Plural Ring Nitrogens In The Additional Hetero Ring (e.g., Imidazole, Pyrazine, Etc.) Patents (Class 514/235.8)
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Publication number: 20110218187Abstract: The invention relates to compounds of formula wherein the substituents R1, R2 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, especially a neoplastic disease, in particular leukaemia, and a method for the treatment of such a disease.Type: ApplicationFiled: May 12, 2011Publication date: September 8, 2011Inventors: Werner BREITENSTEIN, Pascal FURET, Sandra JACOB, Paul William MANLEY
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Patent number: 8012959Abstract: A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided. A pyrimidine derivative or a salt thereof, which has an arylamino or arylethylamino group which may be substituted with a specified substituent, at the 2-position, amino group substituted with benzyl group or the like, at the 4-position, and carbamoyl group which may be substituted, at the 5-position, is provided.Type: GrantFiled: September 22, 2008Date of Patent: September 6, 2011Assignee: Astellas Pharma Inc.Inventors: Shinya Nagashima, Hiroshi Nagata, Masashiro Iwata, Masaki Yokota, Hiroyuki Moritomo, Eiichi Nakai, Sadao Kuromitsu, Keiko Ohga, Makoto Takeuchi
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Publication number: 20110212080Abstract: 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: ApplicationFiled: July 28, 2009Publication date: September 1, 2011Inventors: Umar Faruk Mansoor, Panduranga Adulla Reddy, M. Arshad Siddiqui
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Publication number: 20110212077Abstract: The invention provides biaryl meta-pyrimidine compounds having the general structure (A). The pyrimidine compounds of the invention are capable of inhibiting kinases, such as members of the Jak kinase family, and various other specific receptor and non-receptor kinases.Type: ApplicationFiled: August 24, 2010Publication date: September 1, 2011Applicant: TargeGen, Inc.Inventors: Glenn Noronha, Chi Ching Mak, Jianguo Cao, Joel Renick, Andrew McPherson, Binqi Zeng, Ved P. Pathak, Daniel L. Lohse, John D. Hood, Richard M. Soll
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Patent number: 8008293Abstract: The present invention relates to a compound represented by formula (I): wherein R1 represents a C1-3 alkyl group, R2 represents a hydrogen atom or a C1-3 alkyl group, Ar represents a phenyl group or the like which may be substituted with 1 to 3 substituents, X represents an oxygen atom or the like, n and m are the same or different and integers of 0 to 2, or a pharmacologically acceptable salt, and use thereof as a medicament.Type: GrantFiled: February 27, 2008Date of Patent: August 30, 2011Assignee: Eisai R&D Management Co., Ltd.Inventors: Teiji Kimura, Koki Kawano, Eriko Doi, Noritaka Kitazawa, Mamoru Takaishi, Koichi Ito, Toshihiko Kaneko, Takeo Sasaki, Nobuaki Sato, Takehiko Miyagawa, Hiroaki Hagiwara
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Publication number: 20110207735Abstract: The invention relates to novel cyanopyrimidinones, process for their preparation, and the use thereof for producing medicaments for improving perception, concentration, learning and/or memory.Type: ApplicationFiled: May 2, 2011Publication date: August 25, 2011Inventors: Martin HENDRIX, Lars BĂ„RFACKER, Heike Heckroth, Dagmar KARTHAUS, Adrian TERSTEEGEN
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Publication number: 20110207734Abstract: The present invention relates to Azine Derivatives, pharmaceutical compositions comprising the Azine Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: ApplicationFiled: April 14, 2011Publication date: August 25, 2011Inventors: Anandan Palani, Dong Xiao, Robert G. Aslanian, Michael Y. Berlin, Ashwin U. Rao, Xiao Chen, Yoon Joo Lee, Sylvia Degrado, Ning Shao, Ying R. Huang, Zhidan Liu
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Publication number: 20110207733Abstract: The invention encompasses pyrimidine derivatives as gamma secretase modulators, useful for treating diseases associated with the deposition of beta-amyloid peptide in the brain, such as Alzheimer's disease, or of preventing or delaying the onset of dementia associated with such diseases. Pharmaceutical compositions and methods of use are included.Type: ApplicationFiled: July 31, 2009Publication date: August 25, 2011Inventors: Alexey A. Rivkin, Sean P. Ahearn, Stephanie M. Chichetti
