Ring Chalcogen In The Additional Hetero Ring (e.g., Oxazole, Etc.) Patents (Class 514/236.8)
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Publication number: 20100280019Abstract: The present invention is concerned with novel isoxazole derivatives of formula I wherein X, R1, R2, R3, R4 and R5 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: April 23, 2010Publication date: November 4, 2010Inventors: Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
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Publication number: 20100273798Abstract: This invention provides a process for the preparation of S-Rivaroxaban and/or R-Rivaroxaban comprising reacting, in the presence of a first base, a compound of Formula 9: with a compound of Formula 8:Type: ApplicationFiled: April 28, 2009Publication date: October 28, 2010Applicant: APOTEX PHARMACHEM INC.Inventors: Prabhudas BODHURI, Gamini Weeratunga
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Publication number: 20100267685Abstract: The invention relates to combinations of A) oxazolidinones of formula (I) and B) other active ingredients, to a method for producing said combinations and to the use thereof as medicaments, in particular for the treatment and/or prophylaxis of thrombo-embolic diseases.Type: ApplicationFiled: April 23, 2010Publication date: October 21, 2010Applicant: Bayer Schering Pharma AktiengesellschaftInventors: Alexander Straub, Thomas Lampe, Josef Pernerstorfer, Elisabeth Perzborn, Jens Pohlmann, Susanne Röhrig, Karl-Heinz Schlemmer
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Publication number: 20100267697Abstract: The present teachings provide compounds of Formula (I) and pharmaceutically acceptable salts, hydrates, and esters thereof, wherein Ar, R1, R2, R3, p, and X are defined herein. The present teachings also provide processes for producing said compounds and their pharmaceutically acceptable salts, hydrates and esters, and methods of treating a pathological condition or disorder, or alleviating a symptom thereof, using said compounds including their pharmaceutically acceptable salts, hydrates and esters. The compounds can be useful in modulating ion channel activity including treating a variety of conditions associated with the abnormal modulation of one or more voltage-gated calcium channels.Type: ApplicationFiled: December 11, 2007Publication date: October 21, 2010Applicant: WyethInventors: Vincent P. Galullo, Robert Zelle, Danielle Soenen, Christopher Todd Baker, Paul Will, Hormoz Mazdiyasni, Jinsong Guo, Andrew Fensome, Jeffrey Curtis Kern, William Jay Moore, Edward George Melenski, Justin Kaplan
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Patent number: 7816355Abstract: This invention provides a process for the preparation of S-Rivaroxaban and/or R-Rivaroxaban comprising reacting, in the presence of a first base, a compound of Formula 9: with a compound of Formula 8:Type: GrantFiled: April 28, 2009Date of Patent: October 19, 2010Assignee: Apotex Pharmachem IncInventors: Prabhudas Bodhuri, Gamini Weeratunga
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Patent number: 7816354Abstract: The present invention is directed to compounds of Formula I: Wherein R1, R2, Y, m and n are further defined in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.Type: GrantFiled: December 6, 2006Date of Patent: October 19, 2010Assignee: AstraZeneca ABInventors: Abdelmalik Slassi, Methvin Isaac, Ian Egle, Fupeng Ma, Babu Joseph, Joshua Clayton, Krzysztof Swierczek
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Publication number: 20100256127Abstract: The present invention is concerned with novel hydroxy-methyl isoxazole derivatives of formula I wherein R1, R2 and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: March 29, 2010Publication date: October 7, 2010Inventors: Bernd Buettelmann, Stephen Deems Gabriel, Steven Paul Hanlon, Roland Jakob-Roetne, Matthew C. Lucas, Paul Spurr, Andrew Thomas, Pius Waldmeier
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Publication number: 20100249078Abstract: Certain tetracyclic compounds are described, which may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).Type: ApplicationFiled: May 23, 2008Publication date: September 30, 2010Applicant: The Scrips Research InstituteInventor: Dale L. Boger
