At Least Three Ring Nitrogens In The Bicyclo Ring System Patents (Class 544/236)
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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: 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: 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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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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Patent number: 8450354Abstract: The present invention provides substituted imidazo[1,2-b]pyridazine derivatives, pharmaceutically acceptable salts thereof, and tautomers of any of the foregoing, where such compounds inhibit ?-site amyloid precursor protein-cleaving enzyme (BACE), which may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. The invention also provides pharmaceutical compositions comprising any of these compounds and the use of any of these compounds and compositions in the treatment of diseases, disorders, or conditions in which BACE is involved.Type: GrantFiled: March 21, 2011Date of Patent: May 28, 2013Assignee: High Point Pharmaceuticals, LLCInventors: Adnan M. M. Mjalli, Anitha Hari, Bapu Gaddam, Devi Reddy Gohimukkula, Dharma Rao Polisetti, Mohan Rao, Raju Bore Gowda, Robert Carl Andrews, Rongyuan Xie, Soumya P. Sahoo, Tan Ren, William Kenneth Banner
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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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Patent number: 8450322Abstract: Compounds of Formula (I): in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor.Type: GrantFiled: September 21, 2009Date of Patent: May 28, 2013Assignee: Array BioPharma Inc.Inventors: Steven D. Andrews, Julia Haas, Yutong Jiang, Gan Zhang
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Publication number: 20130131321Abstract: The present invention relates to the use for affinity purification of an antibody or an fragment of an antibody, of a ligand-substituted matrix comprising a support material and at least one ligand covalently bonded to the support material, the ligand being represented by formula (I) wherein Sp is a spacer group; v is 0 or 1; Am is an amide group —NR1—C(O)—, and wherein either NR1 is attached to Ar1 and —C(O)— is attached to Ar2, or —C(O)— is attached to Ar1 and NR1 is attached to Ar2; and R1 is hydrogen or C1 to C4 alkyl, preferably hydrogen or methyl; and more preferably hydrogen; Ar1 is a divalent 5- or 6-membered substituted or unsubstituted aromatic ring; Ar2 is 5- or 6-membered heterocyclic aromatic ring which is (a) attached to a further 5- or 6-membered aromatic ring via a single bond; or (b) fused to a further 5- or 6-membered aromatic ring as part of a multicyclic ring system; or (c) attached to at least one substituent selected from C1 to C4 alkyl; C2 to C4 alkenyl; C2 to C4 alkynyl; aType: ApplicationFiled: August 3, 2011Publication date: May 23, 2013Applicant: GRAFFINITY PHARMACEUTICALS GMBHInventors: Holger Bittermann, Klaus Burkert, Marc Arnold, Oliver Keil, Thomas Neumann, Inge Ott, Kristina Schmidt, Daniel Schwizer, Renate Sekul
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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: 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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Patent number: 8436012Abstract: A compound represented by formula (I) having mTOR inhibitory activity or a pharmacologically acceptable salt thereof.Type: GrantFiled: November 24, 2010Date of Patent: May 7, 2013Assignee: Daiichi Sankyo Company, LimitedInventors: Masami Ohtsuka, Noriyasu Haginoya, Masanori Ichikawa, Hironori Matsunaga, Hironao Saito, Yoshihiro Shibata, Tomoyuki Tsunemi
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Publication number: 20130109661Abstract: 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: October 31, 2012Publication date: May 2, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Patent number: 8431574Abstract: Disclosed are compounds of the Formulas III and IV and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.Type: GrantFiled: January 20, 2009Date of Patent: April 30, 2013Assignee: Array BioPharma Inc.Inventors: James F. Blake, Joseph P. Lyssikatos, Hong-Woon Yang, Eli M. Wallace
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Publication number: 20130096113Abstract: Provided herein are heterocyclic compounds for treatment of CSF1R, FLT3, KIT, and/or PDGFR? kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: October 12, 2012Publication date: April 18, 2013Applicant: Ambit Biosciences CorporationInventor: Ambit Biosciences Corporation
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Patent number: 8420649Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein R1, R2, R3, R4, R5, W and X are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of p38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.Type: GrantFiled: August 26, 2009Date of Patent: April 16, 2013Assignee: Amgen Inc.Inventors: Liping H. Pettus, Andrew Tasker, Bin Wu
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Patent number: 8410264Abstract: The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).Type: GrantFiled: August 19, 2010Date of Patent: April 2, 2013Assignee: Novartis AGInventors: Miao Dai, Xingnian Fu, Feng He, Lei Jiang, Yue Li, Fang Liang, Lei Liu, Yuan Mi, Yao-chang Xu, Guoliang Xun, Xiaoxia Yan, Zhengtian Yu, Ji Yue Zhang
