Phthalazines (including Hydrogenated) Patents (Class 544/237)
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Publication number: 20130131068Abstract: A phthalazinone ketone derivative as represented by formula (I), a preparation method thereof, a pharmaceutical composition containing the derivative, a use thereof as a poly (ADP-ribose) polymerase (PARP) inhibitor, and a cancer treatment method thereof are described.Type: ApplicationFiled: July 26, 2011Publication date: May 23, 2013Applicant: JIANGSU HANSOH PHARMACEUTICAL CO., LTD.Inventors: Peng Cho Tang, Xin Li, Xiangqin Li, Yang Chen, Bin Wang, Zhe Zhu
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Publication number: 20130123266Abstract: A benzene sulphonamide compound of formula I or one of its addition salts with pharmaceutically acceptable acids, for its use in a method for treating a pathology linked to an excessive effect of TNF-alpha and for its use in a method for treating the human or animal body as a direct inhibitor of TNF-alpha.Type: ApplicationFiled: July 19, 2011Publication date: May 16, 2013Applicant: VAX-CONSULTINGInventors: Jean-François Zagury, Matthieu Montes, Hadley Mouhsine, Hélène Guillemain
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Publication number: 20130123253Abstract: Disclosed are agents having pharmacological activity against cellular receptors and intracellular signaling, particularly receptors and signaling pathways of central nervous system (CNS) neurotransmitters. Also disclosed are related methods and compositions for the treatment or prevention of diseases or disorders using the agents.Type: ApplicationFiled: May 1, 2012Publication date: May 16, 2013Applicant: HUMAN BIOMOLECULAR RESEARCH INSTITUTEInventor: John CASHMAN
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Publication number: 20130116246Abstract: 8-Fluorophthalazin-1(2h)-one compounds of Formula II where one or two of X1, X2, and X3 are N, are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula II for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: November 2, 2012Publication date: May 9, 2013Applicant: GENENTECH, INC.Inventor: Genentech, Inc.
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Publication number: 20130116233Abstract: The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.Type: ApplicationFiled: October 29, 2012Publication date: May 9, 2013Applicants: AbbVie Inc., Abbott GmbH & Co. KGInventors: Abbott GmbH & Co. KG, AbbVie Inc.
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Publication number: 20130116229Abstract: The present invention relates to compounds which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.Type: ApplicationFiled: November 8, 2012Publication date: May 9, 2013Applicants: AbbVie Inc., Abbott GmbH & Co. KGInventors: Abbott GmbH & Co.KG, AbbVie Inc.
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Publication number: 20130102576Abstract: Compounds, pyridine N-oxides, and pharmaceutically acceptable salts of formula (I) are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and for preventing and/or treating diseases of the respiratory tract characterized by airway obstruction, such as asthma or COPD.Type: ApplicationFiled: October 19, 2012Publication date: April 25, 2013Applicant: Chiesi Farmaceutici S.p.A.Inventor: Chiesi Farmaceutici S.p.A.