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Publication number: 20100249088Abstract: [Object] To provide a therapeutic and/or prophylactic agent for urinary frequency, urinary urgency, and urinary incontinence associated with various lower urinary tract diseases including overactive bladder, various lower urinary tract diseases accompanied by lower urinary tract pain, such as interstitial cystitis, chronic prostatitis, and the like, and various diseases accompanied by pain, based on an excellent trkA receptor inhibitory action.Type: ApplicationFiled: October 23, 2008Publication date: September 30, 2010Applicant: Astellas Pharma Inc.Inventors: Keizo Sugasawa, Kenichi Kawaguchi, Takaho Nomura, Shunichiro Matsumoto, Takashi Shin, Hidenori Azami, Tomoaki Abe, Akira Suga, Ryushi Seo, Masayuki Tanahashi, Toru Watanabe
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Publication number: 20100234345Abstract: The present application relates to isothiazolylidene containing compounds of Formula (I) wherein R1, R2, R3, R4, and L are as defined in the specification, compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions.Type: ApplicationFiled: November 4, 2009Publication date: September 16, 2010Applicant: ABBOTT LABORATORIESInventors: William A. Carroll, Michael J. Dart, Teodozyj Kolasa, Tongmei Li, Derek W. Nelson, Meena V. Patel, Sridhar Peddi, Arturo Perez-Medrano, Xueqing Wang
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Publication number: 20100234365Abstract: 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: December 12, 2007Publication date: September 16, 2010Applicant: IRM LLCInventors: Hong Liu, Xiaohui He, Dean Phillips, Xuefeng Zhu, Kunyong Yang, Thomas Lau, Baogen Wu, Yongping Xie, Truc Ngoc Nguyen, Xing Wang
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Publication number: 20100227847Abstract: The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) ? (NR1H3) and/or ? (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: March 17, 2010Publication date: September 9, 2010Applicant: ASTRAZENECA ABInventors: Anders Broo, Robert Judkins, Lanna Li, Eva-Lotte Lindstedt-Alstermark, Pernilla Sandberg, Marianne Swanson, Lars Weidolf, Kay Brickmann, Patrik Holm
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Publication number: 20100226918Abstract: The present invention relates to compounds of the formula I, in which R1; R2; R3; R4; R5; R6; R7; R8; R9; R10; R11; R12; R13; A; B, D and E have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: ApplicationFiled: December 16, 2009Publication date: September 9, 2010Applicant: SANOFI-AVENTISInventors: Otmar KLINGLER, Joerg CZECH, Werngard CZECHTIZKY, Tilo WEISS, Melitta JUST
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Patent number: 7790720Abstract: The present invention relates to compounds comprising an oxazole or thiazole moiety of formula (I), processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as H3-receptor ligands, Formula (I), wherein, A1 is CH, C(alkyl), C-halogen or N; R1 is hydrogen, halogen, C1-6 alkyl or alkoxy; R2 is, Formula (II?), A3 is O or S; R3 is hydrogen, halogen, C1-6 alkyl or alkoxy; R4 is hydrogen, halogen, C1-6 alkyl, alkoxy or —O-L; R5 is hydrogen or —O-L, wherein L is an aminoalkyl group and at least one of R4 and R5 should be —O-L.Type: GrantFiled: March 28, 2006Date of Patent: September 7, 2010Assignee: UCB Pharma, S.A.Inventors: Sylvain Celanire, Frederic Denonne
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Publication number: 20100222329Abstract: A 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and an activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colonies. A compound or a pharmaceutically acceptable salt thereof useful in treating thrombocytopenia.Type: ApplicationFiled: November 10, 2009Publication date: September 2, 2010Applicant: Astellas Pharma Inc.Inventors: Keizo Sugasawa, Susumu Watanuki, Yuji Koga, Hiroshi Nagata, Ryutaro Wakayama, Fukushi Hirayama, Ken-ichi Suzuki
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Patent number: 7786110Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.Type: GrantFiled: November 8, 2007Date of Patent: August 31, 2010Assignee: Roche Palo Alto LLCInventors: Michael Patrick Dillon, Ronald Charles Hawley, Li Chen, Lichun Feng, Minmin Yang
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Patent number: 7786117Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein J, B, Y, G and A are as described. Methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: May 6, 2009Date of Patent: August 31, 2010Assignee: Allergan, Inc.Inventor: David W. Old
