The -c(=x)- Group Is Bonded Directly To The Nitrogen Patents (Class 548/195)
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Patent number: 7875639Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and L2, are defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: May 31, 2007Date of Patent: January 25, 2011Assignee: Abbott LaboratoriesInventors: Alan S. Florjancic, Michael J. Dart, Keith B. Ryther, Arturo Perez-Medrano, William A. Carroll, Meena V. Patel, Karin Rosemarie Tietje, Tongmei Li, Teodozyj Kolasa, Megan E. Gallagher, Sridhar Peddi, Jennifer M. Frost, Derek W. Nelson
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Publication number: 20110015240Abstract: The invention provides a thiazole derivative useful as a VAP-1 inhibitor, as well as a pharmaceutical agent for the prophylaxis or treatment of VAP-1 associated diseases and the like, a method of inhibiting VAP-1 in a subject, and a method for the prophylaxis or treatment of VAP-1 associated disease in a subject. The thiazole derivative is a compound represented by the formula (I): R1—NH—X—Y—Z wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: January 30, 2009Publication date: January 20, 2011Applicant: R-TECH UENO, LTD.Inventors: Tatsuya Matsukawa, Kazuhiro Masuzaki, Yosuke Kawai, Akiko Kawasaki, Akiko Akasaka, Makoto Takewaki
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Publication number: 20110009455Abstract: The present invention relates to novel compounds of general formula (I) and uses thereof. The present invention relates to novel compounds of general formula (I) for use as glucokinase activators in the treatment of diabetes and obesity.Type: ApplicationFiled: February 5, 2009Publication date: January 13, 2011Applicant: Merck Patent GesellschaftInventors: Christoph Saal, Lars Burgdorf, Ulrich Emde, Norbert Beier, Johannes Gleitz, Christine Charon
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Publication number: 20110003818Abstract: The present invention relates to compounds of formula I and salts thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameliorated by inhibition of phosphatidylinositol 3-kinase.Type: ApplicationFiled: June 28, 2010Publication date: January 6, 2011Inventors: Robin Alec Fairhurst, Pascal Furet, Marc Gerspacher, Robert Mah
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Publication number: 20110003851Abstract: The present embodiments relate to compounds with physiological effects, such as the activation of hematopoietic growth factor receptors. The present embodiments also relate to use of the compounds to treat a variety of conditions, diseases and ailments such as hematopoietic conditions and disorders.Type: ApplicationFiled: May 6, 2010Publication date: January 6, 2011Applicant: Ligand Pharmaceuticals, Inc.Inventors: Lin Zhi, Andrew R. Hudson, Cornelis A. Van Oeveren, Steven L. Roach, Jason C. Pickens, Yixing Shen, Catalina Cuervo, Lino J. Valdez, Jillian Basinger, Virgina H. Grant
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Publication number: 20100331304Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: October 30, 2008Publication date: December 30, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Angela Berry, Doris Riether, Renee M. Zindell, Nigel James Blumire
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Publication number: 20100331338Abstract: Novel compounds of the Formula (I) in which R1, R2, R3, and R4 have the meanings indicated in Claim 1, are activators of glucokinase and can be used for the prevention and/or treatment of Diabetes Type 1 and 2, obesity, neuropathy and/or nephropathy.Type: ApplicationFiled: February 2, 2009Publication date: December 30, 2010Applicant: Merck Patent GMBHInventors: Lars Burgdorf, Ulrich Emde, Johannes Gleitz, Norbert Beier, Christine Charon
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Publication number: 20100331379Abstract: The present invention relates to N-heteroaryl-benzamides, pharmaceutical compositions comprising the same, and methods of using the same. The N-heteroaryl-benzamides are useful in diseases or medical conditions mediated by glucokinase.Type: ApplicationFiled: April 27, 2007Publication date: December 30, 2010Inventors: Anthony Murray, Jesper Lau, Lone Jeppesen, Per Vedso, Dharma Rao Polisetti, Bapu Gaddam, Daniel P. Christen, Kalpathy Santhosh, Jeremy T. Cooper, Robert Carl Andrews
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Publication number: 20100330021Abstract: Compounds of the formula R—NH-Q??(I) provide pharmacological agents which are glucokinase activators and thus may be employed for the treatment of glucokinase mediated conditions. Accordingly, the compounds of formula (I) may be employed for prevention and treatment of impaired glucose tolerance, Type 2 diabetes and obesity.Type: ApplicationFiled: September 3, 2010Publication date: December 30, 2010Inventor: Gregory Raymond Bebernitz
