Ring Sulfur In The Bicyclo Ring System Patents (Class 514/301)
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Publication number: 20110230472Abstract: It is an object of the present invention to provide a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a ring-fused azole compound shown in the present specification, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 25, 2009Publication date: September 22, 2011Applicant: Shionogi & Co., Ltd.Inventors: Yasunori Mitsuoka, Manami Masuda, Daisuke Taniyama
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Patent number: 8022057Abstract: Compounds of the following formula are provided for use with MEK: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: GrantFiled: November 7, 2008Date of Patent: September 20, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Qing Dong, Toufike Kanouni, Michael B. Wallace
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Publication number: 20110224251Abstract: The present invention provides for compounds of Formula I, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, and R7 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as therapeutic agents in the treatment of TGF?-mediated conditions, including cancer and fibrotic disorders. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.Type: ApplicationFiled: May 20, 2011Publication date: September 15, 2011Applicant: Graceway Pharmaceuticals, LLCInventors: Stephen D. Barrett, Mark L. Boys, Huifen Chen, James B. Kramer
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Publication number: 20110218158Abstract: Cytosine deaminase inhibitors and methods for identifying inhibitors of the anti-retroviral activity of APOBEC3G are described.Type: ApplicationFiled: September 22, 2009Publication date: September 8, 2011Inventors: Reuben S. Harris, Ming Li
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Publication number: 20110217301Abstract: The present invention relates to a method for treating and screening for compounds for the treatment of sepsis. More specifically, the treatment and screening methods are based on the discovery that granzyme B containing platelets (GzmB-platelet) causes apoptosis by direct contact with cells.Type: ApplicationFiled: April 6, 2011Publication date: September 8, 2011Applicant: THE CHILDREN'S RESEARCH INSTUTEInventor: ROBERT J. FREISHTAT
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Publication number: 20110217293Abstract: Provided herein are methods of treating postangiplasty, in-stent restenosis or atherosclerosis in an individual in need of such treatment, comprising the step of administering to said individual an effective dose of morelloflavone with or with a effective dose of one or more of an HMG-CoA reductase inhibitor or a hypolipidemic agent or lipid-lowering agent or other lipid agent or lipid modulating agent or anti-atherosclerotic agent. Also provided are pharmaceutical compositions comprising a morelloflavone or pharmaceutical combinations comprising a morelloflavone and one of an HMG-CoA reductase inhibitor or a hypolipidemic agent or lipid-lowering agent or other lipid agent or lipid modulating agent or anti-atherosclerotic agent.Type: ApplicationFiled: January 28, 2011Publication date: September 8, 2011Inventors: Kenichi Fujise, Nongporn Towatana, Wilawan Mahabusarakam
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Publication number: 20110212930Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: ApplicationFiled: May 5, 2011Publication date: September 1, 2011Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Donald J.P. Pinto, Mimi L. Quan, Michael J. Orwat, Yun-Long Li, Wei Han, Jennifer X. Qiao, Patrick Y.S. Lam, Stephanie L. Koch
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Publication number: 20110206667Abstract: This invention relates to nucleotide polymorphisms in the human Apo(a) gene and to the use of Apo(a) nucleotide polymorphisms in identifying whether a human subject will respond or not to treatment with acetylsalicylic acid.Type: ApplicationFiled: April 19, 2011Publication date: August 25, 2011Applicants: The Brigham and Women's Hospital, Inc., Applera CorporationInventors: Paul Ridker, Daniel Chasman, Dov Shiffman
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Publication number: 20110207767Abstract: This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.Type: ApplicationFiled: November 3, 2009Publication date: August 25, 2011Inventors: Patrick Henry Beusker, Rudy Gerardus Elisabeth Coumans, Ronald Christiaan Elgrtsma, Wiro Michaël Petrus Bernardus Menge, Johannes Albertus Frederikus Joosten, Henri Johannes Spijker, Franciscus Marinus Hendrikus De Groot
