Acyclic Chalcogen Bonded Directly To Ring Carbon Of The Bicyclo Ring System Patents (Class 546/116)
-
Publication number: 20080269279Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia.Type: ApplicationFiled: April 7, 2008Publication date: October 30, 2008Inventors: Matthew J. Clements, John S. Debenham, Jeffrey J. Hale, Christina B. Madsen-Duggan, Thomas F. Walsh, Andrey V. Peresypkin, Roy Helmy
-
Publication number: 20080262029Abstract: The present invention is directed to novel acid salt forms and base salt forms of the compound gabaoxadol (4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol) and hydrates, solvates and polymorphic forms thereof. The invention is further concerned with pharmaceutical compositions containing the salt forms as an active ingredient, methods for treatment of disorders susceptible to amelioration by GABAA receptor agonism with the salt forms, and processes for the preparation of the salt forms.Type: ApplicationFiled: April 25, 2006Publication date: October 23, 2008Applicant: H. Lundbeck A/SInventors: Louis S. Crocker, Jerry A. Murry, Karthik Nagapudi, Kara Beth Rubin
-
Patent number: 7439247Abstract: The present invention discloses compounds corresponding to formula wherein A, R, X, Y, R, R1 and R2 are as defined above, pharmaceutical formulations, methods of making and uses thereof.Type: GrantFiled: November 30, 2005Date of Patent: October 21, 2008Assignee: Roche Palo Altop LLCInventors: Jian Jeffrey Chen, Nolan James Dewdney, Christoph Martin Stahl
-
Patent number: 7423152Abstract: The present invention provides a process for the manufacture of the compound of formula (1): which is a key intermediate in the manufacture of camptothecin (CPT). This compound continues to serve as an attractive and promising lead structure for the development of new anti-cancer drugs.Type: GrantFiled: February 17, 2006Date of Patent: September 9, 2008Assignee: Hoffman-La Roche Inc.Inventor: Rene Peters
-
Patent number: 7407972Abstract: The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thrombotic disorders. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.Type: GrantFiled: December 20, 2004Date of Patent: August 5, 2008Assignee: Pfizer Inc.Inventor: Jeremy John Edmunds
-
Patent number: 7371752Abstract: Disclosed are compounds of the formula: wherein X, Q, W and are as defined herein. These compounds are agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.Type: GrantFiled: December 3, 2004Date of Patent: May 13, 2008Assignee: Neurogen CorporationInventors: Guolin Cai, Pamela Albaugh, Jun Yuan
-
Patent number: 7371863Abstract: The present invention relates to a new method of preparing gaboxadol (THIP), which is useful for treating sleep disorders. In particular a method of preparing THIP comprising reacting a compound of formula (8b) or a salt thereof with an acid, typically a mineral acid, to obtain THIP as an acid addition salt.Type: GrantFiled: September 1, 2004Date of Patent: May 13, 2008Assignee: H. Lundbeck A/SInventors: Hans Petersen, Michael Bech Sommer, Robert Dancer
-
Patent number: 7365079Abstract: The present invention relates to a compound of the formula (I): wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine or nitrogen, said methine being optionally substituted by a substituent, and at least two of T, U, V and W are said methine groups; and X is nitrogen or methine. The compounds of the present invention are useful as agents for the treatment of various kinds of diseases related to NPY, for example, cardiovascular disorders, nervous system disorders, genitative diseases, metabolic diseases, genital or reproductive disorders, gastrointestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.Type: GrantFiled: November 25, 2003Date of Patent: April 29, 2008Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Norikazu Otake, Yuji Haga, Makoto Jitsuoka, Akio Kanatani
-
Publication number: 20080039469Abstract: Muscarinic agonists of the formula (I) with M1 selectivity which are useful as agents for stimulating the cognitive functions of the brain.Type: ApplicationFiled: December 6, 2004Publication date: February 14, 2008Applicant: MUSCAGEN LIMITEDInventors: Maxime Buffat, Eric James Thomas, Robin Havard Davies
-
Patent number: 7323494Abstract: Disclosed is a compound of having the formula: pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as defined herein. The compounds, salts and solvates of this invention are useful as LXR agonists.Type: GrantFiled: March 26, 2003Date of Patent: January 29, 2008Assignee: SmithKline Beecham CorporationInventors: Scott K. Thompson, James S. Frazee, Lara S. Kallander, Chun Ma, Joseph Marino, Michael J. Neeb, Ajita Bhat