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Publication number: 20110206783Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.Type: ApplicationFiled: October 21, 2009Publication date: August 25, 2011Inventors: Christopher S. Burgey, Zhengwu J. Deng, Diem N. Nguyen, Daniel V. Paone, Anthony W. Shaw
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Patent number: 8003643Abstract: The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.Type: GrantFiled: November 18, 2009Date of Patent: August 23, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Mark T. Bilodeau, Peter C. Chua, Nicholas D. P. Cosford, Jacob M. Hoffman, Johnny Yasuo Nagasawa
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Publication number: 20110201602Abstract: The present invention relates to chemical compounds having a general formula I wherein A, B, D, E, G, H1-5 and R1-4 are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of these kinases. For example, the compounds are capable of modulating kinase enzymes thereby influencing the process of angiogenesis and treating angiogenesis-related diseases and other proliferative disorders, including cancer and inflammation. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of protein kinases.Type: ApplicationFiled: November 22, 2010Publication date: August 18, 2011Applicant: Amgen Inc.Inventors: Stephanie D. GEUNS-MEYER, Brian L. HODOUS, Stuart C. CHAFFEE, Paul TEMPEST, Phillip R. OLIVIERI, Rebecca E. JOHNSON, Brian K. ALBRECHT, Vinod F. PATEL, Victor J. CEE, Joseph L. KIM, Steven BELLON, Xiaotian ZHU, Yuan CHENG, Ning XI, Karina ROMERO, Hanh Nho NGUYEN, Holly L. DEAK
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Publication number: 20110201599Abstract: A compound according to Formula I: or a pharmaceutically-acceptable salt thereof, wherein R1, R3, A, B and D are as defined in the specification; pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: July 2, 2009Publication date: August 18, 2011Applicant: EXELIXIS, INC.Inventors: Suleyman Bahceci, Bryan Chan, Diva Sze-Ming Chan, Jeff Chen, Timothy Patrick Forsyth, Maurizio Franzini, Vasu Jammalamadaka, Joon Won Jeong, Lisa Renee Jones, Ryan Michael Kelley, Moon Hwan Kim, James W. Leahy, Morrison B. Mac, Robin Tammie Noguchi, Pallavi Rao, Brian Hugh Ridgway, Wei Xu, Yong Wang
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Publication number: 20110201589Abstract: The invention relates to compounds of formula (I) wherein R1, R1a, R1b, R2, R3 and X, X1, X2, X3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.Type: ApplicationFiled: August 10, 2009Publication date: August 18, 2011Applicant: EVOTEC AGInventors: James Madden, David James Hallett, Alastair Parkes, Ali Raoof, Xialou Wang
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Publication number: 20110195966Abstract: The invention relates to a pharmaceutical combination which comprises (a) a phosphoinositide 3-kinase inhibitor compound of formula (I) and (b) a mTOR inhibitor for the treatment of a target of rapamycin (mTOR) kinase dependent disease, especially a cancer disease; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a proliferative disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal, especially a human.Type: ApplicationFiled: October 29, 2009Publication date: August 11, 2011Applicant: NOVARTIS AGInventors: Carlos Garcia-Echeverria, Sauveur-Michel Maira
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Patent number: 7994204Abstract: The present invention aims to provide compounds which have an inhibitory effect on the binding between S1P and its receptor Edg-1(S1P1) and which are useful for pharmaceutical purposes. A compound represented by formula (I) or a pharmaceutically acceptable salt thereof: [wherein Ar represents a monocyclic heterocyclic ring containing one or two nitrogen atoms, A represents an oxygen atom or the like, Y1, Y2 and Y3 each represent a carbon atom or a nitrogen atom, R1 represents a hydrogen atom, a C1-C6 alkyl group or the like, R2 represents a C1-C6 alkyl group, a C3-C8 cycloalkyl group or the like, R3 represents a C1-C18 alkyl group or the like, R4 represents a hydrogen atom or a C1-C6 alkyl group, and R5 represents a C1-C10 alkyl group or the like].Type: GrantFiled: February 6, 2007Date of Patent: August 9, 2011Assignee: Taisho Pharmaceutical Co., LtdInventors: Naoya Ono, Tetsuo Takayama, Fumiyasu Shiozawa, Hironori Katakai, Tetsuya Yabuuchi, Tomomi Ota, Takeshi Koami, Rie Nishikawa
