Tricyclo Ring System Having The 1,2-diazine Ring As One Of The Cyclos Patents (Class 544/234)
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Publication number: 20100113423Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.Type: ApplicationFiled: October 19, 2009Publication date: May 6, 2010Inventors: Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
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Patent number: 7709482Abstract: Polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: GrantFiled: December 29, 2007Date of Patent: May 4, 2010Assignee: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak
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Patent number: 7687501Abstract: In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J3, X, Z, and R1, R3, and R4 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.Type: GrantFiled: August 16, 2006Date of Patent: March 30, 2010Assignee: Schering CorporationInventors: Chad E. Bennett, William J. Greenlee, Chad E. Knutson, Duane A. Burnett
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Patent number: 7683062Abstract: Disclosed are a novel crystalline form of 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide, processes of preparing said crystalline form of 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide, compositions comprising said form in admixture with one or more pharmaceutically acceptable excipients, and uses for the same.Type: GrantFiled: February 14, 2008Date of Patent: March 23, 2010Assignee: sanofi-aventis U.S. LLCInventors: William Rocco, John D. Higgins
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Patent number: 7671050Abstract: The compounds of formula (I) in which R1, R2 and R3 have the meanings as given in the description are novel effective PDE2 inhibitors.Type: GrantFiled: January 4, 2006Date of Patent: March 2, 2010Assignee: NYCOMED GmbHInventors: Beate Schmidt, Steffen Weinbrenner, Dieter Flockerzi, Raimund Külzer, Hermann Tenor, Hans-Peter Kley
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Publication number: 20100047367Abstract: The present invention relates to novel compounds capable of modulating the stability and/or activity of hypoxia inducible factor (HIF) by inhibiting the activity of at least one HIF hydroxylase enzyme.Type: ApplicationFiled: August 20, 2009Publication date: February 25, 2010Inventors: Shaojiang Deng, Wen-Bin Ho, Lee A. Flippin
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Publication number: 20100035883Abstract: A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.Type: ApplicationFiled: July 27, 2009Publication date: February 11, 2010Applicant: LEAD THERAPEUTICS, INC.Inventors: Bing Wang, Daniel Chu
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Patent number: 7652006Abstract: The invention relates to novel quinazolines and heterocycles which are antagonists or positive modulators of AMPA receptors, and the use thereof for treating, preventing or ameliorating neuronal loss associated with stroke, global and focal ischemia, CNS trauma, hypoglycemia and surgery, as well as treating or ameliorating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease and Down's syndrome, treating, preventing or ameliorating the adverse consequences of the overstimulation of the excitatory amino acids, treating, preventing or ameliorating anxiety, psychosis, convulsions, chronic pain, glaucoma, retinitis, urinary incontinence, muscular spasm and inducing anesthesia, as well as for treating or ameliorating the adverse consequences of excitatory amino acid deficiency such as schizophrenia, myoclonus, Alzheimer's disease and malnutrition and neural maldevelopment, and as cognition and learning enhancers.Type: GrantFiled: February 6, 2004Date of Patent: January 26, 2010Assignee: Euro-Celtique S.A.Inventors: Ravi Upasani, Sui X Cai, Nancy C Lan, Yan Wang, George Field, David B Fick
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Publication number: 20090312334Abstract: Compounds of formula (I) are inhibitors of CD80 and useful in immunomodulation therapy: wherein R1 and R3 independently represent H; F; Cl; Br; —NO2; —CN; C1-C6 alkyl optionally substituted by F or Cl; or C1-C6 alkoxy optionally substituted by F; R4 represents a carboxylic acid group (—COOH) or an ester thereof, or —C(?O)NR6R7, —NR7C(?O)R6, —NR7C(?O)OR6, —NHC(?O)NR7R6 or —NHC(?S)NR7R6 wherein R6 represents H, or a radical of formula -(Alk)m-Q wherein m is 0 or 1, Alk is an optionally substituted divalent straight or branched C1-C12 alkylene, or C2-C12 alkenylene, or C2-C12 alkynylene radical or a divalent C3-C12 carbocyclic radical, any of which radicals may contain one or more —O—, —S— or —N(R8)— links wherein R8 represents H or C1-C4 alkyl, C3-C4 alkenyl, C3-C4 alkynyl, or C3-C6 cycloalkyl, and Q represents H; —NR9R10 wherein R9 and R10 independently represents H; C1-C4 alkyl; C3-C4 alkenyl; C3-C4 alkynyl; C3-C6 cycloalkyl; an ester group; an optionally substituted carbocyclic or heterocyclic group; orType: ApplicationFiled: August 24, 2009Publication date: December 17, 2009Applicant: Medigene LimitedInventor: Ian Richard Matthews
