Nitrogen, Other Than As Nitro Or Nitroso, Attached Directly To The Isoquinoline Ring System By Nonionic Bonding Patents (Class 514/310)
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Publication number: 20120029012Abstract: The present invention relates to 5, 6, or 7-substituted-3-(hetero)arylisoquinolinamine derivatives represented by general formula D, their pharmacologically acceptable salts thereof, and compositions containing such compounds. Methods for treating hyperproliferative disorders by administering the compounds are also included.Type: ApplicationFiled: October 7, 2011Publication date: February 2, 2012Applicant: Rexahn Pharmaceuticals, Inc.Inventors: YOUNG B. LEE, Chang H. Ahn, Won-Jea Cho
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Publication number: 20120028990Abstract: A 3-aryl or heteroaryl-substituted indole derivative which is effective as a preventive or remedy for various diseases is provided. [Means for Resolution] A compound represented by a formula (I) or a pharmaceutically acceptable salt thereof is provided. In the formula, R1 represents a hydrogen atom, C1-6 alkyl et al; R2 represents a hydrogen atom, C1-6 alkyl et al; Z represents aryl or heteroaryl (with the proviso that imidazolyl is excluded); and W represents a group represented by the formula (w-1) or (w-2). In the formula, R3 represents C1-6 alkyl et al; Yl and Y2 both represent a hydrogen atom or Y1 and Y2 together form —CH2-CH2-; Q represents CH or N; Ar represents phenyl, furyl et al; R4 and R5 each independently represent a hydrogen atom or C1-6 alkyl or R4 and R5 together with the nitrogen atom form pyrrolidine et al.Type: ApplicationFiled: April 14, 2010Publication date: February 2, 2012Inventors: Takashi Fujimura, Hiroyuki Kishino, Takashi Mizutani, Shunji Sakuraba, Takahide Sasaki, Nagaaki Sato
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Patent number: 8106066Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the ?7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: GrantFiled: September 22, 2006Date of Patent: January 31, 2012Assignee: Memory Pharmaceuticals CorporationInventors: Richard Schumacher, Mihaela Diana Danca, Jianguo Ma, Brian Herbert, True Minh Nguyen, Wenge Xie, Ashok Tehim
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Patent number: 8097758Abstract: The invention relates to the compounds of formula (I) having antithrombotic activity which especially inhibit blood clotting factor IXa, to methods for producing the same and to the use thereof as drugs.Type: GrantFiled: March 9, 2009Date of Patent: January 17, 2012Assignee: Sanofi-AventisInventors: Henning Steinhagen, Markus Follmann, Jochen Goerlitzer, Herman Schreuder
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Patent number: 8093266Abstract: Substituted amide and urea derivatives useful as inhibitors of Rho kinase are described, which inhibitors can be useful in the treatment of various disorders such as cardiovascular diseases, cancer, neurological diseases, renal diseases, bronchial asthma, erectile dysfunction and glaucoma.Type: GrantFiled: January 2, 2008Date of Patent: January 10, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Georg Dahmann, Eugene Richard Hickey, Xiang Li, Wang Mao, Daniel R. Marshall, Tina M. Morwick, Robert Sibley, Roger John Snow, Ronald J. Sorcek, Frank Wu, Erick Richard Roush Young
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Publication number: 20120004261Abstract: The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression.Type: ApplicationFiled: May 4, 2011Publication date: January 5, 2012Applicant: YALE UNIVERSITYInventors: William L. Jorgensen, Richard J. Bucala
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Patent number: 8088793Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.Type: GrantFiled: August 11, 2008Date of Patent: January 3, 2012Assignee: Cytokinetics, Inc.Inventors: Xiangping Qian, Chihyuan (Grace) Chuang, Pu-Ping Lu, Bing Yao, Qing (Kevin) Lu, Hong Jiang, Wenyue Wang, Bradley P. Morgan, David J. Morgans, Jr.
