Chalcogen Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/312)
-
Publication number: 20090093462Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds (I) pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: October 19, 2005Publication date: April 9, 2009Inventors: Ulricn Abel, Holger Deppe, Achim Feurer, Ulrich Gradler, Kerstin Otte, Renate Sekul, Meinolf Thiemann, Andreas Goutopoulos, Matthias Schwarz, Xuliang Jiang
-
Patent number: 7514564Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. 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, 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: GrantFiled: May 2, 2006Date of Patent: April 7, 2009Assignee: Amgen Inc.Inventors: Guoqing Chen, Jeffrey Adams, Jean Bemis, Lucian Di Pietro, Celia Dominguez, Daniel Elbaum, Julie Germain, Qi Huang, Joseph L. Kim, Xiaohu Ouyang, Vinod F. Patel, Leon M. Smith, Andrew Tasker, Ning Xi, Shimin Xu, Chester Chenguang Yuan, Michael Croghan, Tae-Seong Kim
-
Publication number: 20090082408Abstract: The present invention relates to novel heterocyclic derivatives of the general formula (I), their pharmaceutically acceptable salts, and their pharmaceutical compositions. The present invention more particularly provides novel compounds of the general formula (I).Type: ApplicationFiled: May 18, 2006Publication date: March 26, 2009Inventors: Surendrakumar Satyanarayan Pandey, Gajendra Singh, Kadnur Venkatachalapathi Sanjay, Bishwajit Nag
-
Publication number: 20090075968Abstract: The present invention relates to a compound of formula or a pharmaceutically acceptable salt thereof, wherein the variables are as defined.Type: ApplicationFiled: December 27, 2006Publication date: March 19, 2009Inventors: Junichi Sakaki, Masashi Kishida, Naoko Matsuura, Ichiro Umemura, Eiji Kawahara, Ken Yamada, Kazuhide Konishi, Yuki Iwaki, Hidetomo Imase, Takahiro Miyake
-
Patent number: 7476452Abstract: The present invention is generally directed to electroluminescent Ir(III) compounds, the substituted 2-phenylpyridines that are used to make the Ir(III) compounds, and devices that are made with the Ir(III) compounds.Type: GrantFiled: February 6, 2004Date of Patent: January 13, 2009Assignee: E. I. du Pont de Nemours and CompanyInventors: Kerwin D. Dobbs, Norman Herron, Viacheslav A. Petrov
-
Patent number: 7462634Abstract: The present invention relates to novel compounds, to pharmaceutical compositions comprising the compounds described herein, their pharmaceutically acceptable salts, hydrates and solvates, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme (11?HSD1).Type: GrantFiled: June 15, 2006Date of Patent: December 9, 2008Assignees: Agouron Pharmaceuticals, Inc., Pfizer IncInventors: Sajiv Krishnan Nair, Michael Siu, Wendy Dianne Taylor
-
Publication number: 20080300260Abstract: The present invention relates to heterocyclic compounds which are positive modulators of metabotropic glutamate receptor. The present invention also relates to the use of these compounds for preparing a pharmaceutical composition and to a method of treating a medical disorder, selected from neurological and psychiatric disorders associated with glutamate dysfunction.Type: ApplicationFiled: May 23, 2008Publication date: December 4, 2008Inventors: Herve GENESTE, Daryl Sauer, Wilfried Braje, Wilhelm Amberg, Mario Mezler, Margaretha Henrica Maria Bakker
-
Patent number: 7446117Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever and inflammation of a variety of conditions and diseases.Type: GrantFiled: September 12, 2003Date of Patent: November 4, 2008Assignee: Glaxo Group LimitedInventors: Paul Beswick, Neil Pegg, Martin Swarbrick, John Skidmore, Sandeep Modi
-
Patent number: 7432227Abstract: 4-Aminopicolinic acids having alkyl or alkenyl substituents in the 6-position and their amine and acid derivatives are potent herbicides demonstrating a broad spectrum of weed control.Type: GrantFiled: April 2, 2004Date of Patent: October 7, 2008Assignee: Dow AgroSciences LLCInventors: Terry William Balko, Ann Marie Buysse, Stephen Craig Fields, Nicholas Martin Irvine, William Chi-Leung Lo, Christian Thomas Lowe, John Sanders Richburg, Paul Richard Schmitzer
