The Additional Hetero Ring Is Five-membered And Unsaturated (e.g., Thienyl Piperazines, Etc.) Patents (Class 544/379)
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Publication number: 20130023522Abstract: Novel benzamide derivatives of formula (I) wherein W1, W2, R1 to R7, R8, X and Y have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.Type: ApplicationFiled: July 17, 2012Publication date: January 24, 2013Applicant: MERCK PATENT GMBHInventors: Henry YU, Jiezhen LI, Thomas E. RICHARDSON, Pandi BHARATHI, Brian H. HEASLEY, Andreas GOUTOPOULOS
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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
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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
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Publication number: 20130012708Abstract: A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13, SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10 alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.Type: ApplicationFiled: September 13, 2012Publication date: January 10, 2013Applicant: Nissan Chemical Industries LimitedInventors: Shingo Owada, Shunsuke Iwamoto, Kazufumi Yanagihara, Katsuaki Miyaji, Takanori Nakamura, Norihisa Ishiwata, Yutaka Hirokawa
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Patent number: 8338424Abstract: 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: GrantFiled: May 10, 2012Date of Patent: December 25, 2012Assignee: Theravance, Inc.Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
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Publication number: 20120316173Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: January 11, 2011Publication date: December 13, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alessandra Bartolozzi, Angela Berry, Doris Riether, Monika Ermann, James Edward Jenkins, Innocent Mushi
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Patent number: 8314091Abstract: The present invention relates to N-benzyl,N?-arylcarbonylpiperazine derivatives having the general formula I to pharmaceutical compositions comprising the same, and to the use of a these N-benzyl,N?-arylcarbonylpiperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterol and bile acids transport and metabolism.Type: GrantFiled: August 19, 2008Date of Patent: November 20, 2012Assignees: MSD OSS B.V., Pharmacopeia, Inc.Inventors: Koc-Kan Ho, Andrew Laird Roughton, Irina Neagu, Jui-Hsiang Chan, Nasrin Ansari, Michelle Lee Morris, Yajing Rong, Michael Ohlmeyer, Andrew John Cooke, Andrew Stanley Edwards, David Jonathan Bennett
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Patent number: 8309554Abstract: Hypoxia activated drug compounds having a structure of formula (I) are useful in the treatment of cancer and other hyperproliferative diseases.Type: GrantFiled: May 14, 2009Date of Patent: November 13, 2012Assignee: Threshold PharmaceuticalsInventors: Jason Lewis, Mark Matteucci, Tao Chen, Hailong Jiao
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Publication number: 20120277423Abstract: The present invention relates to: a ketone compound having transglutaminase-inhibiting activity, which is represented by the following Formula 1, 2, or 3: wherein R1 is a substituted or unsubstituted aryl or heterocyclyl group, R2, R3, and R4 are hydrogen atoms, n is 2, X is halogen, R5 and R6 independently represent a hydrogen atom or a substituted or unsubstituted C1-C10 alkyl, aryl, or aralkyl group, wherein R5 and R6 are not hydrogen atoms at the same time, or R5 and R6 may be taken together to form a saturated or unsaturated and substituted or unsubstituted heterocyclyl group containing a nitrogen atom (N); an inhibitor of protein crosslinking comprising the compound; and a composition for preventing or treating a protein-crosslinking causative disease, which comprises the compound or the protein crosslinking inhibitor.Type: ApplicationFiled: May 19, 2010Publication date: November 1, 2012Inventors: Katsuhiko Mikoshiba, Kozo Hamada, Akiko Terauchi, Shouichirou Ozaki, Jun-ichi Goto, Etsuko Ebisui, Akinobu Suzuki
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Publication number: 20120258965Abstract: The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives.Type: ApplicationFiled: June 22, 2012Publication date: October 11, 2012Applicants: The Johns Hopkins University, Cardioxyl PharmaceuticalsInventors: John P. TOSCANO, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