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Patent number: 7858799Abstract: An ionic organic compound having a repeating unit of formula (I) can be synthesized easily from a readily available organic compound through a small number of reaction steps, can be produced without any purification technique such as chromatography, and can be used in a quite small amount for gelation of water or an ionic liquid without any other auxiliary solvent: [-(A-B-C)n-]•m(X)??(I) wherein A represents a group having a quaternary ammonium cation which is formed from a heterocyclic compound having at least one nitrogen atom; B represents a functional group, which may have a substituent, selected from amide, urea, urethane and peptide groups; C represents a divalent hydrocarbon group, which may have a substituent, capable of linking between A and B; X represents an anion; n represents the number of repeating units; m represents the total number of anions; and n and m are the same integer.Type: GrantFiled: January 30, 2006Date of Patent: December 28, 2010Assignee: National Institute of Advanced Industrial Science and TechnologyInventors: Masaru Yoshida, Nagatoshi Koumura, Nobuyuki Tamaoki, Hajime Kawanami, Hajime Matsumoto, Said Kazaoui, Nobutsugu Minami
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Publication number: 20100317842Abstract: The present application discloses methods for identifying inhibitors with high binding-affinity for the carbonic anhydrase-IX (CA-IX) enzyme using click chemistry and uses the candidates thereof as positron emission tomography (PET) imaging agents.Type: ApplicationFiled: August 25, 2010Publication date: December 16, 2010Applicant: SIEMENS MEDICAL SOLUTIONS USA, INC.Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Dhanalakshmi Kasi, Vani P. Mocharla, Bing Wang, Umesh B. Gangadharmath, Brian A. Duclos, Kai Chen, Wei Zhang, Gang Chen, Henry Clifton Padgett, Farhad Karimi, Peter J.H. Scott, Zhiyong Gao, Qianwa Liang, Thomas Lee Collier, Tieming Zhao, Chunfang Xia
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Publication number: 20100316605Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: June 9, 2010Publication date: December 16, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Kevin Michael Cottrell, Alex Aronov, Robert J. Davies, Jon H. Come, David Messersmith
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Publication number: 20100310493Abstract: Acetamide derivatives, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these acetamide derivatives.Type: ApplicationFiled: October 7, 2008Publication date: December 9, 2010Applicant: ADVINUS THERAPEUTICS PRIVATE LIMITEDInventors: Debnath Bhuniya, Sandeep Bhausaheb Bhosale, Gobind Sing Kapkoti, Venkata Poornapragnacharyulu Palle, Siddhartha De, Kasim A. Mookhtiar, Bhavesh Dave, Anil Deshpande, Santosh Kurhade, Balasaheb Kobal, Keshav Naik, Sachin Kandalkar
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Publication number: 20100311703Abstract: This compounds correspond to the formula (I), where: R1 represents and aryl or heteroaryl group optionally substituted by one or more substituents selected from the group consisting of halogen atoms, straight or branched optionally substituted lower alkyl, cycloalkyl, hydroxy, straight or branched, optionally substituted lower alkoxy, cyano, or —CO2R?, wherein R? represents a hydrogen atom or a straight or branched, optionally substituted lower alkyl group; R2 represents a group selected from: a) a straight or branched lower alkyl group substituted by one or more carboxylic groups (—COOH) and optionally substituted by one or more halogen atoms; b) a cycloalkyl group substituted by one or more carboxylic groups (—COOH) and optionally substituted by one or more halogen atoms; c) a straight or branched alkylcycloalkyl or cycloalkylalkyl group substituted by one or more carboxylic groups (—COOH) and optionally substituted by one or more halogen atoms. Formula (I).Type: ApplicationFiled: September 30, 2008Publication date: December 9, 2010Applicant: PALOBIOFARMA, S.L.Inventors: Lyhen Gonzalez Lio, Juan Alberto Camacho Gomez
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Publication number: 20100297097Abstract: The present invention relates to substituted triazole compounds of the formula (I): and salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds for inhibiting SCD activity, such as diseases related to elevated lipid levels, cardiovascular disease, diabetes, obesity, metabolic syndrome, skin disorders such as acne, diseases or conditions related to cancer and the treatment of symptoms linked to the production of the amyloid plaque-forming A?42 peptide such as Alzheimer's disease and the like.Type: ApplicationFiled: November 7, 2008Publication date: November 25, 2010Inventors: Anne Marie Jeanne Bouillot, Alain Laroze
