Halogen Or Acyclic Nitrogen Bonded Directly To The -c(=x)- Group Patents (Class 544/390)
  • Publication number: 20150087629
    Abstract: The invention relates to a DGAT inhibitor of formula including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —O—C(?O)—; —C(?O)—C(?O)—; —NRx—C(?O)—; —Z—C(?O)—; —Z—NRx—C(?O)—; —C(?O)—Z—; —NRx—C(?O)—Z—; —C(?S)—; —NRx—C(?S)—; —Z—C(?S)—; —Z—NRx—C(?S)—; —C(?S)—Z—; —NRx—C(?S)—Z—; Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents —C(?O)—NRx— or —NRx—C(?O)—; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said
    Type: Application
    Filed: December 5, 2014
    Publication date: March 26, 2015
    Inventors: Jean-Pierre Andre Marc Bongartz, Joannes Theodorus Maria Linders, Lieven Meerpoel, Guy Rosalia Eugeen Van Lommen, Erwin Coesemans, Mirielle Braeken, Christophe Francis Robert Nestor Buyck, Monique Jenny Marie Berwaer, Katharina Antonia Germania J.M. De Waepenaert, Peter Walter Maria Roevens, Petr Vladimirivich Davidenko
  • Patent number: 8981094
    Abstract: The invention relates to a DGAT inhibitor of formula (I): including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —C(?O)—; —O—C(?O)—; C(?O)—C(?O)—; —NRx—C(?O)—; —Z1—C(O)—; —Z1—NRx—C(?O)—; —C(?O)—Z1—; —NRx—C(?O)—Z1—; —S(?O)p-; —C(?S)—; —NRx—C(?S)—; —Z1—C(?S)—; —Z1—NRx—C(?S)—; —C(?S)—Z1-; —NRx—C(?S)—Z—; Y represents NRx—C(=0)-Z2—; —NRx—C(=0)-Z2—NRy—; —NRx—C(=0)-Z2—NRy—C(=0)-; —NRx—C(=0)-Z2—NRy—C(=0)-O—; —NRx—C(=0)-Z2-0-; —NRx—C(=0)-Z2-0-C(=0)-; —NRx—C(=0)-Z2—C(=0)-; —NRx—C(=0)-Z2—C(=0)-; —NRx—C(=0)-0-Z2—C(=0)-; —NRx—C(=0)-0-Z2—C(=0)-0-; —NRx—C(?O)—O—Z2—O—C(?O)—; —NRx—C(?O)—Z2—C(?O)—NRy—; —NRx—C(?O)—Z2—NRy—C(=0)-NRy—; —C(?O)—Z2—; —C(?O)—Z2—O—; —C(=0)-NRx—Z2—; —C(=0)-NRx—Z2-0-; —C(=0)-NRx—Z2—C(=0)-0-; —C(=0)-NRx—Z2-0-C(=0)-; —C(=0)-NRx—Z2—NRy—; —C(=0)-NRx—Z2—NRy—C(=0)-; —C(=0)-NRx—Z2—NRy—C(=0)-0-; R1 represents C1-12alkyl optionally substituted with cyano, C1-4alkyloxy, C1-4alkyl-oxyC1-4alkylox
    Type: Grant
    Filed: June 6, 2008
    Date of Patent: March 17, 2015
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jean-Pierre André Marc Bongartz, Joannes Theodorus Maria Linders, Lieven Meerpoel, Guy Rosalia Eugeen Van Lommen, Erwin Coesemans, Mirielle Braeken, Christophe Francis Robert Nestor Buyck, Monique Jenny Marie Berwaer, Katharina Antonia Germania J. M. De Waepenaert, Peter Walter Maria Roevens, Gustaaf Maria Boeckx, Petr Vladimirivich Davidenko
  • Publication number: 20140336375
    Abstract: The disclosure is directed to compounds identified as allosteric modulators of 5-HT 2CR, as well as pharmaceutical compositions and methods using the same. Certain embodiments also include methods of identifying and methods of synthesizing the compounds. Optimization and development of allosteric 5-HT 2CR modulators that bind sites other than the primary ligand binding site generate novel, highly selective, and potent ligands of 5-HT2CR. Such molecules can be used as small molecule probes for the nervous system and as effective therapeutics for a variety of diseases.
