Chalcogen Bonded Directly To Ring Carbon Of 1,4-oxazine Ring Patents (Class 514/230.8)
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Publication number: 20130237535Abstract: This invention relates to the use of spirocyclic piperidine derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of spirocyclic piperidines in the treatment of cancer.Type: ApplicationFiled: November 7, 2011Publication date: September 12, 2013Inventors: Nicholas D. Adams, Amita M. Chaudhari, Terence John Kiesow, Cynthia Ann Parrish, Alexander Joseph Reif, Lance Howard Ridgers, Stanley J. Schmidt, Kenneth Wiggall
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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: 8507478Abstract: The invention relates to antibacterial compounds of formula I wherein R1 is alkoxy or halogen; U and V each independently are CH or N; is a bond or is absent; W is CH or N or, when is absent, W is CH2 or NH, with the proviso that U, V and W are not all N; A is a bond or CH2; R2 is H or, provided A is CH2, may also be OH; m and n each independently are 0 or 1; D is CH2 or a bond; G represents a phenyl group substituted once or twice in the meta and/or para position(s) by substituents selected from alkyl, (C1-C3)alkoxy and halogen, or G is a group G1 or G2 wherein Z1, Z2 and Z3 may each represent CH or N; X is N or CH and Q is O or S; it being understood that if m and n each are 0, then A is CH2; and salts of such compounds.Type: GrantFiled: October 9, 2009Date of Patent: August 13, 2013Assignee: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Publication number: 20130203751Abstract: The present application relates to novel substituted 8-alkoxy-2-aminotetraline derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: May 9, 2011Publication date: August 8, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Walter Hübsch, Michael Hahn, Alexandros Vakalopoulos, Volkhart Min-Jian Li, Frank Wunder, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Friederike Stoll, Niels Lindner
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Publication number: 20130190292Abstract: The present invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z3, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.Type: ApplicationFiled: August 12, 2011Publication date: July 25, 2013Applicant: CELLZOME LIMITEDInventors: Kathryn Bell, Nelly Piton, Claudio Dagostin, Cyrille Boussard, Andrew Ratcliffe, Nigel Ramsden
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Publication number: 20130184261Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R4?, have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: March 5, 2013Publication date: July 18, 2013Inventor: Merck Patent Gesellschaft Mit Beschrankter Haftung
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Publication number: 20130184260Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R4? have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: March 5, 2013Publication date: July 18, 2013Inventor: Merck Patent Gesellschaft Mit Beschrankter Haftung
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Publication number: 20130184263Abstract: The present invention relates to compounds characterized by having a structure according to the following Formula I: or a pharmaceutically acceptable salt thereof. Compounds of the present invention are useful for the treatment or prevention of HIV.Type: ApplicationFiled: December 14, 2012Publication date: July 18, 2013Applicant: GlaxoSmithKline LLCInventor: GlaxoSmithKline LLC
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Publication number: 20130178469Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof.Type: ApplicationFiled: July 15, 2011Publication date: July 11, 2013Applicants: SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY (SIOC), AVEXA LIMITEDInventors: David Ian Rhodes, John Joseph Deadman, Giang Thanh Le, Nicholas Andrew Van de Graff, Lu Long, Li Xinming, Feng Xiao, Yu Changjiang
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Patent number: 8476249Abstract: Invented is a method of treating thrombocytopenia in a human, in need thereof which comprises the in vivo administration of a therapeutically effective amount of a peptide or a non-peptide TPO receptor agonist and an anti-clotting agent or agents, and optional further active ingredients, to such human.Type: GrantFiled: May 6, 2010Date of Patent: July 2, 2013Assignee: GlaxoSmithKline LLCInventors: Connie L. Erickson-Miller, Michael Arning
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Publication number: 20130158005Abstract: Compounds of the formula (I), in which R1, R2 and R3 have the meanings indicated in Claim 1, are kinase inhibitors and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: July 19, 2011Publication date: June 20, 2013Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Timo Heinrich, Christina Esdar, Hartmut Greiner
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Publication number: 20130158021Abstract: Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: wherein m, n, p, R?, R1, R2, R3, R4, R5, R8, Z, W, Y, and Z are as defined herein.Type: ApplicationFiled: October 26, 2012Publication date: June 20, 2013Applicant: Massachusetts Institute of TechnologyInventor: Massachusetts Institute of Technology
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Publication number: 20130143861Abstract: The subject invention provides methods for reducing stroke rate, methods for preventing atrial remodeling, and methods for reversing atrial remodeling by administering budiodarone to reduce atrial fibrillation (AF) episode duration and an anticoagulant (AC). According to some methods of the invention, the average AF episode duration can be reduced to less than about 24, 5, 3 or 1 hour(s), and the maximum AF episode duration may be reduced to less than about 20, 10 or 5 hours. According to some methods of the invention, the reduced stroke rate upon administration of budiodarone and AC is less than the age-adjusted overall stroke rate. Further, some methods provide that patients who were refractory to one or more anti-arrhythmic drugs prior to administration of budiodarone may also be treated. Some methods provide for prevention of atrial remodeling and others provide for the reversal of atrial remodeling, including methods to quantify the reversal of atrial remodeling.Type: ApplicationFiled: February 4, 2013Publication date: June 6, 2013Applicant: ARMETHEON, INC.Inventor: Armetheon, Inc.