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Patent number: 7838681Abstract: The invention relates to a method of synthesizing heterocyclic compounds. The invention is characterised in that it consists in opening a compound having formula (I), wherein: —X represents NH, O, S or a N-p group, p being a protective group, such as Boc or Troc; —Y represents N, O, S; —Z represents NH2 or NH-p; and —R1 represents a C1-C6 alkoxy radical, aryloxy, such as phenyloxy, or a pyrrolyl radical, said radicals being optionally substituted, or the salts thereof, and the isomers of the aforementioned compounds. Moreover, the above-mentioned opening step is performed in conditions such as to produce a heterocycle having formula (II), wherein: —X, Y and Z are as defined above; —R2 represents a —CH?CH—CH2—NH—COR1 or —CH?CH—CH2—NH—CO group; and R3 occupies one, two or three positions and represents a halogen. The invention can be used to synthesise natural products.Type: GrantFiled: April 30, 2004Date of Patent: November 23, 2010Assignees: Centre National de la Recherche Scientifique (C.N.R.S.), Universite de Paris SudInventors: Ali Al Mourabit, Nathalie Travert, Robert Abou-Jneid, Saïd Ghoulami
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Publication number: 20100292274Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.Type: ApplicationFiled: May 11, 2010Publication date: November 18, 2010Inventors: Jean-Francois Rossignol, J. Edward Semple
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Publication number: 20100292143Abstract: Pyrrole-2-carboxamide derivatives, their polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts and formulations thereof, beneficial for prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these pyrrole-2-carboxamides.Type: ApplicationFiled: June 5, 2008Publication date: November 18, 2010Applicant: ADVINUS THERAPEUTICS PRIVATE LIMITEDInventors: Debnath Bhuniya, S. Gobind Kapkoti, S. Jayakumar Warrier, Gagan Kukrejka, N. Jagadeesh Mavinahalli, P. Venkata Palle, A. Kasim Mookhtiar
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Publication number: 20100286171Abstract: A phenylacetamide derivative having sulfonyl group and cycloalkyl group on the phenyl group and having heteroaryl group on the nitrogen atom in the amide has an excellent GK activation action, thereby completing the present invention. The compound of the present invention is useful as an agent for treating diabetes, in particular, type II diabetes, since it has an excellent GK activation action.Type: ApplicationFiled: January 16, 2009Publication date: November 11, 2010Applicant: ASTELLAS PHARMA INC.Inventors: Masahiko Hayakawa, Yoshiyuki Kido, Takahiro Nigawara, Mitsuaki Okumura, Akira Kanai, Keisuke Maki, Nobuaki Amino
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Publication number: 20100280036Abstract: The present invention relates to the use of compounds of the general Formula (I): wherein in Formula (I), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R1 is H, alkyl, cycloalkyl, aryl or heteroaryl; R2 is H, alkyl, cycloalkyl, aryl or heteroaryl; A1 and A2 each independently represent an optionally substituted C1-C20-alkyl group which may contain one or more group(s) Z, or a monocyclic or polycyclic optionally substituted aromatic or non-aromatic ring system which may contain one or more group(s) X, and in case of a polycyclic ring system, said system contains at least one aromatic ring; Z is selected from the group consisting of S, O, N, NR4, CO, CO2, CS, SO or SO2 X is selected from the group consisting of S, O, N, NR4, SO or SO2;Type: ApplicationFiled: December 28, 2007Publication date: November 4, 2010Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
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Publication number: 20100280034Abstract: The present invention relates to the use of compounds of the general Formula (XIII): wherein A7 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; A8 is C(R14)2, O, S, or NR12; A9 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; m is 0, or 1 q is 0, or 1 r is 0, or 1 R12 is H, CH3, CH2—CH3, C6H5, OCH3, OCH2—CH3, OH, or SH; R13 is H, CH3, or CH2—CH3; R14 is H, alkyl, alkoxy, OH, or SH;Type: ApplicationFiled: December 28, 2007Publication date: November 4, 2010Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
