Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/48)
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Publication number: 20120214794Abstract: This invention provides compounds of formula I-A or I-B: wherein HY, G1, G2, R2, R12, W1, W2, n, and Ring A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: October 13, 2011Publication date: August 23, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Brian S. Freeze, Masaaki Hirose, Hong Myung Lee, Todd B. Sells, Zhan Shi, Leo R. Takaoka, Stepan Vyskocil, Tianlin Xu
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Publication number: 20120214990Abstract: A nitrogen-containing heterocyclic compound or pharmaceutically acceptable salt thereof represented by the general formula: which have a potent antibacterial activity and a high safety. Thus, the compounds are useful as antibacterial agents against gram-positive bacteria, gram-negative bacteria and drug resistant bacteria.Type: ApplicationFiled: May 3, 2012Publication date: August 23, 2012Applicants: TAISHO PHARMACEUTICAL CO., LTD., TOYAMA CHEMICAL CO., LTD.Inventors: Taro KIYOTO, Tadashi Tanaka, Yasuhiro Tsutsui, Junichi Ando, Mai Motono, Yasuko Kawaguchi, Toshiya Noguchi, Yasunobu Ushiki, Fumihito Ushiyama, Hiroki Urabe
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Publication number: 20120190848Abstract: Provided are compounds and methods useful for the preparation of compounds useful as inhibitors of beta-site amyloid precursor protein (APP)-cleaving enzyme.Type: ApplicationFiled: January 20, 2012Publication date: July 26, 2012Inventors: Branko Mitasev, Dae-Shik Kim, Huiming Zhang, Matthew J. Schnaderbeck, Christopher N. Farthing, Kazuhiro Yoshizawa
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Publication number: 20120190672Abstract: The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; A is CH or N; Y is methyl, ethyl, monofluoromethyl, difluoromethyl, trifluoromethyl, difluoroethyl, methoxy, ethoxy, methoxymethyl or —C?N; and pharmaceutically acceptable salts thereof; which compound has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.Type: ApplicationFiled: January 20, 2012Publication date: July 26, 2012Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Adrian Hall, Christopher Neil Farthing, Jose Luis Castro Pineiro
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Publication number: 20120149573Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, X is CH or N; Y is C(O) or S(O)2; provided that when Y is S(O)2, then X is CH; A is a radical selected from the group consisting of and B1, B2, B3, T, R1, R2 R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: September 7, 2010Publication date: June 14, 2012Inventors: Kanu Maganbhai Patel, Thomas Paul Selby, Brenton Todd Smith, Andrew Edmund Taggi, Patrick Ryan Kovacs
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Patent number: 8198269Abstract: A compound represented by the general formula: wherein Ring A is a C6-14 aryl group or the like, L is —NRLCO— or the like (wherein RL is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a C1-3 alkylene group or the like, Z is an oxygen atom or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, or a pharmaceutically acceptable salt thereof, or a solvate thereof, has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.Type: GrantFiled: September 28, 2009Date of Patent: June 12, 2012Assignee: Eisai R&D Management Co., Ltd.Inventors: Takafumi Motoki, Kunitoshi Takeda, Yoichi Kita, Mamoru Takaishi, Yuichi Suzuki, Tasuku Ishida
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Patent number: 8183236Abstract: Pharmacophore models to be used in drug design and discovery are provided. An in silico protocol and in vitro assays are presented. Compounds and their pharmaceutically acceptable salts with HIV-1 integrase inhibitory and anti-HIV activity and use thereof in the treatment of HIV/AIDS and related infections either alone or in combination with all the known antiretroviral therapeutics are described.Type: GrantFiled: April 14, 2008Date of Patent: May 22, 2012Assignee: University of Southern CaliforniaInventors: Nouri Neamati, Raveendra S. Dayam
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Publication number: 20120095219Abstract: The present invention refers to the preparation and purification of brinzolamide as well as to novel compounds useful in such processes.Type: ApplicationFiled: March 12, 2010Publication date: April 19, 2012Applicant: Azad Pharmaceutical Ingredients AGInventors: Arul Ramakrishnan, Anil Kumar Soni, Sujit Das Adhikari, Kommula Srinivasa Rao, Soumendu Paul, Ganta Srinivasulu