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Publication number: 20100216794Abstract: Novel heterocyclic compounds of the formula I in which R1, R2, R3, R4 and D have the meanings indicated in claim 1, are activators of glucokinase and can be used for the prevention and/or treatment of Diabetes Typ 1 and 2, obesity, neuropathy and/or nephropathy.Type: ApplicationFiled: August 13, 2008Publication date: August 26, 2010Inventors: Lars Thore Burgdorf, Norbert Beier, Johannes Gleitz, Christine Charon, Daniel Cravo
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Publication number: 20100216792Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the field of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.Type: ApplicationFiled: October 14, 2009Publication date: August 26, 2010Applicant: Bayer CropScience AGInventors: Ulrich Görgens, Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Koichi Araki, Norio Sasaki, Kei Domon, Mamoru Hatazawa, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya
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Publication number: 20100216795Abstract: The present invention relates to Traf2- and Nck-interacting kinase (TNIK) inhibitors, pharmaceutical compositions, and methods for the treatment of cancer patients with TNIK inhibitors. And the present invention relates to a novel aminothiazole derivatives. The TNIK inhibitors are showed by a next formula (I). Wherein R1, R2, R3, R4, R5 and R6 represent independently a hydrogen atom or a substituent group.Type: ApplicationFiled: April 23, 2010Publication date: August 26, 2010Inventors: Tesshi Yamada, Miki Shitashige, Koichi Yokota, Masaaki Sawa, Hideki Moriyama
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Patent number: 7781426Abstract: Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), B or R2 is a phenyl group which has an ortho amine or aminomethyl substituent which is further substituted, and the other of B or R2 is also a cyclic group.Type: GrantFiled: December 29, 2006Date of Patent: August 24, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Zhijian Lu, Peter J. Sinclair, Gayle E. Taylor, Christopher F. Thompson, Cameron J. Smith, Adrian A. Dowst, Yi-Heng Chen
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Publication number: 20100210633Abstract: Chemokine receptor antagonists, in particular, compounds of Formula (I) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein.Type: ApplicationFiled: October 12, 2007Publication date: August 19, 2010Applicant: EPIX Delaware, Inc.Inventors: Jian Lin, Dongli Chen, Steffi Koerner, Rosa E. Melendez, Pradyumma Mohanty, Efrat Ben-Zeev, Merav Fichman, Yael Marantz, Oren Becker, Dilara McCauley, Pini Orbach, Ashis K. Saha, Sharon Shacham, Michael Xie
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Publication number: 20100210651Abstract: The present invention is concerned with isoxazole-isoxazoles and isoxazole-isothiazoles of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as cognitive enhancers or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.Type: ApplicationFiled: February 12, 2010Publication date: August 19, 2010Inventors: Maria-Clemencia Hernandez, Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
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Publication number: 20100210577Abstract: Disclosed are methods for the prevention or treatment of tuberculosis in a subject infected with Mycobacterium tuberculosis by administering rhodanine derivatives of formula (I), as well as some novel such compounds. Other embodiments are also disclosed.Type: ApplicationFiled: June 8, 2007Publication date: August 19, 2010Inventors: Jasbir Singh, Carl F. Nathan, Ruslana Bryk, Raghu Samy, Krzysztof Pupek, Mark Gurney
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Publication number: 20100210630Abstract: 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: April 30, 2010Publication date: August 19, 2010Inventors: Damian Arnaiz, Greg Brown, Emmanuel Claret, Arwed Cleve, David Davey, William Guilford, Seock-Kyu Khim, Thomas Kirkland, Monica J. Kochanny, Amy Liang, David Light, John Parkinson, David Vogel, Guo Ping Wei, Bin Ye
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Publication number: 20100210650Abstract: The use of 5-(2,4-Dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide or a tautomer thereof or a pharmaceutically acceptable salt or a hydrate or a solvate for the treatment of cancer of the bladder, the colon, the liver, the lung, the breast, the vagina, the ovaries, the pancreas, the kidney, the stomach, the gastrointestinal tract, the prostate, the head and neck, the peritoneal cavity, the thyroid, the bone, the brain, the central nervous system and/or the blood and/or for the treatment of myelodysplastic syndrome, systemic mastocytosis, von Hippel-Lindau syndrome, multicentric Castleman disease and/or psioriasis.Type: ApplicationFiled: October 10, 2008Publication date: August 19, 2010Applicant: NOVARTIS AGInventors: Patrick Chene, Carlos Garcia-Echeverria, Michael Rugaard Jensen, Cornelia Quadt, Thomas Radimerski, Joseph Schoepfer
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Publication number: 20100210632Abstract: The present invention provides a compound represented by the formula (I): wherein R1, R2, R3, Z1, Z2, Ra, Rb, q, A and n are as defined in the description, a pharmaceutically acceptable salt or solvate thereof. The compound is useful as P2X3 and/or P2X2/3 receptor antagonist.Type: ApplicationFiled: March 28, 2008Publication date: August 19, 2010Inventors: Hiroyuki Kai, Shunji Shinohara, Takayuki Kameyama
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Publication number: 20100197662Abstract: Disclosed is a compound useful as a type I 11?hydroxysteroid dehydrogenase inhibitor. A compound represented by the formula: a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkenyl or the like, One of R2 and R3 is a group of the formula: —C(?O)—Y—R4, wherein Y is —NR9— or the like, R4 is optionally substituted cycloalkyl or the like, R9 is hydrogen or optionally substituted alkyl, W is optionally substituted alkylene, The other is a group of the formula: —V—R5, wherein V is a bond, —O— or the like, R6 is hydrogen or optionally substituted alkyl, R5 is hydrogen, optionally substituted alkyl or the like, X is a bond, —S—, —SO— or the like, U is a bond or optionally substituted alkylene, R7 is hydrogen or optionally substituted alkyl, Z is —S—, —O— or —NR8—, R8 is hydrogen, optionally substituted alkyl or the like.Type: ApplicationFiled: June 6, 2006Publication date: August 5, 2010Applicant: Shionogi & Co., Ltd.Inventors: Tomoyuki Ogawa, Noriyuki Kurose, Satoru Tanaka, Koichi Nishi
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Publication number: 20100190766Abstract: Antibacterial compounds of formula (I) are provided: as well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.Type: ApplicationFiled: December 10, 2009Publication date: July 29, 2010Applicant: Achaogen, Inc.Inventors: Heinz E. Moser, Qing Lu, Phillip A. Patten, Dan Wang, Ramesh Kasar, Stephen Kaldor, Brian D. Patterson
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Publication number: 20100189687Abstract: The present application provides for a compound of Formula IV, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.Type: ApplicationFiled: February 22, 2008Publication date: July 29, 2010Applicant: GILEAD SCIENCES, INC.Inventors: Manoj C. Desai, Allen Y. Hong, Hon Chung Hui, Hongtao Liu, Randall W. Vivian, Lianhong Xu
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Publication number: 20100184740Abstract: The invention relates to novel substituted oxazolidinones, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders.Type: ApplicationFiled: June 7, 2008Publication date: July 22, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Swen Allerheiligen, Marcus Bauser, Dirk Heimbach, Stefan Heitmeier, Mark Jean Gnoth, Christoph Gerdes, Georges Von Degenfeld, Susanne Röhrig, Ulrich Rester, Elke Dittrich-Wengenroth, Uwe Saatman, Adrian Tersteegen
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Publication number: 20100184767Abstract: The invention relates to novel substituted oxazolidinones, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders.Type: ApplicationFiled: June 7, 2008Publication date: July 22, 2010Inventor: Susanne Rohrig
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Publication number: 20100179138Abstract: 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: ApplicationFiled: February 19, 2010Publication date: July 15, 2010Applicants: Vernalis (Cambridge) 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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Publication number: 20100179150Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.Type: ApplicationFiled: February 16, 2006Publication date: July 15, 2010Applicant: ASTRAZENECA ABInventors: Gregory Basarab, Brian Dangel, Paul Robert Fleming, Michael Barry Gravestock, Oluyinka Green, Sheila Irene Hauck, Pamela Hill, Kenneth Gregory Hull, George Mullen, Brian Sherer, Fei Zhou, Haihong Ni