-
Publication number: 20080221240Abstract: The present invention generally provides compositions including carbon-containing molecules, and related methods. In some cases, the present invention relates to aromatic molecules comprising functional groups bonded to the aromatic portion of the molecule, including nonplanar portions of the molecules. Methods of the invention may provide the ability to introduce a wide range of functional groups to carbon-containing molecules. In some cases, methods of the invention may be performed using relatively mild reaction conditions, such as relatively low temperature, low pressure, and/or in the absence of strong acids or strong bases. The present invention may provide a facile and modular approach to synthesizing molecules that may be useful in various applications including photovoltaic devices, sensors, and electrodes (e.g., for electrocatalysis).Type: ApplicationFiled: March 7, 2008Publication date: September 11, 2008Applicant: Massachusetts Institute of TechnologyInventors: Timothy M. Swager, Wei Zhang
-
Publication number: 20080200523Abstract: The present invention provides derivatives of squaric acid, in particular derivatives of 3,4-diamino-cyclobut-3-ene-1,2-dione and tautomers and isomers thereof, as a single stereoisomer or a mixture of stereoisomers, or as a pharmaceutically acceptable salt thereof. These compounds show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: ApplicationFiled: February 21, 2007Publication date: August 21, 2008Inventors: Krishna K. Murthi, Roland Kostler, Chase Smith, Tilman Brandstetter, Arthur F. Kluge
-
Publication number: 20080196176Abstract: This invention relates to unsubstituted and polymeric leuco colorants for use as consumer product additives to indicate a product function by color change, to make attractive or distinctive visual effects, or to provide latent or delayed color generation. The colorants may be present in a stable, colorless state and may be transformed to an intense colored state upon exposure to certain physical or chemical changes. Alternatively, the colorants may be transformed from one color to another color upon exposure to certain physical or chemical changes. The colored form of the unsubstituted or polymeric leuco colorant may be transient, since the colorant can revert back to its colorless form or its original color after the physical or chemical activation has been removed or changed. Polymeric leuco colorants are typically comprised of at least two components: at least one leuco chromophore component and at least one polymeric component.Type: ApplicationFiled: February 6, 2008Publication date: August 21, 2008Inventors: Eduardo Torres, Patrick D. Moore, Joe Clark
-
Publication number: 20080196177Abstract: This invention relates to unsubstituted and polymeric leuco colorants for use as consumer product additives to indicate a product function by color change, to make attractive or distinctive visual effects, or to provide latent or delayed color generation. The colorants may be present in a stable, colorless state and may be transformed to an intense colored state upon exposure to certain physical or chemical changes. Alternatively, the colorants may be transformed from one color to another color upon exposure to certain physical or chemical changes. The colored form of the unsubstituted or polymeric leuco colorant may be transient, since the colorant can revert back to its colorless form or its original color after the physical or chemical activation has been removed or changed. Polymeric leuco colorants are typically comprised of at least two components: at least one leuco chromophore component and at least one polymeric component.Type: ApplicationFiled: February 6, 2008Publication date: August 21, 2008Inventors: Patrick D. Moore, Eduardo Torres
-
