Acyclic Nitrogen Bonded Directly To A -c(=x)- Group, Wherein X Is Chalcogen Patents (Class 546/308)
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Publication number: 20100190777Abstract: Compounds of formula I active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. Formula (I) wherein Ar is optionally substituted heteroaryl; R2 is hydrogen, lower alkyl or halogen; U is selected from the group consisting of —S(O)2—, —C(X)—, —C(X)—N(R10)—, and —S(O)2—N(R10)—; R3 is optionally substituted lower alkyl, optionally substituted C3.6 cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl or optionally substituted heteroaryl; and wherein R1, R3, R4, m, L1, X R10 are as described herein.Type: ApplicationFiled: July 16, 2008Publication date: July 29, 2010Applicant: PLEXXIKON INC.Inventors: Guoxian Wu, Jiazhong Zhang, Yong-Liang Zhu, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, Dean R. Artis, James Tsai
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Patent number: 7727996Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: September 28, 2006Date of Patent: June 1, 2010Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Christopher Michael Semko, Ying-zi Xu, Frank Stappenbeck, Jenifer Lea Smith, Kassandra Inez Rossiter, Juri Y. Fukuda, Andrei W. Konradi
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Publication number: 20100069443Abstract: This invention provides a novel COX-1-selective inhibitor. This invention relates to a novel compound represented by the formula below or a salt thereof. This invention also relates to an analgesic agent, an antiinflammatory agent, an antitumor agent, an antiplatelet aggregation agent, and a cyclooxygenase-1-selective inhibitor comprising, as an active ingredient, such compound or salt thereof.Type: ApplicationFiled: September 7, 2007Publication date: March 18, 2010Applicant: National University Corporation Okayama UniversityInventors: Hiroki KAKUTA, Kenji SASAKI, Hiroyuki ODA, Xiaoxia ZHENG, Shun HARADA
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Patent number: 7666866Abstract: This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt of the compound) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: November 15, 2005Date of Patent: February 23, 2010Assignee: Eli Lilly and CompanyInventors: Jeffry Bernard Franciskovich, David Kent Herron, Valentine Joseph Klimkowski, Angela Lynn Marquart, John Joseph Masters, David Mendel, Andrew Michael Ratz, Gerald Floyd Smith, Michael Robert Wiley, Ying Kwong Yee
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Publication number: 20090318506Abstract: Flupirtine acid addition salts having the following formula (2), wherein R represents a substituted or unsubstituted C1-C12-alkyl or a substituted or unsubstituted C6-C10-aryl group, have been prepared.Type: ApplicationFiled: June 9, 2009Publication date: December 24, 2009Applicant: AWD. PHARMA GMBH & CO. KGInventors: Christoph Hoock, Asal Qadan
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Publication number: 20090306150Abstract: The preparation of flupirtine carboxylate acid addition salts having the following formula (2), wherein R represents hydrogen or a C1-C6 alkyl group, with the proviso that RCOOH is neither maleic acid nor gluconic acid, is described.Type: ApplicationFiled: June 9, 2009Publication date: December 10, 2009Applicant: AWD. PHARMA GMBH & CO. KGInventors: Christoph Martin Hoock, Asal Qadan
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Publication number: 20090142554Abstract: A process for printing an image on a substrate by means of an ink-jet printer which comprises applying thereto a composition comprising a liquid medium and a mono-azo compound of Formula (1) and salts thereof: wherein: D is an optionally substituted aryl group carrying at least one direct substituent selected from the group consisting of —SO3H, —CO2H, —PO3H2 or an optionally substituted nitrogen heteroaryl group carrying at least one direct substituent selected from the group consisting of —SO3H, —CO2H, —PO3H2; R1 is H: optionally substituted alkyl: amino: —NR4R5; wherein R4 is H, optionally substituted alkyl, optionally substituted alkoxy, optionally substituted acyl, optionally substituted aryl, optionally substituted heterocyclyl; and R5 is optionally substituted alkyl, optionally substituted alkoxy, optionally substituted acyl, optionally substituted aryl, optionally substituted heterocyclyl: —OR6; wherein R6 is H or optionally substituted alkyl: or —SR7; wherein R7 is optionally substituted alkyl; RType: ApplicationFiled: October 13, 2006Publication date: June 4, 2009Inventors: Gavin Wright, Rachel Anne James, Roy Bradbury, Lynn Bradbury
