Nitrogen Or -c(=x)-, Wherein X Is Chalcogen, Attached Directly To The Five- Membered Ring By Nonionic Bonding Patents (Class 546/279.1)
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Publication number: 20120270877Abstract: The invention provides compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.Type: ApplicationFiled: November 1, 2010Publication date: October 25, 2012Applicant: MannKind CorporationInventors: Qingping Zeng, Warren S. Wade, John Bruce Patterson
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Patent number: 8288538Abstract: A compound represented by the following formula, or a salt thereof or a hydrate of the foregoing, has excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity, and cancer metastasis inhibitory activity. R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents —CH?, nitrogen or the like.Type: GrantFiled: September 14, 2009Date of Patent: October 16, 2012Assignee: Eisai R&D Management Co., Ltd.Inventors: Tomohiro Matsushima, Keiko Takahashi, Setsuo Funasaka, Hiroshi Obaishi, Shuji Shirotori
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Patent number: 8288556Abstract: Compounds of Formulas 1 and 2 where the variables have the meaning disclosed in the specification, have analgesic and in some cases immunostimulant activity.Type: GrantFiled: January 25, 2006Date of Patent: October 16, 2012Assignees: Allergan, Inc., Exonhit Therapeutics SAInventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello
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Publication number: 20120252670Abstract: Compounds of the formula (I), or salts thereof, in which R1 to R4 are as defined in formula (I) of claim 1 are suitable as useful-plant-protecting agents for reducing or preventing harmful effects of agrochemicals on the useful plants and their method of preparation are described.Type: ApplicationFiled: June 14, 2012Publication date: October 4, 2012Inventors: Frank ZIEMER, Lothar Willms, Christopher Rosinger, Thomas Auler, Erwin Hacker, Udo Bickers
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Publication number: 20120232049Abstract: A pyridine or pyrimidine derivative represented by the formula (I) has an excellent HGFR inhibitory activity and exhibits strong cell proliferation inhibitory effect and anti-tumor effect against cancer cell lines with amplified HGFR gene. wherein R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents —CH?, nitrogen.Type: ApplicationFiled: February 22, 2008Publication date: September 13, 2012Applicant: Eisai R&D Management Co., Ltd.Inventors: Hiroshi Obaishi, Takayuki Nakagawa, Tomohiro Matsushima, Setsuo Funasaka, Shuji Shirotori, Keiko Takahashi
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Patent number: 8258141Abstract: A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.Type: GrantFiled: April 19, 2007Date of Patent: September 4, 2012Assignee: Novartis AGInventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
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Publication number: 20120220590Abstract: Compounds of formula (I) and pharmaceutical compositions containing them are described. The use of the compounds and compositions are also described.Type: ApplicationFiled: July 30, 2010Publication date: August 30, 2012Inventors: Pravin S. Thombare, Amitgiri Goswami, Edouard Zamaratski, Tomas Hansson, Thomas Norin
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Publication number: 20120196885Abstract: The present invention refers to compounds derived from trisubstituted 1H-pyrrole rings and aromatic rings, which have the following formula (I): wherein: R1 and R2 represent, independently, an optionally substituted C6-C10 aryl radical or an optionally substituted heteroaryl radical; A and M represent, independently, a methylene group or a single bond, in which case the adjacent aromatic ring would be attached directly to the amide group; the Y?Z group represents together and indistinctly an oxygen atom, a sulfur atom, a cis-vinylidene group, an imino group, or a methine group with a sp2-hybridized carbon atom; X represents indistinctly a methine group, a cis-vinylidene group or a nitrogen atom; and W represents a hydroxyl group, an optionally substituted C1-C6 alkyl group, an optionally substituted heteroaryl group or an optionally substituted C6-C10 aryl group; or a salt, solvate or prodrug thereof, as well as to the process for their preparation and the use thereof for the treatment of cancer.Type: ApplicationFiled: October 1, 2010Publication date: August 2, 2012Applicant: IKERCHEM, S.L.Inventors: Fernando Pedro Cossío Mora, Aizpea Zubia Olascoaga, Yosu Vara Salazar, Eider Ion San Sebastián Larzabal, Dorleta Otaegui Ansa, María del Carmen Masdeu Margalef, Eneko Aldaba Arévalo
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Patent number: 8222274Abstract: [Problem] To provide a compound which may be used for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS). [Means for Resolution] It was found that a pyrrole derivative characterized by the possession of a guanidinocarbonyl group or amido group as a substituent group at the 3-position, or a pharmaceutically acceptable salt thereof, has a strong antagonism for both of the 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having the antagonistic activity for both of the receptors showed a good pharmacological action in comparison with the case in which an antagonist selective for either one of the receptors was used alone. Based on the above, the compound of the present invention is useful for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).Type: GrantFiled: February 19, 2007Date of Patent: July 17, 2012Assignee: Astellas Pharma Inc.Inventors: Ryushi Seo, Hidetaka Kaku, Hiroyoshi Yamada, Daisuke Kaga, Shinobu Akuzawa
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Publication number: 20120157433Abstract: The present invention provides a compound of Formula (I): and pharmaceutically acceptable salts thereof. Also provided is a method of using a compound of Formula I for treating a disease or condition mediated by a CDK inhibitor.Type: ApplicationFiled: September 2, 2010Publication date: June 21, 2012Inventors: Keith B. Pfister, Martin Sendzik
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Publication number: 20120142677Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: December 15, 2009Publication date: June 7, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Angela Berry, Rajashekhar Betageri, Eugene Richard Hickey, Someina Khok, Doris Riether, Lifen Wu, Renee M. Zindell
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Publication number: 20120142698Abstract: The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R10R11)—C(?O)—, x-C(R12R13)—C(?S)—, x-O—C(?O)—, x-O—C(?S)—, x-N(R14)—C(?O)—, x-N(R15)—C(?S)—, x-C(R16R17)—SO2— or X—N?C(R30)—, in each case x indicates the bond that is connected to R1; T is CR18 or N; Y1, Y2, Y3, and Y4 are independently CR19 or N; Q is O or S; n is 1 or 2; p is 1 or 2, providing that when n is 2, p is 1.Type: ApplicationFiled: August 6, 2010Publication date: June 7, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Sarah Sulzer-Mosse, Clemens Lamberth, Laura Quaranta, Mathias Stephan Respondek
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Publication number: 20120142691Abstract: The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.Type: ApplicationFiled: August 4, 2010Publication date: June 7, 2012Inventors: Hirohide Noguchi, Tadashi Inoue, Mikio Morita, Yoshimasa Arano
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Publication number: 20120116075Abstract: An acrylamide derivative represented by formula (I), pharmaceutically acceptable salts and solvates thereof, as well as a medicament containing said acrylamide derivative or its pharmaceutically acceptable salts as the active ingredient, which can be used to treat disorders associated with tyrosine kinase especially Bcr-Abl, including proliferative disorders such as cancers, and inflammation and the like are provided.Type: ApplicationFiled: April 27, 2010Publication date: May 10, 2012Applicants: BEIJING JIASHILIANBO PHARM SCI & TECH CO. LTD, BEIJING SHIQIAO BIOPHARM CO. LTDInventor: Shuping Sun
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Patent number: 8173683Abstract: Disclosed herein are methods of treating a patient suffering a cognitive disorder.Type: GrantFiled: February 26, 2008Date of Patent: May 8, 2012Assignees: Allergan, Inc., ExonHit Therapeutics SAInventors: John E. Donello, Fabien J. Schweighoffer, Lauren M. Luhrs
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Publication number: 20120101080Abstract: The invention relates to a pharmaceutical composition comprising a compound of formula (1) wherein R1 is optionally substituted phenyl, optionally substituted pyridyl or optionally substituted indolyl; R2 is (CH2)n wherein n is 0, 1, 2, 3 or 4; R3 is (CH2)mR3A wherein m is 0, 1, 2, 3 or 4, and R3A is methyl, isopropyl, tert-butyl, OCH3, OH, optionally substituted phenoxy, C?CH, C?N, optionally substituted phenyl, furanyl or thienyl; A is a ring containing X1 with the meaning O, S, NH, N(CH3) or CH2; and X2 is O, S or NH; and a compound of formula (2) wherein R4 is optionally substituted phenyl, optionally substituted pyridyl, optionally substituted indolyl, —NR7R8; or —NH—N?CH—R9; and substituents R5 to R9 have the meanings indicated in the description, in particular ethionamide. The pharmaceutical composition is useful, e.g., in the treatment of multidrug-resistant tuberculosis.Type: ApplicationFiled: June 25, 2010Publication date: April 26, 2012Applicant: BioVersys AGInventors: Ronald Schoenmakers, Wilfried Weber, Marc Gitzinger, Martin Fussenegger, Marcel Tigges, Peter Schneider
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Patent number: 8158783Abstract: The present invention is concerned with novel tetrahydro-naphthalene-1-carboxylic acid derivatives having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes. Formula (I).Type: GrantFiled: October 22, 2007Date of Patent: April 17, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Meerpoel, Leo Jacobus Jozef Backx, Peter Ten Holte, Guuske Frederike Busscher