Publication number: 20080166299Abstract: The invention relates to radiolabeled compounds and their use in methods of imaging amyloid deposits, as well as to methods of their manufacture. The invention also relates to compounds for inhibiting the aggregation of amyloid proteins that form amyloid deposits, methods for delivering therapeutic agents to amyloid deposits, as well as methods of making compounds that inhibit the aggregation of amyloid proteins.Type: ApplicationFiled: December 6, 2007Publication date: July 10, 2008Applicant: Trustees of The University of PennsylvaniaInventors: Hank F. Kung, Mei Ping Kung
-
Publication number: 20080161345Abstract: The present invention relates to compounds that modulate various chemokine receptors. These compounds are useful for treating inflammatory and immune diseases.Type: ApplicationFiled: May 12, 2005Publication date: July 3, 2008Inventors: Solomon Ungashe, John Jessen Wright, Andrew Pennell
-
Patent number: 7351825Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.Type: GrantFiled: December 15, 2004Date of Patent: April 1, 2008Assignee: Japan Tobacco Inc.Inventors: Takashi Inaba, Julia Haas, Makoto Shiozaki, Nicole M. Littmann, Katsutaka Yasue, Steven W. Andrews, Atushi Sakai, Andrew M. Fryer, Takafumi Matsuo, Ellen R. Laird, Akira Suma, Yuichi Shinozaki, Yoshikazu Hori, Hiroto Imai, Tamotsu Negoro
-
Patent number: 7351835Abstract: A novel organic molecular catalysts represented by the following formula (1) or (2): and a method for carrying out asymmetric reactions/asymmetric synthesis using these organic molecular catalysts.Type: GrantFiled: March 10, 2005Date of Patent: April 1, 2008Assignee: Meiji Seika Kaisha Ltd.Inventors: Hiroaki Sasai, Shinobu Takizawa, Katsuya Matsui
-
Patent number: 7342115Abstract: 3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptor. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.Type: GrantFiled: November 7, 2003Date of Patent: March 11, 2008Assignee: Neurogen CorporationInventors: Alan J. Hutchison, Jun Yuan, Kyungae Lee, George D. Maynard, Bertrand L. Chenard, Nian Liu, Qin Guo, Zihong Guo, Peter Hrnciar
-
Patent number: 7332498Abstract: A method of modulating KSP kinesin activity in vitro comprising contacting KSP kinesin with at least one chemical entity chosen from compounds represented by Formula I: and pharmaceutically acceptable salts thereof, where the variables are as defined further herein.Type: GrantFiled: November 23, 2005Date of Patent: February 19, 2008Assignees: Cytokinetics, Inc., SmithKline Beecham CorporationInventors: Pu-Ping Lu, David J. Morgans, Jr., Bing Yao, Dashyant Dhanak, Steven David Knight
-
Patent number: 7320993Abstract: The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group, methods for the synthesis of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.Type: GrantFiled: June 16, 2000Date of Patent: January 22, 2008Assignee: Astellas Deutschland GmbHInventors: Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt, Katja Wosikowski, Isabel Schemainda
-
Patent number: 7320990Abstract: The invention provides a crystalline naphthalene-1,5-disulfonic acid salt of biphenyl-2-ylcarbamic acid 1-{9-[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydro-quinolin-5 -yl)ethylamino]nonyl}piperidin-4-yl ester or a solvate thereof. This invention also provides pharmaceutical compositions comprising such a salt or prepared using such a salt; processes and intermediates for preparing such a salt; and methods of using such a salt to treat a pulmonary disorder.Type: GrantFiled: February 11, 2005Date of Patent: January 22, 2008Assignee: Theravance, Inc.Inventors: Robert Chao, Miroslav Rapta, Pierre-Jean Colson, Junning Lee
-
Patent number: 7226936Abstract: New pyridinic sulfonamide derivatives represented by a general formula (I), wherein R1, represents a mono- or polyhalogenated C1–12-alkyl or a mono- or poly-halogenated C3–8-cycloalkyl group. The method of production of such derivatives and their use as active therapeutic substance in the treatment of diseases such as inflammation, arthrosis, cancer, angiogenesis and asthma are also reported.Type: GrantFiled: September 19, 2002Date of Patent: June 5, 2007Assignee: University De LiegeInventors: Jacques Delarge, Bernard Pirotte, Jean-Michel Dogne, Xavier de Leval, Fabien Julemont