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Patent number: 7501413Abstract: The invention is concerned with novel dicarboxamide derivatives of formula (I) wherein A, B, Rc, D and E are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.Type: GrantFiled: October 31, 2005Date of Patent: March 10, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Markus Boehringer, Katrin Groebke Zbinden, Wolfgang Haap, Hans Hilpert, Jacques Himber, Roland Humm, Hans Iding, Dietmar Knopp, Narendra Panday, Fabienne Ricklin, Christoph Martin Stahl
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Publication number: 20080305049Abstract: The invention relates to bifunctional conjugates comprising a receptor ligand moiety and a metal binding moiety and complexes thereof with paramagnetic lanthanide or transition metals, and to the use of the metal complexes as contrast agents in magnetic resonance imaging (MRI) of tumors and other abnormalities.Type: ApplicationFiled: January 31, 2006Publication date: December 11, 2008Inventors: Hadassa Degani, David Stein
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Patent number: 7435743Abstract: Pyrimidine compounds of general formula: wherein —R1 represents in which R11 is hydrogen, C1-6 alkyl, halogen, hydroxy, C1-12 alkoxy, nitro, amino, C1-6 alkylsulfonylamino, C1-6 alkoxycarbonyl, C1-6 alkylamino, di (C1-6 alkyl)amino, C1-6 alkanoylamino, phenyl C1-6 alkylamino, phenylsulfonylamino, or —O—(CH2)n—R111; R2 represents hydrogen or halogen; R3 represents hydrogen, —CR31R32R33; R4 is hydrogen, carbamoyl, CN, carboxyl, etc.; R5 is amino, C1-6 alkylamino, di C1-6 alkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.Type: GrantFiled: September 30, 2005Date of Patent: October 14, 2008Assignee: Bayer AktiengesellschaftInventors: Toshiki Murata, Masaomi Umeda, Sachiko Sakakibara, Takashi Yoshiro, Hiroki Sato, Tsutomu Masuda, Yuji Koriyama, Mitsuiyuki Shimada, Takuya Shintani, Hiroshi Kadono, Timothy B. Lowinger, Karl B. Ziegelbauer, Kinji Fuchikami, Hiroshi Komura
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Patent number: 7432281Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: GrantFiled: October 7, 2004Date of Patent: October 7, 2008Assignee: Renovis, Inc.Inventors: Michael G. Kelly, Satyanarayana Janagani, Ravindra B. Upasani
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Publication number: 20080234273Abstract: Compounds of formula (I) wherein R1, R2, R3, and HET-1 are as described in the specification, and their salts, are activators of glucokinase (GLK) and are thereby useful in the treatment of for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.Type: ApplicationFiled: June 3, 2006Publication date: September 25, 2008Inventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
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Patent number: 7129252Abstract: The present invention relates to six membered amino-amide derivatives, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states associated with angiogenesis and/or increased vascular permeability, to their use as medicaments and to their use in the manufacture of medicaments for use in the production of antiangiogenic and/or vascular permeability reducing effects in warm-blooded animals such as humans.Type: GrantFiled: June 2, 2004Date of Patent: October 31, 2006Inventor: Guoqing P Chen
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Patent number: 7015237Abstract: Selective MMP-13 inhibitors are pyridine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: R1 and R2 independently are hydrogen, halo, hydroxy, C1–C6 alkyl, C1–C6 alkoxy, C2–C6 alkenyl, C2–C6 alkynyl, NO2, NR4R5, CN, or CF3; E is independently O or S; A and B independently are OR4 or NR4R5; R4 and R5 independently are H, C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is an integer of from 0 to 6.Type: GrantFiled: May 10, 2004Date of Patent: March 21, 2006Assignee: Warner-Lambert CompanyInventors: Nicole Chantel Barvian, David Thomas Connor, Patrick Michael O'Brien, Daniel Fred Ortwine, William Chester Patt, Michael William Wilson
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Patent number: 6969723Abstract: Compounds of general formula (I), wherein R4 and R5 stand for hydrogen atom or form together an 1,3-butadienyl group, optionally substituted by a methylenedioxy group or one or more straight or branched C1-4 alkyl group, straight or branched C1-4 alkoxy group, hydroxy group or halogen atom; are strong adenosine A3 receptor ligands preferably antagonists.Type: GrantFiled: May 29, 2002Date of Patent: November 29, 2005Assignee: Sanofi - AventisInventors: Peter Arányi, László Balázs, Mária Balogh, Imre Bata, Sándor Bátori, Lajos T. Nagy, Geza Tímári, Kinga Boér, Olivier Finance, Zoltán Kapui, Endre Mikus, Zsuzsanna Szamosvölgyi, Gábor Szeleczky, Katalin Urbán-Szabó