    Type: Application
    Filed: December 7, 2012
    Publication date: November 13, 2014
    Applicant: The Board of Regents of the University of Texas system
    Inventors: Jia Zhou, Chunyong Ding, Kathryn A. Cunningham
  • Publication number: 20140275037
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel semicarbazides, sulfonyl carbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to Arenaviridae (Junin, Machupo, Guanavito, Sabia and Lassa), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).
    Type: Application
    Filed: December 19, 2013
    Publication date: September 18, 2014
    Applicant: Siga Technologies, Inc.
    Inventors: Yijun Deng, Theodore J. Nitz, Thomas R. Bailey, Yanming Zhang, Sylvie Laquerre
  • Publication number: 20140243334
    Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: May 5, 2014
    Publication date: August 28, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Emily F. Calderwood, Dylan B. England, Alexandra E. Gould, Sean J. Harrison, Liting Ma
  • Publication number: 20130324556
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrate thereof Wherein Y, Z, R3, U, R4, m and n are as defined in the claims.
    Type: Application
    Filed: January 27, 2012
    Publication date: December 5, 2013
    Inventors: Joe William Boyd, Paul Meo, Michael Higginbottom, Iain Simpson, David Mark Mountford, Edward Daniel Savory
  • Patent number: 8598173
    Abstract: The present invention relates to novel quioxaline-piperazine compounds, 1-[(6,7-substituted alkoxyquinoxalinyl)aminocarbonyl]-4-(hetero)arylpiperazine derivatives of formula (1): and their pharmaceutically acceptable salts, a process for their preparation thereof, and compositions containing such compounds. Therapeutic methods for the treatment of hyperproliferative disorders, including cancers, by administering quioxalin-piperazine compounds are also included.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: December 3, 2013
    Assignees: Korea Research Institute of Chemical Technology, Rexahn Pharmaceuticals, Inc.
    Inventors: Young-Dae Gong, Moon-Kook Jeon, Dong-Su Kim, Jae Y. Kong, Gun-Do Kim, Chang Ho Ahn, Young Bok Lee
  • Patent number: 8536184
    Abstract: The present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof and a process for making thereof. The compounds have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention also provides intermediate compounds useful in the process, as well as final products produced by the process, and salts or prodrugs thereof. The invention further provides a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases comprising administering an effective amount of a compound according to the invention to a patient in need thereof.
    Type: Grant
    Filed: November 19, 2009
    Date of Patent: September 17, 2013
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: James Kanter, James Robinson, Anjali Pandey, Robert M. Scarborough
  • Publication number: 20130096138
    Abstract: Disclosed are novel thiourea or urea derivatives inhibitory of HIV activity. Also provided are a method for preparing the thiourea or urea derivatives, and a pharmaceutical composition for the prophylaxis or therapy of AIDS comprising the derivatives. Having high inhibitory activity against HIV, the thiourea or urea derivatives can be effectively used in the prophylaxis or therapy of AIDS.
    Type: Application
    Filed: June 17, 2011
    Publication date: April 18, 2013
    Applicant: AVIXGEN INC.
    Inventors: Ji Chang You, Gyoon Hee Han, Chul Ho Lee, Doo Na Song, Koo Hwan Chung
  • Patent number: 8314100
    Abstract: The present invention related to a novel urea derivative for formula (I): which is useful as an anti-cancer agent, its pharmaceutically acceptable acid addition salt or stereoisomer, and to a process for preparing the urea derivative and an anti-cancer composition comprising the same as an active ingredient.
