Plural Diazine Rings Patents (Class 544/357)
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Publication number: 20100267698Abstract: This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.Type: ApplicationFiled: January 5, 2010Publication date: October 21, 2010Inventors: Guiying Li, Pamela Albaugh, Kevin S. Currie, Guolin Cai, Linda M. Gustavson, Kyungae Lee, Alan Hutchison, George D. Maynard, Jun Yuan, Ling Hong Xie, Manuka Ghosh, Nian Liu, George P. Luke, Scott Mitchell, Martin Patrick Allen, Spiros Liras
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Publication number: 20100267721Abstract: Compound of formula (I) wherein W, X, Y, Z is —C(R?)? or N; R1 is hydrogen or alkyl, V is N or C (i.e.Type: ApplicationFiled: May 19, 2008Publication date: October 21, 2010Applicant: HIGH POINT PHARMACEUTICALS LLCInventors: Rolf Hohlweg, Jane Marie Lundbeck, Johannes Cornelis de Jong
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Publication number: 20100267708Abstract: The present invention relates to new compounds of formula (1) exhibiting excellent activity for glucokinase, and pharmaceutical compositions comprising the same as an active ingredient.Type: ApplicationFiled: December 22, 2008Publication date: October 21, 2010Applicant: LG Life Sciences Ltd.Inventors: Soon Ha Kim, Sung Bae Lee, Seung Hyun Yoon, Mi Kyoung Cho, Kyoung Hee Kim, Heui Sul Park, Hyoung Jin Kim
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Publication number: 20100261705Abstract: The present invention provides a carbostyril compound represented by General Formula (1) or a salt thereof, wherein A is a direct bond, a lower alkylene group, or a lower alkylidene group; X is an oxygen atom or a sulfur atom; R4 and R5 each represent a hydrogen atom; the bond between the 3 and 4 positions of the carbostyril skeleton is a single bond or a double bond; R1 is a hydrogen atom, etc; R2 is a hydrogen atom, etc; and R3 is a hydrogen atom, etc. The carbostyril compound or salt thereof of the present invention induces the production of TFF, and thus is usable for the treatment and/or prevention of disorders such as alimentary tract diseases, oral diseases, upper respiratory tract diseases, respiratory tract diseases, eye diseases, cancers, and wounds.Type: ApplicationFiled: November 3, 2009Publication date: October 14, 2010Inventors: Takeshi Kuroda, Takahito Yamauchi, Tomoichi Shinohara, Kunio Oshima, Chiharu Kitajima, Hitoshi Nagao, Tae Fukushima, Takahiro Tomoyasu, Hironobu Ishiyama, Ohta Kazuhide, Masaaki Takano, Takumi Sumida
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Publication number: 20100256356Abstract: Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: ApplicationFiled: January 26, 2010Publication date: October 7, 2010Applicants: Array BioPharma Inc., Genentech, Inc.Inventors: James F. Blake, Steven Armen Boyd, Jason De Meese, Kin Chiu Fong, John J. Gaudino, Tomas Kaplan, Allison L. Marlow, Jeongbeob Seo, Allen A. Thomas, Hongqi Tian, Frederick Cohen, Wendy B. Young
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Publication number: 20100256374Abstract: The present invention relates to a process for the preparation of compounds which are therapeutically active in the central nervous system. In one aspect, the invention relates to a process for the preparation of compounds of the general formula (I): wherein HA is a pharmaceutically acceptable acid and R1-R4 are each independently selected from the group consisting of hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, and di-C1-C6-alkylamino-C2-C6-alkoxy. The invention also relates to the use of said compound to manufacture a medicament for the treatment of a serotonin-related disorder.Type: ApplicationFiled: June 17, 2010Publication date: October 7, 2010Inventors: Tom Fleck, Bruce Fleck, Magnus Cernerud, Helena Lundström, Claes Löfström, Margit Pelcman, Alexander Paptchikhine, Emma Andersson, Alf Nygren
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Patent number: 7807672Abstract: Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substituents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.Type: GrantFiled: February 13, 2007Date of Patent: October 5, 2010Assignee: Schering CorporationInventors: Yongqi Deng, Gerald W. Shipps, Jr., Alan Cooper, Yang Nan, Tong Wang, M. Arshad Siddiqui, Hugh Zhu, Robert Sun, Joseph M. Kelly, Ronald Doll, Jagdish Desai, James J-S Wang, Youhao Dong, Vincent Madison, Li Xiao, Alan Hruza, Neng-Yang Shih
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Patent number: 7807671Abstract: This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with diketo piperazine and piperadine derivatives that possess unique antiviral activity useful for the treatment of HIV and AIDS.Type: GrantFiled: April 10, 2007Date of Patent: October 5, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, John F. Kadow, Zhongxing Zhang, Zhiwei Yin, Nicholas A. Meanwell, Alicia Regueiro-Ren, Jacob Swidorski, Ying Han, David J. Carini
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Publication number: 20100249127Abstract: The present invention relates to substituted indolo-pyridinone compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted indolo-pyridinone compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: March 31, 2010Publication date: September 30, 2010Applicant: ArQule, Inc.Inventors: Nivedita Namdev, Manish Tandon, Jianqiang Wang, Audra Dalton, David Vensel, Rocio Palma, Mark A. Ashwell, Neil Westlund
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Publication number: 20100240640Abstract: The present invention relates to new D3 and D2 dopamine receptor subtype preferring ligands of formula (I): wherein R1 and R2 represent independently a substituent selected from hydrogen, alkyl, aryl, cycloalkyl, aroyl, or R1 and R2 may form a heterocyclic ring with the adjacent nitrogen atom; X represents an oxygen or sulphur atom; n is an integer of from 1 to 2, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of a condition which requires modulation of dopamine receptors.Type: ApplicationFiled: May 12, 2010Publication date: September 23, 2010Applicant: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: Eva Againe Csongor, Janos Galambos, Katalin Nogradi, Istvan Vago, Istvan Gyertyan, Bela Kiss, Istvan Laszlovszky, Judit Laszy, Katalin Saghy
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Publication number: 20100240618Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: ApplicationFiled: September 8, 2009Publication date: September 23, 2010Applicant: ChemoCentryx, Inc.Inventors: Andrew M.K. Pennell, James B. Aggen, J.J. Kim Wright, Subhabrata Sen, Brian E. McMaster, Daniel Joseph Dairaghi, Wei Chen, Penglie Zhang
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Publication number: 20100240670Abstract: The invention relates to 4-[(arylmethyl)aminomethyl]piperidine derivatives of general formula (I) in the form of a base or an addition salt with an acid, and also in the form of a hydrate or solvate, and their preparation process and therapeutic application.Type: ApplicationFiled: January 26, 2010Publication date: September 23, 2010Applicant: SANOFI-AVENTISInventors: Michael BOSCH, Jean WAGNON
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Publication number: 20100239525Abstract: The present invention relates to substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: December 30, 2009Publication date: September 23, 2010Applicant: ArQule, Inc.Inventors: Syed M. Ali, Mark A. Ashwell, Sudharshan Eathiraj, Eugene Kelleher, Jean-Marc Lapierre, Yanbin Liu, Nivedita Namdev, Rocio Palma, Manish Tandon, David Vensel, Neil Westlund, Hui Wu, Rui-Yang Yang
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Patent number: 7799791Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R1 and R2 is H, and the other is selected from OR6, SR6, NR6R7, N3, Me, Et, CF3, SOR8 and SO2R8; or R1 and R2 are both H; one of R3 and R4 is H, and the other is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl and cyclohexyl; or R3 and R4 are joined together with the adjacent backbone carbon atom to form a spiro-C5-C6 cycloalkyl group; R6 and R7 are each independently selected from H, C1-8-alkyl and C3-8-cycloalkyl; or R6 and R7 are linked to form a cyclic group together with the nitrogen to which they are attached; R8 is C1-8-alkyl or C3-8-cycloalkyl; R9 is a para-substituted 6-membered monocyclic aryl or heteroaryl ring which includes up to five heteroatoms.Type: GrantFiled: January 8, 2009Date of Patent: September 21, 2010Assignee: Amura Therapeutics LimitedInventors: Martin Quibell, John Paul Watts
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Publication number: 20100234391Abstract: Novel N-alkyl substituted piperazines have been discovered, which are useful as insecticides or fungicides. Such compounds are of Formula (I) wherein X, Y, R1 and R2 are as defined herein.Type: ApplicationFiled: May 26, 2010Publication date: September 16, 2010Applicant: DOW AGROSCIENCES LLCInventors: Beth Anne Lorsbach, James Melvin Ruiz, Thomas Clarence Sparks, Michael Thomas Sullenberger, Irene Mae Morrison, Jeffery Dale Webster
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Publication number: 20100234377Abstract: 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: ApplicationFiled: April 7, 2008Publication date: September 16, 2010Applicant: Evotec AGInventors: Babette Aicher, Arndt-Rene Kelter, Thomas Stephen Coulter, Steven Taylor, Adams James Davenport, Thomas Hesterkamp, Christian Kirchhoff
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Publication number: 20100234285Abstract: The present invention provides compounds of Formula (I) that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase.Type: ApplicationFiled: March 10, 2010Publication date: September 16, 2010Inventors: Jeffrey Allen Pfefferkorn, Anthony Lai Ling
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Publication number: 20100234390Abstract: The present invention provides novel compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prodrugs thereof. The novel compounds are useful as antibacterial agents in the treatment of conditions such as nosocomial pneumonia, community acquired pneumonia, infections caused by vancomycin resistant enterococci (VRE), methicillin resistant Staphylococcus aureus (MRSA), Heamophilus influenzae (HI) and penicillin resistant Streptococcus pneumoniae (PRSP). The compounds of the present invention are effective against a number of human or animal pathogens including VRE, PRSP, HI and MRSA.Type: ApplicationFiled: June 20, 2008Publication date: September 16, 2010Inventors: Simi Pushpan, Uma Ramachandran, Mrinalkanti Kundu
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Publication number: 20100234389Abstract: 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: ApplicationFiled: October 9, 2008Publication date: September 16, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masakuni Kori, Mitsunori Kouno
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Patent number: 7795261Abstract: This invention concerns substituted I-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of schizophrenia, anxiety, depression, emesis and IBS. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1.Type: GrantFiled: December 17, 2003Date of Patent: September 14, 2010Assignee: Janssen Pharmaceutica NVInventors: Frans Eduard Janssens, François Maria Sommen, Benoît Christian Albert Ghislain De Boeck, Joseph Elisabeth Leenaerts
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Patent number: 7795257Abstract: The present invention provides compounds of the formula which are activators of glucokinase activity and, thus, may be employed as therapeutic agents for the treatment of glucokinase mediated conditions. Accordingly, the compounds of formula (I) may be employed for the prevention and the treatment of impaired glucose tolerance, type 2 diabetes and obesity.Type: GrantFiled: September 28, 2006Date of Patent: September 14, 2010Assignee: Novartis AGInventor: Gregory Raymond Bebernitz
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Publication number: 20100226882Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: February 17, 2010Publication date: September 9, 2010Inventors: Yat Sun Or, Xiaowen Peng, Ce Wang, Lu Ying, Datong Tang, Yao-Ling Qiu
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Patent number: 7790726Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: August 14, 2006Date of Patent: September 7, 2010Assignee: Chemocentryx, Inc.Inventors: Penglie Zhang, Andrew M. K. Pennell, John J. Kim Wright, Lianfa Li, Edward J. Sullivan, Wei Chen, Kevin Lloyd Greenman
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Publication number: 20100221214Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: February 9, 2010Publication date: September 2, 2010Inventors: Yat Sun Or, Ce Wang, Xiaowen Peng, Lu Ying, Yao-Ling Qiu
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Publication number: 20100222357Abstract: The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R3 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, and methods for preparation of the compounds and compositions. The invention further relates to methods for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders.Type: ApplicationFiled: May 13, 2010Publication date: September 2, 2010Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20100222318Abstract: The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.Type: ApplicationFiled: December 18, 2009Publication date: September 2, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Jean Damien Charrier, Steven Durrant, David Kay, Ronald Knegtel, Somhairle MacCormick, Michael Mortimore, Michael O'Donnell, Joanne Pinder, Alistair Rutherford, Anisa Nizarali Virani, Stephen Young, Philip Michael Reaper
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Publication number: 20100221216Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: February 17, 2010Publication date: September 2, 2010Inventors: Yat Sun Or, Datong Tang
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Patent number: 7786120Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: August 25, 2006Date of Patent: August 31, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Sharn Ramaya, Steven Durrant, Juan-Miguel Jimenez, Julian M. C. Golec, Michael Mortimore
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Publication number: 20100216992Abstract: The present invention generally relates to compositions including six membered heterocyclic 1,4-diaza-2-one moieties covalently bonded by a hydrazine bond and processes for producing the same. The compositions of the present invention may be utilized as peptido- and/or proteomimetics, for example,' in connection with alpha-helical proteins, like Bcl-2 proteins.Type: ApplicationFiled: February 27, 2008Publication date: August 26, 2010Applicant: UNIVERSITY OF SOUTH FLORIDAInventor: Mark L. McLaughlin
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Publication number: 20100216777Abstract: Methods for using aminopyrazine analogs to treat rho kinase-mediated diseases or rho kinase-mediated conditions, including controlling intraocular pressure and treating glaucoma, are disclosed. Ophthalmic pharmaceutical compositions useful in the treatment of eye diseases such as glaucoma, and additionally useful for controlling intraocular pressure, the compositions comprising an effective amount of aminopyrazine analogs, are also disclosed.Type: ApplicationFiled: May 5, 2010Publication date: August 26, 2010Applicant: ALCON, INC.Inventors: Mark R. Hellberg, Andrew Rusinko, Alan J. Henderson, Cheng Guo, Mark Hadden, Hélène Y. Decornez
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Publication number: 20100210621Abstract: A new polymorphic form of 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-{[(1S)-1-methyl-2-(methyloxy)ethyl]oxy}-N-(5-methylpyrazin-2-yl)benzamide, processes for making it and its use as an activator of glucokinase are described.Type: ApplicationFiled: February 15, 2010Publication date: August 19, 2010Applicant: AstraZeneca ABInventors: Sharon Ann BOWDEN, David Peter HOILE, Karin LÖVQVIST
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Publication number: 20100210618Abstract: 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 saiType: ApplicationFiled: June 6, 2008Publication date: August 19, 2010Inventors: 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
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Publication number: 20100210659Abstract: The present invention relates to a compounds of formula I wherein A, Ar, R, R2, R3, R4, p, and o are as defined in the specification and claims or to a pharmaceutically active salt thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, bipolar disorders, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: February 11, 2010Publication date: August 19, 2010Inventors: Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer
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Publication number: 20100210841Abstract: A process for preparing pharmaceutically active compounds of formula (I) or a salt thereof wherein R1, n, m, R3, R6, X1, X2, X3 and X4 are as defined in the specification, is described. Novel intermediates are also described and claimed.Type: ApplicationFiled: February 15, 2010Publication date: August 19, 2010Applicant: AstraZeneca ABInventors: Michael Butters, Jeffrey Crabb, Philip Hopes, Bharti Patel
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Publication number: 20100210661Abstract: An object of the present invention is to provide a STAT3/5 activation inhibitor. The present invention provides a STAT3/5 activation inhibitor containing an aromatic compound represented by the general formula or a salt thereof as an active ingredient: wherein X1 represents a nitrogen atom or a group —CH?, R1 represents a group —Z—R6, in which Z represents a group —CO—, a group —CH(OH)— or the like, R6 represents a 5- to 15-membered monocyclic, dicyclic or tricyclic saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms, R2 represents a hydrogen atom or a halogen atom, Y represents a group —O—, a group —CO—, a group —CH(OH)— or a lower alkylene group, and A represents a group wherein R3 represents a hydrogen atom, a lower alkoxy group or the like, p represents 1 or 2, R4 represents an imidazolyl lower alkyl group or the like.Type: ApplicationFiled: October 2, 2007Publication date: August 19, 2010Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Kazuo Sekiguchi, Takashi Suzuki, Yutaka Ohbuchi, Mitsuhiro Okuno, Naoto Ohi, Kenji Ohnishi, Masaaki Motoyama, Kenji Yoshida, Takeshi Kodama, Kazuhisa Sugiyama, Seiji Akamatsu, Kunihiko Kiyono, Yasuo Yanagihara, Takashi Watanabe, Kazuhiko Hayashi, Hideo Tanaka, Takumi Sumida
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Publication number: 20100210623Abstract: The present invention relates to pyrazine substituted pyrrolopyridines which are inhibitors of JAK kinases (JAK1, JAK2, JAK3 and/or TYK2) and/or PDK1 and are thus useful for the treatment of myeloproliferative disorders or cancer.Type: ApplicationFiled: October 21, 2008Publication date: August 19, 2010Inventors: David J. Guerin, Joon Jung, Elizabeth Stanton
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Publication number: 20100210635Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with Renin that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.Type: ApplicationFiled: March 23, 2007Publication date: August 19, 2010Applicant: Takeda Pharmaceutical Company LimitedInventors: Benjamin Jones, Andre A. Kiryanov, Stephen W. Kaldor
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Publication number: 20100210627Abstract: The invention provides compounds according to formula (I) their use and methods for preparation wherein A, X, Y, R1, R2 and R3 are defined herein. The compounds of the invention inhibit specific serine/threonine kinases involved in inflammatory processes and aberrant cell proliferation, and are thus useful for treating associated diseases and pathological conditions such as Pim kinase-mediated diseases and pathological conditions involving inflammation, including Chron's disease, inflammatory bowel disease, rheumatoid arthritis, and chronic inflammatory disease, or aberrant cell proliferation including various cancers.Type: ApplicationFiled: August 15, 2007Publication date: August 19, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Wang Mao, Tina Marie Morwick, Anthony S. Prokopowicz, III
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Publication number: 20100204213Abstract: The present invention relates to a sulfonamide derivative which is useful as an active ingredient of pharmaceutical preparations. The sulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis and other inflammatory/immunological disorders.Type: ApplicationFiled: April 19, 2010Publication date: August 12, 2010Inventors: Yingfu LI, Akihiko Watanabe, Timothy B. Lowinger, Kevin Bacon, Norihiro Kawamura, Takuya Shintani, Tetsuo Kikuchi, Toshiya Moriwaki, Klaus Urbahns, Keiko Eukushima, Noriko Nunami, Takashi Yoshino, Toshiki Murata, Megumi Yamauchi, Hiroko Yoshino
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Publication number: 20100203012Abstract: Disclosed herein is a compound of Formula 1: or a salt thereof, in which R1, R1a, R100, R100a, R2, R200, R3, R300, A, A1, Q, Q1 and BG are as defined herein. Also disclosed is the use of the compounds of Formula 1 to treat disorders of dysregulated apoptosis, such as cancer and cellular proliferative disorders.Type: ApplicationFiled: May 30, 2008Publication date: August 12, 2010Applicant: Aegera Therapeutics, Inc.Inventors: Alain Laurent, Patrick Bureau, James Jaquith, John Gillard, Yannick Rose
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Publication number: 20100197700Abstract: The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine: where A is —C(H)? or —N? and R1-7 are as defined herein.Type: ApplicationFiled: September 30, 2008Publication date: August 5, 2010Inventors: Valentina O Badescu, Sandra Ann Filla, Peter Thaddeus Gallagher, Maria Ann Whatton
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Patent number: 7767671Abstract: This invention provides a compound of Formula 1 where Ar, X, R1, R2, R3, and R4 are defined herein, or a pharmaceutically acceptable salt thereof useful in the prevention or inhibition of diseases associated with the Ras/Raf/MEK signaling cascade in a mammal, such as neoplasms, strokes, osteoporosis, cancer, rheumatoid arthritis, inflammatory disease, polycystic kidney disease, and colonic polyps, and methods of making the compounds of formula 1 and intermediates.Type: GrantFiled: September 23, 2008Date of Patent: August 3, 2010Assignee: WyethInventors: Dan Maarten Berger, Dennis William Powell, Biqi Wu
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Publication number: 20100190789Abstract: 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-oxyC1-4alkylType: ApplicationFiled: June 6, 2008Publication date: July 29, 2010Inventors: 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
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Publication number: 20100190980Abstract: Disclosed is a pyrazinamide compound represented by the formula (1), a tautomer, stereoisomer or pharmaceutically acceptable salt thereof, or a solvate of the compound or the tautomer, stereoisomer or pharmaceutically acceptable salt thereof, which has an excellent GK-activating activity and is therefore useful as a medicinal agent. (1) wherein R1 represents a hydrogen atom, a C1-8 alkyl group, a C3-8 cycloalkyl group, a C2-9 heterocyclyl group, a phenyl group, a C1-9 heteroaryl group, a C7-14 arylalkyl group or the like; R2 represents a C1-8 alkyl group, a C2-9 heterocyclyl group, a phenyl group, a C1-9 heteroaryl group or the like; Ar represents a monocyclic or fused polycyclic C1-9 heteroaryl group represented by the formula (2) or a C2-9 heterocyclyl group represented by formula (2); Y represents —S—, —O— or —NH—; and Z represents —S—, —O— or —CH2—.Type: ApplicationFiled: June 20, 2008Publication date: July 29, 2010Applicants: Taisho Pharmaceutical Co., Ltd, Nissan Chemical Industries, LtdInventors: Hiroki Umemiya, Kengo Watatani, Takanori Kawaguchi, Kenichi Kawabe, Takumi Okada, Shigetada Sasako, Noriko Saito
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Patent number: 7763616Abstract: The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.Type: GrantFiled: February 14, 2006Date of Patent: July 27, 2010Assignee: Schering CorporationInventors: Wensheng Yu, Seong Heon Kim, Gopinadhan N. Anilkumar, Stuart B. Rosenblum, Bandarpalle B. Shankar, Brian F. McGuinness, Douglas W. Hobbs, Yuefei Shao
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Publication number: 20100184765Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of Alk, Abl, Aurora-A, B-Raf, C-Raf, Bcr-Abl, BRK, Blk, Bmx, BTK, C-Kit, CSK, C-Src, EphB1, EphB2, EphB4, FLT1, Fms, Flt3, Fyn, FRK3, JAK2, KDR, Lck, Lyn, PDGFR?, PDGFR?, PKC?, SAPK2?, Src, SIK, Syk, Tie2 and TrkB kinases.Type: ApplicationFiled: June 10, 2008Publication date: July 22, 2010Inventors: Shenlin Huang, Zuosheng Liu, Pamela A. Albaugh, Xing Wang, Shifeng Pan, Yongping Xie, Guobao Zhang
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Publication number: 20100184776Abstract: The invention relates to a DGAT inhibitor of formula (I) including any stereochemically isomeric form thereof, wherein A represents CH or N; X represents O or NRx; the dotted line represents an optional bond in case A represents a carbon atom; Y represents a direct bond; —NRx—C(?O)—; —C(?O)—NRx—; —NRx—C(?O)—Z—; —NRx—C(?O)—Z—NRy—; —NRx—C(?O)—Z—NRy—C(?O)—; —NRx—C(?O)—Z—NRy—C(?O)—O—; —NRx—C(?O)—Z—O—; —NRx—C(?O)—Z—O—C(?O)—; —NRx—C(?O)—Z—C(?O)—; —NRx—C(?O)—Z—C(?O)—O—; —NRx—C(?O)—O—Z—C(?O)—; —NRx—C(?O)—O—Z—C(?O)—O—; —NRx—C(?O)—O—Z—O—C(?O)—; —NRx—C(?O)—Z—C(?O)—NRy—; —NRx—C(?O)—Z—NRy—C(?O)—NRy—; —C(?O)—Z—; —C(?O)—Z—O—; —C(?O)—NRx—Z—; —C(?O)—NRx—Z—O—; —C(?O)—NRx—Z—C(?O)—O—; —C(?O)—NRx—Z—O—C(?O)—; —C(?O)—NRx—O—Z—; —C(?O)—NRx—Z—NRy—; —C(?O)—NRx—Z—NRy—C(?O)—; —C(?O)—NRx—Z—NRy—C(?O)—O—; R1 represents optionally substituted C1-12alkyl; C2-6alkenyl; C2-6alkynyl; C3-6cycloalkyl; aryl1; aryl1C1-6alkyl; Het1; or Het1C1-6alkyl; provided that when Y represents —NRx—C(?O)—Z—; —NRx—C(?O)—Z—NRy; —NRx—C(?O)—Z—C(?O)—NRy—; —C(?O)—Z—;Type: ApplicationFiled: June 5, 2008Publication date: July 22, 2010Applicant: JANSSEN PHARMACEUTICA N.V.Inventors: Jean-Pierre Andre Marc Bongartz, Guy Rosalia Eugeen Van Lommen, Erwin Coesemans, Christophe Francis Robert Nestor Buyck
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Publication number: 20100184777Abstract: The present invention provides compounds of Formula (I) that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. The variables R1, R2, R3 and R4 are as described herein.Type: ApplicationFiled: January 20, 2010Publication date: July 22, 2010Inventors: John William Benbow, Jeffrey Allen Pfefferkorn
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Publication number: 20100179138Abstract: Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C?O)—, —(C?S)—, —SO.sub.Type: ApplicationFiled: February 19, 2010Publication date: July 15, 2010Applicants: Vernalis (Cambridge) Limited, Cancer Research Technology Ltd., The Institute Of Cancer ResearchInventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
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Publication number: 20100173909Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.Type: ApplicationFiled: December 10, 2009Publication date: July 8, 2010Applicant: ASTRAZENECA ABInventors: Gregory BASARAB, Pamela HILL, Brian SHERER, Fei ZHOU