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Patent number: 6949539Abstract: The invention provides compounds of general formula (I) in which m, A, R1 and Ar have the meanings defined in the specification; a process for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.Type: GrantFiled: June 1, 2001Date of Patent: September 27, 2005Assignee: AstraZeneca ABInventors: Lilian Alcaraz, Mark Furber
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Publication number: 20040214846Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII) 1Type: ApplicationFiled: May 18, 2004Publication date: October 28, 2004Applicant: Elan Pharmaceuticals, Inc.Inventors: Roy Hom, Shumeye S. Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Y. Fang
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Publication number: 20040214868Abstract: The invention related to novel compounds of Formula (I) or a salt, solvate or prodrug thereof, wherein R1, R2, R3, n and m are as described in the specification, useful in the treatment of a 1Type: ApplicationFiled: June 1, 2004Publication date: October 28, 2004Inventors: Barry Raymond Hayter, Gordon Stuart Currie, Rodney Brian Hargreaves, Roger James, Clifford David Jones, Darren McKerrecher, Joanne Victoria Allen, Peter William Rodney Caulkett, Craig Johnstone, Harold Gaskin
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Publication number: 20040058960Abstract: The present application describes modulators of CCR3 of formula (I): 1Type: ApplicationFiled: June 19, 2003Publication date: March 25, 2004Inventors: Soo S. Ko, George V. Delucca, John V. Duncia, Joseph B. Santella, Dean A. Wacker
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Publication number: 20040048904Abstract: Amide compounds of the formula: 1Type: ApplicationFiled: September 4, 2003Publication date: March 11, 2004Applicant: Fujisawa Pharmaceutical Co. Ltd.Inventors: Akira Yamada, Satoshi Aoki
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Patent number: 6699990Abstract: The present patent application relates to 3-(2,5-diaminophenyl)acrylamide derivatives of general formula (I) or to physiologically tolerated, water-soluble-salts thereof and to agents containing said compounds and used for oxidative dyeing of fibers.Type: GrantFiled: October 21, 2002Date of Patent: March 2, 2004Assignee: Wella AktiengesellschaftInventors: Laurent Chassot, Hans-Juergen Braun
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Publication number: 20040014968Abstract: 2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 3-position being a substituted phenyl group and at the 2-position being a methyl cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.Type: ApplicationFiled: July 9, 2003Publication date: January 22, 2004Inventors: Fred Thomas Bizzarro, Wendy Lea Corbett, Joseph Francis Grippo, Nancy-Ellen Haynes, George William Holland, Robert Francis Kester, Paige Erin Mahaney, Ramakanth Sarabu
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Patent number: 6677360Abstract: The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases. The compounds according to the invention have the formula (1) wherein R1, R2, U, V, A, B, W, R3, C and R4 have the meaning as defined in the claims.Type: GrantFiled: April 6, 2001Date of Patent: January 13, 2004Assignee: Bayer AktiengesellschaftInventors: Markus Albers, Klaus Urbahns, Andrea Vaupel, Michael Härter, Delf Schmidt, Beatrix Stelte-Ludwig, Christoph Gerdes, Elke Stahl, Jörg Keldenich, Ulf Brueggemeier, Klemens Lustig
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Patent number: 6673789Abstract: Compounds of formula (I): or a pharmaceutically acceptable salt thereof, or solvate of either entity, wherein R4 is a guanidinyl moiety and the other substituents are as defined in the text, are urokinase inhibitors.Type: GrantFiled: March 12, 2003Date of Patent: January 6, 2004Assignee: Pfizer, Inc.Inventors: Roger Peter Dickinson, Christopher Gordon Barber