-
Patent number: 7304072Abstract: Compounds represented by the general formula (I) wherein Ar1 represents an aryl or heteroaryl which may be substituted; n represents 0 or 1; T, U, V and W each independently represent a nitrogen atom or a methine group which may have a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, wherein at least two of which represent said methine group; X represents methine, hydroxy substituted methine or nitrogen atom; Y represents an imino which may be substituted with lower alkyl, or oxygen; and a salt, ester or N-oxide derivative thereof. The compounds exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metabolic diseases, sexual and reproductive dysfunctions, gastro-intestinal disorders, respiratory disorders, inflammation or glaucoma, and the like.Type: GrantFiled: August 23, 2004Date of Patent: December 4, 2007Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takehiro Fukami, Akio Kanatani, Akane Ishihara, Yasuyuki Ishii, Toshiyuki Takahashi, Yuji Haga, Toshihiro Sakamoto, Takahiro Itoh, Masato Chiba
-
Patent number: 7262300Abstract: Two new crystalline monhydrates and two new crystalline anhydrates of gaboxadol are disclosed together with methods for preparing them.Type: GrantFiled: January 28, 2005Date of Patent: August 28, 2007Assignee: Merck Sharp & Dohme Ltd.Inventor: Vincent Brett Cooper
-
Patent number: 7230009Abstract: Pyridoxal analogues can be useful for treating B6 deficiency and related diseases; cardiovascular and related diseases; melanoma and related diseases; and symptoms thereof. One such analogue is a compound of the formula: or a pharmaceutically acceptable acid addition salt thereof, in which R1 is alkyl, alkenyl, in which alkyl or alkenyl can be interrupted by nitrogen, oxygen, or sulfur, and can be substituted at the terminal carbon by hydroxy, alkoxy, alkanoyloxy, alkanoyloxyaryl, alkoxyalkanoyl, alkoxycarbonyl, or dialkylcarbamoyloxy; alkoxy; dialkylamino; alkanoyloxy; alkanoyloxyaryl; alkoxyalkanoyl; alkoxycarbonyl; dialkylcarbamoyloxy; or aryl, aryloxy, arylthio, or aralkyl, in which aryl can be substituted by alkyl, alkoxy, amino, hydroxy, halo, nito, or alkanoyloxy. These analogues can be administered, either alone or concurrently with known medications, to treat the above-described diseases.Type: GrantFiled: June 3, 2003Date of Patent: June 12, 2007Assignees: Medicure, Inc., University of ManitobaInventors: Wasimul Haque, James L. Charlton
-
Patent number: 7220868Abstract: There are described novel rhodamine dye compounds and imaging members and imaging methods, including thermal imaging members and imaging methods, utilizing the compounds. The dye compounds exhibit a first color when in the crystalline form and a second color, different from the first color, when in the liquid, amorphous form.Type: GrantFiled: March 6, 2006Date of Patent: May 22, 2007Assignee: Zink Imaging, LLCInventors: Kap-Soo Cheon, Michael P. Filosa, John L. Marshall
-
Patent number: 7220860Abstract: A compound has the formula in racemic form, enantiomerically enriched form or enantiomerically pure form. R6 is preferably —Si(R8R9R10) or —(R7)Si(R8R9R10), wherein R7 is an alkylene group, an alkenylene group, or an alkynylene group; and R8, R9 and R10 are independently a C1-10 alkyl group, a C2-10 alkenyl group, a C2-10 alkynyl group, an aryl group or a —(CH2)NR11 group, wherein N is an integer within the range of 1 through 10 and R11 is a hydroxy group, alkoxy group, an amino group, an alkylamino group, a dialkylamino group, a halogen atom, a cyano group, —SRc or a nitro group. R1–R4 can be broadly substituted. R5 is preferably a C1-10 alkyl group, an alkenyl group, an alkynyl group, or a benzyl group. R13 is preferably H, F or —CH3. R16 is R16 is —C(O)Rf or H. The E-ring (the lactone ring) may be opened. A method of synthesis of compound (1) and intermediates in the synthesis thereof are provided.Type: GrantFiled: August 16, 2004Date of Patent: May 22, 2007Assignee: University of PittsburghInventors: Dennis P. Curran, Bom David, Thomas G. Burke
-
