The Additional Hetero Ring Is A Five-membered Nitrogen Hetero Ring Patents (Class 514/252.05)
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Publication number: 20080287444Abstract: This invention describes novel pyrazole compounds of formula III: wherein Z1, Z2, and Z3 are as described in the specification; Q is —S—, —O—, —N(R4)—, or —CH(R6)—; R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and R2 and R2? are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: ApplicationFiled: April 25, 2008Publication date: November 20, 2008Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Francoise Pierard
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Patent number: 7452882Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as obesity, hyperlipidemia, hypercholesterolemia and diabetes and other related disorders and diseases, and may be useful for other diseases such as NASH, atherosclerosis, cardiovascular diseases, hypothyroidism, thyroid cancer and other disorders and diseases related thereto.Type: GrantFiled: July 18, 2006Date of Patent: November 18, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Nancy-Ellen Haynes, Denis J. Kertesz, Sherrie Lynn Pietranico-Cole, Yimin Qian, Nathan Robert Scott, Sung-Sau So, Kshitij Chhabilbhai Thakkar, Jefferson Wright Tilley
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Patent number: 7452885Abstract: The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tangles.Type: GrantFiled: June 29, 2006Date of Patent: November 18, 2008Assignee: WyethInventors: Ping Zhou, Michael Sotirios Malamas, Yanfang Li, Albert Jean Robichaud, Dominick Anthony Quagliato
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Patent number: 7452906Abstract: Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy.Type: GrantFiled: September 5, 2002Date of Patent: November 18, 2008Assignee: SmithKline Beecham P.L.C.Inventors: Mark James Bamford, David Kenneth Dean, Antoinette Naylor, Andrew Kenneth Takle, David Matthew Wilson
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Publication number: 20080275048Abstract: Compounds of formula (I) Z-Ar1—Ar2 ??(I) wherein Z is a diazabicyclic amine, Ar1 is a 5- or 6-membered aromatic ring, and Ar2 is selected from the group consisting of an unsubstituted or substituted 5- or 6-membered heteroaryl ring; unsubstituted or substituted bicyclic heteroaryl ring; 3,4-(methylenedioxy)phenyl; carbazolyl; tetrahydrocarbazolyl; naphthyl; and phenyl; wherein the phenyl is substituted with 0, 1, 2, or 3 substituents in the meta- or para-positions. The compounds are useful in treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods for using such compounds and compositions.Type: ApplicationFiled: June 3, 2008Publication date: November 6, 2008Applicant: ABBOTT LABORATORIESInventors: Jennifer M. Frost, Jianguo Ji, Tao Li, Diana L. Nersesian, Karin R. Tietje
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Publication number: 20080269228Abstract: The present invention relates to novel hydrazide-containing compounds of Formula I or Formula II, including pharmaceutically acceptable salts, esters, or prodrugs thereof which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: April 26, 2007Publication date: October 30, 2008Inventors: JOEL D. MOORE, ERIC L. ELLIOTT, YAT SUN OR, ZHE WANG
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Publication number: 20080269236Abstract: The invention relates to 1,2,4 oxadiazole compounds and analogs thereof, represented by formula (II), and compositions and methods of use thereof.Type: ApplicationFiled: June 6, 2008Publication date: October 30, 2008Applicant: ABBOTT LABORATORIESInventors: Jianguo Ji, Chih-Lung Lee, Kevin B. Sippy, Tao Li, Murali Gopalakrishnan
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Publication number: 20080255136Abstract: The present invention relates to inhibition of viruses, e.g., HIV using pyrrolidones and compounds related to pyrrolidones. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions that inhibit HIV in a cell; as well as to methods of prophylaxis, and therapy related to HIV infection and related disease states such as AIDS.Type: ApplicationFiled: April 22, 2008Publication date: October 16, 2008Applicant: IRM LLCInventors: Baogen Wu, Yun He, Truc Nguyen, Kelli L. Kuhen, David Archer Ellis, Tao Jiang, Xiaohui He, Kunyong Yang, Badry Bursulaya