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Patent number: 8268828Abstract: This invention is directed to a 3-(amido or sulphamido)-4-(4-substituted-azinyl)benzamide or benzsulphonamide compound as defined herein. The 3-(amido or sulphamido)-(4-substituted-azinyl)benzamide or benzsulphonamide compound is useful as a inhibitor of the chemokine receptor CxCR3, and for preventing or treating a CxCR3 chemokine receptor mediated disease or condition related thereto in a patient in need of such.Type: GrantFiled: August 6, 2010Date of Patent: September 18, 2012Assignee: SanofiInventors: David Squire Thorpe, Martin Smrcina, Dagmar Dasha Cabel
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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
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Publication number: 20120220601Abstract: Compositions and methods for treatment of sexual dysfunctions by administering to a subject a pharmaceutical composition comprising a delta opioid receptor agonist in an amount effective to delay the onset of ejaculation in the subject during sexual stimulation.Type: ApplicationFiled: April 5, 2012Publication date: August 30, 2012Inventors: KWEN-JEN CHANG, KLIM KING, KESTUTIS P. BICIUNAS, ROBERT W. MCNUTT, JR., WILLIAM PENDERGAST, SHY-TAI JAN
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Publication number: 20120208807Abstract: This invention is directed to analogs of 5-(tetradecyloxy)-2-furancarboxylic acid (TOFA) and their use in the treatment of dermatological disorders or conditions characterized by sebaceous gland hyperactivity, such as acne and oily skin, and other dermatological disorders and conditions. This invention is also directed to pharmaceutical compositions comprising analogs of TOFA and a pharmaceutically acceptable excipient for dermatological or oral administration.Type: ApplicationFiled: July 1, 2010Publication date: August 16, 2012Applicant: VALOCOR THERAPEUTICS, INC.Inventors: Timothy Scott Daynard, Geoffrey C. Winters, David W.C. Hunt
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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
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Publication number: 20120189539Abstract: Inhibitors of Bcl-2/Bcl-xL and compositions containing the same are disclosed. Methods of using the Bcl-2/Bcl-xL inhibitors in the treatment of diseases and conditions wherein inhibition of Bcl-2/Bcl-xL provides a benefit, like cancers, also are disclosed.Type: ApplicationFiled: January 24, 2012Publication date: July 26, 2012Applicant: THE REGENTS OF UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Haibin Zhou, Jianfang Chen, Angelo Aguilar, Jennifer L. Meagher, Duxin Sun, Chao-Yie Yang, Liu Liu, Longchuan Bai, Donna McEachem, Jeanne Stuckey, Xiaoqin Li
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Publication number: 20120129100Abstract: An actinic ray-sensitive or radiation-sensitive resin composition including: (PA) a compound having a proton acceptor functional group and undergoing decomposition upon irradiation with an actinic ray or radiation to generate a compound reduced in or deprived of proton acceptor property or changed to be acidic from being proton acceptor-functioning, wherein a molar extinction coefficient ? of the compound (PA) at a wavelength of 193 nm as measured in acetonitrile solvent is 55,000 or less, and a pattern forming method using the composition are provided.Type: ApplicationFiled: August 17, 2010Publication date: May 24, 2012Applicant: FUJIFILM CORPORATIONInventors: Akinori Shibuya, Shuhei Yamaguchi, Shohei Kataoka, Michihiro Shirakawa, Takayuki Kato, Naohiro Tango
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Patent number: 8183239Abstract: The invention provides novel non-peptidic NPY Y2 receptor inhibitors useful in treating or preventing: anxiolytic disorders or depression; injured mammalian nerve tissue; conditions responsive to treatment through administration of a neurotrophic factor; neurological disorders; bone loss; substance related disorders; sleep/wake disorders; cardiovascular disease; obesity; or an obesity-related disorder. Compounds of the invention are also useful in modulating endocrine functions, particularly endocrine functions controlled by the pituitary and hypothalamic glands, and are therefore useful in the treatment or prevention of inovulation and infertility.Type: GrantFiled: October 27, 2006Date of Patent: May 22, 2012Assignee: Janssen Pharmaceutica NVInventors: Pascal Bonaventure, Nicholas I. Carruthers, Wenying Chai, Curt A. Dvorak, Jill A. Jablonowski, Dale A. Rudolph, Mark Seierstad, Chandravadan R. Shah, Devin M. Swanson, Victoria D. Wong