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Publication number: 20110319390Abstract: 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: September 12, 2011Publication date: December 29, 2011Applicant: AERIE PHARMACEUTICALS, INC.Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Geoffrey Richard Heintzelman, Susan M. Royalty
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Patent number: 8084451Abstract: Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or the CB2 cannabinoid receptors. One aspect discloses hetero pyrrole analogs acting as antagonists for the CB1 and/or the CB2 receptors. Another aspect discloses hetero pyrrole analogs having selectivity for the CB1 or CB2 cannabinoid receptor. Also disclosed are pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect.Type: GrantFiled: January 10, 2006Date of Patent: December 27, 2011Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Venkata Kiran Rao Vemuri, Teresa Olszewska
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Publication number: 20110312935Abstract: There are provided compounds of formula (I), wherein R1, R6, R8, Q2, Q3, Q3a, Q4, L and A have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation and/or cancer.Type: ApplicationFiled: September 25, 2009Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Roland Pfau, Kirsten Arndt, Henri Doods, Norbert Hauel, Klaus Klinder, Raimund Kuelzer, Juergen Mack, Henning Priepke, Dirk Stenkamp
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Patent number: 8071619Abstract: The invention relates to a novel injectable liquid formulation of paracetamol, comprising an aqueous solvent, a buffer agent with a pKa between 4.5 and 6.5, an isotonic agent and the dimer of paracetamol of formula (I), a method for preparation of said formulation and the use of said dimer for the stabilisation of a liquid paracetamol pharmaceutical formulation.Type: GrantFiled: February 16, 2004Date of Patent: December 6, 2011Inventor: Tho Nguyen-Xuan
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Patent number: 8063036Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: April 7, 2010Date of Patent: November 22, 2011Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
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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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Patent number: 8034829Abstract: The present invention relates to 5, 6, or 7-substituted-3-(hetero)arylisoquinolinamine derivatives represented by general formula D, their pharmacologically acceptable salts thereof, and compositions containing such compounds. Methods for treating hyperproliferative disorders by administering the compounds are also included.Type: GrantFiled: November 15, 2007Date of Patent: October 11, 2011Assignee: Rexahn Pharmaceuticals, Inc.Inventors: Young B. Lee, Chang H. Ahn, Won-Jea Cho
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Publication number: 20110245248Abstract: The invention relates to 6-piperidinyl-substituted isoquinoline derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.Type: ApplicationFiled: June 15, 2011Publication date: October 6, 2011Applicant: SANOFI-AVENTISInventors: Oliver Plettenburg, Armin Hofmeister, Dieter Kadereit, Stefan Peukert, Sven Ruf, Kurt Ritter, Matthias Loehn, Yuri Ivashchenko, Peter Monecke, Matthias Dreyer, Aimo Kannt
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Patent number: 8026256Abstract: Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence, or bladder overactivity.Type: GrantFiled: October 26, 2005Date of Patent: September 27, 2011Assignee: Abbott LaboratoriesInventors: Arthur Gomtsyan, Erol K. Bayburt, John R. Koenig, Chih-Hung Lee
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Patent number: 8017601Abstract: 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: GrantFiled: June 30, 2006Date of Patent: September 13, 2011Assignee: Amgen Inc.Inventors: Tae-Seong Kim, Jean-Christophe Harmange, Steven Bellon, Shon Booker, Noel D'Angelo, Celia Dominguez, Ingrid M. Fellows, Julie Germain, Timothy S. Harvey, Joseph L. Kim, Matthew Lee, Longbin Liu, Vinod F. Patel, Andrew Tasker
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Patent number: 8008323Abstract: Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A/2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.Type: GrantFiled: April 13, 2010Date of Patent: August 30, 2011Assignee: ACADIA Pharmaceuticals Inc.Inventors: David M. Weiner, Robert E. Davis, Mark R. Brann, Carl-Magnus A. Andersson, Allan K. Uldam
