Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 546/284.1)
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Patent number: 8278290Abstract: The present invention relates to compounds of general formula (I) as tublin polymerization inhibitors and methods for preparing such compounds.Type: GrantFiled: February 14, 2006Date of Patent: October 2, 2012Assignee: Biononics LimitedInventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn
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Publication number: 20120232083Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.Type: ApplicationFiled: March 7, 2012Publication date: September 13, 2012Inventors: Usa REILLY, Michael MELNICK, Matthew F. BROWN, Mark S. PLUMMER, Justin MONTGOMERY, Ye CHE, Loren PRICE
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Publication number: 20120214770Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.Type: ApplicationFiled: May 1, 2012Publication date: August 23, 2012Applicant: BIONOMICS LIMITEDInventors: JASON HUGH CHAPLIN, GURMIT SINGH GILL, DAMIAN WOJCIECH GROBELNY, BERNARD LUKE FLYNN, GABRIEL KREMMIDIOTIS
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Publication number: 20120214769Abstract: The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.Type: ApplicationFiled: April 8, 2011Publication date: August 23, 2012Applicant: METABASIS THERAPEUTICS, INC.Inventors: Jorge E. Gomez-Galeno, K. Raja Reddy, Paul D. van Poelje, Robert Huerta Lemus, Thanh Huu Nguyen, Matthew P. Grote, Qun Dang, Scott J. Hecker, Venkat Reddy Mali, Mingwei Chen, Zhili Sun, Serge Henri Boyer, Haiqing Li, William Craigo
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Publication number: 20120214845Abstract: Disclosed herein is an active metabolite (“M20”) of a molecule that is useful as a thrombin receptor antagonist: Also disclosed are formulations of this compound, synthetic routes to this compound, and methods of treating a variety of cardiovascular conditions, including acute coronary syndrome and peripheral arterial disease, and of effecting secondary prevention, by orally administering the active metabolilte.Type: ApplicationFiled: June 2, 2010Publication date: August 23, 2012Inventors: Kimberly Nguyen Voronin, Natalia A. Penner
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Publication number: 20120183660Abstract: The present invention provides isomannide derivatives having structural formula (I) as shown below and certain subgenera or species thereof, as flavoring agents or tastants, flavor or taste modifiers, and/or flavor/taste enhancers, particularly, savory (“umami”) flavoring agent or tastant, savory taste modifiers, and/or savory flavor enhancers, for ingestible compositions. The present invention also provides methods of preparing isomannide derivatives having the structural formula (II) shown below and certain subgenera or species thereof.Type: ApplicationFiled: June 30, 2010Publication date: July 19, 2012Applicant: Senomyx, Inc.Inventors: Catherine Tachdjian, Sara L. Adamski-Werner, Jeffrey M. Yamamoto, Hengyuan Lang, Donald S. Karanewsky
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Publication number: 20120172369Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (DGAT) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: ApplicationFiled: September 3, 2010Publication date: July 5, 2012Inventors: Pauline C. Ting, Joe F. Lee, Robert G. Aslanian
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Publication number: 20120165339Abstract: A cyclopropane derivative represented by the following formula (I) or a pharmaceutically acceptable salt thereof has orexin receptor inhibitory action, and thus, is extremely useful as an agent for preventing or treating sleep disorder or dyssomnia caused by orexin, including insomnia as a typical example: wherein A1, A2 and A3 each independently represent an aryl group, a heterocyclyl group or the like, R1, R2 and R3 each independently represent a hydrogen atom, a C1-6 alkyl group or the like, X represents an oxygen atom or the like, and L represents a bond or the like.Type: ApplicationFiled: December 20, 2011Publication date: June 28, 2012Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Taro Terauchi, Ayumi Takemura, Yuji Kazuta, Fumihiro Ozaki, Takashi Doko, Yu Yoshida, Toshiaki Tanaka, Keiichi Sorimachi, Yoshimitsu Naoe, Carsten Beuckmann
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Publication number: 20120157403Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein E, A, G M, Het, B, X, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.Type: ApplicationFiled: February 24, 2012Publication date: June 21, 2012Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yuguang Wang, Yan Xia