Patent number: 7205401Abstract: Diketo- and pyridine-containing chiral crown ligands having at least two chiral bulky groups attached to two different chiral carbon atoms of the crown that are covalently bonded to or coated on suitable solid supports, and further coated by hydrophobic organic solvents are disclosed. These compositions and associated methods are characterized by selectivity of several target amine or amino acid enantiomers over their counter-enantiomers and derivatives. The composition preferably has an ?-value greater than or equal to 4. This allows for the separation of such enantiomers with non-chromatographic resin bed separations of three separation stages or less.Type: GrantFiled: September 16, 2003Date of Patent: April 17, 2007Assignee: IBC Advanced Technologies, Inc.Inventors: Ronald L. Bruening, Krzysztof E. Krakowiak
-
Patent number: 7196093Abstract: 1. The present invention provides compositions and methods for reversibly inhibiting S-adenosyl-L-homocysteine (SAH) hydrolase. The compounds of the present invention can be used as an anti-hemorrhagic viral infection agent, an immunosuppressant, a homocysteine lowering agent, or an anti-neoplasm agent. The compositions and methods of the present invention can be used for the prevention and treatment of hemorrhagic virus infection, autoimmune diseases, autograft rejection, neoplasm, hyperhomocysteineuria, cardiovascular disease, stroke, Alzheimer's disease, multiple sclerosis or diabetes.Type: GrantFiled: April 9, 2003Date of Patent: March 27, 2007Assignee: General AtomicsInventor: Chong-Sheng Yuan
-
Patent number: 7132418Abstract: The present invention relates to a series of peptidyl heterocyclic ketones which are inflammatory cell serine protease inhibitors and their compositions and methods for the prevention and treatment of a variety of immunomediated inflammatory disorders. More particularly, these compounds are potent and selective inhibitors of tryptase and are therefore effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis.Type: GrantFiled: July 25, 2002Date of Patent: November 7, 2006Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Michael J. Costanzo, Bruce E. Maryanoef, Stephen C. Yabut
-
Patent number: 7087756Abstract: The invention provides compounds of formula I, wherein X, Y, R1, R2, and R3 are as defined in the description, and the preparation thereof. The compounds of formula I are useful as pharmaceuticals.Type: GrantFiled: August 14, 2002Date of Patent: August 8, 2006Assignee: Novartis AGInventors: Samuel Hintermann, Bastian Hengerer, Ulrike Von Krosigk
-
Patent number: 7067515Abstract: The invention provides compounds of Formula I: where in W is These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful to treat diseases or conditions in which ?7 is known to be involved.Type: GrantFiled: June 6, 2002Date of Patent: June 27, 2006Assignee: Pfizer Inc.Inventors: Donn G. Wishka, Steven Charles Reitz, David W. Piotrowski, Vincent E. Groppi, Jr.
-
Patent number: 7053219Abstract: The invention relates to isoxazolopyridone derivatives of a formula (I-a): wherein R1a represents an optionally-substituted heteroaryl or phenyl group, R2a represents an optionally-substituted phenyl or heteroaryl group, and R3a represents a methyl group, provided that, (1) when R1a is an unsubstituted phenyl group, then R2a must not be a para-substituted phenyl group of which the substituent is any of a methoxy group, a chloro group, a methyl group, a trifluoromethyl group, a fluoro group, a bromomethyl group or a dimethylaminomethyl group, and R2a must not be an unsubstituted heteroaryl group, and (2) when R1a is a 4-tolyl group or a 4-fluorophenyl group, then R2a must not be an unsubstituted phenyl group, a 4-methoxyphenyl group or a 4-fluorophenyl group, or their pharmaceutically-acceptable salts.Type: GrantFiled: December 10, 2003Date of Patent: May 30, 2006Assignee: Banyu Pharmaceutical Co. Ltd.Inventors: Masayuki Nakamura, Hideki Kurihara, Mitsuru Ohkubo, Naohiro Tsukamoto
-
Patent number: 6982333Abstract: The present invention provides a short, convergent total synthesis of camptothecin and related compounds which consists of a novel 4+1 radical annulation. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.Type: GrantFiled: September 16, 2003Date of Patent: January 3, 2006Assignee: University of PittsburghInventors: Dennis P. Curran, Hubert Josien, Sung Bo Ko
-
Patent number: 6927293Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.Type: GrantFiled: August 26, 2002Date of Patent: August 9, 2005Assignee: Merck & Co., Inc.Inventors: Yuntae Kim, Barbara Hanney, Keith L. Spencer, George D. Hartman, Kenneth L. Arrington
-