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Publication number: 20130131056Abstract: The present invention relates to phenylethynyl compounds of formula I wherein R1, R2, X, L, R3, R4, R4?, cyc, and n are as defined in the specification and claims and to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They are useful for the treatment of schizophrenia or cognitive diseases.Type: ApplicationFiled: January 15, 2013Publication date: May 23, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130123252Abstract: The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: July 21, 2011Publication date: May 16, 2013Applicant: NOVARTIS AGInventors: David Barnes, Scott Louis Cohen, Jiping Fu, Lei Shu, Rui Zheng
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Publication number: 20130116240Abstract: Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as described in the specification.Type: ApplicationFiled: September 26, 2012Publication date: May 9, 2013Applicant: JAPAN TOBACCO INC.Inventor: Japan Tobacco Inc.
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Patent number: 8435981Abstract: Compounds of the formula (I) in which R1, R2, R3, R4 and R5 have the meanings indicated in claim 1 are inhibitors of tyrosine kinases, in particular of met kinase and can be employed inter alia for the treatment of tumors.Type: GrantFiled: July 12, 2007Date of Patent: May 7, 2013Assignee: Merck Patent Gesellschaft mit Beschränkter HaftungInventors: Dieter Dorsch, Oliver Schadt, Andree Blaukat, Frank Stieber
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Publication number: 20130109656Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.Type: ApplicationFiled: August 15, 2012Publication date: May 2, 2013Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Shelley Allen, Ellen Laird, Joseph P. Lyssikatos, John E. Robinson, Christopher P. Corrette, Robert Kirk DeLisle, Walter C. Voegtli
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Publication number: 20130085132Abstract: The present invention provides a pyrazole compound of the following general Formula [Ib] having SGLT1 inhibitory activity, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and its pharmaceutical use: wherein each symbol is the same as defined in the description.Type: ApplicationFiled: August 30, 2012Publication date: April 4, 2013Applicant: JAPAN TOBACCO INC.Inventors: Tomoya MIURA, Yosuke OGOSHI, Kazuhito UEYAMA, Dai MOTODA, Toshihiko IWAYAMA, Koichi SUZAWA, Hironobu NAGAMORI, Hiroshi UENO, Akihiko TAKAHASHI, Kazuyuki SUGIMOTO
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Publication number: 20130072457Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: ApplicationFiled: April 28, 2011Publication date: March 21, 2013Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Gordon Saxty, Christopher William Murray, Valerio Berdini, Gilbert Ebai Besong, Christopher Charles Frederick Hamlett, Christopher Norbert Johnson, Steven John Woodhead, Michael Reader, David Charles Rees, Laurence Anne Mevellec, Patrick René Angibaud, Eddy Jean Edgard Freyne, Tom Cornelis Hortense Govaerts, Johan Erwin Edmond Weerts, Timothy Pietro Suren Perera, Ronaldus Arnodus Hendrika Joseph Gilissen, Berthold Wroblowski, Jean Fernand Armand Lacrampe, Alexandra Papanikos, Oliver Alexis Georges Querolle, Elisabeth Thérèse Jeanne Pasquier, Isabelle Noëlle Constance Pilatte, Pascal Ghislain André Bonnet, Werner Constant Johan Embrechts, Rhalid Akkari, Lieven Meerpoel
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Publication number: 20130064888Abstract: The present invention provides a pharmaceutical dosage form in the form of a tablet comprising: (a) a compressed inert core, (b) an optional subcoat over the compressed inert core, (c) a drug layer over the compressed core (a) or optional subcoat (b) comprising a drug having a water solubility at 25° C. of about 100 mg/l or less, a coating polymer and optionally a surfactant, and (d) optionally one or more layers coating the drug layer. The present invention also provides a process of making the same.Type: ApplicationFiled: August 8, 2012Publication date: March 14, 2013Inventors: Roey SOLOMONOVICH, Dafna ARIELI
