Nitrogen, Other Than As Nitro Or Nitroso, Attached Directly To The Carbocyclic Ring Of The Quinoline Ring System By Nonionic Bonding Patents (Class 546/171)
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Publication number: 20120202848Abstract: This invention is in the fields of immunology and autoimmunity. More particularly it concerns methods of treating patients with compounds which are useful agents for inhibiting the functions of TIP60 in the treatment of an individual suffering, for example, from ulcerative colitis and other irritable bowel diseases.Type: ApplicationFiled: December 2, 2011Publication date: August 9, 2012Applicant: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIAInventors: MARK I. GREENE, WAYNE W. HANCOCK, MAKOTO KATSUMATO, YAN XIAO
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Publication number: 20120189614Abstract: Organic compounds showing the ability to inhibit viral glycoprotein (GP)-mediated entry of a filovirus into a host cell are disclosed. The disclosed filovirus entry inhibitor compounds are useful for treating, preventing, or reducing the spread of infections by filovirus including the type species Marburg virus (MARV) and Ebola virus (EBOV). Preferred inhibitors of the invention provide therapeutic agents for combating the Ivory Coast, Sudan, Zaire, Bundibugyo, and Reston Ebola virus strains.Type: ApplicationFiled: July 10, 2010Publication date: July 26, 2012Applicant: Crobiotix, Inc.Inventors: Arnab Basu, Debra M. Mills, Norton P. Peet, John D. Williams
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Patent number: 8222248Abstract: The present invention provides compounds of the following structure; A-L1-B—C-D that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.Type: GrantFiled: October 17, 2007Date of Patent: July 17, 2012Assignee: Novartis AGInventors: Moo Je Sung, Gary Mark Coppola, Taeyoung Yoon, Thomas A. Gilmore
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Publication number: 20120177570Abstract: The invention relates to compounds of formula IA? and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula IA? or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula IA? or a pharmaceutically acceptable derivative thereof.Type: ApplicationFiled: February 14, 2012Publication date: July 12, 2012Applicant: Purdue Pharma L.P.Inventor: Laykea TAFESSE
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Publication number: 20120178733Abstract: The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.Type: ApplicationFiled: August 19, 2011Publication date: July 12, 2012Inventors: Bing-Yan Zhu, Shawn M. Bauer, Zhaozhong J. Jia, Gary D. Probst, Yanchen Zhang, Robert M. Scarborough
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Publication number: 20120165276Abstract: Disclosed are compounds having at least one quaternary alkyl ammonium functionality. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effective against bacterial infections that have developed resistance to anti-bacterial agents through an efflux pump mechanism.Type: ApplicationFiled: May 6, 2008Publication date: June 28, 2012Applicant: Mpex Pharmaceuticals, Inc.Inventors: TOMASZ GLINKA, Olga Lomovskaya, Keith Bostian, David M. Wallace
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Publication number: 20120136002Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.Type: ApplicationFiled: May 18, 2010Publication date: May 31, 2012Inventors: Rajeev Goswami, Anil Kumar Vuppala, Ramesh Veludandi, Ramesh Sistla, Chakshusmathi Ghadiyaram, Muralidhara Ramachandra
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Publication number: 20120129818Abstract: Ortho methoxy phenolic compounds are provided that include methylenedioxyphenyl ferulate and ferulylproline and derivatives thereof. Pharmaceutical compositions comprising the compounds and methods of using the compounds for treating cardiovascular diseases, including hypertension, atherosclerosis, coronary heart disease, angina, stroke, and myocardial infarction, are further provided. The compounds are also useful in reducing low-density lipoprotein oxidation, improving or increasing vasodilation, and reducing plaque destabilization in a subject.Type: ApplicationFiled: April 23, 2010Publication date: May 24, 2012Inventor: Desikan Rajagopal