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Publication number: 20120157487Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: December 9, 2011Publication date: June 21, 2012Applicant: ALLERGAN, INC.Inventors: Haiqing Yuan, Richard I. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
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Publication number: 20120148955Abstract: A resist composition including: a base component (A) which exhibits changed solubility in a developing solution under action of acid; a nitrogen-containing organic compound component (C) containing a compound (C1) represented by general formula (c1) shown below; and an acid generator component (B) which generates acid upon exposure, provided that the compound (C1) is excluded from the acid generator component (B): wherein RN represents a nitrogen-containing heterocyclic group which may have a substituent; X0 represents a linear or branched divalent aliphatic hydrocarbon group of 1 to 10 carbon atoms, a cyclic divalent aliphatic hydrocarbon group of 3 to 20 carbon atoms or a divalent aliphatic hydrocarbon group of 3 to 20 carbon having a cyclic partial structure, or any one of these groups in which some or all of the hydrogen atoms thereof have been substituted with fluorine atoms; and M+ represents an organic cation.Type: ApplicationFiled: December 6, 2011Publication date: June 14, 2012Applicant: TOKYO OHKA KOGYO CO., LTD.Inventors: Yoshiyuki Utsumi, Kenichiro Miyashita, Akiya Kawaue
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Publication number: 20120142529Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.Type: ApplicationFiled: August 7, 2008Publication date: June 7, 2012Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Melloney Tyte, Stephane André Marie Jeanmart, Christopher John Mathews, Louisa Robinson
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Publication number: 20120142914Abstract: This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists.Type: ApplicationFiled: February 10, 2012Publication date: June 7, 2012Inventors: Tiruvettipuram K. Thiruvengadam, Anantha R. Sudhakar, Ngiap Kie Lim, Daw-Iong Kwok, George G. Wu, Tao Wang, Mingsheng Huang, Michael D. Green
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Patent number: 8193363Abstract: The present invention relates to novel derivatives that are suitable as precursors to compounds that are useful for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. The compounds deriving from these precursors are useful in methods of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease by positron emission tomography (PET) as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents. Furthermore, the present invention also discloses the precursor compounds in crystalline form.Type: GrantFiled: August 20, 2009Date of Patent: June 5, 2012Assignee: AstraZeneca ABInventors: Seth Björk, Peter Johnström, Nils Anders Nilsson, Katinka Ruda, Per Magnus Schou, Britt-Marie Swahn, Vern Delisser
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Publication number: 20120112179Abstract: A fluoranthene compound represented by the formula (1): wherein Z7 and Z12 are each aryl or heteroaryl; Ar0 is a single bond, aryl, or heteroaryl; R1 to R4 and R6 to R9 are each independently a hydrogen atom, alkyl, cycloalkyl, aryl, heteroaryl, or the like; and I is an integer of 1 to 4.Type: ApplicationFiled: October 26, 2010Publication date: May 10, 2012Applicant: IDEMITSU KOSAN CO., LTD.Inventors: Yumiko Mizuki, Masakazu Funahashi
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Publication number: 20120101091Abstract: The present application provides compounds of formula I wherein X, Y, R2, n, R5 and R6 are defined herein, useful as inhibitors of the hepatitis C virus NS5B polymerase The present application also provides pharmaceutical compositions containing said compounds, methods of using said compounds as pharmaceuticals alone or with other antiviral agent in the treatment of a hepatitis C viral infection in a mammal having or at risk of having the infection.Type: ApplicationFiled: October 1, 2009Publication date: April 26, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Pierre Beaulieu, Pierre Bonneau, René Coulombe, Pasquale Forgione, James Gillard, Araz Jakalian, Jean Rancourt
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Patent number: 8153794Abstract: The present invention relates to a new method of cross-coupling aryl moieties comprising reacting an arylhalide with an arylboronic acid in the presence of a palladium compound and a compound comprising a di-alkylphosphine moiety.Type: GrantFiled: October 3, 2008Date of Patent: April 10, 2012Assignee: E. I. du Pont de Nemours and CompanyInventor: Alex Sergey Ionkin