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Publication number: 20110190259Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.Type: ApplicationFiled: March 15, 2011Publication date: August 4, 2011Applicant: IRM LLCInventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, Bei Chen, Tetsuo Uno, Yunho Jin, Tao Jiang
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Publication number: 20110190280Abstract: The present invention provides thiazole and oxazole compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.Type: ApplicationFiled: August 27, 2008Publication date: August 4, 2011Inventors: George Adjabeng, Neil Bifulco, Ronda G. Davis-Ward, Scott Howard Dickerson, Kelly Horne Donaldson, Philip Anthony Harris, Keith Hornberger, Kimberly Petrov, Tara Renae Rheault, Gregory Schaaf, John Stellwagen, David Edward Uehling, Alex Gregory Waterson
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Publication number: 20110190271Abstract: The present invention provides 2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferative diseases such as tumorigenic cancers.Type: ApplicationFiled: December 29, 2010Publication date: August 4, 2011Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Ankush Argade, Rajinder Singh, Hui Li, David Carroll, Susan Catalano
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Publication number: 20110190298Abstract: The present invention provides compounds of Formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent; diseases or disorders associated with the activity of GPR119.Type: ApplicationFiled: July 9, 2009Publication date: August 4, 2011Applicant: IRM LLCInventors: Robert Epple, Gerald Lelais, Victor Nikulin
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Publication number: 20110183962Abstract: The invention provides methods for modulating, e.g., antagonizing, the activity of the Hedgehog signaling pathway, and for treating Hedgehog related disorders such as cancers (e.g., medulloblastoma). In particular, the invention provides methods for inhibiting aberrant growth states resulting from phenotypes such as Ptch loss-of-function, Hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function by administering to a mammal combinations of Smoothened inhibitors (e.g., a compound of Formula I, Formula II, or Formula III, or any of the compounds listed herein or incorporated by reference) and cholesterol biosynthesis pathway inhibitors (e.g., statins), Gli inhibitors, and/or Phosphatidylinositol 3-kinase (PI3K) inhibitors.Type: ApplicationFiled: September 28, 2009Publication date: July 28, 2011Applicant: Novartis AGInventors: Marion Dorsch, John E. Monahan, Michael Patrick Morrissey, Shifeng Pan, Juliet Williams
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Publication number: 20110183957Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.Type: ApplicationFiled: August 4, 2009Publication date: July 28, 2011Inventors: John Wityak, Leticia M. Toledo-Sherman, Celia Dominguez, Stephen Martin Courtney, Christopher John Yarnold, Paula C. De Aguiar Pena, Andreas Scheel, Dirk Winkler
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Publication number: 20110172231Abstract: There are provided compounds of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as indicated in claim 1, useful in disorders where ZAP-70 and/or Syk inhibition plays a role or caused by a malfunction of signal cascades connected with FAK.Type: ApplicationFiled: March 23, 2011Publication date: July 14, 2011Inventors: Rolf BAENTELI, Gerhard Zenke, Nigel Graham Cooke, Rudolf Duthaler, Gebhard Thoma, Anette Von Matt, Toshiyuki Honda, Naoko Matsuura, Kazuhiko Nonomura, Osamu Ohmori, Ichiro Umemura, Klaus Hinterding, Christos Papageorgiou
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Publication number: 20110172215Abstract: The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.Type: ApplicationFiled: May 4, 2009Publication date: July 14, 2011Inventors: George Adjabeng, Jeffrey Leroy Adams, Scott Howard Dickerson, Keith Hornberger, Neil W. Johnson, Kevin Kuntz, Kimberly Petrov, Jeffrey M. Ralph, Tara Renae Rheault, Gregory Schaaf, John Stellwagen, Xinrong Tian, David E. Uehling, Alex G. Waterson, Brian Wilson