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Patent number: 8420651Abstract: The subject of the present invention is compounds corresponding to the formula (I) in which: X represents a divalent (C2-C5)alkylene radical which is unsubstituted or substituted one or more times by an Alk group; R1 represents a phenyl, a naphthyl, a pyridyl, a 1-benzothienyl or a 1,3-benzodioxolyl; R2 represents a hydrogen atom, a halogen atom, an Alk group, an OAlk group or else a group chosen from —S-Alk, —SO-Alk, —SO2-Alk, —CO—N(R4)-Alk, —N(R4)SO2-Alk, —N(R4)CO-Alk, —N(R4)SO2—N(Alk)2; R3 represents a hydrogen atom, a halogen atom, an Alk group or an OAlk group; R4 represents a hydrogen atom or a (C1-C4)alkyl; Alk represents an unsubstituted or substituted (C1-C4)alkyl. Preparation process and therapeutic application.Type: GrantFiled: April 6, 2010Date of Patent: April 16, 2013Assignee: SanofiInventors: Elodie Barbagallo, Carole Legeay, Murielle Rinaldi-Carmona, Pascale Roux, Claude Vernhet
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Substituted 1-benzyl-cinnolin-4(1)-one derivatives, preparation thereof, and therapeutic use thereof
Patent number: 8410099Abstract: The present invention is related to novel substituted 1-benzylcinnolin-4(1H)-one derivatives having affinity for cannabinoid CB2 receptors, their preparation and their therapeutic application.Type: GrantFiled: January 10, 2011Date of Patent: April 2, 2013Assignee: SanofiInventors: Claude Vernhet, Elodie Barbagallo, Murielle Rinaldi-Carmona, Pascale Roux -
Patent number: 8404687Abstract: The present invention provides novel 1,4-disubstituted phthalazine hedgehog pathway antagonists useful in the treatment of cancer.Type: GrantFiled: October 22, 2009Date of Patent: March 26, 2013Assignee: Eli Lilly and CompanyInventors: Jolie Anne Bastian, Philip Arthur Hipskind, Daniel Jon Sall, Takako Wilson (nee Takakuwa)
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Patent number: 8399480Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: GrantFiled: April 2, 2009Date of Patent: March 19, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Cheng Zhu
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Patent number: 8383623Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, Y, Z, n, and m are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as Cdc7 and methods of treating diseases such as cancer.Type: GrantFiled: April 14, 2011Date of Patent: February 26, 2013Assignee: Abbott LaboratoriesInventors: Gui-Dong Zhu, Virajkumar B. Gandhi, Alexander R. Shoemaker, Thomas D. Penning, Jianchun Gong
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Publication number: 20130045965Abstract: This application discloses compounds according to generic Formula I: wherein the variables are defined as described herein, and which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.Type: ApplicationFiled: August 16, 2012Publication date: February 21, 2013Inventors: Christine E. Brotherton-Pleiss, Saul Jaime-Figueroa, Francisco Javier Lopez-Tapia, Yan Lou, Timothy D. Owens
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Publication number: 20130029995Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).Type: ApplicationFiled: July 25, 2012Publication date: January 31, 2013Applicant: Gruenenthal GmbHInventors: Robert FRANK, Thomas CHRISTOPH, Bernhard LESCH, Jeewoo LEE
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Publication number: 20130018046Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: September 13, 2012Publication date: January 17, 2013Applicant: ARIAD Pharmaceuticals, Inc.Inventors: Yihan Wang, Xiaotian Zhu, Rajeswari Sundaramoorthi, Wei-Sheng Huang, Dong Zou, R. Mathew Thomas, Jiwei Qi, Jan Antoinette C. Romero, David C. Dalgarno, William C. Shakespeare, Tomi K. Sawyer, Chester A. Metcalf, III
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Patent number: 8349836Abstract: The present invention relates to novel phthalazine derivatives and, more particularly, to phthalazine derivatives that are useful as protein kinase inhibitors. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: GrantFiled: June 1, 2011Date of Patent: January 8, 2013Inventors: Gian-Luca Araldi, Matthew Ronsheim, Melanie Ronsheim
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Publication number: 20120329649Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.Type: ApplicationFiled: June 21, 2012Publication date: December 27, 2012Inventors: James E. Hunter, William C. Lo, Gerald B. Watson, Akshay Patny, Gary D. Gustafson, Dan Pernich, William K. Brewster, Debra L. Camper, Beth Lorsbach, Michael R. Loso, Thomas C. Sparks, Hemant Joshi, Adiraj Mandaleswaran, Ramadevi Sanam, Rambabu Gundla, Pravin S. Iyer
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Publication number: 20120329801Abstract: The invention relates to the provision of two novel crystalline forms I and II for 5-amino-2,3-dihydrophthalazine-1,4-dione sodium salt. Surprisingly, it was discovered that form I and form II have differing immunological effects. This advantageous property is useful for immunospecific applications. In addition, both forms have advantageous physicochemical properties, which are useful in the production, further processing and/or use of a pharmaceutical preparation of form I or form II or a mixture of both.Type: ApplicationFiled: March 1, 2011Publication date: December 27, 2012Applicant: Metriopharm AGInventors: Josef Breu, Wolfgang Brysch, Astrid Kaiser, Beate Ludescher, Gerrit Maass, Thomas Martin, Wolfgang Milius, Michael Niedermaier
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Patent number: 8338591Abstract: The present invention provides compounds of Formula (I) or (II) salt form or prodrug thereof, wherein variables are defined herein, that are modulators of metalloproteases such as matrix metalloproteases (MMPs) and ADAMs. The compounds or compositions described herein can be used to treat diseases associated with metalloprotease activity including, for example, arthritis, cancer, cardiovascular disorders, skin disorders, inflammation or allergic conditions.Type: GrantFiled: May 6, 2005Date of Patent: December 25, 2012Assignee: Novartis International Pharmaceutical Ltd.Inventors: Taeyoung Yoon, Jun Yuan, Kyungae Lee, George D. Maynard, Nian Liu
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Patent number: 8334316Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.Type: GrantFiled: February 9, 2009Date of Patent: December 18, 2012Assignee: ACEA Biosciences, Inc.Inventors: Xiao Xu, Haoyun An, Xiaobo Wang
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Publication number: 20120316337Abstract: Method for preparing carboxylic acid derivatives by aromatic nucleophilic substitution, in which a carboxylic acid derivative having a single carboxyl functional group, or one of the salts thereof, the carboxylic acid derivative having, in the ortho position of the carboxyl functional group, a leaving group, which is preferably an atom of fluorine or of chlorine or an alkoxy group, chiral or not, preferably a methoxy group, the carboxylic acid derivative not being substituted by an electro attractive group other than the leaving group if any; is reacted with a reactant MNu, where M is a metal and Nu is a nucleophile, chiral or not, the aromatic nucleophilic substitution reaction being carried out without a catalyst and without a step of protecting/deprotecting the acid functional group of the starting compound.Type: ApplicationFiled: February 17, 2011Publication date: December 13, 2012Applicants: UNIVERSITE DU MAINE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Jacques Mortier, Anne-Sophie Castanet, Mickael Belaud-Rotureau
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Patent number: 8324211Abstract: This application discloses 6-Phenyl-imidazo[1,2-a]pyridine and 6-Phenyl-imidazo[1,2-b]pyridazine derivatives according to generic Formulae I-V: wherein, variables Q, R, X, Y1, Y2, Y3, Y4, n, and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.Type: GrantFiled: July 15, 2009Date of Patent: December 4, 2012Assignee: Roche Palo Alto LLCInventors: Nolan James Dewdney, Yan Lou, Eric Brian Sjogren, Michael Soth
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Publication number: 20120295885Abstract: This application discloses compounds according to generic Formula I: wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.Type: ApplicationFiled: May 16, 2012Publication date: November 22, 2012Inventors: Roland Joseph Billedeau, Rama K. Kondru, Francisco Javier Lopez-Tapia, Yan Lou, Timothy D. Owens, Yimin Qian, Sung-Sau So, Kshitij C. Thakkar, Jutta Wanner
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Publication number: 20120289500Abstract: Disclosed herein are KCNQ potassium channels modulators of formula (I) wherein ring G1, R1, and R2 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.Type: ApplicationFiled: May 8, 2012Publication date: November 15, 2012Applicant: ABBOTT LABORATORIESInventors: Brian S. Brown, Tongmei Li, Sridhar Peddi, Arturo Perez-Medrano, David DeGoey