-
Patent number: 7208507Abstract: The invention relates to pyridines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase ? (LPAAT-?) activity and/or proliferation of cells such as tumor cells.Type: GrantFiled: February 11, 2005Date of Patent: April 24, 2007Assignee: Cell Therapeutics, Inc.Inventors: Feng Hong, J Peter Klein
-
Patent number: 7205411Abstract: The invention relates to novel aminopyridine derivatives of formula (I) wherein R1 is methyl an R4 and amino group —NR6R7 and R5 forms an arylalkynyl- or heteroarylalkynyl-group.Type: GrantFiled: September 2, 2005Date of Patent: April 17, 2007Assignee: Addex Pharmaceuticals SAInventors: Christelle Bolea, Vincent Mutel, Jean-Philippe Rocher, Anne-Sophie Bessis, Emmanuel Le Poul
-
Patent number: 7202247Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.Type: GrantFiled: December 19, 2002Date of Patent: April 10, 2007Assignee: AtheroGenics, Inc.Inventors: James A. Sikorski, Charles Q. Meng, M. David Weingarten
-
Patent number: 7196198Abstract: An agent comprising the benzoic acid of formula (I) wherein A, B, R6, R7 are carbocyclic ring, heterocyclic ring, etc.; R1 is hydroxy etc.; R2, R3, R4 are alkyl etc.; R5, D, E are alkylene, etc.; G is oxygen etc., as active ingredient. The compound of formula (I) is considered to be useful for the treatment and/or prophylaxis of bone diseases, cancer, systemic granuloma, immunological diseases, allergy, atopy, asthma, gumboil, gingivitis, periodontitis, neurocyte death, Alzheimer's diseases, lungs injury, pulmopathy, acute hepatitis, nephritis, myocardial ischemia, Kawasaki disease, ambustion, ulcerative colitis, Crohn's disease, multiple organ failure, sleeping disorder, platelet aggregation, etc.Type: GrantFiled: December 18, 2003Date of Patent: March 27, 2007Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kousuke Tani, Kaoru Kobayashi, Takayuki Maruyama
-
Patent number: 7176312Abstract: General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.Type: GrantFiled: October 12, 2002Date of Patent: February 13, 2007Assignees: The Scripps Research Institute, IRM LLCInventors: Sheng Ding, Qiang Ding, Nathanael S. Gray
-
Patent number: 7153815Abstract: A insecticide characterized by containing as active ingredient a hydrazone derivative of formula (I) wherein A and Q are an aryl or a heterocyclic group, W is oxygen atom, an aminylene, an alkylene group, an oxyalkylene group or an alkyleneoxy, X1 and X2 are hydrogen atom, an alkyl, an alkenyl, an alkynyl, an aryl, a heterocyclic group, formyl, an acyl, an alkoxycarbonyl, an aryloxycarbonyl, a heterocyclic oxycarbonyl, an alkylsulfinyl, an arylsulfinyl, a heterocyclic sulfinyl, an alkylsulfonyl, an arylsulfonyl or a heterocyclic sulfonyl, Y is oxygen atom or sulfur atom, Z is hydrogen atom, a halogen atom, cyano, an alkyl, an alkenyl, an alkynyl, an amino, an alkoxy or an alkylthio, the substituents may be substituted; and novel hydrazon derivatives.Type: GrantFiled: January 10, 2003Date of Patent: December 26, 2006Assignee: Nihon Nohyaku Co., Ltd.Inventors: Shinji Kawata, Shuko Okui, Shigeru Suzuki, Toshiki Fukuchi, Akiyuki Suwa
-
Patent number: 7148229Abstract: The present invention is a sulfonamide substituted xanthine derivative of formula I: or a pharmaceutically acceptable salt thereof, wherein R1 is lower alkyl, lower alkyl substituted by phenyl, or lower alkyl substituted by halogen substituted phenyl; R2 is lower alkyl or lower alkyl substituted by lower cycloalkyl; and R3 is: Compounds of formula I and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.Type: GrantFiled: February 11, 2004Date of Patent: December 12, 2006Assignee: Hoffman-La Roche Inc.Inventors: Peter W. Dunten, Louise H. Foley, Nicholas J. S. Huby, Sherrie L. Pietranico-Cole, Weiya Yun
-
