Polycyclo Ring System Having A 1,2- Or 1,4-diazine As One Of The Cyclos Patents (Class 514/248)
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Publication number: 20130178460Abstract: The present invention relates to the use of novel compounds of Formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.Type: ApplicationFiled: January 10, 2013Publication date: July 11, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Patent number: 8481540Abstract: This application discloses 6-(2-Hydroxymethyl-phenyl)-2-methyl-2H-pyridazin-3-one derivatives according to generic Formula I: wherein, variables X, R, and Y4, 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: GrantFiled: August 11, 2011Date of Patent: July 9, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Steven Joseph Berthel, Roland Joseph Billedeau, Christine E. Brotherton-Pleiss, Fariborz Firooznia, Stephen Deems Gabriel, Xiaochun Han, Ramona Hilgenkamp, Saul Jaime-Figueroa, Buelent Kocer, Francisco Javier Lopez-Tapia, Yan Lou, Lucja Orzechowski, Timothy D. Owens, Jenny Tan, Peter Michael Wovkulich
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Patent number: 8481538Abstract: The present invention provides compounds useful as inhibitors of c-Met tyrosine kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various proliferative disorders.Type: GrantFiled: September 18, 2007Date of Patent: July 9, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Alexander Aronov, Jon Come, John Court, David Deininger, David Lauffer, Pan Li, Kira McGinty, Suganthini Nanthakumar, Dean Stamos, Kirk Tanner
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Patent number: 8481539Abstract: The invention relates to alkynylaryl compounds according to the general formula (I) in which A, B, D, E, Ra, R1, R3, R4, R5 and q are as defined in the claims, and salts, N-oxides, solvates and prodrugs thereof, to pharmaceutical compositions comprising said alkynylaryl compounds, to methods of preparing said alkynylaryl compounds, to intermediate compounds useful in said methods, to uses of said intermediate compounds in the preparation of said alkynylaryl compounds, as well as to uses of said alkynylaryl compounds for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth.Type: GrantFiled: December 4, 2008Date of Patent: July 9, 2013Assignee: Bayer Intellectual Property GmbHInventors: Ingo Hartung, Hans Briem, Georg Kettschau, Karl-Heinz Thierauch, Ulf Bömer
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Publication number: 20130172323Abstract: The present invention relates to pyridazinone derivatives of general formula I, wherein the groups A, G and R1 are as defined in the application, the tautomers thereof, stereoisomers thereof, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: ApplicationFiled: May 6, 2011Publication date: July 4, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias Grauert, Remko Bakker, Steffen Breitfelder, Frank Buettner, Peter Eickelmann, Thomas Fox, Marc Grundl, Thorsten Lehmann-Lintz, Wolfgang Rist
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Publication number: 20130171102Abstract: The invention is related to anti-viral compounds of formula (A) as defined in the claims, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: May 20, 2011Publication date: July 4, 2013Applicant: Gilead Sciences, Inc.Inventors: Kyla Bjornson, Steven S. Bondy, You-chul Choi, Chien-Hung Chou, Ruchika Mishra, James D. Trenkle, Winston C. Tse, Randall W. Vivian, James G. Taylor
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Patent number: 8475842Abstract: The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1 -carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug.Type: GrantFiled: October 7, 2009Date of Patent: July 2, 2013Assignee: Astrazeneca ABInventors: Michael Karl Bechtold, Claudia Bettina Packhaeuser, Katja Maren Fastnacht, Bernd Harald Liepold, Benedikt Steitz, Julie Kay Cahill, Kieran James Lennon
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Publication number: 20130165446Abstract: The present invention addresses the problem of finding a compound having both PPAR activation activity and angiotensin receptor antagonistic activity. The present invention is a benzo- or pyrido-imidazole derivative represented by general formula (I), a pharmaceutically acceptable salt thereof, or a ester or amide thereof (where A is biphenyl methyl-imidazolyl, biphenyl methyl-benzimidazolyl, or the like, B is divalent benzimidazolyl or the like, C is carboxyl or the like, E is divalent phenyl, naphthyl, or the like, G is a dangling bond, oxygen, or the like, Q is oxygen or sulfur, n is an integer from 1 to 6, p is an integer from 1 to 6, V is a dangling bond, oxygen, or the like, and R is hydrogen, alkyl, or the like).Type: ApplicationFiled: May 11, 2011Publication date: June 27, 2013Inventors: Takashi Fujita, Hiroyoshi Horikoshi, Michael Anthony Cawthorne
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Publication number: 20130165445Abstract: The present invention relates to chemical compounds having a general formula I wherein A1-5 and 7-8, D?, L1, L2, R1, R3, R6-8, n and o are defined herein, and synthetic intermediates, which are capable of modulating the activity of Aurora kinase proteins and, thereby, influencing various disease states and conditions related to the activities of Aurora kinases. For example, the compounds are capable of 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: February 1, 2013Publication date: June 27, 2013Applicant: AMGEN INC.Inventor: AMGEN INC.