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Publication number: 20120129887Abstract: The present invention refers to new compounds represented by the general formula (I) where X is represented by the general formula (II) and Y is represented by the general formula (III). The relation X to Y may vary from 1:1 to 1:7. The radicals R1, R2, R3, R4, R5, and R6 in formula (II) are represented by: R1?H, CF3, CH3, OCH3, NH2, halogen; R2?H, CH3, NH2, halogen, NH—CHCH3(CH2)3N(C2H5)(CH2CH2OH), CH(OH)-2(C5H11N), NH—R7—N—(C2H5)2; R3?H, m-OC6H4CF3, NH2; R4?H, CH3, OCH3, NH2, halogen; R5?H, CH3, CF3, NH2, halogen; R6?H, CF3, CH3, NH2, halogen, NH—R8—N—(C2H5)2, NHCH(CH3)(CH2)3NH2; R7?(CH2)2, (CH2)3, CHCH3CH2, (CH2)4, (CH2)5, CHCH3(CH2)3, (CH2)6, (CH2)8, (CH2)10, (CH2)12; R8?CHCH3(CH2)3, CHCH3(CH2)CHCH3, (CH2)2, (CH2)3, (CH2)6, (CH2)3O(CH2)3. This invention also refers to a process of preparation of these compounds (formula I), and antiparasitic pharmaceutical compositions thereof.Type: ApplicationFiled: November 14, 2011Publication date: May 24, 2012Inventors: Núbia Boechat, Marcus Vinicius Nora de Souza, Alessandra Leda Valverde, Antoniana Ursine Krettli
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Publication number: 20120129842Abstract: This invention relates to bisthiazole I and its therapeutic and prophylactic uses, wherein the variables A, R5, R6, and R7 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.Type: ApplicationFiled: November 16, 2011Publication date: May 24, 2012Inventors: Paul Francis JACKSON, Brett Andrew Tounge, Kristi Anne Leonard, Yan Zhang, Aihua Wang, Michael Hawkins, Umar S.M. Maharoof, Joseph Kent Barbay
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Publication number: 20120122849Abstract: Compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are pharmaceutical compositions comprising the compounds, and methods of using the compounds in the treatment of cancer.Type: ApplicationFiled: November 4, 2011Publication date: May 17, 2012Inventors: Francesco G. Salituro, Jeffrey O. Saunders
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Publication number: 20120122885Abstract: Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.Type: ApplicationFiled: October 6, 2011Publication date: May 17, 2012Inventors: Francesco G. Salituro, Jeffrey O. Saunders
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Publication number: 20120122923Abstract: The invention concerns dual molecules corresponding to formula (I): in which: A represents a molecular residue with antimalarial activity of formula (IIa) or (IIIa) or a residue facilitating bioavailability; B represents a cycloalkyl group potentially substituted, or B represents a bi- or tricyclic group capable of being substituted, or B represents 2 cycloalkyl groups linked together through either a single bond or an alkylene chain; m and n represent independently of one another 0, 1 or 2; R5 represents a hydrogen atom, an alkyl, cycloalkyl or C1-3-alkylene-cycloakyl group; Z1 and Z2 represent an alkyl radical, the group Z1+Z2+Ci+Cj representing a mono- or polycyclic structure, with one of the Z1 or Z2 being able to represent a single bond; R1 and R2, identical or different, represent a hydrogen atom or a functional group capable of increasing hydrosolubility; Rx and Ry forming together a cyclic peroxide including 4 to 8 links and including 1 or 2 additional oxygen atoms in the cyclic structure, possibly suType: ApplicationFiled: December 11, 2008Publication date: May 17, 2012Applicants: SANOFI-AVENTIS, PALUMED S.A., CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (C.N.R.S.)Inventors: Frederic COSLEDAN, Bernard MEUNIER, Alain PELLET
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Publication number: 20120108609Abstract: The invention relates to compounds of formula wherein R1, R2, R3, R4, X, Ar, and are defined herein or to a pharmaceutically suitable acid addition salt thereof. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm and cardiovascular disorders.Type: ApplicationFiled: October 24, 2011Publication date: May 3, 2012Inventors: Matthias Nettekoven, Roger Norcross, Alessandra Polara
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Patent number: 8158799Abstract: Compounds of the formula I in which X, Y, R1, R1?, R2, R3 have the meanings indicated in Claim 1, are inhibitors of cell proliferation and can be employed for the treatment of tumors.Type: GrantFiled: November 14, 2006Date of Patent: April 17, 2012Assignee: Merck Patent Gesellschaft MIT Meschraenkter HaftungInventors: Oliver Schadt, Dieter Dorsch, Claus Fittschen, Matthias Grell