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Publication number: 20120094984Abstract: A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.Type: ApplicationFiled: December 21, 2011Publication date: April 19, 2012Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Yuichi Suzuki, Takafumi Motoki, Toshihiko Kaneko, Mamoru Takaishi, Tasuku Ishida, Kunitoshi Takeda, Yoichi Kita, Noboru Yamamoto, Afzal Khan, Paschalis Dimopoulos
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Publication number: 20120094972Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphobType: ApplicationFiled: June 25, 2010Publication date: April 19, 2012Applicant: AMGEN INC.Inventors: Matthew Brown, Yi Chen, Timothy David Cushing, Felix Gonzalez Lopez De Turiso, Xiao He, Todd J. Kohn, Julia Winslow Lohman, Vatee Pattaropong, Jennifer Seganish, Youngsook Shin, Jillian L. Simard
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Patent number: 8158620Abstract: A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.Type: GrantFiled: January 16, 2009Date of Patent: April 17, 2012Assignee: Eisai R&D Management Co., Ltd.Inventors: Yuichi Suzuki, Takafumi Motoki, Toshihiko Kaneko, Mamoru Takaishi, Tasuku Ishida, Kunitoshi Takeda, Yoichi Kita, Noboru Yamamoto, Afzal Khan, Paschalis Dimopoulos
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Patent number: 8138176Abstract: Heterocyclic compounds of the formula (I) and salts, preferably pharmaceutically acceptable salts thereof, are provided in which R, R1, R2, Q, m and n have the meanings explained in detail in the description. Also provided are a process for their preparation and the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.Type: GrantFiled: December 22, 2010Date of Patent: March 20, 2012Assignee: Novartis AGInventors: Peter Herold, Robert Mah, Vincenzo Tschinke, Aleksandar Stojanovic, Christiane Marti, Stjepan Jelakovic, Stefan Stutz
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Publication number: 20120065065Abstract: Herbicidally active pyridylketosultams of the general formula (I) and their use as herbicides are described. In this formula (I), X1, X2, X3 and X4 each represent N or C—R1. R1, R2, R3 and R4 represent radicals such as hydrogen and organic radicals such as alkyl.Type: ApplicationFiled: August 31, 2011Publication date: March 15, 2012Applicant: BAYER CROPSCIENCE AGInventors: Christian WALDRAFF, Stefan LEHR, Elmar GATZWEILER, Isolde HÄUSER-HAHN, Ines HEINEMANN, Christopher Hugh ROSINGER
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Patent number: 8133849Abstract: The present invention relates to compounds of formula (I), wherein R1, R2, R3, R4 and R5 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to intermediates used in the preparation of compounds of formula (I), to methods of controlling plants and compositions comprising compounds of formula (I).Type: GrantFiled: November 10, 2008Date of Patent: March 13, 2012Assignee: Syngenta LimitedInventors: Nigel James Willetts, Matthew Robert Cordingley, Patrick Jelf Crowley, Suzanna Jane Riley, Michael Drysdale Turnbull
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Publication number: 20120058893Abstract: Ketosultams and diketopyridines of the formula (I) and use thereof as herbicides are described. In this formula (I), G, X, Y and Z are each radicals such as hydrogen and organic radicals such as alkyl. W represents organic radicals such as alkyl. A represents a heterocycle.Type: ApplicationFiled: August 31, 2011Publication date: March 8, 2012Applicant: BAYER CROPSCIENCE AGInventors: Stefan LEHR, Christian WALDRAFF, Elmar GATZWEILER, Isolde HÄUSER-HAHN, Ines HEINEMANN, Christopher Hugh ROSINGER
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Patent number: 8124602Abstract: The present invention relates to compounds of Formula V(A): that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans. In particular this invention relates to compounds of Formula V(A) useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans.Type: GrantFiled: December 9, 2010Date of Patent: February 28, 2012Assignee: AstraZeneca ABInventors: Gloria Breault, Charles Joseph Eyermann, Bolin Geng, Marshall Morningstar, Folkert Reck
