The Five-membered Nitrogen Hetero Ring Has Chalcogen As A Ring Member Patents (Class 514/253.1)
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Publication number: 20100297035Abstract: Thiazole amides, imidazole amides and related analogues of the Formula: are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) and other disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).Type: ApplicationFiled: April 12, 2010Publication date: November 25, 2010Applicant: LIGAND PHARMACEUTICALS, INC.Inventors: Wallace C. Pringle, John M. Peterson, Linghong Xie, Ping Ge, Yang Gao, Joseph W. Ochterski, Jiong Lan
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Publication number: 20100298316Abstract: Certain novel benzothiazoles and benzoxazoles, e.g., 2-(piperazin-1-yl)benzothiazoles and 2-(piperazin-1-yl)benzoxazoles, optionally substituted in the 3 and/or 4 positions of the piperazine rings,! of the general formula (1): having histamine H3 antagonistic activity can be used in pharmaceutical compositions.Type: ApplicationFiled: March 22, 2007Publication date: November 25, 2010Inventors: Florencio Zaragoza Dorwald, Rolf Hohlweg, Inge Thoger Christensen, Jane Marie Lundbeck, Erik Knud Andersen
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Publication number: 20100285006Abstract: The present invention relates to novel thiazole-substituted indolin-2-ones as inhibitors of CSCPK and related kinases; to methods of inhibiting cancer stem cells by using a kinase inhibitor; to pharmaceutical compositions containing such compounds; and to methods of using such compounds in the treatment of a protein kinase related disorder in a mammal; and to processes of making such compounds and intermediates thereof.Type: ApplicationFiled: September 5, 2008Publication date: November 11, 2010Inventors: Chiang Jia LI, Ji-Feng Liu, Youzhi Li, Wei Li, Harry Rogoff
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Publication number: 20100286147Abstract: Disclosed are compounds of Formulae 1 and 1A (including all geometric and stereoisomers), N-oxides, and salts thereof, wherein R1, R2, A, G, M, W, Z1, X, J, J1 and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: January 22, 2009Publication date: November 11, 2010Applicant: E.I. DUPONT DE NEMOURS AND COMPANYInventors: Mary Ann Hanagan, Robert James Pasteris
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Publication number: 20100286135Abstract: The present invention relates to novel heterocyclic amide compounds of Formula I: as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are compositions comprising said compounds, and methods for using said compounds for treating or preventing a proliferative disease, an anti-proliferative disorder, inflammation, arthritis, a neurological or neurodegenerative disease, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease or a fungal disease.Type: ApplicationFiled: July 17, 2008Publication date: November 11, 2010Applicant: Schering Corporation Patent Department, K-6-1; 1990Inventors: Panduranga Adulla P. Reddy, Lianyun Zhao, Praveen k. Tadikonda, Tzu Tshin Wong, Shuyi Tang, Luis E. Torres, David F. Cauble, JR., Timothy J. Guzi, M. Arshad Siddiqui
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Publication number: 20100280006Abstract: Benzoxazole and benzothiazole compounds and the stereoisomers, tautomers, solvates, oxides, esters, and prodrugs thereof and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF-1R.Type: ApplicationFiled: May 8, 2009Publication date: November 4, 2010Inventors: James C. Sutton, Marion Wiesmann, Weibo Wang, Mika Lindvall, Jiong Lan, Savithri Ramurthy, Anu Sharma, Elizabeth J. Mieuli, Liana M. Klivansky, William Lenahan, Susan Kaufman, Hong Yang, Simon C. Ng, Keith Pfister, Allan S. Wagman, Victoria Sung, Martin Sendzik
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Patent number: 7825112Abstract: The disclosure relates to 2-carbamide-4-phenylthiazole derivatives having the following general formula (I): wherein R1, R2, R3, Y and p are as defined in the disclosure. The disclosure also relates to pharmaceutical compositions containing a compound of formula (I), to processes for preparing the compounds of formula (I), and to methods of using the compounds of formula (I).Type: GrantFiled: June 26, 2008Date of Patent: November 2, 2010Assignee: sanofi-aventisInventors: Pierre Casellas, Daniel Floutard, Pierre Fraisse, Stephane Hourcade, Samir Jegham
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Publication number: 20100267717Abstract: The present invention relates in one embodiment to compounds of formula (Ih) and/or a pharmaceutically acceptable salt thereof with an acid or a base, and/or a pharmaceutically acceptable prodrug and/or a stereoisomer thereof, wherein A is NR2?, S or O; R3a is H, OH, SH, NH2, —C(NR7)NR7?R8, —(CH2)paryl, —(CH2)pNR7R8, —C(O)NR7R8, —N?CR7R8, —NR7C(O)R8, alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, alkoxy, alkylamino, hydroxyalkylamino, halogen, aryl, or heteroaryl; R3 is H, —C(O)NRaRb, halogen, alkyl, haloalkyl, aryl, heteroaryl, OH, SH, NR4?OR5?, NH2, hydroxyalkylamino, alkylamino, alkoxy, cycloalkyl, heterocycloalkyl, hydroxyalkyl, or haloalkyloxy; X is NR2?, O, or S; Z is N or CR2?.Type: ApplicationFiled: March 14, 2007Publication date: October 21, 2010Applicant: 4SC AGInventors: Johann Leban, Harald Schmitt, Kristina Wolf, Stefano Pegoraro, Andreas Wuzik
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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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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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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: 20100249030Abstract: The present invention relates to a method of treating cancer by pretreatment with anti-mitotic agents followed by at least one aurora kinase inhibitor. Extensive illustrations are provided for the antimitotic agents and aurora kinase inhibitors that are useful in the inventive treatment.Type: ApplicationFiled: July 28, 2008Publication date: September 30, 2010Inventor: Andrea Dawn Basso-Porcaro
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Publication number: 20100240657Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R2 to R4, L, Q and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition with the above-mentioned properties.Type: ApplicationFiled: July 1, 2008Publication date: September 23, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ioannis Sapountzis, Peter Ettmayer, Christian Klein, Andreas Mantoulidis, Martin Steegmaier, Steffen Steurer, Irene Waizenegger
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Patent number: 7799789Abstract: The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, zenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.Type: GrantFiled: June 26, 2008Date of Patent: September 21, 2010Assignees: Schering Corporation, Pharmacopeia Drug Discovery, Inc.Inventors: Gopinadhan N. Anilkumar, Qingbei Zeng, Stuart B. Rosenblum, Joseph A. Kozlowski, Brian F. McGuinness, Douglas W. Hobbs
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Patent number: 7799791Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R1 and R2 is H, and the other is selected from OR6, SR6, NR6R7, N3, Me, Et, CF3, SOR8 and SO2R8; or R1 and R2 are both H; one of R3 and R4 is H, and the other is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl and cyclohexyl; or R3 and R4 are joined together with the adjacent backbone carbon atom to form a spiro-C5-C6 cycloalkyl group; R6 and R7 are each independently selected from H, C1-8-alkyl and C3-8-cycloalkyl; or R6 and R7 are linked to form a cyclic group together with the nitrogen to which they are attached; R8 is C1-8-alkyl or C3-8-cycloalkyl; R9 is a para-substituted 6-membered monocyclic aryl or heteroaryl ring which includes up to five heteroatoms.Type: GrantFiled: January 8, 2009Date of Patent: September 21, 2010Assignee: Amura Therapeutics LimitedInventors: Martin Quibell, John Paul Watts
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Publication number: 20100234389Abstract: An object of the present invention is to provide a novel fused-ring compound which has a FAAH inhibitory effect and is useful as an analgesic. The present invention relates to a compound represented by formula (I): wherein symbols are as defined in the specification, or salt thereof.Type: ApplicationFiled: October 9, 2008Publication date: September 16, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masakuni Kori, Mitsunori Kouno
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Patent number: 7795261Abstract: This invention concerns substituted I-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of schizophrenia, anxiety, depression, emesis and IBS. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1.Type: GrantFiled: December 17, 2003Date of Patent: September 14, 2010Assignee: Janssen Pharmaceutica NVInventors: Frans Eduard Janssens, François Maria Sommen, Benoît Christian Albert Ghislain De Boeck, Joseph Elisabeth Leenaerts
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Publication number: 20100227845Abstract: The present invention relates to compounds represented by Formula (I), Formula (II) and Formula (III) and pharmaceutically acceptable salts thereof. The present invention also provides pharmaceutical compositions comprising the instant compounds. This invention further provides methods to treat and prevent pain, respiratory and non-respiratory diseases.Type: ApplicationFiled: October 14, 2008Publication date: September 9, 2010Inventors: Zhicai Wu, John C. Hartnett
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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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Publication number: 20100222341Abstract: Compounds of the formula (I), in which R1, R2, R3, D, G, Q and W have the meanings indicated in claim (1), can and be employed for the treatment of tumours.Type: ApplicationFiled: September 19, 2008Publication date: September 2, 2010Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HARTUNGInventors: Kai Schiemann, Melanie Schultz, Andree Blaukat, Ingo Kober
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Publication number: 20100222361Abstract: 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: 7786124Abstract: The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, zenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.Type: GrantFiled: March 19, 2007Date of Patent: August 31, 2010Assignee: Schering CorporationInventors: Stuart B. Rosenblum, Joseph A. Kozlowski, Neng-Yang Shih, Brian F. McGuinness, Douglas W. Hobbs
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Patent number: 7786125Abstract: The present application is directed to therapeutic compounds, compositions, and methods for culturing neuronal cells and for preventing and the treatment of neurodegenerative diseases, such as Parkinson's disease and amyotrophic lateral sclerosis (ALS).Type: GrantFiled: April 7, 2009Date of Patent: August 31, 2010Inventor: Leu-Fen H. Lin
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Publication number: 20100215652Abstract: Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.Type: ApplicationFiled: February 26, 2010Publication date: August 26, 2010Inventors: Nicola Mary ASTON, Paul Bamborough, Ann Louise Walker
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Publication number: 20100215661Abstract: Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.Type: ApplicationFiled: February 26, 2010Publication date: August 26, 2010Inventors: Nicola Mary ASTON, Paul Bamborough, Ann Louise Walker
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Publication number: 20100210638Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: April 28, 2010Publication date: August 19, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
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Publication number: 20100210634Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: ApplicationFiled: May 3, 2010Publication date: August 19, 2010Inventors: Bradley P. Morgan, Erica A. Kraynack, Pu-Ping Lu, Alex Muci, David J. Morgans, JR.
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Patent number: 7776862Abstract: The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: and the pharmaceutically acceptable salts, solvates and esters thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.Type: GrantFiled: February 14, 2006Date of Patent: August 17, 2010Assignee: Schering CorporationInventors: Brian F. McGuinness, Stuart B. Rosenblum, Joseph A. Kozlowski, Gopinadhan N. Anilkumar, Seong Heon Kim, Neng-Yang Shih, Chung-Her Jenh, Paul J. Zavodny, Douglas W. Hobbs, Guizhen Dong, Yuefei Shao, Lisa Guise Zawacki, Cangmeng Yang, Carolyn Dilanni Carroll
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Publication number: 20100203039Abstract: The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.Type: ApplicationFiled: April 16, 2010Publication date: August 12, 2010Inventor: Chu-Biao Xue
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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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Patent number: 7754723Abstract: Compounds of formulae: where Ar1, Ar2, R3, R4, and m are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Nitro(cyano)vinylpiperazine Compound”); compositions comprising an effective amount of a Nitro(cyano)vinylpiperazine Compound; and methods for treating or preventing pain and other conditions in an animal comprising administering to an animal in need thereof an effective amount of a Nitro(cyano)vinylpiperazine Compound are disclosed.Type: GrantFiled: June 28, 2006Date of Patent: July 13, 2010Inventors: Qun Sun, Laykea Tafesse
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Patent number: 7754719Abstract: Compound of the formula (I) wherein R1, R2, n and m are as defined in the specification. The compounds of formula (I) are somatostatin sst1 receptor antagonists.Type: GrantFiled: July 13, 2006Date of Patent: July 13, 2010Assignee: Novartis AGInventors: Daniel Hoyer, Konstanze Hurth, Thomas J. Troxler
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Publication number: 20100168124Abstract: The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.Type: ApplicationFiled: December 21, 2009Publication date: July 1, 2010Inventors: Stuart B. Rosenblum, Joseph A. Kozlowski, Neng-Yang Shih, Brian F. McGuinness, Douglas W. Hobbs
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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: 20100152192Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.Type: ApplicationFiled: December 11, 2009Publication date: June 17, 2010Applicant: Glenmark Pharmaceuticals S.AInventors: Sachin Sundarlal Chaudhari, Abraham Thomas, Ashok Bhausaheb Kadam, Sachin Vasantrao Dhone, Suresh Mahdadev Kadam, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
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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: 20100144712Abstract: A triazole derivative of formula 1 or a pharmaceutically acceptable salt, hydrate, solvate or isomer thereof is superior to the conventional antifungal drugs in antifungal activity against a wide spectrum of pathogenic fungi, and has advantageously low toxicity.Type: ApplicationFiled: June 12, 2008Publication date: June 10, 2010Applicants: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY, CHEMON INC.Inventors: Bum Tae Kim, Yong Ki Min, Jung Nyoung Heo, Hyuk Lee, Sung Youn Chang, No Kyun Park, Si-Whan Song, Jung-Ja Oh
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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: 20100125075Abstract: Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(?O) or the formula: —C(?O)NH(OH); R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of the formula: —N(OH)CH(?O), a hydroxy, C1-C6 alkoxy, C1-C6 alkenyloxy, amino, C1-C6 alkylamino, or di-(C1-C6 alkylamino group; R2 represents a substituted or unsubstituted C1-C6 alkyl, cycloalkyl(C1-C6 alkyl)- or aryl(C1-C6 alkyl)-group; and A represents a group of formula (IIA), or (IIB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 when taken together with the nitrogen atom to which they are attached form a saturated heterocyclic first ring of 5 to 7 atoms as specified in the description.Type: ApplicationFiled: December 14, 2006Publication date: May 20, 2010Applicant: British Biotech Pharmaceuticals Ltd.Inventors: Lisa Marie Pratt, Kenneth Noel Keavey, Gilles Denis Pain, Laurent Mounier
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Publication number: 20100113471Abstract: The present invention relates to novel compounds selected from 2-aminoaryloxazoles that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic and degenerative disorders. More particularly, these compounds are potent and selective c-kit, bcr-abl, FGFR3 and/or Flt-3 inhibitors.Type: ApplicationFiled: January 11, 2010Publication date: May 6, 2010Inventors: Alain Moussy, Camille Wermuth, David Grierson, Abdellah Benjahad, Martine Croisy, Marco Ciufolini, Bruno Giethlen
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Publication number: 20100099676Abstract: A compound represented by the general formula (I): wherein R1 is wherein R26 and R28 are each independently lower alkyloxy and the like; n1 is an integer of 0 to 3; Z is a optionally substituted C1-C5 alkynylene which may be interrupted with a substituent selected from Substituent group a and the like; A is a group represented by the formula: wherein R6 and R7 are each independently lower alkyl and the like; m and n are each independently 0, 1, or 2; R2 is a hydrogen atom and the like; R3 is optionally substituted lower alkyl and the like; R4 is a hydrogen atom; or R3 and R4 may be taken together with an adjacent carbon atom to from a ring; R5 is hydroxyl and the like, or an optically active isomer, a pharmaceutically acceptable salt or a solvate thereof.Type: ApplicationFiled: October 31, 2007Publication date: April 22, 2010Applicant: SHIONOGI & CO., LTD.Inventors: Takeshi Endoh, Yasuhiko Fujii, Eiichi Kojima, Genta Tadano, Naoko Yamaguchi, Yo Adachi, Sachie Tagashira, Yuki Tachibana, Naohiro Onodera
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Publication number: 20100093750Abstract: The present invention relates to a method for treating solid cancers including non-small 5 cell lung cancer, pancreatic, bladder, breast and ovarian cancer as well as advanced biliary tract cancers comprising administering at least one antineoplasticagent such as a nucleotide analog, for example gemcitabine, or an antimitotic such as docetaxel, in combination with a tyrosine kinase inhibitor selected from 2-aminoarylthiazoles and 2-aminoaryloxazoles.Type: ApplicationFiled: January 11, 2008Publication date: April 15, 2010Inventors: Alain Moussy, Jean-Pierre Kinet
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Publication number: 20100093689Abstract: The present invention provides novel heteroaryl compounds and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.Type: ApplicationFiled: November 17, 2009Publication date: April 15, 2010Inventors: James C. Sutton, Zulan Pi, Rejean Ruel, Alexandre L'Heureux, Carl Thibeault, Patrick Y.S. Lam
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Publication number: 20100069363Abstract: The present application relates to novel substituted 4-amino-3,5-dicyano-2-thiopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders.Type: ApplicationFiled: November 17, 2007Publication date: March 18, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Peter Nell, Nicole Diedrichs, Barbara Albrecht-Küpper, Alexandros Vakalopoulos, Frank Süssmeier, Joerg Keldenich
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Patent number: 7671077Abstract: The present application is directed to therapeutic compounds, compositions, and methods for culturing neuronal cells and for preventing and the treatment of neurodegenerative diseases, such as Parkinson's disease and amyotrophic lateral sclerosis (ALS).Type: GrantFiled: July 19, 2004Date of Patent: March 2, 2010Inventor: Leu-Fen Hou Lin
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Patent number: 7671056Abstract: The present invention relates to novel piperazine-piperidine compounds. The compounds are useful as 5-HT1A binding agents, particularly as 5-HT1A receptor antagonists and agonists. These compounds are useful in treating central nervous system disorders, such as cognition disorders, anxiety disorders, depression and sexual dysfunction. The invention relates to compounds and pharmaceutically acceptable salts of formula (I?): wherein R1-R16, Ra, Rb, and n are set forth in the specification. The invention also relates to pharmaceutical compositions comprising compounds and pharmaceutically acceptable salts of formula (I?).Type: GrantFiled: June 9, 2006Date of Patent: March 2, 2010Assignee: Wyeth LLCInventors: Magda Asselin, George Theodore Grosu, Annmarie Louise Sabb, Wayne Everett Childers, Lisa Marie Havran, Zhongqi Shen, James Jacob Bicksler, Dan Chaekoo Chong
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Publication number: 20100048574Abstract: The present invention relates to compounds of the general formula (II): or pharmaceutically acceptable salts thereof with an acid or a base, or pharmaceutically acceptable prodrugs or a stereoisomer thereof.Type: ApplicationFiled: October 9, 2009Publication date: February 25, 2010Applicant: 4SC AGInventors: Johann Leban, Harald Schmitt, Kristina Wolf, Stefano Pegoraro, Andreas Wuzik
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Publication number: 20100048583Abstract: The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein R1 is independently hydrogen, alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl or substituted arylalkyl; R2 is independently —NR3R4, R3 is independently alkyl, cycloalkyl, alkoxy, alkylamine, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl, R4 is independently alkyl, cycloalkyl, alkoxy, alkylamine, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R5 is independently H, COR6, CO2R6, SOR6, SO2R6, SO3R6, alkyl, cycloalkyl, alkoxy, —NH2, alkylamine, —NR7COR6, halogen, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R6 is independently H, alkyl, cycloalkyl, —NH2, alkylamine, aryl or heteroaryl; R7 is independently H, alkyl, cycloalkyl, alkoxy, —OH, —SH, alkylthio, hydroxyalkyl, aryl, or heteroaryl; p is 0,Type: ApplicationFiled: August 24, 2009Publication date: February 25, 2010Applicant: 4SC AGInventors: Johann LEBAN, Harald Schmitt, Kristina Wolf, Stefano Pegoraro, Andreas Wuzik
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Publication number: 20100041668Abstract: The present invention in certain embodiments is directed to a pharmaceutical dosage form comprising a therapeutically effective amount of a first agent that agonizes a human TPO receptor by binding to the rhTPO binding site of the human TPO receptor; and a therapeutically effective amount of a second agent that agonizes the human TPO receptor by binding to a binding site of the human TPO receptor distinct from the rhTPO binding site.Type: ApplicationFiled: August 19, 2009Publication date: February 18, 2010Applicant: Astellas Pharma Inc.Inventors: Ken-Ichi Suzuki, Keizo Sugasawa
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Publication number: 20100041667Abstract: The present invention is directed to compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: ApplicationFiled: September 19, 2007Publication date: February 18, 2010Inventor: Shaun R. Stauffer