Patent number: 7145035Abstract: The present invention pertains to methods for preparing a compound of Formula (I), wherein A is O or N-L; each L is independently H or an acyl group; K is, together with the two contiguous linking carbon atoms, a phenyl ring, a 5- or 6-membered heteroaromatic ring or an aromatic 8-, 9- or 10-membered fused carbobicyclic or heterobicyclic ring system wherein each ring or ring system is optionally substituted; R1 is H, C1 to C4 alkyl or CO2R3; R2 is H or C1 to C4 alkyl; and R3 is C1 to C4 alkyl; comprising hydrogenating a compound of Formula (II), wherein n is 0, 1 or 2 in the presence of a catalyst comprising palladium to form the compound of Formula (I). This invention further pertains to methods for preparing compounds of Formula (II) useful for preparing compounds of Formula (I).Type: GrantFiled: March 14, 2002Date of Patent: December 5, 2006Assignee: E. I. du Pont de Nemours and CompanyInventors: Gary David Annis, Richard James Brown, Albert Loren Casalnuovo, Stephen Ernest Jacobson, Philip Osborne Moss
-
Patent number: 7144881Abstract: The present invention provides novel arylcyclopropylcarboxylic amides and related derivatives having the general Formula I wherein R, R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said arylcyclopropylcarboxylic amides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain and anxiety.Type: GrantFiled: November 21, 2003Date of Patent: December 5, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Yong-Jin Wu, Alexandre L'Heureux, Li-Qiang Sun
-
Patent number: 7138418Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: October 5, 2001Date of Patent: November 21, 2006Assignee: Amgen, Inc.Inventors: John Flygare, Julio C. Medina, Bei Shan, David L. Clark, Terry J. Rosen
-
Patent number: 7132425Abstract: The present invention provides a compound according to formula I where the substituent designations are provided in the specification. Pharmaceutical compositions comprising a compound according to formula I are also provided.Type: GrantFiled: December 10, 2003Date of Patent: November 7, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Shaoqing Chen, Wendy Lea Corbett, Kevin Richard Guertin, Nancy-Ellen Haynes, Robert Francis Kester, Francis A. Mennona, Steven Gregory Mischke, Yimin Qian, Ramakanth Sarabu, Nathan Robert Scott, Kshitij Chhabilbhai Thakkar
-
Patent number: 7132546Abstract: The present invention provides a cytokine production inhibitor containing as an active ingredient an aniline derivative of the formula (I) or a salt thereof: [wherein A is CO or SO2; Cy is an aryl group or a heterocyclic group; each of R1 and R2 which are independent of each other, is a halogen atom, a cyano group, a nitro group, an alkyl group which may be substituted, an alkenyl group which may be substituted, an alkynyl group which may be substituted, a cycloalkyl group which may be substituted, a cycloalkenyl group which may be substituted, an aryl group which may be substituted, a heterocyclic group which may be substituted, an amino group which may be substituted or a —B-Q group; R3 is a -M1-M2-R5 group; R4 is a hydrogen atom or an alkyl group which may be substituted; x is an integer of from 0 to 5; y is an integer of from 0 to 4; and z is an integer of from 0 to 1].Type: GrantFiled: December 21, 2001Date of Patent: November 7, 2006Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Fuminori Kato, Hirohiko Kimura, Shunji Yuki, Kazuhiro Yamamoto, Takashi Okada
-
Patent number: 7115746Abstract: The present invention relates to processes for the facile synthesis of diaryl amines and analogues thereof. The processes of the present invention produce diaryl amines in high yield and purity. The present invention also relates to intermediates useful in the process of the present invention.Type: GrantFiled: February 10, 2004Date of Patent: October 3, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: John R. Snoonian, Patricia Ann Oliver-Shaffer
-