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Patent number: 8309543Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: May 23, 2012Date of Patent: November 13, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jesus E. Gonzalez, III, Andreas P. Termin, Esther Martinborough, Nicole Hilgraf
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Patent number: 8299077Abstract: This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-Phenyl-1H-pyrazin-2-one derivatives according to generic Formula I-III: wherein, variables Q, R, X, X?, Y1, Y2, Y2?, Y3, Y4, Y5, m, and n are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I-III and at least one carrier, diluent or excipient.Type: GrantFiled: February 24, 2010Date of Patent: October 30, 2012Assignee: Roche Palo Alto LLCInventors: Steven Berthel, Fariborz Firooznia, Daniel Fishlock, Jun-Bae Hong, Yan Lou, Matthew Lucas, Timothy D. Owens, Keshab Sarma, Zachary Kevin Sweeney, Joshua Paul Gergely Taygerly
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Publication number: 20120269894Abstract: The present invention relates to ophthalmic depot formulations comprising an active agent, e.g. embedded in a pharmacologically acceptable biocompatible polymer or a lipid encapsulating agent, e.g. for periocular or subconjunctival administration.Type: ApplicationFiled: June 14, 2012Publication date: October 25, 2012Inventors: Marklus AHLHEIM, Michael AUSBORN, David BODMER, Christian SCHOCH
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Publication number: 20120264760Abstract: One aspect of the present invention relates to compounds, and pharmaceutically acceptable salts and prodrugs thereof, that are useful as inhibitors of IMPDH. The invention also provides pharmaceutical compositions comprising the compounds of the invention which selectively inhibit parasitic IMPDH. In certain embodiments, the present invention relates to selective inhibition of C. parvum inosine-5?-monophosphate-dehydrogenase over human inosine-5?-monophosphate-dehydrogenase (IMPDH type I and type II). These compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.Type: ApplicationFiled: June 6, 2012Publication date: October 18, 2012Applicants: University of Georgia Research Foundation, Inc., Brandeis UniversityInventors: Lizbeth K. Hedstrom, Boris Striepen
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Publication number: 20120258963Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: ApplicationFiled: June 20, 2012Publication date: October 11, 2012Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Cheng Zhu
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Patent number: 8273742Abstract: The present invention provides novel 1,4-disubstituted phthalazine hedgehog pathway antagonists useful in the treatment of cancer.Type: GrantFiled: June 15, 2010Date of Patent: September 25, 2012Assignee: Eli Lilly and CompanyInventors: Philip Arthur Hipskind, Bharvin Kumar Patel, Takako Wilson (nee Takakuwa)
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Patent number: 8268825Abstract: A method of treating an anthrax infection wherein a compound of formula I wherein R1 and R2 represent, independently of one another unsubstituted or specifically substituted C1-4alkoxy; and R3 represents hydrogen; cyano; unsubstituted or specifically substituted C1-6alkyl; C3-6cycloalkyl; C2-6alkenyl; C7-18bicyclyl; aryl, aryl-C1-4alkyl, aryl-Q-C1-4alkyl heteroaryl, heterocyclyl or heterocyclyl-C1-6alkyl, wherein aryl denotes a mono- or poly-nucleous group with 6 to 14 ring carbon atoms; heterocyclyl denotes a 4- to 6-membered non-aromatic heterocyclic group comprising 1 to 3, nitrogen, oxygen and/or sulfur atoms; heteroaryl denotes a mono- or polynuclear heteroaromatic group consisting 5- and/or 6-membered rings and comprising 5 to 13 carbon atoms and 1 to 4, nitrogen, oxygen and/or sulfur atoms; and Q means —SO— or —SO2—; or a pharmaceutically acceptable salt, solvate or hydrate or a prodrug thereof; is administered to said subject in a quantity effective to inhibit, suppress, or expel an anthrax infType: GrantFiled: September 25, 2006Date of Patent: September 18, 2012Assignee: The Board of Regents for Oklahoma State UniversityInventors: Jurg Dreier, William Barrow, Esther Barrow
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Patent number: 8258134Abstract: 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: September 4, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Steven Joseph Berthel, Nancy-Ellen Haynes, Robert Francis Kester, Lee Apostle McDermott, Yimin Qian, Ramakanth Sarabu, Nathan Robert Scott, Jefferson Wright Tilley
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Patent number: 8247415Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: GrantFiled: April 2, 2009Date of Patent: August 21, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Cheng Zhu
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Patent number: 8247416Abstract: 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one as crystalline Form A.Type: GrantFiled: July 10, 2009Date of Patent: August 21, 2012Assignee: Kudos Pharmaceuticals LimitedInventors: Keith Allan Menear, Anthony Peter Ottridge, Derek John Londesbrough, Michael Raymond Hallett, Keith Raymond Mulholland, John David Pittam, David Dermot Patrick Laffan, Ian Woodward Ashworth, Martin Francis Jones, Janette Helen Cherryman
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Publication number: 20120208820Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: ApplicationFiled: January 31, 2012Publication date: August 16, 2012Inventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
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Patent number: 8207168Abstract: The present invention is directed to novel pyridazinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition disorders.Type: GrantFiled: June 15, 2010Date of Patent: June 26, 2012Assignee: Cephalon, Inc.Inventors: Nadine C. Becknell, Derek Dunn, Robert L. Hudkins, Kurt A. Josef, Lars J. S. Knutsen, Ming Tao, Allison L. Zulli
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Publication number: 20120156213Abstract: The present application relates to a method for treating or preventing Th17 inflammatory disease mediated with IL-6 or IL-17 by administration of medication which inhibits vascular endothelial growth factor receptors, and a pharmaceutical composition therefor.Type: ApplicationFiled: May 20, 2010Publication date: June 21, 2012Applicant: POSTECH ACADEMY-INDUSTRY FOUNDATIONInventors: Yoon Keun Kim, Yong Song Gho, Yu Sun Kim
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Publication number: 20120157403Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein E, A, G M, Het, B, X, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.Type: ApplicationFiled: February 24, 2012Publication date: June 21, 2012Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yuguang Wang, Yan Xia
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Patent number: 8202861Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: August 9, 2004Date of Patent: June 19, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jesus E Gonzales, III, Andreas P Termin, Esther Martinborough, Nicole Zimmerman
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Publication number: 20120142915Abstract: This disclosure concerns a protected cyclopropylboronic acid comprising a substituted cyclopropyl group and a boronic ester group having a protecting group. The protecting group is an N-methyliminodiacetic acid (MIDA) group or MIDA-based group.Type: ApplicationFiled: December 1, 2011Publication date: June 7, 2012Inventors: Matthew Duncton, Rajinder Singh
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Publication number: 20120129863Abstract: Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving chymase. Also disclosed are pharmaceutical compositions, methods of using and making the same.Type: ApplicationFiled: August 5, 2009Publication date: May 24, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha Abeywardane, Ming-Hong Hao, Steven John Taylor
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Publication number: 20120122847Abstract: The present invention relates to chemical compounds having a general formula I wherein A1-8, D?, L1, L2, R1, R6-8 and n are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.Type: ApplicationFiled: June 9, 2011Publication date: May 17, 2012Applicant: Amgen Inc.Inventors: Victor Cee, Holly Deak, Bingfan Du, Stephanie Geuns-Meyer, Zihao Hua, Matthew Martin, Issac Marx, Hanh Nho Nguyen, Philip Olivieri, Kathleen Panter, Karina Romero, Laurie Schenkel, Ryan White
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Publication number: 20120122136Abstract: Provided is a compound comprising the structure: (SIG)-(SI-MOD)m. In this compound, SIG is a signaling molecule, SI is a self-immolative structure bound to SIG such that SIG has a reduced signal relative to the signal of SIG without SI, MOD is a moiety bound to SI that is subject to modification by an activator, and m is an integer from 1 to about 10. With this compound, when MOD is modified by an activator, SI is destabilized and self-cleaved from SIG such that SIG generates an increased signal. Also provided is a method of determining whether a sample comprises an activator, using the above-described compound. Additionally provided is a method of determining whether a cell comprises a nitroreductase using the above-described compound where nitroreductase is the activator. Further provided is a method of determining whether a mammalian cell is hypoxic using the above-described compound where nitroreductase is the activator.Type: ApplicationFiled: November 16, 2010Publication date: May 17, 2012Applicant: ENZO LIFE SCIENCES, INC., C/O ENZO BIOCHEM, INC.Inventors: Maciej Szczepanik, Irina V. Lebedeva, Yuejun Xiang, Praveen Pande, Wayne Forrest Patton
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Patent number: 8168635Abstract: Disclosed are agents having pharmacological activity against cellular receptors and intracellular signaling, particularly receptors and signaling pathways of central nervous system (CNS) neurotransmitters. Also disclosed are related methods and compositions for the treatment or prevention of diseases or disorders using the agents.Type: GrantFiled: June 20, 2005Date of Patent: May 1, 2012Assignee: Human BioMolecular Research InstituteInventor: John Cashman
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Publication number: 20120101272Abstract: The present invention relates to a process for preparation of erlotinib of Formula I or its pharmaceutically acceptable salt thereof. The present invention also relates to process for the preparation of erlotinib trifluoroacetate. The present invention also relates to a nove-ICrystalline form of erlotinib trifluoroacetate designated as Form E and process for its preparation. The present invention further relates to process for the preparation of erlotinib hydrochloride from erlotinib trifluoroacetate.Type: ApplicationFiled: March 26, 2010Publication date: April 26, 2012Applicant: RANBAXY LABORATORIES LIMITEDInventors: Balaguru Murugesan, Anandam Vempali, Swargam Sathyanarayana, Rajesh Kumar Thaper, Mohan Prasad
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Publication number: 20120094971Abstract: This invention relates to compounds of Formula (I) wherein Cy1, L1, Y, R1, L2, and Ar2 are defined herein, for the treatment of cancers, inflammatory disorders, and neurological conditions.Type: ApplicationFiled: September 3, 2009Publication date: April 19, 2012Applicant: REPLIGEN CORPORATIONInventors: James R. Rusche, Norton P. Peet, Allen T. Hopper
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Publication number: 20120094983Abstract: A compound of formula I wherein R1, R2, R3, R4 and R5 are described herein.Type: ApplicationFiled: March 15, 2011Publication date: April 19, 2012Inventors: James A. Johnson, Yoon Jeon, John Lloyd, Heather Finlay
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Publication number: 20120094998Abstract: The invention relates to (among other things) oligomer-PTK inhibitor conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over PTK inhibitor compounds lacking a water soluble, non peptidic oligomer.Type: ApplicationFiled: April 19, 2010Publication date: April 19, 2012Applicant: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Wen Zhang
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Patent number: 8153633Abstract: The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders such as cancer.Type: GrantFiled: June 23, 2008Date of Patent: April 10, 2012Assignee: Amgen Inc.Inventors: Richard J. Austin, Jacob Kaizerman, Brian Lucas, Dustin L. McMinn, Jay Powers
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Patent number: 8148173Abstract: Disclosed are compounds having the formula: wherein R1 is selected from the group consisting of hydrogen, C1-C6 alkyl, amino, N—C1-C6-alkylamino, and N,N—C1-C6-dialkylamino; and ring “A” is selected from the group consisting of unsubstituted or substituted C4-C8-cycloalkenyl, unsubstituted or substituted bicyclo[2,2,1]alkenyl, and unsubstituted or substituted bicyclo[2,2,2]alkenyl, unsubstituted phenyl, and phenyl substituted with a moiety selected from the group consisting of C3-C6-alkenyl, acryl, acryl-C1-C6 alkyl, acrylamido, and acrylamido-C1-C6 alkyl; polymers made from these compounds, and ELISAs that use the compounds and polymers as a chemiluminescent detection label.Type: GrantFiled: March 24, 2008Date of Patent: April 3, 2012Assignee: University of St. ThomasInventors: Joseph Thomas Ippoliti, Joshua Cole Speros