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Patent number: 7432254Abstract: Provided is a method of treating or ameliorating or preventing glaucoma, decreasing intraocular pressure or improving or amemliorting ocular accommodation in an animal, including a human comprising administering an intraocular pressure decreasing or accommodation improving amount of a compound of the formula I:Type: GrantFiled: December 31, 2001Date of Patent: October 7, 2008Assignee: Synvista Therapeutics, Inc.Inventors: John J. Egan, Dilip Wagle, Sara Vasan, Martin Gall, Stanley Bell, Edmond Joseph LaVoie
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Publication number: 20080242653Abstract: Compounds of formula (I) wherein R1, R2, R3, R3a, R3b, R4, and R5 are defined in the description, are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).Type: ApplicationFiled: December 14, 2007Publication date: October 2, 2008Inventors: Huaqing Liu, Lawrence A. Black, Youssef L. Bennani, Marlon D. Cowart, Zhenping Tian, Paul J. Brackemeyer
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Patent number: 7429581Abstract: The present invention is directed to a compound of formula I, in which R0; R1; R2; R3; R4; Q; V, G and M have the meanings indicated below. The compound of formula I is a pharmacologically active compound. It exhibits a strong anti-thrombotic effect and is suitable, for example, for the therapy and prophylaxis of a cardio-vascular disorder like a thromboembolic disease or restenosis. It is a reversible inhibitor of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore is directed to a process for the preparation of the compound of formula I, and pharmaceutical preparation comprising it.Type: GrantFiled: December 23, 2003Date of Patent: September 30, 2008Assignee: Sanofi-Aventis Deutschland GmbHInventors: Marc Nazare, Volkmar Wehner, David W. Will, Hans Matter
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Publication number: 20080207587Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I) where x, y, G, J, K, L, M, Q, W, V, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a arc defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.Type: ApplicationFiled: September 20, 2005Publication date: August 28, 2008Applicant: XENON PHARMACEUTICALS INC.Inventors: Rajender Kamboj, Zaihui Zhang, Jian-Min Fu, Serguei Sviridov, Sultan Chowdhury, Vishnumurthy Kodumuru
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Patent number: 7399765Abstract: Compounds of formula (I) Z-Ar1—Ar2??(I) wherein Z is a diazabicyclic amine, Ar1 is a 5- or 6-membered aromatic ring, and Ar2 is selected from the group consisting of an unsubstituted or substituted 5- or 6-membered heteroaryl ring; unsubstituted or substituted bicyclic heteroaryl ring; 3,4-(methylenedioxy)phenyl; carbazolyl; tetrahydrocarbazolyl; naphthyl; and phenyl; wherein the phenyl is substituted with 0, 1, 2, or 3 substituents in the meta- or para-positions. The compounds are useful in treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods for using such compounds and compositions.Type: GrantFiled: September 16, 2004Date of Patent: July 15, 2008Assignee: Abbott LaboratoriesInventors: William H. Bunnelle, Jianguo Ji, Tao Li, Jennifer M. Pace, Karin R. Tietje, Kathleen H. Mortell, Diana L. Nersesian, Michael R. Schrimpf
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Publication number: 20080167307Abstract: According to the present invention, a compound represented by the following formula (I) having a superior PPAR? agonist action and concurrently showing a hypolipidemic action can be provided, and further, a compound useful as a synthetic intermediate for the compound can be provided.Type: ApplicationFiled: November 4, 2005Publication date: July 10, 2008Applicant: Mitsubishi Phama CorporationInventors: Takashi Tozawa, Osamu Tsuruta, Hiroshi Kitajima, Yoshiyuki Aoki, Naoko Ando, Hiroki Tamakawa
