Quinoline Or Isoquinoline (including Hydrogenated) Patents (Class 544/363)
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Publication number: 20110269709Abstract: The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.Type: ApplicationFiled: December 23, 2010Publication date: November 3, 2011Inventor: Apparao Satyam
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Publication number: 20110269746Abstract: Compounds exhibiting an osteogenesis-promoting action having the general formula (I) or a pharmacologically acceptable salt thereof: wherein A is selected from among a 3- to 10-membered heterocyclyl group, B is selected from among an amino group, and X is selected from N and CH.Type: ApplicationFiled: July 14, 2011Publication date: November 3, 2011Applicant: Daiichi Sankyo Company, LimitedInventors: Osamu Kanno, Katsuyoshi Nakajima, Kazumasa Aoki, Ryoichi Tanaka, Shimpei Hirano, Kiyoshi Oizumi, Daigo Asano
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Publication number: 20110263610Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated B cell activities, particularly diseases or disorders that involve aberrant activation of inositol 1,4,5-trisphosphate 3-kinase B (ITPKb).Type: ApplicationFiled: March 30, 2009Publication date: October 27, 2011Applicant: IRM LLCInventors: Yongqin Wan, Shifeng Pan, Guobao Zhang, Xia Wang, Yun Feng Xie, Jiqing Jiang, Dean Phillips, Yang Yang
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Publication number: 20110257151Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R5 have the significance given in claim 1, can be used as a medicament.Type: ApplicationFiled: April 7, 2011Publication date: October 20, 2011Inventors: Li Chen, Lichun Feng, Mengwei Huang, Yongfu Liu, Guolong Wu, Jim Zhen Wu, Mingwei Zhou
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Publication number: 20110257160Abstract: This disclosure provides a new class of compounds referred to as “reversed chloroquines” (RCQs), which are highly effective against CQR and CQS malaria parasites. RCQs are hybrid molecules, which include an antimalarial quinoline analog (such as chloroquine) moiety and a CQR reversal moiety. Exemplary RCQ chemical structures are provided. Also provided are pharmaceutical compositions including the disclosed RCQ compounds, and methods of using such compounds and compositions for the treatment of malaria and inhibition of CQR or CQS Plasmodium sp. (such as P. falciparum).Type: ApplicationFiled: April 25, 2011Publication date: October 20, 2011Inventors: David H. PEYTON, Steven BURGESS
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Patent number: 8039462Abstract: The present invention provides methods and compositions comprising compounds useful for stimulating neurogenesis. The methods and compositions comprising compounds are also useful for inhibiting neuronal degeneration. Thus, the present invention can be used in the treatment of diseases and conditions characterized by neuronal loss and reduced neurogenesis including Alzheimer's disease, stroke, traumatic brain injury, and depression. This invention could also be used for research products including single agents or mixtures of agents to promote, proliferate, differentiate, or maintain neurons from stem or progenitor cells.Type: GrantFiled: September 19, 2006Date of Patent: October 18, 2011Assignee: Neuronascent, Inc.Inventor: Judith Kelleher-Anderson
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Patent number: 8039621Abstract: Type I anhydrous aripiprazole is prepared by dissolving aripiprazole (or an acid salt thereof) in an alcoholic solvent, optionally containing water, at elevated temperature, adding seed crystals of Type 1 anhydrous aripiprazole to the solution, cooling the mixture, and isolating crystals aripiprazole and drying the isolated crystals to obtain low moisture Type 1 anhydrous aripiprazole.Type: GrantFiled: October 24, 2007Date of Patent: October 18, 2011Assignee: Cambrex Charles City, Inc.Inventor: Brian T. Becicka
