The Other Cyclo In The Bicyclo Ring System Is Also Six-membered (e.g., Naphthyridines, Etc.) Patents (Class 546/122)
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Publication number: 20130005760Abstract: A heterocyclic compound of formula (I) or a salt thereof: wherein R1 is an optionally protected amino group or an optionally substituted C1-6 alkyl group; R2 and R3 are each independently a C1-2 alkyl group; X is a hydrogen atom or a halogen atom; Z1 is N or C—R4; Z2 is N or C—R5; Z3 is N or C—R6; Z4 is N or C—R7; R4, R5, R6, and R7 are each independently a hydrogen atom, a halogen atom, an optionally protected amino group, or a C1-6 alkylsulfonyl group; Z is CH or N; and A is a methylene group or a bond, which has an excellent anti-HIV activity and is useful as an anti-HIV agent.Type: ApplicationFiled: January 20, 2011Publication date: January 3, 2013Applicant: Toyama Chemical Co., Ltd.Inventors: Yuji Oonishi, Kenichiro Awasaguchi, Nobuhiko Nomura, Keisuke Tohdo, Hyouei Kawai, Tomomi Wakatsuki
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Publication number: 20130005724Abstract: The present invention relates to derivatives of pyridino-pyridinones, and to their preparation and use thereof, having activity as inhibitors of kinase activity of receptors for PDGF (platelet derived growth factors) ligands and optionally of receptors for the FLT3 (fms-like tyrosine kinase receptor) ligand receptors, said derivatives comprising compounds of formula (I): wherein the various substituent groups are more specifically defined herein. The compounds are suitable as therapeutics for the treatment of various proliferative diseases.Type: ApplicationFiled: May 22, 2012Publication date: January 3, 2013Applicant: SANOFIInventors: Gilbert LASSALLE, Valérie MARTIN, Gary MCCORT, Cécile VOLLE-CHALLIER
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Patent number: 8343996Abstract: The present invention provides compounds and methods for treating or preventing the development of a disease, disorder, or condition in a subject or patient.Type: GrantFiled: November 13, 2009Date of Patent: January 1, 2013Assignee: AstraZeneca ABInventor: Mark E. Duggan
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Patent number: 8338605Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-formulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.Type: GrantFiled: June 17, 2010Date of Patent: December 25, 2012Assignee: Abbott LaboratoriesInventors: Todd W. Rockway, David A. Betebenner, Allan C. Krueger, Nobuhiko Iwasaki, Curt S. Cooper, David D. Anderson, Dale J. Kempf, Darold L. Madigan, Christopher E. Motter, Jason P. Shanley, Michael D. Tufano, Rolf Wagner, Rong Zhang, Akteruzzaman Molla, Hongmei Mo, Tami J. Pilot-Matias, Sherie V. L. Masse, Robert J. Carrick, Wenping He, Liangjun Lu
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Publication number: 20120322785Abstract: The invention provides novel compounds having the general formula: wherein X1 is N or N+O?, and one of X2, X3 and X4 is N or N+—O? and the remainder of X2, X3 and X4 is C. R2, R3, R4, R5, R6. A, B and Y are as described herein. Additionally compositions compounds of Formula I and methods of use are further described herein.Type: ApplicationFiled: December 14, 2011Publication date: December 20, 2012Applicant: Genentech, Inc.Inventors: Joseph P. Lyssikatos, Lewis J. Gazzard, Emily Hanan, Samuel Kintz, Hans Edward Purkey
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Patent number: 8334294Abstract: New inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) are disclosed herein, as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy.Type: GrantFiled: April 25, 2008Date of Patent: December 18, 2012Assignee: Almirall, S.A.Inventors: Wenceslao Lumeras Amador, Paul Robert Eastwood
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Publication number: 20120316166Abstract: Novel hetarylaminonaphthyridine derivatives of formula (I) wherein X, R1, R2, R3, R4, W1, W2, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.Type: ApplicationFiled: January 10, 2011Publication date: December 13, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Alfred Jonczyk, Dieter Dorsch, Frank Zenke, Christiane Amendt
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Publication number: 20120302576Abstract: The present invention relates to compounds and pharmaceutically acceptable salts, esters and prodrugs of Formula (I) or (II): which are useful as AMPK modulators effective in treating diabetes, obesity and cancer in a subject.Type: ApplicationFiled: August 9, 2012Publication date: November 29, 2012Inventors: Neal C. Birnberg, Hong Liu, Qing Ping Weng, Haibo Shang, Pan Yin, Sharanappa B. Rajur, Hwa-Ok Kim, Paresh D. Salgaonkar, Norton P. Peet
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Publication number: 20120295902Abstract: Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) wherein R1, R2, W1, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.Type: ApplicationFiled: December 17, 2010Publication date: November 22, 2012Applicant: MERCK PATENT GMBHInventors: Alfred Jonczyk, Dieter Dorsch, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
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Publication number: 20120289702Abstract: Provided is an agricultural fungicide that contains at least one selected from the group consisting of a novel nitrogen-containing heterocyclic compound represented by Formula (I), a salt thereof, or an N-oxide compound thereof. In Formula (I), R represents a group represented by CR1R2R3 or a cyano group. R1 to R3 each independently represents a hydrogen atom, an unsubstituted or substituted C1-8 alkyl group, an unsubstituted or substituted hydroxyl group, or the like. R4 or R5 represents a halogeno group or the like. Y or Z represents a carbon atom or the like, and A or D represents a benzene ring or the like. X represents an oxygen atom or a nitrogen atom or the like.Type: ApplicationFiled: December 28, 2010Publication date: November 15, 2012Applicant: Nippon Soda Co., Ltd.Inventors: Kotaro Shibayama, Jun Inagaki, Yuto Saiki, Akira Mitani, Raito Kuwahara, Motoaki Sato, Satoshi Nishimura, Mami Kuboki
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Patent number: 8309734Abstract: This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula wherein A1, A2, B1, B2 and R1 to R11 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.Type: GrantFiled: October 19, 2009Date of Patent: November 13, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Henrietta Dehmlow, Rainer E. Martin, Ulrike Obst Sander, Hans Richter, Christoph Ullmer
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Publication number: 20120258957Abstract: The present invention relates to a heterocyclic derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders or diseases influenced by modulation of orexins, such as sleep disorders.Type: ApplicationFiled: November 22, 2010Publication date: October 11, 2012Inventors: Matilda Jane Bingham, Andrew Dunbar, Margaret Jean Laats, Grant Wishart
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Publication number: 20120258947Abstract: Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: ApplicationFiled: April 18, 2012Publication date: October 11, 2012Applicant: Grunenthal GmbHInventors: Sven KÜHNERT, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder, Simon Lucas
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Publication number: 20120252806Abstract: The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: December 9, 2010Publication date: October 4, 2012Inventors: Michael J. Kelly, III, Mark E. Layton
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Publication number: 20120252814Abstract: Compounds of the following formula are provided for use with glucokinase: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: March 21, 2012Publication date: October 4, 2012Applicant: TAKEDA CALIFORNIA, INC.Inventors: Zacharia Cheruvallath, Jun Feng, Prasuna Guntupalli, Stephen L. Gwaltney, Joanne Miura, Mark Sabat, Mingnam Tang, Haxia Wang
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Publication number: 20120252809Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: January 24, 2012Publication date: October 4, 2012Applicant: SANOFIInventors: Sven RUF, Thorsten SADOWSKI, Klaus WIRTH, Herman SCHREUDER, Christian BUNING
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Publication number: 20120252780Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: October 29, 2010Publication date: October 4, 2012Inventors: Pui Yee Ng, Charles Blum, Lauren McPherson, Robert B. Perni, Chi B. Vu, Mohammed Mahmood Ahmed, Jeremy S. Disch
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Patent number: 8278452Abstract: The invention provides a novel class of compounds of Formula I: (I) pharmaceutical compositions comprising such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFR? and PDGFR? kinases.Type: GrantFiled: February 20, 2009Date of Patent: October 2, 2012Assignee: IRM LLCInventors: Donatella Chianelli, Xiaolin Li, Xiaodong Liu, Jon Loren, Valentina Molteni, Juliet Nabakka, Vince Yeh
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Patent number: 8278337Abstract: Disclosed are compounds of the formula (I) wherein X is N or CH, and Y is N or CR5. Also disclosed are methods of treating JNK and ERK mediated diseases using the compounds of formula 1.0.Type: GrantFiled: December 17, 2007Date of Patent: October 2, 2012Assignee: Merck Sharp & DohmeInventors: David B. Belanger, M. Arshad Siddiqui, Patrick J. Curran, Blake Hamann, Lianyun Zhao, Panduranga Adulla P. Reddy, Praveen K. Tadikonda, Gerald W. Shipps, Jr., Umar Faruk Mansoor
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Publication number: 20120245152Abstract: A compound of the general formula (I): [wherein, R1 represents a halogen atom, or the like, R2 represents a hydrogen atom, or the like, R3 and R4, each independently, represent a hydrogen atom, a C1-4 alkyl group, or the like, R5 represents a hydrogen atom, a halogen atom, or the like, R6 represents a hydrogen atom, a halogen atom, or the like, R7 and R8, each independently, represent a hydrogen atom, a halogen atom, or the like, R9 and R10, each independently, represent a hydrogen atom, a C1-4 alkyl group, R11 and R12, each independently, represent a hydrogen atom, a C1-4 alkyl group, or the like, X represents an oxygen atom, a group —CH2—, or the like, Y represents a nitrogen atom, a group ?CH—, or the like, and Z represents a nitrogen atom, or the like] or a pharmacologically acceptable salt thereof, which has an excellent suppressive action on platelet aggregation, and is useful for prevention and/or treatment of thromboembolism.Type: ApplicationFiled: August 27, 2010Publication date: September 27, 2012Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Tatsuya Nishi, Masashi Hasegawa, Yumi Shinagawa-ku, Yuichi Ochiai, Ryoko Kitazawa, Hiroshi Susaki
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Patent number: 8268803Abstract: The present invention relates to 5,6-ring annulated indole derivatives of the formula (I), compositions comprising at least one 5,6-ring annulated indole derivatives, and methods of using the 5,6-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: GrantFiled: December 17, 2007Date of Patent: September 18, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Frank Bennett, Srikanth Venkatraman, F. George Njoroge, Kevin X. Chen, Neng-Yang Shih, Stuart B. Rosenblum, Joseph A. Kozlowski
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Publication number: 20120232052Abstract: The present invention relates to aryl carboxamide derivatives of formula (I), wherein Ar1 is phenyl; Ar2 is aryl; n is 1-4; X is —O—, —S—, —SO— or —SO2—, a prodrug thereof or a pharmaceutically acceptable salt thereof, which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of such disorders and diseases as pain in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases as pain in which voltage gated sodium channels are involved.Type: ApplicationFiled: November 16, 2010Publication date: September 13, 2012Inventors: Tatsuya Yamagishi, Yoshimasa Arano, Mikio Morita, Tadashi Inoue
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Publication number: 20120226035Abstract: Disclosed is a compound represented by the general formula: wherein R1 represents an aryl or heterocyclic group which may be substituted or the like; X1 represents a C2-C4 alkylene group or the like; X2, X3 and X5 independently represent NH, a bond or the like; X4 represents a lower alkylene group, a bond or the like; Y1 represents a bivalent alicyclic hydrocarbon residue which may be substituted or a bivalent alicyclic amine residue which may be substituted; and Z1, Z2, Z3, Z4, Z5 and Z6 independently represent a nitrogen atom, a group represented by the formula: CH, or the like, provided that at least one of Z3, Z4, Z5 and Z6 represents a nitrogen atom, or a salt thereof, which is useful as an antibacterial agent.Type: ApplicationFiled: May 10, 2012Publication date: September 6, 2012Applicants: Taisho Pharmaceutical Co., Ltd., Toyama Chemical Co., Ltd.Inventors: Taro KIYOTO, Junichi Ando, Tadashi Tanaka, Yasuhiro Tsutsui, Mai Yokotani, Toshiya Noguchi, Fumihito Ushiyama, Hiroki Urabe, Hiromasa Horikiri
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Patent number: 8258301Abstract: Compounds of the formula (I) wherein R1, R2, R3, R4, R5, R6, W, and Y are as described herein, or a tautomer, prodrug, solvate, or salt thereof. These compounds are useful as inhibitors of Urotensin II and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the interaction of Urotensin II with its receptor, including cardiovascular diseases. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds, and intermediates useful in these processes.Type: GrantFiled: May 12, 2008Date of Patent: September 4, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Brian Nicholas Cook, Anne Bettina Eldrup, Ingo Andreas Mugge, Fariba Soleymanzadeh, Sanxing Sun, Yunlong Zhang
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Publication number: 20120220587Abstract: Compounds of the formula (I), in which X1, X2, L, Y, R2, R3, R4, R5, R6, R7, R8, R9, R10 have the meanings indicated in claim 1, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumours.Type: ApplicationFiled: September 6, 2010Publication date: August 30, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Ulrich Emde, Hans Peter Buchstaller, Markus Klein, Christina Esdar, Joerg Bomke