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Patent number: 7998978Abstract: The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein: R1, R2, Z1, t, and ring A are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of JNK, such as diabetes, the method comprising administering to a mammal an effective amount of a compound of formula (I).Type: GrantFiled: April 19, 2007Date of Patent: August 16, 2011Assignee: Pfizer Inc.Inventors: Liming Huang, Song Liu, Elizabeth A. Lunney, Simon P. Planken
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Patent number: 7993670Abstract: A germicidal absorptive material for use in surgical packings, wound bandages, sanitary tampons and bed sore prevention and/or treatment uses is provided by a foam-like matrix of hydrophilic polyurethane polymer to which application-specific loads of a germicidal disinfectant dye have been made. Polyurethane polymer of various densities and thicknesses exhibits an exceptional ability to absorb different levels of a number of disinfectant dyes, both basic and acidic, such as gentian violet and methylene blue, respectively. The relationship between dye-load and application-specific uses permits a totally-bound gentian violet pad to be used as a conventional bandage or pad on a surface wound with the capability of preventing the incursion of external pathogens from entering the wound through the pad, where the pathogens are killed by the bound-dye. The wound exudate is absorbed safely by the pad, where wound-originating pathogens are also killed.Type: GrantFiled: August 20, 2003Date of Patent: August 9, 2011Assignee: General Wound Kare, Inc.Inventors: Richard M. Simonson, Theodore McAllister, Richard R. Suchanec, Daniel A. White
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Patent number: 7994193Abstract: Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A/2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.Type: GrantFiled: April 13, 2010Date of Patent: August 9, 2011Assignee: ACADIA Pharmaceuticals Inc.Inventors: David M. Weiner, Robert E. Davis, Mark R. Brann, Carl-Magnus A. Andersson, Allan K. Uldam
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Patent number: 7994192Abstract: Novel bicyclic heteroaromatic compounds are provided that are inhibitors of bacterial methionyl tRNA synthetase (MetRS). Compounds of the invention generally have a left hand side chroman group or left hand side tetrahydroquinoline group and a right hand side thienopyridone group. Also disclosed are methods for their preparation and their use in therapy as antibacterial agents, particularly as anti-Clostridium difficile agents.Type: GrantFiled: September 11, 2007Date of Patent: August 9, 2011Assignee: Crestone, Inc.Inventors: Joseph Guiles, Xicheng Sun, Nebojsa Janjic, Sarah Strong
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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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Patent number: 7981883Abstract: The present invention relates to substituted spiro compounds, to processes for preparing them, to medicaments comprising these compounds and to the use of these compounds for producing medicaments.Type: GrantFiled: May 17, 2006Date of Patent: July 19, 2011Assignee: Gruenenthal GmbHInventors: Robert Frank, Ruth Jostock, Melanie Reich, Gregor Bahrenberg, Hans Schick, Helmut Sonnenschein
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Publication number: 20110172236Abstract: A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.Type: ApplicationFiled: September 21, 2009Publication date: July 14, 2011Inventors: Prasun K. Chakravarty, Joseph L. Duffy, Pengcheng Patric Shao
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Publication number: 20110172230Abstract: [Object] To provide a compound which can be used for the treatment of a disease associated with fatty acid amide hydrolase (FAAH), particularly urinary frequency, urinary incontinence and/or overactive bladder. [Means for solution] It is confirmed that a urea compound chemical-structurally characterized by having a piperidine or piperazine ring or a salt thereof has an excellent FAAH-inhibitory activity, and thus the present invention is completed. The urea compound or its pharmaceutically acceptable salt of the present invention can increase the effective bladder capacity and ameliorate the state of urinary frequency, and is therefore useful as an agent for treating urinary frequency, urinary incontinence and/or overactive bladder.Type: ApplicationFiled: August 22, 2007Publication date: July 14, 2011Inventors: Takahiro Ishii, Takashi Sugane, Akio Kakefuda, Tatsuhisa Takahashi, Tokatoshi Kanayama, Kentaro Sato, Ikumi Kuriwaki, Chika Kitada, Jotaro Suzuki
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Publication number: 20110166125Abstract: The present invention relates to new substituted prolinamides of general formula (I) wherein D, Y, A, B, R3, R4 and R5 are defined as in the specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.Type: ApplicationFiled: November 14, 2008Publication date: July 7, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Kai Gerlach, Herbert Nar, Henning Priepke, Annette Schuler-Metz, Wolfgang Wienen
