Nitrogen Attached Indirectly To The Six-membered Hetero Ring Through The Directly Attached Nitrogen By Nonionic Bonding Patents (Class 546/162)
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Publication number: 20100093711Abstract: The present invention provides a compound of formula I: said compound is inhibitor of aldosterone synthase, and/or 11beta-hydroxylase (CYP11B1), and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase and/or CYP11B1. Finally, the present invention also provides a pharmaceutical composition.Type: ApplicationFiled: December 14, 2007Publication date: April 15, 2010Inventors: Qi-Ying Hu, Gary Michael Ksander
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Patent number: 7687517Abstract: Novel 3,9-diazabicyclo[3.3.1]nonane derivatives of formula (I) useful as monoamine neurotransmitter re-uptake inhibitors are provided: These compounds can also be used in methods for therapy and be included in pharmaceutical compositions comprising the compounds.Type: GrantFiled: February 9, 2007Date of Patent: March 30, 2010Assignee: Neurosearch A/SInventors: Dan Peters, John Paul Redrobe, Elsebet Østergaard Nielsen
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Publication number: 20100048540Abstract: The invention relates to novel heterocyclic N-oxides which are useful as hypoxic selective cytotoxic agents that mediate and/or inhibit cell proliferation, for example, through the activity of protein kinases. The invention is further related to pharmaceutical compositions containing such compounds and compositions, and to methods of treating cancer as well as other disease states associated with unwanted ahgiogenesis and/or cellular proliferation by administering effective amounts of such compounds.Type: ApplicationFiled: February 1, 2006Publication date: February 25, 2010Applicant: SENTINEL ONCOLOGY LIMITEDInventors: Robert George Boyle, Stuart Travers
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Publication number: 20090312325Abstract: There are provided according to the invention novel compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R19, R20, and R34 are as described in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.Type: ApplicationFiled: May 29, 2009Publication date: December 17, 2009Inventors: Ian Robert Baldwin, Michael David Barker, Anthony William Dean, Colin David Eldred, Brian Evans, Sharon Lisa Gough, Stephen Barry Guntrip, Julie Nicole Hamblin, Stuart Holman, Paul Jones, Mika Kristian Lindvall, Christopher James Lunniss, Tracy Jane Redfern, Alison Judith Redgrave, John Edward Robinson, Michael Woodrow
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Patent number: 7632783Abstract: The invention provides compounds which exert excellent fungicidal activities against various plant diseases and are useful as active ingredients of pesticides permitting the control of rice blast and so on even in low dosages. Compounds represented by the general formulae (1a) to (1d) or salts thereof: (1a) (1b) (1c) (or) (1d) wherein R1 and R2 are each C1-6 alkyl or the like; R3 and R4 are each hydrogen, halogeno, or the like; R5 is hydrogen, C1-6 alkyl, or the like; X is halogeno, C1-6 alkyl, or the like; Y is halogeno, C1-6 alkyl, or the like; n is an integer of 0 to 4; and m is an integer of 0 to 6.Type: GrantFiled: January 21, 2005Date of Patent: December 15, 2009Assignee: Mitsui Chemicals Agro, Inc.Inventors: Hiroyuki Ito, Kota Fujiwara, Munetsugu Morimoto, Harukazu Tanaka, Yasushi Tamagawa, Hiroyuki Komai
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Publication number: 20090275612Abstract: Compounds with high antimalarial activity; and antimalarial drugs containing the same as an active ingredient. There are provided compounds with antimalarial activity represented by the chemical formula: (wherein R1 is H, Cl or OCH3; R2 is H or CH3; R3 is CH, CH2, C(CH3), CH(CH3) or C(CH3)2; Ar is imidazole, triazole, pyridine, benzene, pyrrole, furan, thiophene or derivatives thereof; n is 1 to 5; and m is 1 to 5). Further, there are provided antimalarial drugs containing these compounds with antimalarial activity or pharmacologically acceptable salts thereof as active ingredients.Type: ApplicationFiled: February 26, 2007Publication date: November 5, 2009Applicant: Nagoya City UniversityInventors: Tsunehiko Higuchi, Hirohisa Omiya, Naoki Umezawa, Hye-Sook Kim, Yusuke Wataya