    Type: Grant
    Filed: October 18, 2005
    Date of Patent: November 20, 2012
    Assignees: Rexahn Pharmaceuticals, Inc., Korea Research Institute of Chemical Technology
    Inventors: Young-Dae Gong, Moon-Kook Jeon, Dong-Su Kim, Jae Yang Kong, Gun-Do Kim, Chang-Ho Ahn, Young Bok Lee
  • Publication number: 20120270836
    Abstract: The present invention relates to compositions and methods for the treatment of Alzheimer's disease and related disorders. More specifically, the present invention relates to novel combinatorial therapies of Alzheimer's disease and related disorders. In particular, the invention concerns compounds which, alone or in combination(s), can effectively modulate synapse function and/or angiogenesis and/or cell stress response. The invention also relates to methods of producing a drug or a drug combination for treating Alzheimer's disease and to methods of treating Alzheimer's disease or a related disorder.
    Type: Application
    Filed: May 2, 2012
    Publication date: October 25, 2012
    Applicant: PHARNEXT
    Inventors: Daniel Cohen, Ilya Chumakov, Serguei Nabirochkin
  • Publication number: 20120228151
    Abstract: An extraction component enabling the concurrent recovery of gold and/or palladium selectively from a hydrochloric acid media containing the base metals and other contaminants. The disclosed extractant disclosed eliminates the conventional multi-step process for such extraction by providing for an extraction method which uses a single solvent extraction reagent. Further enhancing the conventional multi step process, the conventional scrubbing stage is eliminated by a single stripping stage. The resulting solutions can be obtained from leaching many types of material such as copper anode slimes, the treatment of scrap such as electronic circuit boards and plating effluents, PGM, or refractory gold ores.
    Type: Application
    Filed: March 7, 2011
    Publication date: September 13, 2012
    Inventors: Loghman Moradi, Hiwa Salimi, Mohammad Piltan, Issa Yavari
  • Patent number: 8242175
    Abstract: 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: Grant
    Filed: December 7, 2010
    Date of Patent: August 14, 2012
    Assignee: 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: 20120189546
    Abstract: This invention relates to novel cyclo alkyl compounds suitable for labeling by 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).
    Type: Application
    Filed: July 9, 2010
    Publication date: July 26, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Keith Graham, Heribert Schmitt-Willich, Dominic Franck
  • Publication number: 20120108603
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, 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: Application
    Filed: December 30, 2011
    Publication date: May 3, 2012
    Applicant: Janssen Pharmaceutica N.V.
    Inventors: Kristof Van Emelen, Hans Louis Jos De Winter, Alexy Borisovich Dyatkin, Marc Gustaal Celine Verdonck, Lieven Meerpoel, Jimmy Arnold Viviane Van heusden
  • Publication number: 20120046292
    Abstract: [Problem] A compound which is useful as an anti-obesity agent is provided. [Means for Solution] The present inventors have investigated a compound having a DGAT1 inhibitory action, which is promising as an active ingredient of a pharmaceutical composition for treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases, and as a result, they have found that the diacylethylenediamine compound of the present invention has an excellent DGAT1 inhibitory action, thereby completing the present invention. That is, the diacylethylenediamine compound of the present invention has a DGAT1 inhibitory action, and can be therefore used as an agent for preventing and/or treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases.
    Type: Application
    Filed: April 19, 2010
    Publication date: February 23, 2012
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Tomoaki Kawano, Yasuhiro Yonetoku, Takeshi Hanazawa, Takahiro Nigawara, Hiroki Fukudome, Hiroshi Moritani
  • Publication number: 20120022080
    Abstract: The present invention provides a novel compound having plasminogen activator inhibitor-1 inhibitory activity, and an inhibitor of PAI-1 comprising the compound as an active ingredient. The present invention also provides a pharmaceutical composition having an inhibitory action on PAI-1 activity and being efficacious in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity.
    Type: Application
    Filed: March 31, 2010
    Publication date: January 26, 2012
    Applicant: RENASCIENCE CO., LTD.