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Patent number: 6664279Abstract: A therapeutic or preventive agent for liver diseases, containing as an active ingredient a diaminotrifluoromethylpyridine derivative represented by the formula (I) or its salt: wherein X is a —CW1R1 group, a —COCOR2 group, a —CW1NHCOR2 group, a —C(═W1)W2R3 group or a —CW1N(R4)R5 group; Y is an alkyl group, a —CW3R6 group, a —COCOR7 group, a —NHCOR7 group, a —C(═W3)W4R8 group, a —(NH)mSO2R9 group, a —(NH)mSO2OR10 group or a —(NH)mSO2N(R11)R12 group; each of R1, R6 and R9 is a chain hydrocarbon group, a monocyclic hydrocarbon group, a polycyclic hydrocarbon group, a monocyclic heterocycle group or a polycyclic heterocycle group; each of R2 and R7 is an alkyl group, an alkoxy group, a phenyl group or a phenoxy group; each of R3, R8 and R10 is an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a phenyl group or a benzyl group; each of R4, R5, R11 and R12 is an alkyl group; each of W1, W2, W3 anType: GrantFiled: July 29, 2002Date of Patent: December 16, 2003Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Shuichi Yotsuya, Kimie Sakai
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Remedies or preventives for digestive diseases containing diaminotrifluoromethylpyridine derivatives
Patent number: 6653333Abstract: A digestive system disease therapeutic or preventive agent containing as an active ingredient a diaminotrifluoromethylpyridine derivative represented by the formula (I) or its salt: wherein X is a —CW1R1 group, a —COCOR2 group, a —CW1NHCOR2 group, a —C(═W1)W2R3 group or a —CW1N(R4)R5 group; Y is an alkyl group, a —CW3R6 group, a —COCOR7 group, a —NHCOR7 group, a —C(═W3)W4R8 group, a —(NH)mSO2R9 group, a —(NH)mSO2OR10 group or a —(NH)mSO2N(R11)R12 group; each of R1, R6 and R9 is a chain hydrocarbon group, a monocyclic hydrocarbon group, a polycyclic hydrocarbon group, a monocyclic heterocycle group or a polycyclic heterocycle group; each of R2 and R7 is an-alkyl group, an alkoxy group, a phenyl group or a phenoxy group; each of R3, R8 and R10 is an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a phenyl group or a benzyl group; each of R4, R5, R11 and R12 is an alkyl group; each of W1, W2,Type: GrantFiled: July 29, 2002Date of Patent: November 25, 2003Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Shuichi Yotsuya, Hirohiko Kimura, Tadao Bamba -
Patent number: 6635665Abstract: A therapeutic or preventive agent for pulmonary insufficiency, containing as an active ingredient a diaminotrifluoromethylpyridine derivative represented by the formula (I) or its salt: wherein X is a —CW1R1 group, a —COCOR2 group, a —CW1NHCOR2 group, a —C(═W1)W2R3 group or a —CW1N(R4)R5 group; Y is an alkyl group, a —CW3R6 group, a —COCOR7 group, a —NHCOR7 group, a —C(═W3)W4R8 group, a —(NH)mSO2R9 group, a —(NH)mSO2OR10 group or a —(NH)mSO2N(R11)R12 group; each of R1, R6 and R9 is a chain hydrocarbon group, a monocyclic hydrocarbon group, a polycyclic hydrocarbon group, a monocyclic heterocycle group or a polycyclic heterocycle group; each of R2 and R7 is an alkyl group, an alkoxy group, a phenyl group or a phenoxy group; each of R3, R8 and R10 is an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a phenyl group or a benzyl group; each of R4, R5, R11 and R12 is an alkyl group; each of W1,Type: GrantFiled: July 25, 2002Date of Patent: October 21, 2003Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Kyuya Morino, Shuichi Yotsuya, Masashi Imamura
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Publication number: 20030195233Abstract: The invention relates to nicotinamide derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The nicotinamide derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions as well as for wounds healing.Type: ApplicationFiled: February 6, 2003Publication date: October 16, 2003Inventor: Thomas V. Magee
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Patent number: 6632823Abstract: In accordance with the present invention, a novel class of substituted pyridine compounds (optionally containing ether, ester, amide, ketone or thioether substitutions) that promote the release of ligands involved in neurotransmission have been discovered. In a particular aspect compounds of the present invention are capable of modulating acetylcholine receptors. The compounds of the present invention are capable of modulating acetylcholine receptors. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors.Type: GrantFiled: December 22, 1997Date of Patent: October 14, 2003Assignee: Merck & Co., Inc.Inventors: Jean-Michel Vernier, Nicholas D. P. Cosford, Ian A. McDonald
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Patent number: 6605626Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: September 21, 2001Date of Patent: August 12, 2003Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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Publication number: 20030139435Abstract: N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed.Type: ApplicationFiled: June 26, 2002Publication date: July 24, 2003Inventors: Gulzar Ahmed, Axel Metzger, Ian Henderson, David J. Diller, James Wen, Stephen T. Wrobleski, Katerina Leftheris