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Patent number: 7601842Abstract: The present invention provides an industrially advantageous production method of optically active tetrahydroquinolines of formula (1), which comprises: 1) a step of reacting a ?-ketoester of formula (2) ?with an amine of formula (3) ?to produce an enaminoester of formula (4); 2) a step of subjecting the enaminoester of formula (4) above obtained in 1) to asymmetric hydrogenation to produce an optically active ?-amino acid derivative of formula (5); 3) a step of amidating the optically active ?-amino acid derivative (5) above obtained in 2) to produce an amide of formula (6); 4) a step of alkoxycarbonylating the amide of formula (6) above obtained in 3) to produce a compound of formula (7); ?and 5) a step of subjecting the compound of formula (7) above to cyclization to produce the optically active tetrahydroquinoline of formula (1).Type: GrantFiled: February 17, 2004Date of Patent: October 13, 2009Assignee: Takasago International CorporationInventors: Takashi Moroi, Tsukasa Sotoguchi, Kazuhiko Matsumura, Motonobu Takenaka, Wataru Kuriyama, Toshiyuki Murayama, Hideki Nara, Tohru Yokozawa, Kenji Yagi
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Patent number: 7572915Abstract: There are provided according to the invention novel compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R19, R20, and R34 are as described in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.Type: GrantFiled: February 8, 2006Date of Patent: August 11, 2009Assignee: Glaxo Group LimitedInventors: Michael David Barker, Anthony William Dean, Brian Evans, Stuart Holman, Michael Woodrow
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Patent number: 7566786Abstract: There are provided according to the invention novel compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R19, R20, and R34 are as described in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.Type: GrantFiled: May 19, 2004Date of Patent: July 28, 2009Assignee: Glaxo Group LimitedInventors: Ian Robert Baldwin, Michael David Barker, Anthony William Dean, Colin David Eldred, Brian Evans, Sharon Lisa Gough, Stephen Barry Guntrip, Julie Nicole Hamblin, Stuart Holman, Paul Jones, Mika Kristian Lindvall, Christopher James Lunniss, Tracy Jane Redfern, Alison Judith Redgrave, John Edward Robinson, Michael Woodrow
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Publication number: 20090186891Abstract: The present invention provides compounds of the following structure; A-Q-B—C-D that are useful for treating conditions or disorders associated with DGAT1 activity in animals, particularly humans.Type: ApplicationFiled: September 26, 2008Publication date: July 23, 2009Inventors: Young-Shin Kwak, Gary Mark Coppola
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Publication number: 20090163485Abstract: The present invention relates to compounds of formula wherein Ar, Het, R1 and n are as defined herein and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. Compounds of formula I are orexin receptor antagonists and are useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder and sleep disorders associated with neurological diseases.Type: ApplicationFiled: December 15, 2008Publication date: June 25, 2009Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
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Publication number: 20090143428Abstract: The invention provides a compound of formula (I) as defined in the specification, a process for its preparation, pharmaceutical compositions containing it, a process for preparing the pharmaceutical composition, and its use in therapy.Type: ApplicationFiled: November 26, 2008Publication date: June 4, 2009Inventors: Simon David Guile, Toby Thompson
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Publication number: 20090111852Abstract: A carboxamide compound represented by the formula (1): [wherein Q represents a nitrogen-containing 6-membered aromatic heterocyclic group optionally fused with a benzene ring, one of ring constitutional atoms of the heterocyclic group is a nitrogen atom and the heterocyclic group may be substituted with a group selected from the group consisting of a C1-C3 alkyl and the like, R1 represents a C1-C3 alkyl group or the like, R2 represents a hydrogen atom or the like, and R3 represents a hydrogen atom or the like] and a plant disease controlling agent comprising this as an active ingredient.Type: ApplicationFiled: July 12, 2006Publication date: April 30, 2009Applicant: Sumitomo Chemical Company, LimitedInventors: Shin-ichiro Souma, Yoshiharu Kinoshita
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Publication number: 20090105230Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.Type: ApplicationFiled: June 9, 2006Publication date: April 23, 2009Inventors: Daniel L. Flynn, Peter A. Petillo
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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