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Publication number: 20120041194Abstract: The present invention provides nitrogen and sulfur-containing heterocycle compounds to be used as scaffolds and, in particular, nitrogen and sulfur-containing heterocycle compounds having a thiomorpholine core. The compounds herein described may be useful in treating diseases such as diabetes, obesity, cancer, cardiovascular, Alzheimer's, inflammatory, antidepressant, rheumatoid arthritis, multiple sclerosis, allergic rhinitis, asthma as well as viral and bacterial infections. The compounds herein described may also be useful in treating CNS disorders such as but not limited to Schizophrenia, Alzheimer's disease (AD).Type: ApplicationFiled: August 29, 2009Publication date: February 16, 2012Applicant: Triad Multitech Pharmaceuticals, Inc.Inventor: Murty N. Armilli
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Publication number: 20120028969Abstract: The present invention provides compounds of formula (I); or pharmaceutically acceptable salts thereof, wherein the variables are defined as herein. The present invention provides a method for manufacturing the compounds of formula (I), their therapeutic uses, combinations with other of pharmacologically active agents, and a pharmaceutical compositions.Type: ApplicationFiled: July 25, 2011Publication date: February 2, 2012Applicant: NOVARTIS AGInventors: David Weninger BARNES, Gregory Raymond BEBERNITZ, Kevin CLAIRMONT, Scott Louis COHEN, Robert Edson DAMON, Robert Francis DAY, Stephanie Kay DODD, Christoph GAUL, Hatice Belgin GULGEZE EFTHYMIOU, Monish JAIN, Rajeshri Ganesh KARKI, Louise Clare KIRMAN, Kai LIN, Justin Yik Ching MAO, Tajesh Jayprakash PATEL, Brian Kenneth RAYMER, Liansheng SU
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Patent number: 8093382Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a member selected from the group consisting of: wherein E is CH or N, Q is selected from the group consisting of CO, CS, SO, SO2, or C?NR4, and L, X, Z, R2 and R3 are as defined herein.Type: GrantFiled: December 9, 2010Date of Patent: January 10, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Jun Feng, Stephen L. Gwaltney, Michael B. Wallace, Jeffrey A. Stafford, Zhiyuan Zhang
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Patent number: 8076327Abstract: The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferable pharmaceutically acceptable salts, thereof, in which R, R1, R2, R3, Q, m and n have the meanings explained in detail in the description, a process for their preparation and the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.Type: GrantFiled: August 16, 2010Date of Patent: December 13, 2011Assignee: Novartis AGInventors: Peter Herold, Robert Mah, Vincenzo Tschinke, Aleksandar Stojanovic, Christiane Marti, Stefan Stutz, Bibia Bennacer
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Publication number: 20110301149Abstract: The present invention provides compounds which antagonize epsilon protein kinase C (PKC?). These compounds have a structural formula (Ia), (Ic) or (II). The present invention also provides pharmaceutical compositions containing these compounds and methods of treating various diseases, conditions, and/or symptoms by using these compounds.Type: ApplicationFiled: October 12, 2009Publication date: December 8, 2011Applicant: VM DISCOVERY INC.Inventor: Jay Jie-Qiang Wu
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Patent number: 8044044Abstract: The invention relates to compounds of formula (I) wherein R0 represents H or OH; R1 represents alkoxy; U and W represent N, V represents CH and R2 represents H or F, or U and V represent CH, W represents N and R2 represents H or F, or U and V represent N, W represents CH and R2 represents H, or U represents N, V represents CH, W represents CRa and R2 represents H; Ra represents CH2OH or alkoxycarbonyl; A represents the group CH?CH—B or a binuclear heterocyclic system D, B representing a mono- or di-substituted phenyl group wherein the substituents are halogen atoms and D representing one of the following groups wherein Z represents CH or N, and Q represents O or S; and to salts of such compounds. These compounds are useful as antibacterial agents.Type: GrantFiled: December 21, 2007Date of Patent: October 25, 2011Assignee: Actelion Pharmaceutical Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Publication number: 20110257165Abstract: 3,4-diaryl-bicyclicpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: ApplicationFiled: December 17, 2009Publication date: October 20, 2011Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Maurizio Pulici, Chiara Marchionni, Claudia Piutti, Fabio Gasparri