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Publication number: 20120083488Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).Type: ApplicationFiled: June 9, 2010Publication date: April 5, 2012Inventors: Kazutomo Kinoshita, Kohsuke Asoh, Noriyuki Furuichi, Toshiya Ito, Hatsuo Kawada, Nobuya Ishii, Hiroshi Sakamoto, WooSang Hong, MinJeong Park, Yoshiyuki Ono, Yashuharu Kato, Kenji Morikami, Takashi Emura, Nobuhiro Oikawa
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Publication number: 20120071487Abstract: Novel piperazine, piperidine and tetrahydropyridine derivatives comprising a dibenzofurane moiety are provided herein, as well as pharmaceutical compositions comprising same and therapeutic uses thereof.Type: ApplicationFiled: May 26, 2010Publication date: March 22, 2012Inventors: Vladimir Kogan, Lev Tabachnik
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Publication number: 20120064062Abstract: Organic compounds showing the ability to inhibit bacterial omptin proteases, specifically Yersinia pestis plasminogen activator (Pla) are disclosed. The disclosed Y. pestis plasminogen activator inhibitor compounds are useful for treating, preventing, or reducing the spread of infections by Y. pestis.Type: ApplicationFiled: September 13, 2011Publication date: March 15, 2012Inventors: Jon D. Goguen, Daniel Aiello, Donald T. Moir, Bing Li
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Publication number: 20120053132Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.Type: ApplicationFiled: November 1, 2011Publication date: March 1, 2012Applicant: Sequoia Pharmaceuticals, Inc.Inventors: Michael Eissenstat, Dehui Duan
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Publication number: 20120053173Abstract: Provision of a prophylactic or therapeutic agent for diabetes, which has superior efficacy. A compound represented by the formula: wherein each symbol is as described in the specification, or a salt thereof.Type: ApplicationFiled: March 4, 2009Publication date: March 1, 2012Inventors: Yoshihiro Banno, Ryoma Hara, Ryosuke Tokunoh
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Patent number: 8119624Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).Type: GrantFiled: October 27, 2010Date of Patent: February 21, 2012Assignee: Pfizer Inc.Inventors: Hao Bai, Simon Bailey, Dilip Ramakant Bhumralkar, Feng C. Bi, Fengli Guo, Mingying He, Paul Stuart Humphries, Anthony Lai Ling, Jihong Lou, Seiji Nukui, Ru Zhou
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Patent number: 8106073Abstract: The invention provides a compound of formula (I) as defined in the specification, a process for its preparation, pharmaceutical compositions containing it, a process for preparing the pharmaceutical composition, and its use in therapy.Type: GrantFiled: November 26, 2008Date of Patent: January 31, 2012Assignee: AstraZeneca ABInventors: Simon David Guile, Toby Thompson
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Publication number: 20120010247Abstract: The present invention provides a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: October 26, 2009Publication date: January 12, 2012Inventors: Makoto Kamata, Tohru Yamashita, Asato Kina, Michiko Amano
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Patent number: 8067602Abstract: Asymmetric cyanine fluorescent dyes are represented by general formula I. These kinds of dyes may be used as a staining agent for nucleic acids, with the spectra at 600-900 nm in the near-infrared region and without interference from background fluorescence. These kinds of dyes may be useful with small-type red semiconductor lasers as the light source (such as 633 nm). Compositions comprising these dyes and methods for staining biological samples using these dyes or compositions are also provided.Type: GrantFiled: December 12, 2008Date of Patent: November 29, 2011Assignee: Shenzhen Mindray Bio-Medical Electronics Co., Ltd.Inventor: Jianhui Shao
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Publication number: 20110272681Abstract: A light-emitting element has high luminous efficiency and excellent durability. The light-emitting element includes at least a light-emitting layer between a positive electrode and a negative electrode, and emits light by electrical energy. The light-emitting element is characterized by containing a naphthacene compound that has a specific structure and organic fluorescent substance that has a fluorescence peak wavelength of not less than 500 nm but not more than 690 nm.Type: ApplicationFiled: January 19, 2010Publication date: November 10, 2011Applicant: TORAY INDUSTRIES, INC.Inventors: Kazunori Sugimoto, Tsuyoshi Tominaga
