Nitrogen Attached Indirectly To The Tetrazole Ring By Nonionic Bonding Patents (Class 548/254)
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Publication number: 20070238765Abstract: The present invention provides a compound of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Y, Ar, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: ApplicationFiled: April 11, 2007Publication date: October 11, 2007Inventors: Xiao-Fa Lin, David Garrett Loughhead, Jason Manka, Counde O'Yang, Michael Soth, Dennis M. Yasuda
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Patent number: 7217706Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.Type: GrantFiled: February 14, 2002Date of Patent: May 15, 2007Assignee: Astellas Pharma Inc.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Patent number: 7205312Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.Type: GrantFiled: November 2, 2004Date of Patent: April 17, 2007Assignee: Janssen Pharmaceutica, N.V.Inventors: Marc Gaston Venet, Dominique Jean-Pierre Mabire, Jean Fernand Armand Lacrampe, Gerard Charles Sanz
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Patent number: 7138415Abstract: Heterocyclic amides of formula (1) wherein: is a single or double bond; A is phenylene or heteroarylene; m is 0, 1 or 2; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; r is 1 or 2; Y is —NR2R3 or —OR3; R2 and R3 are selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R4 is selected from for example hydrogen, halo, nitro, cyano, hydroxy, C1-4alkyl, and C1-4alkanoyl; R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R9), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity.Type: GrantFiled: March 4, 2003Date of Patent: November 21, 2006Assignee: AstraZeneca ABInventors: Paul Robert Owen Whittamore, Stuart Norman Lile Bennett, Iain Simpson
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Patent number: 7125869Abstract: Novel polycyclic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively, into cosmetic compositions.Type: GrantFiled: June 10, 2005Date of Patent: October 24, 2006Assignee: Galderma Research & DevelopmentInventors: Laurence Clary, Pascal Collette, Michel Rivier, Andre Jomard
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Patent number: 7109223Abstract: This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.Type: GrantFiled: August 25, 2003Date of Patent: September 19, 2006Assignee: Merck & Co. Inc.Inventors: Yongxin Han, John Colucci, Xavier Billot, Marie-Claire Wilson, Robert Young
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Patent number: 7041832Abstract: Losartan is prepared by acid catalyzed cleavage of a triarylmethyl group from a triarylmethyl-substituted losartan derivative in a diluent comprising liquid ketone. The reaction mixture is basified and liquid ketone is evaporated from the mixture leaving a residue from which a triarylmethyl alcohol and losartan are each obtained in high yield and high purity. In addition, losartan potassium is prepared by a process that is more convenient that those previously known in the art in which losartan is contacted with potassium ions in substantially pure liquid alcohol and losartan potassium is precipitated from the alcohol.Type: GrantFiled: April 29, 2003Date of Patent: May 9, 2006Assignee: Tava Pharmaceutical Industries, Ltd.Inventor: Ben-Zion Dolitzky
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Patent number: 7041659Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.Type: GrantFiled: October 14, 2003Date of Patent: May 9, 2006Assignee: Wellstat Therapeutics CorporationInventor: Shalini Sharma
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Patent number: 7037880Abstract: Ethylene derivatives of formula (I): where Q is an unsubstituted or substituted phenyl or heterocyclic group, especially a 4-thiazolyl, 1- or 3-pyrazolyl, 1,3-oxazol-4-yl, phenyl or pyridyl group; E is a substituent such as a cyano group; A is a substituent such as a 4-pyrazolyl or thiazolyl group; and B is a substituent such as an alkylcarbonyl group. Agricultural chemicals and agents for preventing the attachment of aquatic organisms containing one or more such ethylene derivatives.Type: GrantFiled: August 8, 2002Date of Patent: May 2, 2006Assignee: Nissan Chemical Industries, Ltd.Inventors: Tomoyuki Ogura, Hiroshi Murakami, Akira Numata, Rika Miyachi, Toshiro Miyake, Norihiko Mimori, Shinji Takii
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Patent number: 7019033Abstract: Phenylamino benzoic acid, benzamides, and benzyl alcohol derivatives of the formula where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, and Z is COOR7, tetrazolyl, CONR6R7, or CH2OR7, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as inflammation, psoriasis and restenosis, as well as stroke, heart failure, and immunodeficiency disorders.Type: GrantFiled: December 10, 2002Date of Patent: March 28, 2006Assignee: Warner-Lambert CompanyInventors: Stephen Douglas Barrett, Alexander James Bridges, Donna Reynolds Cody, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Mel Conrad Schroeder, Haile Tecle
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Patent number: 6972287Abstract: The present invention provides a method of treating Alzheimer's disease using a compound of Formula (I). Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of the Formula (I) and a method of imaging amyloid deposits, as well as new compounds of Formula (I).Type: GrantFiled: May 31, 2000Date of Patent: December 6, 2005Assignee: Pfizer Inc.Inventors: Corinne Elizabeth Augelli-Szafran, Mark Robert Barvian, Christopher Franklin Bigge, Shelly Ann Glase, Shunichiro Hachiya, John Steven Kiely, Takenori Kimura, Yingjie Lai, Annette Theresa Sakkab, Mark James Suto, Larry Craswell Walker, Tomoyuki Yasunaga, Nian Zhuang
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Patent number: 6949575Abstract: The present invention provides compounds of Formula (I) and a method of treating Alzheimer's disease using a compound of Formula (I), wherein: R1 and R2 include alkyl and phenylalkyl; R3 is hydrogen or alkyl; and R4 and R5 include alkyl, alkoxy, carboxyl, alkoxycarbonyl, and nitro. Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of Formula (I) and a method of imaging amyloid deposits using compounds of Formula (I).Type: GrantFiled: April 25, 2001Date of Patent: September 27, 2005Assignee: Pfizer Inc.Inventors: Nancy Sue Barta, Christopher Franklin Bigge
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Patent number: 6927217Abstract: The present invention relates to novel dihydropyrones of Formula I wherein X is NH or NR8, which inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS.Type: GrantFiled: October 16, 2002Date of Patent: August 9, 2005Assignee: Warner-Lambert CompanyInventors: Frederick Earl Boyer, Jr., John Michael Domagala, Edmund Lee Ellsworth, Christopher Andrew Gajda, Elizabeth Ann Lunney, Alexander Pavlovsky, Vara Prasad Venkata Nagendra Josyula, Bradley Dean Tait
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Patent number: 6916819Abstract: This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.Type: GrantFiled: December 21, 2001Date of Patent: July 12, 2005Assignee: Neurogen CorporationInventors: Guiying Li, John M. Peterson, Pamela Albaugh, Kevin S. Currie, Guolin Cai, Linda M. Gustavson, Kyungae Lee, Alan Hutchison, Vinod Singh, George D. Maynard, Jun Yuan, Ling Hong Xie, Manuka Ghosh, Nian Liu
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Patent number: 6835513Abstract: Improved organophotoreceptors have: (a) a charge transport compound having the formula: where R1 is hydrogen, a branched or linear alkyl group, a branched or linear unsaturated hydrocarbon group, an ether group, or an aryl group; and R2 and R3 independently have a structure of: in which Ar is selected form the group consisting of; R4 is a hydrogen, or an aromatic group; (b) a charge generating compound; and (c) an electrically conductive substrate.Type: GrantFiled: March 6, 2003Date of Patent: December 28, 2004Assignee: Samsung Electronic Co., Ltd.Inventors: Nusrallah Jubran, Zbigniew Tokarski, Kam W. Law
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Patent number: 6833375Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.Type: GrantFiled: September 10, 2002Date of Patent: December 21, 2004Assignee: Janssen Pharmaceutica, N.V.Inventors: Marc Gaston Venet, Dominique Jean-Pierre Mabire, Jean Fernand Armand Lacrampe, Gerard Charles Sanz
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Publication number: 20040242661Abstract: Provided are crystalline and amorphous form of valsartan, and processes for their preparation.Type: ApplicationFiled: March 17, 2004Publication date: December 2, 2004Inventors: Igor Rukhman, Evgeni Flyaks, Tamas Koltai, Judith Aronhime
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Publication number: 20040235757Abstract: Are described compounds of Formula (I) in which R, R′, R″, A, and D have the meanings described in the text, as useful agents in the cure of pathologies characterised by altered angiogenesis and as antitumorals.Type: ApplicationFiled: February 2, 2004Publication date: November 25, 2004Inventors: Dallavalle Sabrina, Merlini Lucio, Pisano Claudio, Vesci Loredana, Giannini Giuseppe, Penco Sergio
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Publication number: 20040224998Abstract: A process for the synthesis of Losartan Potassium by reacting Trityl Losartan in a primary alcohol with potassium tertiary alkoxide.Type: ApplicationFiled: May 7, 2003Publication date: November 11, 2004Inventors: Ashok Kumar, Rajeshkumar Singh, Nalinakshya Panda, Abhay Upare, Manmohan Nimbalkar, Satish Soudagar
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Patent number: 6809113Abstract: Compounds which are antagonists of MCP-1 function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection; pharmaceutical compositions comprising these compounds; and the use of these compounds and compositions in the prevention or treatment of such diseases.Type: GrantFiled: February 27, 2002Date of Patent: October 26, 2004Assignees: Telik, Inc., Sanwa Kagaku Kenkyusho Co.Inventors: Edgardo Laborde, Louise Robinson, Fanying Meng, Brian T. Peterson, Hugo O. Villar, Steven E. Anuskiewicz, Yoshiro Ishiwata, Shoji Yokochi, Yukiharu Matsumoto, Takuji Kakigami, Hideaki Inagaki, Takahito Jomori, Kouji Matsushima
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Patent number: 6797708Abstract: This invention provides substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof, and methods for using the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition of pain and inflammation.Type: GrantFiled: November 22, 2002Date of Patent: September 28, 2004Assignee: WyethInventors: John C. McKew, Steven Y. Tam, Katherine L. Lee, Lihren Chen, Paresh Thakker, Fuk-Wah Sum, Mark Behnke, Baihua Hu, James D. Clark
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Publication number: 20040186295Abstract: Tetrazole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, and panic, as well as in the treatment of pain and other diseases.Type: ApplicationFiled: April 2, 2004Publication date: September 23, 2004Inventors: Nicholas D P Cosford, Chixu Chen, Thomas S Reger, Jeffrey R Roppe, Nicholas D Smith
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Publication number: 20040171843Abstract: Provided is a method of improving the flowability of losartan potassium powder having an initial Hausner ratio of 1.45 or more, which method includes reslurrying the losatrtan potassium in a reslurry solvent.Type: ApplicationFiled: October 17, 2003Publication date: September 2, 2004Inventors: Igor Lifshitz, Ilan Kor, Shalom Shabat
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Patent number: 6784197Abstract: The invention concerns 2-oxo-1-pyrrolidine derivatives of formula (I) wherein the substituents are as defined in the specification, as well as their use as pharmaceuticals. The compounds of the invention are particularly suited for treating neurological disorders such as epilepsy.Type: GrantFiled: August 20, 2002Date of Patent: August 31, 2004Assignee: UCB S.A.Inventors: Edmond Differding, Benoît Kenda, Bénédicte Lallemand, Alain Matagne, Philippe Michel, Patrick Pasau, Patrice Talaga
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Publication number: 20040152904Abstract: The invention relates to novel &Dgr;1-pyrrolines of the formula (I) 1Type: ApplicationFiled: December 12, 2003Publication date: August 5, 2004Inventors: Andrew Plant, Fritz Maurer, Albrecht Marhold, Christoph Erdelen, Andreas Turberg, Olaf Hansen, Angelika Lubos-Erdelen