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Patent number: 8012961Abstract: The invention relates to antibacterial compounds of formula (I) wherein U represents CH or N; W represents CH or N; R1 represents alkoxy, halogen or CN; ring A represents a pyrrolidin-1,3-diyl-, a piperidin-1,3-diyl or a morpholin-2,4-diyl group and B represents CH2; or ring A is selected from the groups drawn below: wherein R2 represents H, F or hydroxymethyl, and B is absent; G represents a group selected from the group consisting of ?—CH?CH-E, wherein Y1, Y2, Y3 and Z independently represent CH or N; Q represents O or S; and E represents phenyl which is mono- or di-substituted wherein the substituents are each independently halogen; and to pharmaceutically acceptable salts of such compounds.Type: GrantFiled: April 14, 2009Date of Patent: September 6, 2011Assignee: Actelion Pharmaceutical Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, John-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Publication number: 20110207723Abstract: A compound represented by the general formula (I): a pharmaceutically acceptable salt thereof, or a solvate of the compound or salt has an A? production inhibitory activity or BACE 1 inhibitory activity, and is thus useful as an agent for treating neurodegenerative diseases caused by A? as typified by Alzheimer's disease. In the formula, ring A represents a C6-14 aryl group or the like; L represents —NR1CO— (wherein RL represents a hydrogen atom or the like) or the like; ring B represents a C6-14 aryl group or the like; X represents a C1-3 alkylene group or the like; Y represents a C1-3 alkylene group or the like; Z represents an oxygen atom or the like; R1 and R2 each independently represents a hydrogen atom or the like; and R3, R4, R5 and R6 each independently represents a hydrogen atom, a halogen atom or the like.Type: ApplicationFiled: September 28, 2009Publication date: August 25, 2011Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Takafumi Motoki, Kunitoshi Takeda, Yoichi Kita, Mamoru Takaishi, Yuichi Suzuki, Tasuku Ishida
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Patent number: 7981886Abstract: The invention relates to antibiotic derivatives of formula I wherein: A represents —O—, S, —C(?O)—, —C(?NOR6)—; Z—B represents NCH2CH2, NCOCH2, NCH2CO, NCH2CH(OH), CHN(R8)CH2 or CHN(R8)CO; D represents binuclear heteroaryl; Y1 represents —CR1— or —N—, Y2 represents —CR2— or —N—, Y3 represents —CR3— or —N— and Y4 represents —CR4— or —N—; U represents —NH—, —O— or —S— and V represents —N— or —CH—; W represents —CH2—, —O— or —NR7—; R1 represents H, methyl, ethyl or halogen; R2, R3 and R4 each represent independently H, C1-C4 alkyl, halogen, or C1-C4 alkoxy; R5 represents H, C1-C4 alkyl or fluorine; R6 represents H, C1-C4 alkyl or aryl-C1-C4 alkyl; R7 represents H, C1-C4 alkyl, aryl-C1-C4 alkyl or —CH2—COOH; R8 represents H, C1-C4 alkyl or —CH2—COOH; with the provisos that if Z—B represents NCH2CH2, NCOCH2, NCH2CO or NCH2CH(OH), then W represents —CH2—; if A represents O or S, then W represents —CH2—; and only one or two of Y1, Y2, Y3 and Y4 can represent N at the same time.Type: GrantFiled: May 24, 2006Date of Patent: July 19, 2011Assignee: Actelion Pharmaceutical Ltd.Inventors: Daniel Bur, Christian Hubschwerlen, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Publication number: 20110150873Abstract: The invention relates to the use of Broad-Spectrum Chemokine Inhibitors (BSCIs), and in particular members of the acylaminolactam class of pharmaceutical agents, for the prevention, prophylaxis, treatment or amelioration of symptoms of inflammatory diseases. In particular, improved compositions consisting of BSCI agents combined with one or more additional active pharmaceutical agents in order to achieve improved anti-inflammatory efficacy with a reduced side-effect profile are described and claimed.Type: ApplicationFiled: December 10, 2008Publication date: June 23, 2011Applicant: CAMBRIDGE ENTERPRISE LIMITEDInventor: David John Grainger
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Publication number: 20110118462Abstract: The invention relates to N-heterocyclic substituent-containing antibiotics, their preparation, and their use. Disclosed are sodium and potassium salts of 7-(?-((N,N?-diisopropylamidino)thio)acetylamino)-3-(((1,2,5,6-tetrahydro-2-methyl-5,6-dioxo-1,2,4-triazin-3-yl)thio)methyl) cephalosporanic acid as presented by the general structure (I), their preparation, and their use. The antibiotics of the invention can be used to treat diseases caused by Gram-positive or Gram-negative bacteria such as septicaemia, gastrointestinal tract infection, and urinary tract infection. They have increased half-life in blood and lowered toxicity. They can reduce the frequency of drug use and lower medical treatment costs. They have improved stability and can be stored at ambient temperatures. The method of the invention is simple, and it produces high purity products which can meet the requirements of clinical use.Type: ApplicationFiled: November 18, 2009Publication date: May 19, 2011Applicants: GUANGZHOU BAIYUNSHAN PHARMACEUTICAL CO., LTD. GUANGZHOU BAIYUNSHAN PHARMACEUTICAL FACTORY, GUANGZHOU PHARMACEUTICAL INDUSTRIAL RESEARCH INSTIInventors: Mao CHEN, Shaoxuan Zhu, Xuebin Liu, Lizhen Zheng, Liwei Lin, Shuwen Xu, Yuping Wang, Wei Yang, Yunfeng Li, Fang Ye, Xiaona Zhang