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Patent number: 8003662Abstract: Compounds of Formula I and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula I 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: GrantFiled: January 30, 2007Date of Patent: August 23, 2011Assignee: Array BioPharma, Inc.Inventors: James F. Blake, Steven Boyd, Jason De Meese, John J. Gaudino, Allison L. Marlow, Jeongbeob Seo, Allen A. Thomas, Hongqi Tian
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Publication number: 20110201632Abstract: The present invention is directed to 2,5-disubstituted piperidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: ApplicationFiled: October 15, 2009Publication date: August 18, 2011Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, Izzat T. Raheem, Anthony J. Roecker, John D. Schreier
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Publication number: 20110195953Abstract: The invention generally relates to thienopyridinone 5-HT4 receptor modulators, and in particular the use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating Alzheimer's disease, cognition disorders, depression, and anxiety.Type: ApplicationFiled: September 30, 2009Publication date: August 11, 2011Applicant: EPIX Delaware, Inc.Inventors: Dale S. Dhanoa, Oren Becker, Silvia Noiman, Pradyumna Mohanty, Dongli Chen, Mercedes Lobera, Laurence Wu, Yael Marantz, Boaz Inbal, Alexander Heifetz, Shay Bar-Haim, Sharon Shacham
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Patent number: 7994321Abstract: There are provided compounds of the formula wherein R1, R2, R3, X, Y, Q, Ring A and Ring B are as described. The compounds exhibit activity as anticancer agents.Type: GrantFiled: July 20, 2007Date of Patent: August 9, 2011Assignee: Hoffmann-La Roche Inc.Inventors: David Joseph Bartkovitz, Yi Chen, Xin-Jie Chu, Kin-Chun Luk
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Publication number: 20110190334Abstract: The present invention relates to compounds of Formula I where R1a, R1b, X, R2a, R2b, W, R3, R4, and R5 are as defined herein as well as pharmaceutically acceptable salts thereof. The compounds have been shown to act as MEK inhibitors which may be useful in the treatment of hyperproliferative diseases, like cancer and inflammation.Type: ApplicationFiled: November 3, 2010Publication date: August 4, 2011Applicant: NOVARTIS AGInventors: Mark G. Bock, Dinesh Chikkanna, Clive McCarthy, Henrik Moebitz, Chetan Pandit
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Patent number: 7989625Abstract: The invention relates to novel thienopyridine derivatives of formula (I), wherein R1, R2, R3, R4 and Y have the meaning cited in claim 1, are HSP90-inhibitors and can be used for producing a medicament for treating illnesses, wherein the inhibition, regulation and/or modulation of HSP90 plays a roll.Type: GrantFiled: May 11, 2006Date of Patent: August 2, 2011Assignee: Merck Patent GmbHInventors: Hans-Michael Eggenweiler, Michael Wolf
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Publication number: 20110184014Abstract: The present invention relates to new mGluR1 and mGluR5 receptor subtype preferring ligands of formula (I); wherein Y represents a substituent selected from hydrogen, methyl, fluoro, chloro, bromo, methoxy; Z is hydrogen or methyl; R is an optionally substituted heteroaryl, 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 pathological conditions which require the modulation of mGluR1 and mGluR5 receptors such as neurological disorders, psychiatric disorders, acute and chronic pain and neuromuscular dysfunctions of the lower urinary tract.Type: ApplicationFiled: December 19, 2006Publication date: July 28, 2011Inventors: Katalin Nogradi, Gyorgy Keseru, Attila Bielik, Tamas Gati, Krisztina Gal, Monika Vastag, Amrita Agnes Bobok
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Patent number: 7985859Abstract: The invention relates to processes for the preparation of clopidogrel and salts thereof. The inventors have developed a process for preparing racemic clopidogrel by racemizing R(?) clopidogrel. The process includes the step of reacting R(?) clopidogrel with a powered anhydrous base in one or more solvents.Type: GrantFiled: May 29, 2008Date of Patent: July 26, 2011Assignee: Wockhardt Ltd.Inventors: Jagdish Shukla, Anjum Reyaz Khan, Arvind Merwade, Mohammad Jaweed Mukarram Siddiqui, Yatendra Kumar
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Publication number: 20110178070Abstract: The invention relates to PI3K/mTOR inhibiting compounds consisting of the formula: wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: June 23, 2009Publication date: July 21, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Xianchang Gong, Bohan Jin, Massaki Hirose, Feng Zhou, Qing Dong
