fujii, Mie Kubo, Tomoya Yamamoto, Jiro Shimada, Ryuichi Mihara, Hirokazu Naora, Koji Asai
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Patent number: RE39128Abstract: The present invention relates to pleuromutilin derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly antibacterial therapy.Type: GrantFiled: October 27, 1998Date of Patent: June 13, 2006Assignee: SmithKline Beecham p.l.c.Inventors: Valerie Joan Berry, Steven Dabbs, Colin Henry Frydrych, Eric Hunt, Francis Dominic Sanderson, Gary Woodnutt