Bicyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/552)
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Publication number: 20120184528Abstract: The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.Type: ApplicationFiled: May 11, 2010Publication date: July 19, 2012Applicants: ADDEX PHARMA S.A., JANSSEN PHARMACEUTICALS, INCInventors: Jose Maria Cic-Nunez, Ana Isabel De Lucas Olivares, Andres Avelino Trabanco-Suarez, Gregor James MacDonald
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Publication number: 20120184732Abstract: The present invention provides a nitrogen-containing heterocyclic compound represented by formula (I) and salt thereof, which is useful as an active ingredient of a fungicide for agricultural and horticultural use, having an assured effect and being safely usable.Type: ApplicationFiled: September 22, 2010Publication date: July 19, 2012Inventors: Akira Mitani, Jun Inagaki, Raito Kuwahara, Motoaki Sato
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Patent number: 8222245Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.Type: GrantFiled: December 19, 2008Date of Patent: July 17, 2012Assignee: Glaxo Group LimitedInventors: Emmanuel Hubert Demont, Jag Paul Heer, John Skidmore, Ian David Wall, Jason Witherington, Thomas Daniel Heightman, David Nigel Hurst, Christopher Norbert Johnson
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Publication number: 20120165519Abstract: The present invention provides a compound of formula I or II or a pharmaceutically acceptable salt form thereof, wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, and A5, are as defined herein. The compounds of formula I or II have ALK and/or c-Met inhibitory activity, and may be used to treat proliferative disorders.Type: ApplicationFiled: March 6, 2012Publication date: June 28, 2012Applicant: Cephalon, Inc.Inventors: Gulzar Ahmed, Henry Joseph Breslin, Jason Burke, Matthew A. Curry, James L. Diebold, Bruce Dorsey, Benjamin J. Dugan, Daming Feng, Diane E. Gingrich, Tao Guo, Keith S. Learn, Joseph G. Lisko, Rong-qiang Liu, Eugen Mesaros, Karen Milkiewicz, Gregory R. Ott, Jay P. Theroff, Tho V. Thieu, Rabindranath Tripathy, Theodore L. Underiner, Gregory J. Wells, Craig A. Zificsak
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Publication number: 20120165312Abstract: The present invention relates to a serotonin 5-HT2C receptor activator containing a compound represented by the formula wherein ring A is a 5- or 6-membered aromatic heterocycle optionally having substituent(s), and ring B is a 7- to 9-membered ring optionally having substituent(s) other than an oxo group wherein the combination of m and n (m,n) is (1,2), (2,1), (2,2), (3,1), (3,2) or (4,1), or a salt thereof or a prodrug thereof, and a fused heterocyclic compound having a serotonin 5-HT2C receptor activating action and the like.Type: ApplicationFiled: March 2, 2012Publication date: June 28, 2012Inventors: Junya SHIRAI, Tomokazu Kusumoto, Hiroyuki Nagamiya, Izumi Kamo
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Publication number: 20120157440Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, A, R4, n, and R7 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: ApplicationFiled: December 13, 2011Publication date: June 21, 2012Inventors: TODD W. BUTLER, Ramalakshmi Y. Chandrasekaran, Scot R. Mente, Chakrapani Subramanyam, Travis T. Wager
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Publication number: 20120149573Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, X is CH or N; Y is C(O) or S(O)2; provided that when Y is S(O)2, then X is CH; A is a radical selected from the group consisting of and B1, B2, B3, T, R1, R2 R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: September 7, 2010Publication date: June 14, 2012Inventors: Kanu Maganbhai Patel, Thomas Paul Selby, Brenton Todd Smith, Andrew Edmund Taggi, Patrick Ryan Kovacs
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Publication number: 20120135979Abstract: Provided is a compound having a serotonin 5-HT2C receptor activating action, useful for lower urinary tract conditions, obesity and cancer. A compound represented by the formula (I0): wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: June 14, 2010Publication date: May 31, 2012Inventors: Shigekazu Sasaki, Tomokazu Kusumoto, Izumi Nomura, Hironobu Maezaki
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Publication number: 20120135980Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).Type: ApplicationFiled: December 18, 2009Publication date: May 31, 2012Inventors: Theodros Asberom, Zhaoning Zhu, John W. Clader, Zhong-Yue Sun, Mihirbaran Mandal, Gioconda Gallo, Xiaoxiang Liu