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Publication number: 20110251212Abstract: A compound which specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist is provided. It has been found out that a piperazine derivative represented by the formula (I) binds specifically to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist. A compound represented by: wherein R1 is each independently C1-C3 alkyl or the like, m is an integer of 0 to 4, X is —N(R4)—C(?O)—C(?O)—, —N(R4)—(CR5R6)p—C(?O)—, —N(R4)—C(?O)—(CR7R8)q— or —C(?O)—N(R4)—(CR7R8)q—, p and q are each independently an integer of 1 to 3, R4, R5, R6, R7 and R8 are each independently a hydrogen atom or lower alkyl, A1 is benzoxazolinone or the like, and A2 is optionally substituted phenyl or the like, or a pharmaceutically acceptable salt or a solvate thereof.Type: ApplicationFiled: August 19, 2008Publication date: October 13, 2011Applicant: SHIONOGI & CO., LTD.Inventors: Moriyasu Masui, Minoru Tomida, Naotake Kobayashi, Kousuke Anan, Aya Tazawa, Kayoko Hata
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Publication number: 20110251210Abstract: The disclosure provides modified chloroquine compounds having single ring or fused ring moieties. Also provided are pharmaceutical compositions comprising such compounds, methods of using such compounds to inhibit or treat diseases or conditions caused by chloroquine-resistant (CQR) and chloroquine-sensitive (CqS) malaria parasites and other CQ-susceptible microorganisms, and processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: December 4, 2009Publication date: October 13, 2011Applicants: PORTLAND STATE UNIVERSITY, DESIGNMEDIX, INC.Inventors: David H. Peyton, Steven J. Burgess, Katherine M. Liebman, Bornface Gunsaru
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Publication number: 20110251180Abstract: The present invention provides a pharmaceutical agent that inhibits the chronic progression of Parkinson's disease or protects dopamine neurons from disease etiology, thereby suppressing the progression of neurological dysfunction, so as to prolong the period of time until L-dopa is administered while also improving neuronal function; the pharmaceutical agent of the invention comprising as an active ingredient a quinolone compound represented by Formula (1): or a salt thereof, wherein: R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 represents substituted or unsubstituted phenyl or the like; R4 represents hydrogen or the like; R5 represents hydrogen or the like; R6 represents hydrogen or the like; and R7 represents hydroxy or the like.Type: ApplicationFiled: December 4, 2009Publication date: October 13, 2011Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Kenji Otsubo, Yuji Ochi, Masami Nakai, Atsushi Mori, Takayuki Matsuzaki
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Publication number: 20110243884Abstract: The invention relates to a biodegradable polymer comprising a plurality of releasable bioactive moieties, the releasable bioactive moieties being pendant from and covalently bonded to the biodegradable polymer backbone, wherein the biodegradable polymer backbone is formed from monomeric units that are each coupled via a biodegradable moiety, and wherein the bioactive moieties are capable of being released at a rate equal to or faster than the rate of biodegradation of the polymer backbone.Type: ApplicationFiled: April 8, 2011Publication date: October 6, 2011Inventors: Michael Shane O'Shea, Florian Hans Maximilian Graichen, Russell John Tait, Heng Chy Taing, Justine Leigh Jeffery
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Publication number: 20110237600Abstract: The present invention provides a compound of Formula I: (I) and methods for improving memory in a subject by administering a therapeutically effective amount of the compound.Type: ApplicationFiled: May 11, 2009Publication date: September 29, 2011Inventors: Karoly Nikolich, Laszlo Nadasdi
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Publication number: 20110237792Abstract: Disclosed are quinoline compounds having affinity for the 5-HT6 receptor and having the formula: where R1, R2, R3, R4, R5, n, m, p and A are defined herein, and salts thereof, compositions containing these compounds and salts and processes for making and using the same.Type: ApplicationFiled: June 3, 2011Publication date: September 29, 2011Inventors: Mahmood AHMED, Christopher Norbert Johnson, Martin C. Johnes, Gregor James MacDonald, Stephen Frederick Moss, Mervyn Thompson, Charles Edward Wade, David R. Witty
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Publication number: 20110230476Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: September 9, 2010Publication date: September 22, 2011Applicant: AVILA THERAPEUTICS, INC.Inventors: DEQIANG NIU, RUSSELL C. PETTER, JUSWINDER SINGH, ARTHUR F. KLUGE, HORMOZ MAZDIYASNI, ZHENDONG ZHU, LIXIN QIAO, KEVIN KUNTZ