    Inventors: Toshio Miyata, Kenji Murano, Nagahisa Yamaoka, Akihisa Maeda
  • Publication number: 20110294793
    Abstract: The present invention provides compound of Formula (I): or a stereoisomer, tautomer, salt or solvate thereof, wherein the variables are defined herein. The compounds of formula (I) are inhibitors of Bcl-2 family antiapoptotic proteins, compositions containing the compounds and methods of treating diseases using the compounds.
    Type: Application
    Filed: June 8, 2009
    Publication date: December 1, 2011
    Inventors: kyoung S Kim, Robert M. Borzilleri, Zhen-Wei Cai, Kap-Sun Yeung
  • Patent number: 8049011
    Abstract: The present invention describes a novel process for the preparation of levocetirizine and pharmaceutically acceptable acid addition salts thereof using diglycolic acid or derivatives thereof and new intermediates used in that process.
    Type: Grant
    Filed: March 12, 2008
    Date of Patent: November 1, 2011
    Assignee: KRKA, Tovarna Zdravil, D.D., Novo Mesto
    Inventors: Jaroslav Tihi, Rok Zupet, Anica Pecavar, Ivanka Kolenc, Darja Pavlin
  • Patent number: 8017612
    Abstract: 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: Grant
    Filed: April 17, 2007
    Date of Patent: September 13, 2011
    Assignee: Japan Tobacco Inc.
    Inventors: Hiroyuki Abe, Masahiro Tanaka, Kazuyuki Sugimoto, Akira Suma, Masahiro Yokota, Makoto Shiozaki, Kiyosei Iio, Kazuhito Ueyama, Dai Motoda, Toru Noguchi, Tsuyoshi Adachi, Junichiro Tsuruha, Satoki Doi
  • Publication number: 20110212080
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which is useful for the treatment of diseases or conditions mediated by LpxC.
    Type: Application
    Filed: July 28, 2009
    Publication date: September 1, 2011
    Inventors: Umar Faruk Mansoor, Panduranga Adulla Reddy, M. Arshad Siddiqui
  • Patent number: 7960385
    Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: September 5, 2008
    Date of Patent: June 14, 2011
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
  • Publication number: 20110136827
    Abstract: The invention provides certain bis-acylated hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.
    Type: Application
    Filed: December 7, 2010
    Publication date: June 9, 2011
    Inventors: John P. Toscano, Art Sutton, Vincent J. Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
  • Patent number: 7932255
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts, solvates, hydrates or pharmaceutically acceptable formulations thereof. These compounds may be used to modulate cellular proliferation and to prevent and/or treat proliferative diseases.
    Type: Grant
    Filed: April 13, 2006
    Date of Patent: April 26, 2011
    Assignee: Novartis AG
    Inventors: Robert Eckl, Roswitha Taube, Michael Almstetter, Michael Thormann, Andreas Treml, Christopher Straub, Zhouliang Chen
  • Publication number: 20110077247
    Abstract: 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: Application
    Filed: December 7, 2010
    Publication date: March 31, 2011
    Applicant: DAC S.r.I.
    Inventors: Antonello Mai, Saverio Minucci, Florian Thaler, Gilles Pain, Andrea Colombo, Stefania Gagliardi, Pier Giuseppe Pelicci, Marco Ballarini, Gaetano Gargiulo, Silvio Massa
  • Publication number: 20100324025
    Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
    Type: Application
    Filed: September 21, 2009
    Publication date: December 23, 2010
    Applicant: University of Washington
    Inventors: Niels H. Andersen, Jason Bowman, Alice L. Erwin, Eric A. Harwood, Toni Kline, Khisimuzi E. Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
  • Patent number: 7829713
    Abstract: The invention includes a compound of formula I: wherein R1, X, Z, n, and m have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function in animals.
    Type: Grant
    Filed: February 27, 2007
    Date of Patent: November 9, 2010
    Assignee: Helicon Therapeutics, Inc.
