Chalcogen Attached Directly To Piperazine Ring Nitrogen By Nonionic Bonding Patents (Class 544/383)
-
Publication number: 20130065889Abstract: Provided herein are 2,5-disubstituted arylsulfonamide CCR3 antagonists, e.g., compounds of Formula I, and pharmaceutical compositions thereof: Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: ApplicationFiled: October 26, 2012Publication date: March 14, 2013Applicant: AXIKIN PHARMACEUTICALS, INC.Inventor: Axikin Pharmaceuticals, Inc.
-
Publication number: 20130018044Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.Type: ApplicationFiled: December 21, 2010Publication date: January 17, 2013Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michel Pawlotsky
-
Patent number: 8354412Abstract: The present invention relates to new compounds, ligands of the beta-3 adrenergic receptor, their preparation and their use in therapy or as research tools for said receptor; the invention also relates to a process for the preparation of the compounds of the invention and the use of inverse agonists of the beta-3 adrenergic receptor as medicaments.Type: GrantFiled: August 3, 2011Date of Patent: January 15, 2013Assignee: Universita' Degli Studi di BariInventors: Antonio Scilimati, Maria Grazia Perrone, Ernesto Santandrea
-
Publication number: 20130012709Abstract: An inhibitor of the activity of stearoyl-CoA-desaturase-1 (SCD-1) enzyme for use in the treatment of prostate cancer as well as novel inhibitors of formula (IIa).Type: ApplicationFiled: September 10, 2010Publication date: January 10, 2013Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Lluis Fajas, Zohra Benfodda, Vanessa Fritz
-
Publication number: 20130012701Abstract: A compound useful as a building block for the manufacture of various compounds is represented by Formula A or D. In Formula A and D, z is 0 or 1; Q is a heteroatom; R1 through R11 and Ra through Rf are each independently hydrogen, a substituted or unsubstituted hydrocarbyl group, a substituted or unsubstituted heteroatom containing hydrocarbyl group, or a functional group; d, e and f are each independently 0 or greater; each of A, B and D is independently a carbon atom or a heteroatom; and two or more of R1 though R11, Ra through Rf and Y optionally combine to form a ring. In some embodiments, R8 and R9 combine to form a carbonyl group. In some embodiments, R2 and Y combine to form a ring with the Q atom. In some embodiments, the ring includes at least one double bond.Type: ApplicationFiled: June 22, 2012Publication date: January 10, 2013Applicant: California Institute of TechnologyInventors: Brian M. Stoltz, Scott C. Virgil, David E. White, Taiga Yurino, Yiyang Liu, Douglas C. Behenna, Douglas Duquette, Christian Eidamshaus
-
Publication number: 20120323006Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.Type: ApplicationFiled: June 28, 2010Publication date: December 20, 2012Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Carine Rosignoli, Olivier Roye, Jean-Claude Pascal, Marlene Schuppli
-
Patent number: 8318747Abstract: Provided herein are 2,5-disubstituted arylsulfonamide CCR3 antagonists of Formula I or II, and pharmaceutical compositions thereof: wherein X, Y, Z, and R1-R5 are as defined herein. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: GrantFiled: April 21, 2010Date of Patent: November 27, 2012Assignee: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei Ly, Garrett Thomas Potter
-
Publication number: 20120295910Abstract: The present invention relates to new sulfonamide derivatives of formula (I), wherein R1-R8 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these same compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.Type: ApplicationFiled: August 1, 2012Publication date: November 22, 2012Inventors: Gyula Beke, Eva Bozo, Sandor Farkas, Katalin Hornok, Gyorgy Keseru, Eva Schmidt, Eva Szentirmay, Istvan Vago, Monika Vastag
-