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Publication number: 20120214990Abstract: A nitrogen-containing heterocyclic compound or pharmaceutically acceptable salt thereof represented by the general formula: which have a potent antibacterial activity and a high safety. Thus, the compounds are useful as antibacterial agents against gram-positive bacteria, gram-negative bacteria and drug resistant bacteria.Type: ApplicationFiled: May 3, 2012Publication date: August 23, 2012Applicants: TAISHO PHARMACEUTICAL CO., LTD., TOYAMA CHEMICAL CO., LTD.Inventors: Taro KIYOTO, Tadashi Tanaka, Yasuhiro Tsutsui, Junichi Ando, Mai Motono, Yasuko Kawaguchi, Toshiya Noguchi, Yasunobu Ushiki, Fumihito Ushiyama, Hiroki Urabe
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Publication number: 20120208840Abstract: The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity, wherein these compounds selected from the group consisting of wherein A, B, C, D, X, Y, Z and R3 are defined in the specification. Said compounds are useful for treating a disease or condition of a mammal selected from the group consisting of ocular diseases; systemic vascular barrier related diseases; allergies and other inflammatory diseases; cardiac diseases or conditions; fibrosis; pain and wounds.Type: ApplicationFiled: September 28, 2010Publication date: August 16, 2012Applicant: ALLERGAN, INC.Inventors: Wenkiu K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha-Bin Im
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Publication number: 20120208820Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: ApplicationFiled: January 31, 2012Publication date: August 16, 2012Inventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
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Patent number: 8242275Abstract: Antibacterial compounds, compositions containing them, and methods of use for the inhibition of bacterial activity and the treatment, prevention or inhibition of bacterial infection.Type: GrantFiled: July 9, 2010Date of Patent: August 14, 2012Assignee: Janssen Pharmaceutica NVInventors: Brett D. Allison, Laurent Gomez, Cheryl A. Grice, Michael D. Hack, Brian J. Morrow, S. Timothy Motley, Alejandro Santillan, Jr., Karen J. Shaw, Kimberly L. Schwarz, Liu Y. Tang, Hariharan Venkatesan, John J. M. Wiener
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Patent number: 8242124Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, diketopiperidine derivatives that possess unique antiviral activity are provided. These compounds are useful for the treatment of HIV and AIDS.Type: GrantFiled: June 24, 2009Date of Patent: August 14, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Alicia Regueiro-Ren, Jacob Swidorski, Zheng Liu, Tao Wang, Zhongxing Zhang, Lawrence G. Hamann, Nicholas A. Meanwell, David J. Carini, Wenying Li
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Publication number: 20120196856Abstract: The present invention is directed to aryl aminopyridine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: ApplicationFiled: October 26, 2010Publication date: August 2, 2012Inventors: Michael J. Breslin, Christopher D. Cox, Izzat T. Raheem
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Publication number: 20120189537Abstract: Disclosed are nitrile derivatives and pharmaceutical compositions comprising nitrile derivatives. The pharmaceutical compositions comprise compounds of the formula I and the pharmaceutically acceptable salts of such compounds. Also disclosed are processes for the preparation of such compounds, intermediates used in the preparation of such compounds, and the uses of such compounds in treating hyperproliferative diseases, inflammatory diseases and viral and bacterial infections and inducing apoptosis in cancer cells.Type: ApplicationFiled: November 22, 2011Publication date: July 26, 2012Inventor: Krishna Menon
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Publication number: 20120178776Abstract: In one aspect, the invention relates to dihydronaphthyridinyl(organo)methanone analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: January 12, 2012Publication date: July 12, 2012Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, Jason Manka, Jon Jacobs, Ya Zhou, José Manuel Bartolomé-Nebreda, Gregor James Macdonald, Susana Conde-Ceide, Eric S. Dawson
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Publication number: 20120178723Abstract: This invention provides compounds of formula IA-a or IB-a and subsets thereof: wherein Z, HY, R1, R2, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: August 11, 2011Publication date: July 12, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Masaaki Hirose, Zhigen Hu, Yongbo Hu, Hong Myung Lee, Zhan Shi, Stepan Vyskocil, Tianlin Xu
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Patent number: 8217029Abstract: The invention relates to compounds of formula (I) wherein U, V, W, X, R1, R2, R3, R4, R5, R6, A, B, D, E, G, m, and n are as defined in the description, to pharmaceutically acceptable salts of such compounds for use in the manufacture of a medicament for the prevention or treatment of a bacterial infection. Certain compounds of formula (I) are new and are also part of this invention.Type: GrantFiled: April 11, 2008Date of Patent: July 10, 2012Assignee: Actelion Pharmaceuticals LtdInventors: Daniel Bur, Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Publication number: 20120172391Abstract: In one aspect, the invention relates to naphthyridinone analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: December 29, 2011Publication date: July 5, 2012Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, Jason Manka, Jon Jacobs, Ya Zhou, José Manuel Bartolomé-Nebreda, Gregor James Macdonald, Susana Conde-Ceide, Carrie K. Jones
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Publication number: 20120172376Abstract: The present invention relates to novel heterocyclic compounds of formula I wherein the variables are as defined in the claims or the description, which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), compositions containing the compounds, their use for preparing a medicament for the treatment of a medical disorder susceptible to the treatment with a compound that modulates, preferably inhibits, the activity of glycogen synthase kinase 3?, and methods of treatment of medical disorders susceptible to treatment with a compound that modulates glycogen synthase kinase 3? activity using the compounds.Type: ApplicationFiled: December 29, 2011Publication date: July 5, 2012Applicant: Abbott GmbH & Co. KGInventors: Sean Colm Turner, Helmut Mack, Margaretha Henrica Maria Bakker, Marcel van Gaalen, Carolin Hoft, Wilfried Hornberger
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Patent number: 8211908Abstract: Disclosed is a compound represented by the general formula: [wherein R1 represents an aryl or heterocyclic group which may be substituted or the like; X1 represents a C2-C4 alkylene group or the like; X2, X3 and X5 independently represent NH, a bond or the like; X4 represents a lower alkylene group, a bond or the like; Y1 represents a bivalent alicyclic hydrocarbon residue which may be substituted or a bivalent alicyclic amine residue which may be substituted; and Z1, Z2, Z3, Z4, Z5 and Z6 independently represent a nitrogen atom, a group represented by the formula: CH, or the like, provided that at least one of Z3, Z4, Z5 and Z6 represents a nitrogen atom] or a salt thereof, which is useful as an antibacterial agent.Type: GrantFiled: May 24, 2007Date of Patent: July 3, 2012Assignees: Toyama Chemical Co., Ltd., Taisho Pharmaceutical Co., Ltd.Inventors: Taro Kiyoto, Junichi Ando, Tadashi Tanaka, Yasuhiro Tsutsui, Mai Yokotani, Toshiya Noguchi, Fumihito Ushiyama, Hiroki Urabe, Hiromasa Horikiri
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Publication number: 20120165276Abstract: Disclosed are compounds having at least one quaternary alkyl ammonium functionality. 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: June 28, 2012Applicant: Mpex Pharmaceuticals, Inc.Inventors: TOMASZ GLINKA, Olga Lomovskaya, Keith Bostian, David M. Wallace
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Publication number: 20120142685Abstract: The present invention provides a compound formula I: (formula I) said compound is inhibitor of selective subset of kinases belonging to the AGC or calmodulin kinase family, such as for example MARK1/2/3, PKD-1/2/3, PKN-1/2, CDK-9, CaMKII, ROCK-I/II, inhibitors of histone deacetylase (HDAC) phosphorylation, or inhibitors of other kinases. Finally, the present invention also provides a pharmaceutical composition.Type: ApplicationFiled: April 4, 2008Publication date: June 7, 2012Inventors: Markus Rolf Dobler, Charles Francis Jewell, JR., Erik Meredith, Lauren G. Monovich, Sarah Siska, Anette Von Matt, Maurice Van Eis, Taeyoung Yoon, Christoph Gaul, Michael Paul Capparelli
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Patent number: 8193179Abstract: Antibacterial compounds including 3-amino-6-(1-amino-ethyl)-tetrahydropyran derivatives are provided, and methods of treatment or prevention of bacterial infection with such compounds are provided.Type: GrantFiled: June 13, 2008Date of Patent: June 5, 2012Assignee: Actelion Pharmaceuticals, LtdInventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Patent number: 8188113Abstract: The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.Type: GrantFiled: September 12, 2007Date of Patent: May 29, 2012Assignee: Deciphera Pharmaceuticals, Inc.Inventors: Daniel L. Flynn, Peter A. Petillo, Michael D. Kaufman, William C. Patt
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Patent number: 8183238Abstract: Compounds of Formula X: wherein A, X, Y, Z, R5, R6a, and R6b are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other neurodegenerative and/or neurological disorders in mammals, including humans.Type: GrantFiled: June 16, 2010Date of Patent: May 22, 2012Assignee: Pfizer Inc.Inventors: Michelle M. Claffey, Amy B. Dounay, Matthew M. Hayward, Suobao Rong, Patrick R. Verhoest, Jamison B. Tuttle, Xinmin Gan
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Publication number: 20120122891Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: ApplicationFiled: November 10, 2011Publication date: May 17, 2012Applicant: NEUROCRINE BIOSCIENCES, INC.Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Richard Lowe, Willy Moree, Nicole Smith, Warren Wade, Liren Zhao, Yun-Fei Zhu, Martin Rowbottom, Neil Ashweek
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Publication number: 20120122853Abstract: Annelated N-heterocyclic sulfonamides with oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals The invention relates to annelated N-heterocyclic sulfonamides with oxadiazolone headgroup and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARalpha agonist activity. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: ApplicationFiled: May 22, 2009Publication date: May 17, 2012Applicant: SANOFI-AVENTISInventors: Stefanie Keil, Matthias Urmann, Wolfgang Wendler, Maike Glien, Hans Matter, Eugen Falk, Ulrike Wendler
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Publication number: 20120115899Abstract: Compounds of Formula (I), wherein substituents R1, R2 and R5 are as defined, and Ar represents substituted phenyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, furanyl, imidazolyl and thiophenyl substituted by a hydroxyalkyl substituent and an optional other substituent; compositions containing them, their use in therapy, including their use as antibacterials, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.Type: ApplicationFiled: January 15, 2010Publication date: May 10, 2012Inventors: Carlos Alemparte-Gallardo, David Barros-Aguirre, Monica Cacho-Izquierdo, Jose Maria Fiandor Roman, Jose Luis Lavandera Diaz, Modesto Jesús Remuiñan-Blanco
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Publication number: 20120115900Abstract: The present application discloses novel substituted naphthyridine derivatives of Formula (I) and their use as modulators of the voltage gated Kv7 (KCNQ) potassium ion channels. In other aspects the application discloses the use of these compounds, in a method for therapy and to pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: April 21, 2010Publication date: May 10, 2012Applicant: NEUROSEARCH A/SInventors: William Dalby Brown, Carsten Jessen, Cecilia Mattsson, Richard Sott, Dorte Strøbæk
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Publication number: 20120108581Abstract: The present invention provides a low molecular weight compound having EPO production-promoting action and/or hemoglobin production-promoting action. The present invention relates to a fused piperidine compound represented by the following general formula (1): (wherein, ring A represents a C10-14 aryl group or 5- to 10-membered heterocyclic group, X represents N—R7, a sulfur atom or an oxygen atom, R1, R2, R2?, R3 and R3? independently represent a hydrogen atom, C1-6 alkyl group or C3-6 cycloalkyl group, and R4, R5 and R6 independently represent a hydrogen atom or halogen atom), or a salt thereof, or a solvate thereof.Type: ApplicationFiled: March 25, 2010Publication date: May 3, 2012Applicant: Kowa Company, LtdInventors: Masanori Ashikawa, Toshiharu Morimoto, Hajime Yamada, Shunji Takemura, Tatsuaki Nishiyama, Takeshi Doi, Hiroyuki Ishiwata
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Publication number: 20120108576Abstract: The present invention provides compounds, salts and hydrates of Formula I, wherein the variables Ar1, R2, R3, R4, r, q, and t are defined herein. Certain compounds of Formula I described herein possess potent antiviral activity. The invention also provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. Certain compounds described herein inhibit assembly of the HCV replication complex. The invention also provides pharmaceutical compositions containing one or more compounds of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease. These infectious diseases include viral infections, particularly HCV infections.Type: ApplicationFiled: November 30, 2011Publication date: May 3, 2012Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Suoming Zhang, Avinash Phadke, Cuixian Liu, Xiangzhu Wang, Jesse Quinn, Dawei Chen, Venkat Gadhachanda, Shouming Li, Milind Deshpande
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Patent number: 8168651Abstract: The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the invention can modulate Pim kinase activity and/or FMS-like tyrosine kinase (Flt) activity. The invention also relates in part to methods for using such molecules.Type: GrantFiled: March 2, 2009Date of Patent: May 1, 2012Assignee: Cylene Pharmaceuticals, Inc.Inventors: Peter C. Chua, Mustapha Haddach, Johnny Y. Nagasawa, Fabrice Pierre, Jeffrey P. Whitten