1,3-diazole Ring (including Hydrogenated) Patents (Class 544/370)
-
Publication number: 20120202775Abstract: Compounds having drug and bio-affecting properties are described herein, including their properties, pharmaceutical compositions and methods of use. In particular, tricyclic aryl or heteroaryl piperazine diamide derivatives that possess unique antiviral activity are set forth. These compounds are useful for the treatment of HIV and AIDS.Type: ApplicationFiled: August 4, 2011Publication date: August 9, 2012Inventors: Tao Wang, Zhongxing Zhang, Zhiwei Yin, John F. Kadow, Nicholas A. Meanwell
-
Publication number: 20120202794Abstract: Disclosed herein are compounds useful for treating a viral infection, such as HCV.Type: ApplicationFiled: January 19, 2012Publication date: August 9, 2012Applicant: PHARMASSET, INC.Inventors: MICHAEL JOSEPH SOFIA, RAMESH KAKARLA, JIAN LIU, DEVAN NADUTHAMBI, RALPH MOSLEY, HOLLY MICOLOCHICK STEUER
-
Patent number: 8236954Abstract: A process for preparing benzimidazole thiophenes including 5-{6-[(4-methylpiperazin-1-yl)methyl]-1H-benzimidazol-1-yl}-3-{(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy}thiophene-2-carboxamide.Type: GrantFiled: June 23, 2008Date of Patent: August 7, 2012Assignee: GlaxoSmithKline LLCInventors: Amanda Caroline Lucas, Robert M. Harris, Christopher James Nichols, Andrew Jonathan Whitehead
-
Publication number: 20120190673Abstract: The invention provides a compound of the formula (I): or a salt, solvate, tautomer or N-oxide thereof, wherein M is selected from a group D1 and a group D2: and R?, E, A and X are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, processes for making the compounds and the use of the compounds in the prophylaxis or treatment of a disease state mediated by a CDK kinase, GSK-3 kinase or Aurora kinase.Type: ApplicationFiled: December 19, 2011Publication date: July 26, 2012Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Valerio BERDINI, Maria Grazia CARR, Adrian Liam GILL, Steven HOWARD, Eva Figueroa NAVARRO, Gary TREWARTHA, David Charles REES, Mladen VINKOVIC, Paul Graham WYATT
-
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
-
Publication number: 20120184535Abstract: A compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine and tyrosine kinases and a serine/threonine and tyrosine kinases modulating agent. Novel small-molecule compounds with kinase inhibitory activity, having superior properties as pharmaceutical agents, production method thereof and uses thereof. In particular, new derivatives of tetrahalogenated benzimidazole with serine/threonine and tyrosine kinases inhibitory properties, preferably selected from the group of PIM, HIPK, DYRK, CLK, CDK, FLT, PKG, Haspin, MER, TAO, MNK, TRK kinases which exhibit superior pharmacological actions, and can be useful for the treatment of disease conditions, especially cancers depending on serine/threonine and tyrosine kinases, such as but not limited to leukemias and solid tumors.Type: ApplicationFiled: December 28, 2011Publication date: July 19, 2012Applicant: SELVITA S.A.Inventors: Krzysztof BRZÓZKA, Wojciech CZARDYBON, Aleksandra SABINIARZ, Mariusz MILLIK, Renata WINDAK, Adrian ZAREBSKI, Nicolas BEUZEN
-
Patent number: 8222413Abstract: A method for synthesizing a heterocyclic compound includes: reacting 1-methylpiperazine with 5-chloro-2-nitroaniline at an internal temperature sufficient to provide a compound of Formula VIH The 1-methylpiperazine and the 5-chloro-2-nitroaniline are reacted in a solvent that comprises water in an amount greater than 50 percent by volume based on the amount of the solvent and/or are reacted in a solvent that comprises an organic solvent component that has a boiling point of greater than 100° C. at atmospheric pressure.Type: GrantFiled: May 17, 2006Date of Patent: July 17, 2012Assignee: Novartis AGInventors: Gabriel Galvin, Eric Harwood, David Ryckman, Shuguang Zhu
-