Publication number: 20120282387Abstract: The present invention aims to provide extracts available for use in acidic beverage production and containing 2,5-piperazinedione,3,6-bis(phenylmethyl)-,(3S,6S)-, which is a useful substance with an improving effect on learning motivation. When an acid treatment step is included in the production of extracts containing 2,5-piperazinedione,3,6-bis(phenylmethyl)-,(3S,6S)-, it is possible to obtain acidic extracts which cause no sedimentation even when added to beverages. The extracts of the present invention can be added to beverages and so on without impairing the taste inherent to foods and beverages, and can be used for production of acidic beverages preferred by most consumers.Type: ApplicationFiled: February 26, 2010Publication date: November 8, 2012Applicants: CEREBOS PACIFIC LIMITED, SUNTORY HOLDINGS LIMITEDInventors: Hideki Matsubayashi, Kenji Yamamoto, Hiroshi Watanabe
-
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
-
Publication number: 20120271049Abstract: A process for preparing phenyl iso(thio)cyanates of the formula I in which a compound of the formula II or its HCl adduct is reacted with a phosgenating agent where W is oxygen or sulfur and Ar and A are as defined in claim 1 is described. Moreover, the invention relates to the use of the phenyl iso(thio)cyanates for preparing crop protection agents.Type: ApplicationFiled: June 28, 2012Publication date: October 25, 2012Applicant: BASF AKTIENGESELLSCHAFTInventors: Gerhard Hamprecht, Michael Puhl, Bernd Wolf, Norbert Götz, Michael Keil, Robert Reinhard, Ingo Sagasser, Werner Seitz
-
Patent number: 8278308Abstract: Drug delivery systems have been developed based on the formation of diketopiperazine carboxylate salts and microparticles containing the same. The systems may further comprise a bioactive agent. Related methods for making and using the biologically active agent delivery compositions are also provided. In certain embodiments, the pharmaceutically acceptable salts described can be formed by removal of solvent by methods including distillation, evaporation, spray drying or lyophilization.Type: GrantFiled: September 20, 2010Date of Patent: October 2, 2012Assignee: MannKind CorporationInventors: Andrea Leone-Bay, Destardi Moye-Sherman, Bryan R. Wilson
-
Publication number: 20120245141Abstract: Disclosed are pyruvate kinase M2 activators, which are, bis sulfonamide piperazinyl compounds of Formula (I) and 2,4-disubstituted 4H-thieno[3,2-b]pyrrole-2-(substituted benzyl)pyridazin-3(2H)ones of Formula (II), wherein L and R1 to R16 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia,Type: ApplicationFiled: March 29, 2012Publication date: September 27, 2012Applicant: The United States of America, as represented by the Secretary, Dept. of Health and Human ServicesInventors: Craig J. Thomas, Douglas S. Auld, James Inglese, Amanda P. Skoumbourdis, Jian-Kang Jiang, Matthew B. Boxer
-
Publication number: 20120225854Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: August 23, 2011Publication date: September 6, 2012Applicant: AMGEN INC.Inventors: Kate Ashton, Michael David Bartberger, Yunxin Bo, Marian C. Bryan, Michael Croghan, Christopher Harold Fotsch, Clarence Henderson Hale, Roxanne Kay Kunz, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Lewis Dale Pennington, Steve Fong Poon, Markian Myroslaw Stec, David Joseph St. Jean, JR., Nuria A. Tamayo, Christopher Michael Tegley, Kevin Chao Yang
-
Publication number: 20120225890Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A? amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.Type: ApplicationFiled: March 6, 2012Publication date: September 6, 2012Inventors: Alan D. Snow, Beth Nguyen, Gerardo Castillo, Virginia Sanders, Thomas Lake, Lesley Larsen, Rex T. Weavers, Stephen Lorimer, David Larsen, David L. Coffen, Charlotte Coffen
-
Patent number: 8252786Abstract: The invention relates to a compound (I) wherein R is a heterocyclyl radical; R1 and R2 are independently H or alkyl; R3 is H, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, aryl, arylalkyl, heterocyclyl or heterocyclylalkyl; R4 and R5 are independently H or alkyl; q is a number selected from 0 and 1; and the salts, solvates, prodrugs or stereoisomers thereof having inhibitory activity for UBC13-UEV interactions and which can be used in the production of pharmaceutical compositions intended for antitumor therapy or the treatment and/or prophylaxis of diseases associated to metabolic pathways involving the UBC13 enzyme, metabolic pathways involving transcriptional factor NF-?B, or pathways involving PCNA or RAD6.Type: GrantFiled: March 7, 2007Date of Patent: August 28, 2012Assignee: Consejo Superior de Investigaciones CientificasInventors: Timothy Thomson Okatsu, Johanna Scheper Sigmund, Ángel Messeguer Peypoch, Ángel Ramírez Ortiz, María Luz Ortiz Melguizo, legal representative, Ma Carmen Fabrega Claveria, legal representative, Gloria Sanclimens Pérez de Rozas, Isabel Masip Masip, Alejandra Moure Fernández, Domingo González Ruiz, Antonio Morreale de León