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Publication number: 20040147482Abstract: Thee present invention relates to therapeutically active cubane compounds, a method of preparing the same, and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in creating diseases of the central nervous system related to the metabotropic glutamate receptor system.Type: ApplicationFiled: January 14, 2004Publication date: July 29, 2004Applicant: Prescient NeuroPharma Inc.Inventors: Hassan Pajouhesh, Kenneth Curry
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Publication number: 20040147575Abstract: Nitric acid salts with medicines having an antihypertensive activity.Type: ApplicationFiled: September 29, 2003Publication date: July 29, 2004Applicant: Nicox S.A.Inventor: Piero Del Soldato
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Patent number: 6740758Abstract: A process for preparing 6-hydroxy-3,4-dihydroquinolinone by intramolecular Friedel-Crafts alkylation of N-(4-methoxyphenyl)-3-chloropropionamide in which an equivalent of N-(4-methoxphenyl)-3-chloropropionamide is contacted with a Lewis acid in DMSO or a high boiling amide or amine at an elevated temperature of from about 150° C. to about 220° C. is provided. The process produces 6-HQ in high yield and a high state of purity such that it may be used in subsequent reactions toward the preparation of cilostazol without intermediate purification. A process for preparing cilostazol from 6-hydroxy-3,4-dihydroquinolinone prepared by the process and improved processes for preparing N-(4-methoxyphenyl)-3-chloropropionamide are also provided.Type: GrantFiled: June 20, 2003Date of Patent: May 25, 2004Assignee: Teva Pharmaceutical IndustriesInventors: Marioara Mendelovici, Gideon Pilarsky, Tamar Nidam, Ben-Zion Dolitzky
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Publication number: 20040097568Abstract: A compound that is a crystalline Form III of losartan potassium is provided. Also provided are compositions containing the compound and methods for its preparation.Type: ApplicationFiled: July 29, 2003Publication date: May 20, 2004Applicants: DR. REDDY'S LABORATORIES LIMITED, DR. REDDY'S LABORATORIES, INC.Inventors: Manne Satyanarayana Reddy, Sajja Eswaraiah, Ravinder Reddy Koppera, Vajrala Venkata Reddy
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Publication number: 20040087552Abstract: 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. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.Type: ApplicationFiled: July 17, 2003Publication date: May 6, 2004Inventors: 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, Christopher A. Willoughby, Yuan Cheng
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Publication number: 20040063673Abstract: This invention provides compounds defined by Formula IType: ApplicationFiled: August 5, 2003Publication date: April 1, 2004Inventor: Adam Richard Johnson
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Publication number: 20040043995Abstract: The invention relates to a compound of formula 1Type: ApplicationFiled: December 12, 2002Publication date: March 4, 2004Inventors: Eric Bignon, Jean Pierre Bras, Paul De Cointet, Pierre Despeyroux, Daniel Frehel, Danielle Gully
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Patent number: 6699904Abstract: PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.Type: GrantFiled: February 14, 2002Date of Patent: March 2, 2004Assignee: Pfizer Inc.Inventors: Cheryl M. Hayward, David A. Perry
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Publication number: 20040034077Abstract: Losartan is prepared by acid catalyzed cleavage of a triarylmethyl group from a triarylmethyl-substituted losartan derivative in a diluent comprising liquid ketone. The reaction mixture is basified and liquid ketone is evaporated from the mixture leaving a residue from which a triarylmethyl alcohol and losartan are each obtained in high yield and high purity. In addition, losartan potassium is prepared by a process that is more convenient that those previously known in the art in which losartan is contacted with potassium ions in substantially pure liquid alcohol and losartan potassium is precipitated from the alcohol.Type: ApplicationFiled: April 29, 2003Publication date: February 19, 2004Inventor: Ben-Zion Dolitzky