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Publication number: 20110275625Abstract: Disclosed are compounds and compositions of the formula (I) as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula (I).Type: ApplicationFiled: November 5, 2009Publication date: November 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Neil Alexander Farrow, Donghong Amy Gao, Alexander Heim-Riether, Shuang Liang, Sabine Schlyer, Lana Louise Smith Keenan, Steven John Taylor, Bernd Wellenzohn, Dieter Wiedenmayer, Zhaoming Xiong, Qiang Zhang
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Patent number: 8039450Abstract: Compounds and methods of treating anti-inflammatory conditions are disclosed.Type: GrantFiled: March 5, 2009Date of Patent: October 18, 2011Assignee: Anacor Pharmaceuticals, Inc.Inventors: Tsutomu Akama, Yong-Kang Zhang, Charles Z. Ding, Jacob J. Plattner, Kirk R. Maples, Yvonne Freund, Virginia Sanders, Yi Xia, Stephen J. Baker, James A. Nieman, Xiaosong Lu, Marcelo Sales, Rashmi Sharma, Rajeshwar Singh, Robert Jacobs, Daitao Chen, Michael Richard Kevin Alley
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Publication number: 20110230350Abstract: Use of substituted sulfonamides of the formula (I) or salts thereof for enhancing stress tolerance in plants to abiotic stress, especially for enhancing plant growth and/or for increasing plant yield.Type: ApplicationFiled: March 17, 2011Publication date: September 22, 2011Applicant: BAYER CROPSCIENCE AGInventors: Jens Frackenpohl, Ines Heinemann, Thomas Müller, Pascal Von Koskull-Döring, Jan Dittgen, Dirk Schmutzler, Christopher Hugh Rosinger, Isolde Häuser-Hahn, Martin Jeffrey Hills
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Patent number: 8022088Abstract: Substituted bicyclic and tricyclic modified himbacine derivative of the formula: or a pharmaceutically acceptable salt or solvate of said compound wherein represents an optional double bond and wherein En, Fn, Gn, Zn, Jn, X, R3, R9, R10, R11, R32, R33, B and Het are herein defined are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other agents is also claimed.Type: GrantFiled: June 27, 2007Date of Patent: September 20, 2011Assignee: Schering CorporationInventors: Mariappan V. Chelliah, Samuel Chackalamannil, Yan Xia
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Publication number: 20110212940Abstract: The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.Type: ApplicationFiled: February 25, 2011Publication date: September 1, 2011Applicant: EPIX PHARMACEUTICALS, INC.Inventors: Roland Burli, Victor J. Cee, Jennifer Golden, Brian Alan Lanman, Susana Neira, Ashis Saha, Nili Schutz, Xiang Yu, Dilara McCauley, Mercedes Lobera, Yael Marantz, Jian Lin, Srinivasa R. Cheruku, Pini Orbach, Anurag Sharadendu, Robert C. Penland, Kimberley Gannon, Sharon Shacham, Silvia Noiman, Oren Becker, Zhaoda Zhang
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Patent number: 8008305Abstract: The invention relates to a compound of formula wherein R1, R2, X, L, W, n, and o are defined herein and to pharmaceutically suitable acid addition salts thereof, with the exception of the following compounds 6-(4-methyl-piperazin-1-yl)-N-phenethyl-nicotinamide (CAS 199478-31-4), N-(3,4-dichloro-benzyl)-3-fluoro-benzamide (CAS 424815-98-5), N-(4-chloro-benzyl)-3-fluoro-benzamide (CAS 544661-83-8), N-(3-chloro-benzyl)-3-fluoro-benzamide (CAS 796051-07-5), and N-phenethyl-6-phenylamino-nicotinamide (CAS 571913-74-1). The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of CNS disorders.Type: GrantFiled: July 28, 2008Date of Patent: August 30, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Publication number: 20110201815Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal plasma uric acid level and the like. The present invention relates to fused heterocyclic derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of plasma uric acid level, prodrugs thereof, salts thereof or the like. In the formula (I), T represents trifluoromethyl, nitro or cyano; ring Q represents heteroaryl; X1 and X2 independently represent CH or N; ring U represents aryl or heteroaryl; m represents integral number from 0 to 2; n represents integral number from 0 to 3; R1 represents a hydroxy group, amino or C1-6 alkyl; R2 represents C1-6 alkyl, C1-6 alkoxy C1-6 alkyl or the like.Type: ApplicationFiled: October 14, 2009Publication date: August 18, 2011Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Kazuo Shimizu, Masato Iizuka, Hideki Fujikura, Yasushi Takigawa, Masahiro Hiratochi
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Patent number: 7968724Abstract: The invention provides inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are new ester derivatives, methods of preparing such compounds, compositions containing them, and therapeutic uses thereof.Type: GrantFiled: December 15, 2008Date of Patent: June 28, 2011Assignee: Chiesi Farmaceutici S.p.A.Inventors: Elisabetta Armani, Gabriele Amari, Gino Villetti