-
Publication number: 20120214991Abstract: An indenone derivative of formula (1) is effective in enhancing the activity of osteoblastic cells and inhibiting bone resorption by osteoclastic cells, and a pharmaceutical composition comprising the indenone derivative or a pharmaceutically acceptable salt thereof is useful for preventing or treating bone diseases such as osteoporosis.Type: ApplicationFiled: October 21, 2009Publication date: August 23, 2012Applicant: Korea Research Institute of Chemical TechnologyInventors: Jung Nyoung Heo, Myung Ae Bae, Nack Jeong Kim, Sung Youn Chang, Nam Sook Kang, Sung Eun Yoo, Eun Sook Hwang
-
Patent number: 8242175Abstract: New histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH2, CH—NR3R4, NR5 or oxygen, X is CH or nitrogen, Y is a bond, CH2, oxygen or NR6, Z is CH or nitrogen, R1, R2 are, independently, hydrogen, halogen, C1-C6 alkyl or C1-C6 haloalkyl, R11, R12 are, independently, hydrogen or C1-C6 alkyl, and R3, R4, R5 and R6 are as further defined in the specification.Type: GrantFiled: December 7, 2010Date of Patent: August 14, 2012Assignee: DAC S.R.L.Inventors: Antonello Mai, Saverio Minucci, Florian Thaler, Gilles Pain, Andrea Colombo, Stefania Gagliardi, Pier Giuseppe Pelicci, Marco Ballarini, Gaetano Gargiulo, Silvio Massa
-
Publication number: 20120178934Abstract: The present invention relates to novel benzene-carboxamide compounds having a structure that corresponds to the general formula (I), and also to their method of synthesis and to their use in pharmaceutical compositions intended for use in human or veterinary medicine or else to their use in cosmetic compositions.Type: ApplicationFiled: September 16, 2010Publication date: July 12, 2012Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Sandrine Chambon, Laurence Clary, Marlene Schuppli
-
Patent number: 8217063Abstract: The present application relates to novel lactam-substituted dicarboxylic acid derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.Type: GrantFiled: March 15, 2008Date of Patent: July 10, 2012Assignee: Bayer Intellectual Property GmbHInventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Dieter Lang
-
Publication number: 20120165324Abstract: Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.Type: ApplicationFiled: December 29, 2011Publication date: June 28, 2012Inventors: Francesco G. Salituro, Jeffrey Saunders
-
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
-
Publication number: 20120107273Abstract: The present invention relates to a compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof and an anti-HCV agent and an HCV polymerase inhibitor containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.Type: ApplicationFiled: April 25, 2011Publication date: May 3, 2012Applicant: Japan Tobacco Inc.Inventors: Hiroyuki Abe, Masahiro Tanaka, Kazuyuki Sugimoto, Akira Suma, Masahiro Yokota, Makoto Shiozaki, Kiyosei Ilo, Kazuhito Ueyama, Dai Motoda, Toru Noguchi, Tsuyoshi Adachi, Junichiro Tsuruha, Satoki Doi
-
Patent number: 8163735Abstract: The present invention is directed to compounds of formula (I) that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them. Wherein R3 is -alkylene-SO2NR5R6.Type: GrantFiled: December 1, 2005Date of Patent: April 24, 2012Assignee: Virobay, Inc.Inventors: Soon H. Woo, Randall W. Vivian, John O. Link
-