Patent number: 7056909Abstract: The present invention relates to novel chain-fluorinated alkanoic acid derivatives thereof, their synthesis, and their use as ?v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors ?v?3 and/or ?v?5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.Type: GrantFiled: July 20, 2001Date of Patent: June 6, 2006Assignee: Merck & Co., Inc.Inventor: Jiabing Wang
-
Patent number: 7034044Abstract: The present invention relates to compounds of formulae The compounds of the present invention are NMDA (N-methyl-D-aspartate)-receptor subtype blockers and are used in the treatment of diseases related to this receptor.Type: GrantFiled: September 26, 2003Date of Patent: April 25, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Bernd Buettelmann, Marie-Paule Heitz Neidhart, Emmanuel Pinard, Rene Wyler
-
Patent number: 7030145Abstract: The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.Type: GrantFiled: March 12, 2004Date of Patent: April 18, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Richard A. Hartz, Argyrios G. Arvanitis
-
Patent number: 7026487Abstract: Compounds of the formula where the symbols are as defined in the specification, have retinoid agonist, antagonist or negative hormone-like biological activity.Type: GrantFiled: July 2, 2003Date of Patent: April 11, 2006Assignee: Allergan, Inc.Inventors: Richard L. Beard, Thong Vu, Diana F. Colon, Vidyasagar Vuligonda, Roshantha A. Chandraratna
-
Patent number: 7026476Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are and pharmaceutical compositions containing, intermediate compounds and processes of making such compounds.Type: GrantFiled: April 28, 2003Date of Patent: April 11, 2006Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier F. Cirillo, Steffen Breitfelder, Usha R. Patel, John R. Proudfoot, Alan D. Swinamer
-
Patent number: 7019019Abstract: The present invention provides matriptase inhibitors and compositions thereof useful for treating cancer. Martripase is a trypsin-like serine protease active in the development of cancerous conditions, such as tumors and metastasis of cancer.Type: GrantFiled: December 18, 2003Date of Patent: March 28, 2006Assignee: Dendreon CorporationInventors: David F. Duncan, L. Josue Alfaro-Lopez, Mallareddy Komandla, Odile Esther Levy, Ofir Moreno, Joseph E. Semple, Amir P. Tamiz
-
Patent number: 6984649Abstract: Pyridine 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 1.2.3.6-tetrahydro-pyridine, or —CR31R32R33 wherein R31 represents H or C1-6 alkyl and R32 and R33 are joined to form a 5-8 membered saturated ring optionally containing up to three heteroatoms; R4 is 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: March 28, 2003Date of Patent: January 10, 2006Assignee: Bayer AktiengesellschaftInventors: Toshiki Murata, Masaomi Umeda, Sachiko Sakakibara, Takashi Yoshino, Hiroki Sato, Tsutomu Masuda, Yuji Koriyama, Mitsuyuki Shimada, Takuya Shintani, Hiroshi Kadono, Timothy B. Lowinger, Karl B. Ziegelbauer, Kinji Fuchikami, Hiroshi Komura
-
Patent number: 6962994Abstract: An improved process for the preparation of cis-1,3-diols is described where a beta hydroxy ketone is treated with a trialkylborane or dialkylalkoxyborane or a mixture of a trialkylborane and a dialkylalkoxyborane followed by recovery and reuse of the alkylborane species to convert additional beta hydroxy ketone to the cis-1,3-diol.Type: GrantFiled: April 11, 2003Date of Patent: November 8, 2005Assignee: Warner-Lambert Company, LLCInventors: Robert Lee Bosch, Richard Joseph McCabe, Thomas Norman Nanninga, Robert Joseph Stahl
-
Patent number: 6962929Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, vascular restenosis, microbial infections, and psoriasis, or as lead compounds for the development of such agents.Type: GrantFiled: October 11, 2002Date of Patent: November 8, 2005Assignee: Tularik Inc.Inventors: John A. Flygare, Julio Cesar Medina, Bei Shan, David Louis Clark, Terry J. Rosen
-