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Patent number: 7973052Abstract: Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed.Type: GrantFiled: February 25, 2009Date of Patent: July 5, 2011Assignee: Wellstat Therapeutics CorporationInventors: Kirvin L. Hodge, Shalini Sharma, Reid W. von Borstel, Stephen D. Wolpe
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Patent number: 7973050Abstract: Novel compounds in enantiomeric excess that are inhibitors of bacterial methionyl synthetase (MetRS) are disclosed. Also disclosed are methods for their preparation and their use in therapy as antibacterial agents, and in particular their use in therapy for Clostridium difficile infection.Type: GrantFiled: September 11, 2007Date of Patent: July 5, 2011Assignee: Crestone, Inc.Inventors: Joseph Guiles, Xicheng Sun, Nebojsa Janjic, Sarah Strong, Albert Charles Gyorkos
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Combination therapy with glatiramer acetate and mitoxantrone for the treatment of multiple sclerosis
Patent number: 7968511Abstract: The subject invention provides a method of treating a subject afflicted with a form of multiple sclerosis comprising periodically administering to the subject an amount of glatiramer acetate and an amount of mitoxantrone, wherein the amounts when taken together are effective to alleviate a symptom of the form of multiple sclerosis in the subject so as to thereby treat the subject. The subject invention also provides a package comprising glatiramer acetate, mitoxantrone and instructions for use of the together to alleviate a symptom of a form of multiple sclerosis in a subject. Additionally, the subject invention provides a pharmaceutical composition comprising an amount of glatiramer acetate and an amount of mitoxantrone, wherein the amounts when taken together are effective to alleviate a symptom of a form of multiple sclerosis in a subject.Type: GrantFiled: May 14, 2004Date of Patent: June 28, 2011Assignee: Teva Pharmaceutical Industries, Ltd.Inventor: Timothy Vollmer -
Publication number: 20110152282Abstract: The invention provides a method, compounds and compositions for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or GIi gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula (I).Type: ApplicationFiled: August 24, 2009Publication date: June 23, 2011Applicant: IRM LLCInventors: Dai Cheng, Dong Han, Guobao Zhang, Yongqin Wan, Yun Feng Xie, Jiqing Jiang, Wenqi Gao, Shifeng Pan
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Publication number: 20110136860Abstract: A compound of formula (I): Or its salts or pharmaceutically acceptable derivatives thereof wherein: A represents a chemical moiety with the general formula (II): X and Y are independently selected from a group consisting of CH2, CH(R5) or C(R5)(R6); R1 is selected from the group consisting of optionally substituted arylalkyl, and optionally substituted heteroarylalkyl; R2 is selected from the group consisting of optionally substituted aryl or optionally substituted heteroaryl or NR7R8; R3 R4 R5 R6 R7 and R8 are as defined herein, n=0, 1, 2 or 3; o=0, 1 or 2, with the proviso that when o=0, then n is 1, 2 or 3 and when o=1, then n is 1 or 2 is provided. Pharmaceutical compositions comprising the compounds are also provided. These compounds are useful in the treatment of various disorders including arrhythmia.Type: ApplicationFiled: June 4, 2010Publication date: June 9, 2011Applicant: Xention Ltd.Inventors: Richard John Hamlyn, Mushtaq Mulla, David Madge
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Publication number: 20110130431Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: February 8, 2011Publication date: June 2, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Angela BERRY, Pier Francesco CIRILLO, Eugene Richard HICKEY, Doris RIETHER, David THOMSON, Renee M. ZINDELL, Nigel BLUMIRE, Chandana CHOWDHURY, Monika ERMANN, James Edward JENKINS, Innocent MUSHI, Christopher Francis PALMER, Malcolm TAYLOR
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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: 20110124680Abstract: The invention relates to novel anthranilamide pyridinureas as VEGF receptor kinase inhibitors, their production and use as pharmaceutical agents for preventing or treating diseases that are triggered by persistent angiogenesis.Type: ApplicationFiled: February 2, 2011Publication date: May 26, 2011Inventors: Rolf BOHLMANN, Martin Haberey, Andreas Huth, Stuart James Ince, Martin Krueger, Karl-Heinz Thierauch, Holger Hess-Stumpp, Andreas Reichel