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Publication number: 20110118461Abstract: The present invention relates to a process for the preparation of Brinzolamide, or 2H-thieno[3,2-e]-1, 2-thiazin-6-sulfonamide, 4-(ethyl amino)-3, 4-dihydro-2-(3-methoxypropyl)-, 1,1-dioxide,(4R)- via intermediates 2,3-dihydro-4H-thieno[3,2-e]-1, 2-thiazin-4-ones, 1,1-dioxide. Further objects of the present invention are the intermediates mentioned above and other intermediates of the synthesis.Type: ApplicationFiled: June 15, 2009Publication date: May 19, 2011Inventors: Alessandro Falchi, Ottorino De Lucchi, Andrea Castellin
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Publication number: 20110092492Abstract: Heterocyclic compounds of the formula (I) and salts, preferably pharmaceutically acceptable salts thereof, are provided in which R, R1, R2, Q, m and n have the meanings explained in detail in the description. Also provided are a process for their preparation and the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.Type: ApplicationFiled: December 22, 2010Publication date: April 21, 2011Inventors: Peter HEROLD, Robert Mah, Vincenzo Tschinke, Aleksandar Stojanovic, Christiane Marti, Stjepan Jelakovic, Stefan Stutz
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Publication number: 20110087022Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a member selected from the group consisting of: wherein E is CH or N, Q is selected from the group consisting of CO, CS, SO, SO2, or C?NR4, and L, X, Z, R2 and R3 are as defined herein.Type: ApplicationFiled: December 9, 2010Publication date: April 14, 2011Inventors: Jun Feng, Stephen L. Gwaltney, II, Jeffrey A. Stafford, Michael B. Wallace, Zhiyuan Zhang
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Publication number: 20110082132Abstract: The invention relates to antibacterial compounds of formula I wherein R1 represents alkoxy or halogen; U, V and W each represent CH, or one of U, V and W represents N and the others each represent CH; A represents CH2 or O; G is CH?CH—E wherein E represents a phenyl group mono- or di-substituted with halogen, or G is a group of one of the formulae hereafter wherein Z represent CH or N, Q represents O or S and K represents O or S; and salts of such compounds.Type: ApplicationFiled: June 2, 2009Publication date: April 7, 2011Applicant: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Publication number: 20110071143Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein X, Y, R1, R2, and R3 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.Type: ApplicationFiled: September 15, 2010Publication date: March 24, 2011Inventors: Christine E. Brotherton-Pleiss, Ralph New Harris, III, Bradley E. Loe, Francisco Javier Lopez-Tapia, Pankaj D. Rege, David Bruce Repke, Russell Stephen Stabler, Keith Adrian Murray Walker
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Publication number: 20110065684Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, L1, L2, X, Y, Q and Z have defined meanings.Type: ApplicationFiled: August 13, 2010Publication date: March 17, 2011Inventors: Laurence Anne Mevellec, Ludo E.J. Kennis, Josephus Carolus Mertens, Jacobus A.J. Van Dun, Maria V.F. Somers, Walter B.L. Wouters
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Publication number: 20110053915Abstract: The invention relates to novel heterocyclic compounds and to the use thereof, to pharmaceutical compositions containing said chemical compounds as an active ingredient and to the use thereof for producing medicinal preparations for the human being and warm-blood animals for treating diseases caused by the aberrant activity of an Hedgehog (Hh)-signal system, in particular oncological diseases. The invention also relates to the use of the above-mentioned compounds in the form of ‘molecular pharmacological tools’ for examining (in vitro and in vivo) the biochemical features of the Hh-signal system, in particular, the interaction of Hh protein and transmembrane proteins, namely, suppressor Patched (Ptc) and protooncogenic proteins.Type: ApplicationFiled: December 12, 2008Publication date: March 3, 2011Applicant: ALLA CHEM, LLCInventors: Andrey Alexandrovich Ivaschenko, Yan Vadimovich Lavrovsky, Sergey Viktorovich Malyarchuk, Ilya Matusovich Okun, Nikolay Filippovich Savchuk, Sergey Yevgenievich Tkachenko, Alexander Viktorovich Khvat, Alexander Vasilievich Ivaschenko