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Publication number: 20090306082Abstract: The present invention relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the formula (1) and analogs, tautomers, enantiomers, a 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: ApplicationFiled: December 15, 2005Publication date: December 10, 2009Applicant: GLENMARK PHARMACEUTICALS S.A.Inventors: Laxmikant Atmaram Gharat, Balasubramanian Gopalan, Neelima Khairatkar Joshi
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Publication number: 20090298837Abstract: The present invention provides compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.Type: ApplicationFiled: August 13, 2009Publication date: December 3, 2009Applicant: Eisai Corporation of North AmericaInventors: Vincent J. Kalish, Jie Zhang, Weizheng Xu, Jia-He Li, Amy Dongxia Xing, Qun Liu
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Publication number: 20090247559Abstract: A compound according to formula I: or a pharmaceutically acceptable salt thereof; wherein R1, R2, R3a, R3b, R3c and R3d are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: December 22, 2008Publication date: October 1, 2009Applicant: Exelixis, Inc.Inventors: S. David Brown, Hongwang Du, Maurizio Franzini, Adam Antoni Galan, Ping Huang, Patrick Kearney, Moon Hwan Kim, Elena S. Koltun, Steven James Richards, Amy L. Tsuhako, Cristiana A. Zaharia
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Publication number: 20090233936Abstract: The present invention is directed to novel substituted fused aminopiperidines of structural formula (I) which are inhibitors of the dipeptidyl peptidase-4 enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-4 enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-4 enzyme is involved.Type: ApplicationFiled: December 8, 2006Publication date: September 17, 2009Applicant: MERCK & CO., INC.Inventors: Jason M. Cox, Scott D. Edmondson, Anthony Mastracchio
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Publication number: 20090221590Abstract: The choline salt of the CD80 antagonist compound 4-(6-fluoro-3-oxo-1,3-dihydro-pyrazolo[4,3-c]cinnolin-2-yl)-N-(2,2-difluoro-ethyl)-benzamide (I) has good aqueous solubility and is therefore convenient for pharmaceutical use.Type: ApplicationFiled: February 19, 2007Publication date: September 3, 2009Applicant: MEDIGENE LIMITEDInventor: Ian Richard Matthews
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Publication number: 20090221529Abstract: This invention relates to the design, synthesis and use of synthetic vitamin D and other steroidal analogs. It further relates to the therapeutic use of such analogs and their manufacture.Type: ApplicationFiled: December 12, 2006Publication date: September 3, 2009Applicant: Women's & Infants Hospital of Rhode IslandInventors: Laurent Brard, Satyan Kalkunde, Rakesh Kumar Singh
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Publication number: 20090215736Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.Type: ApplicationFiled: September 23, 2008Publication date: August 27, 2009Applicant: Vertex Pharmaceuticals, IncorporatedInventors: Michael Mortimore, Andrew Miller, John Studley, Jean-Damien Charrier
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Publication number: 20090198051Abstract: An intermediate compound for total synthesis of ecteinascidins comprising, a compound represented by general formula 2 having thioether group at C4 site, and the substituent R2 of N12 site is trichloroethoxicarbonyl (Troc) to which various substituents can be introduced by mild condition, further having 10 members ring structure which can be converted to a ring of other numbered members.Type: ApplicationFiled: April 25, 2007Publication date: August 6, 2009Inventors: Tohru FUKUYAMA, Toshiyuki KAN