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Publication number: 20100173413Abstract: This invention features compounds of formula (I): pharmaceutical compositions of the compounds, and methods of using the compounds for the treatment of, inter alia, IL-12-related diseases and disorders.Type: ApplicationFiled: March 11, 2010Publication date: July 8, 2010Applicant: Synta Pharmaceuticals CorporationInventors: Mitsunori Ono, Lijun Sun, Yumiko Wada, Teresa Przewloka, Hao Li, Howard P. Ng, Zachary Demko
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Publication number: 20100168111Abstract: A polymorphic form of rivaroxaban, 5-chloro-N-{[(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]oxa-zolidin-5-yl]-methyl}thiophene-2-carboxamide (termed form APO-A), processes for the preparation thereof, and compositions and formulations comprising form APO-A are provided. Also provided are compositions comprising a crystalline form of rivaroxaban and solvents selected from C3 to C6 ketones, C3 to C4 amides and mixtures thereof.Type: ApplicationFiled: December 31, 2008Publication date: July 1, 2010Applicant: Apotex Pharmachem Inc.Inventors: Prabhudas Bodhuri, Gamini Weeratunga
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Publication number: 20100166710Abstract: The present invention provides compositions and methods for inducing neuronal cell differentiation.Type: ApplicationFiled: December 1, 2006Publication date: July 1, 2010Applicants: The Scripps Research Institute, The Salk Institute for Biological StudiesInventors: Masaki Warashina, Kyung Hoon Min, Fred Gage, Peter G. Schultz, Sheng Ding, Tomoko Kuwabara
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Publication number: 20100168076Abstract: The instant invention provides compounds of Formula I which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: ApplicationFiled: August 29, 2007Publication date: July 1, 2010Inventors: Anthony Ogawa, Feroze Ujjainwalla, Ellenk Vande Bunte, Lin Chu, Debra Ondeyka, Ihor Kopka, Bing Li, Hyun Ok, Minal J. Patel, Jinyou Xu, Rosemary Sisco
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Publication number: 20100160301Abstract: The present invention relates to the use of selective factor Xa inhibitors, in particular of oxazolidinones of the formula (I) for the treatment and/or prophylaxis of microangiopathies and also their use for the production of medicaments for the treatment and/or prophylaxis of microangiopathies.Type: ApplicationFiled: September 27, 2006Publication date: June 24, 2010Applicant: BAYER HEALTHCARE AGInventors: Elisabeth Perzborn, Frank Misselwitz
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Publication number: 20100160247Abstract: The present invention is directed to a process for preparing a 2,26,6-d4-morpholine derivative represented by Structural Formula (I): or a salt thereof.Type: ApplicationFiled: June 17, 2009Publication date: June 24, 2010Applicant: CoNCERT Pharmaceuticals, Inc.Inventors: Julie F. Liu, Xuejun Tang, Scott L. Harbeson, Craig E. Masse
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Publication number: 20100151035Abstract: The present invention relates to a stable pharmaceutical composition of a poorly water-soluble drug with a view to increasing its solubility and bioavailability. The present invention relates to a solid dispersion of a poorly water-soluble drug.Type: ApplicationFiled: March 10, 2008Publication date: June 17, 2010Applicant: Sandoz AGInventors: Bharatrajan Ramaswami, Manisha Rajesh Patil, Aditi Das
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Publication number: 20100152189Abstract: The present invention relates to a novel polymorphic form and the amorphous form of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophene-carboxamide, processes for their preparation, medicaments comprising these forms, and their use in the control of diseases.Type: ApplicationFiled: September 22, 2006Publication date: June 17, 2010Applicant: BAYER HEALTHCARE AGInventors: Alfons Grunenberg, Jana Lenz, Gerhard Arnold Braun, Birgit Keil, Christian R. Thomas