Patent number: 6911543Abstract: The invention provides compounds of Formula I: wherein Azabicyclo is These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which ?7 is known to be involved.Type: GrantFiled: October 1, 2002Date of Patent: June 28, 2005Assignee: Pfizer Inc.Inventors: Daniel Patrick Walker, David W. Piotrowski, Eric Jon Jacobsen, Brad A. Acker, Donn G. Wishka, Steven Charles Reitz
-
Patent number: 6878705Abstract: The invention provides a compound of formula I: wherein G, R2, R3, and R4 have any of the values defined in the specification, or a pharmaceutically acceptable salt thereof, as well as processes and intermediates useful for preparing such compounds or salts, and methods of treating a herpesvirus infection using such compounds or salts.Type: GrantFiled: January 14, 2003Date of Patent: April 12, 2005Assignee: PfizerInventors: Michele M. Cudahy, Mark E. Schnute, Steven P. Tanis, William R. Perrault, Paul Matthew Herrinton, Sajiv K. Nair
-
Patent number: 6867217Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyridone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: GrantFiled: May 18, 2000Date of Patent: March 15, 2005Assignee: Pharmacia CorporationInventors: Michael S. South, Qingping Zeng, Ashton T. Hamme, II, Melvin L. Rueppel
-
Patent number: 6841559Abstract: Novel pyridinones and their derivatives which are effective in treating or preventing Gram-negative bacterial infections are provided. The pyridinones are stable and easily derivatized; the methods by which these derivatizations occur is described. Two regioselective and functional group tolerant methods for the synthesis of the novel pyridinones are also provided. One such synthetic method involves reacting an imine and a Meldrum's acid derivative in solution. The other synthetic method is a solid phase synthesis of the pyridinones in which an imine is prepared bound to a solid support and a Meldrum's acid derivative is reacted with the imine. Novel imine intermediates useful in the solid phase and solution methods of synthesizing the pyridionones are also described.Type: GrantFiled: November 20, 2000Date of Patent: January 11, 2005Assignee: Washington University of St. LouisInventors: Frederic Almqvist, Hans Emtenas, Scott J. Hultgren, Jerome S. Pinkner
-
Publication number: 20040259907Abstract: The invention provides a compound of formula I: 1Type: ApplicationFiled: January 14, 2003Publication date: December 23, 2004Inventors: Michele M. Cudahy, Mark E. Schnute, Steven P. Tanis, William R. Perrault, Paul Matthew Herrinton, Sajiv K. Nair
-
Patent number: 6833370Abstract: Heterocyclic substituted aminoazacyclic compounds of formula I Z—R3 I, wherein Z is a defined aminoazacycle and R3 is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: April 26, 2000Date of Patent: December 21, 2004Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Kevin B. Sippy, Jerome F. Daanen, Keith Brian Ryther, Jianguo Ji
-
Publication number: 20040254200Abstract: Compounds of formulae (1a) and (1b) are described: in which the dashed line represents an optional bond; A is a —N=atom or a —N(Rb)—, —C(Rb)═ or —C(Rb)(RC)— group; Ra, Rb and Rc is each independently a hydrogen atom or an optionally substituted C1-6alkyl group; X is an —O— or —S— atom or —NH— group or substituted N atom; each Y is independently a N atom or CH group or substituted C atom; n is zero or the integer 1; Alk1 is an optionally substituted aliphatic or heteroaliphatic chain L1 is a covalent bond or a linker atom or group; Cy1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Ar is an optionally substituted aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof; The compounds are potent inhibitors of p38 kinase and are use in the prophylaxis or treatment of p38 kinase medType: ApplicationFiled: July 20, 2004Publication date: December 16, 2004Inventors: Jeremy Martin Davis, Daniel Christopher Brookings, Barry John Langham
-
Publication number: 20040235848Abstract: Phenylalanine derivatives of the following formula, analogues thereof and pharmaceutically acceptable salts thereof have an antagonistic activity to &agr;4 integrin. They are used as therapeutic agents or preventive agents for various diseases concerning &agr;4 integrin in which &agr;4 integrin-depending adhesion process participates in the pathology, such as inflammatory diseases, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection.Type: ApplicationFiled: June 14, 2004Publication date: November 25, 2004Applicant: Ajinomoto Co., Inc.Inventors: Tatsuya Okuzumi, Kazuyuki Sagi, Toshihiko Yoshimura, Yuji Tanaka, Eiji Nakanishi, Miho Ono, Masahiro Murata
-