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Patent number: 7897592Abstract: The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: GrantFiled: November 14, 2006Date of Patent: March 1, 2011Assignee: Bristol-Myers Squibb CompanyInventor: B. Narasimhulu Naidu
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Publication number: 20110039836Abstract: The invention relates to antibacterial compounds of formula (I) wherein U represents CH or N; W represents CH or N; R1 represents alkoxy, halogen or CN; ring A represents a pyrrolidin-1,3-diyl-, a piperidin-1,3-diyl or a morpholin-2,4-diyl group and B represents CH2; or ring A is selected from the groups drawn below: wherein R2 represents H, F or hydroxymethyl, and B is absent; G represents a group selected from the group consisting of —CH?CH-E, wherein Y1, Y2, Y3 and Z independently represent CH or N; Q represents O or S; and E represents phenyl which is mono- or di-substituted wherein the substituents are each independently halogen; and to pharmaceutically acceptable salts of such compounds.Type: ApplicationFiled: April 14, 2009Publication date: February 17, 2011Applicant: ACTELION PHARMACEUTICALS LTD.Inventors: Christian Hubschwerlen, Georg Rueedi, John-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Publication number: 20110009395Abstract: The present invention provides BACE inhibitors of Formula I: methods for their use, intermediates, and methods for their preparation.Type: ApplicationFiled: July 6, 2010Publication date: January 13, 2011Applicant: ELI LILLY AND COMPANYInventors: James Edmund AUDIA, Dustin James MERGOTT, Grant Mathews VAUGHT, Brian Morgan WATSON, Leonard Larry WINNEROSKI, JR., Chongsheng Eric SHI
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Publication number: 20110009394Abstract: Tricyclic nitrogen containing compounds and their use as antibacterials.Type: ApplicationFiled: January 7, 2009Publication date: January 13, 2011Applicant: Glaxo Group LimitedInventors: Pamela Brown, Steven Dabbs, Alan Joseph Hennessy
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Publication number: 20100331283Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.Type: ApplicationFiled: June 23, 2010Publication date: December 30, 2010Applicant: Array BioPharma Inc.Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Shelley Allen, Ellen Laird, Joseph P. Lyssikatos, John E. Robisnson, Christopher P. Corrette, Robert Kirk DeLisle, Walter C. Voegtti
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Publication number: 20100324030Abstract: The present invention describes novel anti-bacterial compounds of the formula (I). These compounds are, amongst others, of interest as inhibitors of DNA gyrase and topoisomerases, for example of topoisomerase II and IV.Type: ApplicationFiled: April 11, 2008Publication date: December 23, 2010Applicant: Morphochem Aktiengesellschaft Fur Kombinatorische ChemieInventors: Glenn Dale, Sabine Pierau, Michael W. Cappi, Christopher Gray, Christian Hubschwerlen, Jean P. Surivet, Cornelia Zumbrunn
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Publication number: 20100323889Abstract: The present invention relates to compounds of formula (I), wherein R1, R2, R3, R4 and R5 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to intermediates used in the preparation of compounds of formula (I), to methods of controlling plants and compositions comprising compounds of formula (I).Type: ApplicationFiled: November 10, 2008Publication date: December 23, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Nigel James Willetts, Matthew Robert Cordingley, Patrick Jelf Crowley, Suzanna Jane Riley, Michael Drysdale Turnbull
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Publication number: 20100317850Abstract: Disclosed is a compound represented by General formula (I), a pharmaceutically acceptable salt thereof, or a solvate of the compound or the pharmaceutically acceptable salt, which has an inhibitory activity of the production of A? or a BACE1-inhibiting activity, and is therefore useful as a prophylactic or therapeutic agent for A?-induced neurodegenerative diseases typified by Alzheimer-type dementia. Wherein the ring A represents a C6-14 aryl group or the like; L represents —NReCO— [wherein Re represents a hydrogen atom or the like] or the like; the ring B represents a C6-14 aryl group or the like; X represents a C1-3 alkylene group or the like; Y represents a single bond or the like; Z represents a C1-3 alkylene group or the like; R1 and R2 independently represent a hydrogen atom or the like; and R3, R4, R5 and R6 independently represent a hydrogen atom, a halogen atom or the like.Type: ApplicationFiled: January 16, 2009Publication date: December 16, 2010Inventors: Yuichi Suzuki, Takafumi Motoki, Toshihiko Kaneko, Mamoru Takaishi, Tasuku Ishida, Kunitoshi Takeda, Yoichi Kita, Noboru Yamamoto, Afzal Khan, Paschalis Dimopoulos