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Publication number: 20120135981Abstract: The present invention is concerned with novel substituted triazole and imidazole derivatives of Formula (I) wherein R1, R2, A1, A2, A3, A4, X, and Het1 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.Type: ApplicationFiled: July 13, 2010Publication date: May 31, 2012Inventors: Tongfei Wu, Henricus Jacobus Maria Gijsen, Frederik Jan Rita Rombouts, François Paul Bischoff, Didier Jean-Claude Berthelot, Daniel Oehlrich, Michel Anna Jozef De Cleyn, Serge Maria Aloysius Pieters, Garrett Berlond Minne, Adriana Ingrid Velter', Sven Franciscus Anna Van Brandt, Michel Surkyn
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Publication number: 20120122843Abstract: The present invention relates to novel compounds of formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising said compounds, processes for making said compounds, and their use as medicaments for treatment and/or prevention of A?-related diseases.Type: ApplicationFiled: November 9, 2011Publication date: May 17, 2012Applicant: ASTRAZENECA ABInventors: István MACSÁRI, Kim PAULSEN, Laszlo RAKOS, Britt-Marie SWAHN, Magnus WALDMAN, Didier ROTTICCI, Stefan VON BERG
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Publication number: 20120114588Abstract: The present invention regards specific IBAT inhibitors with improved effect in prophylaxis and treatment of metabolic syndrome, obesity, disorders of fatty acid metabolism, glucose utilization disorders, disorders in which insulin resistance is involved, diabetes mellitus, type 1 and type 2 diabetes. It also relates to compositions comprising these IBAT inhibitors, a method for treatment of the disorders and a kit comprising the substances or the compositions.Type: ApplicationFiled: May 26, 2011Publication date: May 10, 2012Applicant: ALBIREO ABInventors: Ingemar Starke, Hans Graffner, Per-Göran Gillberg, Ann-Margret Lindqvist, Bo Angelin
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Publication number: 20120101085Abstract: The present teachings provide compounds of Formulae I and II: and pharmaceutically acceptable salts, hydrates, complexes, esters, and prodrugs thereof, wherein R1, R1?, R2, R2?, R3, R3?, and X are as defined herein. The present teachings also provide methods of making the compounds of formulae I and II, and methods of treating RyR-associated conditions, disorders, and diseases that include administering a therapeutically effective amount of a compound of formula I or II to a subject in need thereof. In addition, the present teachings relate to methods of reducing the open probability of a ryanodine receptor, and methods of reducing Ca2+ release across a ryanodine receptor (e.g., into the cytoplasm of a cell), by contacting a compound of formula I or II with a ryanodine receptor.Type: ApplicationFiled: April 15, 2010Publication date: April 26, 2012Applicant: State of Oregon By and Through the State Board of Higher Education on Behalf of Portland State Univ.Inventors: Jonathan J. Abramson, Robert Michael Stongin
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Patent number: 8158617Abstract: The present invention relates to a serotonin 5-HT2C receptor activator containing a compound represented by the formula wherein ring A is a 5- or 6-membered aromatic heterocycle optionally having substituent(s), and ring B is a 7- to 9-membered ring optionally having substituent(s) other than an oxo group wherein the combination of m and n (m,n) is (1,2), (2,1), (2,2), (3,1), (3,2) or (4,1), or a salt thereof or a prodrug thereof, and a fused heterocyclic compound having a serotonin 5-HT2C receptor activating action and the like.Type: GrantFiled: May 15, 2007Date of Patent: April 17, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Junya Shirai, Tomokazu Kusumoto, Hiroyuki Nagamiya
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Publication number: 20120071462Abstract: Compounds of formula (I): wherein R1 represents a hydrogen atom or a heterocyclic, cyano, alkoxycarbonyl, alkylsulphonylaminoalkyl or N-hydroxycarboximidamide group. Medicinal products containing the same which are useful as modulators of the AMPA receptor.Type: ApplicationFiled: September 15, 2011Publication date: March 22, 2012Applicant: LES LABORATOIRES SERVIERInventors: Alexis Cordi, Patrice Desos, Pierre Lestage, Laurence Danober
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Publication number: 20120015930Abstract: The present invention provides substituted imidazoheterocycles having the general structure of formula I: wherein Y is chosen from —O—, —OCRgRh—, —CRgRhO—, —CRgRh—, —(CRgRh)2—, —NRi—, —CRgRhNRi— and —NRiCRgRh—. Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.Type: ApplicationFiled: December 1, 2009Publication date: January 19, 2012Applicant: CARA THERAPEUTICS, INC.Inventors: Stephen J. O'Connor, Jason S. Newcom, Janet L. Ralbovsky, Gary R. Gustafson, R. Paul Beckett, Robert Zhiyong Luo