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Publication number: 20120122868Abstract: Derivatives of 2,5-piperazinedione of formula (I) are apoptotic peptidase activating factor 1 (Apaf-1) inhibitors, therefore they are useful as active pharmaceutical ingredients for the prophylaxis and/or treatment of a pathological and/or physiological condition associated with an increase of apoptosis.Type: ApplicationFiled: July 29, 2010Publication date: May 17, 2012Applicant: LABORATORIOS SALVAT, S.A.Inventors: Ángel Messeguer Pyepoch, Alejandra Moure Fernández, Daniel Gonzáles Pinacho, Isabel Masip Masip, Enrique Pérez Payá, Natividad García, Ester Monlleó Mas, Juanlo Catena Ruiz
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Patent number: 8153793Abstract: The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the general formula (II): wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the ring C is an aromatic carbocyclic ring etc.; R1 is carboxy etc.; R2 is independently a halogen atom etc.; R3 is optionally substituted alkyloxy etc.; R4 is independently a halogen atom etc.; R5 is independently optionally substituted alkyl etc.; M is sulfonyl etc.; Y is a single bond etc.; L1 is a single bond etc.; L2 is a single bond etc.; k is 0, 1, 2, 3 or 4; n is 0, 1 or 2; and q is 0, 1, 2 or 3; provided that a) k is not 0 when the ring B is a 6-membered nitrogen-containing heterocyclic ring containing one or two nitrogen atom(s) and the ring C is a benzene ring, etc.Type: GrantFiled: November 20, 2009Date of Patent: April 10, 2012Assignee: Shionogi & Co., Ltd.Inventors: Akira Kugimiya, Masahiko Fujioka, Yuki Tachibana, Takami Murashi
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Publication number: 20120022059Abstract: The present invention relates to novel substituted furancarboxamides, methods for their production, their use for the treatment and/or prevention of diseases, as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially retroviral diseases, in humans and/or animals.Type: ApplicationFiled: June 16, 2011Publication date: January 26, 2012Applicant: AiCuris GmbH & Co. KGInventors: Kai THEDE, Susanne Greschat, Steffen Wildum, Daniela Paulsen
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Publication number: 20120015958Abstract: The present invention relates to 1-(4-ureidobenzoyl)piperazine derivatives having the general Formula I (We bring to your attention that formula I is not provided on this electronic version as it is provided in the abstract of the paper copy) Wherein R1 is (C1-8)alkyl, (C3-8)cycloalkyl or (C3-8)cycloalkyl(C1-3)alkyl, each of which may be substituted by hydroxy, cyano or halogen; R2 represents 1 or 2 optional halogens; R3 is (C1-6)alkyl, (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl, each of which may be substituted by one or more halogens; A represents a heteroaryl ring system comprising 1-3 heteroatoms selected from N, O and S, which ring system is 5- or 6-membered when X is C, and 5-membered when X is N; n is 1 or 2; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same, and to the use of a these 1-(4-ureidobenzoyl)piperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterType: ApplicationFiled: August 26, 2009Publication date: January 19, 2012Inventors: Andrew John Cooke, David Jonathan Bennett, Andrew Stanley Edwards, Andrew Laird Roughton, Irina Neagu, Jui-Hsiang Chan, Koc Kan Ho, Nasrin Ansari, Michelle Lee Morris, Yajing Rong, Michael Ohlmeyer
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Publication number: 20110319448Abstract: 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: ApplicationFiled: September 9, 2011Publication date: December 29, 2011Applicant: THERAVANCE, INC.Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
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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