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Publication number: 20130165440Abstract: JAK1 inhibitors of structural formula (I), wherein Ar1, Ar2, Q, W, X, Y, and Z are defined in the specification, pharmaceutically acceptable salts thereof, compositions thereof, and use of the compounds and compositions for treating diseases. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases.Type: ApplicationFiled: September 13, 2011Publication date: June 27, 2013Applicant: EXELIXIS, INC.Inventors: Neel Kumar Anand, S. David Brown, Zerom Tesfai, Cristiana A. Zaharia
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Patent number: 8470825Abstract: The present invention relates to diazabenzo[de]anthracen-3-one compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.Type: GrantFiled: September 27, 2011Date of Patent: June 25, 2013Assignee: Eisai Inc.Inventors: Weizheng Xu, Greg Delahanty, Jie Zhang
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Publication number: 20130158006Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.Type: ApplicationFiled: November 28, 2012Publication date: June 20, 2013Applicant: GENENTECH, INC.Inventor: Genentech, Inc.
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Publication number: 20130158028Abstract: The present invention relates to the novel use of stimulators and activators of soluble guanylate cyclase for the treatment of sickle cell anemia and for the preservation of blood substitutes. The present invention furthermore relates to the use of stimulators and activators of soluble guanylate cyclase in combination with PDE5 inhibitors for the treatment of sickle cell anemia and for the preservation of blood substitutes.Type: ApplicationFiled: June 21, 2011Publication date: June 20, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Johannes-Peter Stasch, Eva-Maria Becker, Hubert Trübel, Herbert Himmel
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Patent number: 8466151Abstract: The invention relates to a compound of Formula (I) and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, E-isomer, Z-isomer, or combination thereof, wherein X is selected from S or O; R5 is selected from a substituted or unsubstituted aromatic group, a substituted or unsubstituted heteroaromatic group, or (Formula II) and the remaining substituents are described herein; and a composition comprising the thiosemicarbazone and/or the semicarbazone. The invention also relates to a method of administration of a thiocarbazone and/or a semicarbazone; and use thereof to treat a cancer.Type: GrantFiled: December 24, 2008Date of Patent: June 18, 2013Assignee: Critical Outcome Technologies, Inc.Inventors: Wayne R Danter, Cheuk Kun Kun Lau
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Patent number: 8466152Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.Type: GrantFiled: May 26, 2011Date of Patent: June 18, 2013Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
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Patent number: 8466150Abstract: Inhibitors of poly(ADP-ribose)polymerase, ways to make them and methods of treating patients using them are disclosed.Type: GrantFiled: June 12, 2008Date of Patent: June 18, 2013Assignee: Abbott LaboratoriesInventors: Virajkumar B. Gandhi, Vincent L. Giranda, Jianchun Gong, Thomas D Penning, Gui-Dong Zhu
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Publication number: 20130150351Abstract: Methods for treating a central nervous system (CNS) injury in a subject are provided. As of the methods include administering to the subject an effective amount of gamma aminobutyric acid (GABA) receptor signaling inhibitor to treat the subject for the CNS injury. Also provided are compositions useful in embodiments of the methods. Methods and compositions of the invention find use in the treatment of a variety of different CNS injuries, including but not limited to, treating a subject for CNS injury associated with the occurrence of stroke.Type: ApplicationFiled: June 2, 2011Publication date: June 13, 2013Inventors: Stanley T. Carmichael, Istvan Mody, Ben Huang, Andrew N. Clarkson
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Publication number: 20130150360Abstract: 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: December 6, 2012Publication date: June 13, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Patent number: 8461159Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).Type: GrantFiled: November 24, 2009Date of Patent: June 11, 2013Assignee: Jannsen Pharmaceutica BVInventors: J. Guy Breitenbucher, John M. Keith, Mark S. Tichenor, Alison L. Chambers, William M. Jones, Natalie A. Hawryluk, Amy K. Timmons, Jeffrey E. Merit, Mark J. Seierstad
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Publication number: 20130143866Abstract: Compositions of matter including ?-tocotrienol and SU11274 are disclosed herein. A variety of Met kinase inhibitors may be used in conjunction with tocotrienols in the treatment or prevention of cancer. Combinations of ?-tocotrienol and SU11274 inhibit the cell growth of +SA mammary tumor cells.Type: ApplicationFiled: December 2, 2012Publication date: June 6, 2013Inventor: Paul W. Sylvester
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Publication number: 20130143888Abstract: Phenoxymethyl compounds that inhibit at least one phosphodiesterase 10 are described as are pharmaceutical compositions containing such compounds an methods for treating various CNS disorders by administering such compounds to a patient in need thereof.Type: ApplicationFiled: December 20, 2012Publication date: June 6, 2013Applicant: ENVIVO PHAMACEUTICALS, INC.Inventor: ENVIVO PHAMACEUTICALS, INC.