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Patent number: 7507828Abstract: One aspect of the invention relates to HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided. The invention also provides methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.Type: GrantFiled: May 11, 2004Date of Patent: March 24, 2009Assignee: Georgetown UniversityInventors: Alan P. Kozikowski, Bin Chen
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Patent number: 7488823Abstract: Cyanoguanidine quinazoline and cyanoamidine quinazolamine derivatives that are useful in the treatment of hyperproliferative diseases are disclosed. Methods of treating hyperproliferative diseases in mammals are also disclosed.Type: GrantFiled: November 10, 2003Date of Patent: February 10, 2009Assignee: Array Biopharma, Inc.Inventors: Eli Wallace, George Topolov, Qian Zhao, Joseph P. Lyssikatos
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Publication number: 20090023775Abstract: The invention relates to 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea as a crystalline, stoichiometrically defined and non-hygroscopic sulfate salt and a process for its preparation. Further, the present invention relates to the use of said 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea as a crystalline, stoichiometrically defined and non-hygroscopic sulfate salt alone or in combination with other compounds. Further, the present invention relates to formulations of said 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea as a crystalline, stoichiometrically defined and non-hygroscopic sulfate salt in the preparation of pharmaceutical compositions. The invention also relates to the use of such sulfate salts in formulations as neurohormonal antagonists.Type: ApplicationFiled: October 11, 2005Publication date: January 22, 2009Applicant: Actelion Pharmaceuticals Ltd.Inventors: Jean-Michel Bonard, Stephan Buchmann, Stephane Redey, Bertrand Woinet
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Publication number: 20080318957Abstract: Disclosed are compounds having polybasic functionalities. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effective against bacterial infections that have developed resistance to anti-bacterial agents through an efflux pump mechanism.Type: ApplicationFiled: May 6, 2008Publication date: December 25, 2008Applicant: Mpex Pharmaceuticals, Inc.Inventors: TOMASZ GLINKA, Olga Lomovskaya, Keith Bostian, David M. Wallace
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Publication number: 20080312273Abstract: The invention relates to compounds of formula (I) wherein: either any one of G1, G2, G3, G4 and G5 is nitrogen and the other four are —CH— or G1, G2, G3, G4 and G5 are all —CH—; Z is —O—, —NH—, —S—, —CH2— or direct bond; Z is linked to any one of G1, G2, G3, and G4; n is an integer from 0 to 5; m is an integer from 0 to 3; Ra represents hydrogen or fluoro; Rb, R1 and R2 are defined herein and salt thereof, process for the preparation so such compounds, pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient and the use of a compound of formula I in the manufacture of a medicament for the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals. The compounds of formula I and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of diseases states including cancer and rheumatoid arthritis.Type: ApplicationFiled: November 29, 2007Publication date: December 18, 2008Inventor: Laurent Francois Andre Hennequin
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Publication number: 20080312276Abstract: The invention is directed to 4,5-dihydro-(1H)-pyrazole (pyrazoline) derivatives as cannabinoid CB1 receptor modulators, to pharmaceutical compositions comprising these compounds, to methods for their syntheses, to methods for preparing novel intermediates useful for their syntheses, and to methods for preparing compositions. The invention also relates to the uses of compounds and compositions administered to patients to achieve a therapeutic effect in multiple sclerosis, traumatic brain injury, pain including chronic pain, neuropathic pain, acute pain and inflammatory pain, osteoporosis, appetite disorders, epilepsy, Alzheimer's disease, Tourette's syndrome, cerebral ischaemia, emesis, nausea, and gastrointestinal disorders. Compounds of the present disclosure are directed to formula (I): wherein the substituents have the definitions given in the specification.Type: ApplicationFiled: June 11, 2008Publication date: December 18, 2008Inventors: Josephus H.M. Lange, Hendrik C. Wals, Bernard J. Vliet Van, Mahmut Yildirim
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Publication number: 20080312275Abstract: Novel pyridyl cyanoguanidine compounds of general formula I (I) wherein R1, X, R2 and R3 are as defined herein, exhibit a high antiproliferative activity and may be used in the treatment of hyperproliferative and neo-plastic diseases.Type: ApplicationFiled: December 20, 2005Publication date: December 18, 2008Applicant: LEO Pharma A/SInventors: Fredrik Bjørkling, Heinz Wilhelm Dannacher