Patent number: 8163898Abstract: [PROBLEMS] To provide compounds useful as preventives or remedies for circulatory diseases, nervous diseases, metabolic diseases, reproductive system diseases, and digestive diseases. [MEANS FOR SOLVING PROBLEMS] Compounds represented by the general formula (I) or pharmaceutically acceptable salts thereof: wherein R1 is C1-6 alkyl, C3-8 cycloalkyl, or the like; R2 is phenyl, heteroaryl, or the like; Q is N or CH; and M1, M2, M3 and M4 are each independently hydrogen or C1-6 alkyl, or alternatively M1 together with M2 or M3 forms —CH2-CH2- or the like, or M4 together with M2 or M3 forms —CH2-CH2- or the like, with the proviso that M1, M2, M3, and M4 are such that one —CH2- or —CH2-CH2- group is formed thereamong.Type: GrantFiled: September 12, 2008Date of Patent: April 24, 2012Assignee: MSD K. K.Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi
-
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: 20120088769Abstract: Provided herein are arylsulfonamide salts, e.g., a salt of a compound of Formula I, which are useful for modulating CCR3 activity, and their pharmaceutical compositions. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: ApplicationFiled: October 10, 2011Publication date: April 12, 2012Applicant: Axikin Pharmaceuticals, Inc.Inventor: Tai Wei LY
-
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: 8143242Abstract: The present invention relates to compounds of formula I, The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are inhibitors of the blood clotting enzymes, especially factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: GrantFiled: January 7, 2010Date of Patent: March 27, 2012Assignee: Sanofi-AventisInventors: Henning Steinhagen, Hauke Szillat, Markus Follmann, Reinhard Kirsch, Volkmar Wehner, Hans Matter, Martin Lorenz, Kent W. Neuenschwander, Anthony C. Scotese
-
Publication number: 20120071653Abstract: The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role.Type: ApplicationFiled: June 23, 2011Publication date: March 22, 2012Applicant: SYMPHONY EVOLUTION, INC.Inventors: Lynne Canne Bannen, Erick W. Co, Vasu Jammalamadaka, John M. Nuss, Moon Hwan Kim, Donna Tra Le, Amy Lew, Morrison B. Mac, Shumeye Mamo, Zhaoyang Wen, Wei Xu, Richard George Khoury
-
Patent number: 8119633Abstract: Substituted sulfonamide compounds corresponding to formula I pharmaceutical compositions comprising them, a process for preparing them, and the use of such compounds to treat or inhibit pain and other disorders or disease states.Type: GrantFiled: April 30, 2008Date of Patent: February 21, 2012Assignee: Gruenenthal GmbHInventors: Beatrix Merla, Stefan Oberboersch, Melanie Reich, Bernd Sundermann, Werner Englberger, Timo Struenker, Ruth Jostock, Sabine Hees, Edward Bijsterveld, Fritz Theil, Heinz Graubaum
-
Publication number: 20120022070Abstract: Novel classes of molecular chaperone Heat shock protein 90 (Hsp90) inhibitors are disclosed. These compounds are useful in treating and preventing cancer and other Hsp90-related diseases and conditions, such as inflammation and neurodegenerative disorders. Methods of treating and preventing cancer and other Hsp90 related diseases and conditions are disclosed that include administering to the subject a therapeutically effective amount of an Hsp90 inhibitor. Methods of preparing the novel Hsp90 inhibitors are also provided.Type: ApplicationFiled: October 6, 2009Publication date: January 26, 2012Applicant: EMORY UNIVERSITYInventors: Jaeki Min, Pahk Thepchatri, Yuhong Du, Dennis C. Liotta, Haian Fu
-
Publication number: 20120022081Abstract: The invention provides a method of inhibiting the effects of platelet activating factor (PAF). For instance, a disease or condition mediated by PAF (particularly inflammation) can be treated or platelet aggregation can be inhibited. The invention also provides a method of inhibiting the production and/or release of interleukin 8 (IL-8) by cells. The effects of PAF and the production and/or release of IL-8 are inhibited according to the invention by a compound of the formula: wherein R1 and R2 are defined in the application, or a physiologically-acceptable salt thereof. The invention also provides pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: October 4, 2011Publication date: January 26, 2012Inventors: David Bar-Or, C. Gerald Curtis, Nagaraja K.R. Rao, Greg Thomas
-