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Publication number: 20110172230Abstract: [Object] To provide a compound which can be used for the treatment of a disease associated with fatty acid amide hydrolase (FAAH), particularly urinary frequency, urinary incontinence and/or overactive bladder. [Means for solution] It is confirmed that a urea compound chemical-structurally characterized by having a piperidine or piperazine ring or a salt thereof has an excellent FAAH-inhibitory activity, and thus the present invention is completed. The urea compound or its pharmaceutically acceptable salt of the present invention can increase the effective bladder capacity and ameliorate the state of urinary frequency, and is therefore useful as an agent for treating urinary frequency, urinary incontinence and/or overactive bladder.Type: ApplicationFiled: August 22, 2007Publication date: July 14, 2011Inventors: Takahiro Ishii, Takashi Sugane, Akio Kakefuda, Tatsuhisa Takahashi, Tokatoshi Kanayama, Kentaro Sato, Ikumi Kuriwaki, Chika Kitada, Jotaro Suzuki
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Publication number: 20110172212Abstract: Novel amine compounds which are represented by the following formula (1) and efficacious against diseases such as a viral infectious disease with HIV, rheumatism, and cancer metastasis; typically, A1 and A2 represent a hydrogen atom or a substitutable monocyclic or polycyclic heteroaromatic ring and W represents a substitutable benzene ring or any group represented by the following formula (10) or (11): where X represents O, CH2, C(?O), NR11, or CHR35 and D represents a group represented by the following formula (6): [Formula 4] -Q-Y—B??(6) where Q represents a single bond, NR12, or a group represented by the formula (13): and Y represents a group represented by the following formula (7): [Formula 6] —(CR18R19)m3- or —(CR20R21)m4-z-(CR22R23)m5-??(7) where z represents a substitutable monocyclic or polycyclic aromatic ring; and B represents —NR25R26; and R1 to R26 in the above formulae represent a hydrogen atom, an alkyl group, an alkenyl group, or an alkynyl group.Type: ApplicationFiled: March 18, 2011Publication date: July 14, 2011Applicant: KUREHA CORPORATIONInventors: Atsushi SAITOU, Shigeyuki Kikumoto, Masahiro Ono, Ryo Matsui, Masashi Yamamoto, Tomohiro Sawa, Shigeru Suzuki, Mikiro Yanaka
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Publication number: 20110166117Abstract: The invention relates to substituted phenoxyacetic acids (I) as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: ApplicationFiled: December 30, 2010Publication date: July 7, 2011Inventors: Roger Bonnert, Stephen Brough, Andrew Davies, Timothy Luker, Thomas McInally, Ian Millichip, Garry Pairaudeau, Anil Patel, Rukhsana Rasul, Stephen Thom
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Publication number: 20110166137Abstract: The present invention relates to substituted naphthalenyl-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted naphthalenyl-pyrimidine 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 29, 2010Publication date: July 7, 2011Applicant: ArQule, Inc.Inventors: Mark A. Ashwell, Chris Brassard, Audra Dalton, Jason Hill, Robert Nicewonger, David Vensel
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Publication number: 20110166120Abstract: The present invention relates to a compound of the formula I wherein R1 to R6, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: March 11, 2011Publication date: July 7, 2011Inventors: Michael Joseph Luzzio, Kevin Daniel Freeman-Cook, Samit Kumar Bhattacharya, Matthew Merrill Hayward, Catherine Angela Hulford, Christopher Lowell Autry, Xumiao Zhao, Jun Xiao, Kendra Louise Nelson
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Patent number: 7973039Abstract: The present invention is related to 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: December 19, 2005Date of Patent: July 5, 2011Assignee: Merck Serono SAInventors: Dominique Swinnen, Agnes Bombrun, Patrick Gerber, Catherine Jorand-Lebrun