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Publication number: 20110172191Abstract: A series of thieno[2,3-b]pyridine derivatives, attached at the 2-position to a substituted anilino moiety, which are substituted in the 3-position by a carbonyl group linked to a pyrrolidin-1-yl ring which in turn forms part of a heteroatom-containing fused bicyclic ring system, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.Type: ApplicationFiled: December 17, 2010Publication date: July 14, 2011Applicant: UCB Pharma S.A.Inventors: James Andrew Johnson, Daniel Christopher Brookings, Barry John Langham, Judi Charlotte Neuss, Joanna Rachel Thorne
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Patent number: 7973050Abstract: Novel compounds in enantiomeric excess that are inhibitors of bacterial methionyl synthetase (MetRS) are disclosed. Also disclosed are methods for their preparation and their use in therapy as antibacterial agents, and in particular their use in therapy for Clostridium difficile infection.Type: GrantFiled: September 11, 2007Date of Patent: July 5, 2011Assignee: Crestone, Inc.Inventors: Joseph Guiles, Xicheng Sun, Nebojsa Janjic, Sarah Strong, Albert Charles Gyorkos
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Patent number: 7973051Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R3 have the significance given in claim 1 and which can be used in the form of pharmaceutical compositions.Type: GrantFiled: November 10, 2008Date of Patent: July 5, 2011Assignee: Hoffman-La Roche Inc.Inventors: Paul Hebeisen, Eric A. Kitas, Rudolf E. Minder, Peter Mohr, Hans Peter Wessel
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Publication number: 20110159049Abstract: The present invention relates to a granular pharmaceutical composition comprising a drug having a disagreeable taste, a wax and a sugar alcohol; a method for preparing the same; and a pharmaceutical product for oral administration, comprising the granular composition. The product excellently masks a disagreeable taste possessed by a drug and provides good sensation upon oral administration, and therefore is easily ingested by even the elderly, children, and patients suffering dysphagia. Moreover, the product is suitable for administration using tube.Type: ApplicationFiled: January 6, 2011Publication date: June 30, 2011Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Hiroaki NAKAGAMI, Tatsuya SUZUKI, Hideo KOBAYASHI, Akira KUROSAWA
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Publication number: 20110152301Abstract: The present invention describes novel methods of identifying compounds which inhibit HIV particle formation and Rev-dependent HIV production. The present invention also provides methods and compounds for inhibiting HIV particle formation and or treating patients infected with HIV.Type: ApplicationFiled: December 22, 2010Publication date: June 23, 2011Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: David Rekosh, Marie-Louise Hammarskjöld
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Publication number: 20110152254Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: January 24, 2011Publication date: June 23, 2011Applicant: Sirtris Pharmaceuticals, Inc.Inventors: Jean Bemis, Jeremy S. Disch, Pui Yee Ng, Christopher Oalmann, Robert B. Perni, Chi B. Vu
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Patent number: 7964612Abstract: The present invention provides for compounds of Formula I, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, and R7 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as therapeutic agents in the treatment of TGF?-mediated conditions, including cancer and fibrotic disorders. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.Type: GrantFiled: October 12, 2007Date of Patent: June 21, 2011Assignee: Graceway Pharmaceuticals, LLCInventors: Stephen D. Barrett, James B. Kramer, Mark L Boys, Huifen Chen
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Publication number: 20110144104Abstract: The present invention relates to pyrrolidinyl-alkyl-amide derivatives of formula (I) or (IA) wherein the variables are as defined herein, to their preparation and to their therapeutic use as CCR3 receptor ligands.Type: ApplicationFiled: January 26, 2011Publication date: June 16, 2011Applicant: SANOFI-AVENTISInventors: Agnes BEHR, Sandor BATORI, Veronika BARTANE BODOR, Zoltan SZLAVIK, Imre BATA, Katalin URBAN-SZABO, Zoltan KAPUI, Endre MIKUS
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Publication number: 20110144052Abstract: The invention relates to prodrugs of niacin and their use in pharmaceutical composition and therapeutic treatment of disease.Type: ApplicationFiled: November 17, 2010Publication date: June 16, 2011Inventor: Roger Tung