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Patent number: 7943638Abstract: 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: GrantFiled: July 12, 2006Date of Patent: May 17, 2011Assignee: Sumitomo Chemical Company, LimitedInventors: Shin-ichiro Souma, Yoshiharu Kinoshita
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Publication number: 20110112071Abstract: A compound represented by formula (I?): (wherein m, n, and p each represent 0 to 2; q represents 0 or 1; R1 represents halogen, a hydrocarbon group, a heterocyclic group, an alkoxy group, an alkoxycarbonyl group, a sulfamoyl group, a CN group, an NO2 group, or the like; R2 represents halogen, amino, a hydrocarbon group, an aromatic heterocyclic group, or an oxo group; X1 represents O, —NR3—, or —S(O)r-; X2 represents a methylene group, O, —NR3—, or —S(O)r-; Q? represents a heteroaryl group, a heteroarylalkyl group, a substituted aryl group, or an aralkyl group; Cycle moiety represents an aryl ring or a heteroaryl ring; and the wavy line represents an E-isomer or a Z-isomer), a salt of the compound, or a solvate of the compound or the salt. A pharmaceutical composition and a transient receptor potential type I (TRPV1) receptor antagonist each contain, as an active ingredient, at least one of the compound, a salt of the compound, and a solvate of the compound or the salt.Type: ApplicationFiled: January 18, 2011Publication date: May 12, 2011Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventors: Hideharu UCHIDA, Naoto Kosuga, Tsutomu Satoh, Daido Hotta, Tomoyuki Kamino, Yoshitaka Maeda, Ken-ichi Amano, Yasushige Akada
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Publication number: 20110105463Abstract: Compounds of Formula (I): in which A1, A2, W, L, G, R7a, R7b, R8, R9 and R10 have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.Type: ApplicationFiled: June 24, 2009Publication date: May 5, 2011Applicant: ARRAY BIOPHARMA INC.Inventors: Laurence E. Burgess, Christopher T. Clark, Adam Cook, Christopher P. Corrette, Robert Kirk DeLisle, George A. Doherty, Kevin W. Hunt, Todd T. Romoff
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Publication number: 20110092514Abstract: 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: November 19, 2010Publication date: April 21, 2011Applicant: CanBas Co., Ltd.Inventors: TAKUMI KAWABE, Machiyo Ishigaki, Takuji Sato, Sayaka Yamamoto, Yoko Hasegawa
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Publication number: 20110092540Abstract: The invention relates to compounds having pharmacological activity towards the 5-HT6; receptor, and more particularly to some N-phenyl-2,3-dihydroimidazol[2,1-b]thiazole-5-sulfonamide derivatives, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT6 is involved.Type: ApplicationFiled: May 8, 2009Publication date: April 21, 2011Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Josep Mas Prio, Antoni Torrens Jover
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Publication number: 20110086838Abstract: The present invention relates to thiophene containing compounds of formula (I) wherein m, n, p, q, r, s, R1, R2, and R3 are as defined in the description. Included also are pharmaceutical compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and pharmaceutical compositions.Type: ApplicationFiled: December 14, 2010Publication date: April 14, 2011Applicant: ABBOTT LABORATORIESInventors: Derek W Nelson, Jennifer M. Frost
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Patent number: 7923446Abstract: The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.Type: GrantFiled: May 31, 2007Date of Patent: April 12, 2011Assignee: Wyeth LLCInventors: Jason Shaoyun Xiang, Steve Yikkai Tam, Yonghan Hu, Phaik-Eng Sum, David Brian How, Darrin William Hopper, Matthew Douglas Vera, Joshua James Sabatini, Thomas Saltmarsh Rush, III, Elisabeth Ann Morris, Katy Evangelia Georgiadis
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Publication number: 20110071165Abstract: Aza- and polyazanthranyl amides and their use as medicaments in the treatment of diseases caused by persistent angiogenesis are described, as well as the intermediates used in the preparation of the aza- and polyazanthranyl amides.Type: ApplicationFiled: November 24, 2010Publication date: March 24, 2011Applicant: NOVARTIS AGInventors: Dieter SEIDELMANN, Martin KRÜGER, Orlin PETROV, Andreas HUTH, Karl-Heinz THIERAUCH, Andreas MENRAD, Martin HABEREY
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Publication number: 20110065713Abstract: The present invention is directed to benzazole compounds that inhibit ?-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment or prevention of diseases in which BACE is involved, such as Alzheimer's disease. 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 BACE is involved.Type: ApplicationFiled: November 19, 2010Publication date: March 17, 2011Applicant: High Point Pharmaceuticals, LLCInventors: Adnan M.M. Mjalli, David Jones, Devi Reddy Gohimmukkula, Guoxiang Huang, Jeff Zhu, Mohan Rao, Robert C. Andrews, Tan Ren