    Inventors: Terrence P. Keenan, Alan P. Kaplan
  • Publication number: 20100249411
    Abstract: In an illustrative embodiment, the present invention describes the synthesis of the following compound and similar compounds, in high stereochemical purity by a novel stereoselective alkylation process:
    Type: Application
    Filed: March 29, 2010
    Publication date: September 30, 2010
    Inventors: Wenxue Wu, Hongbiao Liao, David J.S. Tsai, David R. Andrews, Dinesh Gala, Gary M. Lee, Martin Lawrence Schwartz, Timothy L. McAllister, Xiaoyong Fu, Donal Maloney, Tiruvettipuram K. Thiruvengadam, Chou-Hang Tann
  • Publication number: 20100240893
    Abstract: The present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof and a process for making thereof. The compounds have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention also provides intermediate compounds useful in the process, as well as final products produced by the process, and salts or prodrugs thereof. The invention further provides a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases comprising administering an effective amount of a compound according to the invention to a patient in need thereof.
    Type: Application
    Filed: November 19, 2009
    Publication date: September 23, 2010
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: James Kanter, Anjali Pandey, James Robinson, Robert M. Scarborough
  • Publication number: 20100234377
    Abstract: The present invention relates to compounds of general formula (I): wherein A, Y, X, n and B are as defined herein; and their use in the treatment and prevention of metabolic disorders, inflammatory conditions, allergic conditions, fever, pain including allodynia and nociception, eating disorders, cachexia, brain injuries, cancer of the genitals, sleep apnea, cardiovascular disease, flush effect associated with nicotinic acid and related compounds or for the promotion of wound healing. Certain compounds of general formula (I) are new and the invention also relates to these compounds and to their use in medicine.
    Type: Application
    Filed: April 7, 2008
    Publication date: September 16, 2010
    Applicant: Evotec AG
    Inventors: Babette Aicher, Arndt-Rene Kelter, Thomas Stephen Coulter, Steven Taylor, Adams James Davenport, Thomas Hesterkamp, Christian Kirchhoff
  • Publication number: 20100234389
    Abstract: An object of the present invention is to provide a novel fused-ring compound which has a FAAH inhibitory effect and is useful as an analgesic. The present invention relates to a compound represented by formula (I): wherein symbols are as defined in the specification, or salt thereof.
    Type: Application
    Filed: October 9, 2008
    Publication date: September 16, 2010
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Masakuni Kori, Mitsunori Kouno
  • Publication number: 20100210618
    Abstract: The invention relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —O—C(?O)—; —C(?O)—C(?O)—; —NRX—C(?O)—; —Z—C(?O)—; —Z—NRX—C(?O)—; —C(?O)—Z—; —NRX—C(?O)—Z—; —C(?S)—; —NRX—C(?S)—; —Z—C(?S)—; —Z—NRX—C(?S)—; —C(?S)—Z—; —NRX—C(?S)—Z—; Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents —C(?O)—NRX— or —NRX—C(?O)—; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein sai
    Type: Application
    Filed: June 6, 2008
    Publication date: August 19, 2010
    Inventors: Jean-Pierre Andre Marc Bongartz, Joannes Theodorus Maria Linders, Lieven Mieerpoel, Guy Rosalia Eugeen Van Lommen, Erwin Coesemans, Mirielle Braeken, Christophe Francis Robert Nestor Buyck, Monique Jenny Marie Berwaer, Katharina Antonia Germania J.M. De Waepenaret, Peter Walter Maria Roevens, Petr Vladimirivich Davidenko
  • Publication number: 20100197919
    Abstract: The present invention provides a method for producing a 12-membered ring macrolide compound expected as a prophylactic or therapeutic agent for solid tumors and the like, and a production intermediate thereof. In detail, by acetalizing hydroxyl groups at 6- and 7-positions of a 12-membered ring macrolide compound being a raw material with dialkyl tin (IV) oxide and, after that, reacting the product with a carbamoyl halide derivative, the 7-position urethane derivative of the 12-membered ring macrolide compound being the target is effectively produced, without protecting hydroxyl groups at other positions.