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Publication number: 20110118248Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.Type: ApplicationFiled: January 13, 2009Publication date: May 19, 2011Inventors: Solomon Ungashe, Zheng Wei, Arindrajit Basak, Trevor T. Charvat, Wei Chen, Jeff Jin, Jimmie Moore, Yibin Zeng, Sreenivas Punna, Daniel Dairaghi, Derek Hansen, Andrew M. K. Pennell, John J. Wright, Antoni Krasinski, Qiang Wang
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Patent number: 7943634Abstract: The present invention relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the formula (1) and analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxides, pharmaceutically acceptable solvates thereof and the pharmaceutical compositions containing them which are useful in the treatment of allergic and inflammatory diseases including asthma, chronic bronchitis, atopic dermatitis, urticaria, allergic rhinitis, allergic conjunctivitis, vernal conjunctivitis, eosinophilic granuloma, psoriasis, rheumatoid arthritis, septic shock, ulcerative colitis, Crohn's disease, reperfusion injury of the myocardium and reperfusion injury of the brain, chronic glomerulonephritis, endotoxic shock and adult respiratory distress syndrome.Type: GrantFiled: December 15, 2005Date of Patent: May 17, 2011Assignee: Glenmark Pharmaceuticals S.A.Inventors: Laxmikant Atmaram Gharat, Balasubramanian Gopalan, Neelima Khairatkar Joshi
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Publication number: 20110112142Abstract: The invention provides a pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt: wherein R3 is selected from the group consisting of ORA; —CHO; —C(O)C1-4alkyl; —C(O)phenyl; —O—C(O)RA; and N(RB)2; R6 is selected from certain cyclic groups defined in the specification; and the remaining groups are defined in the specification; together with a pharmaceutically acceptable carrier. Most of the compounds are novel. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.Type: ApplicationFiled: April 8, 2009Publication date: May 12, 2011Inventors: Daniel Nöteberg, Elisabet Kallin, Mattias Wennerstål
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Publication number: 20110098237Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.Type: ApplicationFiled: February 23, 2009Publication date: April 28, 2011Applicant: Sequoia Pharmaceuticals, Inc.Inventors: Michael Eissenstat, Dehui Duan, Sergi Gulnik, John W. Erickson
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Publication number: 20110098236Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.Type: ApplicationFiled: February 23, 2009Publication date: April 28, 2011Applicant: Sequoia Pharmaceuticals, Inc.Inventors: Michael Eissenstat, Dehui Duan
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Publication number: 20110086877Abstract: Disclosed herein are methods of inhibiting the activity of Botulinum neurotoxin A metalloprotease with the compounds disclosed herein. Also disclosed are methods of treating, inhibiting or preventing intoxication caused by bacteria of at least one bacterial strain in a subject, and pharmaceutical and cosmetic compositions comprising the compounds disclosed herein.Type: ApplicationFiled: October 1, 2010Publication date: April 14, 2011Inventors: SINA BAVARI, RICK GUSSIO, JAMES C. BURNETT
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Publication number: 20110061723Abstract: The present invention pertains to an electrode layer comprising a porous film made of oxide semiconductor fine particles sensitized with certain methin dyes. Moreover the present invention pertains to a photoelectric conversion device comprising said electrode layer, a dye sensitized solar cell comprising said photoelectric conversion device and to novel methin dyes.Type: ApplicationFiled: February 26, 2009Publication date: March 17, 2011Applicant: BASF SEInventors: Kazuhiko Kunimoto, Hiroshi Yamamoto, Shinji Nakamichi, Ryuichi Takahashi, Junichi Tanabe
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Publication number: 20110065631Abstract: A process for the synthesis of bisfuran intermediates of formula (0) useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed. Furthermore disclosed is a HIV protease inhibitor of formula (IV) as well as various intermediates thereof.Type: ApplicationFiled: March 29, 2007Publication date: March 17, 2011Applicant: Gilead Sciences, IncInventors: Kenneth R. Crawford, Eric D. Dowdy, Arnold Gutierrez, Richard Polniaszek, Richard H. Yu
