Polycyclo Ring System Having The Diazole Ring As One Of The Cyclos Patents (Class 514/387)
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Publication number: 20080255185Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.Type: ApplicationFiled: November 19, 2007Publication date: October 16, 2008Applicant: Dendreon CorporationInventors: Ofir Moreno, Sateesh Natarajan, David F. Duncan
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Publication number: 20080249152Abstract: Formula (I) compounds are described: Formula (I) where the radicals are as defined in the description, processes for their preparation, and their uses for the preparation of conjugates with radionuclides for use in human and animal therapy and diagnostics, particularly for the diagnosis and therapy of pathological conditions such as tumours.Type: ApplicationFiled: September 18, 2006Publication date: October 9, 2008Applicant: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A.Inventors: Paolo Carminati, Mauro Ginanneschi, Giovanni Paganelli, Marco Chinol
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Publication number: 20080226696Abstract: The present invention provides methods of improving learning ability of aged companion animals (such as aged dogs) by administering an effective amount of a carnitine and an effective amount of a lipoic acid. Also provided are kits and animal treats for improving learning ability of aged companion animals comprising effective amounts of carnitine and lipoic acid.Type: ApplicationFiled: April 20, 2007Publication date: September 18, 2008Inventors: Ben Treadwell, Nathan Hamilton
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Publication number: 20080221185Abstract: The invention provides a compound of formula (I) or a solvate thereof: wherein R1, R2, R3, R4, R5, R6, and n are as defined in the specification, and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.Type: ApplicationFiled: July 31, 2006Publication date: September 11, 2008Inventors: Anthony William Dean, Roderick Alan Porter
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Publication number: 20080206290Abstract: A cosmetic combination product, wherein the product comprises at least two components selected from (a) one or more dietary supplements, (b) one or more cosmetic preparations for topical application to human skin, and (c) one or more patches for adhesion to human skin. Each of the selected components (a) to (c) comprises at least one cosmetically active substance which is also comprised in the other selected component(s). This Abstract is not intended to define the invention disclosed in the specification, nor intended to limit the scope of the invention in any way.Type: ApplicationFiled: August 15, 2007Publication date: August 28, 2008Applicant: BEIERSDORF AGInventors: Jens SCHULZ, Rainer Kroepke, Andreas Schepky, Julia Eckert, Urte Koop, Sabine Faenger
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Patent number: 7416750Abstract: A Composition to provide nutritional support for mammals having glycemic control and deficit concerns, and assist in managing glycemic controls deficits, with a synergistic combination of natural ingredients.Type: GrantFiled: February 26, 2007Date of Patent: August 26, 2008Assignee: NBTY, Inc.Inventors: Angelica Vrablic, Glenn Schneider, Robert Silverman
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Patent number: 7407952Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins having the following structure are disclosed: wherein A, R1, R2, R2a and R3 are as defined herein. Such compounds have utility over a wide range of fields, including use as diagnostic and therapeutic agents. In particular, compounds of this invention are useful in pharmaceutical compositions as anti-inflammatory agents as well as inhibitors of central nervous disorders. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening the same to identify biologically active members.Type: GrantFiled: July 6, 2005Date of Patent: August 5, 2008Assignee: Myriad Genetics, Inc.Inventors: Gangadhar Nagula, Jan Urban, Hwa-Ok Kim, Christopher Lum, Hiroshi Nakanishi
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Patent number: 7407950Abstract: The invention concerns compounds of general formula (I), wherein n, X1, X2, X3, X4, Z1, Z2, Z3, Z4, Z5 and W are as defined herein. Said compounds are ligands of the TRPV1 vanilloid receptor, and are therefore, useful for treating diseases associated with TRPV1 receptors, such as pain and inflammation.Type: GrantFiled: June 20, 2007Date of Patent: August 5, 2008Assignee: Sanofi-AventisInventors: Laurent Dubois, Yannick Evanno, Andre Malanda