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Publication number: 20030125345Abstract: The present invention generally relates to nicotinic compounds, in the form of aryl substituted olefinic compounds, as well as pro-drug, N-oxide, metabolite and pharmaceutically acceptable salt forms thereof. Methods of modulating neurotransmitter release via administration of the compounds, pro-drugs, N-oxides and/or pharmaceutically acceptable salts are also disclosed.Type: ApplicationFiled: October 2, 2002Publication date: July 3, 2003Inventors: William S. Caldwell, Gary M. Dull, Balwinder S. Bhatti, Srishailkumar B. Hadimani, Haeil Park, Jared M. Wagner, Peter A. Crooks, Patrick M. Lippiello, Merouane Bencherif
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Patent number: 6586459Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: September 28, 2001Date of Patent: July 1, 2003Inventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Junior, Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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Publication number: 20030119749Abstract: The present invention provides novel compounds possessing one or more of the following activities: antibacterial, antifungal and antitumor activity.Type: ApplicationFiled: October 23, 2002Publication date: June 26, 2003Inventors: Wentao Zhang, Sebastian Johannes Reinhard Liehr, Mark Douglas Velligan, Natalia B. Dyatkina, Janos Botyanszki, Dong-Fang Shi, Christopher Don Roberts, Alexander Khorlin, Peter Harold Nelson, Joseph Martin Muchowski
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Patent number: 6583173Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: September 28, 2001Date of Patent: June 24, 2003Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffrey Bernard Franciskovich, Theodore Goodson, Junior, Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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Patent number: 6569860Abstract: This invention relates to compounds which are IP receptor antagonists and which are represented by Formula (I): wherein G2 is a heteroaryl group containing one or two nitrogen atoms substituted with a carboxylic acid group, said heteroaryl ring containing one or two nitrogen atoms, and G1 is as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.Type: GrantFiled: March 1, 2002Date of Patent: May 27, 2003Assignee: Roćhe Palo Alto LLCInventors: Francisco Javier Lopez-Tapia, Dov Nitzan, Counde O'Yang
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Patent number: 6566409Abstract: A lock unimolecular micelle includes at least one engineered acceptor specifically binding a ligand (or specifically a “key” unimolecular micelle) thereto. A key unimolecular micelle comprises a core molecule and a plurality of branches extending therefrom, at least one of the branches including a shank portion extending therefrom having a terminal moiety at an end thereof for binding to a complimentary acceptor of a lock unimolecular micelle. Together, the lock and key micelles form a unit, either irreversibly or reversibly bound wherein the lock micelles is a soluble receptor engineered to specifically bind to the specifically engineered key micelle.Type: GrantFiled: May 8, 2000Date of Patent: May 20, 2003Assignee: University of South FloridaInventors: George R. Newkome, Charles N. Moorefield, Gregory Baker
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Patent number: 6563002Abstract: The present invention discloses biscyclopropanecarboxamide compounds and pharmaceutically acceptable salts thereof; and also NF-kappa B activation inhibitors, Inflammatory cytokine production inhibitors, matrix metalloprotease production inhibitors, inflammatory cell adhesion molecules incidence inhibitors, antiinflammatory agents, antirheumatic agents, immunosuppressive agents, cancerous metastasis inhibitors or antiviral agents each containing such a compound as the active ingredient.Type: GrantFiled: March 1, 2002Date of Patent: May 13, 2003Assignee: Ajinomoto Co., Inc.Inventors: Yukio Iino, Kohichi Fujita, Takashi Yamamoto, Kenji Takehana, Tsuyoshi Kobayashi
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Publication number: 20030083333Abstract: Disclosed are novel 1,4-disubstituted benzo-fused compounds wherein G, X, L, Q, n and Y are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.Type: ApplicationFiled: April 10, 2002Publication date: May 1, 2003Inventors: Pier Francesco Cirillo, Daniel R. Goldberg, Abdelhakim Hammach, Neil Moss, Kristen Mueller, John Robinson Regan