Patent number: 8221737Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: June 15, 2010Date of Patent: July 17, 2012Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Xiaowen Peng, Lu Ying, Ce Wang, Yao-Ling Qiu
-
Publication number: 20120177712Abstract: This invention relates to a bipolar antimicrobial particle for use in laundry detergent compositions, fabric conditioners, personal care and cosmetic compositions and a process for making the same. In view of the foregoing, it is an object of the present invention to provide a stabile antimicrobial agent immobilised on a carrier particle. It is a further objective to provide an antimicrobial particle with improved retention to the fabric so that larger amounts of antimicrobial will be available even after rinsing. Surprisingly it has been found that antimicrobial molecules tagged by surface reaction onto naturally occurring asymmetric clay surfaces, act as an antimicrobial particle with improved retention properties with improved stability.Type: ApplicationFiled: August 30, 2010Publication date: July 12, 2012Inventors: Arpita Bhattacharya, Sudipta Ghosh Dastidar, Vidula Iyer, Suresh Sambamurthy Jayaraman, Maya Treesa Saji
-
Publication number: 20120172364Abstract: Rate-controlled particles, comprising compounds of the formula as a solid dispersion.Type: ApplicationFiled: March 14, 2012Publication date: July 5, 2012Inventors: Thomas Hantke, Bettina Rehbock, Jörg Rosenberg, Jörg Breitenbach
-
Publication number: 20120157463Abstract: The present invention relates to chromone derivatives, their preparation, their pharmaceutical compositions and their application as D3 dopaminergic ligands as a medicament for disorders of the central nervous system.Type: ApplicationFiled: August 31, 2010Publication date: June 21, 2012Applicant: PIERRE FABRE MEDICAMENTInventors: Pierre Sokoloff, Thierry Imbert, Jean-François Patoiseau, Jean-Pierre Rieu
-
Publication number: 20120149676Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.Type: ApplicationFiled: December 8, 2011Publication date: June 14, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Henri DOODS, Alexander HEIM-RIETHER, Raimund KUELZER, Roland PFAU, Klaus RUDOLF, Dirk STENKAMP
-
Publication number: 20120135997Abstract: The present invention provides, for example, the following compounds as a pharmaceutical composition for treating diseases induced by production, secretion or deposition of amyloid ? proteins. The present invention provides a pharmaceutical composition for suppressing amyloid ? production comprising a compound of the formula: wherein A is a benzene ring, a pyridine ring or a pyrimidine ring, X is sultam, lactam, sulfonamide or the like, C is substituted or unsubstituted imidazolyl, substituted or unsubstituted oxazolyl or the like, R2, R3 and R4 are each independently hydrogen, halogen, hydroxy, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy or the like, its pharmaceutically acceptable salt or a solvate thereof.Type: ApplicationFiled: July 15, 2010Publication date: May 31, 2012Applicant: Shionogi & Co., Ltd.Inventors: Issei Kato, Kazuya Kano
-
Publication number: 20120129870Abstract: The present invention is directed to piperidinyl and piperazinyl derivatives of formula (II) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds for the treatment and/or prevention of disorders, diseases and conditions mediated by the NPY Y2 receptor.Type: ApplicationFiled: December 17, 2008Publication date: May 24, 2012Inventors: Wenying Chai, Jill A. Jablonowski, Dale A. Rudolph, Chandravadan R. Shah, Devin M. Swanson, Victoria D. Wong
-
Publication number: 20120122883Abstract: The present invention relates to new crystalline salt forms of flibanserine which have valuable pharmacological properties, to a process for their manufacture, to pharmaceutical formulations containing them and to their use as medicament.Type: ApplicationFiled: December 14, 2009Publication date: May 17, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Jaroslaw Mazurek, Mihaela Pop
-
Patent number: 8178693Abstract: Disclosed are compounds of the Formula and pharmaceutically acceptable salts and prodrugs thereof, wherein A, R1, R2, R7, R8, and R9 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.Type: GrantFiled: June 28, 2010Date of Patent: May 15, 2012Assignee: Array Biopharma Inc.Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley
-
Publication number: 20120115881Abstract: A novel arylpiperazine-containing imidazole 4-carboxamide derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same as an active ingredient for preventing or treating a depressive disorder are provided.Type: ApplicationFiled: July 9, 2010Publication date: May 10, 2012Applicant: GREEN CROSS CORPORATIONInventors: Jinhwa Lee, Hee Jeong Seo, Suk Youn Kang, Eun-Jung Park, Min Ju Kim, Suk Ho Lee, Jong yup Kim, Jeongmin Kim, Myung Eun Jung, Hyun Jung Kim, Mi-soon Kim, Ho kyun Han, Kwang Woo Ahn, Min Woo Lee, Ki-Nam Lee, Ae Nim Pae, Woo-Kyu Park
-
Publication number: 20120114600Abstract: The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of replication of the hepatitis C virus. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat hepatitis C viral infections, and processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: November 3, 2011Publication date: May 10, 2012Applicant: THERAVANCE, INC.Inventors: Robert Murray McKINNELL, Daniel D. LONG, Lori Jean VAN ORDEN, Lan JIANG, Mandy LOO, Daisuke Roland SAITO, Shella ZIPFEL, Eric L. Stangeland, Kassandra Lepack, Gavin Ogawa
-
Publication number: 20120088754Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: December 14, 2011Publication date: April 12, 2012Inventors: Kristof Van Emelen, Janine Arts, Leo-Jacobus Jozef Backx, Hans Louis Jos De Winter, Sven Franciscus Anna Van Brandt, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Isabelle Noëlle Constance Pilatte, Virginie Sophie Poncelet, Alexey Borisovich Dyatkin, Jimmy Arnold Viviene Van heusden
-
Publication number: 20120088752Abstract: Heterocyclic compounds that modulate the hedgehog signaling pathway, pharmaceutical composition thereof and their therapeutic applications.Type: ApplicationFiled: June 9, 2010Publication date: April 12, 2012Applicant: SIENA BIOTECH S.p.A.Inventors: J. Russell Thomas, Gal.la Pericot Mohr, Chiara Caramelli, Giacomo Minetto, Marta Bellini
-
Publication number: 20120088779Abstract: Certain substituted sulfonamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: ApplicationFiled: December 19, 2011Publication date: April 12, 2012Inventors: Bradley Paul MORGAN, Fady Malik, Erica Anne Kraynack, Alexander Ramon Muci, Xiangping Qian, David J. Morgans, JR.
-
Patent number: 8148363Abstract: The present invention relates to novel heterocyclic compounds of Formulae I-III; as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.Type: GrantFiled: May 18, 2009Date of Patent: April 3, 2012Assignee: Schering CorporationInventors: Martin C. Clasby, William J. Greenlee, Yan Xia, Tin-Yau Chan, Mariappan V. Chelliah, Samuel Chackalamannil, Haiyan Pu, Keith A. Eagen, Henry Vaccaro, Brian A. McKittrick, Liyuan Wang, Xiaobang Gao
-
Patent number: 8148367Abstract: Disclosed are compounds, pharmaceutical compositions, kits, articles of manufacture, methods of using, and methods of preparing compounds having the formula: wherein the variables are as defined herein. The disclosed compounds are inhibitors of Renin.Type: GrantFiled: January 9, 2008Date of Patent: April 3, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Lily Kwok, Betty Lam, Zhe Li, Zhiyuan Zhang
-
Publication number: 20120071489Abstract: The present invention relates to a compound represented by the formula wherein each symbol is as defined in the present specification, which has a superior RBP4-lowering action and is useful as a pharmaceutical composition for the prophylaxis or treatment of a disease or condition mediated by an increase in RBP4.Type: ApplicationFiled: April 16, 2010Publication date: March 22, 2012Inventors: Shizuo Kasai, Kevin Francis McGee, JR.
-
Patent number: 8138174Abstract: Compounds with a combination of cannabinoid CB1 antagonism and serotonin reuptake inhibition, pharmaceutical compositions containing these compounds, methods for preparing these compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing these compositions are disclosed. Uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in psychosis, anxiety, depression, attention deficits, cognitive disorders, obesity, drug dependence, Parkinson's disease, Alzheimer's disease, pain disorders, neuropathic pain disorders and sexual disorders are disclosed. In at least one embodiment, the invention relates to compounds of the general formula (1): wherein the substitutents have the definitions given in the specification.Type: GrantFiled: January 7, 2008Date of Patent: March 20, 2012Assignee: Solvay Pharmaceuticals B.V.Inventors: Josephus H. M. Lange, Cornelis G. Kruse
-
Publication number: 20120065193Abstract: Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method of using at least one cyclopropyl amide derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith.Type: ApplicationFiled: November 21, 2011Publication date: March 15, 2012Inventors: James Arnold, Andrew Todd Brugel, Scott Throner, Steven Wesolowski, Phil Edwards, Andrew Griffin, Thierry Groblewski, Denis Labrecque
-
Patent number: 8129527Abstract: Compounds represented by the following structure (II) are disclosed: as are methods for making such compounds. Compositions and methods for treating various disease conditions including cancer and non-cancer diseases associated with vascular proliferation are also disclosed.Type: GrantFiled: November 2, 2007Date of Patent: March 6, 2012Assignee: Nereus Pharmacuticals, Inc.Inventors: Michael A. Palladino, George Kenneth Lloyd, Yoshio Hayashi
-
Patent number: 8129393Abstract: Compounds of general formula: as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain, depression and anxiety.Type: GrantFiled: December 22, 2009Date of Patent: March 6, 2012Assignee: AstraZeneca ABInventors: William Brown, Andrew Griffin, Thomas Hudzik, Carla Maciag, Gennady Smagin, Christopher Walpole
-
Publication number: 20120039913Abstract: The invention relates to Histamine H4 receptor antagonists or inhibitors of Histamine H4 receptor gene expression for the treatment and/or the prevention of vestibular disorders.Type: ApplicationFiled: December 23, 2009Publication date: February 16, 2012Applicant: INSERM (institut National de la Sante de la Recher Medicale)Inventors: Gilles Desmadryl, Christian Chabbert
-
Publication number: 20120040977Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: February 22, 2010Publication date: February 16, 2012Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
-
Publication number: 20120028963Abstract: The present invention relates to hydroxamate derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof, the use thereof for preparing pharmaceutical compositions, pharmaceutical compositions containing the same, a method of treating disease using the compositions, and a method for preparing the hydroxamate derivatives.Type: ApplicationFiled: March 18, 2010Publication date: February 2, 2012Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.Inventors: Sung Sook Lee, Kyung Joo Lee, Chang Sik Lee, Hyun Mo Yang, Do Hoon Kim, Dae Kyu Choi, Ho Jin Choi, Dal Hyun Kim, In Chang Hwang, Mi Jeong Kim, Byeong Hoon Han
-