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Publication number: 20100317655Abstract: The present invention relates to new sulfonamide inhibitors of carbonic anhydrase activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: June 4, 2010Publication date: December 16, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Tadimeti Rao, Chengzhi Zhang
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Publication number: 20100305110Abstract: The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferable pharmaceutically acceptable salts, thereof, in which R, R1, R2, R3, Q, m and n have the meanings explained in detail in the description, a process for their preparation and the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.Type: ApplicationFiled: August 16, 2010Publication date: December 2, 2010Inventors: Peter HEROLD, Robert Mah, Vincenzo Tschinke, Aleksandar Stojanovic, Christiane Marti, Stefan Stutz, Bibia Bennacer
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Publication number: 20100298141Abstract: Disclosed are compounds of Formula 1, including N-oxides, and salts thereof, wherein W is O or NR7, n is 0 or 1, and R1, R2, R3, R4, R5, R6, R7 and m are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention. Also disclosed are mixtures and compositions comprising a herbicidally effective amount of a compound of Formula 1 and an effective amount of another herbicide or herbicide safener.Type: ApplicationFiled: February 8, 2008Publication date: November 25, 2010Applicant: E. I. DU PONT DE NEMOURS AND COMPANYInventors: Thomas Paul Selby, Brenton Todd Smith, Thomas Martin Stevenson
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Publication number: 20100292225Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: May 14, 2010Publication date: November 18, 2010Inventors: Sylvie Chamoin, Qi-Ying Hu, Julien Papillon
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Patent number: 7834008Abstract: The present invention relates to cyclopropyl derivatives of formula (I) and salt thereof. These compounds are NK3 receptor antagonists and may therefore be useful for treatment of diseases where the NK3 receptor is implicated, e.g. psychotic disorders.Type: GrantFiled: August 13, 2004Date of Patent: November 16, 2010Assignee: H. Lundbeck A/SInventors: Jan Kehler, Tore Hansen, Anders Poulsen, Berith Bjørnholm, Thomas Ruhland, Morten Bang Nørgaard, Søren Møller Nielsen
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Publication number: 20100279311Abstract: The invention provides a screening method and screening kit for a cell protecting agent. Specifically, the invention provides a method for screening a cell protecting agent showing an Hsp90-binding activity and a heat shock protein expression-inducing activity but having no Hsp90 client protein degradation-promoting activity. The method comprises the following steps (1) to (3): (1) measuring the binding property of a test compound to Hsp90; (2) measuring the activity of a test compound to induce the expression of a heat shock protein, or measuring the activity of a test compound to disrupt an Hsp90/HSF-1 complex, by using a cell capable of expressing the heat shock protein; and (3) measuring the activity of a test compound to induce the degradation of an Hsp90 client protein by using a cell capable of expressing the Hsp90 client protein.Type: ApplicationFiled: December 26, 2008Publication date: November 4, 2010Inventor: Haruhide Kimura
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Preparation of antimicrobial formulations using 7-oxa-2-thia-1,5-diazabicyclo[3.3.1]nonane-2,2-dione
Patent number: 7820651Abstract: Use of 7-oxa-2-thia-1,5-diazabicyclo[3.3.1]nonane-2,2-dione (“cyclotaurolidin”) for the preparation of antimicrobial formulations, in particular antimicrobial solutions for technical or medical purposes and of aqueous lock solutions for catheters and port systems for preventing infections and sepsis of patients.Type: GrantFiled: February 8, 2007Date of Patent: October 26, 2010Inventors: Claus Herdeis, Christian Edwin Weis