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Publication number: 20110159019Abstract: Provided is a compound which is useful as an active ingredient for a pharmaceutical having a PKC? inhibition activity, particularly a pharmaceutical composition for inhibiting acute rejection occurring in transplantation. The present inventors have conducted extensive studies on a compound having a PKC? inhibition activity, and as a result, they have found that a compound having a structure such as aralkyl and the like on an amino group at the 2-position and also having a structure such as an adamantylalkyl group and the like on an amino group at the 4-position of 2,4-diaminopyrimidine, or a salt thereof has an excellent PKC? inhibition activity, thereby completing the present invention. The 2,4-diaminopyrimidine compound of the present invention can be used as a PKC? inhibitor or an inhibitor of acute rejection occurring in transplantation.Type: ApplicationFiled: August 31, 2009Publication date: June 30, 2011Inventors: Akira Tanaka, Koichiro Mukoyoshi, Shigeki Kunikawa, Yuji Takasuna, Jun Maeda, Noboru Chida, Shinya Nagashima
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Publication number: 20110159085Abstract: A pharmaceutical capsule comprises a shell having encapsulated therewithin a liquid solution of ABT-263 or a pharmaceutically acceptable salt thereof in a substantially non-ethanolic carrier that comprises as pharmaceutically acceptable excipients (a) at least one phospholipid, (b) at least one solubilizing agent for the at least one phospholipid, selected from the group consisting of glycols, glycerides and mixtures thereof, (c) at least one non-phospholipid surfactant and (d) at least one sulfur-containing antioxidant. The capsule is useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.Type: ApplicationFiled: December 21, 2010Publication date: June 30, 2011Applicant: ABBOTT LABORATORIESInventors: Ping Tong, Deliang Zhou, Geoff G.Z. Zhang, Katherine R. Heemstra, Cristina M. Fischer, Nathaniel D. Catron, Eric A. Schmitt, Yeshwant D. Sanzgiri
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Publication number: 20110152235Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway.Type: ApplicationFiled: December 23, 2010Publication date: June 23, 2011Applicant: Jasco Pharmaceuticals, LLCInventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Robert B. Nicewonger, Yvonne L. Flanders, Stephane A. Dumas
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Publication number: 20110152262Abstract: Compounds of formula (I) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is a group selected from 2,6-dimethyl-3-pyridyl or 4,6-dimethyl-3-pyridyl, R4 represents methyl and R5 represents hydrogen or methyl or, R4 and R5 together with the nitrogen atom to which they are attached represent morpholino and pharmaceutically acceptable derivatives thereof are described, as are processes for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.Type: ApplicationFiled: February 25, 2011Publication date: June 23, 2011Applicant: GLAXO GROUP LIMITEDInventors: Alan David Borthwick, Deirdre Mary Bernadette Hickey, John Liddle, Andrew McMurtrie Mason
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Publication number: 20110152245Abstract: The invention relates to compounds of formula wherein R, R1, R2, X, and Y are as defined herein and to a pharmaceutically suitable acid addition salt thereof. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: ApplicationFiled: December 16, 2010Publication date: June 23, 2011Inventors: Katrin Groebke Zbinden, Roger Norcross, Philippe Pflieger
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Patent number: 7964592Abstract: Novel pyrimidine derivatives of formula I to process for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: GrantFiled: March 12, 2004Date of Patent: June 21, 2011Assignee: Novartis AGInventors: Carlos Garcia-Echeverria, Takanori Kanazawa, Eiji Kawahara, Keiichi Masuya, Naoko Matsuura, Takahiro Miyake, Osamu Ohmori, Ichiro Umemura
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Patent number: 7964597Abstract: Disclosed are motilin agonists, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.Type: GrantFiled: November 26, 2008Date of Patent: June 21, 2011Assignee: Glaxo Group LimitedInventors: Darren Jason Mitchell, Jonathan Thomas Seal, Geoffrey Stemp, Mervyn Thompson, Susan Marie Westaway