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Publication number: 20080182834Abstract: The invention provides multi-nuclear metal complexes partially encapsulated by one or more cucurbit[7 to 12]urils or analogues thereof. The invention further relates to methods for treating cancer by administering a multi-nuclear metal complex having anti-tumour activity partially encapsulated by one or more cucurbit[7 to 12]urils or analogues thereof.Type: ApplicationFiled: January 14, 2005Publication date: July 31, 2008Applicant: NEWSOUTH INNOVATIONS PTY LIMITEDInventors: Nial Joseph Wheate, Anthony I. Day, Rodney J. Blanch, John G. Collins
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Publication number: 20080153873Abstract: The present invention is directed to dihydrobenzofuranyl derivatives of formula I: or a pharmaceutically acceptable salt thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorder, cognitive disorder, diabetic neuropathy, pain, and other diseases or disorders.Type: ApplicationFiled: December 12, 2007Publication date: June 26, 2008Applicant: WyethInventors: Puwen Zhang, Joseph Peter Sabatucci, Eugene Anthony Terefenko, Eugene John Trybulski
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Patent number: 7390828Abstract: Formula (I) compounds are described where the groups are as defined here below, processes for their preparation, and their uses for the preparation of conjugates with radionuclides for use in human and animal therapy and diagnostics, particularly for the diagnosis and therapy of pathological conditions such as tumoursType: GrantFiled: February 15, 2002Date of Patent: June 24, 2008Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Giovanni Paganelli, Marco Chinol, Mauro Ginanneschi
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Patent number: 7390798Abstract: The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache.Type: GrantFiled: February 9, 2005Date of Patent: June 24, 2008Assignee: Merck & Co., Inc.Inventors: Theresa M. Williams, Christopher S. Burgey, Thomas J. Tucker, Craig A. Stump, Ian M. Bell
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Patent number: 7351732Abstract: New cycloalkanedione derivatives that are serotonin (5-hydroxytriptamine, 5-HT) 5-HT1A receptor subtype agonists and, consequently, they are useful in the treatment of pathological states for which an agonist of these receptors is indicated. They are particularly useful as neuroprotective agents, of special interest in the treatment and prophylaxis of cerebral damage produced by traumatic or ischemic stroke.Type: GrantFiled: July 29, 2003Date of Patent: April 1, 2008Assignee: Schwarz Pharma S.L.Inventors: Joaquin Del Río Zambrana, Diana Frechilla Manso, M. Luz López Rodríguez, Bellinda Benhamú Salama, José Ángel Fuentes Cubero, Mercedes Delgado Wallace
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Patent number: 7345074Abstract: Derivatives of [6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonylamino]-propionamide which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.Type: GrantFiled: October 20, 2004Date of Patent: March 18, 2008Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Terence Alfred Kelly, Jin Mi Kim, René Marc Lemieux
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Patent number: 7335384Abstract: The present disclosure describes a novel composition for the treatment and/or prevention of neurogenic inflammation. Such composition is also useful in the treatment and/or prevention of disease states and conditions associated with neurogenic inflammation. Such disease states and conditions include, but are not limited to, migraine headache, arthritis and fibromyalgia. The composition comprises nutrient compounds in a novel combination and formulation to treat and/or prevent neurogenic inflammation and disease states and conditions associated therewith. By reducing neurogenic inflammation, the compositions of the present disclosure reduce the symptoms associated with neurogenic inflammation, such as pain and systemic inflammation in general.Type: GrantFiled: March 17, 2006Date of Patent: February 26, 2008Assignee: 4K Nutripharma InternationalInventor: F. Mahnaz Khaled
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Patent number: 7304067Abstract: Derivatives of [6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonylamino]-propionamide which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.Type: GrantFiled: January 13, 2005Date of Patent: December 4, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Terence Alfred Kelly, Jin Mi Kim, René Marc Lemieux
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Patent number: 7300927Abstract: Disclosed is a method for treating or preventing Alzheimer's disease by restricting the level of metabolizable carbohydrate in the diet and/or administering to the patient an effective amount of an agent which reduces serum insulin levels.Type: GrantFiled: September 23, 2003Date of Patent: November 27, 2007Inventors: Robert W. Esmond, Jack R. Wands, Suzanne de la Monte
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Publication number: 20070259850Abstract: The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.Type: ApplicationFiled: May 1, 2007Publication date: November 8, 2007Inventors: Stephen E. Mercer, Prasad V. Chaturvedula
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Patent number: 7285562Abstract: The present invention provides methods for the use of compounds as depicted by structure I, pharmaceutical compositions containing the same, and methods for the prophylaxis, management and treatment of metabolic diseases and diseases modulated by MCD inhibition. The compounds disclosed in this invention are useful for the prophylaxis, management and treatment of diseases involving in malonyl-CoA regulated glucose/fatty acid metabolism pathway.Type: GrantFiled: July 28, 2004Date of Patent: October 23, 2007Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Mark D. Kafka, Mark E. Wilson, Anna Russell, Gary D. Lopaschuk, Jason R. Dyck
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Patent number: 7256207Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.Type: GrantFiled: August 18, 2004Date of Patent: August 14, 2007Assignee: IRM LLCInventors: Hong Liu, Phillip B. Alper, Donald S. Karanewsky
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Patent number: 7244756Abstract: Certain 1,5-disubstituted benzimidazol-2-one compounds useful as therapeutic agents. The compounds may be of the Formula I wherein: R? represents hydrogen or alkyl; R? represents halogen or trihalogenmethyl; and Hlg represents halogen; provided, however, that if Hlg is F, then R? is not Cl. Also, use of the 1,5-disubstituted benzimidazol-2-one compounds, or pharmaceutically-acceptable addition salts thereof, in applications that benefit from increasing the blood-brain barrier permeability.Type: GrantFiled: June 17, 2003Date of Patent: July 17, 2007Assignee: Poseidon Pharmaceuticals A/SInventors: Lars Siim Madsen, Camilla ærteberg Bæk, Annette Lauridsen, Søren Peter Olesen
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Patent number: 7214802Abstract: Disclosed compounds of formula (I) which inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.Type: GrantFiled: March 7, 2005Date of Patent: May 8, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Derek Cogan, Ming-Hong Hao, Victor Marc Kamhi, Craig Andrew Miller, Matthew Russell Netherton, Alan David Swinamer
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Patent number: 7196108Abstract: The invention relates to certain bicyclic heterocycles havng the structure shown below which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, and atherosclerosis.Type: GrantFiled: March 6, 2003Date of Patent: March 27, 2007Assignees: Incyte San Diego Inc., Ortho McNeil Pharmaceutical Inc.Inventors: Magnus Pfahl, Catherine Tachdjian, Hussien A. Al-Shamma, Andrea Fanjul Giachino, Karine Jakubowicz-Jaillardon, Jianhua Guo, Richard M. Fine, Lyle W. Spruce, James W. Zapf
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Patent number: 7176320Abstract: A benzimidazole derivative or its medically acceptable salt, represented by the following formula (1), that is a human chymase activity inhibitor capable of being applied clinically: wherein, R1 and R2 represent a hydrogen atom, an alkyl group or an alkoxy group, etc., A represents an alkylene group or an alkenylene group, E represents —COOR3, —SO3R3, —CONHR3 or —SO2NHR3, etc., G represents an alkylene group, M represents a single bond or —S(O)m—, J represents a heterocyclic group, and X represents —CH? or a nitrogen atom.Type: GrantFiled: February 13, 2004Date of Patent: February 13, 2007Assignee: Teijin LimitedInventors: Naoki Tsuchiya, Yoshiyuki Matsumoto, Hiroshi Saitou, Tsuyoshi Mizuno
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Patent number: 7173057Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.Type: GrantFiled: February 24, 2005Date of Patent: February 6, 2007Assignee: Schering CorporationInventors: Kevin X. Chen, F. George Njoroge, Mousumi Sannigrahi, Latha G. Nair, Weiying Yang, Bancha Vibulbhan, Srikanth Venkatraman, Ashok Arasappan, Stephane L. Bogen, Frank Bennett, Viyyoor M. Girijavallabhan
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Patent number: 7122534Abstract: The present invention relates to compounds of formula (I) and their pharmaceutically acceptable salts, wherein R1, R2, R3 and Z are as defined herein, intermediates in the synthesis of such compounds, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of neurological and psychological disorders.Type: GrantFiled: January 23, 2004Date of Patent: October 17, 2006Assignee: Pfizer IncInventor: Jotham Wadsworth Coe
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Patent number: 7115644Abstract: Disclosed are benzimidazolone compounds of formulas (I) & (II): wherein R1, R2, R3, R4, R5, X, L, m, n and t are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease.Type: GrantFiled: September 3, 2003Date of Patent: October 3, 2006Assignee: Boehringer Ingelheim Pharmaceuticals Inc.Inventors: Antonio Jose del Moral Barbosa, Jr., Daniel R. Goldberg, Abdelhakim Hammach, Pingrong Liu, Neil Moss, Mark Stephen Ralph, Gregory Paul Roth, Christopher Ronald Sarko, Fariba Soleymanzadeh, Andre White
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Patent number: 7105550Abstract: This invention concerns the use of a compound of formula (I?) a N-oxide, pharmaceutically acceptable addition salt, quaternary amine and stereochemically isomeric form thereof, wherein Q is optionally substituted C3-6cycloalkyl, phenyl, naphthyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl; or Q is a radical of formula wherein X and Y each independently are O, NR3, CH2 or S, with R3 being hydrogen or C1-4alkyl; q is 1 to 4; Z is O or NR4 with R4 being hydrogen or C1-4alkyl; r is 1 to 3; L is optionally substituted phenyl or L is Het with Het being an optionally substituted five- or six-membered heterocyclic ring or an optionally substituted bicyclic heterocyclic ring; for the manufacture of a medicament for the prevention or the treatment of diseases mediated through cytokines.Type: GrantFiled: February 20, 2001Date of Patent: September 12, 2006Inventors: Christopher Love, Jean Pierre Frans Van Wauwe, Marc De Brabander, Ludwig Cooymans, Nele Vandermaesen, Ludo Edmond Josephine Kennis
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Patent number: 7081466Abstract: Disclosed is a compound represented by Structural Formula (I): R1 is a substituted or unsubstituted 2-imidazolyl group which is optionally fused to a substituted or unsubstituted aryl group. Z1 is ?O, ?S, ?NOR11. R is represented by a Structural Formula selected from (II)–(VII): The variables in Structural Formulas (II)–(VII) are described herein.Type: GrantFiled: March 16, 2004Date of Patent: July 25, 2006Assignee: Synta Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Mitsunori Ono, David James, Weiwen Ying, Shoujun Chen
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Patent number: 7056918Abstract: The present invention relates to novel triazolo-pyridines of the formula I wherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from nitrogen, sulfur and oxygen wherein at least one of said heteroatoms atoms must be nitrogen; R2 is selected from the group consisting of hydrogen, (C1–C6)alkyl or other suitable substituents; R3 is selected from the group consisting of hydrogen, (C1–C6)alkyl or other suitable substituents; s is an integer from 0–5; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.Type: GrantFiled: March 11, 2002Date of Patent: June 6, 2006Assignee: Pfizer, Inc.Inventors: Mark A. Dombroski, Michael A. Letavic, Kim F. McClure
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Patent number: 7034048Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors.Type: GrantFiled: May 4, 2001Date of Patent: April 25, 2006Assignee: James Black Foundation LimitedInventors: Sarkis Barret Kalindjian, Ildiko Maria Buck, Caroline Minli Rachel Low, Matthew John Tozer
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Patent number: 6974815Abstract: The present invention is directed to compounds having the formula (I): useful in treating inflammatory and immune diseases, in which K is O or S; Q is —C(?O)— or optionally substituted C1-4alkylene; Ar is optionally-substituted aryl or heteroaryl; J1, J2, J3, and Y are selected so that ring A is a five-to-six membered optionally-substituted cycloalkenyl or heterocyclo ring having 0 to 2 nitrogen heteroatoms; Z is N or C(R9); and R1, R2, R3 and R9 are as defined in the specification.Type: GrantFiled: October 9, 2003Date of Patent: December 13, 2005Assignees: Bristol-Myers Squibb Company, Cerep SAInventors: T G. Murali Dhar, Dominique Potin, Magali Jeannine Blandine Maillet, Michele Launay, Eric Antoine Nicolai, Edwin J. Iwanowicz
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Patent number: 6974823Abstract: The present invention relates generally to novel hydantoin derivative compounds, pharmaceutical compositions containing such compounds, and methods for their use in preventing and/or treating neurological disorders, including physically damaged nerves and neurodegenerative diseases; for treating alopecia and promoting hair growth; for treating vision disorders and/or improving vision; for treating memory impairment and/or enhancing memory performance; and for treating sensorineural hearing loss by administering such compounds.Type: GrantFiled: December 21, 2000Date of Patent: December 13, 2005Assignee: GPI NIL Holdindgs, Inc.Inventor: Gregory S. Hamilton
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Patent number: 6964977Abstract: The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.Type: GrantFiled: August 23, 2001Date of Patent: November 15, 2005Assignee: SmithKline Beecham CorporationInventors: Philip Anthony Harris, Robert N Hunter, Robert Walton McNutt, Jr., Lee Frederick Kuyper, Karen Elizabeth Lackey, Michael Robert Peel, Edgar Raymond Wood, III