Publication number: 20120020915Abstract: Disclosed are compounds of the general formula (I): compositions comprising an effective amount of said compounds either alone or in combination with other chemotherapeutic agents, and methods useful for treating or preventing cancer and for inhibiting tumour tissue growth. These compounds attenuate the oxidative damage associated with increased heme-oxygenase activity and can reduce cell proliferation in transformed cells. In addition, the described compounds and compositions are useful as neuroprotectants and for treating or preventing neurodegenerative disorders and other diseases of the central nervous system.Type: ApplicationFiled: January 13, 2011Publication date: January 26, 2012Applicants: QUEENS UNIVERSITY AT KINGSTON, THE SIR MORTIMER B. DAVIS JEWISH GENERAL HOSPITAL, OSTA BIOTECHNOLOGIES, INC.Inventors: Ajay Gupta, Hyman M. Schipper, Moulay Alaoui-Jamali, Walter A. Szarek, Kanji Nakatsu, Jason Z. Vlahakis
-
Patent number: 8097611Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: April 13, 2010Date of Patent: January 17, 2012Assignee: Janssen Pharmaceutica, N.V.Inventors: Kristof Van Emelen, Janine Arts, Leo-Jacobus Jozef Backx, Hans Louis Jos De Winter, Sven Franciscus Anna Van Brandt, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Isabelle Noëlle Constance Pilatte, Virginie Sophie Poncelet, Alexey Borisovich Dyatkin, Jimmy Arnold Viviane Van heusden
-
Publication number: 20120010181Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF—or combinations thereof.Type: ApplicationFiled: November 9, 2009Publication date: January 12, 2012Inventors: Joseph A. Kozlowski, Wensheng Yu, Michael K.C. Wong, Seong Heon Kim, Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, De-Yi Yang, Robert Feltz, Aneta Maria Kosinski, Guowei Zhou, Razia K. Rizvi, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristen E. Rosner, M. Arshad Siddiqui, Liping Yang
-
Publication number: 20120004196Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: ApplicationFiled: May 4, 2011Publication date: January 5, 2012Applicant: ABBOTT LABAORATORIESInventors: David A. DeGoey, Warren M. Kati, Charles W. Hutchins, Pamela L. Donner, Allan C. Krueger, John T. Randolph, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, Mark A. Matulenko, Ryan G. Keddy, Tammie K. Jinkerson, Yi Gao, Dachun Liu, John K. Pratt, Todd W. Rockway, Clarence J. Maring, Douglas K. Hutchinson, Charles A. Flentge, Rolf Wagner, Michael D. Tufano, David A. Betebenner, Kathy Sarris, Kevin R. Woller, Seble H. Wagaw, Jean C. Califano, Wenke Li, Daniel D. Caspi, Mary E. Bellizzi, William A. Carroll
-
Patent number: 8088368Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: May 12, 2010Date of Patent: January 3, 2012Assignee: Gilead Sciences, Inc.Inventors: Hongyan Guo, Darryl Kato, Thorsten A. Kirschberg, Hongtao Liu, John O. Link, Michael L. Mitchell, Jay P. Parrish, Jianyu Sun, James Taylor, Elizabeth M. Bacon, Eda Canales, Aesop Cho, Choung U. Kim, Jeromy J. Cottell, Manoj C. Desai, Randall L. Halcomb, Scott E. Lazerwith, Richard L. Mackman, Hyung-Jung Pyun, Joseph H. Saugier, James D. Trenkle, Winston C. Tse, William J. Watkins, Lianhong Xu
-
Publication number: 20110312969Abstract: Compounds of general formula (I): wherein R1, R2, R3, R4, R5, R6, X and Y are as defined herein are inhibitors of Bcl-2 and are useful for treating diseases characterised by abnormal cell growth and/or dysregulated apoptosis.Type: ApplicationFiled: December 8, 2009Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephen Peter East, Mark Whittaker, Osamu Ichihara, Adrian Kotei Kotei, Smantha Jayne Bamford
-
Publication number: 20110312931Abstract: The compounds of the present invention are represented by the following formula (I): wherein the substituents R1, R2, R3, R4, (R5)m, R6, A, X, and Y are as defined herein. The compounds are useful in methods of treating a disorder which is created by or is dependent upon inhibiting GlyT-1.Type: ApplicationFiled: June 2, 2011Publication date: December 22, 2011Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Christopher L. CIOFFI, Mark A. WOLF, Peter R. GUZZO, Shuang LIU, Kashinath SADALAPURE, Visweswaran PARTHASARATHY, Jun-Ho MAENG
-
Publication number: 20110306615Abstract: According to the present invention, a compound represented by formula (I): wherein Q is: A is a hydrogen atom, a halogen atom, —ORa or a C1-4 alkyl group which may be substituted by one or more halogen atoms; E is independently selected from a C1-6 alkyl group; m is selected from integers from 0 to 3; R2 and R3 are independently selected from a C1-6 alkyl group; X1 and X2 are independently selected from O and S; Y is selected from an arylene group and a divalent 5- or 6-membered monocyclic or 8- to 10-membered condensed heterocyclic group, wherein the arylene group and the heterocyclic group may be substituted by 1 to 3 substituents independently selected from E1; E1 is independently selected from a hydroxyl group, a halogen atom, a C1-4 alkyl group, a cyano group, a C1-4 alkoky group, a carbamoyl group, a C1-4 alkylcarbamoyl group, a di(C1-4 alkyl)carbamoyl group, an amino group, a C1-4 alkylamino group, a di(C1-4 alkylamino group, a sulfamoyl group, a C1-4 alkylsulfamoyl group and a di(C1-4 alkyl)suType: ApplicationFiled: September 9, 2005Publication date: December 15, 2011Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Kazutaka Tachibana, Haruhiko Sato, Masateru Ohta, Mitsuaki Nakamura, Takuya Shiraishi, Hitoshi Yoshino, Takashi Emura, Akie Honma, Etsuro Onuma, Hiromitsu Kawata, Kenji Taniguchi
-
Publication number: 20110306620Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I), in which the symbols have the meanings given in the description and agrochemically active salts thereof and their use for controlling phytopathogenic harmful fungi and also processes for preparing compounds of the formula (I).Type: ApplicationFiled: October 27, 2010Publication date: December 15, 2011Applicant: Bayer CropScience AGInventors: Pierre Cristau, Nicola Rahn, Tomoki Tsuchiya, Joachim Kluth, Pierre Wasnaire, Sebastian Hoffmann, Jürgen Benting, Ulrike Wachendorff-Neumann, Thomas Seitz
-
Publication number: 20110301146Abstract: GSK-3beta inhibitors comprising 7-Hydroxy-benzoimidazole-4-yl-methanone Derivatives are provided. For example, the inhibitors have following general formula (I).Type: ApplicationFiled: September 29, 2009Publication date: December 8, 2011Applicant: ONCOTHERAPY SCIENCE, INC.Inventors: Yo Matsuo, Ryuji Ohsawa, Shoji Hisada
-
Patent number: 8071600Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: GrantFiled: August 31, 2006Date of Patent: December 6, 2011Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hiroshi Yamashita, Hideaki Kuroda, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Haruka Takahashi, Tae Fukushima, Satoshi Shimizu, Kazumi Kondo, Yohji Sakurai, Takeshi Kuroda, Shinichi Taira, Motohiro Itotani, Tatsuyoshi Tanaka
-
Publication number: 20110294822Abstract: The invention relates to a substituted phenylpiperazine aryl alkanol derivative represented by the following general formula and its salt and hydrate, wherein C1 and C2 represent chiral carbon atoms, and the compound is one of the six isomers: (1RS, 2SR), (1RS, 2RS), (1R, 2S), (1S, 2S), (1R, 2R) or (1S, 2R); and R, R1, R2, R3 and Ar are as defined in the specification. The derivative is non-opioid analgesic, has good analgesic effect and relatively small side effects. The invention also relates to a composition comprising the derivative and its use.Type: ApplicationFiled: December 22, 2009Publication date: December 1, 2011Applicant: NHWA PHARMA. CORPORATIONInventors: Jianqi Li, Guan Wang, Guisen Zhang, Xiangping Yang, Peng Xie, Linjie Zhang, Xiangqing Xu, Yumei Wang
-
Publication number: 20110294804Abstract: The invention provides a compound for the treatment or prophylaxis of pathology involving SNS, specifically diseases such as neuropathic pain, nociceptive pain, dysuria, multiple sclerosis and the like.Type: ApplicationFiled: December 25, 2009Publication date: December 1, 2011Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Katsunori Tsubio, Yusuke Yamai, Hitoshi Watanabe, Hironori Kinoshita
-
Patent number: 8063053Abstract: The invention relates to 1-(arylsulfonyl)-4-(piperazin-1-yl)-1H-benzimidazole compounds of the Formula I: or a tautomer, stereoisomer, or pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.Type: GrantFiled: November 11, 2009Date of Patent: November 22, 2011Assignee: Wyeth LLCInventors: Simon Nicolas Haydar, Patrick Michael Andrae, Heedong Yun, Albert Jean Robichaud
-
Publication number: 20110280804Abstract: Compounds having the general formula III?, or IV? wherein R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle or a radical of an optionally substituted cyclic or acyclic tertiary amine or isoindoline-1,3-dione: R2,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate, optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y is S; Z can be either H, O, S, S—R or NR where R groups can be either H, aryls, alkyls, or cycloalkyls; “n” can be 1 to 5 carbons in length and stereoisomers, functional analogs, and pharmaceutically acceptable salts thereof and wherein the moiety bridging R1 and N can be a substituted alkylene, optionally substituted alkenylene or optionally substituted alkynylene and where the alkylene group can include an inserted C3-C5 cycloalkyl group, aromatic, and heterocycliType: ApplicationFiled: June 1, 2011Publication date: November 17, 2011Applicants: The Board of Trustees of the Leland Stanford Junior University, University of MississippiInventors: Christopher R. McCurdy, Christophe Mesangeau, Frederick T. Chin, Michelle L. James, Bin Shen, Sanjiv Gambhir
-
Patent number: 8053457Abstract: The invention relates to 3-heterocyclyl indolyl compounds of formula I capable of inhibiting the interaction between p53, or variants thereof, and MDM2 and/or MDM4, or variants thereof, respectively: wherein R1, R2, R3, R4, RA, Y and Y are as defined in the specification. Due to their activity, the compounds are useful in the treatment of various disorders and diseases mediated by the activity of MDM2 and/or MDM4, or variants thereof, such as inflammatory or proliferative diseases or in the protection of cells.Type: GrantFiled: March 27, 2008Date of Patent: November 8, 2011Assignee: Novartis AGInventors: Andreas Boettcher, Nicole Buschmann, Pascal Furet, Jean-Marc Groell, Jorg Kallen, Joanna Hergovich Lisztwan, Keiichi Masuya, Lorenz Mayr, Andrea Vaupel
-
Publication number: 20110269768Abstract: This invention is directed to a compound of Formula (I): and forms thereof, wherein A, B, E, G, X and L2 are as defined herein and their use as urotensin II receptor antagonists.Type: ApplicationFiled: July 14, 2011Publication date: November 3, 2011Inventors: William A. Kinney, Edward C. Lawson, Shyamali Ghosh, Diane K. Luci, David F. McComsey
-
Publication number: 20110270151Abstract: Disclosed are compositions and methods for targeted drug delivery using image-guided energy deposition to help localize active compounds to particular sites within the body of an animal. Also provided are compounds and formulations thereof for use in the targeted administration of therapeutically, prophylactically, and/or diagnostically effective amounts of such agents to a population of cells or tissues of a mammal in need thereof.Type: ApplicationFiled: September 8, 2009Publication date: November 3, 2011Applicant: The Methodist Hospital Research InstituteInventor: King Chuen Li
-
Publication number: 20110263566Abstract: 7-Hydroxy-benzoimidazole-4-yl-methanone Derivatives, which are useful for PBK inhibitors, are provided.Type: ApplicationFiled: July 30, 2009Publication date: October 27, 2011Inventors: Yo Matsuo, Yingfu Li, Joel Walker, Feryan Ahmed, Ryuji Ohsawa, Shoji Hisada