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Publication number: 20130143887Abstract: Novel compound having the following formula: Also disclosed are a pharmaceutical compositions comprising the same, methods for treating cancer using the same, and methods for the synthesis of the same. The novel compounds of the present invention are found to inhibit protein kinases, especially Checkpoint kinase Chk1/Chk2.Type: ApplicationFiled: November 2, 2012Publication date: June 6, 2013Inventor: Zhanggui WU
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Publication number: 20130143889Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides heterocycles, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, seizure, retinal degeneration, hearing and vision loss, Alzheimer's disease, age-10 related memory loss, learning deficiencies, anxiety, neuronal degeneration and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.Type: ApplicationFiled: February 1, 2013Publication date: June 6, 2013Applicant: ICAGEN INC.Inventor: Icagen Inc.
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Patent number: 8455490Abstract: The present invention discloses methods of use of facially amphiphilic polymers and oligomers, including pharmaceutical uses of the polymers and oligomers as antimicrobial agents and antidotes for hemorrhagic complications associated with heparin therapy. The present invention also discloses novel facially amphiphilic polymers and oligomers and their compositions, including pharmaceutical compositions. The present invention further discloses the design and synthesis of facially amphiphilic polymers and oligomers.Type: GrantFiled: July 26, 2012Date of Patent: June 4, 2013Assignee: The Trustees of the University of PennsylvaniaInventors: William F. DeGrado, Gregory N. Tew, Michael L. Klein, Dahui Liu, Jing Yuan, Sungwook Choi
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Patent number: 8455491Abstract: The invention relates to the 6-cycloamino-3-(pyridazin-4-yl)imidazo[1,2-b]pyridazine derivatives corresponding to general formula (I): Wherein R2, R7, R8, A, L and B are as defined herein. Also disclosed are the preparative methods and therapeutic use thereof.Type: GrantFiled: January 11, 2010Date of Patent: June 4, 2013Assignee: SanofiInventors: Frederic Puech, Yulin Chiang, Sylvain Cote Des Combes, Adrien Tak Li, Philippe Burnier
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Patent number: 8455504Abstract: The present invention provides a method of treating diseases or disorders benefiting from inactivating or down-regulating the activity of the capsaicin receptor in a mammal by inhibiting the activity of the capsaicin receptor. The present invention also provides a method of treating obesity and obesity-related diseases and disorders in a mammal by inhibiting the activity of the capsaicin receptor.Type: GrantFiled: December 22, 2010Date of Patent: June 4, 2013Assignee: Xenia PharmaInventors: Dorte Xenia Gram, Anker Jon Hansen
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Publication number: 20130137694Abstract: There is provided modulators of Nrf2 protein which comprises a compound which binds at least one of the BTB domain, IVR domain and Kelch domain of Keap1 protein, activating or inhibiting Nrf2. There is also provided pharmaceutical compositions containing the modulators, as well as uses and method of use of the modulators for the treatment of conditions.Type: ApplicationFiled: May 31, 2011Publication date: May 30, 2013Inventors: Gerald Batist, Jian Hui Wu
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Publication number: 20130137693Abstract: Analogs of a Lisofylline (LSF), and synthetic methods for the preparation of such analogs are provided. The analogs of LSF provided have the ability to protect cell viability, particularly the ability to protect pancreatic ?-cells.Type: ApplicationFiled: May 22, 2012Publication date: May 30, 2013Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Timothy L. MACDONALD, Jerry L. NADLER, Peng CUI
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Publication number: 20130137695Abstract: Disclosed are compounds of general formula (I), their stereoisomers, regioisomers, tautomeric forms and novel intermediates involved in their synthesis, their pharmaceutically acceptable salts. These compounds are suitable as Poly (ADP-ribose) polymerase-1 inhibitors (PARP-1 inhibitors).Type: ApplicationFiled: July 7, 2011Publication date: May 30, 2013Applicant: CADILA HEALTHCARE LIMITEDInventor: Brijesh Kumar Shrivastava
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Publication number: 20130137675Abstract: The present invention aims to provide a compound having a PDE inhibitory action and useful as a medicament for the prophylaxis or treatment of schizophrenia and the like. A compound represented by the formula (1x): wherein each symbol is as described in the DESCRIPTION, or the formula (1): W1—W2??(1) wherein each symbol is as described in the DESCRIPTION, or a salt thereof.Type: ApplicationFiled: August 9, 2011Publication date: May 30, 2013Inventors: Takahiko Taniguchi, Shinkichi Suzuki, Masato Yoshikawa, Tomoaki Hasui, Makoto Fushimi, Jun Kunitomo
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Patent number: 8450319Abstract: The present invention discloses a pyrrolopyridazinone compound represented by the formula (1): useful, for example, as an anti-inflammatory agent or an inhibitor of respiratory tract contraction.Type: GrantFiled: January 16, 2007Date of Patent: May 28, 2013Assignee: Ube Industries, Ltd.Inventors: Masahiko Hagihara, Masayuki Tanaka, Tetsushi Katsube, Makoto Okudo, Noriaki Iwase, Manabu Shigetomi, Tomoko Kanda, Takayuki Nakanishi
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Publication number: 20130131062Abstract: The present invention is directed to pyridazinone compounds of formula (I) and furan compounds of formula (II), pharmaceutical compositions of compounds of formula (I) and (II), kits containing these compounds, methods of syntheses, and a method of treatment of a proliferative disease in a subject by administration of a therapeutically effective amount of a compound of formulae (I) or (II). Both classes of compounds were identified through screening of a collection of small molecule libraries.Type: ApplicationFiled: December 21, 2007Publication date: May 23, 2013Inventors: Hakim Djaballah, Harold E. Varmus, David Shum, Romel Somwar, Alexander Chucholowski, Mohan Santhanam Thiruvazhi
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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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Patent number: 8445491Abstract: 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: GrantFiled: May 27, 2009Date of Patent: May 21, 2013Assignee: The Board of Regents of the University of Texas SystemInventors: Lawrence Lum, Michael G. Roth, Baozhi Chen, Chuo Chen, Michael E. Dodge, Wei Tang
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Publication number: 20130123265Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: January 4, 2013Publication date: May 16, 2013Applicant: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Frank King, Yazhong Pei, Jeffrey P. Whitten
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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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Patent number: 8440706Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease.Type: GrantFiled: February 28, 2011Date of Patent: May 14, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Kevin M. Cottrell, John Maxwell, Qing Tang, Anne-Laure Grillot, Arnaud Le Tiran, Emanuele Perola
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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: 20130116235Abstract: Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X1, X2, and X3 are N, and 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 I 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: 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: 20130115313Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.Type: ApplicationFiled: November 9, 2012Publication date: May 9, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20130116245Abstract: Alkylated piperazine compounds of Formula I 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 I 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: 20130116262Abstract: Bicyclic piperazine compounds of Formula I 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 I 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: 20130115314Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.Type: ApplicationFiled: November 9, 2012Publication date: May 9, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20130116241Abstract: 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 25, 2012Publication date: May 9, 2013Applicants: AbbVie Inc., Abbott GmbH & Co. KGInventors: Abbott GmbH & Co. KG, AbbVie Inc.
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Publication number: 20130116258Abstract: Described herein are compounds that are androgen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such androgen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon androgen receptors.Type: ApplicationFiled: February 16, 2011Publication date: May 9, 2013Applicant: ARAGON PHARMACEUTICALS, INC.Inventors: Nicholas D. Smith, Celine Bonnefous, Jackaline D. Julien
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Publication number: 20130115310Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.Type: ApplicationFiled: November 9, 2012Publication date: May 9, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20130115311Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.Type: ApplicationFiled: November 9, 2012Publication date: May 9, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: Vertex Pharmaceuticals Incorporated