The Additional Hetero Ring Is Five-membered Consisting Of Carbon And Plural Nitrogens As The Only Ring Members Patents (Class 514/266.23)
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Publication number: 20130158003Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.Type: ApplicationFiled: May 26, 2011Publication date: June 20, 2013Applicant: SUNOVION PHARMACEUTICALS INCInventors: John Emmerson Campbell, Michael Charles Hewitt, Philip Jones, Linghong Xie
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Publication number: 20130143871Abstract: Aminoquinazolinyl compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.Type: ApplicationFiled: August 12, 2011Publication date: June 6, 2013Inventors: Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
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Publication number: 20130137658Abstract: A plant disease controlling composition is provided containing a pyridazine compound represented by formula (I): wherein R1 represents a chlorine atom, a bromine atom, a cyano group or a methyl group, and R2 represents a hydrogen atom or a fluorine atom; and at least one azole compound selected from the group consisting of propiconazole, prothioconazole, triadimenol, prochloraz, penconazole, tebuconazole, flusilazole, diniconazole, bromuconazole, epoxiconazole, difenoconazole, cyproconazole, metconazole, triflumizole, tetraconazole, myclobutanil, fenbuconazole, hexaconazole, fluquinconazole, triticonazole, bitertanol, imazalil, ipconazole, simeconazole, and flutriafol.Type: ApplicationFiled: August 9, 2011Publication date: May 30, 2013Applicant: Sumitomo Chemical Company, LimitedInventor: Yuichi Matsuzaki
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Publication number: 20130131047Abstract: The present invention relates to inhibitors of ROCK1 and ROCK2 and methods of modulating the pharmacokinetic and/or pharmacodynamic properties of such compounds. Also provided are methods of inhibiting ROCK1 and or ROCK2 that are useful for the treatment of disease.Type: ApplicationFiled: December 14, 2012Publication date: May 23, 2013Applicant: SURFACE LOGIX, INC.Inventor: SURFACE LOGIX, INC.
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Publication number: 20130130898Abstract: The present invention relates to compositions of fungicidally active compounds comprising at least one active compound I selected from 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid (3?,4?,5?-trifluoro-biphenyl-2-yl)-amide (fluxapyroxade), bixafen, fluopyram, isopyrazam, sedaxane, penflufen and penthiopyrad and at least one further active component II as defined below.Type: ApplicationFiled: August 2, 2011Publication date: May 23, 2013Inventors: Markus Gewehr, Jochen Dietz, Egon Haden
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Publication number: 20130123244Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.Type: ApplicationFiled: July 26, 2011Publication date: May 16, 2013Applicant: JANSSEN R&D IRELANDInventors: Koen Vandyck, Wim Gaston Verschueren, Pierre Jean-Marie Bernard Raboisson
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Publication number: 20130123284Abstract: Provided herein are compounds useful for kinase inhibition.Type: ApplicationFiled: March 24, 2011Publication date: May 16, 2013Applicant: AMITECH THERAPEUTIC SOLUTIONS INCInventors: Lee Daniel Arnold, Eric A. Murphy
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Patent number: 8436005Abstract: Macrocyclic pyrimidine compounds, compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions, and disorders using such compounds and compositions are described herein.Type: GrantFiled: March 27, 2009Date of Patent: May 7, 2013Assignee: Abbott LaboratoriesInventors: Huaqing Liu, Irene Drizin, John R. Koenig, Marlon D. Cowart, Chen Zhao, Brian D. Wakefield, Lawrence A. Black, Robert J. Altenbach
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Publication number: 20130109706Abstract: Quinazoline derivatives are provided that specifically inhibit proliferation of T cells without affecting the level of IL-2 secreted from said T cells. These compounds as well as pharmaceutical composition comprising them are useful for the treatment of indications mediated by T cell proliferation.Type: ApplicationFiled: January 27, 2011Publication date: May 2, 2013Applicant: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERSALEM LTD.Inventors: Alexander Levitzki, Idit Sagiv
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Publication number: 20130096101Abstract: Provided herein are compounds, pharmaceutical compositions, and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: December 4, 2012Publication date: April 18, 2013Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventor: PRESIDIO PHARMACEUTICALS, INC.