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Publication number: 20110142856Abstract: The present invention relates to a compound represented by formula (I-0): wherein symbols in formula have the same meanings as described in the present specification, a salt thereof, an N-oxide thereof or a solvate thereof or a prodrug thereof, and medical use thereof. The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoidarthritis, arthritis, retinopathy, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.Type: ApplicationFiled: February 15, 2011Publication date: June 16, 2011Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Masaya KOKUBO, Yoshikazu Takaoka, Shiro Shibayama
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Patent number: 7960560Abstract: The invention relates to A 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivative having the general Formula I wherein R1 is H, (C1-6)alkyl (optionally substituted with oxo, OR4, COOR5, halogen or CN), (C2-6)alkenyl, (C2-6)alkynyl, (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl; R2 and R2? are independently H or (C1-3)alkyl; or R2 and R2? form together with the carbon atom to which they are bound a (C3-5)cycloalkyl group; R3 represents H or 1 to 4 F substituents; Y represents or NR8R9; X represents CHR6, CF2, O, S, SO or SO2; R4 and R5 are (C1-6)alkyl; R6 is H, OR7 or CN; R7 is (C1-3)alkyl; R8 is (C5-7)cycloalkyl comprising a heteroatom selected from O, S, SO and SO2; R9 is H or (C1-4)alkyl; o and m represent the ortho or meta position of the substituent Y—CH2; or a pharmaceutically acceptable salt thereof; as well as to the use of said 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivatives in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, canceType: GrantFiled: December 1, 2009Date of Patent: June 14, 2011Assignee: N.V. OrganonInventors: Marcelis van der Stelt, Joseph Maria Gerardus Barbara Cals
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Publication number: 20110136796Abstract: Presently provided are compounds according to the formula (I) or (II), and pharmaceutical compositions comprising the compounds, wherein R1, R4, and R5 are defined herein. Such compounds and compositions are useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine -2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.Type: ApplicationFiled: April 24, 2009Publication date: June 9, 2011Applicants: NEWLINK GENETICS, LANKEANAU INSTITUTE FOR MEDICAL RESEARCHInventors: Mario R. Mautino, Sanjeev Kumar, Firoz Jaipuri, Jesse Waldo, Tanay Kesharwani, Nicholas N. Vahanian, Charles J. Link, Judith Lalonde, George Prendergast, Alexander Muller, William Malachowski
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Publication number: 20110135604Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: December 1, 2010Publication date: June 9, 2011Applicant: Gilead Sciences, Inc.Inventors: Anthony Casarez, Mingzhe Ji, Choung U. Kim, Xiaoning C. Sheng, Qiaoyin Wu
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Publication number: 20110135600Abstract: Compounds of the formula (I), in which X1, X2, X3, X4, X5, R1, R2, R3, R3?, R4, R6 and R7 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: July 16, 2009Publication date: June 9, 2011Inventors: Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
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Publication number: 20110136797Abstract: Certain cyclopropyl amines are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases.Type: ApplicationFiled: February 16, 2011Publication date: June 9, 2011Inventors: Nicholas I. Carruthers, Michael A. Letavic
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Publication number: 20110135650Abstract: The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt or a solvate thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.Type: ApplicationFiled: June 1, 2010Publication date: June 9, 2011Inventors: Samuel CHACKALAMANNIL, Tin-Yau CHAN, Mariappan V. CHELLIAH, Martin C. CLASBY, Michael DWYER, William J. GREENLEE, Tomokazu HIRABAYASHI, Santhosh NEELAMKAVIL, Hidemitsu NISHIDA, Fumihiko SAITOH, Unmesh SHAH, Yan XIA
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Patent number: 7956053Abstract: The invention relates to compounds of formula wherein the substituents R1, R2 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, especially a neoplastic disease, in particular leukaemia, and a method for the treatment of such a disease.Type: GrantFiled: June 22, 2009Date of Patent: June 7, 2011Assignee: Novartis AGInventors: Werner Breitenstein, Pascal Furet, Sandra Jacob, Paul W Manley
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Publication number: 20110129440Abstract: The present invention relates to novel Heterocyclic Urea and Thiourea Derivatives of formula (I), compositions comprising the Heterocyclic Urea and Thiourea Derivatives, and methods for using the Heterocyclic Urea and Thiourea Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase.Type: ApplicationFiled: October 27, 2008Publication date: June 2, 2011Inventors: Praveen K. Tadikonda, David F. Cauble, Timothy J. Guzi, M. Arshad Siddiqui
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Publication number: 20110130386Abstract: A compound of formula (I) wherein: R1 and R2 are independently selected from hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; and RN1 and RN2 are selected from hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms.Type: ApplicationFiled: April 24, 2009Publication date: June 2, 2011Inventors: Mark Frigerio, Heather Mary Ellen Duggan, Marc Geoffrey Hummersone, Keith Allan Menear, Niall Morrison Barr Martin, Celine Cano, Roger John Griffin, Bernard Thomas Golding, Ian Robert Hardcastle
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Publication number: 20110130401Abstract: Compounds of general formula (1) wherein A, B, R1 to R5, Rx m, n and p are defined as described in the specification, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and the use thereof [as] medicaments.Type: ApplicationFiled: May 21, 2010Publication date: June 2, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ioannis Sapountzis, Daniel Kuhn, Heinz Stadtmueller
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Publication number: 20110124646Abstract: A method of treating a disease associated with angiogenesis by administering a therapeutically effective amount of a compound represented by the formula (1) or a salt thereof wherein the ring X represents R1 and R2 independently represent a hydrogen atom, an alkyl, an aryl or an aromatic heterocyclic; R3 represents a hydrogen atom, a halogen atom, a hydroxy, an alkoxy, an aryloxy, an alkyl, an aryl, an amino, an alkylamino, a cycloalkylamino, an arylamino, an alkylcarbonylamino, an arylcarbonylamino, a mercapto, an alkylthio, an arylthio, an alkylsulfinyl or a nonaromatic heterocyclic; A1 represents a sulfur atom, a sulfinyl or a sulfonyl; and A2 represents an alkylene.Type: ApplicationFiled: January 24, 2011Publication date: May 26, 2011Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Hisashi Tajima, Takahiro Honda, Kenji Kawashima, Kazuyoshi Okamoto, Minoru Yamamoto
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Publication number: 20110124619Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.Type: ApplicationFiled: November 17, 2010Publication date: May 26, 2011Inventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Neal Michael Smith, Jeffrey Paul Stonehouse, Cherylin Francis Preston
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Publication number: 20110118263Abstract: The invention discloses benzothiophene alkanol piperazine derivatives and their use as antidepressants. The invention discloses the said benzothiophene alkanol piperazine derivative having triple inhibition effect on the reuptake of 5-HT, NA and DA. Compared with clinical used antidepressants so far having single target, e.g. desipramine and fluoxetine, and clinical used antidepressants so far having double targets, e.g venlafaxine and duloxetine, the said benzothiophene alkanol piperazine derivatives of the present invention may have a broader indication range and less toxic and side effects to nervous system. The benzothiophene alkanol piperazine derivatives are the compounds with the following formula or their pharmaceutically acceptable salts, wherein Ar1, R1-R4, X, Y, m and n have the same definition as defined in claim 1.Type: ApplicationFiled: June 30, 2009Publication date: May 19, 2011Applicant: CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang) Co. Ltd.Inventors: Jianqi Li, Kai Gao, Na Lv