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Publication number: 20120010193Abstract: Compounds of Formula (I) (wherein variables A1, A2, A3, ring-B, m, n, J, E1, E2, E3, R5, RPG and Y are as described herein), which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and the use of these compounds and compositions in the prevention or treatment of diseases in which CGRP receptors are involved.Type: ApplicationFiled: March 8, 2010Publication date: January 12, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: Craig A. Stump, Amy G. Quigley, Cory R. Theberge, Michael R. Wood
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Publication number: 20110312937Abstract: This invention relates to compounds of the formula wherein A, B and R1 to R7 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE1 and/or BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as Alzheimer's disease, diabetes, particularly type 2 diabetes, and other metabolic disorders.Type: ApplicationFiled: April 28, 2011Publication date: December 22, 2011Inventors: David Banner, Wolfgang Guba, Hans Hilpert, Roland Humm, Harald Mauser, Alexander V. Mayweg, Robert Narquizian, Eoin Power, Mark Rogers-Evans, Didier Rombach, Thomas Woltering, Wolfgang Wostl
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Publication number: 20110306594Abstract: Provided are novel compound that is useful as a treatment agent or a prophylactic agent for cardiac failure, cardiac failure due to dystelectasis, left ventricular diastolic impairment, angina or cardiac infarct, hypertension, ischemic cardiac disease, and myocardial relaxation impairment recognized in cardiac failure, atrial fibrillation or ventricular arrhythmia, and a pharmaceutical composition containing the same. The invention pertains to a 1,4-benzothiazepine-1-oxide derivative represented by general formula [I] (In the formula, R represents a hydrogen atom or a hydroxyl group.) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same [I].Type: ApplicationFiled: February 24, 2010Publication date: December 15, 2011Inventors: Noboru Kaneko, Mitsuru Takahashi
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Patent number: 8076322Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n1, n2, n3, n4, A, B, D, E, G, Y, Z, R1 and R2 are defined herein.Type: GrantFiled: February 8, 2011Date of Patent: December 13, 2011Assignee: Bristol-Myers Squibb CompanyInventors: John M. Fevig, Dean A. Wacker
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Publication number: 20110294784Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).Type: ApplicationFiled: December 18, 2009Publication date: December 1, 2011Inventors: Theodros Asberom, Xianhai Huang, Zhaoning Zhu, John Clader, Dmitri Pissarnitski, Hubert Josien, Hongmei Li
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Publication number: 20110288291Abstract: Provided is a compound having a serotonin 5-HT2C receptor activating action. A compound represented by the formula (I0): wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: July 28, 2011Publication date: November 24, 2011Inventors: Shigekazu SASAKI, Tomokazu Kusumoto
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Publication number: 20110282054Abstract: Provided is a compound having a serotonin 5-HT2C receptor activating action. A compound represented by the formula (I0): wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: July 28, 2011Publication date: November 17, 2011Inventors: Shigekazu SASAKI, Tomokazu Kusumoto
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Publication number: 20110269743Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: September 22, 2009Publication date: November 3, 2011Applicant: CalciMedica, IncInventors: Jeffrey P. Whitten, Yazhong Pei, Kenneth A. Stauderman, Jack Roos
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Publication number: 20110263569Abstract: Increasing the affinity of calstabin-2 for the cardiac calcium channel RyR2 and thereby stabilizing the channel in the closed state has recently been identified as novel mechanism for treating heart failure, particularly ventricular arrhythmias. JTV-519, a 1,4-benzothiazepine derivative, has been shown to stabilize the calstabin2/RyR2 complex. Novel derivatives of JTV-519 that may be useful in treatment or prevention of heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmias are provided. Synthetic methodology and intermediates in the synthesis of the inventive JTV-519 derivatives are also described.Type: ApplicationFiled: August 21, 2008Publication date: October 27, 2011Inventor: Elias James Corey