    Type: Application
    Filed: July 4, 2008
    Publication date: August 5, 2010
    Inventors: Toshio Tsuchida, Masashi Yoshida, Kazuo Ohta, Katsura Kaneko, Kaichiro Kominato
  • Publication number: 20100190789
    Abstract: The invention relates to a DGAT inhibitor of formula (I): including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —C(?O)—; —O—C(?O)—; C(?O)—C(?O)—; —NRx—C(?O)—; —Z1—C(O)—; —Z1—NRx—C(?O)—; —C(?O)—Z1—; —NRx—C(?O)—Z1—; —S(?O)p-; —C(?S)—; —NRx—C(?S)—; —Z1—C(?S)—; —Z1—NRx—C(?S)—; —C(?S)—Z1-; NRx—C(?S)—Z—; Y represents NRx—C(=0)-Z2—; —NRx—C(=0)-Z2—NRy—; —NRx—C(=0)-Z 2—NRy—C(=0)—; —NRx—C(=0)-Z2—NRy—C(=0)-; O—; —NRx—C(=0)-Z2-0-; —NRx—C(=0)-Z2-0-C(=0)-; —NRx—C(=0)-Z2—C(=0)-; —NRx—C(=0)-Z2—C(=0)-; —NRx—C(=0)-0-Z2—C(=0)-; —NRx—C(=0)-0-Z2—C(=0)-0-; —NRx—C(?O)—O—Z2—O—C(?O)—; —NRx—C(?O)—Z2—C(?O)—NRy—; —NRx—C(?O)—Z2—NRy—C(=0)-NRy—; —C(?O)—Z2—; —C(?O)—Z2—O—; —C(=0)-NRx—Z2—; —C(=0)-NRx—Z2-0-; —C(=0)-NRx—Z2—C(=0)-0-; —C(=0)-NRx—Z2-0-C(=0)-; —C(=0)-NRx—Z2—NRy—; —C(=0)—NRx—Z2—NRy—C(=0)-; —C(=0)-NRx—Z2—NRy—C(=0)-0-; R1 represents C1-12alkyl optionally substituted with cyano, C1-4alkyloxy, C1-4alkyl-oxyC1-4alkyl
    Type: Application
    Filed: June 6, 2008
    Publication date: July 29, 2010
    Inventors: Jean-Pierre Andre Marc Bongartz, Joannes Theodorus Maria Linders, Lieven Meerpoel, Guy Rosalia Eugeen Van Lommen, Erwin Coesemans, Mirielle Braeken, Christophe Francis Robert Nestor Buyck, Monique Jenny Marie Berwaer, Katharina Antonia Germania J.M De Waepenaert, Peter Walter Maria Roevens, Gustaaf Maria Boeckx, Peter Vladimirivich Davidenko
  • Patent number: 7754722
    Abstract: The invention provides 2-carboxamide piperazine compounds of formula I, R3.IN\?N˜?R2I(0)z-oR4I wherein R?, R2, R3 and R4 are as defined in the claims and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for the treatment of mammalian infertility.
    Type: Grant
    Filed: September 19, 2003
    Date of Patent: July 13, 2010
    Assignee: Merck Serono SA
    Inventors: Sharad Magar, Andreas Goutopoulos, Yihua Liao, Matthias Schwarz, Russell J. Thomas
  • Publication number: 20100137336
    Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
    Type: Application
    Filed: July 10, 2008
    Publication date: June 3, 2010
    Inventor: Christelle Boléa
  • Patent number: 7709640
    Abstract: The present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof and a process for making thereof. The compounds have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention also provides intermediate compounds useful in the process, as well as final products produced by the process, and salts or prodrugs thereof. The invention further provides a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases comprising administering an effective amount of a compound according to the invention to a patient in need thereof.