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Publication number: 20110288052Abstract: The class compounds of the present invention may be represented by Formula (I), wherein X may be O, S, or N. R1 and R2 are independently either H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl. R3 and R4 are independently either H, an aryl group, a heteroaryl group, and a heterocyclic ring group having 4 to 6 carbon atoms, wherein the aryl, heteroaryl, and heterocyclic moieties are optionally substituted with one or more of a first substitution group defined herein. In a further embodiment, R3 and R4 along with the atoms and bonds to which they are attached, form an optionally substituted 5-7 membered ring having at least one nitrogen atom within the ring structure.Type: ApplicationFiled: June 2, 2009Publication date: November 24, 2011Inventors: Craig A. Townsend, Kandasamy Subburaj, Jill Marie McFadden
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Publication number: 20110269747Abstract: Polyarylcarboxamide compounds of formula (I) are useful as lipid lowering agents.Type: ApplicationFiled: July 13, 2011Publication date: November 3, 2011Inventors: Lieven Meerpoel, Peter Walter Maria Roevens, Leo Jacobus Jozef Backx, Louis Jozef Elisabeth Van der Veken, Marcel Viellevoye
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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
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Publication number: 20110245264Abstract: The present disclosure is generally directed to compounds which can modulate G-protein coupled receptor 88, compositions comprising such compounds, and methods for modulating G-protein coupled receptor 88.Type: ApplicationFiled: October 1, 2010Publication date: October 6, 2011Inventors: Yingzhi Bi, Carolyn Diane Dzierba, Joanne J. Bronson, Kenneth Carson, Giovanni Cianchetta, Li Dong, Cynthia Fink, Michael Green, David Kimball, John E. Macor, Soojin Kwon, Jiancheng Wang, Yulian Zhang, Greg Zipp
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Patent number: 8022064Abstract: The present invention relates to compounds of general formula (I): wherein: R1 and R2, identical or different, represent: an atom of hydrogen or halogen, CN or NO2, with R1 and R2 not representing hydrogen simultaneously, m represents: 1 or 2 n represents: 0, 1 or 2 R3 represents: phenyl substituted or not by one or more residues chosen among halogen, hydroxyl or C1-C6 alkyl; C2-C6 alkyl substituted or not by one or more residues chosen among halogen or hydroxyl; cycloalkyl; pyridine; thiophene; pyrrole substituted or not by C1-C6 alkyl; thiazole or furan; or the therapeutically-acceptable salts or solvates thereof.Type: GrantFiled: June 19, 2007Date of Patent: September 20, 2011Assignee: Pierre Fabre MedicamentInventors: Michel Perez, Marie Lamothe, Bruno Le Grand, Robert Letienne
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Patent number: 8008302Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof, in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: GrantFiled: July 25, 2005Date of Patent: August 30, 2011Assignee: Merck Serono SAInventors: Dominique Swinnen, Agnes Bombrun, Jerome Gonzalez, Stefano Crosignani, Patrick Gerber, Catherine Jorand-Lebrun
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Publication number: 20110207609Abstract: 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 piperazines 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: October 26, 2009Publication date: August 25, 2011Applicant: BASF SEInventors: Liliana Parra Rapado, Frank Stelzer, Matthias Witschel, Thomas Seitz, Trevor William Newton, Julia Major, Tao Qu, William Karl Moberg, Dschun Song, Michael Rack, Timo Frassetto, Anja Simon, Robert Reinhard, Bernd Sievernich, Klaus Grossmann, Thomas Ehrhardt, Klaus Kreuz
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Publication number: 20110200553Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.Type: ApplicationFiled: April 7, 2011Publication date: August 18, 2011Applicant: Vertex Pharmaceuticals IncorporatedInventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen Ba, Oswy Z. Pereira, Thumkunta Jagadeeswar Reddy, Mohammed Arshad Siddiqui, Wuyi Wang, Constanin G. Yannopoulos
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Publication number: 20110201583Abstract: 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: ApplicationFiled: April 28, 2011Publication date: August 18, 2011Applicant: THERAVANCE, INC.Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