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Patent number: 7396831Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritis, vitiligo, general gastrointestinal disorders, gastric ulceration, dType: GrantFiled: August 1, 2005Date of Patent: July 8, 2008Assignee: Amgen Inc.Inventors: Elizabeth M. Doherty, Jiawang Zhu, Markian Stec, Mark H. Norman, Vassil I. Ognyanov, Christopher H. Fotsch, Ning Chen, Partha P. Chakrabarti, Liping H. Pettus, Hui-Ling Wang, Xianghong Wang, Premilla Arasasingham
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Publication number: 20080161310Abstract: The present invention relates to new, potent DPP-IV enzyme inhibitors of the general formula (I), which contain fluorine atoms.Type: ApplicationFiled: March 5, 2008Publication date: July 3, 2008Applicant: Sanofi-AventisInventors: Peter Aranyi, Laszlo Balazs, Imre Bata, Sandor Batori, Eva Boronkay, Philippe Bovy, Karoly Kanai, Zoltan Kapui, Edit Susan, Tibor Szabo, Lajos T. Nagy, Katalin Urban-Szabo, Marton Varga
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Publication number: 20080153838Abstract: The invention relates to a compound of the Formula I. or salt, prodrug or solvate thereof, wherein R1, R5, R6, D, A, B, L, n, m and p are as defined in the description. The invention also relates to pharmaceutical compositions of said compounds, the use of said compounds as medicaments and in the production of an anti-angiogenic effect in a warm-blooded animal. The invention also relates to processes for the preparation of said compounds.Type: ApplicationFiled: February 2, 2006Publication date: June 26, 2008Applicant: ASTRAZENECA ABInventors: Clifford David Jones, Richard Williams Arthur Luke, William McCoull
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Publication number: 20080125436Abstract: The present invention is directed to compounds of formula I: Wherein R1 to R5, X and Z are further defined in the description. The invention also relates to processes for the preparation of the compounds and to intermediates used in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.Type: ApplicationFiled: September 25, 2007Publication date: May 29, 2008Applicant: AstraZeneca ABInventors: Methvin Isaac, Abdelmalik Slassi, Louise Edwards, Peter Dove, Tao Xin, Tomislav Stefanac
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Publication number: 20080125432Abstract: The present invention relates to compounds that interact with ion channels. In particular, the invention relates to compounds having the structural Formula having the structural Formula I, II, III or IV, stereoisomers, tautomers, racemics, prodrugs, metabolites thereof, or a pharmaceutically acceptable salt and/or solvate thereof, wherein X, Y1, Y2, R1, n, R3, R8, R9, R10, L1, L2, Ar1 and Ar2 are defined in claim 1. The invention also relates to methods for preparing said compounds, to pharmaceutical compositions comprising said compounds, and to the use of said compounds in methods for treatment of the human and animal body.Type: ApplicationFiled: December 1, 2005Publication date: May 29, 2008Applicant: Devgen NVInventors: Petra Blom, Jan Octaaf De Kerpel, Eric Pierre Paul Rene Fourmaintraux, Titus Jan Kaletta, Dirk Leysen
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Publication number: 20080119476Abstract: Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.Type: ApplicationFiled: July 1, 2005Publication date: May 22, 2008Inventors: Amjad Ali, Joann M. Napolitano, Qiaolin Deng, Zhijian Lu, Peter J. Sinclair, Gayle E. Taylor, Christopher F. Thompson, Nazia Quraishi, Cameron J. Smith, Julianne A. Hunt, Adrian A. Dowst, Yi-Heng Chen, Hong Li
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Publication number: 20080113990Abstract: Biphenyl derivatives useful as ion channel antagonists are disclosed herein. The compositions thereof are useful for treating or relieving pain-related conditions.Type: ApplicationFiled: October 12, 2006Publication date: May 15, 2008Inventors: Esther Martinborough, Danielle Lehsten, Timothy Neubert, Aarti Sameer Kawatkar, Nicole Zimmermann, Andreas Termin
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Patent number: 7361654Abstract: The present invention relates to new class of non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory- and immune-associated diseases, and have the structure including all stereoisomers thereof, tautomers thereof, or a prodrug thereof, or a pharmaceutically acceptable salt thereof, wherein X is selected from N, O, and S; Y is N or CR6; Z is a ring; and where R, Ra, Rb, Rc, Rd, R1, R2, R3, R4, and R5 are as defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising such compounds.Type: GrantFiled: January 12, 2006Date of Patent: April 22, 2008Assignee: Bristol-Myers Squibb Co.Inventors: James Sheppeck, T. G. Murali Dhar, Lidia Doweyko, John Gilmore, David Weinstein, Hai-Yun Xiao, Bingwei V. Yang, Arthur M. Doweyko
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Publication number: 20080081815Abstract: A novel heteroaryl-pyrazole compound of formula (I) or a pharmaceutically acceptable salt thereof is effective as a cannabinoid CB1 receptor inverse agonist or antagonist, which is useful for preventing or treating obesity and obesity-related metabolic disorders. The prevention also provide a method for preparing same, a pharmaceutical composition containing same, and a method for preventing or treating obesity and obesity-related metabolic disorders.Type: ApplicationFiled: September 29, 2006Publication date: April 3, 2008Applicant: GREEN CROSS CorporationInventors: Jinhwa Lee, Jeong Min Kim, Chong-Hwan Jonathan Chang, Suk Youn Kang, Hee Jeong Seo, Kwang-Seop Song, Sung-Han Lee, Kwang-Woo Ahn
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Publication number: 20080076771Abstract: A compound of the formula (I) useful as promoters of thrombopoiesis and megakaryocytopoiesis, wherein A, B, D, E, W, X, Y, Z, R1 and R2 are defined as above.Type: ApplicationFiled: September 12, 2005Publication date: March 27, 2008Inventors: Lawrence A. Reiter, Robert G. Linde
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Publication number: 20080044379Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: August 8, 2007Publication date: February 21, 2008Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Lawrence G. Hamann
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Patent number: 7323480Abstract: The present invention is directed to certain novel triazole compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof. The present invention is also directed to methods of making and using such compounds and pharmaceutical compositions containing such compounds to treat or control a number of diseases mediated by PPAR such as glucose metabolism, lipid metabolism and insulin secretion, specifically Type 2 diabetes, hyperinsulemia, hyperlipidemia, hyperuricemia, hypercholesteremia, atherosclerosis, one or more risk factors for cardiovascular disease, Syndrome X, hypertriglyceridemia, hyperglycemia, obesity, and eating disorders.Type: GrantFiled: May 24, 2005Date of Patent: January 29, 2008Assignee: Metabolex, Inc.Inventors: Yan Zhu, Jingyuan Ma, Peng Cheng, Zuchun Zhao, Francine M. Gregoire, Vera A. Rakhmanova
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Publication number: 20080015198Abstract: The present invention relates to substitute pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.Type: ApplicationFiled: February 16, 2005Publication date: January 17, 2008Applicant: LABORATORIOS DEL DR.ESTEVE S.A.Inventor: Rosa Cuberes Altisen
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Patent number: 7309701Abstract: The present invention relates to novel pyridazinone derivatives of the general formula (I) wherein A is A1 or A2; R is unsubstituted or at least monosubstituted C1-C10-alkyl, aryl, aryl-(C1-C10-alkyl)-, heteroaryl, heteroaryl-(C1-C10-alkyl)-, heterocyclyl, heterocyclyl-(C1-C10-alkyl)-, C3-C10-cycloalkyl, polycycloalkyl, C2-C10-alkenyl or C2-C10-alkinyl and Ar is unsubstituted or at least monosubstituted aryl or heteroaryl.Type: GrantFiled: November 19, 2003Date of Patent: December 18, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Swen Hölder, Thorsten Naumann, Karl Schönafinger, David William Will, Hans Matter, Günther Müller, Dominique Le Suisse, Bernard Baudoin, Thomas Rooney, Franck Halley, Gilles Tiraboschi
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Patent number: 7288542Abstract: The present invention relates to a compounds according to formula I, methods for treating diseases mediated by human immunodeficieny virus by administration of a compound according to formula I and pharmaceutical compositions for treating diseases mediated by human immunodeficieny virus containing a compound according to formula I where R1, R2, R3, R4, R5, R6, R7 and R8 are as defined hereinType: GrantFiled: March 22, 2005Date of Patent: October 30, 2007Assignee: Roche Palo Alto LLCInventors: James Patrick Dunn, Todd Richard Elworthy, Joan Heather Hogg, Dimitrios Stefanidis
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Patent number: 7259175Abstract: The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts thereof, Formula I: wherein: (a) R5 is selected from the group consisting of (C1-C6) alkyl, (C1-C6) alkenyl, substituted aryl(C0-C4)alkyl, substituted aryloxy(C0-C4)alkyl, substituted arylthio(C0-C4)alkyl, unsubstituted aryl(C0-C4)alkyl, unsubstituted aryloxy(C0-C4)alkyl, and unsubstituted arylthio(C0-C4)alkyl; (b) T1 is C or N; (c) Q is selected from the group consisting of O, a single bond, O(CH2)q and C; (d) q is 1 or 2; (e) W is selected from the group consisting of O, S, (CH2)rN(R20)(CH2)k, NHSO2, C(O)N(R20)(CH2)r, (CH2)rN(R20)C(O), and SO2; (f) X is CmH2m; (g) m is 0, 1 or 2; (h) A is an functional group selected from the group consisting of carboxyl, C1-C3 alkylnitrile, carboxamide, and (CH2)n COOR19; and (i) R19 is selected from the group consisting of hydrogen, optionally substituted C1-C4alkyl and optionally substituted arylmethylType: GrantFiled: February 13, 2003Date of Patent: August 21, 2007Assignee: Eli Lilly and CompanyInventors: Scott Eugene Conner, Nathan Bryan Mantlo, Guoxin Zhu
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Patent number: 7253170Abstract: The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where W, X, R1, R2, R3, R4, R5, R6 and m are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.Type: GrantFiled: June 28, 2006Date of Patent: August 7, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Alaric J. Dyckman, Jagabandhu Das, Katerina Leftheris, Chunjian Liu, Robert V. Moquin, Stephen T. Wrobleski
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Patent number: 7253169Abstract: The present invention relates to N-substituted cyclic aza compounds, pharmaceutical compositions comprising such compounds, and methods of their use for effecting neuronal activities.Type: GrantFiled: April 17, 2001Date of Patent: August 7, 2007Assignee: Gliamed, Inc.Inventors: Yong-Qian Wu, Wei Huang, Gregory S. Hamilton
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Patent number: 7241760Abstract: The present invention relates to imidazole derivatives of the general formula wherein R1, R2, R3 and R4 are described hereinbelow. These compounds can be used in the treatment or prevention of mGluR5 receptor mediated disorders. These compounds are useful, interalia, in the treatment or prevention of acute and/or chronic neurological disorders such as psychosis, epilepsy, schizophrenia, Alzheimer's disease, cognitive disorders and memory deficits, as well as chronic and acute pain.Type: GrantFiled: June 12, 2004Date of Patent: July 10, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Buettelmann, Simona Maria Ceccarelli, Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira
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Patent number: 7214678Abstract: According to the invention there is provided a compound the formula I; wherein A, X, B, R1, R2, R3 and R4 are as defined in the specification.Type: GrantFiled: June 1, 2006Date of Patent: May 8, 2007Assignee: Allergan, Inc.Inventors: Robert M. Burk, Sophie Beauchemin
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Patent number: 7186722Abstract: Novel ?1-pyrrolines of the Formula (I) in which R1, R2, R3 and Het have the meanings given in the description, a plurality of processes for preparing these compounds and their use for controlling pests, and also novel intermediates and processes for their preparation.Type: GrantFiled: January 31, 2002Date of Patent: March 6, 2007Assignee: Bayer Cropscience AGInventors: Andrew Plant, Rüdiger Fischer, Thomas Seitz, Christoph Erdelen, Andreas Turberg, Olaf Hansen
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Patent number: 7179812Abstract: The present invention provides compounds of formula (I): their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.Type: GrantFiled: March 31, 2005Date of Patent: February 20, 2007Assignee: Hoffmann-la Roche Inc.Inventors: Birgit Bossenmaier, Walter-Gunar Friebe, Wolfgang Jenni, Matthias Rueth, Edgar Voss
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Patent number: 7179806Abstract: The invention relates to novel ?1-pyrrolines of the formula (I) in which R1, R2, R3, m, and Q have the meanings given in the disclosure, to a plurality of processes for preparing these substances, and to their use for controlling pests.Type: GrantFiled: November 22, 2001Date of Patent: February 20, 2007Assignee: Bayer Cropscience AGInventors: Andrew Plant, Thomas Seitz, Johannes Rudolf Jansen, Christoph Erdelen, Andreas Turberg, Olaf Hansen
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Patent number: 7135471Abstract: Aryl oxime derivatives of the formula (I), in which R1, R2, R3, X and B are as defined in claim 1, act as phosphodiesterase IV inhibitors and can be employed for the treatment of osteoporosis, tumours, cachexia, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases, myocardial diseases and AIDSType: GrantFiled: May 16, 2003Date of Patent: November 14, 2006Assignee: Merck Patent GmbHInventors: Hans-Michael Eggenweiler, Norbert Beier, Pierre Schelling, Michael Wolf
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Patent number: 7129241Abstract: Pyridazine derivatives of the formula (I) act as phosphodiesterase IV inhibitors and can be employed for the treatment of osteoporosis, tumours, cachexia, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases, myocardial diseases and AIDSType: GrantFiled: May 12, 2003Date of Patent: October 31, 2006Assignee: Merck Patent GesellschaftInventors: Hans-Michael Eggenweiler, Michael Wolf
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Patent number: 7091343Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: March 14, 2003Date of Patent: August 15, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Hayley Binch, Jean-Damien Charrier, Simon Everitt, Julian M. C. Golec, David Kay, Ronald Knegtel, Andrew Miller, Francoise Pierard
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Patent number: 7074785Abstract: Novel ?1-pyrrolines of the formula (I) in which R1, R2, R3, A, R4 and m have the meanings given in the description, a number of processes for preparing these substances, and their use for controlling pests, and also novel intermediates and their preparation.Type: GrantFiled: September 4, 2002Date of Patent: July 11, 2006Assignee: Bayer Cropscience AGInventors: Thomas Seitz, Martin Füsslein, Johannes Rudolf Jansen, Udo Kraatz, Angelika Lubos-Erdelen, legal representative, Andreas Turberg, Olaf Hansen, Christoph Erdelen, deceased
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Patent number: 7022706Abstract: Pharmaceutical compositions incorporate compounds that are capable of affecting nicotinic cholinergic receptors. A wide variety of conditions and disorders, and particularly conditions and disorders associated with dysfunction of the central and autonomic nervous systems can be treated using pharmaceutical compositions incorporating compounds in which an aromatic ring is bridged with an ethylenic or acetylenic unit to an azabicyclic moiety.Type: GrantFiled: September 23, 2003Date of Patent: April 4, 2006Assignee: Targacept, Inc.Inventors: Thomas Jeffrey Clark, Balwinder Singh Bhatti
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Patent number: 7022705Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein, for example, HET is an N-linked 5-membered, fully or partially unsaturated heterocyclic ring, or HET is an N-linked 6-membered di-hydro-heteroaryl ring; Q is, for example, Q1 or Q2: wherein R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example a group of the formula (TC7) wherein Rc is, for example, hydrogen, R13CO—, R13SO2— or R13CS—; wherein R13 is, for example, optionally substituted (1–10C)alkyl or R14C(O)O(1–6C)alkyl wherein R14 is optionally substituted (1–10C)alkyl; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.Type: GrantFiled: October 23, 2002Date of Patent: April 4, 2006Assignee: AstraZeneca ABInventor: Michael John Betts
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Patent number: 7005432Abstract: The present invention relates to compounds of formula wherein A is an unsubstituted or substituted cyclic group; and R is hydrogen or lower alkyl; or a pharmaceutically acceptable acid addition salt thereof. These compounds are NMDA NR-2B receptor subtype specific blockers and are useful in the treatment of neurodegeneration, depression and pain.Type: GrantFiled: May 9, 2003Date of Patent: February 28, 2006Assignee: Hoffman-La Roche Inc.Inventors: Bernd Buettelmann, Marie-Paule Heitz Neidhart, Georg Jaeschke, Emmanuel Pinard
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Patent number: 6995261Abstract: Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: wherein R1 is a halogen, or an oxygen linked leaving group including an aromatic ether, an alkyl sulfonate, an aryl sulfonate, an alkyl phosphonate, an aryl phosphonate, an alkyl phosphate or aryl phosphate; R2 is COOR5, C(?O)NH(CHR5)m—COOR5, NH(CHR5)mCON(R5)R6, C(?O)N(R5)R6 or NH(CHR5)mOH; R3 is H or alkyl; R4 is H, substituted or unsubstituted aryl, heteroaryl or alkyl; R5 and R6 are independently H, lower alkyl, aryl, hydroxy alkyl, amino alkyl, heteroaryl, lower alkylene-aryl, lower alkylene-heteroaryl or lower cycloalkyl; and m=0–6; pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1? protease activity in a mammal utilizing the compounds and compositions.Type: GrantFiled: September 22, 2003Date of Patent: February 7, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: Roland E. Dolle, Denton W. Hoyer, Tina Morgan Ross, James M. Rinker, Stanley J. Schmidt, Mark A. Ator
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Patent number: 6991801Abstract: This invention provides for inter alia, topical anthelmintic formulations which comprise a pharmaceutically active combination consisting of at least one macrocyclic compound and at least one compound selected from the group consisting of praziquantel, morantel and pyrantel, which are dissolved in a non-aqueous solvent or solvent mixture and optionally a thickening agent.Type: GrantFiled: April 5, 2004Date of Patent: January 31, 2006Assignee: Merial LimitedInventors: Mark D. Soll, Krishan Kumar, Robert P. Waranis, Natalya Shub
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Patent number: 6919329Abstract: The present invention provides antibacterial agents having the formulae I, II, and III described herein.Type: GrantFiled: February 24, 2003Date of Patent: July 19, 2005Assignee: Pharmacia & Upjohn CompanyInventors: Richard Charles Thomas, Toni-Jo Poel, Michael Robert Barbachyn, Mikhail F. Gordeev, Gary W. Luehr, Adam Renslo, Upinder Singh
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Patent number: 6919323Abstract: aP2 inhibiting compounds are provided having the formula wherein A, X, R and Z are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing such aP2 inhibitors alone or in combination with other therapeutic agents, including other antidiabetic agent such as metformin, glyburide, troglitazone and/or insulin.Type: GrantFiled: July 12, 2002Date of Patent: July 19, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Richard Sulsky, Jeffrey A. Robl
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Patent number: 6878709Abstract: Disclosed are compounds of the formula (I) or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.Type: GrantFiled: January 2, 2003Date of Patent: April 12, 2005Assignees: Schering Corporation, Pharmacopeia Drug Discovery, Inc.Inventors: Arthur G. Taveras, Michael Dwyer, Jianping Chao, John J. Baldwin, J. Robert Merritt, Ge Li, Jianhua Chao, Younong Yu
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Patent number: 6869945Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N?(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; -G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems reType: GrantFiled: November 20, 2002Date of Patent: March 22, 2005Assignee: Pfizer IncInventors: Anthony Marfat, Michael William McKechney