    Type: Grant
    Filed: December 19, 2005
    Date of Patent: May 4, 2010
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: James Kanter, Anjali Pandey, James Robinson, Robert M. Scarborough
  • Patent number: 7678796
    Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
    Type: Grant
    Filed: April 25, 2007
    Date of Patent: March 16, 2010
    Assignee: AstraZeneca AB
    Inventors: Andreas Wallberg, Karolina Nilsson, Björn Holm, Mats Nagard, Kenneth Granberg, Abdelmalik Slassi, Louise Edwards, Methvin Isaac, Tao Xin, Tomislav Stefanac
  • Publication number: 20100048588
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, 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: Application
    Filed: January 27, 2009
    Publication date: February 25, 2010
    Inventors: Kristof Van Emelen, Hans Louis Jos De Winter, Alexy Borisovich Dyatkin, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Jimmy Arnold Viviane Van heusden
  • Patent number: 7638627
    Abstract: A process of preparing imatinib, either as the free base or as an acid addition salt, which process comprises reacting N-(2-methyl-5-aminophenyl-4-(3-pyridyl)-2-pyrimidine amine of formula (II) with a 4-(4-methyl-piperazino methyl)benzoyl halide of formula (III) in the presence of an inert organic solvent, so as to yield a hydrohalide salt of imatinib formula (I) where n represents 1, 2 or 3 and Hal represents bromo, chloro, fluoro or iodo, either in anhydrous or hydrated form, which can as desired optionally be further converted either to the free base or a further acid addition salt. The present invention is also concerned with imatinib prepared according to the above process.
    Type: Grant
    Filed: January 8, 2004
    Date of Patent: December 29, 2009
    Assignee: Cipla Limited
    Inventors: Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao
  • Publication number: 20090298845
    Abstract: The present application describes modulators of MIP-1? of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, T, W, R1, R4, R5, R5a and R5b are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using said modulators are disclosed.
    Type: Application
    Filed: August 5, 2009
    Publication date: December 3, 2009
    Inventors: Percy H. Carter, Cullen L. Cavallaro, George V. De Lucca
  • Publication number: 20090286261
    Abstract: An exemplary embodiment may be directed to a fluorescence polarization assay that screens compounds or agents for their affinity to hematopoietic prostaglandin D synthase (H-PGDS) based on their ability to displace a fluorophore-containing detection analyte bound to an enzyme comprising the primary amino acid sequence of H-PGDS. Another exemplary embodiment utilizes an enzyme having a maltose binding protein amino-acid sequence fused with an N-terminus of the enzyme.
    Type: Application
    Filed: May 13, 2009
    Publication date: November 19, 2009
    Applicant: CAYMAN CHEMICAL COMPANY
    Inventors: Kirk W. Maxey, Jeffrey K. Johnson, Karie L. McGowan, Nisha Palackal, Gregory W. Endres
  • Patent number: 7615557
    Abstract: This invention relates to a hydroxy-tetrahydro-naphthalene or an urea derivative formula (I) and salts thereof which are useful as active ingredients of pharmaceutical preparations, wherein A represents formula (II) or (III) wherein # represents the connection position to the molecule and Q1a, Q2a, Q3a and Q4a are defined, and E represents formula (IV) or (V) wherein # represents the connection position to the molecule and Q1b, Q2b, Q3b, Q4b, Q5b, R1b, na, ma, Xa and Ra are defined.
    Type: Grant
    Filed: September 22, 2004
    Date of Patent: November 10, 2009
    Assignee: Xention Limited
    Inventors: Axel Bouchon, Nicole Diedrichs, Achim Hermann, Klemens Lustig, Heinrich Meier, Josef Pernerstorfer, Elke Reissmuller, Jean De Vry, Muneto Mogi, Klaus Urbahns, Takeshi Yura, Hiroshi Fujishima, Masaomi Tajimi, Noriyuki Yamamoto, Yasuhiro Tsukimi, Hiroaki Yuasa, Jang Gupta, Fumihiko Hayashi
  • Publication number: 20090191125
    Abstract: Piperidine or piperazine compounds useful for treating neurodegenerated diseases characterized by the lack of dopamine neurons activity or for imaging the dopamine neurons are provided.