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Publication number: 20110046182Abstract: Aspirin is one of the most widely used drugs in the treatment of inflammation, pain and fever. It has more recently found application in the prevention of heart attacks and stroke and is being studied as a cancer chemopreventative agent. Despite its value aspirin continues to be underutilized because it causes gastric bleeding. The technology under development potentially removes this problem. It is designed to reduce contact between the drug and the intestinal lining. An isosorbide aspirinate prodrug compound is thus provided. The compound has the general structure as shown in general formula (I) wherein Y is a C1-C8 alkyl ester, a C1-C8 alkoxy ester, a C3-C10 cycloalkyl ester, an arylester, a C1-C8 alkylaryl ester or —C(O)ORring, wherein Rring is a 5-membered aromatic or nonaromatic 5-member ring having at least one heteroatom substituted for a carbon of the ring system, which can be unsubstituted or substituted with at least one nitric oxide releasing group.Type: ApplicationFiled: December 19, 2008Publication date: February 24, 2011Applicant: The Provost, Fellows and Scholars of the College of the Holy and Undivided Trinity of Queen ElizabeInventors: John Francis Gilmer, Louise Clune-Moriarty, Maeve Lally
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Publication number: 20110039821Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).Type: ApplicationFiled: October 27, 2010Publication date: February 17, 2011Inventors: Hao Bai, Simon Bailey, Dilip Ramakant Bhumralkar, Feng C. Bi, Fengli Guo, Mingying He, Paul Stuart Humphries, Anthony Lai Ling, Jihong Lou, Seiji Nukui, Ru Zhou
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Publication number: 20110021540Abstract: The invention provides compounds of formula wherein R1, R3, L1, L2, G1, G2, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.Type: ApplicationFiled: November 14, 2008Publication date: January 27, 2011Applicant: ASTRAZENECA ABInventors: Johan Bylund, Maria Ek, Jorg Holenz, Martin H. Johansson, Annika Kers, Katja Narhi, Gunnar Nordvall, Liselotte Ohberg, Daniel Sohn, Jenny Viklund, Stefan Von Berg
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Publication number: 20110015185Abstract: The present invention relates to compounds of formula (I): wherein P, R3, W1, and W2 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds for the preparation of a medicament against 5-HT6 receptor-related disorders.Type: ApplicationFiled: September 28, 2010Publication date: January 20, 2011Applicant: BIOVITRUM ABInventors: Gary Johansson, Peter Brandt, Björn M. Nilsson
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Publication number: 20100331370Abstract: Isobenzofuran analogs of sclerophytin A are prepared in a highly concise fashion via an aldol-cycloaldol sequence. The analogs exhibit IC50's as low as 1 ?M in growth inhibitory studies against KB3 cells using an MTT assay. Preferred analogs have one of the following structural formulas, where R is hydrogen or a substituted or unsubstituted lower alkyl group and Ar is a substituted or unsubstituted aryl group.Type: ApplicationFiled: June 30, 2010Publication date: December 30, 2010Inventor: Matthias C. McIntosh
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Publication number: 20100311582Abstract: A compound of the formula (I) where, for example, W, X and Y are each CH; R1 and R6, independently of each other, are for example, selected from the group consisting of H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkoxy, C3-C8-cycloalkyl, R7C(?O), and a ring system; provided that at least one of R1 and R6 is a —C2-C6-alkenylthio-C1-C6-alkyl, —C1-C6-alkoxy-C(?O)NRx-C1-C6-alkyl, —partially or fully unsaturated ring system containing in at least one ring in the ring system at least one hetero atom selected from N, O and S, which ring system is bound (i.e. through the N bonded to R1 and R6 in formula I) either directly or via a a C1-C6-alkylene group to the remainder of the compound, —partially or fully unsaturated ring system containing a ring that is bound to the remainder of the compound (i.e.Type: ApplicationFiled: January 23, 2009Publication date: December 9, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Thomas Pitterna, Peter Renold, Ottmar Franz Hueter, Peter Maienfisch, Werner Zambach
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Publication number: 20100292190Abstract: The present invention relates to compounds of general formula (I) as tublin polymerisation inhibitors and methods for preparing such compounds.Type: ApplicationFiled: February 14, 2006Publication date: November 18, 2010Applicant: Bionomics LimitedInventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn