The Five-membered Hetero Ring Has At Least Oxygen And Nitrogen As Ring Hetero Atoms Patents (Class 544/137)
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Publication number: 20130231340Abstract: The invention provides a method of inhibiting a TYK2 kinase, which method comprises bringing into contact with the TYK2 kinase an effective TYK2 kinase-inhibiting amount of a compound having the formula (0): or a salt or stereoisomer thereof. The invention also provides a novel subset of compounds within formula (0) as well as pharmaceutical compositions containing them and their use in medicine.Type: ApplicationFiled: March 1, 2013Publication date: September 5, 2013Applicant: SAREUM LIMITEDInventor: John Charles READER
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Publication number: 20130225586Abstract: The present invention provides a compound having Formula I or II: wherein B, R, X, Ar, and Y are defined herein, pharmaceutically acceptable salts thereof and pharmaceutically acceptable prodrugs thereof. The present invention also provides methods of making and using the compound.Type: ApplicationFiled: September 25, 2012Publication date: August 29, 2013Applicant: CPSI STOCKHOLDER TRUSTInventor: CPSI Stockholder Trust
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Publication number: 20130210769Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1).Type: ApplicationFiled: March 15, 2013Publication date: August 15, 2013Applicant: IRM LLCInventors: Hong Liu, Xiaohui He, Dean Paul Phillips, Xuefeng Zhu, Kunyong Yang, Thomas Lau, Baogen Wu, Yongping Xie, Truc Ngoc Nguyen, Xing Wang
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Patent number: 8507480Abstract: Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C?O)—, —(C?S)—, —SO.sub.Type: GrantFiled: February 19, 2010Date of Patent: August 13, 2013Assignees: Vernalis (R&D) Limited, Cancer Research Technology Limited, The Institute of Cancer ResearchInventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
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Publication number: 20130196990Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3? OH kinase family (hereinafter PI3 kinases), suitably, PI3K?, PI3K?, PI3K?, and/or PI3K?. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3K? selective benzimidazoles compounds for treating cancer.Type: ApplicationFiled: September 23, 2011Publication date: August 1, 2013Inventors: Junya Qu, Ralph A. Rivero, Robert Sanchez, Rosanna Tedesco
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Publication number: 20130196984Abstract: The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.Type: ApplicationFiled: March 13, 2013Publication date: August 1, 2013Applicants: Siena Biotech S.p.A., Hoffmann-La Roche Inc.Inventors: Hoffmann-La Roche Inc., Siena Biotech S.p.A.
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Publication number: 20130196996Abstract: One embodiment provides a method, comprising treating or preventing at least one disease selected from the group consisting of bladder cancer, weight loss accompanying bladder cancer, bone pain accompanying bladder cancer, bladder cancer carcinoma in-situ (CIS), TA stage bladder cancer, T1 stage bladder cancer, T2 stage bladder cancer, T3 stage bladder cancer, T4 stage bladder cancer, lymph node metastasis therefrom, solid organ metastasis therefrom, bony metastasis therefrom, cachexia/anorexia associated with bladder cancer, generalized wasting syndrome associated with bladder cancer, or a combination thereof, by administering to a subject in need thereof one or more compounds described herein, prodrug thereof, salt thereof, or a combination thereof.Type: ApplicationFiled: January 19, 2011Publication date: August 1, 2013Applicant: CPSI STOCKHOLDER TRUSTInventors: John Arthur Taylor, III, Thais Sielecki-Dzurdz
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Publication number: 20130184457Abstract: The present invention relates to the use of a compound having the formula (II) for the preparation of a compound having the formula (V). Methods of preparing the compound having the formula (V) using the compound having the formula (II) are also described. Individual reaction steps as well as intermediates are additionally claimed.Type: ApplicationFiled: February 10, 2011Publication date: July 18, 2013Applicant: SANDOZ AGInventors: Hubert Sturm, Dominic De Souza, Kerstin Knepper, Martin Albert
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Patent number: 8487095Abstract: The present invention relates to new salt forms of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide, in particular the mesylate, hydrochloride, tartrate, phosphate and hemi fumarate salt thereof; to crystalline forms of such salts; to polymorphs of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide; to hydrates and polymorphs of the new salt forms mentioned above; to the use of the new salt forms mentioned above for the manufacture of a medicament for the treatment of a disorder mediated by Hsp90; to a method for treating a disorder mediated by Hsp90 using the new salt forms; to formulations comprising such salt forms, in particular aqueous solutions suitable for intravenous administration; and to amber glass containers being filled with such formulations.Type: GrantFiled: March 8, 2012Date of Patent: July 16, 2013Assignees: Novartis AGInventors: Martin James Drysdale, Brian William Dymock, Christoph Krell, Michael Mutz, Holger Petersen, Weijia Zheng
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Patent number: 8481532Abstract: 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: GrantFiled: July 9, 2009Date of Patent: July 9, 2013Assignee: EnVivo Pharmaceuticals, Inc.Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Publication number: 20130172553Abstract: Processes for the chiral syntheses of isoxazolines and intermediates are described. Compounds prepared thereby, and methods of using the compounds are also described.Type: ApplicationFiled: November 26, 2010Publication date: July 4, 2013Applicant: CPSI STOCKHOLDER TRUSTInventors: Thais Sielecki-Dzurdz, James Pruitt
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Publication number: 20130172554Abstract: The present invention provides processes for the preparation of 4-{4-[5(S)-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl}morpholin-3-one which are simple, eco-friendly, cost-effective, reproducible, robust and are well amenable on industrial scale.Type: ApplicationFiled: August 1, 2011Publication date: July 4, 2013Applicant: SYMED LABS LIMITEDInventors: Dodda Mohan Rao, Pingili Krishna Reddy, Ambati Anna Reddy, Buthukuri Venkat Reddy
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Patent number: 8470821Abstract: Compounds active on phosphodiesterase PDE4B are provided. Also provided herewith are compositions useful for treatment of PDE4B-mediated diseases or conditions, and methods for the use thereof.Type: GrantFiled: July 20, 2009Date of Patent: June 25, 2013Assignee: Plexxikon Inc.Inventors: Prabha N. Ibrahim, Hanna Cho, Bruce England, Sam Gillette, Dean R. Artis, Rebecca Zuckerman, Chao Zhang
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Publication number: 20130137864Abstract: The present invention provides an improved process for the preparation of Linezolid of formula (D. The present invention relates to preparation of intermediate (R)—N-[[3-[3-fluoro-4-morpholinyl]phenyl|-2-oxo-5-oxazolidinyl]methanol of formula (II), Linezolid amine of formula (Ia) and their use in the preparation of Linezolid. The present invention further provides process for the preparation of Form I of Linezolid of formula (I).Type: ApplicationFiled: December 9, 2010Publication date: May 30, 2013Inventors: Jayaraman Venkat Raman, Dhiraj Rathod, Irfan Vohra, Mangesh Chavan, Manoj Ahirrao, Ravi Ponnaiah
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Patent number: 8450310Abstract: Isoxazoles of formula (A) or (B) wherein R1 is a group of formula (IB) The isoxazoles are inhibitors of HSP90 activity, and useful for the treatment of, for example, cancers.Type: GrantFiled: June 18, 2012Date of Patent: May 28, 2013Assignees: Vernalis (R&D) Limited, Cancer Research Technology Ltd., The Institute of Cancer ResearchInventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
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Patent number: 8445480Abstract: Compounds having the structure of Formula I1 including pharmaceutically acceptable salts of the compounds, are potent CETP (cholesterol ester transfer protein) inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis Atherosclerosis and its clinical consequences, coronary heart disease (CHD), stroke and penpheral vascular disease, represent a truly enormous burden to the health care systems of the industrialized world In formula I, A-B is an arylamide moiety.Type: GrantFiled: June 16, 2008Date of Patent: May 21, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Julianne A. Hunt, Ramzi F. Sweis, Dooseop Kim, Florida Kallashi, Peter J. Sinclair
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Publication number: 20130123243Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.Type: ApplicationFiled: October 18, 2012Publication date: May 16, 2013Inventor: Celtaxsys, Inc.