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Patent number: 8017615Abstract: The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous aripiprazole crystals is stored for an extended period.Type: GrantFiled: April 26, 2007Date of Patent: September 13, 2011Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Takuji Bando, Satoshi Aoki, Junichi Kawasaki, Makoto Ishigami, Youichi Taniguchi, Tsuyoshi Yabuuchi, Kiyoshi Fujimoto, Yoshihiro Nishioka, Noriyuki Kobayashi, Tsutomu Fujimura, Masanori Takahashi, Kaoru Abe, Tomonori Nakagawa, Koichi Shinhama, Naoto Utsumi, Michiaki Tominaga, Yoshihiro Ooi, Shohei Yamada, Kenji Tomikawa
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Patent number: 8017612Abstract: The present invention relates to a compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof and an anti-HCV agent and an HCV polymerase inhibitor containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.Type: GrantFiled: April 17, 2007Date of Patent: September 13, 2011Assignee: Japan Tobacco Inc.Inventors: Hiroyuki Abe, Masahiro Tanaka, Kazuyuki Sugimoto, Akira Suma, Masahiro Yokota, Makoto Shiozaki, Kiyosei Iio, Kazuhito Ueyama, Dai Motoda, Toru Noguchi, Tsuyoshi Adachi, Junichiro Tsuruha, Satoki Doi
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Publication number: 20110217699Abstract: Chemical compounds having a high selectivity for double stranded DNA over RNA and single stranded DNA are disclosed. The chemical compounds are stains that become fluorescent upon illumination and interaction with double stranded DNA, but exhibit reduced or no fluorescence in the absence of double stranded DNA. The compounds can be used in a variety of biological applications to qualitatively or quantitatively assay DNA, even in the presence of RNA.Type: ApplicationFiled: May 10, 2011Publication date: September 8, 2011Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Jolene A. Bradford, Ching-Ying Cheung, Shih Jung Huang, Patrick R. Pinson, Stephen T. Yue
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Patent number: 8012980Abstract: The present invention relates to isoquinolinone derivatives of formula (I): wherein are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: October 1, 2009Date of Patent: September 6, 2011Assignee: AstraZeneca ABInventors: Stephen John Brough, Timothy Jon Luker, Bryan Glyn Roberts, Stephen Anthony St-Gallay
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Patent number: 8012979Abstract: The present invention relates to isoquinolinone derivatives of formula (I): wherein R1, R2, R3, R4, R5, R6 and R7 are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: April 4, 2008Date of Patent: September 6, 2011Assignee: AstraZeneca ABInventors: Matthew Hallam, Barrie Martin, Piotr Raubo, Bryan Roberts, Stephen St-Gallay, Paul Willis
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Publication number: 20110212946Abstract: The present invention is directed to quinolone compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the neuropeptide S receptor is involved.Type: ApplicationFiled: November 3, 2009Publication date: September 1, 2011Inventors: James C. Barrow, Mark T. Bilodeau, Christopher D. Cox, John C. Hartnett, Nathan R. Kett, Yiwei Li, Peter J. Manley, Jeffrey Melamed, William D. Shipe, B. Wesley Trotter, Amy Zartman
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Patent number: 8008299Abstract: This invention is directed to a compound of Formula (I): and forms thereof, wherein A, B, E, G, X and L2 are as defined herein and their use as urotensin II receptor antagonists.Type: GrantFiled: June 5, 2008Date of Patent: August 30, 2011Assignee: Janssen Pharmaceutica, N.V.Inventors: William A. Kinney, Edward C. Lawson, Shyamali Ghosh, Diane K. Luci, David F. McComsey
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Patent number: 8008302Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof, in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: GrantFiled: July 25, 2005Date of Patent: August 30, 2011Assignee: Merck Serono SAInventors: Dominique Swinnen, Agnes Bombrun, Jerome Gonzalez, Stefano Crosignani, Patrick Gerber, Catherine Jorand-Lebrun
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Patent number: 8008490Abstract: The present invention relates to novel polymorphic forms of aripiprazole and processes for producing them. It further relates to pharmaceutical compositions comprising the novel forms and to the use of the novel forms in the treatment of schizophrenia.Type: GrantFiled: January 27, 2006Date of Patent: August 30, 2011Assignee: Sandoz AGInventors: Josef Wieser, Hannes Lengauer, Doris Braun, Ulrich Griesser, Richard Tessadri
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Patent number: 7998963Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein Ar is indolyl, indazolyl or dihydroindolyl, and R1, R2, R3 and R4 are as defined herein. Also provided are pharmaceutical compositions, methods of using the compounds in the treatment of depressive, anxiolytic and other disorders associated with inhibition of the reuptake of norepinephrine, serotonin, and dopamine, and methods of preparing the compounds.Type: GrantFiled: February 12, 2009Date of Patent: August 16, 2011Assignee: Roche Palo Alto LLCInventors: David Scott Carter, Matthew C. Lucas, Ryan Craig Schoenfeld, Robert James Weikert
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Patent number: 7998962Abstract: Racemic mixtures and individual enantiomers of fluorine-18 or carbon-11 radiolabelled 2?-alkyl-6-nitroquipazine ligands are serotonin transporter (SERT) tracers for positron emission tomography (PET) imaging. The non-radioactive ligand forms possess therapeutic antidepressant in vitro and in vivo pharmacological binding profiles in rodent brain and cells expressing human serotonin transporter (hSERT). Twelve 2?-alkyl-6-nitroquipazine ligands potently bind in sub-nanomolar concentrations to the pre-synaptic SERT binding site where established antidepressant drugs bind and inhibit the re-uptake of the neurotransmitter serotonin (5-HT). In vivo tracer studies in rats as well as monkey PET scan trial have demonstrated the fluorine-18 and carbon-11 positron radionuclide labeled tracers perform as quantitative tracers of specific binding the SERT protein in live brain.Type: GrantFiled: September 22, 2010Date of Patent: August 16, 2011Assignee: The University of MontanaInventors: John M. Gerdes, David B. Bolstad, Brian R. Kusche
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Patent number: 7994165Abstract: The invention provides novel ?2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with ?2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: October 6, 2009Date of Patent: August 9, 2011Assignee: Theravance, Inc.Inventors: Robert Murray McKinnell, John R. Jacobsen, Sean G. Trapp, Daisuke Roland Saito
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Patent number: 7989455Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: GrantFiled: December 14, 2006Date of Patent: August 2, 2011Assignee: Cytokinetics, Inc.Inventors: Bradley P. Morgan, David J. Morgans, Jr., Alex Muci, Pu-Ping Lu, Erica A. Kraynack, Todd Tochimoto
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Publication number: 20110183974Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts, stereoisomers or tautomers thereof which are inhibitors of the Sonic Hedgehog pathway, in particular Smo antagonists. Thus the compounds of this invention are useful for the treatment of diseases associated with abnormal hedgehog pathway activation, including cancer, for example basal cell carcinoma, medulloblastoma, prostate, pancreatic, breast, colon, bone and small cell lung cancers, and cancers of the upper GI tract.Type: ApplicationFiled: July 27, 2009Publication date: July 28, 2011Inventors: Gabriella Dessole, Philip Jones, Laura Llauger Bufi, Ester Muraglia, Jesus Maria Ontoria Ontoria, Caterina Torrisi
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Publication number: 20110183965Abstract: 6-Amino isoquinoline compounds are provided that influence, inhibit or reduce the action of a kinase. Pharmaceutical compositions including therapeutically effective amounts of the 6-aminoisoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, obesity and glaucoma are also provided.Type: ApplicationFiled: January 31, 2011Publication date: July 28, 2011Applicant: AERIE PHARMACEUTICALS, INC.Inventors: Mitchell A. deLong, Susan M. Royalty, Jill Marie Sturdivant, Geoffrey Richard Heintzelman
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Publication number: 20110178091Abstract: The present invention relates to novel arylpiperazine-containing pyrrole 3-carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof which is useful for preventing or treating depressive disorders. The present invention also provides a method for preparing the arylpiperazine-containing pyrrole 3-carboxamide derivatives or the pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and a method for preventing or treating depressive disorders.Type: ApplicationFiled: September 23, 2009Publication date: July 21, 2011Applicant: GREEN CROSS CORPORATIONInventors: Jinhwa Lee, Suk Youn Kang, Eun-Jung Park, Kwang-Seop Song, Min Ju Kim, Hee Jeong Seo, Suk Ho Lee, Jeongmin Kim, Ae Nim Pae, Woo-Kyu Park
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Publication number: 20110178097Abstract: The present invention relates to non-hydrate crystalline forms of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one lactic acid salts, solid pharmaceutical formulations containing the same and methods of use. The present invention also relates to crystalline hydrates of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one lactic acid salts, pharmaceutical formulations containing the same and methods of use related thereto. The present invention further relates to crystalline solvates of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one lactic acid salts.Type: ApplicationFiled: May 23, 2006Publication date: July 21, 2011Applicant: NOVARTIS AGInventors: Augustus O. Okhamafe, Joyce Chou, Rampurna Gullapalli, Eric Harwood, David Ryckman, Shuguang Zhu, Xiao Shang
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Publication number: 20110178083Abstract: Vicinal substituted cyclopropyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function, for example neurological, neurodegenerative and psychiatric disorders including, but not limited to, those comprising cognitive deficits or schizophrenic symptoms.Type: ApplicationFiled: July 9, 2009Publication date: July 21, 2011Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Publication number: 20110172415Abstract: It was found out that the nitrogen-containing heterocyclic derivative represented by the formula (I) specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist. A compound represented by: wherein Z is N or CR1, A1 is a nitrogen-containing aromatic monocyclic group which is optionally substituted, a nitrogen-containing aromatic fused cyclic group which is optionally substituted etc., A2 is an aromatic hydrocarbon cyclic group or an aromatic heterocyclic group, each optionally having a substituent, R1, R2, Ra, Rb, Rc and Rd are each independently hydrogen, hydroxy, etc., w is 2 or 3, t is 1 or 2, X is —(CR3R4)m-, —CO(CR3R4)n-, —CONR5(CR3R4)n- etc., m is an integer of 1 to 4, n is an integer of 0 to 4, R3 and R4 are each independently hydrogen, halogen, hydroxy etc., and R5 is hydrogen or lower alkyl, or a pharmaceutically acceptable salt, or a solvate thereof.Type: ApplicationFiled: March 17, 2011Publication date: July 14, 2011Applicant: SHIONOGI & CO., LTD.Inventors: Moriyasu Masui, Makoto Adachi, Hidenori Mikamiyama, Akira Matsumura, Naoki Tsuno
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Publication number: 20110166352Abstract: A process is provided for making sterile aripiprazole having an average particle size less than 100 microns but preferably greater than 25 microns employing an impinging jet crystallization procedure. The resulting bulk aripiprazole of desired particle size may be used to form a sterile freeze-dried aripiprazole formulation, which upon constitution with water and intramuscular injection releases aripiprazole over a period of at least about one week and up to about eight weeks.Type: ApplicationFiled: March 11, 2011Publication date: July 7, 2011Inventors: Margaret M. Gleeson, Soojin Kim, Donald C. Kientzler, San Kiang
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Patent number: 7973039Abstract: The present invention is related to derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: GrantFiled: December 19, 2005Date of Patent: July 5, 2011Assignee: Merck Serono SAInventors: Dominique Swinnen, Agnes Bombrun, Patrick Gerber, Catherine Jorand-Lebrun
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Publication number: 20110160199Abstract: The present invention discloses an aralkyl substituted piperidine or piperazine derivative and the use of the derivative in preparation of medicaments for treating schizophrenia and correlative psychoneuroses. It is shown by pharmacological tests that the derivative of the present invention has better antischizophrenic effect and less toxicity. Said derivative is a free base or salt of the compound having the following general formula.Type: ApplicationFiled: July 28, 2008Publication date: June 30, 2011Applicants: JIANGSU GOWORTH INVESTMENT CO. LTD., SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRYInventors: Jianqi Li, Shaoping Peng, Wangping Cai, Kai Gao