Patent number: 8101614Abstract: The present application relates to calcium channel inhibitors comprising compounds of formula (I), formula (II), formula (III), or formula (IV), wherein L1, R1, R2, R3, R4, R5, R6, R7 and Rc are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: January 14, 2010Date of Patent: January 24, 2012Assignee: Abbott LaboratoriesInventors: Qingwei Zhang, Andrew O. Stewart, Zhiren Xia
-
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: 20120004213Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: ApplicationFiled: September 15, 2011Publication date: January 5, 2012Applicant: FOREST LABORATORIES HOLDINGS LIMITEDInventors: Kumar SUNDARESAN, Sandeep N. RAIKAR, Srinivasa Raju SAMMETA, Ganesh PRABHU, Hosahalli SUBRAMANYA, Alexander BISCHOFF
-
Patent number: 8084606Abstract: The present invention relates to a novel and commercially viable process for substantially optically pure levorotatory and dextrorotatory enantiomers of cetirizine intermediate, 1-[(4-chlorophenyl)phenylmethyl]piperazine, thereby producing substantially optically pure levorotatory and dextrorotatory enantiomers of cetirizine and their pharmaceutical acceptable acid addition salts thereof in high purity and in high yield using novel intermediates.Type: GrantFiled: June 15, 2007Date of Patent: December 27, 2011Assignee: Symed Labs LimitedInventors: Dodda Mohan Rao, Bitra Satyanarayana Rao
-
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: 20110295006Abstract: Feed additives containing essential amino acids which are diketopiperazines of formulas (IV) or (V) or salts thereof are provided: In formulas (IV) and (V), R1 and R2 may be an amino acid residue such as methionine, lysine, threonine, tryptophan, histidine, valine, leucine, isoleucine, phenylalanine, arginine, and cysteine, and may optionally be the same residue. Additionally provided are the diketopiperazines of formulas (IV) and (V) and a method to for their production.Type: ApplicationFiled: May 26, 2011Publication date: December 1, 2011Applicant: EVONIK DEGUSSA GMBHInventors: Christoph KOBLER, Thomas HAEUSSNER, Christoph WECKBECKER
-
Publication number: 20110288104Abstract: The present invention relates to new compounds, ligands of the beta-3 adrenergic receptor, their preparation and their use in therapy or as research tools for said receptor; the invention also relates to a process for the preparation of the compounds of the invention and the use of inverse agonists of the beta-3 adrenergic receptor as medicaments.Type: ApplicationFiled: August 3, 2011Publication date: November 24, 2011Applicant: UNIVERSITA' DEGLI STUDI DI BARIInventors: Antonio Scilimati, Maria Grazia Perrone, Ernesto Santandrea
-
Publication number: 20110288066Abstract: The present invention provides phenoxyacetic acid derivatives of Formula (I) for the treatment of CRTH2 related disorders and disease selected from asthma, atopic dermatitis and inflammatory dermatoses.Type: ApplicationFiled: February 9, 2010Publication date: November 24, 2011Applicant: MERCK SERONO S.A.Inventors: Stefano Crosignani, Catherine Jorand-Lebrun, Christophe Cleva, Adeline Pretre
-
Publication number: 20110275810Abstract: This invention pertains to certain carbamic acid compounds which inhibit HDAC (histone deacetylase) activity of the following formula: The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.Type: ApplicationFiled: July 18, 2011Publication date: November 10, 2011Inventors: Clare J. Watkins, Maria-Rosario Romero-Martin, James Ritchie, Paul W. Finn, Ivars Kalvinsh, Einars Loza, Klara Dikovska, Igor Starchenkov, Daina Lolya, Vija Gailite
-
Patent number: 8039463Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: GrantFiled: March 20, 2009Date of Patent: October 18, 2011Assignee: Forest Laboratories Holdings LimitedInventors: Kumar Sundaresan, Sandeep N. Raikar, Srinivasa Raju Sammeta, Ganesh Prabhu, Hosahalli Subramanya, Alexander Bischoff
-
Publication number: 20110218207Abstract: Provided herein are isotopically enriched arylsulfonamides, for example, of Formula I, that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: ApplicationFiled: March 1, 2011Publication date: September 8, 2011Applicant: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei Ly, Garrett Thomas Potter