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Patent number: 7569567Abstract: A subject-matter of the invention is the compounds of general formula (I) in which X represents a hydrogen or halogen atom; R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 and R3 each represent, independently of one another, a hydrogen atom or a (C1-C4)alkyl group or else R2 and R3 form, with the nitrogen atom which carries them, a pyrrolidinyl, piperidinyl, morpholinyl or 4-alkylpiperazinyl group; and Het represents a heteroaromatic group of pyridinyl, 1-oxidopyridinyl, quinolinyl, isoquinolinyl, pyrimidinyl, pyrazinyl or pyridazinyl type, it being possible for the heteroaromatic group to carry one or more halogen atoms and/or one or more (C1-C4) alkyl or (C1-C4) alkoxy groups; in the form of bases, of addition salts with acids, of solvates or of hydrates, the pharmaceutical compositions comprising them, processes for their preparation and synthetic intermediates.Type: GrantFiled: June 17, 2008Date of Patent: August 4, 2009Assignee: sanofi-aventisInventors: Philippe Burnier, Jacques Froissant, Benoit Marabout, Frank Marguet, Frederic Puech
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Patent number: 7566713Abstract: Compounds of formula (I) are CD80 inhibitors, and of value for immunomodulation, e.g. in rheumatoid arthritis, multiple sclerosis, diabetes, asthma, transplantation, systemic lupus erythematosis and psoriasis: wherein Y is —CH2—, —CH2CH2—, or CH2CH2CH2—; R1 represents H; F; methyl, trifuoromethyl, methoxy or triflioromethoxy; R3 represents H; F; CI; Br; NO2; CN; C1C6 alkyl optionally substituted by F or Cl; or C1-C6 alkoxy optionally substituted by F; R4 represents a carboxylic acid group (—COOH) or an ester thereof, or —C(?O) NR6R7—NR7C(?O)R6, NR7C(?O)OR6, NHC(?O) or NHC(?S)NR7R6 wherein R6 and R7 are as defined in the specification and X represents a bond or a divalent radical as defined in the specification.Type: GrantFiled: April 26, 2005Date of Patent: July 28, 2009Assignee: Medigene LimitedInventor: Ian Richard Mathews
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Patent number: 7547697Abstract: Compounds of formula (I): as well as pharmaceutically acceptable salts and esters thereof for use as pharmaceutical compositions.Type: GrantFiled: July 2, 2007Date of Patent: June 16, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Kurt Amrein, Daniel Hunziker, Bernd Kuhn, Werner Neidhart, Alexander V. Mayweg
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Patent number: 7538112Abstract: Hydroxy-substituted pyrazinopyrrolopyridazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I) wherein R1, R2, R3, R4, R5, R6 and R7 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: May 3, 2005Date of Patent: May 26, 2009Assignee: Merck & Co., Inc.Inventors: John S. Wai, Joseph P. Vacca, Linghang Zhuang, Boyoung Kim, Terry A. Lyle, Catherine M. Wiscount, Melissa S. Egbertson, Lou Anne Neilson, Mark Embrey, Thorsten E. Fisher, Donnette D. Staas
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Publication number: 20090111816Abstract: Polycyclic aryl and polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl catalytic activity are also disclosed.Type: ApplicationFiled: December 29, 2007Publication date: April 30, 2009Applicant: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Dane Goff, Jiaxin Yu, Sacha Holland, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak, Jing Zhang
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Publication number: 20090098084Abstract: The present invention relates to tetraaza phenalen-3-one compounds which inhibit poly (ADP-ribose) polymerase (PARP) and are useful in the chemosensitization of cancer therapeutics. The induction of peripheral neuropathy is a common side-effect of many of the conventional and newer chemotherapies. The present invention further provides means to reliably prevent or cure chemotherapy-induced neuropathy. The invention also relates to the use of the disclosed PARP inhibitor compounds in enhancing the efficacy of chemotherapeutic agents such as temozolomide. The invention also relates to the use of the disclosed PARP inhibitor compounds to radiosensitize tumor cells to ionizing radiation. The invention also relates to the use of the disclosed PARP inhibitor compounds for treatment of cancers with DNA repair defects.Type: ApplicationFiled: October 2, 2008Publication date: April 16, 2009Applicant: MGI GP, Inc.Inventors: Weizheng Xu, Greg Delahanty, Ling Wei, Jie Zhang
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Patent number: 7511041Abstract: The present invention relates to hovel fused azolepyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-? inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-? activity. More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoixnmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis.Type: GrantFiled: September 18, 2003Date of Patent: March 31, 2009Assignee: Bayer Pharmaceuticals CorporationInventors: Mitsuyuki Shimada, Toshiki Murata, Kinji Fuchikami, Hideki Tsujishita, Naoki Omori, Issei Kato, Mami Miura, Klaus Urbahns, Florian Gantner, Kevin Bacon
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Patent number: 7501418Abstract: The invention concerns fused heterocyclic isoxazoline derivatives of Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof, more in particular, tetrahydropyranoisoxazole, hexahydroisoxazolopyridine, tetrahydrothiopyrano isoxazole and hexahydrobenzoisoxazole derivatives fused to a heterocyclic ring system via the 6-membered ring of the bicyclic moiety as well as processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for treating depression, anxiety, movement disorders, psychosis, Parkinson's disease and body weight disorders including anorexia nervosa and bulimia, wherein the variables are defined as in Claim 1.Type: GrantFiled: August 13, 2003Date of Patent: March 10, 2009Assignee: Janssen Pharmaceutica, N.V.Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, José Manuel Bartolomé -Nebreda, Francisco Javier Fernández-Gadea, Margaretha Henrica Maria Bakker, Antonius Adrianus Hendrikus Megens
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Publication number: 20090062289Abstract: N-(1-Aza-bicyclo[2.2.2]oct-3-yl)-4-(6,9-difluoro-3-oxo-1,3-dihydro-pyrazolo[4,3-c]cinnolin-2-yl)-benzamide is a CD80 antagonist, useful in the treatment of dieases which benefit from immuno-inhibition.Type: ApplicationFiled: August 9, 2004Publication date: March 5, 2009Applicant: AVIDEX LIMITEDInventor: Ian Richard Matthews
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Publication number: 20090029985Abstract: The invention relates to novel chemical compounds, compositions and methods of making and using the same. In particular, the invention provides pyridazine compounds and/or related heterocyclic derivatives, compositions comprising the same, and methods of using pyridazine compounds and/or related heterocyclic derivatives and compositions comprising the same, for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for research, drug screening, and therapeutic applications.Type: ApplicationFiled: May 12, 2008Publication date: January 29, 2009Inventors: Martin Watterson, Linda Van El Dik, Jacques Haiech, Marcel Hibert, Jean-Jacques Bourguignon, Anastasia Valeniza, Wenhui Hu, Magdena Zasadzki
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Publication number: 20090023739Abstract: This invention provides novel caspase inhibitors of formula I: wherein R1 is hydrogen, CHN2, R, or —CH2Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group, or a heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; X2—X1 is N(R3)—C(R3), C(R3)2—C(R3), C(R3)2—N, N?C, C(R3)?C, C(?O)—N, or C(?O)—C(R3); each R3 is independently selected from hydrogen or C1-6 aliphatic; Ring C is a fused aryl ring; n is 0, 1 or 2; and each methylene carbon in Ring A is optionally and independently substituted by ?O, or one or more halogen, C1-4 alkyl, or C1-4 alkoxy. The compounds are useful for treating caspase-mediated diseases.Type: ApplicationFiled: July 1, 2008Publication date: January 22, 2009Applicant: Vertex Pharmaceuticals, IncorporatedInventors: Jean-Damien Charrier, Guy Brenchley
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Publication number: 20090005372Abstract: The compounds of formula I in which R1 and R2 have the meanings as given in the description are novel effective PDE2 inhibitors.Type: ApplicationFiled: August 31, 2005Publication date: January 1, 2009Applicant: Altana Pharma AGInventors: Beate Schmidt, Steffen Weinbrenner, Dieter Flockerzi, Raimund Kuelzer, Hermann Tenor, Hans-Peter Kley
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Publication number: 20080312225Abstract: The compounds of formula (I) in which R1, R2 and R3 have the meanings as given in the description are novel effective PDE2 inhibitors.Type: ApplicationFiled: January 4, 2006Publication date: December 18, 2008Applicant: NYCOMED GMBHInventors: Beate Schmidt, Steffen Weinbrenner, Dieter Flockerzi, Raimund Kulzer, Hermann Tenor, Hans-Peter Kley