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Publication number: 20110152286Abstract: The present invention provides a heterocyclic compound represented by the general formula (1): The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: ApplicationFiled: December 16, 2010Publication date: June 23, 2011Inventors: Hiroshi YAMASHITA, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Hideaki Kuroda, Haruka Takahashi, Satoshi Shimizu, Tatsuyoshi Tanaka
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Patent number: 7964603Abstract: The present invention refers to substituted tetrahydro-quinoline-sulfonamide compounds of general formula (I): a method for their preparation, a medicament comprising these compounds and the use of substituted tetrahydro-quinoline-sulfonamide compounds for the preparation of medicaments for 5-HT6 receptor regulation as well as for the treatment of disorders related thereto.Type: GrantFiled: July 18, 2008Date of Patent: June 21, 2011Assignee: Laboratorios Del Dr. Esteve, S.A.Inventors: Jose Luis Diaz-Fernandez, Ramon Merce-Vidal, Lajos Novak
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Publication number: 20110144100Abstract: Compounds of Formula (I): I in which B, R1, R1a, R2, R3, R4, R5, R6, R7, R10 and R11 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by PIM-1 and/or PIM-2 and/or PIM-3 kinases.Type: ApplicationFiled: August 18, 2009Publication date: June 16, 2011Applicant: ARRAY BIOPHARMA INC.Inventors: Shelley Allen, Robert Kirk DeLisle, Julie Marie Greschuk, Erik James Hicken, Joseph P. Lyssikatos, Fredrik P. Marmsater, Mark C. Munson, John E. Robinson, Qian Zhao
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Publication number: 20110135650Abstract: The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt or a solvate thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.Type: ApplicationFiled: June 1, 2010Publication date: June 9, 2011Inventors: Samuel CHACKALAMANNIL, Tin-Yau CHAN, Mariappan V. CHELLIAH, Martin C. CLASBY, Michael DWYER, William J. GREENLEE, Tomokazu HIRABAYASHI, Santhosh NEELAMKAVIL, Hidemitsu NISHIDA, Fumihiko SAITOH, Unmesh SHAH, Yan XIA
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Publication number: 20110130394Abstract: The invention provides kinase inhibitor compounds of the formula (1): or salts, solvates, tautomers or N-oxides thereof; wherein X is O, CO, X1C(X2), C(X2)X1, X1C(X2)X1, S, SO, SO2, NRc, SO2NRc or NRcSO2; m is 0-2; n is 0-1; q is 0-2; A is C1-6 alkylene optionally interrupted by O; R1 is halogen, cyano, nitro, an optionally substituted acyclic C1-6 hydrocarbon group, optionally substituted C3-7 cycloalkyl, optionally substituted phenyl, optionally substituted five membered heteroaryl, NR2R3, Ra—Rb, O—Rb or C(O)NR2R8; R4 is fluorine, chlorine, methyl or cyano; R2 is hydrogen or optionally substituted C1-4 alkyl; R3 is Ra—Rb; or NR2R3 forms a 4 to 7 membered non-aromatic heterocyclic ring; Ra is a bond, C(X2), C(X2)X1, SO, SO2 or SO2NRc; Rb is hydrogen or an optionally substituted 3 to 7-membered carbocyclic or heterocyclic ring or an optionally substituted C1-12 acyclic hydrocarbon group; Rc is hydrogen or a C1-4 hydrocarbon group; Rd is O, CO, X1C(X2), C(X2)X1, X1C(X2)X1, S, SO, SO2, NRc, SO2NRc or NRcSO2Type: ApplicationFiled: July 15, 2009Publication date: June 2, 2011Applicant: SENTINEL ONCOLOGY LIMITEDInventors: Robert George Boyle, David Winter Walker
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Publication number: 20110130407Abstract: Isoquinolone derivatives of the general formula I are provided. The compounds are NK3 antagonists and useful for the treatment of e.g. psychosis and schizophrenia.Type: ApplicationFiled: June 19, 2009Publication date: June 2, 2011Applicant: H. LUNDBECK A/SInventors: Nikolay Khanzhin, Karsten Juhl, Søren Møller Nielsen, Klaus Baek Simonsen
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Patent number: 7947701Abstract: The invention relates to dual molecule compounds containing a peroxide derivative, to processes for the synthesis of such compounds, to pharmaceutical compositions comprising such compounds, and to methods of treatment and prevention of malaria comprising administering such compounds and such pharmaceutical compositions.Type: GrantFiled: May 12, 2006Date of Patent: May 24, 2011Assignee: Sanofi-AventisInventors: Jérôme Cazelles, Frédéric Cosledan, Bernard Meunier, Alain Pellet