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Publication number: 20130059835Abstract: The present invention provides heterocyclylamine derivatives of Formula I: wherein the variables are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.Type: ApplicationFiled: August 31, 2012Publication date: March 7, 2013Applicant: INCYTE CORPORATIONInventors: Yun-Long Li, Wenqing Yao, Andrew P. Combs, Eddy W. Yue, Song Mei, Wenyu Zhu, Joseph Glenn, Thomas P. Maduskuie, JR., Richard B. Sparks, Brent Douty
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Publication number: 20130040930Abstract: Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: April 27, 2011Publication date: February 14, 2013Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Kazuhiro Maeda, Jun-ichi Endoh, Akiko Tarao, Kaoru Tashiro, Seigo Ishibuchi, Hidemasa Hikawa
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Publication number: 20130040931Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein ring A, B1, B2, B3, L, R1, R2, ring Z, m and n of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula (I), intermediates and processes useful for the preparation of compounds of Formula (I).Type: ApplicationFiled: January 14, 2011Publication date: February 14, 2013Applicant: Amgen Inc.Inventors: Nick A. Paras, James Brown, Yuan Cheng, Stephen A. Hitchcock, Ted Judd, Patricia Lopez, Ana Elena Minatti, Thomas Nixey, Timothy Powers, Christopher M. Tegley, Qiufen Xue, Bryant Yang, Wenge Zhong
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Patent number: 8372833Abstract: Disclosed is a novel compound having an NPY Y5 receptor antagonistic activity. A compound represented by the formula: its pharmaceutically acceptable salt or solvate thereof, wherein X is hydrogen or the like, Y is a group of the formula: Z is —NR7— or the like, R1 is hydrogen or the like, R2 and R3 are each independently hydrogen or the like, n is 0 or 1, p is 0 to 6.Type: GrantFiled: November 30, 2011Date of Patent: February 12, 2013Assignee: Shionogi & Co., Ltd.Inventor: Toshisada Yano
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Publication number: 20130035327Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: October 8, 2012Publication date: February 7, 2013Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
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Patent number: 8362008Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.Type: GrantFiled: December 11, 2008Date of Patent: January 29, 2013Assignee: The University Of EdinburghInventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
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Publication number: 20130023502Abstract: The invention relates to new substituted pyridinyl-pyrimidines of formula 1 wherein ring A is a five-membered saturated or unsaturated carbocyclic ring which optionally comprises one, two or three heteroatoms each independently from each other selected from the group N, S and O, wherein R1, R2, R4, R3, R5 and R6 are defined as in claim 1 and wherein ring A is further optionally substituted by one or two further substituents and the pharmaceutically acceptable salts, diastereomers, enantiomers, racemates, hydrates and solvates of the aforementioned compounds.Type: ApplicationFiled: January 25, 2012Publication date: January 24, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GmbHInventors: Georg Dahmann, Dennis Fiegen, Martin Fleck, Matthias Hoffmann, Jasna Klicic, Stephen Peter East, Spencer Charles R. Napier, John Scott
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Publication number: 20130023503Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.Type: ApplicationFiled: September 24, 2012Publication date: January 24, 2013Applicant: OPKO Health, Inc.Inventor: OPKO Health, Inc.
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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: 20120329773Abstract: This invention relates to bicyclic ring system substituted amide functionalized phenols of general formula 1, their use as inhibitors of CXCR2 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.Type: ApplicationFiled: December 13, 2011Publication date: December 27, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Riccardo GIOVANNINI, Dieter HAMPRECHT, Barbara KISTLER, Iain LINGARD
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Patent number: 8334284Abstract: 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: December 16, 2011Date of Patent: December 18, 2012Assignee: Bayer Intellectual Property GmbHInventors: Hans-Georg Lerchen, Ursula Krenz, Karl-Heinz Schlemmer, Elisabeth Perzborn, Joerg Keldenich
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Publication number: 20120316155Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1?), the TGF? pathway and/or the Wnt pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1?), the TGF? pathway and/or the Wnt pathway.Type: ApplicationFiled: February 17, 2011Publication date: December 13, 2012Applicant: Jasco Pharmaceuticals, LLCInventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Robert B. Nicewonger
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Publication number: 20120302547Abstract: The present invention relates to a melanin concentrating hormone antagonist compound of formula (I) wherein R1, Ra, Rb, R2, L1, R3, R4 and R5 are as defined, or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture of diasteromers thereof useful in the treatment, obesity and related diseases.Type: ApplicationFiled: August 8, 2012Publication date: November 29, 2012Applicant: ELI LILLY AND COMPANYInventors: Macklin Brian Arnold, Yen Dao, Kevin Matthew Gardinier, David Joseph Garmene, Steven James Green, Erik James Hembre, Jianliang Lu
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Publication number: 20120289502Abstract: A CB2 receptor modulator comprising an imidazole derivative represented by the general formula (I): [wherein, R1 represents optionally substituted lower alkyl or the like; R2 represents optionally substituted cycloalkyl or the like; R3 represents optionally substituted aryl or the like; and n represents an integer of 0 to 3] or a pharmaceutically acceptable salt thereof as an active ingredient, and the like are provided.Type: ApplicationFiled: July 25, 2012Publication date: November 15, 2012Applicant: Kyowa Hakko Kirin Co., Ltd.Inventors: Naoto Osakada, Mariko Osakada, Takashi Sawada, Satoshi Kaneko, Atsuko Mizutani, Noriaki Uesaka, Yoshisuke Nakasato, Keishi Katayama, Masamori Sugawara, Yushi Kitamura
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Publication number: 20120288492Abstract: The present invention relates to pyrimidine compounds of formula (I): which are useful in treating mTOR kinase- or PI3K kinase-related diseases.Type: ApplicationFiled: December 27, 2010Publication date: November 15, 2012Applicants: DCB-USA LLC, DEVELOPMENT CENTER FOR BIOTECHNOLOGYInventors: Mann-Yan Kuo, Ying-Shuan Lee, Paonien Chen, Li Jung Chen, Yann Yu Lu, Yi-Ting Huang, Hung-Yi Hsu, Ping-Kuei Tsai
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Publication number: 20120277204Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0), wherein R1 represents a substituent; R2 represents a hydrogen atom, or a substituent; R3 represents a hydrogen atom, or a substituent; Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.Type: ApplicationFiled: July 6, 2012Publication date: November 1, 2012Inventors: Takahiko TANIGUCHI, Akira Kawada, Mitsuyo Kondo, John F. Quinn, Jun Kunitomo, Masato Yoshikawa, Makoto Fushimi
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Publication number: 20120270838Abstract: The present invention relates to a compound represented by the following formula (1): wherein W, X, Y, R1, R2, R33, R34, m and n are as defined in the claims, or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: April 27, 2010Publication date: October 25, 2012Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Toru Esaki, Yoshikazu Nishimura, Yoshiaki Isshiki, Naoki Okamoto, Yoshiyuki Furuta, Akemi Mizutani, Masateru Ohta, Wayne Wen Lai, Tomoya Kotake
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Publication number: 20120258964Abstract: The invention relates to novel 2-heteroaryl carboxamides and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory.Type: ApplicationFiled: March 6, 2012Publication date: October 11, 2012Applicant: Bayer Schering Pharma AGInventors: Joachim Luithle, Frank-Gerhard Böss, Christina Erb, Frank-Thorsten Hafner, Katrin Schnizler, Timo Flessner, Marja Van Kampen, Franz-Josef Van Der Staay
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Publication number: 20120252801Abstract: The present invention relates to a series of novel compounds which have been shown to possess antifungal activity. The invention therefore relates to the new compounds, methods for their preparation, pharmaceutical compositions comprising them and to the compounds for use as a medicament, more in particular antifungal medicament.Type: ApplicationFiled: December 15, 2010Publication date: October 4, 2012Applicant: Katholieke Universiteit Leuven, K.U.Leuven R&DInventors: Dorothée Bardiot, Bruno Cammue, Patrick Chaltin, Arnaud Marchand, Karin Thevissen
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Patent number: 8273738Abstract: A CB2 receptor modulator comprising an imidazole derivative represented by the general formula (I): [wherein, R1 represents optionally substituted lower alkyl or the like; R2 represents optionally substituted cycloalkyl or the like; R3 represents optionally substituted aryl or the like; and n represents an integer of 0 to 3] or a pharmaceutically acceptable salt thereof as an active ingredient, and the like are provided.Type: GrantFiled: September 5, 2007Date of Patent: September 25, 2012Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Naoto Osakada, Mariko Osakada, Takashi Sawada, Satoshi Kaneko, Atsuko Mizutani, Noriaki Uesaka, Yoshisuke Nakasato, Keishi Katayama, Masamori Sugawara, Yushi Kitamura
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Publication number: 20120214806Abstract: 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: May 1, 2012Publication date: August 23, 2012Inventors: Matteo Andreini, David Banner, Emanuele Gabellieri, Wolfgang Guba, Hans Hilpert, Harald Mauser, Alexander V. Mayweg, Robert Narquizian, Eoin Power, Mark Rogers-Evans, Massimiliano Travagli, Michela Valacchi, Thomas Woltering, Wolfgang Wostl
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Publication number: 20120201888Abstract: Methods and compositions are provided which comprise effective amounts of analgesic to treat a subject, including reducing or eliminating an adverse effect associated with the analgesic.Type: ApplicationFiled: January 10, 2012Publication date: August 9, 2012Applicant: CHARLESTON LABORATORIES, INC.Inventors: Paul Bosse, John Ameling, Bernard Schachtel, Ray Takigiku
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Publication number: 20120189623Abstract: The present invention relates to new substituted imidazole compounds have the following Formula (I) and to the pharmaceutically acceptable salts, esters, or prodrugs thereof, to compositions of the compounds together with pharmaceutically acceptable carriers, and to uses of the compounds:Type: ApplicationFiled: April 3, 2012Publication date: July 26, 2012Inventors: Rustum Boyce, Eric Martin, Weibo Wang, Hong Yang, Paul A. Barsanti
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Publication number: 20120184544Abstract: The present invention relates to substituted benzamide derivatives of the general Formula I and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, prodrugs, metabolites, and polymorphs and can be useful for treating disease states mediated by glucokinase. Compounds disclosed herein can be used for reducing blood glucose levels and for increasing insulin secretion for treating type II diabetes. The invention also relates to processes for the preparation of the compounds of invention, pharmaceutical compositions containing the compounds, and their use.Type: ApplicationFiled: July 22, 2010Publication date: July 19, 2012Applicant: CADILA HEALTHCARE LIMITEDInventors: Rajendra Kharul, Makul R. Jain, Pankaj R. Patel
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Publication number: 20120148689Abstract: The present invention is related to the composition and methods of manufacture of orally-dissolvable, edible films as a vehicle for the non-invasive administration of active drugs through the mucosal tissues of the oral cavity. The films include a water soluble film-forming polymer such as pullulan. Methods for producing the films are also disclosed.Type: ApplicationFiled: February 17, 2012Publication date: June 14, 2012Inventor: Todd Maibach
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Patent number: 8188270Abstract: 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: GrantFiled: September 22, 2006Date of Patent: May 29, 2012Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Alfons Grunenberg, Jana Lenz, Gerhard Arnold Braun, Birgit Keil, Christian R. Thomas
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Publication number: 20120122854Abstract: The invention is concerned with novel carbocyclyl fused cyclic amines of formula (I) wherein A, X1 to X3, Y1 to Y3, Z, R1, R2, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.Type: ApplicationFiled: January 11, 2012Publication date: May 17, 2012Inventors: Markus Boehringer, Katrin Groebke Zbinden, Wolfgang Haap, Narendra Panday, Fabienne Ricklin, Martin Stahl, Petra Schmitz
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Publication number: 20120121530Abstract: The present invention relates to certain DPP-4 inhibitors for treating and/or preventing oxidative stress, vascular stress and/or endothelial dysfunction as well as to the use of such DPP-4 inhibitors in treatment and/or prevention of diabetic or non-diabetic patients, including patient groups at risk of cardiovascular and/or renal disease.Type: ApplicationFiled: November 14, 2011Publication date: May 17, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thomas KLEIN, Andreas DAIBER, Odd-Eric JOHANSEN, Michael MARK, Sanjaykumar PATEL, Hans-Juergen WOERLE
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Patent number: 8178671Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.Type: GrantFiled: July 30, 2004Date of Patent: May 15, 2012Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Hui Li, Somasekhar Bhamidipati, David Carroll, Catherine Sylvain, Jeffrey Clough, Holger Keim