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Publication number: 20110263567Abstract: The present invention relates to compounds of general formula (i) having an oxime moiety or a pharmaceutically acceptable salt, hydrate or solvate thereof and its use for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1), a pharmaceutical composition comprising the compound or a salt, hydrate or solvate thereof as an active ingredient, a method for the prevention or the treatment of a SSAO/VAP-1 related disease, said diseases including acute or chronic inflammatory diseases, diseases related to carbohydrate metabolism, diabetes-associated complications, diabetic retinopathy and macular oedema, diseases related to adipocyte or smooth muscle dysfunctions, neurodegenerative diseases and vascular diseases.Type: ApplicationFiled: September 11, 2009Publication date: October 27, 2011Applicant: Semmelweis EgyetemInventors: Péter Mátyus, Kálmán Magyar, Marjo Pihlavisto, Klára Gyires, Norbert Haider, Yinghua Wang, Patrick Woda, Petra Dunkel, Éva Tóth-Sarudy, Gÿorgy Túrós
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Patent number: 8039458Abstract: The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: GrantFiled: October 31, 2006Date of Patent: October 18, 2011Assignee: Bristol-Myers Squibb CompanyInventors: B. Narasimhulu Naidu, Yasutsugu Ueda, John D. Matiskella, Michael A. Walker, Jacques Banville, Francis Beaulieu, Carl Ouellet, Serge Plamondon
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Patent number: 8022058Abstract: The present invention provides novel compounds of Formula I and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The invention additionally provides pharmaceutical compositions comprising the compounds of Formula I and methods of using the pharmaceutical compositions of Formula I to treat and prevent disorders and diseases associated with the RyR receptors that regulate calcium channel functioning in cells. Such disorders and diseases include, by way of example only, cardiac disorders and diseases, skeletal muscular disorders and diseases, cognitive disorders and diseases, malignant hyperthermia, diabetes, and sudden infant death syndrome.Type: GrantFiled: August 25, 2005Date of Patent: September 20, 2011Assignee: The Trustees of Columbia University in the City of New YorkInventors: Andrew Robert Marks, Donald W. Landry, Shixian Deng
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Patent number: 7981879Abstract: Compounds of Formula I are inhibitors of FHV integrase and inhibitors of FHV replication (I), wherein m, n, X, R1, R2, R3, R4, R5, R6, R7; R8, R9 and R10 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HTV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HTV infection and ADDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: March 22, 2006Date of Patent: July 19, 2011Assignee: Instituto di Ricerchi di Biologia Molecolare P. Angeletti S.p.A.Inventors: Vincenzo Summa, Paola Pace
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Publication number: 20110172190Abstract: The present invention provides compounds of Formula I and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The invention additionally provides pharmaceutical compositions comprising the compounds of Formula I and methods of using the pharmaceutical compositions of Formula I to treat and prevent disorders and diseases associated with the RyR receptors that regulate calcium channel functioning in cells.Type: ApplicationFiled: November 2, 2010Publication date: July 14, 2011Inventors: Andrew Robert Marks, Donald W. Landry, Shixian Deng
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Publication number: 20110152247Abstract: The invention provides a novel benzoxazepine compound of the general formula (I): wherein R1 and R2 are as defined in the specification; or a stereoisomer, a geometric isomer, a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate, or a polymorph thereof; a process for its preparation; and a pharmaceutical composition including an effective amount of the compound. The compounds are useful in the treatment of insulin resistance and clinical conditions associated therewith.Type: ApplicationFiled: November 1, 2007Publication date: June 23, 2011Inventors: Swati Bal-Tembe, Bansi Lal, Satish Namdeo Sawant, Anagha Suhas Kulkarni
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Publication number: 20110136782Abstract: The present invention provides a nitrogen-containing heterocyclic compound represented by formula (I) and salt thereof (wherein, R1 to R6 each independently represents a hydrogen atom, unsubstituted or substituted C1-20 alkyl group and the like, R1 and R2, R3 and R4, or R5 and R6 may together form an unsubstituted or substituted 5- to 8-membered ring, A-B, in which A represents a carbon atom and B represents a nitrogen atom, represents the formula: C?N and the like, Y represents an oxygen atom and the like, X and X? each independently represent an unsubstituted or substituted C1-20 alkyl group and the like, m represents an integer of 0 to 2, and n represents an integer of 0 to 4), and a fungicide for agricultural and horticultural use that contains at least one of these compounds as an active ingredient thereof, demonstrates reliable effects and can be used safely.Type: ApplicationFiled: August 10, 2009Publication date: June 9, 2011Applicant: Nippon Soda Co., LtdInventors: Akira Mitani, Jun Inagaki, Raito Kuwahara, Masahiro Yokoyama, Kotaro Shibayama, Motoaki Sato