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Publication number: 20100273839Abstract: The invention provides compositions, pharmaceutical preparations and methods for increasing activity of a mutant cystic fibrosis transmembrane conductance regulator protein (mutant-CFTR). The compositions pharmaceutical preparations and methods are useful for the study and treatment of disorders associated with mutant-CFTR, such as cystic fibrosis. The compositions and pharmaceutical preparations of the invention may comprise one or more bithiazole-containing compounds of the invention, or an analog or derivative thereof.Type: ApplicationFiled: September 5, 2008Publication date: October 28, 2010Inventors: Mark J. Kurth, Alan S. Verkman
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Publication number: 20100273843Abstract: The present invention provides heterocyclic linker compounds useful for linking drug moieties to ligands. The compounds also include drug-ligand conjugates comprising a ligand capable of targeting a selected cell population, and a drug connected to the ligand by a heterocyclic linker moiety. The linker moiety comprises a peptide sequence that is a substrate for an intracellular enzyme, for example a cathepsin, that cleaves the peptide at an amide bond. The peptide further contains a self-immolating moiety which connects the drug and the protein peptide sequence. Upon cleavage of the peptide sequence by an intracellular enzyme the self-immolating moiety cleaves itself from the drug moiety such that the drug moiety is in an underivatized and active form.Type: ApplicationFiled: April 21, 2010Publication date: October 28, 2010Inventor: Bainian Feng
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Publication number: 20100267783Abstract: An optically active 4-phenylthiazole derivative having a thrombopoietin receptor agonist activity and a pharmaceutical composition containing the present compound as an active ingredient are created, and a platelet production regulating agent which can be orally administered is provided. Disclosed is a pharmaceutical composition containing, as an active ingredient, an optically active compound represented by the formula: wherein, R1 is a halogen atom or C1-C3 alkyloxy; R2 is C1-C8 alkyl; R3 is C1-C8 alkyl; R4 and R5 are each independently a fluorine atom or chlorine atom; R6 is C1-C3 alkyl or C1-C3 alkyloxy; * indicates that a carbon atom marked with an asterisk is an asymmetric carbon, a pharmaceutically acceptable salt thereof, or a solvate thereof.Type: ApplicationFiled: July 29, 2008Publication date: October 21, 2010Inventors: Masami Takayama, Noriyuki Kurose
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Patent number: 7799933Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R1, R2, R3, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.Type: GrantFiled: December 6, 2007Date of Patent: September 21, 2010Assignee: Hoffman-La Roche Inc.Inventors: Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei, Ulrike Obst Sander
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Patent number: 7799738Abstract: 2-Acylaminothiazole-4-carboxamides of the formula (I) and application thereof as an insecticide. wherein R1 represents phenyl which may be optionally substituted, or a 5- or 6-membered heterocyclic group containing at least one hetero atom selected from a group consisting of N, O and S which may be optionally substituted, R2 represents halogen, C1-6 alkyl or C1-6 haloalkyl, R3 represents C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 haloalkylthio, C1-6 haloalkylsulfinyl or C1-6 haloalkylsulfonyl, R4 represents halogen, C1-6 alkyl or C1-6 haloalkyl, and X represents hydrogen, halogen, C1-6 alkyl or C1-6 haloalkyl, and the use of the new compounds as insecticides.Type: GrantFiled: October 26, 2006Date of Patent: September 21, 2010Assignee: Bayer CropScience AGInventors: Akihiko Yanagi, Yukiyoshi Watanabe, Jun Mihara, Katsuhiko Shibuya, Eiichi Shimojo, Akira Emoto
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Patent number: 7795304Abstract: The invention relates to hydroxamic acid derivatives having carbamate linkage with the structural formula that are inhibitors of histone deacetylase (HDAC), and are useful in the prevention and/or treatment of cellular proliferative diseases, for example cancer, autoimmune, allergic and inflammatory diseases, diseases of the central nervous systems (CNS) such as neurodegenerative diseases, and in the prevention and/or treatment of restenosis.Type: GrantFiled: August 22, 2005Date of Patent: September 14, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Sandro Belvedere, Christopher Laurence Hamblett, Thomas A. Miller, David J. Witter, Jiaming Yan
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Patent number: 7795290Abstract: 2-Amido-4-substituted-aryl-thiazole-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, methods of using compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions comprising compounds exhibiting ATP-utilizing enzyme inhibitory activity, are disclosed.Type: GrantFiled: July 3, 2008Date of Patent: September 14, 2010Assignee: Genentech, Inc.Inventors: John K. Dickson, Jr., Carl Nicholas Hodge, Jose Serafin Mendoza, Ke Chen
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Publication number: 20100222329Abstract: A 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and an activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colonies. A compound or a pharmaceutically acceptable salt thereof useful in treating thrombocytopenia.Type: ApplicationFiled: November 10, 2009Publication date: September 2, 2010Applicant: Astellas Pharma Inc.Inventors: Keizo Sugasawa, Susumu Watanuki, Yuji Koga, Hiroshi Nagata, Ryutaro Wakayama, Fukushi Hirayama, Ken-ichi Suzuki
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Publication number: 20100222217Abstract: N-[2-(Haloalkoxy)phenyl]heteroarylcarboxamides of the formula I, where n=0 or 1, Hal=halogen, X=C2-C4-haloalkyl, Het=a pyrazole, thiazole or pyridine radical (a), (b) or (c), where R1=C1-C4-alkyl or C1-C4-haloalkyl, R2=hydrogen or halogen, R3=C1-C4-alkyl or C1-C4-haloalkyl and R5=halogen, C1-C4-alkyl or C1-C4-haloalkyl; except for N-[2-(1,1,2,2-tetrafluoroethoxy)phenyl]-1,3-dimethylpyrazol-4-yl-carboxamide, N-[2-(1,1,2,2-tetrafluoroethoxy)phenyl]-3-trifluoromethyl-1-methylpyrazol-4-yl-carboxamide and N-[2-(2,2,2-trifluorethoxy)phenyl]-3-trifluormethyl-1-methylpyrazol-4-yl-carboxamide. A fungicidal composition comprising at least one compound I, the use of the compounds I for preparing a composition suitable for controlling harmful fungi, a method for controlling harmful fungi using the compounds I and also seed comprising at least one compound I.Type: ApplicationFiled: August 2, 2006Publication date: September 2, 2010Inventors: Markus Gewehr, Jochen Dietz, Thomas Grote, Wassilios Grammenos, Bernd Müller, Jan Klaas Lohmann
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Publication number: 20100216760Abstract: Disclosed herein are cannabinoid receptor ligands of formula (I) wherein L1, A1, R1g, z, R2, R3, and R4 are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.Type: ApplicationFiled: December 16, 2009Publication date: August 26, 2010Applicant: ABBOTT LABORATORIESInventors: Jennifer M. Frost, Steven P. Latshaw, Michael J. Dart, William A. Carroll, Arturo Perez-Medrano, Teodozyj Kolasa, Meena V. Patel, Derek W. Nelson, Tongmei Li, Sridhar Peddi, Xueqing Wang, Bo Liu
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Publication number: 20100216795Abstract: The present invention relates to Traf2- and Nck-interacting kinase (TNIK) inhibitors, pharmaceutical compositions, and methods for the treatment of cancer patients with TNIK inhibitors. And the present invention relates to a novel aminothiazole derivatives. The TNIK inhibitors are showed by a next formula (I). Wherein R1, R2, R3, R4, R5 and R6 represent independently a hydrogen atom or a substituent group.Type: ApplicationFiled: April 23, 2010Publication date: August 26, 2010Inventors: Tesshi Yamada, Miki Shitashige, Koichi Yokota, Masaaki Sawa, Hideki Moriyama
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Publication number: 20100196502Abstract: One aspect of the invention relates to isoform-selective HDAC inhibitors. Also provided are methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy. The invention also provides methods for treating cancer, methods for treating neurological diseases and methods for treating malaria. Additionally, the invention provides pharmaceutical compositions comprising an HDAC inhibitor of the invention; and kits comprising a an HDAC inhibitor of the invention.Type: ApplicationFiled: August 2, 2007Publication date: August 5, 2010Applicant: Georgetown UniversityInventors: Alan P. Kozikowski, Mira Jung, Anatoly Dritschilo, Arsen Gaysin, Pavel A. Petukhov, Werner Tueckmantel, Hongbin Yuan
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Patent number: 7759377Abstract: Compounds of formula (I) as defined herein: inhibit the formation of the ?-amyloid peptide (?-A4) and are, therefore, useful in the treatment of pathologies in which a ?-amyloid peptide (?-A4) formation inhibitor provides a therapeutic benefit. Particular such pathologies are senile dementia, Alzheimer's disease, Down's syndrome, Parkinson's disease, amyloid angiopathy, cerebrovascular disorders, frontotemporal dementias and Pick's disease, post-traumatic dementias, pathologies linked to neuroinflammatory processes, Huntington's disease and Korsakov's syndrome.Type: GrantFiled: March 20, 2008Date of Patent: July 20, 2010Assignee: Sanofi-AventisInventors: Sylvie Baltzer, Marc Pascal, Viviane Van Dorsselaer
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Publication number: 20100179201Abstract: The present invention relates to novel thiazole-based compounds and T-type calcium channel inhibitors containing the compound. The T-type calcium channel inhibitor of the present invention is useful as a treating agent for disease associated with overexpression of T-type calcium channel.Type: ApplicationFiled: December 8, 2006Publication date: July 15, 2010Applicant: Korea Institute of Science and TechnologyInventors: Hoh-Gyu Hahn, Dong-Yun Shin, Kee-Dal Nam
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Patent number: 7754743Abstract: Compounds having glucokinase activating effects and being useful as treatments for diabetes, which are represented by the following formula (I): [wherein X1 represents oxygen, etc., X2 represents oxygen, etc., R1 represents a group on Ring A such as alkylsulfonyl, etc., R2 represents C3-7 cyclic alkyl optionally substituted with a halogen, etc., R3 represents a substituent on Ring B such as lower alkyl, etc., formula (II): [Chemical Formula 1] represents 6- to 10-membered aryl, etc., and formula (III): [Formula 1] represents monocyclic or bicyclic heteroaryl optionally having on Ring B a substituent represented by R3 above, wherein the carbon atom of Ring B which is bonded to the nitrogen atom of the amide group of formula (I) forms a C?N bond with the nitrogen atom of the ring], as well as their pharmaceutically acceptable salts.Type: GrantFiled: September 5, 2008Date of Patent: July 13, 2010Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Tomoharu Iino, Noriaki Hashimoto, Hiroshi Nakashima, Keiji Takahashi, Teruyuki Nishimura, Jun-ichi Eiki
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Publication number: 20100173899Abstract: Disclosed are novel dipeptide analogs compounds of Formula (I), (II) or (III): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a solvate, or a prodrug thereof, which are inhibitors of factor XIa and/or plasma kallikrein, compositions containing them, and methods of using them, for example, for the treatment or prophylaxis of thrombotic diseases.Type: ApplicationFiled: June 11, 2008Publication date: July 8, 2010Inventors: Donald J.P. Pinto, Mimi L. Quan, Leon M. Smith, II, Michael J. Orwat, Paul J. Gilligan
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Publication number: 20100168070Abstract: The invention relates to substituted 1,2-ethylenediamines of general formula (I), wherein the radicals R1-R13, A, B, L and i are as defined in the description and in the claims. The invention also relates to the use thereof for treating Alzheimer's disease (AD) and similar diseases.Type: ApplicationFiled: August 8, 2006Publication date: July 1, 2010Inventors: Niklas Heine, Klaus Fuchs, Christian Eickmeier, Stefan Peters, Cornelia Dorner-Ciossek, Sandra Handschuh, Herbert Nar, Klaus Klinder
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Publication number: 20100160327Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: June 21, 2006Publication date: June 24, 2010Inventors: Jonathan Grimm, Paul Harrington, Richard Heidebrecht, JR., Thomas Miller, Karin Otte, Phieng Siliphaivanh, David Sloman, Matthew Stanton, Kevin Wilson, David Witter, Solomon Kattar, Paul Tempest
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Patent number: 7741491Abstract: The invention therefore relates to compounds of the formula I in which the variables are as defined in the specification, to pharmaceutical compositions containing them and to their use for therapeutically lowering blood glucose levels.Type: GrantFiled: December 12, 2006Date of Patent: June 22, 2010Assignee: Sanofi-Aventis Deutschland GmbHInventors: Stefan Petry, Karl-Heinz Baringhaus, Norbert Tennangels, Guenter Mueller, Reinhard Kirsch
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Patent number: 7741327Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: GrantFiled: March 9, 2009Date of Patent: June 22, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Steven Joseph Berthel, John A Brinkman, Stuart Hayden, Nancy-Ellen Haynes, Robert Francis Kester, Lee Apostle McDermott, Yimin Qian, Ramakanth Sarabu, Nathan Robert Scott, Jefferson Wright Tilley
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Publication number: 20100143499Abstract: Compounds, compositions, and methods of using such compounds to modulate apoptosis including IAP antagonists are provided herein. Compositions including mimetics of the invention and, optionally, secondary agents, may be used to treat proliferative disorders such as, cancer and autoimmune diseases.Type: ApplicationFiled: July 24, 2007Publication date: June 10, 2010Applicant: TETRALOGIC PHARMACEUTICALS CORPORATIONInventor: Stephen M. Condon
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Publication number: 20100144772Abstract: Compounds of the present disclosure are 2,2,2-tri-substituted acetamide derivatives of formula (I), its polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts and formulations thereof, useful as Glucokinase activator. Processes of their preparation are also described in the disclosure. The disclosure also describes method to characterize partial glucokinase activators.Type: ApplicationFiled: February 25, 2008Publication date: June 10, 2010Applicant: ADVINUS THERAPEUTICS PRIVATE LIMITEDInventors: Kasim A. Mookhtiar, Debnath Bhuniya, Bhavesh Dave, Gobind S. Kapkoti, Sujay Basu, Anita Chugh, Siddhartha De, Venkata P. Palle
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Publication number: 20100144721Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: September 4, 2007Publication date: June 10, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Tiansheng Wang, Jeremy Green, Brain Ledford, Francois Maltais, Andreas Termin
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Publication number: 20100135960Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: November 17, 2009Publication date: June 3, 2010Inventors: Yat Sun Or, Lu Ying, Ce Wang, Xiaowen Peng, Yao-Ling Qiu
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Patent number: 7718808Abstract: (Wherein n is an integer of from 0 to 3; R1 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, a substituted or unsubstituted alicyclic heterocyclic group, or a substituted or unsubstituted aromatic heterocyclic group; R2 is halogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, a substituted or unsubstituted alicyclic heterocyclic group, a substituted or unsubstituted aromatic heterocyclic group, —COR8, or the like; R3 and R4 may be the same or different, and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl, —COR12, or the like) For example, provided are adenosine A2A receptor antagonists comprising, as the active ingredient, a thiazole derivative represented by a general formula (I), or a pharmaceutically acceptable salt thereof, and the like.Type: GrantFiled: December 24, 2004Date of Patent: May 18, 2010Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Takao Nakajima, Masamori Sugawara, Shin-ichi Uchida, Tetsuji Ohno, Yuji Nomoto, Noriaki Uesaka, Yoshisuke Nakasato
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Publication number: 20100105914Abstract: The present invention provides a compound of formula I: wherein the variables are as defined herein. The present invention also provides processes for preparing the compounds of formula I, and intermediates thereof, pharmaceutical compositions comprising those compounds, and methods of using the compounds and compositions.Type: ApplicationFiled: December 3, 2009Publication date: April 29, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Jean-Damien Charrier, Steven Durrant, Michael Mortimore, Michael O'Donnell, Alistair Rutherford, Sharn Ramaya, John R. Studley, Martin Trudeau, Adam Looker
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Patent number: 7705158Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted aryl sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel.Type: GrantFiled: November 2, 2006Date of Patent: April 27, 2010Assignee: Icagen, Inc.Inventors: Xiaodong Wang, Alan Fulp, Brian Marron, Serge Beaudoin, Darrick Seconi, Mark Suto
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Publication number: 20100099671Abstract: A compound, or a pharmaceutically acceptable salt thereof, represented by the formula (1), (wherein, the carbon atom marked with an * is in the R-configuration, R1 represents a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1-C6 alkyl group, or a C1-C6 alkoxy group, R2 represents a C3-C6 cycloalkylsulfanyl group, a C3-C6 cycloalkylsulfinyl group, or a C3-C6 cycloalkylsulfonyl group, and A represents a substituted or unsubstituted heteroaryl group).Type: ApplicationFiled: March 6, 2008Publication date: April 22, 2010Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Masanori Takadoi, Kohei Ohata, Tomohiro Ide, Fumiyoshi Kobayashi, Shinji Kobayashi, Kanji Komatsu, Masanori Yamamoto
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Publication number: 20100099662Abstract: A hydrazone derivative of formula [I]: wherein Ring A is aryl or heteroaryl, Ring T is heteroaryl or heterocycle, R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl, etc., R3 and R4 combine each other together with the adjacent nitrogen atom to form substituted or unsubstituted heterocycle, R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl, etc., and R6 is hydrogen atom, etc.; or a pharmaceutically acceptable salt thereof is useful as a glucokinase activation agent.Type: ApplicationFiled: January 9, 2008Publication date: April 22, 2010Inventors: Iwao Takamuro, Kazutoshi Sugawara, Hiroshi Sugama