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Patent number: 7456196Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).Type: GrantFiled: May 5, 2006Date of Patent: November 25, 2008Assignee: Abbott LaboratoriesInventors: Robert J. Altenbach, Marlon D. Cowart, Huaqing Liu
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Publication number: 20080275057Abstract: Novel substituted azole diones are provided that kill cells, suppress cell proliferation, suppress cell growth, abrogate the cell cycle G2 checkpoint and/or cause adaptation to G2 cell cycle arrest. Methods of making and using the invention compounds are provided. The invention provides substituted azole diones to treat cell proliferation disorders. The invention includes the use of substituted azole diones to selectively kill or suppress cancer cells without additional anti-cancer treatment. The invention includes the use of cell cycle G2-checkpoint-abrogating substituted azole diones to selectively sensitize cancer cells to DNA damaging reagents, treatments and/or other types of anti-cancer reagents.Type: ApplicationFiled: April 11, 2008Publication date: November 6, 2008Applicant: CanBas Co., Ltd.Inventors: Takumi Kawabe, Machiyo Ishigaki, Takuji Sato, Sayaka Yamamoto, Yoko Hasegawa
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Publication number: 20080269284Abstract: Compounds of Formula I wherein n, q, Y, R1, R2a, R2b, R3a, R3b, R4, R5, and R6 are as defined herein and their pharmaceutical compositions and methods of use are disclosed.Type: ApplicationFiled: June 22, 2005Publication date: October 30, 2008Applicant: ELI LILLY AND COMPANYInventors: Ana Maria Escribano, Maria Carmen Fernandez, Nathan Bryan Mantlo, Ana Isabel Mateo-Herranz, Eva Maria Martin De La Nava, Xiaodong Wang
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Publication number: 20080262035Abstract: The present invention relates to carboxylic acid derivatives that are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.Type: ApplicationFiled: July 11, 2005Publication date: October 23, 2008Inventors: Prasun K. Chakravarty, Steven L. Colletti, Raffaele Ingenito, Peter T. Meinke, Alessia Petrocchi, Christian Steinkuhler
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Publication number: 20080249130Abstract: Compounds represented by formula (I): are inhibitors of gut microsomal triglyceride transfer protein. Such compounds are useful in treating diseases or conditions such as diabetes and obesity, along with patients are risk for developing such diseases or conditions.Type: ApplicationFiled: February 8, 2008Publication date: October 9, 2008Applicant: Sirtris Pharmaceuticals, Inc.Inventor: Chi B. Vu
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Publication number: 20080234318Abstract: The present invention provides compounds that demonstrate protective effects on target cells from HIV infection in a manner as to bind to chemokine receptor, and which affect the binding of the natural ligand or chemokine to a receptor such as CXCR4 of a target cell.Type: ApplicationFiled: August 30, 2006Publication date: September 25, 2008Inventors: Kristjan Gudmundsson, Sharon Davis Boggs
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Publication number: 20080227812Abstract: The present invention relates to spiro (tetracarbon) substituted compound of Formula I, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states associated with angiogenesis, such as cancers associated with protein tyrosine kinases, to their use as medicaments for use in the production of inhibition of tyrosine kinases reducing effects in warm-blooded animals such as humans.Type: ApplicationFiled: February 23, 2008Publication date: September 18, 2008Inventor: Guoqing Paul Chen
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Publication number: 20080199875Abstract: Embodiments of the present invention provide methods and nucleic acid reporter molecules for the detection of nucleic acid in a sample. The nucleic acid reporter molecule comprises two unsymmetrical cyanine monomer moieties, which may be the same or different, that are covalently attached by a linker comprising at least one aromatic, heteroaromatic, cyclic or heterocyclic moiety comprising 3-20 non-hydrogen atoms selected from the group consisting of O, N, S, P and C. The linker may be rigid, relatively flexible or some degree thereof. The unsymmetrical cyanine monomer moieties comprise a substituted or unsubstituted benzazolium moiety and a substituted or unsubstituted pyridinium or quinolinium moiety that is connected by a methine bridge that is monomethine, trimethine or pentamethine. The linkers form the cyanine dimer compounds by attaching to the pyridinium or quinolinium moiety of the monomer moieties.Type: ApplicationFiled: April 7, 2008Publication date: August 21, 2008Applicant: INVITROGEN CORPORATIONInventors: Stephen Yue, Ching-Ying Cheung
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Publication number: 20080132507Abstract: A compound represented by the following general formula (1) or a salt thereof or a hydrate of the foregoing is safe while exhibiting suitable physicochemical stability, and is useful as therapeutic or prophylactic agents for diseases associated with thrombus formation. wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc., R2 represents optionally substituted phenyl, etc., R3 represents optionally substituted C6-10 aryl, etc., Z1, Z2 and Z3 each independently represent hydrogen, etc., Z4 represents hydrogen, etc. and X represents a single bond or —CO—, etc.Type: ApplicationFiled: October 13, 2005Publication date: June 5, 2008Applicant: Eisai R&D Management Co., Ltd.Inventors: Richard Clark, Shinsuke Hirota, Hiroshi Azuma, Kazunobu Kira, Nobuhisa Watanabe, Tadashi Nagakura, Tatsuo Horizoe
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Publication number: 20080125463Abstract: The present invention relates to (het)aryl-3-[(het)arylpiperidin-4-yl]amides, to processes for their preparation and to their use for producing pharmaceutical compositions for treatment of disorders and indications connected to the EP2 receptor.Type: ApplicationFiled: September 6, 2007Publication date: May 29, 2008Inventors: Nico Braeuer, Bernd Buchmann, Marcus Koppitz, Antonius Ter Laak, Gernot Langer, Bernhard Lindenthal, Olaf Peters, Tim Wintermantel
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Publication number: 20080119516Abstract: It was an object of the present invention to provide novel compounds that are suitable in particular as active substances in medicaments, preferably in medicaments for the regulation of neuropeptide Y receptors, particularly preferably of neuropeptide Y5 (NPY5) receptor, for the regulation of food ingestion (food intake), preferably for the prophylaxis and/or treatment of disorders of food ingestion, such as obesity, anorexia, cachexia, bulimia or type II (non insulin dependent) diabetes, for the prophylaxis and/or treatment of disorders of the peripheral nervous system, disorders of the central nervous system, anxiety, depression, cognitive disorders, preferably memory disorders, cardiovascular diseases, pain, epilepsy, arthritis, hypertensive syndrom, inflammatory diseases, immune diseases and other NPY5 mediated disorders in animals and mammals, including man. Said object was achieved by providing 1,4-disubstituted piperidine compounds of general formula (I) wherein the substituents are defined in claim 1.Type: ApplicationFiled: July 29, 2004Publication date: May 22, 2008Applicant: LABORATORIOS DEL DR. ESTEVE S.A.Inventors: Antoni Torrens Jover, Josep Mas Prio, Alberto Dordal Zueras, Maria Angeles Fisas Escasany
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Patent number: 7368573Abstract: This invention relates to MTP/Apo-B secretion inhibitors of Formula (I) wherein R1-R7, X1, m and n are as defined in the specification, as well as pharmaceutical compositions comprising the compounds, and methods of use of the compounds and compositions. The compounds of the invention are useful in treating obesity and associated diseases, conditions or disorders.Type: GrantFiled: June 15, 2006Date of Patent: May 6, 2008Assignee: Pfizer Inc.Inventors: Peter Bertinato, Michel A. Couturier, Ernest S. Hamanaka, Marcus D. Ewing, Ralph P. Robinson, Derek L. Tickner
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Patent number: 7365081Abstract: The invention relates to novel indole derivatives of the general formula 1, to their preparation and to their use as medicaments, in particular for treating tumorsType: GrantFiled: July 20, 2001Date of Patent: April 29, 2008Assignee: AEterna Zentaris GmbHInventors: Peter Emig, Gerald Bacher, Dietmar Reichert, Silke Basner, Beate Aue, Bernd Nickel, Eckhard Günther
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Patent number: 7332504Abstract: Heterocyclic substituted aminoazacyclic compounds of formula I Z-R3I, 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: September 22, 2004Date of Patent: February 19, 2008Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Kevin B. Sippy, Jerome F. Daanen, Keith Brian Ryther, Jianguo Ji
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Patent number: 7314939Abstract: The present invention provides compounds of the formula: and pharmaceutically acceptable isomers, salts, hydrates, solvates, and prodrug derivatives thereof, wherein R1, R6, R7, R8, Pg, and n are those defined herein. The present invention also provides pharmaceutical compositions comprising the same and methods for using the same. In particular, compounds of Formula I are useful in modulating TGF-? activity.Type: GrantFiled: June 15, 2004Date of Patent: January 1, 2008Assignee: Millennium Pharmaceuticals, Inc.Inventors: Anjali Pandey, Robert M. Scarborough, Meenakshi S. Venkatraman
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Patent number: 7312230Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: wherein: R1, R2, and R3 are each independently in each occurrence aryl or heteroaryl; R4 is —COOH or tetrazolyl; A, B, m, n, and r are 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 processes for their preparation.Type: GrantFiled: September 30, 2005Date of Patent: December 25, 2007Assignee: Roche Palo Alto LLCInventors: Richard Leo Cournoyer, Paul Francis Keitz, Lee Edwin Lowrie, Jr., Alexander Victor Muehldorf, Counde O'Yang, Dennis Mitsugu Yasuda
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Patent number: 7183414Abstract: The present invention relates to a process for preparing a compound of the formula I or a pharmaceutically acceptable salt, prodrug, hydrate or solvate thereof, wherein R1, R2, R3 and R4 are as defined herein. The compound of formula I is useful in the treatment of abnormal cell growth, such as cancer, in mammals.Type: GrantFiled: June 23, 2004Date of Patent: February 27, 2007Assignee: Pfizer IncInventors: Norma J. Tom, Michael J. Castaldi, David B. Ripin
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Patent number: 7183413Abstract: 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: GrantFiled: April 6, 2004Date of Patent: February 27, 2007Assignee: Taigen BiotechnologyInventors: Chu-Chung Lin, Jen-Fuh Liu, Chih-Wei Chang, Shu-Jen Chen, Yibin Xiang, Pei-Chin Cheng, Jiing-Jyh Jan
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Patent number: 7151110Abstract: Novel pyrazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-? signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer, and fibrotic diseases.Type: GrantFiled: September 23, 2005Date of Patent: December 19, 2006Assignees: Pfizer Inc., Pfizer Products Inc.Inventors: Michael J. Munchhof, Laura C. Blumberg
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Patent number: 7084156Abstract: The present invention is concerned with compounds of the general Formula I: and pharmaceutically acceptable salts thereof, which are useful as melanin concentrating hormone receptor antagonists, particularly MCH-1R antagonists. As such, compounds of the present invention are useful for the treatment or prevention of obesity or eating disorders associated with excessive food intake and complications thereof, osteoarthritis, certain cancers, AIDS wasting, cachexia, frailty (particularly in elderly), mental disorders stress, cognitive disorders, sexual function, reproductive function, kidney function, locomotor disorders, attention deficit disorder (ADD), substance abuse disorders and dyskinesias, Huntington's disease, epilepsy, memory function, and spinal muscular atrophy. Compounds of formula I may therefore be used in the treatment of these conditions, and in the manufacture of a medicament useful in treating these conditions.Type: GrantFiled: November 22, 2002Date of Patent: August 1, 2006Assignee: Merck & Co., Inc.Inventors: Robert J. DeVita, Lehua Chang, Danny Chaung, MyLe Hoang, JinLong Jiang, Peter Lin, Andreas W. Sailer, Jonathan R. Young
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Patent number: 7060834Abstract: Compounds useful for the treatment of pain in accord with the following structural diagram, wherein A, R1, b, R4, R5, R6, R7 and R8 are any of a number of groups as defined in the specification, and pharmaceutical compositions and methods of treatment utilizing such compounds.Type: GrantFiled: August 23, 2002Date of Patent: June 13, 2006Assignee: AstraZeneca ABInventor: Derin D'Amico
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Patent number: 6995175Abstract: The present invention relates to cancer therapy and to novel anticancer agents having a mechanism of action which is quite specific. It also relates to novel chemical compounds as well as their therapeutic application in humans.Type: GrantFiled: November 25, 2003Date of Patent: February 7, 2006Assignee: Aventis Pharma S.A.Inventors: Hervé Bouchard, Augustin Hittinger
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Patent number: 6989392Abstract: The present invention is related to compounds of formula (I), or a therapeutically suitable salt or prodrug thereof, which antagonize the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor and are useful for the prevention or treatment of eating disorders, weight gain and obesity.Type: GrantFiled: June 12, 2003Date of Patent: January 24, 2006Assignee: Abbott LaboratoriesInventors: Christine A. Collins, Ju Gao, Philip R. Kym, Jared C. Lewis, Andrew J. Souers, Anil Vasudevan, Dariusz Wodka