-
Patent number: 8012982Abstract: The present invention is directed to compounds of formula (I): where X, Y, R1, R2 and R3 are defined therein, which can act as modulators of viral replication and/or virus production, especially of the hepatitis C virus (HCV).Type: GrantFiled: September 29, 2005Date of Patent: September 6, 2011Assignee: Istituto di Ricerche Biologia Molecolare P. Angeletti SpAInventors: Immacolata Conte, Caterina Ercolani, Claudio Giuliano, Giovanni Migliaccio, Gessica Filocamo, legal representative, Veronica Suriano, legal representative, Ian Stansfield
-
Patent number: 8008303Abstract: Use of a compound which is a biphenyl derivative of formula (I), or a pharmaceutically acceptable salt thereof, for the treatment of Hepatitis C wherein the variables are described herein.Type: GrantFiled: September 18, 2006Date of Patent: August 30, 2011Assignee: AstraZeneca ABInventors: Christopher James Wheelhouse, Alexander James Floyd Thomas, David John Bushnell, James Lumley, James Iain Salter, Malcolm Clive Carter, Neil Mathews, Christopher John Pilkington, Richard Martyn Angell
-
Patent number: 8008305Abstract: The invention relates to a compound of formula wherein R1, R2, X, L, W, n, and o are defined herein and to pharmaceutically suitable acid addition salts thereof, with the exception of the following compounds 6-(4-methyl-piperazin-1-yl)-N-phenethyl-nicotinamide (CAS 199478-31-4), N-(3,4-dichloro-benzyl)-3-fluoro-benzamide (CAS 424815-98-5), N-(4-chloro-benzyl)-3-fluoro-benzamide (CAS 544661-83-8), N-(3-chloro-benzyl)-3-fluoro-benzamide (CAS 796051-07-5), and N-phenethyl-6-phenylamino-nicotinamide (CAS 571913-74-1). The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of CNS disorders.Type: GrantFiled: July 28, 2008Date of Patent: August 30, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
-
Publication number: 20110190495Abstract: Disclosed are N-{1-[3-(2-ethoxy-5-(4-ethylpiperazinyl)sulfonylphenyl)-4,5-dihydro-5-oxo-1,2,4-triazin-6-yl]ethyl}butyramide (which is represented by formula III), its preparation method, intermediates during preparation procedure, preparation method for such intermediates and a method for preparing vardenafil from the compound. In the method for preparing vardenafil, a chloro-sulfonation reaction carries out in the early stage of the preparation procedure.Type: ApplicationFiled: December 28, 2007Publication date: August 4, 2011Applicant: Topharman Shanghai Co., Ltd.Inventors: Guanghui Tian, Zheng Liu, Jin Zheng, Jingshan Shen
-
Publication number: 20110183848Abstract: Piperazine compounds of the formula I in which the variables are defined according to the description, their agriculturally suitable salts, processes and intermediates for preparing the piperazine compounds of the formula I, compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidally effective amount of at least one piperazine compound of the formula I to act on plants, their seed and/or their habitat.Type: ApplicationFiled: September 29, 2009Publication date: July 28, 2011Applicant: BASF SEInventors: Liliana Parra Rapado, Frank Stelzer, Matthias Witschel, Thomas Seitz, Anja Simon, Robert Reinhard, Bernd Sievernich, Klaus Grossmann, Thomas Ehrhardt, Trevor Wlliam Newton, Julia Major, Tao Qu, William Karl Moberg, Dschun Song, Michael Rack, Timo Frassetto, Klaus Kreuz
-
Publication number: 20110166157Abstract: The present invention relates to 2-(substituted sulphur, sulphone or sulphoxide)-3-(substituted phenyl)propionic acid derivatives, 2-(substituted oxygen)-3-(substituted phenyl)propionic acid derivatives, benzoic acid derivatives, and derivatives of 2-methyl-2-(phenoxy or phenylthio)propanoic acid and 2-(methyl or ethyl)-2-(phenoxy or phenylthio)butanoic acid, to processes for preparing such compounds, to their use in the treatment of inflammatory conditions, and to pharmaceutical compositions containing them.Type: ApplicationFiled: March 11, 2011Publication date: July 7, 2011Applicant: ALBIREO ABInventors: Anders Broo, Johan Gottfries, Michael Kossenjans, Li Lanna, Eva-Lotte Lindstedt-Alstermark, Kristina A. Nilsson, Bengt Ohlsson, Maria Thorstensson, Maria Boije, Per Olof Sjögren