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Publication number: 20110136858Abstract: Composition and use of a medicament comprising a fixed dose combination of droloxifene and clopidogrel, or the pharmaceutically acceptable salts thereof, for treating or preventing a disorder associated with the loss of normal adult tissue architecture.Type: ApplicationFiled: December 4, 2009Publication date: June 9, 2011Inventor: David J. Grainger
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Publication number: 20110136779Abstract: The subject invention provides methods for reducing stroke rate, methods for preventing atrial remodeling, and methods for reversing atrial remodeling by administering a multiple ion channel blocker anti-arrhythmic to reduce atrial fibrillation (AF) episode duration and an anticoagulant (AC). According to some methods of the invention, the average AF episode duration can be reduced to less than about 24, 5, 3 or 1 hour(s), and the maximum AF episode duration may be reduced to less than about 20, 10 or 5 hours. According to some methods of the invention, the reduced stroke rate upon administration of multiple ion channel blocker and AC is less than the age-adjusted overall stroke rate. Further, some methods provide that patients who were refractory to one or more anti-arrhythmic drugs prior to administration of the multiple ion channel blocker may also be treated.Type: ApplicationFiled: November 23, 2010Publication date: June 9, 2011Inventors: Peter G. Milner, David Jack Ellis
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Publication number: 20110135603Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. 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.Type: ApplicationFiled: October 15, 2010Publication date: June 9, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Tiansheng Wang, Alexander Aronov, Mark Cornebise, Francois Maltais, Mark Ledeboer, Arnaud Le Tiran, Valerie Marone, David Messesrsmith, Kevin Cottrell, Jon H. Come, Gabriel Martinez Botella
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Patent number: 7956068Abstract: The present invention relates to compounds of formula (I) wherein c, X, Y, R2, R3, R4 and R6 are as defined herein, compositions and uses thereof for treating human immunodeficiency virus (HIV) infection. In particular, the present invention provides novel inhibitors of HIV integrase, pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HIV infection.Type: GrantFiled: November 3, 2008Date of Patent: June 7, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Rebekah J. Carson, Lee Fader, Stephen Kawai, Serge R. Landry, Youla S. Tsantrizos, Christian Brochu, Sebastien Morin, Mathieu Parisien, Bruno Simoneau
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Publication number: 20110130387Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: November 29, 2010Publication date: June 2, 2011Applicant: Sirtris Pharmaceuticals, Inc.Inventors: Joseph J. Nunes, Jill Milne, Jean Bemis, Roger Xie, Chi B. Vu, Pui Yee Ng, Jeremy S. Disch, Thomas Salzmann, David Armistead
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Publication number: 20110124675Abstract: The present invention provides the prasugrel bisulfate of formula (II) and pharmaceutical composition and use thereof. Prasugrel bisulfate of the present invention has good stability, oral absorbability, metabolic activity and platelet aggregation inhibition effect, and low toxicity, and is therefore a promising anticoagulant for preventing or treating diseases associated with thrombosis or embolism.Type: ApplicationFiled: July 31, 2008Publication date: May 26, 2011Inventor: Zhiquan Zhao
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Publication number: 20110124674Abstract: Disclosed are a compound of a formula (I) and its pharmaceutically-acceptable salt: wherein Q is CH or N; R1a, R1b, R1c and R1d are independently a C1-6 alkyl, a halo-C1-6 alkyl, etc.; R2 is a hydrogen atom, etc.; R3 is independently a hydrogen atom, a C1-6 alkyl, etc., or two R3's, taken together, form a bridge such as methylene, etc.; R4a and R4b are independently a hydrogen atom, a C1-6 alkyl, etc.; Z is a bicyclic aromatic hetero ring, etc.; Ar is a benzene ring, etc.; m1 and m2 are independently 0, 1 or 2; n is an integer of from 1 to 4. The compound and its salt act as a melanin concentrating hormone receptor antagonist, and are useful as a preventive or remedy for central system disorders, cardiovascular disorders, metabolic disorders, etc.Type: ApplicationFiled: July 14, 2009Publication date: May 26, 2011Inventors: Hiroyuki Kishino, Nagaaki Sato, Takao Suzuki