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Publication number: 20110065138Abstract: The present invention relates to a quantitative method for detecting yessotoxins in fishery products based on the activation the toxin produces on cellular phosphodiesterases and the therapeutic use of this activation. The cellular target of yessotoxin (YTX) and its analogs is the activation of phosphodiesterases (PDEs). The PDEs-YTX bond produces a measurable signal. The bond can be quantified by means of an affinity biosensor or by fluorescence. The biosensor detects biomolecular interactions and allows determining the presence of YTX due to its interaction with PDEs. The variations in the degradation rate of the fluorescent derivative anthraniloyl-cAMP are determined by means of plate fluorescence. The rate at which the PDEs degrade this molecule increases in the presence of YTX. YTX inhibits immunological activation of mastocytes in rats and induces a cytotoxic effect in human hepatocarcinoma cells, which implies two therapeutic uses of YTXs as an antiallergic and antitumor compound.Type: ApplicationFiled: July 21, 2004Publication date: March 17, 2011Applicant: UNIVERSIDADE DE SANTIAGO DE COMPOSTELAInventors: Luis Miguel Botana López, Amparo Alfonso Rancaño, Maria Jose Pazos Guldris, Mercedes Rodrugues Vieytes, Maria Isabel Loza Garcia, JUan Manuel Vieites Baptista De Sousa
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Patent number: 7902223Abstract: Novel compounds of the formula (I), in which D, W, X, Y, T and R1 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumors.Type: GrantFiled: July 12, 2002Date of Patent: March 8, 2011Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Bertram Cezanne, Christos Tsaklakidis, Werner Mederski, Johannes Gleitz, Christopher Barnes
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Patent number: 7902224Abstract: The present invention is directed to compounds of formula (I): wherein R represents a methyl or an ethyl group X represents N, C—H or C—CH3 when X represents C—H or C—CH3, Y represents N when X represents N, Y represents C—H and physiologically functional derivatives thereof, pharmaceutical compositions comprising the compounds, the use of the compounds for the manufacture of medicaments particularly for the treatment of inflammatory and/or allergic conditions, processes for the preparation of the compounds, and chemical intermediates in the processes for the manufacture of the compounds.Type: GrantFiled: August 10, 2005Date of Patent: March 8, 2011Assignee: Glaxo Group LimitedInventors: Christine Edwards, Garry Fenton, Simon John Fawcett MacDonald, Gordon Gad Weingarten
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Patent number: 7897589Abstract: The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.Type: GrantFiled: July 14, 2006Date of Patent: March 1, 2011Assignee: Laboratorios Del Dr. Esteve, S.A.Inventors: Antoni Torrens, Jordi Quintana, Helmut Buschmann, Albert Dordal, Josep Mas
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Patent number: 7897618Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: where the variables are as define herein, and their use as pharmaceuticals, specifically as orexin receptor antagonists.Type: GrantFiled: October 29, 2007Date of Patent: March 1, 2011Assignee: SmithKline Beecham LimitedInventors: Clive Leslie Branch, Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, David John Nash, Riccardo Novelli, Jean-Pierre Pilleux, Roderick Alan Porter, Rachel Elizabeth Anne Stead, Geoffrey Stemp
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Patent number: 7888372Abstract: The key function of TNAP in bone is degradation of PPi to remove this mineralization inhibitor and provide free phosphate for apatite deposition. PC-1 is a direct antagonist of TNAP function. ANK also antagonizes TNAP-dependent matrix calcification. Specifically, the activity of PC-1 inhibits initial MV apatite deposition, but ANK inhibits propagation of apatite outside the MVs. Furthermore, loss of function of the two distinct skeletal TNAP antagonists, PC-1 and ANK, ameliorates TNAP deficiency-associated osteomalacia in vivo. Conversely, the hyperossification associated with both PC-1 null mice and ANK-deficient (ank/ank) mice is ameliorated by deficiency of TNAP in vivo.Type: GrantFiled: April 28, 2003Date of Patent: February 15, 2011Assignees: National Institutes of Health (NIH), The Regents of the University of CaliforniaInventors: Jose Luis Millan, Robert Terkeltaub