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Patent number: 8435989Abstract: Provided are process for the preparation of (R)- and/or (S)-Rivaroxaban, and compounds which are intermediate compounds used in the processes for the preparation of (R)- and/or (S)-Rivaroxaban.Type: GrantFiled: November 12, 2012Date of Patent: May 7, 2013Inventors: Prabhudas Bodhuri, Gamini Weeratunga
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Publication number: 20130102592Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted en by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.Type: ApplicationFiled: December 5, 2012Publication date: April 25, 2013Applicant: SAREUM LIMITEDInventor: Sareum Limited
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Publication number: 20130102462Abstract: The present invention relates to a process for producing aromatic carbonyl compounds of formula I and aromatic imine compounds of formula III comprising the step of reacting a (hetero)aromatic halogen or sulfonate compound II wherein the variables are as defined in the claims and description, with a mixture of carbon monoxide and hydrogen in the presence of a transition metal complex catalyst. The invention also relates to specific compounds III, to compositions comprising them and to their use for combating invertebrate pests.Type: ApplicationFiled: June 22, 2011Publication date: April 25, 2013Applicant: BASF SEInventors: Karsten Koerber, Florian Kaiser, Christian Rein, Joachim Schmidt-Leithoff, Wolfgang Von Deyn, Prashant Deshmukh, Arun Narine, Joachim Dickhaut, Nina Gertrud Bandur, Juergen Langewald
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Publication number: 20130096124Abstract: The present invention relates to new isoxazoline compounds of formula wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful in the control of parasites, in particular ectoparasites, in and on vertebrates.Type: ApplicationFiled: June 11, 2011Publication date: April 18, 2013Inventors: Steve Nanchen, Noelle Gauvry, Thomas Goebel
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Publication number: 20130096117Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): And salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.Type: ApplicationFiled: October 2, 2012Publication date: April 18, 2013Inventors: Julie Nicole HAMBLIN, Paul Spencer JONES, Suzanne Elaine KEELING, Joelle LE, Nigel James PARR
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Publication number: 20130079339Abstract: The invention discloses compounds of formula I wherein Y is a group of formula A, B, C, D, or E: and W, Q, n, R1, R2, R3, U1-U5, J and K have the meanings given in the description. The compounds of formula I are TRPV1 antagonists and are useful as active ingredients of pharmaceutical compositions for the treatment of pain and other conditions ameliorated by the inhibition of the vanilloid receptor TRPV1.Type: ApplicationFiled: December 22, 2010Publication date: March 28, 2013Applicant: PHARMESTE S.R.L.Inventors: Mauro Napoletano, Marcello Trevisani, Maria Giovanna Pavani, Francesca Fruttarolo
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Publication number: 20130072680Abstract: Provided are process for the preparation of (R)- and/or (S)-Rivaroxaban, and compounds which are intermediate compounds used in the processes for the preparation of (R)- and/or (S)-Rivaroxaban.Type: ApplicationFiled: November 12, 2012Publication date: March 21, 2013Applicant: Apotex Pharmachem Inc.Inventor: Apotex Pharmachem Inc.
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Publication number: 20130059852Abstract: Some embodiments of this invention include methods for treating disease and methods for administering a compound of Formula (I). In some aspects of the invention, diseases can be treated by administration of compositions comprising a compound of Formula (I). Pharmaceutical compositions of some embodiments of the present invention comprise a compound of Formula (I).Type: ApplicationFiled: April 8, 2011Publication date: March 7, 2013Applicant: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.Inventors: John O. Trent, Jason B. Meier, Kelby B. Napier
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Publication number: 20130059833Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R5, W, X, X1, Y, Y1, Z and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used in the treatment of CNS disorders such as schizophrenia, Alzheimer's disease, and Parkinson's disease.Type: ApplicationFiled: August 30, 2012Publication date: March 7, 2013Inventors: Stephan Bachmann, Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Markus Rudolph
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Publication number: 20130053557Abstract: Processes and intermediates for preparing linezolid, and pharmaceutically acceptable salts thereof, are described herein.Type: ApplicationFiled: April 28, 2011Publication date: February 28, 2013Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATIONInventor: James R. McCarthy
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Patent number: 8383616Abstract: The present invention relates to formula I compounds having antitumoural activities through, as one possible biological target, the molecular chaperone heat shock protein 90 (Hsp90) inhibition. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of Hsp90 is responsive, and the pharmaceutical compositions containing such compounds.Type: GrantFiled: June 30, 2009Date of Patent: February 26, 2013Assignee: Sigma-Tau Industrie Farmaceutiche Riunite SpAInventors: Giuseppe Giannini, Walter Cabri, Daniele Simoni, Riccardo Baruchello, Claudio Pisano, Gabriella Singrossi, Silvia Carminati, Giuseppe Paolo Carminati
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Patent number: 8378095Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.Type: GrantFiled: May 9, 2008Date of Patent: February 19, 2013Assignee: Saruem LimitedInventors: John Charles Reader, John Mark Ellard, Michael Cherry
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Patent number: 8372984Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: July 14, 2010Date of Patent: February 12, 2013Assignee: Theravance, Inc.Inventors: Paul R. Fatheree, Ryan Hudson, Robert Murray McKinnell
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Publication number: 20130029966Abstract: The invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R1, R2, A, B, and Y are defined as in Claim 1. The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases.Type: ApplicationFiled: September 23, 2011Publication date: January 31, 2013Applicant: Abbott GmbH & Co. KGInventors: Thorsten Oost, Wilfried Lubisch, Wilfried Hornberger, Liliane Unger, Herve Geneste, Astrid Netz
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Patent number: 8362015Abstract: The present application relates to prodrug derivatives of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of thromboembolic disorders.Type: GrantFiled: August 23, 2007Date of Patent: January 29, 2013Assignee: Bayer Intellectual Property GmbHInventors: Hans-Georg Lerchen, Ursula Krenz, Karl-Heinz Schlemmer, Elisabeth Perzborn
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Publication number: 20130018048Abstract: The present invention is directed to certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.Type: ApplicationFiled: April 4, 2011Publication date: January 17, 2013Applicant: Merck Sharp & Dohme Corp.Inventors: ZhiQiang Yang, Philippe G. Nantermet, Constantine Kreatsoulas, Keith P. Moore, Evan Foster Shalen
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Patent number: 8354400Abstract: The present invention provides benzoxazole compounds and pharmaceutically acceptable salts thereof and pharmaceutical compositions including the same. The present invention further provides methods of use as described herein.Type: GrantFiled: September 25, 2009Date of Patent: January 15, 2013Assignee: Eisai R&D Co., Ltd.Inventors: Wanjun Zheng, Mark Spyvee, Fabian Gusovsky, Sally T. Ishizaka
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Publication number: 20130005701Abstract: The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.Type: ApplicationFiled: January 27, 2012Publication date: January 3, 2013Applicant: Bayer Pharma AktiengesellschaftInventors: Alexander Straub, Thomas Lampe, Jens Pohlmann, Susanne Röhrig, Elisabeth Perzborn, Karl-Heinz Schlemmer, Joseph Pernerstorfer
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Publication number: 20130005730Abstract: The present invention relates to certain novel 1,3-oxazolidine compounds of formula (I), to processes for making such compounds and to their utility as renin inhibitors or prodrugs of renin inhibitors.Type: ApplicationFiled: October 29, 2010Publication date: January 3, 2013Inventors: Piaoyang Sun, Mikhajlovich Antonov Dmitry, Xiao Xiong Zhou
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Publication number: 20120316124Abstract: The present invention relates to compounds formula (I), wherein P is P1, P2, heterocyclyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5, R6, R17, R18, R19 and R20 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: February 17, 2011Publication date: December 13, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Thomas Pitterna, Myriem El Qacemi, Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik
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Publication number: 20120309750Abstract: Disclosed are a novel 5-membered heterocycle derivatives of Formula I, a tautomer, pharmaceutically acceptable salt, prodrug thereof and a pharmaceutical use thereof. The 5-membered heterocycle derivatives of Formula I, a tautomer, pharmaceutically acceptable salt, prodrug thereof and compositions containing them are useful for treating a tumor.Type: ApplicationFiled: February 17, 2011Publication date: December 6, 2012Applicant: ILDONG PHARM CO., LTD.Inventors: Jae-Hoon Kang, Hong-Sub Lee, Jin-Sun Kwon, Joon-Tae Park, Chang-Sung Hong, Dong-Hyung Sin, Soo-Jung Hong, An-Na Moon, Jin-Ah Jeong, Sung-Wook Kwon
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Publication number: 20120283434Abstract: A process for the preparation of rivaroxaban, or a pharmaceutically acceptable salt thereof, or a solvate thereof, including a hydrate, comprising submitting an amine compound of formula (III) wherein R1 is a (C4-C10)-alkyl radical which is attached to the N atom by a tertiary C atom, first to an acylation reaction and then to a dealkylation reaction.Type: ApplicationFiled: January 3, 2011Publication date: November 8, 2012Applicant: ENANTIA, S.L.Inventors: Llorenç Rafecas Jané, Alexander Christian Comely, Alessandro Ferrali, Celia Amela Cortés, Mireia Pastó Aguilà
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Publication number: 20120252797Abstract: Isoxazoles of formula (A) or (B) wherein R1 is a group of formula (IB) The isoxazoles are inhibitors of HSP90 activity, and useful for the treatment of, for example, cancers.Type: ApplicationFiled: June 18, 2012Publication date: October 4, 2012Applicants: Vernalis (Cambridge) Limited, The Institute of Cancer Research, Cancer Research Technology Ltd.Inventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
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Publication number: 20120252796Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation.Type: ApplicationFiled: September 29, 2010Publication date: October 4, 2012Inventors: Harikishore Pingali, V.V.M. Sairam Kalapatapu, Pankaj Makadia, Mukul R. Jain
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Publication number: 20120225867Abstract: The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: October 27, 2010Publication date: September 6, 2012Inventors: Gerd Wohlfahrt, Olli Törmäkangas, Harri Salo, lisa Höglund, Arja Karjalainen, Pia Knuuttila, Patrik Holm, Sirpa Rasku, Anniina Vesalainen
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Publication number: 20120225880Abstract: A compound of formula (I): wherein A, B, D, X, Y, R1, R2, R3, m, p, and q are defined herein. Also disclosed is a method for inhibiting FMS-like tyrosine kinase 3, aurora kinase, or vascular endothelial growth factor receptor.Type: ApplicationFiled: March 1, 2012Publication date: September 6, 2012Applicant: National Health Research InstitutesInventors: Weir-Torn Jiaang, Tsu-An Hsu, Wen-Hsing Lin, Yu-Sheng Chao
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Publication number: 20120214767Abstract: Disclosed are compounds of Formula (I) or stereoisomers or salts thereof, wherein: X1, X2, X3, W, Q1, Q2, and G2 are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.Type: ApplicationFiled: October 29, 2010Publication date: August 23, 2012Inventors: T.G. Murali Dhar, Hai-Yun Xiao, Scott Hunter Watterson, Soo S. Ko, Alaric J. Dyckman, Charles M. Langevine, Jagabandhu Das
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Patent number: 8247412Abstract: The present invention provides compounds of formula (I): in which R1, R?1, R2, R?2, R3, Y and G have the meanings given in the description, to a process for their preparation, their application by way of medicaments, and to pharmaceutical compositions containing them.Type: GrantFiled: April 24, 2006Date of Patent: August 21, 2012Assignee: Galapagos SasuInventors: Pierre Deprez, Hélène Jary, Taoues Temal
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Publication number: 20120196862Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.Type: ApplicationFiled: January 27, 2012Publication date: August 2, 2012Applicant: 4SC Discovery GmbHInventors: Johann LEBAN, Stefan TASLER, Wael SAEB, Carine CHEVRIER
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Publication number: 20120196861Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.Type: ApplicationFiled: January 27, 2012Publication date: August 2, 2012Applicant: 4SC Discovery GmbHInventors: Johann LEBAN, Stefan TASLER, Roland BAUMGARTNER, Wael SAEB, Carine CHEVRIER
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Patent number: 8222243Abstract: The invention provides a compound of formula I: wherein A1, A2, A3, R1, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.Type: GrantFiled: August 26, 2008Date of Patent: July 17, 2012Assignee: Dart NeuroScience (Cayman) LtdInventors: Alan P. Kaplan, Terence P. Keenan, Andrew J. McRiner
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Publication number: 20120178733Abstract: The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.Type: ApplicationFiled: August 19, 2011Publication date: July 12, 2012Inventors: Bing-Yan Zhu, Shawn M. Bauer, Zhaozhong J. Jia, Gary D. Probst, Yanchen Zhang, Robert M. Scarborough
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Publication number: 20120172592Abstract: The present invention relates to new salt forms of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide, in particular the mesylate, hydrochloride, tartrate, phosphate and hemi fumarate salt thereof; to crystalline forms of such salts; to polymorphs of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide; to hydrates and polymorphs of the new salt forms mentioned above; to the use of the new salt forms mentioned above for the manufacture of a medicament for the treatment of a disorder mediated by Hsp90; to a method for treating a disorder mediated by Hsp90 using the new salt forms; to formulations comprising such salt forms, in particular aqueous solutions suitable for intravenous administration; and to amber glass containers being filled with such formulations.Type: ApplicationFiled: March 8, 2012Publication date: July 5, 2012Inventors: Martin James Drysdale, Brian William Dymock, Christoph Krell, Michael Mutz, Holger Petersen, Weijia Zheng