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Publication number: 20040034076Abstract: The present invention relates to carbamates and urea derivatives of the formula I 1Type: ApplicationFiled: June 16, 2003Publication date: February 19, 2004Inventors: Wilhelm Amberg, Georg Kettschau
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Publication number: 20040002525Abstract: Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.Type: ApplicationFiled: October 28, 2002Publication date: January 1, 2004Inventors: Jeffrey A. Robl, Joseph A. Tino, Andres S. Hernandez, Jun Li
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Publication number: 20030232786Abstract: Novel tricyclic-bis-enone derivatives (TBEs) as well as the process for the preparation of such TBEs are provided. Also provided are methods for prevention and/or treatment of cancer, Alzheimer's disease, Parkinson's disease, multiple sclerosis, amyotropic lateral sclerosis, rheumatoid arthritis, inflammatory bowel disease, and all other diseases whose pathogenesis is believed to involve excessive production of either nitric oxide (NO) or prostaglandins or the overexpression of iNOS or COX-2 genes or gene products. Further, methods for the synthesis of the TBE compounds of the invention utilize cheap commercially available reagents and are highly cost effective and amenable to scale-up. Additional high efficiency synthetic methods that utilize novel intermediates as well as the synthesis of these intermediates are also provided. Furthermore, the invention also provides methods for designing novel and water-soluble TBEs.Type: ApplicationFiled: January 15, 2003Publication date: December 18, 2003Inventors: Tadashi Honda, Frank G. Favaloro, Gordon W. Gribble, Michael B. Sporn, Nanjoo Suh
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Publication number: 20030229054Abstract: Novel amines of formulas 1A and 1B 1Type: ApplicationFiled: February 14, 2003Publication date: December 11, 2003Inventors: Thomas Richard Belliotti, Justin Stephen Bryans, Thomas Capiris, David Christopher Horwell, Clare Octavia Kneen, David Juergen Wustrow
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Publication number: 20030225053Abstract: Disclosed are amide compounds of formula(I): 1Type: ApplicationFiled: April 10, 2003Publication date: December 4, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Donghong Amy Gao, Daniel R. Goldberg, Abdelhakim Hammach, Ming-Hong Hao, Victor Marc Kamhi, Neil Moss, Kevin Chungeng Qian, Gregory Paul Roth, Christopher Ronald Sarko, Alan David Swinamer, Zhaoming Xiong
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Publication number: 20030220382Abstract: The present invention provides compounds of Formula (I) and a method of treating Alzheimer's disease using a compound of Formula (I), wherein: R1 and R2 include alkyl and phenylalkyl; R3 is hydrogen or alkyl; and R4 and R5 include alkyl, alkoxy, carboxyl, alkoxycarbonyl, and nitro. Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of Formula (I) and a method of imaging amyloid deposits using compounds of Formula (I).Type: ApplicationFiled: November 4, 2002Publication date: November 27, 2003Inventors: Nancy Sue Barta, Christopher Franklin Bigge
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Publication number: 20030220350Abstract: A novel class of 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 glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity.Type: ApplicationFiled: August 30, 2002Publication date: November 27, 2003Inventors: Jesper Lau, Peter Madsen, Christian Sams, Carsten Behrens, Josef Vagner, Inge Thoger Christensen, Behrend Frederik Lundt, Ulla Grove Sidelmann, Henning Thogersen, Anthony L. Ling, Michael Bruno Plewe, Larry Kenneth Truesdale, Anker Steen Jogensen, Janos Tibor Kodra, Shenghua Shi
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Publication number: 20030212120Abstract: Novel compounds, compositions and methods effective for the prevention and treatment of mast-cell mediated inflammatory disorders are described. The compounds, compositions and methods are effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis, as well as other types of immunomediated inflammatory disorders, such as rheumatoid arthritis, conjunctivitis and inflammatory bowel disease, various dermatological conditions, as well as certain viral conditions. The compounds comprise potent and selective inhibitors of the mast cell protease tryptase. The compositions for treating these conditions include oral, inhalant, topical and parenteral preparations as well as devices comprising such preparations.Type: ApplicationFiled: March 14, 2003Publication date: November 13, 2003Applicants: Axys Pharmaceuticals, Inc., ARRIS PHARMACEUTICAL CORPORATION a Delaware CorporationInventors: Timothy J. Church, Neil Scott Cutshall, Anthony R. Gangloff, Thomas E. Jenkins, Martin S. Linsell, Joane Litvak, Kenneth D. Rice, Jeffrey R. Spencer, Vivian R. Wang
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Publication number: 20030207188Abstract: Improved organophotoreceptors have:Type: ApplicationFiled: March 6, 2003Publication date: November 6, 2003Inventors: Nusrallah Jubran, Zbigniew Tokarski, Kam W. Law
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Patent number: 6642379Abstract: Benzamide derivatives represented by the general formula (I): and insecticides for agricultural and horticultural use and usage thereof, wherein Z1 is O or S; R is H, (substituted) alkyl, or alkoxycarbonyl; X is halogeno, cyano, nitro, C3-C6(halo)cycloalkyl, (substituted) phenyl, a (substituted) heterocyclic group, or —A1—R1 [wherein A1 is —O—, —S—, —SO—, —SO2—, —C(═O)—, or —C(═NOR2)— (wherein R2 is H, C1-C6(halo)alkyl, (substituted) phenylated C1-C4 alkyl, or the like); and R1 is halogeno, C3-C6 cycloalkyl, C3-C6 halocycloalkenyl, (substituted) phenyl, or the like]; n is 0 to 4; Y is halogeno, cyano, nitro, C3-C6 halocycloalkyl, (substituted) phenyl, or the like; m is 1 to 5; Q is a heterocycle such as oxazoline; and B1 to B4 are each CH or N.Type: GrantFiled: April 4, 2002Date of Patent: November 4, 2003Assignee: Nihon Nohyaku Co., Ltd.Inventors: Takashi Furuya, Eiji Kohno, Masanori Tohnishi, Kazuyuki Sakata, Masayuki Morimoto, Akira Seo
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Publication number: 20030204085Abstract: Disclosed are compounds of the formula: 1Type: ApplicationFiled: July 30, 2002Publication date: October 30, 2003Inventors: Arthur G. Taveras, Cynthia J. Aki, Richard W. Bond, Jianping Chao, Michael Dwyer, Johan A. Ferreira, Jonathan A. Pachter, John J. Baldwin, Bernd Kaiser, Ge Li, J. Robert Merritt, Kingsley H. Nelson, Laura L. Rokosz
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Publication number: 20030199565Abstract: Substituted imidazoles (1) are useful as angiotensin II blockers. These compounds have activity in treating hypertension and congestive heart failure. Pharmaceutical compositions containing the novel imidazoles and pharmaceutical methods using them, alone and in conjunction with other drugs, especially diuretics and non-steroidal antiinflammatory drugs (NSAID's) are also described.Type: ApplicationFiled: April 7, 2003Publication date: October 23, 2003Inventors: Sarkis Barret Kalindjian, Ildiko Maria Buck, Katherine Isobel Mary Steel, Paul Trevor Wright, Matthew John Tozer, Michael John Pether, Caroline Minli Rachel Low
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Publication number: 20030199689Abstract: The present invention relates to compounds of formula I, 1Type: ApplicationFiled: November 21, 2002Publication date: October 23, 2003Inventors: Marc Nazare, Melanie Essrich, David William Will, Hans Matter, Kurt Ritter, Volkmar Wehner
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Patent number: 6635634Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.Type: GrantFiled: February 14, 2002Date of Patent: October 21, 2003Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Publication number: 20030181496Abstract: Pyrrole derivatives represented by the following formula: 1Type: ApplicationFiled: January 28, 2003Publication date: September 25, 2003Inventors: Teruhisa Tokunaga, William Ewan Hume, Makoto Kitoh, Ryu Nagata
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Publication number: 20030180236Abstract: The present invention relates to certain resorcinol derivatives and their use as skin lightening agents.Type: ApplicationFiled: May 27, 2003Publication date: September 25, 2003Inventors: Stuart E. Bradley, Eric W. Collington, Matthew C. Fyfe, Martin J. Procter, Colin P. Sambrook Smith