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Publication number: 20110123606Abstract: The invention relates to non hemolytic compositions containing an antiplatelet agent such as clopidogrel or ticlopidine; these compositions being characterized in that the antiplatelet agent is in the form of free base, and the composition contains at least one hydrophilic non ionic surfactant. The invention relates also a galenic form, a method of preparation of thereof, as well as therapeutic uses of thereof, especially in patients who suffer from undesirable effects related to hemolysis and/or gastrointestinal acidity.Type: ApplicationFiled: June 15, 2009Publication date: May 26, 2011Inventors: Thierry Breul, Claude Laruelle
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Patent number: 7947692Abstract: There are presented compounds of the formula or a pharmaceutically acceptable salt thereof, which are active adenosine A2B receptor antagonists and useful in the treatment of diabetes, diabetic retinopathy, asthma and diarrhea.Type: GrantFiled: May 11, 2007Date of Patent: May 24, 2011Assignee: Hoffmann-La Roche Inc.Inventors: John A. Brinkman, Adrian Wai-Hing Cheung, Fariborz Firooznia, Kevin Richard Guertin, Nicholas Marcopulos, Lida Qi, Jagdish Kumar Racha, Ramakanth Sarabu, Jenny Tan, Jefferson Wright Tilley
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Publication number: 20110118302Abstract: This invention relates to certain biphenyl-4-yl carbonylamino acid compounds, compositions, and methods for treating or preventing obesity and related diseases.Type: ApplicationFiled: July 14, 2010Publication date: May 19, 2011Applicant: Bayer Pharmaceuticals CorporationInventors: Roger Smith, Stephen J. O'Connor, Philip Coish, Derek Lowe, Roger B. Clark, Jeffrey Stebbins, Ann-Marie Campbell, Christiana Akuche, Tatiana Shelekhin
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Publication number: 20110118303Abstract: The present invention relates to compounds derived from taurine with non-steroidal anti inflammatory activity. In a first embodiment, the present invention relates to compounds derived from taurine, in which taurine is bound directly by means of an amide bond or through an spacing group, to a compound selected from the group of non-steroidal anti inflammatory compounds, cited as derived from taurine presenting the Formula (I): in which R means the component with non-steroidal anti inflammatory activity. In a second embodiment, the invention provides a process for obtaining the compounds of Formula (I) by reaction of taurine with a compound belonging to the group of non-steroidal anti inflammatory (NSAIs), in order to obtain a compound derived from taurine by direct bond or through a spacing group of the taurine to the NSAI. The invention also relates to the pharmaceutical compositions comprising at least one compound derived from taurine presenting non-steroidal anti inflammatory activity.Type: ApplicationFiled: April 9, 2009Publication date: May 19, 2011Applicants: EMS S.A., Universidade Estadual Paulista Julio De Mesquita Filho - UNESPInventors: Ednir de Oliveira Vizioli, Chung Man Chin, Renato Farina Menegon, Lorena Blau, Jean Leandro Dos Santos, Maria do Carmo Longo
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Patent number: 7943637Abstract: Novel thienopyridine derivatives of the formula (I), in which R1, R2, R3 and Y have the meanings indicated in claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: GrantFiled: February 10, 2006Date of Patent: May 17, 2011Assignee: Merck Patent GmbHInventors: Hans-Michael Eggenweiler, Michael Wolf
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Patent number: 7939527Abstract: Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.Type: GrantFiled: April 9, 2009Date of Patent: May 10, 2011Assignee: Janssen Pharmaceutica NVInventors: Genesis M. Bacani, Diego Broggini, Eugene Y. Cheung, Christa C. Chrovian, Xiaohu Deng, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Jimmy T. Liang, Susanne Lochner, Neelakandha S. Mani, Alejandro Santillán, Jr., Kathleen Sappey, Kia Sepassi, Virginia M. Tanis, Alvah T. Wickboldt, John J. M. Wiener, Hartmut Zinser
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Publication number: 20110105496Abstract: This invention relates generally to methods for the treatment of myosin heavy chain (MyHC)-mediated conditions, and in particular, cardiovascular conditions.Type: ApplicationFiled: December 19, 2006Publication date: May 5, 2011Inventors: Gabriel G. Gamber, Rishi K. Jain, Gary M. Ksander, Leslie W. McQuire, Lawrence S. Melvin, Moo J. Sung
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Publication number: 20110098293Abstract: This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and opthalmological diseases, disorders and conditions.Type: ApplicationFiled: February 27, 2009Publication date: April 28, 2011Inventors: Michael Mannion, Stephane Raeppel, Stephen William Claridge, Frederic Gaudette, Lijie Zhan, Ljubomir Isakovic, Oscar Mario Saavedra, Tetsuyuki Uno, Masashi Kishida, Arkadii Vaisburg
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Patent number: 7932390Abstract: There are provided compounds of the formula wherein R1, R2, R3, X, ring A and ring B are as described. The compounds exhibit anticancer properties.Type: GrantFiled: June 18, 2007Date of Patent: April 26, 2011Assignee: Hoffman-La Roche Inc.Inventors: Yi Chen, Kin-Chun Luk, Pamela Loreen Rossman, Sung-Sau So
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Publication number: 20110085985Abstract: The present invention relates to novel amyloid binding compounds of formula (I) and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET/) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents.Type: ApplicationFiled: May 28, 2009Publication date: April 14, 2011Inventors: James C. Barrow, Scott Harrison, James Mulhearn, Cyrille Sur, David L. Williams, Scott Wolkenberg
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Patent number: 7923450Abstract: The invention relates to compounds of formula wherein R1, R2, R3, R4, X and Y are as defined herein and to pharmaceutically active acid addition salts thereof. The compounds can be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.Type: GrantFiled: January 5, 2009Date of Patent: April 12, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Karlheinz Baumann, Alexander Flohr, Erwin Goetschi, Helmut Jacobsen, Synese Jolidon, Thomas Luebbers
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Publication number: 20110082136Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.Type: ApplicationFiled: June 8, 2009Publication date: April 7, 2011Inventors: Michelle Machacek, Gabriela de Almeida, Jonathan B. Grimm, Rachel N. MacCoss, Eric Romeo, Tony Siu, Catherine White, Kevin Wilson
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Publication number: 20110082170Abstract: The present invention discloses fused thienopyridyl compounds of general formula (I) wherein X1-X6, R5-R7, Z1 and L are as defined in the description. The resent invention also discloses a method for inhibiting the VR1 receptor in mammals using these compounds, a method for controlling pain, urinary incontinence, bladder overactivity, and inflammatory thermal hyperalgesia in mammals, and pharmaceutical compositions including those compounds.Type: ApplicationFiled: December 15, 2010Publication date: April 7, 2011Applicant: ABBOTT LABORATORIESInventors: Sean C. Turner, Tammie K. Jinkerson, Arthur R. Gomtsyan, Chih-Hung Lee
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Publication number: 20110077240Abstract: This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and opthalmological diseases, disorders and conditions.Type: ApplicationFiled: December 9, 2010Publication date: March 31, 2011Inventors: Michael Mannion, Stéphane Raeppel, Stephen William Claridge, Frédéric Gaudette, Lijie Zhan, Ljubomir Isakovic, Oscar Mario Saavedra, Tetsuyuki Uno, Masashi Kishida, Arkadii Vaisburg
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Publication number: 20110077154Abstract: The present invention relates to pyridin-4-ylmethyl sulfonamides of formula I wherein Het, Ra, Rc, Rf, m, n, p, R, A and Y are as defined in the claims, to the N-oxides, and salts thereof and their use for combating harmful fungi, and also to compositions and seed comprising at least one such compound. The invention also relates to a process and intermediates for preparing these compounds.Type: ApplicationFiled: May 20, 2009Publication date: March 31, 2011Applicant: BASF SEInventors: Alice Glaettli, Wassilios Grammenos, Bernd Mueller, Jan Klaas Lohmann, Marianna Vrettou
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Publication number: 20110077265Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds having the general formula U1-M-U2 wherein M is a linking group covalently joining R2, R3, R4 or R5 of U1 to an R2, R3, R4 or R5 group of U2; U1 and U2 have the general formula (I) and G, X1, X2, R2, R3, R3?, R4, R4? and R5, are as described herein.Type: ApplicationFiled: April 29, 2008Publication date: March 31, 2011Applicant: Genentech, Inc.Inventors: John A. Flygare, Frederick Cohen, Kurt Deshayes, Michael F. T. Koehler, Lewis J. Gazzard, Lan Wang, Chudi Ndubaku