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Patent number: 6960571Abstract: A method of treating Restless Leg Syndrome, includes administering to a subject an iron complex having an iron release rate greater than IDI. The iron release rate is determined at a concentration of at least 2,000 ?g/dl.Type: GrantFiled: March 14, 2003Date of Patent: November 1, 2005Assignee: Luitpold Pharmaceuticals, Inc.Inventors: Mary Jane Helenek, Ralf A. Lange, Fred B. Oldham, Marc L. Tokars
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Patent number: 6960586Abstract: The present invention provides a compound having a steroid C17,20-lyase inhibitory activity, which is useful as a prophylactic or therapeutic agent of prostatism and tumor such as breast cancer and the like. A compound represented by the formula: wherein R is a hydrogen atom or a protecting group, R1 is a lower alkyl group or a cyclic alkyl group, and ring A and ring B are each an optionally substituted 5-membered or 6-membered ring having an amide bond in the ring, or a salt thereof.Type: GrantFiled: November 19, 2001Date of Patent: November 1, 2005Assignee: Takeda Pharmaceutical Company LimitedInventors: Akihiro Tasaka, Nobuyuki Matsunaga, Akio Ojida, Masami Kusaka
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Patent number: 6960474Abstract: Selective androgen receptor modulators (SARMs) having antagonist activity in hormone-dependent tumors while exhibiting no activity or agonist activity against other nontumor tissues containing the androgen receptor as well as methods for identifying, designing and using SARMs are provided.Type: GrantFiled: June 20, 2001Date of Patent: November 1, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Mark E. Salvati, Marco M. Gottardis, Ricardo M. Attar, Stanley R. Krystek, Jr., John S. Sack
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Patent number: 6943157Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins having the following structure are disclosed: wherein A, R1, R2, R2a and R3 are as defined herein. Such compounds have utility over a wide range of fields, including use as diagnostic and therapeutic agents. In particular, compounds of this invention are useful in pharmaceutical compositions as anti-inflammatory agents as well as inhibitors of central nervous disorders. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening the same to identify biologically active members.Type: GrantFiled: October 9, 2002Date of Patent: September 13, 2005Assignee: Myriad Genetics, Inc.Inventors: Gangadhar Nagula, Jan Urban, Hwa-Ok Kim, Christopher Lum, Hiroshi Nakanishi
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Patent number: 6943149Abstract: The invention is directed to novel benzimidazolone peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis, hypertension, heart failure, arrhythmia, inflammation, angina, stroke, atherosclerosis, ischemic conditions, Angiogenesis related disorders, cancer, and neurodegenerative disorders. Pharmaceutical compositions comprising the substituted benzimidazolone peptidomimetics of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.Type: GrantFiled: March 17, 2003Date of Patent: September 13, 2005Assignees: Ortho McNeil Pharmaceutical, Inc., Millennium Pharmaceuticals, Inc.Inventors: Han-Cheng Zhang, Bruce E. Maryanoff, David F. McComsey, Kimberly B. White
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Patent number: 6939887Abstract: The present invention can provide novel compounds useful as orally administrable growth hormone releaser, more specifically a benzimidazolidinone derivative of formula (1) or a pharmaceutically acceptable salt thereof: (1) wherein R1 is optionally substituted alkyl or the like; R2, R3 and R4 are each hydrogen, optionally substituted alkyl, or the like; R5 is optionally substituted aryl; q is 0 or 1; and W1 is a group represented by formula (2): (2) n is 1, 2 or 3; m is 0, 1, 2 or 3; R6 and R7 are each hydrogen, optionally substituted alkyl, or the like; and R8 and R9 are each hydrogen, optionally substituted alkyl, or the like.Type: GrantFiled: January 30, 2002Date of Patent: September 6, 2005Assignee: Sumitomo Pharmaceuticals Co., Ltd.Inventors: Kazuhiko Okazaki, Yasuyuki Ueki
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Patent number: 6921771Abstract: The present invention is a method of treating sexual disturbances in humans and inducing mating in non-human mammals using the compounds of formula (A) in a dosage range where the sexually therapeutic amount is from about 0.2 thru 8 mg/person/dose and where the sexually mating amount is from about 0.003 thru 0.2 mg/kg/dose.Type: GrantFiled: February 19, 2002Date of Patent: July 26, 2005Assignee: Pharmacia & Upjohn CompanyInventors: Robert B. McCall, Martin Durham Meglasson
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Patent number: 6919331Abstract: The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides heterocyclic substituted 2-methylbenzimidazole derivatives for the treatment of respiratory syncytial virus infection.Type: GrantFiled: December 4, 2002Date of Patent: July 19, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Kuo-Long Yu, Xiangdong Wang, Yaxiong Sun, Christopher Cianci, Jan Willem Thuring, Keith Combrink, Nicholas Meanwell, Yi Zhang, Rita L. Civiello
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Patent number: 6906090Abstract: The invention provides the use of certain isatin and oxindole derivatives in the preparation of a medicament for use in the treatment of mycobacterial disease.Type: GrantFiled: March 4, 1999Date of Patent: June 14, 2005Assignee: AstraZeneca ABInventor: Ramachandran Janakiraman
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Patent number: 6903126Abstract: The invention relates to novel benzimidazole derivatives with general formula I, whereby radicals R1, R2, R3, A, B, Y and Z have the meanings that are indicated in the description and the claims, the use of these compounds for the production of a pharmaceutical agent for treatment and prevention of diseases associated with microglia activation as well as pharmaceutical preparations that contain these compoundsType: GrantFiled: July 9, 2002Date of Patent: June 7, 2005Assignee: Schering AGInventors: Thorsten Blume, Wolfgang Halfbrodt, Joachim Kuhnke, Ursula Monning, Herbert Schneider
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Patent number: 6903127Abstract: The present invention is a method of treating sexual disturbances in humans and inducing mating in non-human mammals using the compounds of formula (A) in a dosage range where the sexually therapeutic amount is from about 0.2 thru 8 mg/person/dose and where the sexually mating amount is from about 0.003 thru 0.2 mg/kg/dose.Type: GrantFiled: July 30, 2002Date of Patent: June 7, 2005Assignee: Pharmacia & Upjohn CompanyInventors: Robert B. McCall, Martin Durham Meglasson
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Patent number: 6897225Abstract: The present invention relates to a compound of the following formula: or a pharmaceutically acceptable salt thereof. Also disclosed are compositions containing the compound and methods of preparing and using the compounds. The compounds of the invention are useful in treating ?L?2 adhesion mediated conditions in a mammal.Type: GrantFiled: October 19, 2000Date of Patent: May 24, 2005Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Ila Sircar, Marshall Morningstar, Paul Furth, Nicholas Smith, Bradley R. Teegarden, Ronald C. Griffith
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Patent number: 6897208Abstract: The invention is directed to physiologically active compounds of the general formula (Ix) and compositions containing such compounds, and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (Ix), and to processes for their preparation. Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.Type: GrantFiled: October 24, 2002Date of Patent: May 24, 2005Assignee: Aventis Pharmaceuticals Inc.Inventors: Michael L. Edwards, Paul J. Cox, Shelley Amendola, Stephanie D. Deprets, Timothy A. Gillespy, Christopher D. Edlin, Andrew D. Morley, Charles J. Gardner, Brian Pedgrift, Herve Bouchard, Didier Babin, Laurence Gauzy, Alain Le-Brun, Tahir N. Majid, John C. Reader, Lloyd J. Payne, Nawaz M. Khan, Michael Cherry
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Patent number: 6890945Abstract: The present invention is a method of treating sexual disturbances in humans and inducing mating in non-human mammals using the compounds of formula (A) in a dosage range where the sexually therapeutic amount is from about 0.2 thru 8 mg/person/dose and where the sexually mating amount is from about 0.003 thru 0.2 mg/kg/dose.Type: GrantFiled: July 30, 2002Date of Patent: May 10, 2005Assignee: Pharmacia & Upjohn CompanyInventors: Robert B. McCall, Martin Durham Meglasson
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Patent number: 6867208Abstract: 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: May 13, 2002Date of Patent: March 15, 2005Assignees: 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: RE39480Abstract: A method for treating Type II diabetes by administering to an affected individual a combination of chromic tripicolinate and biotin. The two compounds are administered orally or parenterally at in daily dosages which provide between 50 and 1,000 ?g of chromium and between 25 ?g and 200 mg biotin, the amounts of chromium and biotin being selected together to provide a greater than additive effect.Type: GrantFiled: July 24, 2001Date of Patent: January 23, 2007Assignee: Nutrition 21, Inc.Inventor: Mark F. McCarty