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Publication number: 20130090346Abstract: The invention concerns the use of competitive AMPA receptor antagonists for the treatment or prevention of photosensitive epilepsy.Type: ApplicationFiled: September 5, 2012Publication date: April 11, 2013Inventors: Donald Johns, Georges Imbert, Klaus Kucher
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N3-HETEROARYL SUBSTITUTED TRIAZOLES AND N5-HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS
Publication number: 20130090330Abstract: N3-Heteroaryl substituted triazoles and N5-heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: October 4, 2012Publication date: April 11, 2013Applicant: RIGEL PHARMACEUTICALS, INC.Inventor: RIGEL PHARMACEUTICALS, INC. -
Patent number: 8410120Abstract: A compound in combination with a pharmaceutically acceptable carrier, the compound having a formula: wherein: R1 is a member of the group consisting of hydrogen, halogen, nitro, benzo, lower alkyl, phenyl, and lower alkoxy; R2 is a member of the group consisting of hydroxy, acetoxy, and lower alkoxy; and R3 is a member of the group consisting of hydrogen and lower alkenoxy-carbonyl; and n is either 1 or 2; and pharmaceutically acceptable salts thereof; for use in treatment of or prevention of skeletal muscle fibrosis and/or for inducing skeletal muscle regeneration.Type: GrantFiled: January 21, 2008Date of Patent: April 2, 2013Inventors: Mark Pines, Arnon Nagler
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Publication number: 20130072477Abstract: The present invention relates to a therapeutic or prophylactic method for treating Parkinson's disease by administering an effective amount of a compound having a phosphodiesterase 10 inhibitory activity; and also relates to a pharmaceutical composition for treatment or prophylaxis of Parkinson's disease comprising as an active ingredient a compound having a phosphodiesterase 10 inhibitory activity. Moreover, the present invention relates to a method for enhancing dopamine signal in the brain, which comprises administering an effective amount of a compound having a phosphodiesterase 10 inhibitory activity; and also relates to pharmaceutical composition for enhancing dopamine signal in brain comprising as an active ingredient a compound having a phosphodiesterase 10 inhibitory activity.Type: ApplicationFiled: November 16, 2012Publication date: March 21, 2013Applicant: MITSUBISHI TANABE PHARMA COPORATIONInventor: MITSUBISHI TANABE PHARMA COPORATION
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Publication number: 20130064835Abstract: A method is provided for treating a RAGE-related disorder in a subject afflicted therewith comprising administering to the subject a therapeutically effective amount of an antagonist of rho-associated protein kinase 1 (ROCK1) so as to thereby treat the RAGE-related disorder. A method is also provided for treating a ROCK1-related disorder in a subject afflicted therewith comprising administering to the subject therapeutically effective amount of antagonist of receptor for advanced glycation end products (RAGE) so as to thereby treat the ROCK-related disorder.Type: ApplicationFiled: October 8, 2010Publication date: March 14, 2013Inventor: Ann Marie Schmidt
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Publication number: 20130065854Abstract: A composition comprising a carboxamide compound represented by following formula (I), wherein R1 represents a hydrogen atom or a methyl group, and R2 represents a methyl group, a difluoromethyl group or a trifluoromethyl group, and one or more azole compounds selected from group (A) consisting of propiconazole, prothioconazole, triadimenol, prochloraz, penconazole, tebuconazole, flusilazole, diniconazole, bromuconazole, epoxiconazole, difenoconazole, cyproconazole, metconazole, triflumizole, tetraconazole, myclobutanil, fenbuconazole, hexaconazole, fluquinconazole, triticonazole, bitertanol, imazalil, ipconazole, simeconazole, hymexazol, etridiazole and flutriafol.Type: ApplicationFiled: April 25, 2011Publication date: March 14, 2013Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: Yuichi Matsuzaki
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Publication number: 20130053381Abstract: The invention relates to a 2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl-sulfonamide derivative being (A) a compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; or (B) a compound selected from a certain group of 2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl-sulfonamide derivatives disclosed in the specification; in free form or in salt form; to their preparation, to their use as medicament and to medicaments comprising them. In a first aspect, the invention provides prodrugs of AMPA receptor antagonists which potentially useful in the treatment of a wide range of disorders, particularly epilepsy.Type: ApplicationFiled: May 18, 2011Publication date: February 28, 2013Inventors: Yves Auberson, David Carcache, Andreas Lerchner, Joachim Nozulak
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Publication number: 20130053362Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.Type: ApplicationFiled: July 18, 2012Publication date: February 28, 2013Applicants: INTELLKINE, LLC, INFINITY PHARMACEUTICALS, INC.Inventors: Alfredo C. CASTRO, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Daniel A. SNYDER, Martin R. TREMBLAY, Pingda REN, Yi LIU, Liansheng LI, Katrina CHAN
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Publication number: 20130029942Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof that are effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: ApplicationFiled: October 4, 2012Publication date: January 31, 2013Applicant: Myrexis, Inc.Inventor: Myrexis, Inc.
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Patent number: 8362065Abstract: Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are useful as kinase modulators, including Btk modulation.Type: GrantFiled: November 9, 2011Date of Patent: January 29, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Qingjie Liu, Douglas G. Batt, George V. DeLucca, Qing Shi, Andrew J. Tebben
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Patent number: 8357693Abstract: The present invention relates to inhibitors of ROCK1 and ROCK2 and methods of modulating the pharmacokinetic and/or pharmacodynamic properties of such compounds. Also provided are methods of inhibiting ROCK1 and or ROCK2 that are useful for the treatment of disease.Type: GrantFiled: March 27, 2006Date of Patent: January 22, 2013Assignee: Surface Logix, Inc.Inventors: Alessandra Bartolozzi, Stewart Campbell, Hope Foudoulakis, Brian Kirk, Siya Ram, Paul Sweetnam
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Publication number: 20130012503Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: June 20, 2012Publication date: January 10, 2013Applicant: VIAMET PHARMACEUTICALS, INC.Inventors: William J. Hoekstra, Robert J. Schotzinger, Gary D. Gustafson
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Patent number: 8349857Abstract: A compound which inhibits both of EGF receptor tyrosine kinase and HER2 tyrosine kinase is provided. A compound represented by the general formula (I): wherein RX is a group represented by the formula: wherein R1 is a hydrogen atom, optionally substituted alkyl, etc.; Z is —O—, —N(R10)—, etc.; R10 is a hydrogen atom, alkyl, etc.; R2 is a hydrogen atom, optionally substituted alkyl, etc.; R18 is a hydrogen atom, optionally substituted alkyl, etc.; R19 is optionally substituted alkyl, etc.; W1 is an optionally substituted non-aromatic nitrogen-containing group; R17 is a hydrogen atom, optionally substituted alkyl, etc.; R3 and R4 are independently a hydrogen atom, optionally substituted alkyl, etc.; X is —O—, —S—, or —N(R12)—, etc.; R12 is a hydrogen atom, alkyl, etc.; and A is phenyl optionally having a substituent, etc., its pharmaceutically acceptable salt, or a solvate thereof.Type: GrantFiled: January 26, 2012Date of Patent: January 8, 2013Assignee: Shionogi & Co., Ltd.Inventors: Masaharu Kume, Kenji Matsuo, Naoki Omori, Masami Takayama, Aiko Omori, Takeshi Endo
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Patent number: 8349851Abstract: Provided herein are quinazoline compounds of formula (I): The compounds are useful for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: GrantFiled: February 26, 2010Date of Patent: January 8, 2013Assignee: Ambit Biosciences Corp.Inventors: Sunny Abraham, Qi Chao, Michael J. Hadd, Mark W. Holladay, Gang Liu, Eduardo Setti
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Publication number: 20130005719Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: June 19, 2012Publication date: January 3, 2013Applicant: Viamet Pharmaceuticals, Inc.Inventors: William J. Hoekstra, Stephen W. Rafferty, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Michael T. Sullenberger, Gary D. Gustafson
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Publication number: 20120329788Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: June 19, 2012Publication date: December 27, 2012Applicant: Viamet Pharmaceuticals, Inc.Inventors: William J. Hoekstra, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Zachary A. Buchan, Michael T. Sullenberger, Gary D. Gustafson
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Publication number: 20120316151Abstract: This invention relates to the use of triazolone derivatives of Formula (I) for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones in the treatment of cancer.Type: ApplicationFiled: February 22, 2011Publication date: December 13, 2012Inventors: Nicholas D. Adams, Christopher Joseph Aquino, Amita M. Chaudhari, Jonathan M. Ghergurovich, Terence John Kiesow, Cynthia A. Parrish, Alexander Joseph Reif, Kenneth Wiggall