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Publication number: 20100152187Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I), where V, W, R1, R2, R3 and R4 are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.Type: ApplicationFiled: June 5, 2006Publication date: June 17, 2010Applicant: XENON PHARMACEUTICALS INC.Inventors: Jianmin Fu, Duanjie Hou, Rajender Kamboj, Vishnumurthy Kodumuru, Natalia Pokrovskaia, Vandna Raina, Shaoyi Sun, Serguei Sviridov, Zaihui Zhang
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Publication number: 20100152188Abstract: The present invention relates to novel compounds of the general formula (I), their derivatives, their analogs, their stereoisomers, their pharmaceutically acceptable salts and compositions. The present invention more particularly provides novel heterocyclic compounds of the general formula (I).Type: ApplicationFiled: August 4, 2006Publication date: June 17, 2010Inventors: Akella Satya Surya Visweswara Srinivas, Kasinathan Mathiyazhagan, Duddu Savaraiah Sharada, Thanasekaran Ponpandian, Kulasekharan Revathy, Gaddam Om Reddy, Mani Kamarai, Sriram Raiagopal
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Publication number: 20100151011Abstract: The present invention relates to solid pharmaceutical dosage forms which can be administered orally and comprise 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide in amorphous form and/or thermodynamically metastable crystal modification and have rapid release of active ingredient, and to process for the production thereof, the use thereof as medicament, the use thereof for the prophylaxis, secondary prophylaxis and/or treatment of disorders, and to the use thereof for producing a medicament for the prophylaxis, secondary prophylaxis and/or treatment of disorders.Type: ApplicationFiled: September 21, 2006Publication date: June 17, 2010Applicant: BAYER HEALTHCARE AGInventor: Klaus Benke
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Publication number: 20100152162Abstract: It is intended to provide an agent for treating and/or preventing sleep disorder containing as an active ingredient a thiazole derivative represented by the general formula (I) (in the formula, R1 represents a five-membered aromatic heterocyclic group containing at least one oxygen atom or the like, R2 represents halogen or the like, and R3 represents —NR10R11 (in the formula, R10 and R11 are the same or different and represent a hydrogen atom or the like) or the like) or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: August 2, 2006Publication date: June 17, 2010Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Noriaki Uesaka, Shunji Ichikawa, Takao Nakajima
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Publication number: 20100144735Abstract: The present invention provides agents having antimicrobial activity for preventing and treating infectious diseases. Thus, the present invention provides novel substituted piperidino phenyloxazolidinone derivatives, processes for making compounds as well as antimicrobial compositions containing said derivatives as active ingredients and methods of treating bacterial infections with the said derivatives.Type: ApplicationFiled: February 12, 2010Publication date: June 10, 2010Inventors: Prasad Keshav Deshpande, Milind Dattatraya Sindkhedkar, Mahesh Shriram Phansalkar, Ravindra Dattatraya Yeole, Shrikant Vinayak Gupte, Yati Chugil, Nitin Shetty, Sachin Subhash Bhagwat, Milind Chintaman Shukla, Noel John De Souza, Mahesh Vithalbhai Patel
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Publication number: 20100137274Abstract: 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: June 30, 2009Publication date: June 3, 2010Applicant: Bayer Schering Pharma AGInventors: Alexander Straub, Thomas Lampe, Jens Pohlmann, Susanne Rohrig, Elisabeth Perzborn, Karl-Heinz Schlemmer, Joseph Pernerstorfer
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Publication number: 20100137315Abstract: The invention relates to compounds, pharmaceutical compositions thereof, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.Type: ApplicationFiled: November 30, 2009Publication date: June 3, 2010Applicant: APOGEE BIOTECHNOLOGY CORPORATIONInventors: Charles D. Smith, Kevin J. French, Zuping Xia
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Patent number: 7727981Abstract: 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: October 25, 2007Date of Patent: June 1, 2010Assignee: 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