Publication number: 20040229889Abstract: A compound having the following formula (I): 1Type: ApplicationFiled: January 12, 2004Publication date: November 18, 2004Applicant: FUJISAWA PHARMACEUTICAL CO., LTD.Inventors: Yasuharu Urano, Shigeki Satoh, Naoki Ishibashi, Kazunori Kamijo
-
Patent number: 6809203Abstract: Thiazolo-, oxazolo- and selenazolo[4,5-c]quinolin-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators and induce cytokine biosynthesis, including interferon and/or tumor biosynthesis, necrosis factor, and inhibit the T-helper-type 2 immune response. The compounds are further useful in the treatment of viral and neoplastic diseases.Type: GrantFiled: December 2, 2003Date of Patent: October 26, 2004Assignee: 3M Innovative Properties CompanyInventors: John F. Gerster, Kyle J. Lindstrom, Gregory J. Marszalek, Bryon A. Merrill, John W. Mickelson, Michael J. Rice
-
Publication number: 20040209902Abstract: This invention relates to treating inflammatory and immune diseases with certain aminoquinoline compounds that bind to CXCR3 receptors. The aminoquinoline compounds are covered by the formula (I) shown below. Each variable is defined in the specification.Type: ApplicationFiled: April 6, 2004Publication date: October 21, 2004Inventors: Chu-Chung Lin, Jen-Fuh Liu, Chih-Wei Chang, Shu-Jen Chen, Yibin Xiang, Pei-Chin Cheng, Jiing-Jyh Jan
-
Patent number: 6803372Abstract: Compounds of the general formula (I): wherein Ar1 represents optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V, and W each independently represent nitrogen atom or optionally substituted methine group, where at least two of them represent the said methine group; X represents methine or hydroxy substituted methine; Y represents an optionally substituted imino or oxygen atom are described and claimed. These novel spiro compounds are useful as neuropeptide Y receptor antagonists and as agents for the treatment of various kinds of cardiovascular disorders, central nervous system disorders, metabolic diseases and the like.Type: GrantFiled: March 8, 2002Date of Patent: October 12, 2004Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takehiro Fukami, Akio Kanatani, Akane Ishihara, Yasuyuki Ishii, Toshiyuki Takahashi, Yuji Haga, Toshihiro Sakamoto, Takahiro Itoh
-
Patent number: 6797717Abstract: The invention relates to a novel anilide compound and a pharmaceutical composition comprising the same. The invention relates to a compound represented by the following general formula: represents a divalent residue of benzene with a substituent(s), heterocycle-condensed benzene which may or may not have a substituent, pyridine which may or may not have a substituent, cyclohexane or naphthalene Ar represents an aryl group which may or may not have a substituent, X represents —NH—, oxygen atom or sulfur atom; Y represents —NR4—, oxygen atom, sulfur atom, sulfoxide or sulfone; Z represents single bond or —NR5—; R4 represents hydrogen atom, a lower alkyl group, an aryl group or a silylated lower alkyl group which may or may not have a substituent; R5 represents hydrogen atom, a lower alkyl group, an aryl group or a silylated lower alkyl group which may or may not have a substituent; and n represents an integer of 0 to 15.Type: GrantFiled: December 19, 2001Date of Patent: September 28, 2004Assignee: Kowa Company, Ltd.Inventors: Kimiyuki Shibuya, Katsumi Kawamine, Yukihiro Sato, Toshiyuki Edano, Mitsuteru Hirata, Chiyoka Ozaki
-
Patent number: 6794393Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.Type: GrantFiled: April 18, 2002Date of Patent: September 21, 2004Assignee: Merck & Co., Inc.Inventors: Mark E. Fraley, Kenneth L. Arrington, Mark T. Bilodeau, George D. Hartman, William F. Hoffman, Yuntae Kim, Randall W. Hungate
-
Publication number: 20040176325Abstract: This invention relates to inhibitors of p38, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders mediated by p38.Type: ApplicationFiled: March 3, 2003Publication date: September 9, 2004Inventors: Mark Munson, James Rizzi, Martha Rodriguez, Ganghyeok Kim
-
Patent number: 6762301Abstract: A process for the preparation of a compound of the formula wherein the substituents are defined as set forth in the specification comprising reacting a compound of the formula with a 2-halo-3-quinoline-methanol of the formula to obtain a compound of the formula which is then cyclized to form the compound of Formula I.Type: GrantFiled: January 30, 2002Date of Patent: July 13, 2004Assignee: Societe de Conseils de Recherches et Applications Scientifiques (S.C.R.A.S.)Inventors: Dennis Bigg, Olivier Lavergne, Francesc Pla Rodas, Jacques Pommier, Gerard Ulibarri, Jerry Harnett, Alain Rolland, Anne-Marie Liberatore, Christophe Lanco, Jean-Bernard Cazaux, Christine Le Breton, Eric Manginot