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Publication number: 20120316136Abstract: The present patent application relates to treatment of a respiratory disorder using TRPA1 antagonists. Particularly, the present patent application relates to treatment of a respiratory disorder using a TRPA1 antagonist, wherein the TRPA1 antagonist is administered by inhalation route to a subject in need thereof.Type: ApplicationFiled: June 13, 2012Publication date: December 13, 2012Applicant: GLENMARK PHARMACEUTICALS S.A.Inventors: Neelima KHAIRATKAR-JOSHI, Abhay KULKARNI, Indranil MUKHOPADHYAY, Vidya Ganapati KATTIGE, Vikram Mansingh BHOSALE, Dinesh Pradeep WALE, Abraham THOMAS, Sukeerthi KUMAR, Sachin Sundarlal CHAUDHARI
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Publication number: 20120282345Abstract: The present invention relates to a pesticide composition intended for protecting plants, crops or seeds against phyto-pathogenic fungi or damaging insects, and the corresponding methods of treatment using the said composition. More precisely, the subject of the present invention is a pesticide composition based on propamocarb-HCl, an insecticide active substance and optionally a further fungicide active substance.Type: ApplicationFiled: June 5, 2012Publication date: November 8, 2012Applicant: Bayer Intellectual Property GMBHInventors: Koen Van Den Eynde, Wolfgang Thielert, Heike Hungenberg
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Publication number: 20120283280Abstract: A series of new chemical agents that demonstrate anti-tumor activity are described herein. The new chemical agents exhibit a dual mode of anti-tumor action: blocking epidermal growth factor receptor (EGFR) mediated signal transduction and damaging DNA by alkylation.Type: ApplicationFiled: April 18, 2012Publication date: November 8, 2012Inventor: Bertrand Jean-Claude
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Publication number: 20120270858Abstract: The invention provides isoquinoline, quinoline, and quinazoline derivatives to treat a variety of disorders, diseases and pathologic conditions, and more specifically to the use of isoquinoline, quinoline, and quinazoline derivatives to inhibit the hedgehog signaling pathway and to the use of those compounds to the treatment of hyperproliferative diseases and pathologic angiogenesis.Type: ApplicationFiled: June 9, 2010Publication date: October 25, 2012Applicant: CALIFORNIA CAPITAL EQUITY, LLCInventors: Chunlin Tao, Xiaowen Sun, Hongna Han, Lukasz Koroniak, Neil Desai
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Publication number: 20120270856Abstract: Disclosed are compounds of the following formula and their pharmaceutically-acceptable salts, which have an effect of glucokinase activation and are useful in the field of medicines for treatment for diabetes, obesity, etc. (wherein ring A represents a pyrazolyl group optionally having a lower alkyl group, etc.; ring B represents a heteroaryl group; R represents a lower alkyl group, etc.; R1 represents a group of a formula: (wherein R11 and R12 each independently represent a hydrogen atom, etc.; m indicates an integer of from 2 to 6), etc.; R2 represents a lower alkyl group, etc.; r indicates an integer of from 0 to 3; k indicates an integer of from 0 to 4).Type: ApplicationFiled: July 2, 2012Publication date: October 25, 2012Inventors: Tomoharu IINO, Akio OHNO, Norikazu OTAKE, Takuya SUGA, Masanori ASAI
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Publication number: 20120263791Abstract: The present invention relates to pharmaceutical formulations comprising a 1H-quinazoline-2,4-dione AMPA receptor antagonist. More particularly, the invention relates to immediate release formulations comprising such a compound.Type: ApplicationFiled: December 21, 2010Publication date: October 18, 2012Applicant: NOVARTIS AGInventors: Joseph L. Zielinski, John Vrettos, Qin Ji, Subash Patel
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Patent number: 8288426Abstract: A composition comprising fenamidone (a) and an insecticide compound (b) in a (a)/(b) weight ratio of from 1/1000 to 1000/1. A composition further comprising an additional fungicidal compound. A method for preventively or curatively combating the pests and diseases of crops by using this composition.Type: GrantFiled: December 21, 2007Date of Patent: October 16, 2012Assignee: Bayer CropScience AGInventors: Heike Hungenberg, Wolfgang Thielert, Koen Van Den Eynde
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Patent number: 8278300Abstract: The present invention is concerned with the use of PDE5 inhibitors in medicine.Type: GrantFiled: January 4, 2010Date of Patent: October 2, 2012Assignee: Nycomed GmbHInventors: Torsten Dunkern, Christian Schudt, Friedrich Grimminger, Hossein Ardeschir Ghofrani, Manfred Kaps, Bernhard Rosengarten
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Publication number: 20120245139Abstract: The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.Type: ApplicationFiled: June 4, 2012Publication date: September 27, 2012Applicant: EXELIXIS PATENT COMPANY LLCInventors: Suleyman Bahceci, William Bajjalieh, Jeff Chen, Sergey Epshteyn, Timothy Patrick Forsyth, Tai Phat Huynh, Byung Gyu Kim, James W. Leahy, Matthew Sangyup Lee, Gary L. Lewis, Morrison B. Mac, Grace Mann, Charles K. Marlowe, Brian Hugh Ridgway, Joan C. Sangalang, Xian Shi, Craig Stacy Takeuchi, Yong Wang
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Patent number: 8273740Abstract: The invention relates to 2-sulfanyl-benzoimidazol-1-yl-acetic acid derivatives and their use as potent “chemoattractant receptor-homologous molecule expressed on Th2 cells” antagonists in the treatment of prostaglandin mediated diseases, to pharmaceutical compositions containing these derivatives and to processes for their preparation.Type: GrantFiled: August 23, 2005Date of Patent: September 25, 2012Assignee: Actelion Pharmaceuticals, Ltd.Inventors: Heinz Fretz, Markus Gude, Kurt Hilpert, Julien Pothier, Markus Riederer, Matthias Steger
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Publication number: 20120238570Abstract: The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.Type: ApplicationFiled: June 4, 2012Publication date: September 20, 2012Applicant: EXELIXIS PATENT COMPANY LLCInventors: Suleyman Bahceci, William Bajjalieh, Jeff Chen, Sergey Epshteyn, Timothy Patrick Forsyth, Tai Phat Huynh, Byung Gyu Kim, James W. Leahy, Matthew Sangyup Lee, Gary L. Lewis, Morrison B. Mac, Grace Mann, Charles K. Marlowe, Brian Hugh Ridgway, Joan C. Sangalang, Xian Shi, Craig Stacy Takeuchi, Yong Wang
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Publication number: 20120238582Abstract: Novel quinazolinamide derivatives of the formula (I), in which R1-R4 and X have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: ApplicationFiled: October 26, 2010Publication date: September 20, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER hAFTUNGInventors: Hans Michael Eggenweiler, Christian Sirrenberg, Hans Peter Buchstaller
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Patent number: 8268857Abstract: This invention provides compounds that are useful for treating patients having a TGF-?-mediated disease, particularly an ALK5-mediated disease. The compounds are represented by formula I: wherein: a-b is CH2CH2, CH2CH2CH2, CH?CH, CH?N, or N?CH; Z is N or C—F; and G is C1-6 aliphatic or a phenyl, naphthyl, or 5-6 membered heteroaryl ring.Type: GrantFiled: January 16, 2007Date of Patent: September 18, 2012Assignee: Millennium Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Anjali Pandey, Meenakshi S. Venkatraman
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Patent number: 8268841Abstract: Quinazoline derivatives of formula (I): wherein A is 5-membered heteroaryl containing a nitrogen atom and one or two further nitrogen atoms; compositions containing them, processes for their preparation and their use in therapy.Type: GrantFiled: April 28, 2009Date of Patent: September 18, 2012Assignee: Astrazeneca ABInventors: Nicola Murdoch Heron, Andrew Austen Mortlock, Frederic Henri Jung, Georges Rene Pasquet
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Patent number: 8252806Abstract: This invention relates to novel potassium channel modulating agents, and their use in the preparation of pharmaceutical compositions.Type: GrantFiled: March 13, 2006Date of Patent: August 28, 2012Assignee: Neurosearch A/SInventors: Birgitte L. Eriksen, Lene Teuber, Charlotte Hougaard, Ulrik Svane Sørensen
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Publication number: 20120208812Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.Type: ApplicationFiled: October 21, 2010Publication date: August 16, 2012Applicant: Janssen Pharmaceutica N.V.Inventors: Wenying Chai, Michael A. Letavic, Kiev S. Ly, Daniel J. Pippel, Dale A. Rudolph, Kathleen C. Sappey, Brad M. Savall, Chandravadan R. Shah, Brock T. Shireman, Akinola Soyode-Johnson, Emily M. Stocking, Devin M. Swanson