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Publication number: 20110190310Abstract: Hypoxia activated drug compounds having a structure of formula (I) are useful in the treatment of cancer and other hyperproliferative diseases.Type: ApplicationFiled: May 14, 2009Publication date: August 4, 2011Inventors: Jason Lewis, Mark Matteucci, Tao Chen, Hailong Jiao
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Publication number: 20110172195Abstract: Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins.Type: ApplicationFiled: March 15, 2011Publication date: July 14, 2011Applicant: ARIZONA BOARD OF REG. ON BEHALF OF THE UNIV. OF AZInventors: Gary A. Flynn, Andrea J. Yool, Elton Rodrigues Migliati, Leslie S. Ritter
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Patent number: 7968542Abstract: A compound represented by the formula (I) (wherein R1, R2, R3 and R4 are as defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.Type: GrantFiled: July 13, 2006Date of Patent: June 28, 2011Assignee: Nissan Chemical Industries, Ltd.Inventors: Katsuaki Miyaji, Kazufumi Yanagihara, Yukihiro Shigeta, Shunsuke Iwamoto, Masato Horikawa, Yutaka Hirokawa, Shingo Owada, Satoshi Nakano, Hirofumi Ota, Norihisa Ishiwata
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Publication number: 20110152234Abstract: The invention relates to thiophene carboxamides of formula (I), wherein A, R1, R2, R3, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: December 23, 2010Publication date: June 23, 2011Inventors: Alan Faull, Craig Johnstone, Andrew Morley, Jeffrey Philip Poyser
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Patent number: 7960385Abstract: 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: GrantFiled: September 5, 2008Date of Patent: June 14, 2011Assignee: Theravance, Inc.Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
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Publication number: 20110130381Abstract: Inhibitors of dihydroorotate dehydrogenase (DHODH) for the Plasmodium enzyme have been identified and characterized. The inhibitors have high specificity, submicromolar efficacy against cultured parasite strains, exhibit drug-like properties, and are not overtly cytotoxic.Type: ApplicationFiled: May 7, 2009Publication date: June 2, 2011Inventors: Cecilia Bastos, Michael L. Booker, Cassandra A. Celatka, Jon C. Clardy, Joseph Cortese, Vishal P. Patel, Renato Skerlj, Roger C. Wiegand, Dyann F. Wirth
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Patent number: 7951806Abstract: The present invention relates to an inhibitor of plasminogen activator inhibitor-1. The present invention further relates to a pharmaceutical composition that has an inhibitory action on PAI-1 activity and is useful in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity. Furthermore, the present invention relates to a novel compound having PAI-1 inhibitory activity represented by the following general formula (I), and a salt thereof. Each symbol is defined as those in the specification.Type: GrantFiled: March 12, 2008Date of Patent: May 31, 2011Assignee: Renascience Co., Ltd.Inventors: Toshio Miyata, Nagahisa Yamaoka, Hidehiko Kodama
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Publication number: 20110112081Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2). The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 and TYK2 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.Type: ApplicationFiled: July 1, 2009Publication date: May 12, 2011Inventors: Kevin Wilson, Gabriela de Almeida, Andrew Haidle, Kaleen Konrad, Michelle Machacek, Ann Zabierek
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Publication number: 20110104162Abstract: The present invention relates to a compound of general formula (I): and also to the pharmaceutically acceptable salts thereof, to the isomers or isomer mixtures thereof in all proportions, in particular to an enantiomer mixture, and especially to a racemic mixture. The present invention also relates to the use of these compounds as a medicament, and in particular for the treatment of cancer, and also to the compositions containing them.Type: ApplicationFiled: June 15, 2009Publication date: May 5, 2011Applicant: Cytomics SystemsInventors: Denis Carniato, Karine Jaillardon, Olivier Busnel, Mathieu Gutmann, Jean-Francois Briand, Benoit Deprez, Dominique Thomas, Cécile Bougeret