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Patent number: 8153666Abstract: The compounds shown by their structural formulas in the specification have analgesic and or immunostimulant activity in mammals.Type: GrantFiled: January 25, 2006Date of Patent: April 10, 2012Assignee: Allergan, Inc.Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello
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Publication number: 20120077793Abstract: The present invention is directed to therapeutic compounds which have activity as agonists of GPR119 and are useful for the treatment of metabolic disorders including type II diabetes.Type: ApplicationFiled: March 12, 2010Publication date: March 29, 2012Applicant: PROSIDION LIMITEDInventors: Oscar Barba, Peter Timothy Fry, Matthew Colin Thor Fyfe, William Gattrell, Revathy Perpetua Jeevaratnam, Thomas Martin Krulle, Martin James Procter, Colin Peter Sambrook-Smith, Karen Lesley Schofield, Donald Smyth, Alan John William Stewart, David French Stonehouse, Simon Andrew Swain
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Publication number: 20120065225Abstract: Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein m, n, Ar, R1, R2, Ra and Rb are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: ApplicationFiled: November 21, 2011Publication date: March 15, 2012Inventors: Pravin Iyer, Clara Jeou Jen Lin, Stephen M. Lynch, Matthew C. Lucas, Ann Marie Madera, Kerem Erol Ozboya, Robert James Weikert, Ryan Craig Schoenfeld
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Publication number: 20120041019Abstract: Compounds useful as protease inhibitors are provided, as are methods of use and preparation of such compounds and compositions containing such compounds. In one embodiment, the compounds are useful for inhibiting HIV protease enzymes, and are therefore useful in slowing the proliferation of HIV.Type: ApplicationFiled: December 17, 2009Publication date: February 16, 2012Inventors: Mitchell W. Mutz, Kenneth J. Barr, Jason Gestwicki
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Publication number: 20120035168Abstract: The invention relates to compound of the formula I in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.Type: ApplicationFiled: July 29, 2011Publication date: February 9, 2012Applicant: NOVARTIS AGInventors: Trixi BRANDL, Stefanie FLOHR, Sebastian KOPEC, Julie LACHAL, Christian MARKERT, Kenji NAMOTO, Perle NGANGA, Bernard PIRARD, Martin RENATUS, Richard SEDRANI, Thomas ZOLLER
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Publication number: 20120022255Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.Type: ApplicationFiled: March 23, 2010Publication date: January 26, 2012Inventors: Toshio Fujishita, Minako Mikamiyama, Makoto Kawai, Toshiyuki Akiyama
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Publication number: 20110319626Abstract: This invention relates to the discovery of novel atorvastatin analogues. More specifically, the invention relates to novel atorvastatin analogues which have utility in treating conditions treatable by the inhibition of HMG-CoA reductase.Type: ApplicationFiled: March 10, 2010Publication date: December 29, 2011Applicant: BRADFORD PHARMA LIMITEDInventors: Derek Lindsay, Peter Jackson
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Publication number: 20110318359Abstract: The present invention relates to methods of reducing blood pressure in a subject by administering a plasma kallikrein inhibitor.Type: ApplicationFiled: December 2, 2009Publication date: December 29, 2011Inventors: Edward P. Feener, Allen Clermont
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Publication number: 20110312996Abstract: The embodiments provide compounds of the general Formulae VI, VII, VIII, IX, X, XI, XII, XIII, XIV, and XV as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: ApplicationFiled: May 16, 2011Publication date: December 22, 2011Applicant: InterMune, Inc.Inventors: Brad Buckman, John B. Nicholas, Vladimir Serebryany, Scott D. Seiwert
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Publication number: 20110312974Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: September 28, 2009Publication date: December 22, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Brian Andrew Stearns, Nicholas Simone Stock, Yen Pham Truong, Jeffrey Roger Roppe, Deborah Volkots, Jill Melissa Scott, Timothy Andrew Parr, Bowei Wang, Thomas Jon Seiders, Ryan Clark, Heather Renee Coate
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Publication number: 20110294819Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.Type: ApplicationFiled: December 21, 2010Publication date: December 1, 2011Inventors: Omar D. Lopez, Denis R. St. Laurent, Jason Goodrich, Jeffrey Lee Romine, Michael Serrano-Wu, Fukang Yang, Ramesh Kakarla, Xuejie Yang, Yuping Qiu, Lawrence B. Snyder