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Publication number: 20120208827Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of benzimidazoles in the treatment of cancer.Type: ApplicationFiled: October 27, 2010Publication date: August 16, 2012Inventors: Steven Dock, Jason Hallman, Christopher Laudeman, Ronggang Liu, Aaron Miller, Michael Lee Moore, David Musso, Cynthia Parrish
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Publication number: 20120202793Abstract: The present invention relates to inhibitors of ROCK1 and ROCK2, which may be selective for ROCK2, and methods of modulating the pharmacokinetic and/or pharmacodynamic properties of such compounds. Also provided are methods of inhibiting ROCK1 and/or ROCK2. Also provided are treatments combining inhibitors of ROCK1 and/or ROCK2 with statins.Type: ApplicationFiled: March 9, 2010Publication date: August 9, 2012Inventors: Paul Sweetnam, Alessandra Bartolozzi, Anthony Stewart Campbell, Bridget Cole, Hope Foudoulakis, Brian Kirk, Hemalatha Seshadri, Siya Ram
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Patent number: 8232285Abstract: The present invention relates to quinazolinone compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the quinazolinone compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a quinazolinone compound of the present invention.Type: GrantFiled: June 19, 2008Date of Patent: July 31, 2012Assignee: ArQule, Inc.Inventors: Jifeng Liu, Syed M. Ali, Mark A. Ashwell, Ping Ye, Yousheng Guan, Shi-Chung Ng, Rocio Palma, Dan Yohannes
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Publication number: 20120184518Abstract: Methods for the treatment and/or prevention of an inflammatory disease or disorder through administration of an inhibitor of a glutaminyl peptide cyclotransferase. Inflammatory diseases or disorders treated or prevented by methods disclosed herein include mild cognitive impairment (MCI), rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis, sepsis and peritonitus. Further provided are respective diagnostic methods, assays and kits.Type: ApplicationFiled: January 20, 2012Publication date: July 19, 2012Applicant: PROBIODRUG AGInventors: Stephan Schilling, Holger Cynis, Torsten Hoffman, Hans-Ulrich Demuth
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Publication number: 20120178622Abstract: The invention relates to aminoquinazoline compounds or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein A1, A2, A3, A4, R1, R2, R3, R4, R5a, R5b, R5c, R5d and p are defined as in the description.Type: ApplicationFiled: September 15, 2010Publication date: July 12, 2012Applicant: BASF SEInventors: Steffen Gross, Matthias Pohlman, Arun Narine, Claudia Rosenbaum, Prashant Deshmukh, Joachim Dickhaut, Nina Gertrud Bandur, Karsten Koerber, Florian Kaiser, Wolfgang Von Deyn, Juergen Langewald, Deborah L. Culbertson, Cecille Ebuenga
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Patent number: 8216971Abstract: The present invention relates to a pesticide composition intended for protecting plants, crops or seeds against phyto-pathogenic fungi or damaging insects, and the corresponding methods of treatment using the said composition. More precisely, the subject of the present invention is a pesticide composition based on propamocarb-HCl, an insecticide active substance and optionally a further fungicide active substance.Type: GrantFiled: December 21, 2007Date of Patent: July 10, 2012Assignee: Bayer Intellectual Property GmbHInventors: Koen van Den Eynde, Wolfgang Thielert, Heike Hungenberg
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Publication number: 20120171183Abstract: This invention provides a composition comprising a biologically effective amount of a compound of Formula 1, an N-oxide or an agriculturally suitable salt thereof wherein R1, R2, R3, R4a, R4b and R5 are as defined in the disclosure, and an effective amount of at least one fungicide.Type: ApplicationFiled: March 6, 2012Publication date: July 5, 2012Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventors: George Philip Lahm, Thomas Paul Selby, Thomas Martin Stevenson