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Patent number: 6555561Abstract: This invention provides compounds of formula I having the structure Wherein substitutions at X, G, R1, R2, R3, R4, R5 are set forth in the specification.Type: GrantFiled: March 15, 2002Date of Patent: April 29, 2003Assignee: WyethInventors: Jonathan Bloom, Martin DiGrandi, Russell Dushin, Stanley Lang, Bryan O'Hara
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Publication number: 20030065188Abstract: This invention relates to novel compounds of Formula (I) to (VII), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: ApplicationFiled: September 6, 2002Publication date: April 3, 2003Inventors: Katherine Louisa Widdowson, Qi Jin
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Patent number: 6537994Abstract: This invention provides compounds of Formula I having the structure wherein, U, V, and W are as defined hereinbefore, or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, glaucoma, ocular hypertension and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.Type: GrantFiled: July 12, 2001Date of Patent: March 25, 2003Assignee: WyethInventors: Mark Anthony Ashwell, William Ronald Solvibile
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Publication number: 20020173631Abstract: Compounds of the formula 1Type: ApplicationFiled: May 8, 2002Publication date: November 21, 2002Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
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Patent number: 6472414Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2; Rx is H, alkyl, aryl or halogen; A is (1) a bond; (2) —O—; or (3) B is: and wherein L2, L1, R1, R2, R3, R3′, R3a, R3b, R4, R4′, R5, X, are as defined herein.Type: GrantFiled: May 18, 1999Date of Patent: October 29, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Jeffrey A. Robl, William A. Slusarchyk, Richard B. Sulsky, Joseph A. Tino
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Publication number: 20020035094Abstract: Selected novel substituted pyridine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: August 17, 2001Publication date: March 21, 2002Applicant: Amgen Inc.Inventors: Nathan B. Mantlo, Stephen T. Schlachter, John A. Josey
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Publication number: 20020026055Abstract: Compounds of the formula 1Type: ApplicationFiled: March 12, 2001Publication date: February 28, 2002Applicant: American Home Products CorporationInventors: Jonathan Bloom, Martin DiGrandi, Russell Dushin, Stanley Lang, Bryan O'Hara
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Publication number: 20010051727Abstract: An improved and efficient synthesis for the preparation of 2-amino-6-[(4-aminopiperidin-1-yl]methyl]pyridine, an intermediate compound in the preparation of muscarinic M3 receptor antagonists, includes as a final step the removal of trimethylacetyl and an amino protecting group from 2-trimethylacetyl-amino-6-[(4-protected aminopiperidin-1-yl)methyl]pyridine.Type: ApplicationFiled: March 5, 2001Publication date: December 13, 2001Inventors: Peter E. Maligres, Jaemoon Lee
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Patent number: 6316632Abstract: A process for preparing 2-phenyl-3-aminopyridine, and substituted phenyl derivatives and salts thereof.Type: GrantFiled: May 11, 2000Date of Patent: November 13, 2001Assignee: Pfizer IncInventors: Tamim F. Braish, Stephane Caron, Michael James Castaldi
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Patent number: 6316503Abstract: The invention provides compounds, compositions and methods for modulating the effects of LXR in a cell. The compounds and compositions are useful both as diagnostic indicators of LXR function and as pharmacologically active agents. The compounds and compositions find particular use in the treatment of disease states associated with cholesterol metabolism, particularly atherosclerosis and hypercholesterolemia.Type: GrantFiled: March 14, 2000Date of Patent: November 13, 2001Assignee: Tularik Inc.Inventors: Leping Li, Julio C. Medina, Kevin Lustig, Bei Shan, Hirohiko Hasegawa, Serena T. Cutler, Jiwen Liu, Liusheng Zhu
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Patent number: 6313151Abstract: This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: March 31, 2000Date of Patent: November 6, 2001Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee