Polycyclo Ring System Having The Thiazole Ring As One Of The Cyclos Patents (Class 514/366)
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Patent number: 7300949Abstract: This invention concerns novel thiazolopyrazole compounds and compositions comprising them. Methods of using these compounds for the treatment, prevention and management of various diseases and disorders are also encompassed by the invention.Type: GrantFiled: March 31, 2005Date of Patent: November 27, 2007Assignee: Lexicon Pharmaceuticals, Inc.Inventors: Joseph Barbosa, Cynthia A. Fink, Spencer D. Kimball, Hartmuth Kolb, Zhi-Cai Shi, Ashok R. Tunoori
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Patent number: 7294641Abstract: Heterocyclic compounds useful for stimulating/inducing the growth of keratinous fibers, notably human hair/eyelashes, and/or slowing the loss of same, have the following structural formula (I) or salt thereof: in which Hy is a heterocycle of 4 to 7 atoms, optionally comprising carbonyl/thiocarbonyl functional groups, and G is O, S or NH.Type: GrantFiled: September 29, 2003Date of Patent: November 13, 2007Assignee: L'OrealInventors: Christophe Boulle, Roger Rozot, Maria Dalko
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Patent number: 7250429Abstract: This invention relates to the provision of novel aminomethyl-substituted thiazolobenzimidazole derivatives represented by the following general formula (I) or a salt thereof. The aforementioned derivative or a salt thereof has a metabotropic glutamate receptor action and excellent oral activity and is therefore useful as a medicament. (In the formula, R1: an oxygen-containing saturated hetero ring or the like, Alk1: a lower alkylene, m: 0 or 1, Alk2: a lower alkylene which may be substituted with oxo group, n: 0 or 1, X: a bond, O, S or NR5, R3: H or the like, and R2, R4, R5, R6 and R7: the same or different from one another and each represents H or the like. Provided that R3 does not represent a lower alkyl or a halogeno-lower alkyl when X is a bond and n is 1. Also, R4 represents a group other than Me when m is 1, R1 is OH or OMe and Alk1 is a C1-3 alkylene, and further 1) when X is a bond, n is 1 and R3 is H, or 2) when X is a bond, n is 0 and R3 is cyclohexane.Type: GrantFiled: March 19, 2003Date of Patent: July 31, 2007Assignee: Astellas Pharma Inc.Inventors: Hirotsune Itahana, Jiro Fujiyasu, Satoshi Hayashibe, Toshihiro Watanabe, Masamichi Okada, Takashi Toya
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Patent number: 7247635Abstract: Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-dependent calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-dependent calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning: B: phenylene, a nitrogen-containing, divalent, saturated ring group, or a monocyclic, divalent heteroaromatic ring group which may be substituted with Alk, X: —NR1—CR2R3—, —CR2R3—NR1—, —NR1—SO2—, —SO2—NR1— or —CR4?CR5—, and A: benzene ring which may have one or more substituents; mono-, di- or tricyclic fused heteroaryl which may have one or more substituents; cycloalkyl which may have one or more substituents; a nitrogen-containing, saturated ring group which may have one or more substituents; lower alkenyl which may have one or more substituents; lower alkynyl which may have one or more substituents; or Alk which may have one or more sType: GrantFiled: June 17, 2005Date of Patent: July 24, 2007Assignee: Astellas Pharma Inc.Inventors: Hirokazu Kubota, Yasuhiro Yonetoku, Keizo Sugasawa, Masashi Funatsu, Souichirou Kawazoe, Akira Toyoshima, Yoshinori Okamoto, Jun Ishikawa, Makoto Takeuchi
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Patent number: 7241755Abstract: The present invention relates to compounds of the formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1–R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.Type: GrantFiled: August 30, 2006Date of Patent: July 10, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Gregory D. Vite, Soong-Hoon Kim, Robert M. Borzilleri, James A. Johnson
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Patent number: 7230019Abstract: This invention relates to compounds of Formula (I) and the use of compounds of Formula (I) as neuroprotective agents in the treatment of neuronal disorders of the central and peripheral nervous systems.Type: GrantFiled: December 16, 2002Date of Patent: June 12, 2007Assignee: Aegera Therapeutics, Inc.Inventors: James B. Jaquith, Gerald Villeneuve, Alain Boudreault, Stephen Morris, Jon Durkin, John W. Gillard, Kimberly Hewitt, H. Nicholas Marsh
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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: 7132436Abstract: The present invention relates to compounds with the formula (I) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.Type: GrantFiled: May 22, 2001Date of Patent: November 7, 2006Assignee: Biovitrum ABInventors: Guido Kurz, Marianne Nilsson
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Patent number: 7125887Abstract: Pyrrolidine compounds of Formula (I), (wherein R1, R2, R3, R4, R5, R6a, R6b, R7 and R8 are defined herein) are described. The compounds are modulators of CCR5 chemokine receptor activity. The compounds are useful, for example, in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: October 9, 2001Date of Patent: October 24, 2006Assignee: Merck & Co., Inc.Inventors: Jeffrey J. Hale, Charles G. Caldwell, Dooseop Kim, Dong-Ming Shen, Sander G. Mills, Kevin T. Chapman, Liya Chen, Malcolm MacCoss, Amy Gentry, Christopher L. Lynch, Yuan Cheng, legal representative, Christopher A. Willoughby, deceased
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Patent number: 7115632Abstract: A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity. A contemplated compound corresponds in structure to the formula wherein W and the R groups are defined elsewhere.Type: GrantFiled: May 11, 2000Date of Patent: October 3, 2006Assignee: G. D. Searle & Co.Inventors: Louis J Bedell, Joseph J McDonald, Thomas E Barta, Daniel P Becker, Rao N Shashidhar, John N Freskos, Brent V Mischke, Daniel P Getman, Gary A DeCrescenzo, Clara I Villamil
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Patent number: 7078400Abstract: The present invention relates to an inhibitor for production of 20-hydroxyeicosatetraenoic acid, comprising, as an effective ingredient, specific hydroxyformamidine derivatives or pharmaceutically-acceptable salts thereof. The inhibitors according to the present invention are useful as therapeutic agents for kidney diseases, cerebrovascular diseases, or circulatory diseases. In addition, the present invention also provides novel hydroxyformamidine derivatives or pharmaceutically-acceptable salts thereof.Type: GrantFiled: July 1, 2003Date of Patent: July 18, 2006Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
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Patent number: 7067516Abstract: Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.Type: GrantFiled: December 12, 2001Date of Patent: June 27, 2006Assignee: Tularik LimitedInventors: Sarah Elizabeth Lively, Martin James Harrison, Neil Jason Naylor, Christopher Neil Farthing, Bohdan Waszkowycz
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Patent number: 7022721Abstract: In one embodiment, the present invention relates to compounds and compositions including pharmaceutical compositions containing the compounds and associated methods that uncouple sugar-mediated coupling of proteins, lipids, nucleic acids, and other biomaterials, and any combination thereof. In another embodiment, the compositions and associated methods have utility in vivo to reduce the deleterious effects of sugar-mediated coupling processes in an organism, when the organism is exposed to the compound or composition internally, by ingestion, transdermal application, or other means. In yet another embodiment, the compositions and associated methods are useful for the ex-vivo treatment of organs, cells and tissues and external treatment of hair, nails and skin to rejuvenate them by changing deformability and increase the tissue diffusion coefficient. In a further embodiment, the present invention relates to novel compounds and pharmaceutical compositions.Type: GrantFiled: March 8, 2004Date of Patent: April 4, 2006Inventors: Peter C Ulrich, Sheng Ding Fang, Michael L Brines, Qiao-Wen Xie, Anthony Cerami
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Patent number: 7022720Abstract: The application discloses novel synthetic compounds, modeled after unique toxins extracted from the marine invertebrate Diazona angulata useful in the treatment abnormal cell mitosis. The application also discloses novel methods for synthesis of these compounds and methods of using these compounds.Type: GrantFiled: August 23, 2002Date of Patent: April 4, 2006Assignee: Board of Regents, The University of Texas SystemInventors: Patrick G. Harran, Jing Li, Susan Jeong
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Patent number: 7008956Abstract: The therapeutic use of temporary p53 inhibitors in the treatment of p53-mediated diseases, conditions, and injuries is disclosed.Type: GrantFiled: January 28, 2003Date of Patent: March 7, 2006Assignee: The Board of Trustees of the University of IllinoisInventors: Andrei V. Gudkov, Pavel G. Komarov, Elena A. Komarova
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Patent number: 6989379Abstract: This invention is directed to triazine derivatives, bicyclic compounds and tricyclic compounds which are selective antagonists for a NPY (Y5) receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of this invention and a pharmaceutically acceptable carrier. This invention provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The invention further provides the use of a compound of the invention for the preparation of a pharmaceutical composition for treating an abnormality, wherein the abnormality is alleviated by decreasing the activity of a human Y5 receptor.Type: GrantFiled: April 21, 2000Date of Patent: January 24, 2006Assignee: H. Lundbick A/SInventors: Mohammad R. Marzabadi, Wai C. Wong, Stewart A. Noble, Manesh N. Desai
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Patent number: 6936628Abstract: The invention relates to methods of increasing the bioavailability of orally administered epothilones. Epothilones administered by the methods of the invention are sufficiently bioavailable to have a pharmacological effect. The invention further relates to pharmaceutical compositions, pharmaceutical dosage forms, and kits for use in the methods of the invention.Type: GrantFiled: April 1, 2003Date of Patent: August 30, 2005Assignee: Bristol-Myers Squibb CompanyInventor: Francis Y. F. Lee
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Patent number: 6887877Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating Flaviviridae viral infection.Type: GrantFiled: June 11, 2002Date of Patent: May 3, 2005Assignee: ViroChem Pharma Inc.Inventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen Ba, Oswy Z. Pereira, Stephen Joseph Shuttleworth, Mohammad Arshad Siddiqui, Wuyi Wang
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Patent number: 6864254Abstract: An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular diseases, or circulatory diseases. The novel hydroxyformamidine derivative or pharmacologically acceptable salt thereof is also provided.Type: GrantFiled: November 1, 2000Date of Patent: March 8, 2005Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
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Patent number: 6858607Abstract: The present invention is directed to substituted 4H-chromene and analogs thereof, represented by the general Formula I: or pharmaceutically acceptable salts or prodrugs thereof, wherein: wherein A, R1, R2, R5, X, Y, and Z, are defined herein and B is a fused thiazole, oxazole, 2-imino-imidazole, 2,1,3-thiadiazo-2-one, thiazol-2-one, oxazol-2-one, imidazol-2-thione, thiazol-2-thione, oxazol-2-thione, imidazoline, oxazoline, thiazoline, triazole, oxazine, oxazine-2,3-dione, or piperazine ring. The present invention also relates to the discovery that compounds having Formula I 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: May 16, 2002Date of Patent: February 22, 2005Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Lifen Xu, Richard Storer, Giorgio Attardo
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Publication number: 20040259896Abstract: The present invention provides a compound of Formula I or Formula II: 1Type: ApplicationFiled: April 23, 2004Publication date: December 23, 2004Inventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Fenglei Zhang, Brian Metcalf
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Publication number: 20040229324Abstract: The invention relates to an enzymatic process for the production of an intermediate, bicyclic-heteroaryl-2-carboxylic acid, of the formula 1Type: ApplicationFiled: May 12, 2004Publication date: November 18, 2004Applicant: Wyeth Holdings CorporationInventors: Ramesh Venkat Matur, Mark Edward Ruppen
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Publication number: 20040223913Abstract: Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.Type: ApplicationFiled: December 23, 2003Publication date: November 11, 2004Applicant: Mallinckrodt, Inc.Inventors: Samuel Achilefu, Raghavan Rajagopalan, Richard B. Dorshow, Joseph E. Bugaj, Muthunadar P. Periasamy
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Publication number: 20040213740Abstract: Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.Type: ApplicationFiled: January 2, 2004Publication date: October 28, 2004Applicant: Mallinckrodt Inc.Inventors: Samuel Achilefu, Raghavan Rajagopalan, Richard B. Dorshow, Joseph E. Bugaj, Hermo N. Jimenez, Muthunadar P. Periasamy
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Patent number: 6759422Abstract: The present invention relates to ion channel modulating agents. More particularly, the present invention relates to a particular class of chemical compounds represented by general formula (I) that has proven useful as modulators of SKCa, IKCa and BKCa channels. In further aspects, the present invention relates to the use of these SK/IK/BK channel modulating agents for the manufacture of medicaments and pharmaceutical compositions comprising the SK/IK/BK channel modulating agents. The SK/IK/BK channel modulating agents of the invention are useful for the treatment or alleviation of diseases and conditions associated with the SK/IK/BK channels.Type: GrantFiled: August 2, 2002Date of Patent: July 6, 2004Assignee: Neurosearch A/SInventors: Bo Skaaning Jensen, Lene Teuber, Dorte Strobaek, Palle Christophersen, Soren Peter Olesen
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Publication number: 20040106597Abstract: Novel fused indazoles and indoles are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions containing one or more of the compounds of the present invention.Type: ApplicationFiled: November 25, 2003Publication date: June 3, 2004Inventors: Jesse A. May, Anura P. Dantanarayana
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Patent number: 6743785Abstract: The present invention provides selective kinase inhibitors of formula (I).Type: GrantFiled: May 21, 2002Date of Patent: June 1, 2004Assignee: Eli Lilly and CompanyInventors: Rima Salim Al-Awar, Kyle Andrew Hecker, Jianping Huang, Sajan Joseph, James Edward Ray, Philip Parker Waid
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Publication number: 20040063764Abstract: Compounds of the general formula (III), prodrugs thereof, pharmaceutically acceptable salts of both, or solvates of them and exhibiting thrombopoietin receptor agonism: 1Type: ApplicationFiled: July 25, 2003Publication date: April 1, 2004Inventors: Hiroshi Takemoto, Masami Takayama, Takeshi Shiota
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Publication number: 20040053923Abstract: This invention relates to compounds represented by the general formula [I] 1Type: ApplicationFiled: April 8, 2003Publication date: March 18, 2004Applicant: Banyu Pharmaceutical Co., Ltd.Inventors: Toshio Nagase, Tomoharu Iino, Yoshiyuki Sato, Teruyuki Nishimura, Jun-Ichi Eiki
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Patent number: 6706744Abstract: Novel compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism and obesity.Type: GrantFiled: November 16, 2001Date of Patent: March 16, 2004Assignee: Novo Nordisk A/SInventors: Peter Madsen, Jesper Lau, Anthony Ling
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Patent number: 6689777Abstract: The present invention is directed to substituted naphthothiazolium, aromatic guanylhydrazones, and other compounds and compositions with anti-malarial activity useful for the treatment and prophylaxis of malaria. The compounds are provided for the treatment of malaria or the sequelae of malarial infection, for depolymerizing malaria pigment (hemozoin), and for ameliorating the adverse effects of hemozoin on host cells.Type: GrantFiled: October 23, 2002Date of Patent: February 10, 2004Assignee: Kenneth S. Warren InstituteInventors: Peter C. Ulrich, Anthony Cerami
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Publication number: 20040009976Abstract: This invention relates to certain novel imidazoline compounds and analogues thereof, to their use for the treatment of diabetes, diabetic complications, metabolic disorders, or related diseases where impaired glucose disposal is present, to pharmaceutical compositions comprising them, and to processes for their preparation.Type: ApplicationFiled: April 30, 2002Publication date: January 15, 2004Inventors: Kumiko Takeuchi, Michael Robert Jirousek, Michael Paal, Gerd Ruhter, Theo Schotten
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Patent number: 6669926Abstract: Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.Type: GrantFiled: October 16, 2000Date of Patent: December 30, 2003Assignee: Mallinckrodt, Inc.Inventors: Samuel Achilefu, Raghavan Rajagopalan, Richard B. Dorshow, Joseph E. Bugaj
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Patent number: 6656954Abstract: A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: November 29, 2001Date of Patent: December 2, 2003Assignee: Pharmacia CorporationInventors: Louis J. Bedell, Joseph J. McDonald, Thomas E. Barta, Daniel P. Becker, Shashidhar N. Rao, John N. Freskos, Brent V. Mischke, Daniel P. Getman, Gary A. DeCrescenzo
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Patent number: 6656939Abstract: 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: GrantFiled: December 20, 2001Date of Patent: December 2, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Jean-Damien Charrier
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Publication number: 20030191165Abstract: A compound which has the following formula (1), 1Type: ApplicationFiled: March 31, 2003Publication date: October 9, 2003Inventors: Haruo Seto, Kazuo Shin-Ya, Konstanty Wierzba
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Publication number: 20030191164Abstract: Provided is a pharmaceutical composition containing a propane-1,3-dione derivative as the active ingredient, particularly a GnRH receptor antagonist. Also, provided is a propane-1,3-dione derivative having a GnRH antagonistic effect.Type: ApplicationFiled: December 19, 2002Publication date: October 9, 2003Inventors: Masaaki Hirano, Eiji Kawaminami, Akira Toyoshima, Hiroyuki Moritomo, Norio Seki, Ryutaro Wakayama, Minoru Okada, Toshiyuki Kusayama
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Publication number: 20030185756Abstract: Novel tumor specific phototherapeutic and photodiagnostic agents are disclosed. The compounds consist of a carbocyanine dye for visualization, photosensitizer for photodynamic treatment, and tumor receptor-avid peptide for site-specific delivery of the probe and phototoxic agent to diseased tissues A combination of these elements takes full advantage of the unique and efficient properties of each component for an effective patient care management.Type: ApplicationFiled: October 17, 2001Publication date: October 2, 2003Applicant: MALLINCKRODT INCInventors: Samuel Achilefu, Richard B. Dorshow, Raghavan Rajagopalan, Joseph E. Bugaj
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Publication number: 20030186993Abstract: The present invention is directed to substituted naphthothiazolium, aromatic guanylhydrazones, and other compounds and compositions with anti-malarial activity useful for the treatment and prophylaxis of malaria. The compounds are provided for the treatment of malaria or the sequelae of malarial infection, for depolymerizing malaria pigment (hemozoin), and for ameliorating the adverse effects of hemozoin on host cells.Type: ApplicationFiled: October 23, 2002Publication date: October 2, 2003Inventors: Peter C. Ulrich, Anthony Cerami
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Patent number: 6624171Abstract: Substituted aza-oxindole derivatives useful as cyclin dependent kinase 11 inhibitors, for preventing/reducing the severity of epithelial cytotoxicity side-effects (e.g., alopecia, plantar-palmar syndrome, mucositis) induced by chemoptherapy and/or radiation therapy in a patient receiving such therapy.Type: GrantFiled: August 28, 2001Date of Patent: September 23, 2003Assignee: SmithKline Beecham CorporationInventors: Philip Anthony Harris, Lee Frederick Kuyper, Karen Elizabeth Lackey, James Marvin Veal
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Patent number: 6608098Abstract: This invention relates to compounds represented by the general formula [I] wherein, R represents an azido group, etc., R1 and R2 are the same or different and represent hydrogen atoms, etc., R3 and R4 are the same or different and represent hydrogen atoms, etc., X1 represents an oxygen atom, etc., X2 represents an oxygen atom, etc., Y represents an oxygen atom, etc., and Z represents a condensed aryl group, etc., or a pharmaceutically acceptable salt thereof, preparation processes thereof, and an agent for treating diabetes, a prophylactic agent for chronic complications of diabetes or a drug against obesity, containing, as an effective ingredient, the compound or the pharmaceutically acceptable salt thereof.Type: GrantFiled: February 25, 2002Date of Patent: August 19, 2003Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Toshio Nagase, Tomoharu Iino, Yoshiyuki Sato, Teruyuki Nishimura, Jun-ichi Eiki
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Patent number: 6605599Abstract: The present invention relates to epothilone derivatives, having the following formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1-R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.Type: GrantFiled: May 26, 1998Date of Patent: August 12, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Gregory D. Vite, Soong-Hoon Kim, Robert M. Borzilleri, James A. Johnson