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Patent number: 6962930Abstract: Compounds, composition and method for ameliorating alcohol or drug dependency withdrawal syndromes and withdrawal-induced brain damage are disclosed. In particular, a series of N-substituted-4-uredo-5,7-dihalo-2-carboxy quinoline compounds are disclosed having combined properties as antagonists of voltage-sensitive sodium channels (VSNaC) and as selective competitive antagonists at the strychnine-intensive glycine site of N-methyl-D-aspartate (NMDA) receptors. The disclosed compounds prevent or reduce the signs and symptoms of neurohyperexcitability and particularly the neurohyperexcitability associated with withdrawal syndrome manifested by patients upon withdrawal from chronic use of dependence inducing agents (e.g. ethanol, barbiturates, opiates etc.).Type: GrantFiled: June 5, 1998Date of Patent: November 8, 2005Assignee: Lohocla Research CorporationInventors: Boris Tabakoff, Lawrence Snell, Paula L. Hoffman
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Patent number: 6946473Abstract: Compounds of the formula which are useful in disease conditions mediated by TNF-?, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.Type: GrantFiled: March 17, 2003Date of Patent: September 20, 2005Assignee: Wyeth Holdings CorporationInventors: Jeremy I. Levin, James M. Chen, Xue-Mei Du, Jay D. Albright, Arie Zask
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Patent number: 6930185Abstract: A melanin-concentrating hormone antagonist comprising a compound of the formula (I): wherein Ar1 is a cyclic group which may be substituted; X and Y are the same or different and are a spacer having a main chain of 1 to 6 atoms; Ar is a condensed polycyclic aromatic ring which may be substituted; R1 and R2 are the same or different and are hydrogen atom or a hydrocarbon group which may be substituted; or R1 and R2, together with the adjacent nitrogen atom, may form a nitrogen-containing heterocyclic ring which may be substituted; or R2, together with the adjacent nitrogen atom and Y, may form a nitrogen-containing heterocyclic ring which may be substituted; or R2, together with the adjacent nitrogen atom, Y and Ar, may form a condensed ring; or a salt thereof is useful as an agent for preventing or treating obesity, etc.Type: GrantFiled: April 26, 2001Date of Patent: August 16, 2005Assignee: Takeda Chemical Industries, Ltd.Inventors: Yuji Ishihara, Nobuhiro Suzuki, Shiro Takekawa
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Patent number: 6903094Abstract: The present invention relates to a compound of the formula [1?] ? wherein R2 is lower alkyl optionally substituted by hydroxy, amino and the like, ring B is phenyl, thienyl and the like, E is a single bond, —O—, —S— and the like, ring G is aryl, heterocyclic group and the like, R5 is halogen atom, hydroxy, lower alkyl optionally substituted by halogen atom etc., and the like, t is 0 or an integer of 1 to 5, when t is an integer of 2 to 5, each R5 may be the same or different, m is 0 or an integer of 1 to 8, and n is 0 or an integer of 1 to 4, and a nociceptin antagonist containing compound [1?] as an active ingredient. The compound [1?] shows, due to nociceptin antagonistic action, analgesic effect against sharp pain such as postoperative pain and the like. The present invention also relates to the use of certain amide derivative inclusive of compound [1?] as a nociceptin antagonist or analgesic.Type: GrantFiled: May 10, 2002Date of Patent: June 7, 2005Assignee: Japan Tabacco, Inc.Inventors: Hisashi Shinkai, Takao Ito, Hideki Yamada
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Patent number: RE40278Abstract: Tricyclic nitrogen containing compounds, having anxiolytic and anti-depressant activity and central nervous system activity of the following structural formula: and pharmaceutically acceptable salts thereof wherein R1 and R2 are independently hydrogen, C1-6 alkyl or R1 and R2 are joined to form pyrrolidiae, piperidine, morpholine or imidazole. X is OCH3, SO2R3, SO2CF3 or CN where R3 is C1-6 alkyl or an Aryl; and Y is hydrogen, Cl, Br, F, CN, CONR1R2, CF3, OCH3, SO2NR1R2. These new compounds are suitable for treating anxiolytic disorder, schizophrenia, Parkinson's disease, anxiety, depression or as compounds for lowering blood pressure or treating migraine headaches in patients in need of such treatment.Type: GrantFiled: June 17, 1994Date of Patent: April 29, 2008Assignee: Pharmacia & Upjohn CompanyInventor: Arthur G. Romero