1,2,4-triazoles (including Hydrogenated) Patents (Class 546/272.4)
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Patent number: 7304062Abstract: The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-2-alkyl, heteroaryl-C0-2-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl or phenyl. W is O or S. R2 is H or a substituted or unsubstituted group selected from C1-C6 alkyl, C3-C6 cycloalkyl and heteroaryl. X is a C2-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S. Y is C, O, S, NH or a single bond. Furthermore, E is (CH2)nCOOH, wherein n is 0, 1, 2 or 3, or C(R3)(R4)A, wherein A is an acidic functional group such as carboxyl, carboxamide substituted or unsubstituted sulfonamide, or substituted or unsubstituted tetrazole. R3 is H, saturated or unsaturated C1-C5 alkyl, C1-C5 alkoxy.Type: GrantFiled: November 9, 2001Date of Patent: December 4, 2007Assignee: Eli Lilly and CompanyInventors: Samuel James Dominianni, Garret Jay Etgen, Richard Duane Johnston, Nathan Bryan Mantlo, Daniel Ray Mayhugh, Ashraf Saeed, Richard Craig Thompson, Xiaodong Wang, Christopher Randall Schmid, Yanping Xu
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Patent number: 7297797Abstract: The invention relates to novel ?1-pyrrolines of the formula (I) in which R1, R2, R3, R4, A1, A2, R5, R6, R7, R8, R9 and Q are as defined in the disclosure, to a process for preparing these compounds and to their use for controlling pests.Type: GrantFiled: September 8, 2003Date of Patent: November 20, 2007Assignee: Bayer CropScience AGInventors: Johannes Rudolf Jansen, Udo Kraatz, Hubertus Stakemeier, Thomas Seitz, Fritz Maurer, Martin Füsslein, Bernd Alig, Christian Funke, Werner Hallenbach, Jörg Konze, Udo Beckmann, Ulrich Görgens
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Publication number: 20070259923Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.Type: ApplicationFiled: April 25, 2007Publication date: November 8, 2007Applicants: AstraZeneca AB, NPS PHARMACEUTICALS, INC.Inventors: Methvin Isaac, Abdelmalik Slassi, Louise Edwards, Tao Xin, Andreas Wallberg, Tomislav Stefanac
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Patent number: 7253187Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein Z1 and Z2 are each independently nitrogen or CH and Ring A, TmR1, QR2, UnR3, and Sp are as described in the specification. The compounds are especially useful as inhibitors of ERK2 and for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, diabetes, and cardiovascular disease.Type: GrantFiled: February 3, 2004Date of Patent: August 7, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jingrong Cao, Jeremy Green, Michael Hale, Francois Maltais, Judy Straub, Qing Tang, Alex Aronov
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Patent number: 7241758Abstract: Disclosed are novel aromatic compounds of the formula (I) wherein G, X, Ar, L and Q are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.Type: GrantFiled: October 15, 2002Date of Patent: July 10, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Ming-Hong Hao, Sanxing Sun
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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: 7205406Abstract: An azomethine dye represented by the following Formula 1: wherein Y represents a substituent of 0.2??p?0.9, Z1 and Z2 each represent —CR1?, where R1 represents a hydrogen atom or a substituent, or —N?, L represents the group represented by the following Formula 1a, X represents an unsubstituted or substituted di-alkylamino group, R represents an unsubstituted or substituted alkyl group, and n represents an integer more than 0. wherein B represents a group of non-metallic atoms which are necessary to form a heterocyclic ring.Type: GrantFiled: July 1, 2005Date of Patent: April 17, 2007Assignee: Konica Minolta Holdings, Inc.Inventors: Emiko Kataoka, Takatugu Suzuki, Dai Ikemizu