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Publication number: 20030114432Abstract: The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.Type: ApplicationFiled: September 19, 2002Publication date: June 19, 2003Inventors: Michael Clare, Joyce Z. Crich, Timothy J. Hagen, Gunnar J. Hanson, Stephen C. Houdek, He Huang, Richard M. Weier
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Publication number: 20030087909Abstract: This invention relates generally to a novel class of fused heterocyclic compounds of the Formula (I) or Formula (II): 1Type: ApplicationFiled: April 8, 2002Publication date: May 8, 2003Inventors: Irina C. Jacobson, Mimi L. Quan, Ruth R. Wexler
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Publication number: 20030087928Abstract: The invention relates to novel anilide compounds represented by the following formula IV: 1Type: ApplicationFiled: February 20, 2002Publication date: May 8, 2003Applicant: Kowa Company, Ltd., JapanInventors: Kimiyuki Shibuya, Katsumi Kawamine, Yukihiro Sato, Toshiyuki Edano, Mitsuteru Hirata, Chiyoka Ozaki
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Patent number: 6555540Abstract: This invention is directed to methods, pharmaceutical compositions and kits comprising an aldose reductase inhibitor (ARI), a prodrug thereof or a pharmaceutically acceptable salt of said ARI or said prodrug and a selective COX-2 inhibitor, a prodrug thereof or a pharmaceutically acceptable salt of said selective COX-2 inhibitor or said prodrug. This invention further relates to methods of using those pharmaceutical compositions for the treatment of diabetic complications such as diabetic neuropathy, diabetic nephropathy, diabetic retinopathy and diabetic cardiomyopathy.Type: GrantFiled: June 23, 2000Date of Patent: April 29, 2003Assignee: Pfizer IncInventor: Banavara L. Mylari
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Publication number: 20030055092Abstract: This invention is to provide remedies for ischemic stroke which contain as an active ingredient a compound having mGluR1 antagonism, pharmaceutical compositions which are remedies for ischemic stroke at the acute stage, pharmaceutical compositions which contain as an active ingredient a compound having selective mGluR1 antagonism, and pharmaceutical compositions wherein the compound having selective mGluR1 antagonism is 6-amino-N-cyclohexyl-N,3 -dimethylthiazolo[3,2-a]benzoimidazole-2-carboxamide dihydrochloride.Type: ApplicationFiled: October 29, 2002Publication date: March 20, 2003Applicant: YAMANOUCHI PHARMACEUTICAL CO., LTD.Inventors: Masamichi Okada, Masayasu Takahashi, Satoshi Hayashibe
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Publication number: 20030013747Abstract: Antiatherosclerotic agents are provided which are represented by Formulas I or II: 1Type: ApplicationFiled: August 6, 2002Publication date: January 16, 2003Applicant: WyethInventors: Robert J. Steffan, Amedeo A. Failli
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Patent number: 6504058Abstract: Compounds of Formula I are disclosed which are useful as fungicides wherein R1 is hydrogen; halogen; C1-C2 alkoxy; C1-C2 haloalkoxy; cyano; or C1-C2 alkyl optionally substituted with halogen, C1-C2 alkoxy or cyano; R2 is hydrogen; halogen; or C1-C4 alkyl optionally substituted with halogen, C1-C2 alkoxy or cyano; R3 is hydrogen; halogen; C1-C4 alkoxy; C1-C4 haloalkoxy; or C1-C4 alkyl optionally substituted with halogen, C1-C2 alkoxy or cyano; or R2 and R3 can be taken together as —CH2CH2—; R4 is C1-C2 alkyl; R5 is R6, CH(R8)OR6, CH(R8)CH(R7)R6 or C(R8)═C(R7)R6; and R6, R7 and R8 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula I and a method for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound of Formula I.Type: GrantFiled: February 6, 2002Date of Patent: January 7, 2003Assignee: The Board of Trustees of the University of ArkansasInventors: Gregory S. Basarab, Lee Dalton Jennings, Dennis R. Rayner
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Patent number: 6498176Abstract: Compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, D, X, Y and Z have the meaning as defined in the claims exhibit protein tyrosine kinase and protein serin/threonine kinase inhibitory activity.Type: GrantFiled: August 22, 2001Date of Patent: December 24, 2002Assignee: SmithKlineBeecham CorporationInventors: Karen Elizabeth Lackey, Robert Walton McNutt, Jr.