Patent number: 6927290Abstract: There is disclosed an advantageous mixed acid anhydride production method of formula (1): R1C(O)OY(O)n(R2)p??(1) wherein R1, R2 and Y denote the same as defined below, n and p denote an integer of 1 or 2, which is characterized by adding a carboxylic acid of formula (2); R1COOH??(2) wherein R1 denotes a hydrogen atom, an optionally substituted alkyl group or the like, an organic base to a solution of a carboxylic acid activating agent of formula (3); (R2)pY(O)nX??(3) wherein R2 denotes an optionally substituted aliphatic hydrocarbyl group or the like, Y denotes a carbon atom, a phosphorus atom, or a sulfur atom, and X denotes a chlorine atom or the like.Type: GrantFiled: May 10, 2004Date of Patent: August 9, 2005Assignee: Sumitomo Chemical Company, LimitedInventors: Takashi Miki, Hideki Ushio, Isao Kurimoto
-
Patent number: 6911595Abstract: A charge transfer material comprising a basic compound having negative charge and represented by the following general formula (I): (A1-L)n1-A2·M??(I), wherein A1 represents a group having negative charge; A2 represents a basic group; M represents a cation for neutralizing the negative charge of (A1-L)n1-A2; L represents a divalent linking group or a single bond; and n1 represents an integer of 1 to 3. A photoelectric conversion device and a photo-electrochemical cell comprising the charge transfer material. A new nonvolatile pyridine compound, which is a low-viscosity liquid at room temperature, is preferably used for A2.Type: GrantFiled: June 14, 2002Date of Patent: June 28, 2005Assignee: Fuji Photo Film Co., Ltd.Inventors: Masaru Yoshikawa, Chang-yi Qian
-
Patent number: 6900232Abstract: The present invention relates to a class of compounds represented by the Formula I Wherein A1 is a pyridinyl of the formula optionally substituted by one or more Rk selected from the group consisting of hydroxy, alkyl, alkoxy, alkoxyalkyl, thioalkyl, haloalkyl, cyano, amino alkylamino, halogen, acylamino, sulfonamide and —COR; and R is hydroxy, alkoxy, alkyl or amino; and pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the ?v?3 and/or ?v?5 integrin.Type: GrantFiled: June 15, 2001Date of Patent: May 31, 2005Assignee: Pharmacia CorporationInventors: Ish Kumar Khanna, Michael Clare, Alan F. Gasiecki, Thomas Rogers, Barbara Chen, Mark Russell, Hwang-Fun Lu
-
Patent number: 6881736Abstract: Compounds of the formula (I) are disclosed which are vitronectin receptor antagonists and are useful in the treatment of osteoporosis: wherein R1 is Het or Ar R2 is or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 7, 2000Date of Patent: April 19, 2005Assignee: SmithKline Beecham CorporationInventors: Peter J. Manley, William H. Miller, Irene N. Uzinskas
-
Patent number: 6875781Abstract: The invention relates to pyridines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase ? (LPAAT-?) activity and/or proliferation of cells such as tumor cells.Type: GrantFiled: September 22, 2003Date of Patent: April 5, 2005Assignee: Cell Therapeutics, Inc.Inventors: Feng Hong, J. Peter Klein
-
Patent number: 6846833Abstract: Compounds of formula (1): wherein: G represents an optionally substituted phenyl or optionally substituted heterocycle, G1 and G2 being N or C, T1 represents —CH2—CH2—, —CH?CH— or ?CH—CH2—, and T2 is a bond, or T1 represents —CH2— or ?CH— and T2 is —CH2—, ?CH—, R5 represents —(CH2)m—COOR6, R6 and R6? represent hydrogen, alkyl, optionally substituted aryl or optionally substituted arylalkyl, A represents —CO—, —CH2—, ?CH— or —CH? and W represents —CH—, ?C— or —C?, or A represents —CO— or —CH2— and W represents N, X represents —CO—X1—, —CO—NR6—X1—, —NR6—CO—X1—, —O—X1—, —SO2—NR6—X1— or —S(O)n—X1—, Y represents —Y1—, —Y2—Y1— or —Y1—Y2—Y1—, Y1 being an alkylene, alkenylene or alkynylene, and Y2 being an arylene, heteroarylene, cycloalkylene or heterocycloalkylene, Z represents —Z1—, —Z10—NR6—, and —Z10—NR6—CO—, Z1 being a heteroaryl, heterocycloalkyl, heteroarylalkyl, heterocycloalkylalkyl, fused arylheteroaryl, fused arylheterocycloalkyl, fused heteroarylheterocycloalkyl, fused heterocycloalkylheteroarType: GrantFiled: March 6, 2001Date of Patent: January 25, 2005Assignee: Les Laboratories ServierInventors: Patrick Casara, Françoise Perron-Sierra, Ghanem Atassi, Gordon Tucker, Dominique Saint-Dizier