At Least Three Ring Hetero Atoms In The Bicyclo Ring System (e.g., Furo- Imidazole, (1,2-a) Imidazole, Pyrazo (1,2-a) Imidazolidine, Etc.) Patents (Class 548/303.1)
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Patent number: 7750034Abstract: The present invention is directed to novel substituted aminocyclohexanes of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: January 19, 2007Date of Patent: July 6, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Tesfaye Biftu, Jason Cox, Danqing Feng, Anthony Mastracchio, Xiaoxia Qian, Ann E. Weber
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Publication number: 20100160330Abstract: The present invention is directed to novel bicyclic heterocycles, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: ApplicationFiled: October 15, 2009Publication date: June 24, 2010Inventors: Xuqing Zhang, Zhihua Sui
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Patent number: 7741355Abstract: 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: GrantFiled: February 15, 2007Date of Patent: June 22, 2010Assignee: Dendreon CorporationInventors: Ofir Moreno, Sateesh Natarajan, David F. Duncan
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Publication number: 20100056592Abstract: A prodrug that has a prodrug moiety that degrades into a compound having the general Formula I with R3 being an alcoholic moiety can be useful in therapies for neurodegenerative diseases as well as cancer. Accordingly, the prodrug compounds can have a structure of Formula I, analogs thereof, derivatives thereof, or salts thereof, wherein: A and B are sulfur or oxygen; R1 and R2, in para, meta, or ortho position, are independently halogen, alkyl, alkoxy, haloalkyl, where R1 and R2 independently are straight chain, branched, substituted or unsubstituted; and R3 is a prodrug moiety. As examples, the prodrug can have a structure of any of Formulas I-V, which as shown in the specification.Type: ApplicationFiled: August 10, 2009Publication date: March 4, 2010Inventors: Roger A. Rajewski, Mehmet Tanol, Ingrid Gunda Georg, Michelle P. McIntosh
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Patent number: 7662841Abstract: The present invention relates to compounds of formula (I) and a process for producing the same. In formula (I), X represents a halogen atom, and R1 represents group —COR2 wherein R2 represents group OM or C1-12 alkyloxy wherein M represents a hydrogen atom, an alkali metal, an alkaline earth metal, or quaternary ammonium. The use of this compound as a synthetic intermediate can realize the production of carbapenem derivatives having potent antimicrobial activity in an efficient and safe manner at low cost.Type: GrantFiled: January 19, 2006Date of Patent: February 16, 2010Assignees: Meiji Seika Kaisha, Ltd., Sagami Chemical Research CenterInventors: Eiki Shitara, Kunio Atsumi, Keiichi Ajito, Shinya Ikeda, Tadashi Katoh, Munenori Inoue, Mari Nakatani
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Patent number: 7655683Abstract: The present invention is directed to novel imidazolopyrazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: GrantFiled: February 1, 2007Date of Patent: February 2, 2010Assignee: Janssen Pharmaceutica NVInventors: Xuqing Zhang, Zhihua Sui
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Publication number: 20090291948Abstract: Acyl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed.Type: ApplicationFiled: August 3, 2009Publication date: November 26, 2009Applicant: DECODE GENETICS EHFInventors: Jasbir Singh, Mark E. Gurney, Georgeta Hategan, Peng Yu, David Zembower, Nian Zhou
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Patent number: 7622497Abstract: The present invention is directed to novel derivatives of gambogic acid and analogs thereof. The present invention also relates to the discovery that novel derivatives of gambogic acid are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: GrantFiled: December 17, 2004Date of Patent: November 24, 2009Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Songchun Jiang, Han-Zhong Zhang
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Publication number: 20090275573Abstract: Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein A and R1 to R4 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.Type: ApplicationFiled: April 16, 2009Publication date: November 5, 2009Inventors: Jean Ackermann, Kurt Amrein, Bernd Kuhn, Alexander V. Mayweg, Werner Neidhart
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Publication number: 20090270467Abstract: The present invention is directed to novel substituted aminocyclohexanes of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: January 19, 2007Publication date: October 29, 2009Applicant: MERCK & CO., INC.Inventors: Tesfaye Biftu, Jason Cox, Danqing Feng, Anthony Mastracchio, Xiaoxia Qian, Ann E. Weber
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Patent number: 7589114Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-?]imidazole-3-sulfonyl]-azetidine-carboxylic acids, esters and amides which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.Type: GrantFiled: April 4, 2006Date of Patent: September 15, 2009Assignee: Boehringer Ingelheim International GmbHInventor: Steven Richard Brunette
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Patent number: 7589115Abstract: 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 15, 2007Date of Patent: September 15, 2009Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Terence Alfred Kelly, Jin Mi Kim, René Marc Lemieux
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Patent number: 7550494Abstract: Compounds of the formula I which are useful for treating or preventing inflammatory and immune cell-mediated diseases.Type: GrantFiled: September 25, 2003Date of Patent: June 23, 2009Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Jiang-Ping Wu, Terence Alfred Kelly, Rene M. Lemieux, Daniel R. Goldberg, Jonathan Emillian Emeigh, Ronald John Sorcek
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Patent number: 7528251Abstract: The present invention concerns enantioselective preparation of sulphoxide derivatives or their salts. The method consist in performing an enantioselective oxidation of a sulphur of general formula (I) A —CH2—SB, wherein: A is a diversely substituted pyridinyl ring and B is a heterocyclic radical comprising an imidazo-pyridinyl ring, using an oxidizing agent in the presence of a titanium (IV)-based catalyst and a chiral ligand consisting of a cyclic beta or gamma-amino-alcohol, in an organic solvent, followed, if required, by salt formation with a base. The invention is useful for preparing sulphoxides useful in therapeutics.Type: GrantFiled: October 5, 2005Date of Patent: May 5, 2009Assignee: Sidem Pharma SAInventors: Avraham Cohen, Suzy Charbit, François Schutze, Frédéric Martinet, Patricia Gizecki
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Patent number: 7517897Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonic acid which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.Type: GrantFiled: May 12, 2006Date of Patent: April 14, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Magnus Carl Arne Eriksson, Rene Marc Lemieux
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Publication number: 20090088571Abstract: Disclosed is a multi-step process for preparing a compound of Formula I: wherein R1 to R3 are as defined herein. The compounds of formula I inhibit the binding of human intercellular adhesion molecules to the Leukointegrins. As a result, these compounds are useful in the treatment of inflammatory and immune cell-mediated diseases.Type: ApplicationFiled: December 5, 2008Publication date: April 2, 2009Applicants: BOEHRINGER INGELHEIM INTERNATIONAL GMBH, BOEHRINGER INGELHEIM PHARMACEUTICALS, INC.Inventors: Xiao-jun WANG, Thomas WIRTH, Thomas NICOLA, Li ZHANG, Rogelio Perez FRUTOS, Yibo XU, Dhileepkumar KRISHNAMURTHY, Laurence John NUMMY, Richard J. VARSOLONA, Chris Hugh SENANAYAKE, Jutta KROEBER, Diana REEVES
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Patent number: 7511034Abstract: Novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups are disclosed. The novel compounds are used as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species and/or excess Zn ions, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds have not only low toxicity but also similar or superior LPO inhibition activity to references. They also effectively inhibit the cerebral neuronal cell death by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.Type: GrantFiled: January 11, 2006Date of Patent: March 31, 2009Assignee: Samsung Electronics Co., Ltd.Inventors: Eu-Gene Oh, Sung-Bo Ko, Kyung-Hwa Kim, In-Kyu Chang, Dennis W. Choi, Laura L. Dugan, Jae-Young Koh, In-Jae Shin, Moo-Ho Won
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Patent number: 7498439Abstract: An improved process for the preparation of a heteroaryl acetamide from a heteroaryl ?-hydroxyacetamide is provided. The process comprises directly hydrogenating the heteroaryl ?-hydroxyacetamide in the presence of a strong acid, a halide and a catalyst wherein the molar ratio of the starting heteroaryl ?-hydroxyacetamide to water at the initiation of hydrogenolysis is at least about 2:1. In one embodiment, the heteroaryl acetamide is zolpidem and the heteroaryl ?-hydroxyacetamide is ?-hydroxyzolpidem.Type: GrantFiled: June 3, 2005Date of Patent: March 3, 2009Assignee: Mallinckrodt Inc.Inventors: Esa Jarvi, Douglas C. Miller, Frank W. Moser, Robert E. Halvachs
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Patent number: 7498354Abstract: or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of tumors and cancers.Type: GrantFiled: March 30, 2006Date of Patent: March 3, 2009Assignee: OSI Pharmaceuticals, Inc.Inventors: Andrew Philip Crew, Bijoy Panicker, Han-Qing Dong
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Publication number: 20090043106Abstract: The present invention relates to a process for the manufacture of cyclic monocarboxylic esters (lactones) and related compounds by hydrogenation of cyclic dicarboxylic acid anhydrides in the presence of metal catalysts.Type: ApplicationFiled: April 7, 2006Publication date: February 12, 2009Inventors: Werner Bonrath, Reinhard Kargo, Felix Roessler
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Patent number: 7470795Abstract: Disclosed is a multi-step process for preparing a compound of Formula I: wherein R1 to R3 are as defined herein. The compounds of formula I inhibit the binding of human intercellular adhesion molecules to the Leukointegrins. As a result, these compounds are useful in the treatment of inflammatory and immune cell-mediated diseases.Type: GrantFiled: July 25, 2005Date of Patent: December 30, 2008Assignees: Boehringer Ingelheim Pharmaceuticals, Inc., Boehringer Ingelheim International GmbHInventors: Xiao-jun Wang, Thomas Wirth, Thomas Nicola, Li Zhang, Rogelio Perez Frutos, Yibo Xu, Dhileepkumar Krishnamurthy, Laurence John Nummy, Richard J. Varsolona, Chris Hugh Senanayake, Jutta Kroeber, Diana Reeves
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Derivatives of [6,7-dihydro-5-imidazo[1,2-]imidazole-3-sulfonyl]-pyrrolidine-2-carboxylic acid amide
Patent number: 7462637Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonyl]-pyrrolidine-2-carboxylic acid amide 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: December 9, 2008Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Terence A. Kelly, Jin Mi Kim, René Marc Lemieux, Matt Aaron Tschantz -
Patent number: 7385056Abstract: An improved process for the preparation of a heteroaryl acetamide from a heteroaryl ?-hydroxyacetamide is provied. The process comprises directly hydrogenating the heteroaryl ?-hydroxyacetamide in the presence of a strong acid, a halide and a catalyst. In one embodiment, the heteroaryl acetamide is zolpidem and the heteroaryl ?-hydroxyacetamide is ?-hydroxyzolpidem.Type: GrantFiled: December 16, 2003Date of Patent: June 10, 2008Assignee: Mallinckrodt Inc.Inventors: Esa T. Jarvi, Douglas C. Miller
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Patent number: 7351481Abstract: The present invention is related to an imidazole ring-containing compound and an organic electroluminescence (EL) display device using the same. In particular, the imidazole ring-containing compound may be used alone or in combination with a dopant as a material for organic films such as an electroluminescent layer. The organic EL display device using an organic film made of the imidazole ring-containing compound has improved characteristics such as luminance, efficiency, driving voltage, and color purity.Type: GrantFiled: October 6, 2004Date of Patent: April 1, 2008Assignee: Samsung SDI Co., Ltd.Inventors: Seok-Jong Lee, Young-Kook Kim, Seok-Hwan Hwang, Seung-Gak Yang, Hee-Yeon Kim, Young-Rag Do, Joo-Han Song
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Patent number: 7253154Abstract: The invention relates to compounds of the following formula (I) or their salts: in which R1 represents OR4 or others, in which R4 is an alkyl group having 1-8 carbon atoms which may have a substituent or the like; R2 is halogen, nitro, cyano, carboxyl, or the like; R3 is hydrogen, halogen, hydroxyl, amino, carboxyl, or the like; X is NR11, oxygen, or sulfur, in which R11 is hydrogen, or an alkyl group having 1-8 carbon atom which may have a substituent; and each of Y and Z is CR12 or nitrogen, in which R12 has the same meaning as R3 above, and a xanthine oxidase inhibitor containing the compound as an active ingredient.Type: GrantFiled: November 14, 2002Date of Patent: August 7, 2007Assignee: Nippon Chemiphar Co., Ltd.Inventors: Shinichi Yoshida, Atsushi Tendo, Kunio Kobayashi, Nobutaka Mochiduki, Tomio Yamakawa, Yoriko Shinohara
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Patent number: 7241788Abstract: Compounds of Formula (I) and (II) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described hereinType: GrantFiled: May 12, 2006Date of Patent: July 10, 2007Assignee: Pfizer Inc.Inventors: Philip A. Carpino, Robert L. Dow
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Patent number: 7238699Abstract: The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.Type: GrantFiled: February 4, 2004Date of Patent: July 3, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Vivekananda M. Vrudhula, Bireshwar Dasgupta, Gene M. Dubowchik, John E. Macor
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Patent number: 7229988Abstract: The present invention provides novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups and the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species and/or excess Zn ions, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds of the invention have not only low toxicity but also similar or superior LPO inhibition activity to references. They also effectively inhibit the cerebral neuronal cell death by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.Type: GrantFiled: June 5, 2003Date of Patent: June 12, 2007Assignee: Samsung Electronics Co., Ltd.Inventors: Eu-Gene Oh, Sung-Bo Ko, Kyung-Hwa Kim, In-Kyu Chang, Dennis W. Choi, Laura L. Dugan, Jae-Young Koh, In-Jae Shin, Moo-Ho Won
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Patent number: 7211669Abstract: The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.Type: GrantFiled: January 29, 2004Date of Patent: May 1, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Vivekananda M. Vrudhula, Dmitry Zuev, Bireshwar Dasgupta
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Patent number: 7205406Abstract: An azomethine dye represented by the following Formula 1: wherein Y represents a substituent of 0.2??p?0.9, Z1 and Z2 each represent —CR1?, where R1 represents a hydrogen atom or a substituent, or —N?, L represents the group represented by the following Formula 1a, X represents an unsubstituted or substituted di-alkylamino group, R represents an unsubstituted or substituted alkyl group, and n represents an integer more than 0. wherein B represents a group of non-metallic atoms which are necessary to form a heterocyclic ring.Type: GrantFiled: July 1, 2005Date of Patent: April 17, 2007Assignee: Konica Minolta Holdings, Inc.Inventors: Emiko Kataoka, Takatugu Suzuki, Dai Ikemizu
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Patent number: 7186740Abstract: In its many embodiments, the present invention provides a novel class of imidazo[1,2-a] pyrazine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.Type: GrantFiled: September 19, 2003Date of Patent: March 6, 2007Assignee: Schering CorporationInventors: Kamil Paruch, Timothy J. Guzi, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan
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Patent number: 7153873Abstract: Salts of a bicyclic, N-acylated imidazo-3-amine or an imidazo-5-amine of the formula: addition products thereof with acids, and methods for preparing the salts and addition products. Also disclosed are pharmaceutical compositions comprising the same and methods using the pharmaceutical compositions for the treatment or prophylaxis of pain, drug or alcohol abuse, diarrhoea, gastritis, ulcers, urinary incontinence, depression, narcolepsy, overweight, asthma, glaucoma, tinnitus, itching, hyperkinetic syndrome, epilepsy, or schizophrenia, for inducing anesthesia, and for anxiolysis.Type: GrantFiled: June 6, 2006Date of Patent: December 26, 2006Assignee: Gruenenthal GmbHInventors: Matthias Gerlach, Corinna Sundermann
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Patent number: 7126006Abstract: The present invention provides novel glycoluril derivatives for use as core molecules in combinatorial chemistry. Core molecules of the present invention can contain from one to six building blocks. Preferred building blocks are substituted amine radicals. Combinatorial libraries containing such core molecules are also provided.Type: GrantFiled: May 19, 2005Date of Patent: October 24, 2006Assignee: The Scripps Research InstituteInventors: Julius Rebek, Jr., Kent E. Pryor
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Patent number: 7105564Abstract: The present invention provides novel compounds having a dual antagonistic activity against thromboxane A2 receptor and prostaglandin D2 receptor and pharmaceutical compositions comprising them. A compound of the formula (I): wherein R1 is —CH2—CH?CH—CH2—CH2—CH2—COOR2 or —CH?CH—CH2—CH2—CH2—COOR2; R2 is hydrogen or alkyl; m is 0 or 1; p is 0 or 1; X1 and X3 each is independently optionally substituted aryl or optionally substituted heteroaryl; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(?O)—, or the like, have a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor.Type: GrantFiled: March 2, 2000Date of Patent: September 12, 2006Assignee: Shionogi & Co., Ltd.Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu, Akinori Arimura
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Patent number: 6962942Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds having Formula I: or pharmaceutically acceptable salts thereof; wherein Q is phenyl, benzyl, pyridyl, thienyl, indolyl, quinolinyl, benzothienyl, biphenylyl, or imidazolyl; any of which can include one or more optional substituents independently selected from halo, trifluoromethyl, hydroxy, amino, nitro, cyano, C1 alkoxy, C1-3 alkyl, methylenedioxy, carboxamido, acetamido, or amidino; X is methylene, carbonyl, or sulfonyl; Z is methylene, ethylene, or propylene; M is methylene or ethylene; and R1 R2 and R3 are independently hydrogen or C1-3 alkyl.Type: GrantFiled: September 16, 2002Date of Patent: November 8, 2005Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Scott C. Miller, Juan José Marugán Sánchez, Kristin D. Haslow, Jonathan Hall
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Patent number: 6939973Abstract: The present invention provides novel glycoluril derivatives for use as core molecules in combinatorial chemistry. Core molecules of the present invention can contain from one to six building blocks. Preferred building blocks are substituted amine radicals. Combinatorial libraries containing such core molecules are also provided.Type: GrantFiled: February 9, 1999Date of Patent: September 6, 2005Assignee: The Scripps Research InstituteInventors: Julius Rebek, Jr., Kent E. Pryor
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Patent number: 6936631Abstract: A novel bicyclic imidazo-5-yl-amine derivative of Formula I, wherein X denotes CR5, N or S, and Y in the case where X denotes S, denotes CR6 or N and in all other cases denotes N, and methods for preparation thereof are disclosed. Also disclosed are methods for treating pain using the compound of Formula I, and pharmaceutical compositions comprising the compound of Formula I.Type: GrantFiled: August 5, 2003Date of Patent: August 30, 2005Assignee: Gruenenthal GmbHInventors: Matthias Gerlach, Corinna Maul
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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: 6888004Abstract: The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.Type: GrantFiled: January 11, 2002Date of Patent: May 3, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Gene M. Dubowchik, Vivekananda M. Vrudhula, Dmitry Zuev, Bireshwar Dasgupta, John E. Macor
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Patent number: 6884893Abstract: The invention relates to a method for selectively dissociating cyclic carboxylic acid anhydrides. According to the inventive method, a chiral amino alcohol with a tertiary amino group that may have a partially or completely bridged structure is used as the chiral auxiliary reagent.Type: GrantFiled: October 2, 2000Date of Patent: April 26, 2005Assignee: MERCK Patent GmbHInventors: Michael Schwarz, Jürgen Eckstein
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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: 6838074Abstract: The present invention describes a method of concurrent imaging in a mammal comprising: a) administering to said mammal a vitronectin receptor targeted imaging agent and a perfusion imaging agent; and b) concurrently detecting the vitronectin receptor targeted imaging agent bound at the vitronectin receptor and the perfusion imaging agent; and c) forming an image from the detection of said vitronectin targeted imaging agent and said perfusion imaging agent.Type: GrantFiled: August 7, 2002Date of Patent: January 4, 2005Assignee: Bristol-Myers Squibb CompanyInventor: Alan P. Carpenter, Jr.
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Patent number: 6838462Abstract: The present invention relates to novel heterocyclic compounds of formula (I) where A, R1, R2, Y, Z, and n are defined in the disclosure, to processes for their preparation, and to their use as crop protection agents, in particular for controlling animal pests.Type: GrantFiled: April 16, 2002Date of Patent: January 4, 2005Assignee: Bayer CropScience LPInventors: Peter Jeschke, Michael Beck, Wolfgang Krämer, Detlef Wollweber, Angelika Lubos-Erdelen, Andreas Turberg, Olaf Hansen, Hans-Dieter Martin, Piet Sauer, Christoph Erdelen
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Publication number: 20040242874Abstract: There is provided a process for the preparation of bicyclicheteroaryl carboxaldehydes having the structural Formula I where X and Y are defined in the specification 1Type: ApplicationFiled: May 12, 2004Publication date: December 2, 2004Applicant: Wyeth Holdings CorporationInventors: Michael William Winkley, Anita Wai-Yin Chan, Ivo L. Jirkovsky, Kenneth Alfred Martin Kremer, Joseph Zeldis, Antonia Aristotelevna Nikitenko, Henry Lee Strong, Tarek Mansour, Gulnaz Khafizova, Aranapakam M. Venkatesan
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Publication number: 20040235864Abstract: The present invention provides novel compounds of formula I 1Type: ApplicationFiled: April 23, 2004Publication date: November 25, 2004Inventors: Piotr Graczyk, Hiroshi Numata, Afzal Khan, Vanessa Palmer, Darren Peter Medland, Hitoshi Oinuma, Gurpreet Bhatia
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Patent number: 6815440Abstract: Cyclic and heterocyclic N-substituted &agr;-iminohydroxamic and -carboxylic acids Compounds of the formula I are suitable for preparing pharmaceuticals for the treatment of disorders in the course of which is involved an increased activity of matrix-degrading metalloproteinases.Type: GrantFiled: March 3, 2003Date of Patent: November 9, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Eckart Bartnik, Klaus-Ulrich Weithmann
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Patent number: 6812349Abstract: The invention relates to compounds of formula (2) in which R1, R2, R3 and R4 have the meanings indicated in the description, their preparation and their further reaction to give compounds of formula (1), in which A1, A2 and R4 have the meanings indicated in the description. The compounds of the formula (1) are valuable intermediates for the preparation of medicaments.Type: GrantFiled: September 23, 2003Date of Patent: November 2, 2004Assignee: Altana Pharma AGInventors: Wolf-Rüdiger Ulrich, Christian Scheufler, Thomas Fuchss, Jörg Senn-Bilfinger
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Publication number: 20040209896Abstract: The present application relates to novel heterocyclic compounds of formula (I) 1Type: ApplicationFiled: May 3, 2004Publication date: October 21, 2004Inventors: Peter Jeschke, Michael Beck, Wolfgang Kramer, Detlef Wollweber, Christoph Erdelen, Andreas Turberg, Olaf Hansen, Hans-Dieter Martin, Piet Sauer, Angelika Lubos-Erdelen
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Publication number: 20040181064Abstract: The invention provides compounds according to formula I 1Type: ApplicationFiled: February 17, 2004Publication date: September 16, 2004Inventors: Chong-Qing Sun, Lawrence Hamann, David Augeri, Yingzhi Bi, Jeffrey Robl, Yan-Ting Huang, Tammy Wang, Alexandra Holubec, Ligaya Simpkins, James C. Sutton, James J. Li
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Publication number: 20040127534Abstract: 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: ApplicationFiled: October 15, 2003Publication date: July 1, 2004Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Terence Alfred Kelly, Jin Mi Kim, Rene Marc Lemieux