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Publication number: 20110135601Abstract: The invention relates to a compound of a general formula (I): wherein A1 and A2 each mean a nitrogen atom or an optionally-substituted methine group; Ring B means a 5-membered to 7-membered aliphatic ring, or a spiro or bicyclo ring formed from the aliphatic ring and any other 3-membered to 7-membered aliphatic ring; R1 means a hydrogen atom, or an optionally-substituted C1-C6 alkyl group, or an optionally-substituted aryl, aralkyl or heteroaryl group; R2 means an optionally-substituted aryl, aralkyl or heteroaryl group; and X means a group of ?NH or ?O, etc. Based on its excellent Wee1 kinase-inhibitory effect, the compound of the invention has cell growth-inhibitory effect and has an additive/synergistic effect with any other anticancer agent, and is therefore useful in the field of medicine.Type: ApplicationFiled: June 12, 2008Publication date: June 9, 2011Inventor: Makoto Bamba
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Publication number: 20110136783Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n1, n2, n3, n4, A, B, D, E, G, Y, Z, R1 and R2 are defined herein.Type: ApplicationFiled: February 8, 2011Publication date: June 9, 2011Inventors: John M. Fevig, Dean A. Wacker
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Patent number: 7943607Abstract: Compounds of formula (I), wherein R1, R4, HET-1 and HET-2 are as described in the specification, and their salts and pro-drugs, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.Type: GrantFiled: May 23, 2006Date of Patent: May 17, 2011Assignee: AstraZeneca ABInventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
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Publication number: 20110112068Abstract: The described invention relates to novel human immunodeficiency virus protease inhibitors, pharmaceutical compositions containing at least one such inhibitor, methods of preparing such inhibitors, and methods of utilizing such inhibitors to treat HIV and HIV-related disorders.Type: ApplicationFiled: November 10, 2009Publication date: May 12, 2011Inventors: A.K. Ganguly, Dipshikha Biswas, Sesha Sridevi Alluri, Danielle Caroccia, Chih-Hung Wang, Eun Hee Kang
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Publication number: 20110082294Abstract: The invention is concerned with novel bicyclic compounds of formula (I), wherein A, L, E, F, G, R1, R2, R3, R4, R5, R6, R7, V, W and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor and can be used as medicaments.Type: ApplicationFiled: September 29, 2010Publication date: April 7, 2011Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei
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Publication number: 20110046112Abstract: The invention is concerned with novel heterobicyclic derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, V, W, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.Type: ApplicationFiled: November 8, 2010Publication date: February 24, 2011Inventors: Jean Ackermann, Konrad Bleicher, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei, Ulrike Obst Sander
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Patent number: 7879840Abstract: The present invention provides compounds of Formula I and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The invention additionally provides pharmaceutical compositions comprising the compounds of Formula I and methods of using the pharmaceutical compositions of Formula I to treat and prevent disorders and diseases associated with the RyR receptors that regulate calcium channel functioning in cells.Type: GrantFiled: August 17, 2006Date of Patent: February 1, 2011Assignee: The Trustees of Columbia University in the City of New YorkInventors: Andrew Robert Marks, Donald W. Landry, Shixian Deng
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Publication number: 20110015176Abstract: The disclosure relates to a series pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: Y, Z, R1, R2, R3, R4 and n are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.Type: ApplicationFiled: July 27, 2010Publication date: January 20, 2011Applicants: SANOFI-AVENTIS, MITSUBISHI TANABE PHARMA CORPORATIONInventors: Aude FAYOL, Alistair LOCHEAD, Mourad SAADY, Julien VACHE, Philippe YAICHE
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Publication number: 20110015158Abstract: The presently disclosed subject matter is described to metalloenzyme inhibitors having metal binding moieties linked to a targeting moiety through a linking group or a direct bond, method of screening for metalloenzyme inhibitors, and methods for treating a metalloenzyme related disorder by administering a metalloenzyme inhibitor to a subject in need of treatment thereof.Type: ApplicationFiled: December 3, 2008Publication date: January 20, 2011Applicant: Viamet Pharmaceuticals, Inc.Inventors: Robert J. Schotzinger, William J. Hoekstra