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Publication number: 20110117591Abstract: Chemical stain compounds containing a fluorophore and a reducible quenching unit are disclosed. The reducible quenching unit quenches the fluorophore while in its oxidized state. Upon reduction, the quenching properties of the quenching unit are diminished or eliminated. The chemical compounds can be used in a variety of applications, including the detection of bacterial cells, monitoring the electron transport chain function of bacterial cells, monitoring the oxidation state of non-biological systems, and assaying the effectiveness of antibacterial or antimicrobial agents.Type: ApplicationFiled: October 20, 2010Publication date: May 19, 2011Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Ching-Ying CHEUNG, Diane R. Gray, Stephen T. Yue
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Publication number: 20110118199Abstract: The present invention relates to the treatment of protozoal diseases by administering cytotoxic and/or cytostatic compounds, in particular those used in anticancer therapy, to patients. In particular, the invention relates to the use of anticancer agents that can penetrate into the CNS for treatment of late stage African sleeping sickness or cerebral malaria.Type: ApplicationFiled: January 11, 2007Publication date: May 19, 2011Inventor: Matthias Dormeyer
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Publication number: 20110118252Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF 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: ApplicationFiled: November 12, 2010Publication date: May 19, 2011Applicant: Amgen Inc.Inventors: Tae-Seong Kim, David Bauer, Steven Bellon, Alessandro Boezio, Shon Booker, Deborah Choquette, Derin C. D'Amico, Noel D'Angelo, Celia Dominguez, Ingrid M. Fellows, Julie Germain, Russell Graceffa, Jean-Christophe Harmange, Satoko Hirai, Daniel La, Matthew Lee, Longbin Liu, Mark H. Norman, Michele Potashman, Philip Roveto, Aaron C. Siegmund, Ning Xi, Kevin Yang
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Patent number: 7943769Abstract: The invention relates to a fluorinated derivate of quinolin-2(1H)-one (I), to a method for preparing the same, and to the use thereof as an intermediate in the synthesis of 7-fluoro-2-oxo-4-[2-[4-[thieno[3,2-c]pyridine-4-yl)piperazin-1-yl]ethyl]-1,2-dihydro-quinolin-1-acetamide. The invention also relates to the pharmaceutically acceptable salts thereof.Type: GrantFiled: June 12, 2009Date of Patent: May 17, 2011Assignee: Sanofi-AventisInventors: Didier Legroux, Veronique Moragues, Jose Ruiz-Montes, Laurent Salle
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Patent number: 7943768Abstract: A compound of formula (I) P—W—C(?X)-L-Q??(I) wherein P is an optionally substituted aryl or heteroaryl group; W is an optionally substituted 6 or 7-membered aliphatic ring comprising ring atoms Y1 and Y2 independently selected from Oxygen and Nitrogen, X is selected from Oxygen, Nitrogen and Sulphur; L is an optional C1-4 linker; and Q is an optionally substituted 4-7 membered aliphatic ring: for use in the treatment of chemokine mediated diseases or disorders.Type: GrantFiled: December 18, 2006Date of Patent: May 17, 2011Assignee: AstraZeneca ABInventors: Justin Fairfield Bower, Peter Wedderburn Kenny, Jeffrey Philip Poyser
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Publication number: 20110112092Abstract: The present invention relates to an adenosine A3 receptor ligand of the general formula (I).Type: ApplicationFiled: January 18, 2011Publication date: May 12, 2011Applicant: sanofi-aventisInventors: Peter ARANYI, Sandor BATORI, Geza TIMARI, Kinga BOER, Zoltan KAPUI, Endre MIKUS, Katalin URBAN-SZABO, Katalin GERBER, Judit VARGANE SZEREDI, Michel FINET
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Patent number: RE42376Abstract: This invention provides compounds of formula I having the structure wherein G1, G2, R1, R4, Z, n, and X are defined in the specification or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.Type: GrantFiled: May 21, 2010Date of Patent: May 17, 2011Assignee: Wyeth Holdings CorporationInventors: Allan Wissner, Hwei-Ru Tsou, Dan M. Berger, Middleton B. Floyd, Jr., Philip R. Hamann, Nan Zhang, Philip Frost