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Patent number: 7183278Abstract: Disclosed are novel compounds useful for the control of harmful organisms, harmful organism control agents using the same, and processes for producing the novel compounds. The useful novel compounds according to the present invention include compounds represented by formula (1).Type: GrantFiled: November 4, 1999Date of Patent: February 27, 2007Assignee: Meiji Seika Kaisha, Ltd.Inventors: Keiichi Imamura, Kouichi Mitomo, Natsuko Yamada, Kazumi Yamamoto, Takashi Teraoka, Osamu Sakanaka, Hiroshi Kurihara, Makoto Taniguchi
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Patent number: 7135572Abstract: The present invention relates to a novel diaryl 1,2,4-triazole derivative of the following formula 1 as a highly selective cyclooxygenase-2 inhibitor: Wherein, R1, R2, R3, R4, R5, W and A is as defined in this specification.Type: GrantFiled: September 12, 2005Date of Patent: November 14, 2006Assignee: CJ CorpInventors: Il-hwan Cho, Jee-woong Lim, Ji-young Noh, Jong-hoon Kim, Sang-wook Park, Hyung-chul Ryu, Je-hak Kim, Jong-ho Kim, So-young Wang, Dal-hyun Kim, Chun-seon Lyu
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Patent number: 7105549Abstract: This invention relates aryl substituted pyridines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Ar and R1–R4 are set in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.Type: GrantFiled: September 6, 2002Date of Patent: September 12, 2006Assignee: Euro-Celtique S.A.Inventors: Bin Shao, R. Richard Goehring, Samuel F Victory, Qun Sun
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Patent number: 7091222Abstract: The present invention relates to imidazole derivatives of the general formula wherein R1, R2, R3 and R4 are as defined hereinabove. This invention also relates to the compound's pharmaceutically acceptable salt and processes for the preparation thereof. These compounds can be used for the manufacture of pharmaceutical compositions for the treatment and prevention of mGluR5 receptor mediated disorders. These compounds are useful, inter alia, in the treatment or prevention of acute and/or chronic neurological disorders such as psychosis, epilepsy, schizophrenia, Alzheimer's disease, cognitive disorders and memory deficit disorders, as well as chronic and acute pain.Type: GrantFiled: June 23, 2004Date of Patent: August 15, 2006Assignee: 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: 7074810Abstract: The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, L, and R11 are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof.Type: GrantFiled: October 3, 2003Date of Patent: July 11, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Bryan W. King, James Sheppeck, John L. Gilmore
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Patent number: 7019144Abstract: A 1,2,4-Triazole derivative of formula 1 or a non-toxic salt thereof, a preparation method thereof, and a pharmaceutical composition containing the derivative or the salt as an active ingredient are provided.Type: GrantFiled: June 27, 2003Date of Patent: March 28, 2006Assignee: CJ Corp.Inventors: Il Hwan Cho, Hyun Jung Park, Ji Young Noh, Hyung Chul Ryu, Sang Wook Park, Sung Hak Jung, Sung Hak Lee, Jong Hoon Kim, Jee Woong Lim, Chun Seon Lyu, Dal Hyun Kim, Young Hoon Kim, Kyu Jeong Yeon, Myeong Yun Chae, In Ki Min, Hae Tak Jin, Kyoung Rae Kang
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Patent number: 6987189Abstract: A method of making a compound of Formula VI: wherein Tr is a triphenyl group; R1, R2 and R3 are each independently selected from the group consisting of H, C1–C4 alkyl, C1–C4 alkoxy, aryl, heteroaryl, and arylalkyl; R4 is C2–C6 alkyl, and R5 and R6 are each independently H or C1–C4 alkyl, involves the step of reacting a compound of Formula V: with Tr-OH to produce a compound of Formula VI. The compounds of Formula VI are useful as intermediates in the manufacture of antibiotic agents. Methods of making compounds of Formula V, and intermediates made or used in the foregoing methods, are also described.Type: GrantFiled: September 28, 2004Date of Patent: January 17, 2006Assignee: North Carolina State UniversityInventors: Daniel L. Comins, Shenlin Huang
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Patent number: 6916933Abstract: Compounds of Formula I have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4 and are useful for treating disease whose symptoms and or damage are related to the binding of VCAM-1 to cells expressing VLA-4.Type: GrantFiled: September 24, 2003Date of Patent: July 12, 2005Assignee: Hoffman-La Roche Inc.Inventors: Gerald Lewis Kaplan, Achyutharao Sidduri, Jefferson Wright Tilley
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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: 6897228Abstract: The invention provides pyridoxal and pyridoxine analogues, pharmaceutical compositions containing pyridoxine and pyridoxal analogues, and methods of administering pharmaceutical compositions containing a therapeutically effective amount of at least one of these analogues. In accordance with the present invention, the pyridoxal and pyridoxine analogues can be used in the treatment or prevention of of heparin induced thrombocytopenia (HIT, stroke, and ischemia, and in the treatment of symptoms thereof. The the pyridoxal and pyridoxine analogues can be used in neuroprotection.Type: GrantFiled: April 10, 2003Date of Patent: May 24, 2005Assignee: Medicure International Inc.Inventor: Wasimul Haque
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Patent number: 6875768Abstract: Heterocyclic amine derivatives represented by general formula (I): wherein R1, R2 and R3 represent each H, optionally halogenated C3-6 cycloalkyl, etc.; Q represents an optionally substituted heterocycle containing O, S or N; X represents halogeno, cyano, halo(C1-6)alkyl, etc.; n is from 1 to 4; and Z1 and Z2 represent each O or S; and intermediates thereof represented by the following general formula (IV?): Q?—NH2 wherein Q? represents a definite heterocycle selected from among those represented by Q. Agricultural/horticultural insecticides having a remarkable effect of controlling pest insects of crops such as rice, fruit trees and vegetables, as well as various agricultural, forestry, horticultural and stored grain pest insects.Type: GrantFiled: July 4, 2000Date of Patent: April 5, 2005Assignee: Nihon Nohyako Co., Ltd.Inventors: Kouzou Machiya, Kazuyoshi Endoh, Takashi Furuya, Hayami Nakao, Makoto Gotoh, Eiji Kohno, Masanori Tohnishi, Kazuyuki Sakata, Masayuki Morimoto, Akira Seo
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Patent number: 6875779Abstract: The present invention relates to compounds of the formula wherein R1, R3, R5 and A are defined as in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment of inflammation and other inflammation associated disorders, such as osteoarthritis, rheumatoid arthritis, colon cancer and Alzheimer's disease, in mammals (preferably humans, dogs, cats and livestock).Type: GrantFiled: April 22, 2004Date of Patent: April 5, 2005Assignee: Pfizer Inc.Inventors: Subas M. Sakya, Andrei Shavnya, Bryson Rast
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Patent number: 6855825Abstract: A method of making a compound of Formula VI: wherein Tr is a triphenyl group; R1, R2 and R3 are each independently selected from the group consisting of H, C1-C4 alkyl, C1-C4 alkoxy, aryl, heteroaryl, and arylalkyl; R4 is C2-C6 alkyl, and R5 and R6 are each independently H or C1-C4 alkyl, involves the step of reacting a compound of Formula V: with Tr-OH to produce a compound of Formula VI. The compounds of Formula VI are useful as intermediates in the manufacture of antibiotic agents. Methods of making compounds of Formula V, and intermediates made or used in the foregoing methods, are also described.Type: GrantFiled: December 18, 2003Date of Patent: February 15, 2005Assignee: North Carolina State UniversityInventors: Daniel L. Comins, Shenlin Huang
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Patent number: 6849636Abstract: Triazole derivatives of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.Type: GrantFiled: December 18, 2003Date of Patent: February 1, 2005Assignee: Merck & Co., Inc.Inventors: Sherman T. Waddell, Gina M. Santorelli, Milana M. Maletic, Aaron H. Leeman, Xin Gu, Donald W. Graham, James M. Balkovec, Susan D. Aster
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Patent number: 6846828Abstract: Aminopyrimidine and aminopyridine (I) compounds, compositions and methods useful in the treatment of inflammatory, metabolic or malignant conditions, are provided herein.Type: GrantFiled: November 6, 2002Date of Patent: January 25, 2005Assignee: Roche Palo Alto LLCInventors: Ronald Charles Hawley, Sharada Shenvi Labadie, Eric Brian Sjogren, Francisco Xavier Talamas
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Publication number: 20040266738Abstract: A fungicidally active compound of the formula:Type: ApplicationFiled: May 27, 2004Publication date: December 30, 2004Inventors: Gaik-Lean Chee, Mark A. Dekeyser, Kenneth W. Seebold, Ewa Maria Osika, Walter G. Brouwer, Sheldon B. Park, Hoi Kiong Lai
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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: 20040198735Abstract: The present invention relates to compounds of the formula 1Type: ApplicationFiled: April 22, 2004Publication date: October 7, 2004Inventors: Subas M. Sakya, Andrei Shavnya, Bryson Rast
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Publication number: 20040192704Abstract: This invention relates to novel heterocyclic compounds of formula I wherein R1—R4, X1 and X2 are as defined in the summary and pharmaceutically acceptable salts and solvates thereof, methods to inhibit or modulate Human Immunodeficiency Virus (HIV) reverse transcriptase with compounds of formula I, pharmaceutical compositions containing of formula I admixed with at least one solvent, carrier or excipient and processes to prepare compounds of formula I.Type: ApplicationFiled: March 23, 2004Publication date: September 30, 2004Applicant: Roche Palo Alto LLCInventors: James Patrick Dunn, Steven Swallow, Zachary Kevin Sweeney
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Publication number: 20040192922Abstract: The invention concerns novel azole or triazole derivatives of formula (I), wherein: X, Ar1, Ar3, A, R1, R5, R6, R7 and B are such as defined in the description, their preparation method and their use as antifungal medicines.Type: ApplicationFiled: April 27, 2004Publication date: September 30, 2004Inventors: Didier Babin, John Bernard Weston
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Publication number: 20040171650Abstract: The present invention relates to novel anthelmintic and insecticidal compositions in general, and, more specifically, compositions containing triazole derivatives as active ingredients.Type: ApplicationFiled: February 11, 2004Publication date: September 2, 2004Inventors: Byung Hyun Lee, Martha Jane Larsen, Teresa Maria Kubiak
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Patent number: 6784195Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: where R1, R2, T and Ht are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.Type: GrantFiled: October 5, 2001Date of Patent: August 31, 2004Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Hale, James Janetka, Francois Maltais, Jingrong Cao
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Patent number: 6762197Abstract: A triazolone compound of the formula [I]: wherein; R1 represents optionally substituted phenyl or the like, T represents m-phenylene optionally substituted by methyl or the like; and a fungicidal composition containing it as an active ingredient.Type: GrantFiled: June 6, 2002Date of Patent: July 13, 2004Assignee: Sumitomo Chemical Company, LimitedInventors: Tomohiro Araki, Yoshiharu Kinoshita, Hiroshi Sakaguchi, Akio Manabe
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Patent number: 6753332Abstract: The present invention relates to compounds of the formula wherein R1, R3, R5 and A are defined as in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment of inflammation and other inflammation associated disorders, such as osteoarthritis, rheumatoid arthritis, colon cancer and Alzheimer's disease, in mammals (preferably humans, dogs, cats and livestock).Type: GrantFiled: July 3, 2002Date of Patent: June 22, 2004Assignee: Pfizer, Inc.Inventors: Subas M. Sakya, Andrei Shavnya, Bryson Rast
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Publication number: 20040116426Abstract: Compounds of the formula I 1Type: ApplicationFiled: September 25, 2003Publication date: June 17, 2004Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Jiang-Ping Wu, Terence Alfred Kelly, Rene M. Lemieux, Daniel R. Goldberg, Jonathan Emilian Emeigh, Ronald John Sorcek
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Publication number: 20040116440Abstract: Bombesin receptor antagonists are provided which are useful for the diagnosis, prevention, or treatment of male sexual dysfunction in humans and animals, female sexual dysfunction in humans and animals, anxiety and panic disorders, social phobia, depression, psychoses, sleeping disorders, memory impairment, pulmonary hypertension, lung repair and lung development disorders, cancer including prostate cancer and pancreatic cancer, hepatic porphyria, gastrointestinal secretory disturbances, gastrointestinal disorders including colitis, Crohn's disease and inflammatory bowel disease, emesis, anorexia, pain, seasonal affective disorders, feeding disorders, or pruritus.Type: ApplicationFiled: December 4, 2003Publication date: June 17, 2004Inventors: Michael Higginbottom, Martyn Clive Pritchard, Herman Thijs Stock
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Publication number: 20040106612Abstract: A 1,2,4-triazole derivative of formula 1 or a non-toxic salt thereof, a preparation method thereof, and a pharmaceutical composition containing the derivative or the salt as an active ingredient are provided: 1Type: ApplicationFiled: August 1, 2003Publication date: June 3, 2004Inventors: Il Hwan Cho, Dong Hyun Ko, Myeong Yun Chae, Taerho Kim, Kyoung Rae Kang, Jong Hoon Kim, Sung Hak Jung, Sang Wook Park, Hyung Ok Chun, Hyung Chul Ryu, Ji Young Noh, Hyun Jung Park, Jie Eun Park, Young Mee Chung
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Patent number: 6734143Abstract: The present invention provides 2-methoxyimino-2-(pyridinyloxymethyl) phenyl acetamides according to formula (I) as well as their use as fungicidal compounds.Type: GrantFiled: February 27, 2003Date of Patent: May 11, 2004Assignee: Dow AgroSciences LLCInventors: Neil Vincent Kirby, Jenifer Lynn Adamski Butz, Brent Jeffrey Rieder, James M. Renga, Jeannie Rachel Phillips Cetusic, Irene Mae Morrison, John Todd Mathieson, Gary David Gustafson
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Patent number: 6723742Abstract: The use is described of 3,5-diphenyl-1,2,4-triazoles of the formula I in which R1-R5 are as defined in the description. The compounds have useful pharmaceutical properties and are particularly active as iron chelators. They can be used for the treatment of iron overload in warm-blooded animals.Type: GrantFiled: May 29, 2003Date of Patent: April 20, 2004Assignee: Novartis AG.Inventors: René Lattmann, Pierre Acklin
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Publication number: 20040072692Abstract: A description is given of 4-trifluoromethylpyrazolyl-substituted pyridines and pyrimidines of formula (I) and of their use as herbicides.Type: ApplicationFiled: July 24, 2003Publication date: April 15, 2004Inventors: Michael Gerhard Hoffmann, Hendrik Helmke, Lothar Willms, Thomas Auler, Hermann Bieringer, Hubert Menne
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Patent number: 6710125Abstract: The invention provides a method for preparing a 1-benzotriazolylcarbonate ester of a water-soluble and non-peptidic polymer by reacting a terminal hydroxyl group of a water-soluble and non-peptidic polymer with di(1-benzotriazolyl)carbonate in the presence of an amine base and an organic solvent. The polymer backbone can be poly(ethylene glycol). The 1-benzotriazolylcarbonate ester can then be reacted directly with a biologically active agent to form a biologically active polymer conjugate or reacted with an amino acid, such as lysine, to form an amino acid derivative.Type: GrantFiled: February 6, 2002Date of Patent: March 23, 2004Assignee: Nektar Therapeutics AL, CorporationInventor: Antoni Kozlowski
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Patent number: 6706743Abstract: The instant invention provides &bgr;3 adrenergic receptor agonists of structural Formula (I), the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers and prodrugs, wherein Ar, R, R1, R2, R3, R4, R5, R6, R7, R8, X, and Y, are as defined herein.Type: GrantFiled: March 5, 2003Date of Patent: March 16, 2004Assignee: Pfizer IncInventors: Robert F. Day, Jennifer A. Lafontaine
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Publication number: 20040019085Abstract: Compounds having the formula (I), 1Type: ApplicationFiled: June 17, 2003Publication date: January 29, 2004Inventors: William A. Slusarchyk, Scott A. Bolton, Timothy Herpin, Gregory S. Bisacchi, Zulan Pi, E. Scott Priestley
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Patent number: 6677341Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral heteroaryl aminoalcohols.Type: GrantFiled: December 12, 2001Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6667326Abstract: The invention relates to compounds of the general formula wherein R1, R2, R3, R4, R5, X1, X2, X3, m and n have the significances given in claim 1, and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for the control of pests on domestic and farm animals.Type: GrantFiled: May 16, 2002Date of Patent: December 23, 2003Assignee: Novartis Animal Health US, Inc.Inventors: Pierre Ducray, Jacques Bouvier, Urs Müller
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Publication number: 20030229092Abstract: Bradykinin B1-receptor antagonists of formula 1Type: ApplicationFiled: January 14, 2002Publication date: December 11, 2003Applicant: PHARMACOPEIA, INC.Inventors: Michael H.J. Ohlmeyer, John G. Baldwin, Roland E. Dolle, Vidyadhar Paradkar, Jorge Gabriel Quintero, Gonghua Pan
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Publication number: 20030229110Abstract: Novel substituted triazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.Type: ApplicationFiled: March 26, 2003Publication date: December 11, 2003Applicant: SmithKline Beecham CorporationInventors: Jerry L. Adams, Dennis Lee
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Patent number: 6656910Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.Type: GrantFiled: August 10, 2001Date of Patent: December 2, 2003Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
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Patent number: 6656911Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.Type: GrantFiled: April 18, 2002Date of Patent: December 2, 2003Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W Spruce
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Patent number: 6653330Abstract: A compound of formula (I) or a pharmacologically acceptable prodrug or salt thereof which exhibits excellent antifungal activity: wherein Ar1 represents a phenyl group or the like; Ar2 represents a phenylene group or the like. X represents a sulfur atom or a methylene group. R1 represents a hydrogen atom or a C1-3 alkyl group; R2 represents a hydrogen atom or a C1-3 alkyl group; and R3 represents an optionally substituted C6-10 aryl group or the like. Fungal infections may be prevented and/or treated by administering said compound (I) or said prodrug or salt thereof.Type: GrantFiled: September 27, 2002Date of Patent: November 25, 2003Assignee: Sankyo Company, LimitedInventors: Takuya Uchida, Toshiyuki Konosu
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Publication number: 20030208073Abstract: The invention relates to novel substituted N-aryl nitrogen-containing heterocyclic compounds of the general formula (I) 1Type: ApplicationFiled: January 29, 2003Publication date: November 6, 2003Inventors: Karl-Heinz Linker, Kurt Findeisen, Otto Schallner, Andreas Lender, Hans-Joachim Santel, Markus Dollinger, Akihiko Yanagi, Toshio Goto
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Publication number: 20030203914Abstract: Compounds of formula (I):- 1Type: ApplicationFiled: March 12, 2003Publication date: October 30, 2003Inventors: Roger Peter Dickinson, Christopher Gordon Barber
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Publication number: 20030191155Abstract: A compound of the formula (I): 1Type: ApplicationFiled: February 19, 2003Publication date: October 9, 2003Inventors: Satoshi Aoki, Toshiya Nakagawa, Nobukiyo Konishi, Katsuya Nakamura, Hiroki Omori, Ariyoshi Kubota, Norio Hashimoto