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Patent number: 7935703Abstract: Compounds of Formula I or pharmaceutically acceptable salts or solvates thereof: wherein Ar1, Ar2, A, X, Y, m, n and R1, R2, R3, R4 and R5 are as described in the specification, processes for their preparation, pharmaceutical formulations comprising them and their use in therapy, particularly in the therapy of neurological and psychiatric disorders associated with glutamate dysfunction.Type: GrantFiled: January 5, 2007Date of Patent: May 3, 2011Assignee: AstraZeneca ABInventors: Abdelmalik Slassi, Methvin Isaac, Jalaj Arora, Dean Brown
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Publication number: 20110092496Abstract: A compound represented by the formula (I) (wherein R1, R2, R3 and R4 are as defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.Type: ApplicationFiled: November 29, 2010Publication date: April 21, 2011Applicant: Nissan Chemical Industries, Ltd.Inventors: Katsuaki MIYAJI, Kazufumi Yanagihara, Yukihiro Shigeta, Shunsuke Iwamoto, Masato Horikawa, Yutaka Hirokawa, Shingo Owada, Satoshi Nakano, Hirofumi Ota, Norihisa Ishiwata
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Publication number: 20110086822Abstract: The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.Type: ApplicationFiled: October 8, 2010Publication date: April 14, 2011Inventors: Mark L. Nelson, Kwasi Ohemeng, Roger Frechette, Paul Abato, Victor Amoo, Upul Bandarage, Joel Berniac, Beena Bhatia, Jackson Chen, Mohamed Y. Ismail, Oak Kim, Laura Honeyman, Rachid Mechiche, Andre Pearson, Laxma Reddy Nagavelli, Paul Sheahan, Atul K. Verma, Peter Viski, Tadeusz Warchol
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Patent number: 7915413Abstract: The invention relates to at least one compound of general formula I wherein R1 is phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, or pyridine N-oxide, where each R1 phenyl and R1 heteroaromatic ring may optionally and independently be substituted by 1, 2 or 3 substituents selected from CF3, methyl, iodo, bromo, fluoro, and chloro; R2 is independently selected from ethyl and isopropyl; R3 is hydrogen or fluoro; R4 is —NH2 or —NHSO2R5; and R5 is hydrogen, —CF3, or C1-C6 alkyl, or pharmaceutically acceptable salts thereof, at least one process for making at least one compound in accordance with Formula I; at least one method for treating at least one ? receptor associated condition with at least one compound in accordance with Formula I; and at least one pharmaceutical composition comprising at least one compound in accordance with Formula I.Type: GrantFiled: May 3, 2007Date of Patent: March 29, 2011Assignee: AstraZeneca ABInventors: William Brown, Christopher Walpole, Niklas Plobeck
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Patent number: 7868205Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: GrantFiled: September 24, 2004Date of Patent: January 11, 2011Assignee: MethylGene Inc.Inventors: Oscar Moradei, Isabelle Paquin, Silvana Leit, Sylvie Frechette, Arkadii Vaisburg, Jeffrey M. Besterman, Pierre Tessier, Tammy C. Mallais
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Publication number: 20100324025Abstract: 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: ApplicationFiled: September 21, 2009Publication date: December 23, 2010Applicant: University of WashingtonInventors: 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
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Publication number: 20100305088Abstract: This invention is directed to a 3-(amido or sulphamido)-4-(4-substituted-azinyl)benzamide or benzsulphonamide compound as defined herein. The 3-(amido or sulphamido)-(4-substituted-azinyl)benzamide or benzsulphonamide compound is useful as a inhibitor of the chemokine receptor CxCR3, and for preventing or treating a CxCR3 chemokine receptor mediated disease or condition related thereto in a patient in need of such.Type: ApplicationFiled: August 6, 2010Publication date: December 2, 2010Applicant: SANOFI-AVENTISInventors: David S. Thorpe, Martin Smrcina, Dagmar D. Cabel
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Publication number: 20100280018Abstract: A compound of formula (I), or an enantiomer or diastereoisomer thereof, or a salt, hydrate or solvate thereof: for the treatment or prophylaxis of arthritis in mammals.Type: ApplicationFiled: July 20, 2010Publication date: November 4, 2010Applicants: Laboratoires Serono S.A., Vernalis (Oxford) LimitedInventors: Gilles Pain, Stephen John Davies, Agnes Bombrun