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Publication number: 20110294827Abstract: IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPs (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in cells treated with such molecules. Embodiments of these compounds have a Kd of less that 0.1 micromolar. Methods of using these IAP binding molecules for therapeutic, diagnostic, and assay purposes are also disclosed.Type: ApplicationFiled: June 3, 2011Publication date: December 1, 2011Applicant: TETRALOGIC PHARMACEUTICALS CORPORATIONInventors: Stephen M. Condon, Matthew G. LaPorte, Yijun Deng, Susan R. Rippin
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Patent number: 8067442Abstract: Compounds having the formula I wherein R1, R2a, R2b, R2c, R3, Y and p are as defined herein and C2-C3 is a single or double bond are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: GrantFiled: September 25, 2009Date of Patent: November 29, 2011Assignee: Roche Palo Alto LLCInventors: Elbert Chin, Jim Li, Francisco Xavier Talamas, Beihan Wang
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Patent number: 8067457Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.Type: GrantFiled: October 26, 2006Date of Patent: November 29, 2011Assignee: Millennium Pharmaceuticals, Inc.Inventors: Shomir Ghosh, Prakash Raman, Kevin Sprott, Amy M. Elder, Sian Griffiths, Francois Soucy, Qing Ye
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Patent number: 8063078Abstract: Certain compounds of formula (I), or a pharmaceutically acceptable salt thereof, or a solvate thereof, wherein R1, R2, P, P?, n, p, q, r and s are as defined in the specification, a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and composition in medicine.Type: GrantFiled: September 13, 2002Date of Patent: November 22, 2011Assignee: GlaxoSmithKline LLCInventors: Harshad Kantilal Rami, Mervyn Thompson
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Publication number: 20110281875Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).Type: ApplicationFiled: July 8, 2011Publication date: November 17, 2011Inventors: Mark G. PALERMO, Sushil Kumar SHARMA, Christopher STRAUB, Run-Ming WANG, Leigh ZAWEL, Yanlin ZHANG, Zhuoliang CHEN, Yaping WANG, Fan YANG, Wojciech WRONA, Gang LIU, Mark G. CHAREST, Feng HE
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Patent number: 8044209Abstract: The present invention relates to novel IAP inhibitor compounds of: Formula (I).Type: GrantFiled: October 10, 2007Date of Patent: October 25, 2011Assignee: Novartis AGInventors: Mark G. Charest, Christine Hiu-Tung Chen, Ming Chen, Zhuoliang Chen, Miao Dai, Feng He, Huangshu Lei, Christopher Sean Straub, Run-Ming David Wang, Leigh Zawel
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Publication number: 20110251168Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: ApplicationFiled: June 16, 2011Publication date: October 13, 2011Inventors: Chu-Biao Xue, Brian W. Metcalf, Hao Feng, Ganfeng Cao, Taisheng Huang, Changsheng Zheng, Darius J. Robinson, Amy Qi Han
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Publication number: 20110245227Abstract: 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 Formula I or Formula IA.Type: ApplicationFiled: June 14, 2011Publication date: October 6, 2011Inventors: Dean A. Wacker, Karen A. Rossi, Ying Wang
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Publication number: 20110230419Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, solvates or prodrugs thereof, that bind to Inhibitor of Apoptosis Proteins (IAPs). The compounds of the invention may be used as diagnostic and therapeutic agents in the treatment of proliferative diseases, such as cancer, for promoting apoptosis in proliferating cells, and for sensitizing cells to inducers of apoptosis. The present invention furthermore provides a polymeric compound of formulas (VI) or (VII), comprising either at least two monomeric units of compounds of formula (I), or at least one monomeric unit of a compound of formula (I) and an entity E. The present invention further relates to pharmaceutical compositions comprising said compounds of formulas (I), (VI), and (VII) and the use of said compounds in medicine.Type: ApplicationFiled: June 16, 2009Publication date: September 22, 2011Applicant: Nuevolution A/SInventors: Mikkel Dybro Lundorf, Kim Birkebaek Jenson, Sanne Schrøder Glad, Alek Haahr Gouliaev, Anette Holtmann, Michael Anders Godskesen
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Publication number: 20110230498Abstract: This invention provides compounds of Formula (I) which are PAFR antagonists: Formula (I) and the pharmaceutically acceptable salts thereof. The compounds are useful for treating PAF-mediated disorders, and can be used in methods for treating atherosclerosis and preventing or reducing risk for atherosclerotic disease events. The compounds are also useful for treating or ameliorating pain, e.g. inflammatory pain and/or nociceptive pain, and for treating or ameliorating autoimmune and/or inflammatory diseases, among other conditions.Type: ApplicationFiled: December 8, 2009Publication date: September 22, 2011Inventors: Anthony Ogawa, Hyun O. Ok, Debra Ondeyka, Feroze Ujjainwalla, Ellen Vande Bunte
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Patent number: 8022096Abstract: Pyrrolidine compounds described herein and methods for using them to inhibit dipeptidyl peptidase IV and treat Type II diabetes.Type: GrantFiled: February 25, 2009Date of Patent: September 20, 2011Assignee: National Health Research InstitutesInventors: Weir-Torn Jiaang, Yu-Sheng Chao, Ting-Yueh Tsai, Tsu Hsu
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Patent number: 8017607Abstract: There are provided compounds of the formula wherein X, Y, R1, R2, R3, R3, R4, and R5 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof which are useful as anticancer agents.Type: GrantFiled: October 6, 2010Date of Patent: September 13, 2011Assignee: Hoffmann-La Roche Inc.Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Jin-Jun Liu, Tina Morgan Ross, Zhuming Zhang
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Publication number: 20110218160Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.Type: ApplicationFiled: May 12, 2011Publication date: September 8, 2011Inventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
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Publication number: 20110212965Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions. One aspect of the invention provides compounds of formula (1): in which T, A and X are as described herein.Type: ApplicationFiled: May 11, 2011Publication date: September 1, 2011Applicant: METHYLGENE INC.Inventors: Sylvie Frechette, Lubo Isakovic, Isabelle Paquin, Simon Roy, Oscar Moradei, Arkadii Vaisburg
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Patent number: 8008301Abstract: The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, which have histamine—H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds.Type: GrantFiled: November 2, 2009Date of Patent: August 30, 2011Assignee: Eli Lilly and CompanyInventors: Lisa Selsam Beavers, Don Richard Finley, Terry Patrick Finn, Robert Alan Gadski, Philip Arthur Hipskind, William Joseph Hornback, Cynthia Darshini Jesudason, Richard Todd Pickard, Takako Takakuwa, Grant Mathews Vaught
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Publication number: 20110207781Abstract: Compounds of Formula (I), in which the substituents are as defined in claim 1, are suitable for use as microbiocides.Type: ApplicationFiled: June 9, 2009Publication date: August 25, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Daniel Stierli, Harald Walter, Sebastian Wendeborn, Antoine Daina
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Publication number: 20110207771Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides.Type: ApplicationFiled: June 6, 2007Publication date: August 25, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Daniel Stierli, John J. Taylor, Harald Walter, Paul Anthony Worthington, Ramya Rajan
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Publication number: 20110190258Abstract: The present invention relates to substituted aryl-benzylamine compounds, to processes for their production, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: ApplicationFiled: January 28, 2011Publication date: August 4, 2011Applicant: NOVARTIS AGInventors: Daniela ANGST, Birgit BOLLBUCK, Philipp JANSER, Jean QUANCARD, Nikolaus Johannes STIEFL
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Publication number: 20110190297Abstract: The present invention relates to pyridine and pyrimidine based compounds, pharmaceutical compositions comprising these compounds and their potential use as therapeutic agents for the treatment and/or prevention of cancer.Type: ApplicationFiled: October 6, 2009Publication date: August 4, 2011Inventors: Edward McDonald, Julian Blagg, Mark Pichowicz, Simon Ross Crumpler
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Patent number: 7989459Abstract: A chemical genus of purinones and 1H-imidazopyridinones, which are useful as PKC?. inhibitors, and their methods of use are disclosed. The genus is represented by the formula I: wherein R1 is chosen from nitrogen-attached heterocyclyl, nitrogen-attached substituted heterocyclyl wherein the point of attachment is a nitrogen heteroatom, and R2 is chosen from aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroaryl, substituted heteroaryl, hetroarylalkyl, and substituted heteroarylalkyl.Type: GrantFiled: February 2, 2007Date of Patent: August 2, 2011Assignee: Pharmacopeia, LLCInventors: Andrew Roughton, Yajing Rong, Koc Kan Ho, Michael Ohlmeyer, David Diller
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Patent number: 7985730Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: GrantFiled: April 27, 2009Date of Patent: July 26, 2011Assignee: Incyte CorporationInventors: Chu-Biao Xue, Brian W. Metcalf, Hao Feng
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Publication number: 20110178101Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: January 18, 2011Publication date: July 21, 2011Inventors: Paul R. Fatheree, Robert Murray McKinnell