    Type: Application
    Filed: April 9, 2008
    Publication date: July 30, 2009
    Applicant: The General Hospital Corporation
    Inventors: David R. Elmaleh, Choi Sungwoon, Alan J. Fischman
  • Publication number: 20090118303
    Abstract: A serotonin 5-HT3 receptor agonist containing a compound represented by the general formula (1) [R1, R3 and R5 represent hydrogen atom, a lower alkyl group, a lower alkenyl group, a halogen atom, hydroxyl group, amino group, a lower alkoxy group, carboxyl group, carbamoyl group, or nitro group, R2 and R4 represent a halogen atom, hydroxyl group, or amino group, R6 represents hydrogen atom, a lower alkyl group, or a lower alkenyl group, R7 represents hydrogen atom, a lower alkyl group, a lower alkenyl group, or an aralkyl group, and m and n are integers of 1 to 3] or a physiologically acceptable salt thereof as an active ingredient and having both a serotonin 5-HT3 receptor antagonistic action and a serotonin 5-HT3 receptor activating action.
    Type: Application
    Filed: December 29, 2008
    Publication date: May 7, 2009
    Applicant: Research Foundation Itsuu Laboratory
    Inventors: Tamaki JIKYO, Koichi SHUDO
  • Patent number: 7514436
    Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where x, y, W, V, R2, R3, R4, R5, R6, R6a, R7, R7a, R8, R8a, R9 and R9a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
    Type: Grant
    Filed: July 29, 2004
    Date of Patent: April 7, 2009
    Assignee: Xenon Pharmaceuticals Inc.
    Inventors: Heinz W. Gschwend, Vishnumurthy Kodumuru, Shifeng Liu, Rajender Kamboj
  • Publication number: 20090048226
    Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1? converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-? inducing factor-(IGIF), or interferon-?-(“IFN-?”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting caspase activity and decreasing IGIF production and IFN-? production and methods for treating interleukin-1, apoptosis-, and interferon-?-mediated diseases using the compounds and compositions of this invention.
    Type: Application
    Filed: January 22, 2008
    Publication date: February 19, 2009
    Inventors: Marion W. Wannamaker, Guy W. Bemis, Paul S. Charifson, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, Keith P. Wilson, James W. Janetka, Robert J. Davies, Anne-Laure Grillot, Zhan Shi, Cornelia J. Forster
  • Patent number: 7485646
    Abstract: A serotonin 5-HT3 receptor agonist containing a compound represented by the general formula (1) [R1, R3 and R5 represent hydrogen atom, a lower alkyl group, a lower alkenyl group, a halogen atom, hydroxyl group, amino group, a lower alkoxy group, carboxyl group, carbamoyl group, or nitro group, R2 and R4 represent a halogen atom, hydroxyl group, or amino group, R6 represents hydrogen atom, a lower alkyl group, or a lower alkenyl group, R7 represents hydrogen atom, a lower alkyl group, a lower alkenyl group, or an aralkyl group, and m and n are integers of 1 to 3] or a physiologically acceptable salt thereof as an active ingredient and having both a serotonin 5-HT3 receptor antagonistic action and a serotonin 5-HT3 receptor activating action.
    Type: Grant
    Filed: September 8, 2005
    Date of Patent: February 3, 2009
    Assignee: Research Foundation Itsuu Laboratory
    Inventors: Tamaki Jikyo, Koichi Shudo
  • Publication number: 20080261978
    Abstract: The invention provides compounds of Formula (I) and pharmaceutical compositions comprising compounds of Formula (I).
    Type: Application
    Filed: March 7, 2008
    Publication date: October 23, 2008
    Inventors: Michael P. Clark, Mark A. Lockwood, Florence F. Wagner, Michael G. Natchus
  • Publication number: 20080207633
    Abstract: Urea derivatives which comprise piperidine or piperazine rings and further substitution are effective in ameliorating conditions characterized by unwanted calcium ion channel activity.
    Type: Application
    Filed: April 28, 2008
    Publication date: August 28, 2008
    Inventors: Hassan Pajouhesh, Hossein Pajouhesh, Yanbing Ding, Terrance P. Snutch