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Publication number: 20110015177Abstract: The disclosure relates to a series pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: Y, Z, R1, R2, R3, R4 and n are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.Type: ApplicationFiled: July 27, 2010Publication date: January 20, 2011Applicants: SANOFI-AVENTIS, MITSUBISHI TANABE PHARMA CORPORATIONInventors: Aude FAYOL, Alistair LOCHEAD, Mourad SAADY, Julien VACHE, Philippe YAICHE
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Publication number: 20100317651Abstract: Provided is a compound having a serotonin 5-HT2C receptor activating action. A compound represented by the formula (I0): wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: June 14, 2010Publication date: December 16, 2010Inventors: Shigekazu Sasaki, Tomokazu Kusumoto, Izumi Nomura, Hironobu Maezaki
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Publication number: 20100305093Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.Type: ApplicationFiled: April 8, 2010Publication date: December 2, 2010Applicant: EXELIXIS, INC.Inventors: Neel Kumar Anand, Arlyn Arcalas, Charles M. Blazey, Chris A. Buhr, Jonah Cannoy, Sergey Ephsteyn, Henry William Beecroft Johnson, Anagha Joshi, Byung Gyu Kim, James W. Leahy, Matthew Sangyup Lee, Sunghoon Ma, Morrison B. Mac, John M. Nuss, Craig Stacy Takeuchi, Longcheng Wang, Yong Wang
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Publication number: 20100298290Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.Type: ApplicationFiled: May 20, 2010Publication date: November 25, 2010Applicant: EXELIXIS, INC.Inventors: Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Chris Allen Buhr, Joerg Bussenius, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Jason R. Harris, Eileen E. Jackson-Ugueto, Anagha Joshi, Angie Inyoung Kim, Amy Lew Tsuhako, Sunghoon Ma, Jean-Claire Limun Manalo, Stephanie Ng, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang, Cristiana A. Zaharia
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Publication number: 20100292210Abstract: The present invention relates to novel compounds of formulae I and II and therapeutically acceptable salts thereof, their pharmaceutical compositions processes for making them and their use in therapeutic methods for treatment and/or prevention of various diseases. In particular, the invention relates to compounds which interfere with ?-secretase and/or its substrate and hence modulate the formation of A? peptides.Type: ApplicationFiled: May 11, 2010Publication date: November 18, 2010Applicant: AstraZeneca ABInventors: Yvonne Lo-Alfredsson, Kim Paulsen, Laszlo Rakos, Didier Rotticci, Magnus Waldman
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Publication number: 20100286120Abstract: The present invention provides a compound having a superior serotonin 5-HT2C receptor activating action, which is represented by the formula wherein A is —OR1 or —S(O)pR2, R1 and R2 are the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), or a heterocyclic group to optionally having substituent(s), and p is 0, 1 or 2, or a salt thereof.Type: ApplicationFiled: November 14, 2008Publication date: November 11, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Takahiro Matsumoto, Tomokazu Kusumoto
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Publication number: 20100273772Abstract: Disclosed are compounds of Formula I: pharmaceutical compositions containing compounds of Formula I, and the use of compounds of Formula I to treat diseases and disorders including schizophrenia, paranoia, depression, manic-depressive illness and anxiety wherein W1-W5, X1-X4, Y, Z1-Z5, m, n, p, and R1-R6 in Formula I are defined in the specification.Type: ApplicationFiled: April 22, 2010Publication date: October 28, 2010Applicant: Wyeth LLCInventors: Steven Victor O'Neil, Benjamin Miller Zegarelli, Dane Mark Springer, David Zenan Li
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Publication number: 20100273770Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.Type: ApplicationFiled: December 19, 2008Publication date: October 28, 2010Inventors: Jag Paul Heer, Thomas Daniel Heightman, David Nigel Hurst, Christopher Norbert Johnson, John Skidmore, Ian David Wall
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Publication number: 20100273771Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.Type: ApplicationFiled: December 19, 2008Publication date: October 28, 2010Inventors: Emmanuel Hubert Demont, Jag Paul Heer, John Skidmore, Ian David Wall, Jason Witherington, Thomas Daniel Heightman, David Nigel Hurst, Christopher Norbert Johnson