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Publication number: 20120088770Abstract: Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a chemical library relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.Type: ApplicationFiled: May 7, 2010Publication date: April 12, 2012Applicant: Prism BioLab CorporationInventors: Takenao Odagami, Yiji Kogami, Hiroyuki Kouji
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Patent number: 8153803Abstract: The present invention is based, in part, on our discovery of compounds that inhibit an activity of a sirtuin (e.g., compounds that inhibit or preferentially inhibit an activity of SIRT2) and are therefore believed useful in the treatment or prevention of diseases associated with sirtuin activity. These diseases include, but are not limited to, neurological disorders such as Parkinson's Disease (PD).Type: GrantFiled: June 20, 2008Date of Patent: April 10, 2012Assignee: The General Hospital CorporationInventor: Aleksey G. Kazantsev
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Publication number: 20120039847Abstract: The present invention provides compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: August 12, 2011Publication date: February 16, 2012Inventor: Shu-Hai Zhao
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Publication number: 20120035371Abstract: The current invention describes novel chiral synthetic routes and intermediates for the manufacture of chiral anti-inflammatory agents of general formula VIII in which at least one of the groups X1, X2, X3 is selected from fluoro, chloro, bromo, hydroxy, methoxy, ethoxy, trifluoromethyl, amino whereas the other groups X1, X2, X3 have the meaning of a hydrogen atom, in which at least one of the groups Z1, Z2, Z3 is selected from —O—, —S—, —NH—, —N(—CH3)—, whereas the other groups Z1, Z2, Z3 have the meaning of a —CH2— group, and in which Ar is an aromatic group.Type: ApplicationFiled: October 14, 2011Publication date: February 9, 2012Inventor: Steffen SCHWEIZER
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Publication number: 20120035213Abstract: The present invention provides a compound having a melanin-concentrating hormone receptor antagonistic action and low toxicity, which is useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: January 29, 2010Publication date: February 9, 2012Inventors: Toshiki Murata, Masahiro Kamaura
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Patent number: 8106206Abstract: Provided is a solid luminescent quinoline compound capable of emitting light in a crystalline state, capable of changing the luminescent color not requiring modification of molecular configuration and capable of emitting light in response to external pressure such as heat, physical pressure, etc. The quinoline compound is represented by the following general formula (1): wherein R1 may be the same or different, each representing any of CF3 or CF3CF2; R2 represents any of an amino group, an N,N-dimethylamino group, an N-phenylamino group, a carbazole group, an N-methylamino group or an N-methyl-N-phenylamino group.Type: GrantFiled: November 19, 2010Date of Patent: January 31, 2012Assignee: Kyushu University, National University CorporationInventors: Noboru Koga, Satoru Karasawa, Yuichiro Abe
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Publication number: 20120022070Abstract: Novel classes of molecular chaperone Heat shock protein 90 (Hsp90) inhibitors are disclosed. These compounds are useful in treating and preventing cancer and other Hsp90-related diseases and conditions, such as inflammation and neurodegenerative disorders. Methods of treating and preventing cancer and other Hsp90 related diseases and conditions are disclosed that include administering to the subject a therapeutically effective amount of an Hsp90 inhibitor. Methods of preparing the novel Hsp90 inhibitors are also provided.Type: ApplicationFiled: October 6, 2009Publication date: January 26, 2012Applicant: EMORY UNIVERSITYInventors: Jaeki Min, Pahk Thepchatri, Yuhong Du, Dennis C. Liotta, Haian Fu
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Publication number: 20120015946Abstract: A compound of formula (I): wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5a, R5b and R6 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: February 18, 2010Publication date: January 19, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Peter Renold, Thomas Pitterna, Jerome Yves Cassayre, Myriem El Qacemi
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Publication number: 20120015952Abstract: The invention relates to compounds of formulae (1) and (2): and pharmaceutically acceptable salts thereof for the treatment of cancer, inflammation, auto-immune diseases, diabetes and diabetic complications, infection, cardiovascular disease and ischemia-reperfusion injuries.Type: ApplicationFiled: March 25, 2010Publication date: January 19, 2012Applicant: Profectus Biosciences, Inc.Inventors: Jie Zhang, Drago Robert Sliskovic, Charles E. Ducker
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Publication number: 20110319447Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.Type: ApplicationFiled: September 9, 2011Publication date: December 29, 2011Applicant: Synta Pharmaceuticals Corp.Inventors: Lijun Sun, Weiwen Ying, Junghyun Chae, Teresa Przewloka, Shijie Zhang, Dinesh U. Chimmanamada, Kevin Foley, Zhenjian Du, Hao Li, David James, Howard P. Ng, Zachary Demko, Dan Zhou, Shuzhen Qin
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Publication number: 20110305632Abstract: The present invention relates to a method of making asymmetrical bis(thiosemicarbazones), compounds useful as synthetic intermediates in the method, new bis(thiosemicarbazones) that can be readily accessed by use of the method and methods of treatment and imaging utilising some of the new bis(thiosemicarbazones).Type: ApplicationFiled: December 11, 2009Publication date: December 15, 2011Applicant: THE UNIVERSITY OF MELBOURNEInventors: Paul Stephen Donnelly, Brett Michael Paterson
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Publication number: 20110301347Abstract: The present invention relates to the compounds of formula I, processes for their production and their use as anti-inflammatory agents.Type: ApplicationFiled: August 15, 2011Publication date: December 8, 2011Inventors: Markus BERGER, Jan Dahmen, Hartmut Rehwinkel, Stefan Jaroch, Heike Schäcke
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Publication number: 20110294850Abstract: The present invention provides a novel indoline derivative or a pharmacologically acceptable salt thereof or a solvate of the derivative or a salt thereof represented by the following formula (1) that has an excellent butyrylcholinesterase inhibitory activity. In the formula, R1 represents an alkyl group, a cycloalkyl group, a heterocycloalkyl group, an aryl group, a heteroaryl group, an arylalkyl group, a heteroarylalkyl group, a cycloalkylalkyl group, a heterocycloalkylalkyl group, a dihydrofurylalkyl group, an alkenyl group, a tetrahydronaphthyl group, or an indanyl group; R2 represents a hydrogen atom, an alkyl group, an arylalkyl group, a cycloalkylalkyl group, a heteroarylalkyl group, a heterocycloalkylalkyl group, an aryl group, or an acyl group; R3 each independently represents a hydrogen atom, an alkyl group, or a dialkylaminocarbonyl group; R4 each independently represents a hydrogen atom or an alkyl group; and R5 represents a hydrogen atom or an alkyl group.Type: ApplicationFiled: February 3, 2010Publication date: December 1, 2011Applicants: TOKYO INSTITUTE OF TECHNOLOGY, KYOTO UNIVERSITYInventors: Hachiro Sugimoto, Jun Takahashi, Takashi Takahashi, Ichiro Hijikuro
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Publication number: 20110288089Abstract: A compound of Formula (I): wherein A1, A2, A3, A4, A5, G1, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: January 13, 2010Publication date: November 24, 2011Applicant: SYNGENTA CROP PROTECTION LLCInventors: Peter Renold, Jerome Yves Cassayre, Jagadish Pabba, Myriem El Qacemi, Thomas Pitterna
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Patent number: 8063046Abstract: Compounds having high angiogenesis inhibiting activity useful as agents for effective treatment and prevention of diseases involving pathologic angiogenesis, e.g.Type: GrantFiled: March 23, 2010Date of Patent: November 22, 2011Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Hiroshi Koyano, Atsushi Suda, Kousuke Aso, Kihito Hada, Miyuki Asai, Masami Hasegawa, Yasuko Sato
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Patent number: 8063049Abstract: This invention concerns to N-(2-aylamino)aryl sulfonamides, which are inhibitors of MEK, methods of using such compounds in the treatment of hyperproliferative diseases, and to pharmaceutical compositions containing such compounds.Type: GrantFiled: September 10, 2010Date of Patent: November 22, 2011Assignee: Ardea Biosciences, Inc.Inventors: Yung-hyo Koh, Zhi Hong, Jean-Michel Vernier, Andreas Maderna
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Publication number: 20110281908Abstract: Novel classes of molecular chaperone Heat shock protein 90 (Hsp90) inhibitors and methods for making these classes are provided herein. These compounds are useful in treating and preventing cancer and other Hsp90-related diseases, such as inflammation and neurodegenerative disorders. Also provided herein are methods of treating and preventing cancer and other Hsp90 related disease. The methods include administering to a subject a therapeutically effective amount of an Hsp90 inhibitor.Type: ApplicationFiled: October 6, 2009Publication date: November 17, 2011Applicant: EMORY UNIVERSITYInventors: Aiming Sun, Ganesh Thota, Jaeki Min, Pahk Thepchatri, Yuhong Du, James P Snyder, Dennis C. Liotta
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Patent number: 8058441Abstract: The present invention relates to tetrahydroquinoline derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 is formyl, (1-6C)alkylcarbonyl or (1-6C)alkylsulfonyl; R2 and R3 are H or (1-4C)alkyl; R4 is phenyl; R5 is (1-4C)alkyl; Y—X is (CO)—O, (SO)2—O, NHC(O)—O, NHC(S)—O, OC(O)—O, bond-O, C(O)—NH, S(O)2—NH, NHC(O)—NH, NHC(S)—NH, OC(O)—NH, bond-NH, NH—C(O), O—C(O), NH—S(O)2, or O—S(O)2 or Y—X is a bond; R6 is H, trifluormethyl, (1-6C)alkyl, 1- or 2-adamantyl(1-4C)alkyl, (2-6C)alkenyl, (3-9C)heteroaryl, (3-6C)cycloalkyl, (2-6C)heterocycloalkyl, (1-4C)alkylthio(1-4C)alkyl, (6-10C)aryl(1-4C)alkyl, (3-9C)heteroaryl(1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl(1-4C)alkyl, R8,R9-aminocarbonyl(1-4C)alkyl, R8,R9-amino(1-4C)alkyl, R8-oxycarbonyl(1-4C)alkyl, R8-oxy(1-4C)alkyl, R8-carbonyl(1-4C)alkyl or (6-10C)aryl; R7 is H, (1-4C)alkyl, (1-4C)alkoxy, halogen, trifluoromethyl, cyano, nitro hydroxyl; and R8 and/or R9 is H, (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyType: GrantFiled: June 25, 2002Date of Patent: November 15, 2011Assignee: N.V. OrganonInventors: Nicole Corine Renée Van Straten, Rudolf Gijsbertus Van Someren, Jurgen Schulz
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Publication number: 20110269761Abstract: The invention relates to substituted aryl-sulphonylglycine derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as in the specification and claims, which are suitable for preparing a pharmaceutical composition for the treatment of metabolic disorders, particularly type 1 or type 2 diabetes mellitus.Type: ApplicationFiled: April 17, 2009Publication date: November 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Elke Langkopf, Frank Himmelsbach, Juergen Mack, Alexander Pautsch, Corinna Schoelch, Annette Schuler-Metz, Ruediger Streicher, Holger Wagner
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Publication number: 20110263861Abstract: Provided is a solid luminescent quinoline compound capable of emitting light in a crystalline state, capable of changing the luminescent color not requiring modification of molecular configuration and capable of emitting light in response to external pressure such as heat, physical pressure, etc. The quinoline compound is represented by the following general formula (1): wherein R1 may be the same or different, each representing any of CF3 or CF3CF2; R2 represents any of an amino group, an N,N-dimethylamino group, an N-phenylamino group, a carbazole group, an N-methylamino group or an N-methyl-N-phenylamino group.Type: ApplicationFiled: November 19, 2010Publication date: October 27, 2011Applicant: KYUSHU UNIVERSITY, NATIONAL UNIVERSITY CORPORATIONInventors: Noboru Koga, Satoru Karasawa, Yuichiro Abe
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Publication number: 20110224253Abstract: The present invention provides tetrahydropyrvinium (THP), derivatives thereof, benzoxazole compounds, and derivatives thereof. The present invention provides a method of using tetrahydropyrvinium (THP), derivatives thereof, benzoxazole compounds, and derivatives thereof.Type: ApplicationFiled: April 24, 2009Publication date: September 15, 2011Applicant: The Regents of the University of CaliforniaInventors: Marc Diamond, Jeremy Jones, Adam Renslo
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Publication number: 20110212994Abstract: Small molecule choline kinase inhibitors, pharmaceutical compositions thereof, and screening methods for identifying and evaluating choline kinase inhibitors are provided. Safe and effective methods for treating subjects suffering from a disorder or disease characterized by neoplastic cell proliferation employing the choline kinase inhibitors are also provided.Type: ApplicationFiled: June 28, 2010Publication date: September 1, 2011Inventors: BRIAN CLEM, SUCHETA TELANG, JOHN TRENT, JASON CHESNEY, POORAN CHAND, GILLES TAPOLSKY
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Patent number: 8008324Abstract: The invention relates to novel indole derivatives of the general formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.Type: GrantFiled: March 6, 2008Date of Patent: August 30, 2011Assignee: AEterna Zentaris GmbHInventors: Peter Emig, Gerald Bacher, Dietmar Reichert, Silke Basner, Beate Aue, Bernd Nickel, Eckhard Gunther
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Publication number: 20110190299Abstract: An object of the present invention is to provide thiazolidinone derivatives. More specifically, an object of the present invention is to provide novel compounds having a CDC7 inhibitory action. The present invention provides thiazolidinone derivatives represented by the formula (I) The compounds of the present invention inhibit the CDC7 protein kinase activity, and suppress cell proliferation.Type: ApplicationFiled: April 19, 2010Publication date: August 4, 2011Applicants: SBI BIOTECH CO., LTD., CRYSTALGENOMICS, INC.Inventors: Takayuki Irie, Masaaki Sawa, Sayuri Ito, Chika Tanaka, Seong Gu Ro, Choul Hong Park
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Publication number: 20110186831Abstract: An aromatic amine derivative represented by the following formula (1):Type: ApplicationFiled: August 12, 2009Publication date: August 4, 2011Applicant: IDEMITSU KOSAN CO., LTD.Inventor: Yumiko Mizuki
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Patent number: 7989453Abstract: The invention relates to novel indole derivatives of the general formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.Type: GrantFiled: December 20, 2007Date of Patent: August 2, 2011Assignee: AEterna Zentaris GmbHInventors: Peter Emig, Gerald Bacher, Dietmar Reichert, Silke Basner, Beate Aue, Bernd Nickel, Eckhard Gunther
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Publication number: 20110172236Abstract: A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.Type: ApplicationFiled: September 21, 2009Publication date: July 14, 2011Inventors: Prasun K. Chakravarty, Joseph L. Duffy, Pengcheng Patric Shao
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Publication number: 20110172212Abstract: Novel amine compounds which are represented by the following formula (1) and efficacious against diseases such as a viral infectious disease with HIV, rheumatism, and cancer metastasis; typically, A1 and A2 represent a hydrogen atom or a substitutable monocyclic or polycyclic heteroaromatic ring and W represents a substitutable benzene ring or any group represented by the following formula (10) or (11): where X represents O, CH2, C(?O), NR11, or CHR35 and D represents a group represented by the following formula (6): [Formula 4] -Q-Y—B??(6) where Q represents a single bond, NR12, or a group represented by the formula (13): and Y represents a group represented by the following formula (7): [Formula 6] —(CR18R19)m3- or —(CR20R21)m4-z-(CR22R23)m5-??(7) where z represents a substitutable monocyclic or polycyclic aromatic ring; and B represents —NR25R26; and R1 to R26 in the above formulae represent a hydrogen atom, an alkyl group, an alkenyl group, or an alkynyl group.Type: ApplicationFiled: March 18, 2011Publication date: July 14, 2011Applicant: KUREHA CORPORATIONInventors: Atsushi SAITOU, Shigeyuki Kikumoto, Masahiro Ono, Ryo Matsui, Masashi Yamamoto, Tomohiro Sawa, Shigeru Suzuki, Mikiro Yanaka
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Patent number: 7967872Abstract: The present invention relates to thiol/disulphide azo quinolinium compounds for dyeing keratin fibres. The invention relates to a dye composition comprising a particular thiol/disulphide azo quinolinium chromophore-containing thiol or disulphide dye, and to a process for dyeing keratin fibres such as the hair, using said composition. It similarly relates to novel particular thiol/disulphide azo quinolinium chromophore-containing dyes and to the uses thereof in dyeing keratin fibres. The dyeing process according to the invention makes it possible to dye keratin fibres without damaging them, in a manner which is particularly persistent with respect to shampooing operations and common attacks. Moreover, the novel dyes according to the invention extend the colour range to violets and blues. This process also makes it possible to dye bleached keratin fibres in a strong and chromatic manner.Type: GrantFiled: September 8, 2008Date of Patent: June 28, 2011Assignee: L'Oreal S.A.Inventors: Nicolas Daubresse, Andrew Greaves
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Patent number: 7964729Abstract: Peptidyl sensors comprise a metal-binding peptide and one or two kinase recognition sequences with a hydroxyamino acid that can be phosphorylated in the presence of a kinase.Type: GrantFiled: August 28, 2006Date of Patent: June 21, 2011Assignee: Massachusetts Institute of TechnologyInventors: Barbara Imperiali, Elvedin Lukovic, Dora Carrico-Moniz
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Publication number: 20110136813Abstract: The present invention generally relates to protein signalling. In particular, compounds that inhibit the Wnt protein signalling pathway are disclosed. Such compounds may be used in the treatment of Wnt protein signalling-related diseases and conditions such as cancer, degenerative diseases, type II diabetes and osteopetrosis.Type: ApplicationFiled: May 27, 2009Publication date: June 9, 2011Inventors: Lawrence Lum, Michael G. Roth, Baozhi Chen, Chuo Chen, Michael E. Dodge, Wei Tang
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Publication number: 20110137038Abstract: A process for producing one selected stereoisomer of a substituted alcohol comprises reacting a stereoisomeric epoxide with an amine, a carboxylic acid, an amide, a sulfonyl, or a cyanide. The process avoids the production of a racemic mixture of stereoisomers of the prior art. Such a stereoisomeric substituted alcohol can be used for anti-inflammatory therapy.Type: ApplicationFiled: February 17, 2011Publication date: June 9, 2011Inventor: Arthur E. Harms
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Publication number: 20110118234Abstract: The present invention provides compounds Formula (I) that are gamma secretase modulators and are therefore useful for the treatment of diseases treatable by modulation of gamma secretase such as Alzheimer's disease. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.Type: ApplicationFiled: May 4, 2009Publication date: May 19, 2011Inventors: Kaustav Biswas, Jian J. Chen, James R. Falsey, Vijay Keshav Gore, Qingyian Liu, Vu Van Ma, Stephanie J. Mercede, Robert M. Rzasa, Christopher M. Tegley, Jiawang Zhu
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Publication number: 20110112071Abstract: A compound represented by formula (I?): (wherein m, n, and p each represent 0 to 2; q represents 0 or 1; R1 represents halogen, a hydrocarbon group, a heterocyclic group, an alkoxy group, an alkoxycarbonyl group, a sulfamoyl group, a CN group, an NO2 group, or the like; R2 represents halogen, amino, a hydrocarbon group, an aromatic heterocyclic group, or an oxo group; X1 represents O, —NR3—, or —S(O)r-; X2 represents a methylene group, O, —NR3—, or —S(O)r-; Q? represents a heteroaryl group, a heteroarylalkyl group, a substituted aryl group, or an aralkyl group; Cycle moiety represents an aryl ring or a heteroaryl ring; and the wavy line represents an E-isomer or a Z-isomer), a salt of the compound, or a solvate of the compound or the salt. A pharmaceutical composition and a transient receptor potential type I (TRPV1) receptor antagonist each contain, as an active ingredient, at least one of the compound, a salt of the compound, and a solvate of the compound or the salt.Type: ApplicationFiled: January 18, 2011Publication date: May 12, 2011Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventors: Hideharu UCHIDA, Naoto Kosuga, Tsutomu Satoh, Daido Hotta, Tomoyuki Kamino, Yoshitaka Maeda, Ken-ichi Amano, Yasushige Akada
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Patent number: RE42376Abstract: This invention provides compounds of formula I having the structure wherein G1, G2, R1, R4, Z, n, and X are defined in the specification or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.Type: GrantFiled: May 21, 2010Date of Patent: May 17, 2011Assignee: Wyeth Holdings CorporationInventors: Allan Wissner, Hwei-Ru Tsou, Dan M. Berger, Middleton B. Floyd, Jr., Philip R. Hamann, Nan Zhang, Philip Frost