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Patent number: 7459414Abstract: Compounds of formula wherein the substituents have the meanings given in claim 1, and agronomically tolerable salts, isomers and enantiomers of those compounds, are suitable for use as herbicides.Type: GrantFiled: March 18, 2005Date of Patent: December 2, 2008Assignee: Syngenta Crop Protection, Inc.Inventors: Thomas Maetzke, André Stoller, Sebastian Wendeborn, Henry Szczepanski
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Publication number: 20080287394Abstract: Hydroxy-substituted pyrazinopyrrolopyridazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I) wherein R1, R2, R3, R4, R5, R6 and R7 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: May 3, 2005Publication date: November 20, 2008Applicant: MERCK & CO., INC.Inventors: John S. Wai, Joseph P. Vacca, Linghang Zhuang, Boyoung Kim, Terry A. Lyle, Catherine M. Wiscount, Melissa S. Egbertson, Lou Anne Neilson, Mark Embrey, Thorsten E. Fisher, Donnette D. Staas
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Publication number: 20080287465Abstract: Acrylic n-hydroxy imides and their use in pharmaceutical compositions and in the inhibition of flap endonuclease are disclosed.Type: ApplicationFiled: July 20, 2005Publication date: November 20, 2008Applicant: ATHERSYS, INC.Inventors: Lawrence N. Tumey, Youssef Bennani, Bayard Huck, David C. Bom
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Patent number: 7407964Abstract: This invention provides novel caspase inhibitors of formula I: wherein R1 is hydrogen, CHN2, R, or —CH2Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group, or a heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; X2—X1 is N(R3)—C(R3), C(R3)2—C(R3), C(R3)2—N, N?C, C(R3)?C, C(?O)—N, or C(?O)—C(R3); each R3 is independently selected from hydrogen or C1-6 aliphatic; Ring C is a fused aryl ring; n is 0, 1 or 2; and each methylene carbon in Ring A is optionally and independently substituted by ?O, or one or more halogen, C1-4 alkyl, or C1-4 alkoxy. The compounds are useful for treating caspase-mediated diseases.Type: GrantFiled: June 7, 2001Date of Patent: August 5, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Guy Brenchley
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Patent number: 7402682Abstract: A subject-matter of the invention is the compounds of general formula (I) in which X represents a hydrogen or halogen atom; R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 and R3 each represent, independently of one another, a hydrogen atom or a (C1-C4)alkyl group or else R2 and R3 form, with the nitrogen atom which carries them, a pyrrolidinyl, piperidinyl, morpholinyl or 4-alkylpiperazinyl group; and Het represents a heteroaromatic group of pyridinyl, 1-oxidopyridinyl, quinolinyl, isoquinolinyl, pyrimidinyl, pyrazinyl or pyridazinyl type, it being possible for the heteroaromatic group to carry one or more halogen atoms and/or one or more (C1-C4)alkyl or (C1-C4)alkoxy groups; in the form of bases, of addition salts with acids, of solvates or of hydrates, the pharmaceutical compositions comprising them, processes for their preparation and synthetic intermediates.Type: GrantFiled: June 29, 2006Date of Patent: July 22, 2008Assignee: Sanofi-AventisInventors: Philippe Burnier, Jacques Froissant, Benoit Marabout, Frank Marguet, Frederic Puech
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Publication number: 20080139569Abstract: Disclosed are a novel crystalline form of 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide, processes of preparing said crystalline form of 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide, compositions comprising said form in admixture with one or more pharmaceutically acceptable excipients, and uses for the same.Type: ApplicationFiled: February 14, 2008Publication date: June 12, 2008Applicant: SANOFI-AVENTIS U.S. LLC.Inventors: William L. ROCCO, John D. HIGGINS
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Patent number: 7365196Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.Type: GrantFiled: March 15, 2001Date of Patent: April 29, 2008Assignees: Merck Sharp & Dohme Ltd., Merck Frosst Canada & Co.Inventors: Patrice Charles Belanger, Ian James Collins, Joanne Claire Hannam, Timothy Harrison, Stephen John Lewis, Andrew Madin, Edward Giles McIver, Alan John Nadin, Joseph George Neduvelil, Mark Steven Shearman, Adrian Leonard Smith, Timothy Jason Sparey, Graeme Irvine Stevenson, Martin Richard Teall
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Patent number: 7365071Abstract: The invention relates to novel heterocyclic compounds of general formula (I) and to their salts with a base or an acid: The invention also relates to processes and to intermediates for the preparation of these compounds, and to their use as medicaments, in particular as antibacterials and ?-lactamase inhibitors.Type: GrantFiled: September 4, 2003Date of Patent: April 29, 2008Inventor: Branislav Musicki
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Patent number: 7351827Abstract: Oxetane-containing nucleosides, particularly non-reducing psiconucleoside oxetanes are described herein. Therapeutic application of these oxetane compounds toward the treatment of nucleoside analog related disorders such as disorders involving cellular proliferation and infection are also described.Type: GrantFiled: November 19, 2004Date of Patent: April 1, 2008Assignee: The University of ConnecticutInventors: Amy R. Howell, Rosa C. Taboada, Stewart K. Richardson
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Patent number: 7326709Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.Type: GrantFiled: May 30, 2006Date of Patent: February 5, 2008Assignee: Neurogen CorporationInventors: Jun Yuan, Pamela A. Albaugh, Kenneth Shaw, Alan J. Hutchison
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Publication number: 20080009499Abstract: Compounds of formula (I): as well as pharmaceutically acceptable salts and esters thereof for use as pharmaceutical compositions.Type: ApplicationFiled: July 2, 2007Publication date: January 10, 2008Inventors: Kurt Amrein, Daniel Hunziker, Bernd Kuhn, Alexander V. Mayweg, Werner Neidhart
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Patent number: 7288543Abstract: A compound of the formula (I) (I) wherein the variables X1 to X6, Ra, Rb, R1 to R7 including R3?, E, p, j, y, z, A, B and C are as described or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosedType: GrantFiled: March 8, 2005Date of Patent: October 30, 2007Assignee: Eli Lilly and CompanyInventors: Howard Barff Broughton, Nuria Diaz Buezo, Charles Howard Mitch, Concepcion Pedregal-Tercero
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Patent number: 7276505Abstract: Compounds of formula (I) are inhibitors of CD80 and useful in immunomodulation therapy: wherein R1 and R3 independently represent H; F; CI; Br; —NO2; —CN; C1-C6 alkyl optionally substituted by F or Cl; or C1-C6 alkoxy optionally substituted by F; R4 represents a carboxylic acid group (—COOH) or an ester thereof, or —C(?O)NR6R7, —NR7C(?O)R6, —NR7C(?O)OR6, —NHC(?O)NR7R6 or —NHC(?S)NR7R6 wherein R6 represents H, or a radical of formula -(Alk)m-Q wherein m is 0 or 1, Alk is an optionally substituted divalent straight or branched C1-C12 alkylene, or C2-C12 alkenylene, or C2-C12 alkynylene radical or a divalent C3-C12 carbocyclic radical, any of which radicals may contain one or more —O—, —S— or —N(R8)— links wherein R8, represents H or C1-C4 alkyl, C3-C4 alkenyl, C3-C4 alkynyl, or C3-C6 cycloalkyl, and Q represents H; —NR9R10 wherein R9 and R10 independently represents H; C1-C4 alkyl; C3-C4 alkenyl; C3-C4 alkynyl; C3-C6 cycloalkyl; an ester group; an optionally substituted carbocyclic or heterocyclic group; or R9Type: GrantFiled: March 10, 2004Date of Patent: October 2, 2007Assignee: Medigene LimitedInventor: Ian Richard Matthews
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Patent number: 7268138Abstract: The present invention provides compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.Type: GrantFiled: May 26, 2004Date of Patent: September 11, 2007Assignee: MGI GP, Inc.Inventors: Vincent J. Kalish, Jie Zhang, Weizheng Xu, Jia-He Li, Amy Dongxia Xing, Qun Liu
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Patent number: 7235554Abstract: The invention provides compounds of general formula (I) in which X represents a hydrogen or halogen atom; R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 and R3 each independently of one another represent a hydrogen atom or a (C1-C4)alkyl group, or else R2 and R3, together with the nitrogen atom bearing them, form a pyrrolidinyl, piperidinyl, morpholinyl or 4-(C1-C4)alkylpiperazinyl group; and Het represents a heteroaromatic group of pyridinyl, quinolinyl, isoquinolinyl, pyrimidinyl, pyrazinyl or pyridazinyl type which may carry one or more halogen atoms and/or one or more (C1-C4)alkyl and/or (C1-C4)alkoxy groups; in the form of bases, addition salts with acids, solvates or hydrates; the pharmaceutical compositions comprising them, processes for preparing them, and synthesis intermediates.Type: GrantFiled: April 2, 2003Date of Patent: June 26, 2007Assignee: Sanofi-AventisInventors: Jacques Froissant, Benoît Marabout, Frank Marguet, Frédéric Puech
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Patent number: 7230139Abstract: The present invention relates to Diterpenoid Compounds, compositions comprising an effective amount of a Diterpenoid Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering an effective amount of a Diterpenoid Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, or for inducing apoptosis in a cancer or neoplastic cell. The compounds, compositions, and methods of the invention are further useful for treating or preventing a fungal infection. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a fungus.Type: GrantFiled: June 10, 2004Date of Patent: June 12, 2007Assignee: Gemin X BiotechnologiesInventors: Jean-Francois Lavallee, Terrence W. Doyle, Elise Rioux, Laurent Belec, Daniel Rabouin, Xavier Billot, Samuel Fortin
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Patent number: 7220857Abstract: A compound represented by formula (I): Formula (I) wherein Z1 and Z2 each are atoms necessary for forming an aromatic ring; V1 and V2 each are a substituent W1 or W2; when at least one V1 is W1, at least one V2 is W2, or when at least one V1 is W2, at least one V2 is W1; r is 1 to 4; s is 1 to 4; M1 is a counter ion; m1 is the number necessary for neutralizing charge; W1 is a hydroxyl, primary- or secondary- or tertiary-amino, acylamino, or sulfonamido group; W2 is a nitro, cyano, alkoxycarbonyl, aryloxycarbonyl, alkyl- or aryl-sulfonyl, carbamoyl, sulfamoyl, alkenyl, alkynyl, aryl, heterocyclic, sulfo, carboxyl, heterocyclic oxy, ammonio, alkyl- or aryl-sulfinyl, alkyl- or aryl-sulfonyl, acyl, or aryl- or heterocyclic-azo group; and the aromatic ring may have a substituent other than V1 and V2.Type: GrantFiled: November 17, 2005Date of Patent: May 22, 2007Assignee: Fujifilm CorporationInventors: Katsumi Kobayashi, Yasuhiro Ishiwata, Kiyoshi Takeuchi
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Patent number: 7217844Abstract: The present invention relates to Diterpenoid Compounds, compositions comprising an effective amount of a Diterpenoid Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering an effective amount of a Diterpenoid Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, or for inducing apoptosis in a cancer or neoplastic cell. The compounds, compositions, and methods of the invention are further useful for treating or preventing a fungal infection. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a fungus.Type: GrantFiled: December 1, 2003Date of Patent: May 15, 2007Assignee: Gemin X BiotechnologiesInventors: Pierre Beauparlant, Giorgio Attardo, Zhiying Zhang, Angela M. Stafford, Rosa Ubillas, James B. McAlpine, Jean-Francois Lavallee, Samuel Fortin, Sasmita Tripathy
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Patent number: 7160884Abstract: The present invention relates to 1-/2-substituted-1H/-2H-[1,2,3]triazolo[4,5-g]phthalazine-4,9-dione compounds and their pharmaceutically acceptable salts, a process for preparing the compounds and a pharmaceutical composition comprising the compounds. The compounds are shown to effectively inhibit cell proliferation and are thus expected to be used for treatment or prevention or treatment of various cancers or as an ancillary(auxiliary) means of the same.Type: GrantFiled: January 12, 2006Date of Patent: January 9, 2007Assignee: EWHA University-Industry Collaboration FoundationInventors: Hea Young Park Choo, Jin Sung Kim, Hee Kyung Rhee, Hyun Joo Park, Sang Kook Lee, Chong Ock Lee
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Patent number: 7109194Abstract: The invention concerns compounds of general formula (I), wherein: X represents a hydrogen or halogen atom; R1 represents a hydrogen atom or a (C1–C4)alkyl group; R2 and R3, represent each, independently of each other, a hydrogen atom or a (C1–C4)alkyl group, or R2 and R3 form, with the atom which bears them, a pyrrolidinyl, piperidinyl, morpholinyl or 4-alkylpiperazinyl group; and Het represents a heteroaromatic group of pyridinyl, 1-oxidopyridinyl, quinolinyl, isoquinolinyl, pyrimidinyl, pyrazinyl, pyridazinyl type, the heteroaromatic group may represent one or several halogen atoms and/or one or several (C1–C4)alkyl, (C1–C4)alkoxyl groups; in the form of bases, addition salts to acids, solvates or hydrates.Type: GrantFiled: November 20, 2002Date of Patent: September 19, 2006Assignee: Sanofi-AventisInventors: Philippe Burnier, Jacques Froissant, Benoît Marabout, Frank Marguet, Frédéric Puech