-
Patent number: 6753331Abstract: The invention relates to heterocyclic derivatives of formula (I), or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect.Type: GrantFiled: January 4, 2001Date of Patent: June 22, 2004Assignee: AstraZeneca ABInventors: Peter WR Caulkett, Roger James, Stuart E Pearson, Anthony M Slater, Rolf P Walker
-
Publication number: 20040077680Abstract: The present invention relates to chemical compounds, pharmaceutical compositions comprising said compounds, uses of said compounds and compositions, methods of treatment employing said compounds and compositions, and processes for preparing said compounds. Specifically, this invention relates to novel 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. More specifically, the invention is related to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases.Type: ApplicationFiled: November 17, 2003Publication date: April 22, 2004Applicants: Telik, Inc., Sanwa Kagaku Kenkyusho Co., Ltd.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
-
Publication number: 20040048868Abstract: The invention is directed to physiologically active compounds of the general formula (Ix) 1Type: ApplicationFiled: October 24, 2002Publication date: March 11, 2004Inventors: Michael L. Edwards, Paul J. Cox, Shelley Amendola, Stephanie D. Deprets, Timothy A. Gillespy, Christopher D. Edlin, Andrew D. Morley, Charles J. Gardner, Brian Pedgrift, Herve Bouchard, Didier Babin, Laurence Gauzy, Alain Le-Brun, Tahir N. Majid, John C. Reader, Lloyd J. Payne, Nawaz M. Khan, Michael Cherry
-
Publication number: 20040043994Abstract: The present invention relates to a class of compounds represented by the Formula I.Type: ApplicationFiled: January 21, 2003Publication date: March 4, 2004Inventors: Ish Kumar Khanna, Yi Yu, Hwang-Fun Lu, Nizal S. Chandrakumar, Renee M. Huff, Mark Russell, Mark L. Boys, Lori A. Schretzman, Barbara B. Chen, Bipinchandra N. Desai, Srinivasan Raj Nagarajan, Alan F. Gasiecki, Thomas D. Penning, Thomas Rogers, John Adam Wendt, Albert Khilevich, Yaping Wang
-
Publication number: 20040033910Abstract: A composition comprising: (a) from 0.Type: ApplicationFiled: August 7, 2003Publication date: February 19, 2004Inventor: Ravindranath Mukkamala
-
Publication number: 20040024211Abstract: Compounds having the general structure 11 are provided: 1Type: ApplicationFiled: April 30, 2003Publication date: February 5, 2004Applicant: Chiron CorporationInventors: Rustum Boyce, David Duhl
-
Publication number: 20030216399Abstract: This invention is directed to compounds of the formula 1Type: ApplicationFiled: February 21, 2003Publication date: November 20, 2003Inventors: Philip Albert Carpino, David Andrew Griffith, Bruce Allen Lefker
-
Patent number: 6635633Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.Type: GrantFiled: August 10, 2001Date of Patent: October 21, 2003Assignee: Ortho-Pharmaceutical, Inc.Inventors: Hui Cai, James P. Edwards, Steven P. Meduna, Barbara A. Pio, Jianmei Wei
-
Publication number: 20030181420Abstract: Compounds, compositions and methods for modulating the activity of nuclear receptors are provided. In particular, heterocyclic compounds are provided for modulating the activity of nuclear receptors, including liver X receptor (LXR) and orphan nuclear receptors. In certain embodiments, the compounds are N-substituted pyridones.Type: ApplicationFiled: December 20, 2002Publication date: September 25, 2003Inventors: Christopher D. Bayne, Alan T. Johnson, Shao-Po Lu, Raju Mohan, Ronald C. Griffith
-
Publication number: 20030176432Abstract: Cyclic and heterocyclic N-substituted &agr;-iminohydroxamic and -carboxylic acidsType: ApplicationFiled: March 3, 2003Publication date: September 18, 2003Applicant: Aventis Pharma Deutschland GmbH.Inventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Eckart Bartnik, Klaus-Ulrich Weithmann
-
Patent number: 6620937Abstract: The present invention provides a short, convergent total synthesis of camptothecin and related compounds which consists of a novel 4+1 radical annulation. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.Type: GrantFiled: March 23, 2001Date of Patent: September 16, 2003Assignee: University of PittsburghInventors: Dennis P. Curran, Hubert Josien, Sung Bo Ko