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Publication number: 20130072492Abstract: A compound of Formula (I): or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of Formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 24, 2011Publication date: March 21, 2013Inventors: Subharekha Raghavan, John E. Stelmach, Cameron J. Smith, Hong Li, Alan Whitehead, Sherman T. Waddell, Yi-Heng Chen, Shouwu Miao, Olga A. Ornoski, Joie Garfunkle, Xibin Liao, Jiang Chang, Xiaoqing Han, Jian Guo, Jonathan A. Groeper, Linda L. Brockunier, Keith Rosauer, Emma R. Parmee
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Publication number: 20130072495Abstract: Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as but not limited to tumors driven at least in part by at least one of RON, MET, IR, IGF-1R, or ALK. This Abstract is not limiting of the invention.Type: ApplicationFiled: May 16, 2011Publication date: March 21, 2013Inventors: An-Hu Li, Mark J. Mulvihill, Arno G. Steinig
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Patent number: 8399467Abstract: This invention relates to novel substituted triazolo-pyridazines, their derivatives, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an ?1-GABA-A receptor antagonist and/or a ?2, ?3 and ?5 GABA-A receptor agonist.Type: GrantFiled: June 30, 2011Date of Patent: March 19, 2013Assignee: Concert Pharmaceuticals, Inc.Inventor: Scott L. Harbeson
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Patent number: 8399462Abstract: Compounds of formula I modulate JNK: wherein the variables are as defined herein.Type: GrantFiled: December 7, 2007Date of Patent: March 19, 2013Assignee: Roche Palo Alto LLCInventors: James Patrick Dunn, Leyi Gong, David Michael Goldstein, Xiaochun Han, Joan Heather Hogg, Wylie Solang Palmer, Lubica Raptova, Tania Silva, Parcharee Tivitmahaisoon, Teresa Alejandra Trejo-Martin, Christophe Michoud, Achyutharao Sidduri
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Patent number: 8399381Abstract: The present invention provides a compound represented by the formula: wherein Q represents a fused heterocyclic group, X and Y are the same or different and each represent an optionally halogenated lower alkyl group, an optionally halogenated lower alkoxy group, etc., or a salt thereof, as well as a herbicide comprising the compound or a salt thereof, which exhibits a significant effect for control of sulfonylurea herbicide-resistant weeds in paddy fields and can reduce the number of active ingredients in a combined preparation and a method of controlling sulfonylurea herbicide-resistant weeds which comprises using the same.Type: GrantFiled: February 26, 2010Date of Patent: March 19, 2013Assignee: Sumitomo Chemical Company, LimitedInventors: Yasushi Tanaka, Yukari Kajiwara, Makoto Noguchi, Takeshi Kajiwara, Takanori Tabuchi
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Publication number: 20130059848Abstract: The present specification discloses cannabinoid-2 agonists, compositions comprising such cannabinoid-2 agonists, and methods of treating an individual suffering from a disease by administering compositions comprising such cannabinoid-2 agonists.Type: ApplicationFiled: February 7, 2011Publication date: March 7, 2013Applicant: ALLERGAN, INCInventors: June Chen, Simon Pettit, Hans Flirl
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Publication number: 20130059845Abstract: The present disclosure relates to compounds that act as agonists of, or otherwise modulate the activity of, GPR131 and to their use in the treatment of various diseases. In particular embodiments, the structure of the compounds is given by Formula I: wherein the variables are as described herein. Related compositions, formulations and methods for the preparation of compounds of formula I are also described.Type: ApplicationFiled: August 24, 2012Publication date: March 7, 2013Inventors: Jiangao SONG, Phuongly Pham, Jingyuan Ma, Aaron Robert Novack, Imad Nashashibi, David W. G. Wone, Dong-Fang Shi, Xin Chen
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Patent number: 8389527Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I imidazopyridazines inhibit protein kinase activity thereby making them useful as anticancer agents.Type: GrantFiled: February 6, 2009Date of Patent: March 5, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Brian E. Fink, Soong-Hoon Kim, Yufen Zhao, Ping Chen, Wayne Vaccaro, Litai Zhang, Ashvinikumar V Gavai, Dharmpal S Dodd, Libing Chen
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Patent number: 8389526Abstract: The invention relates to compounds of formula (I) and salts thereof wherein the substituents are as defined in the specification, the application of a compound of formula (I) in a process for the treatment of the human or animal body, in particular with regard to C-Met tyrosine kinase mediated disease; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner; processes for the preparation of a compound of formula (I).Type: GrantFiled: August 3, 2010Date of Patent: March 5, 2013Assignee: Novartis AGInventors: Pascal Furet, Clive McCarthy, Joseph Schoepfer, Stefan Stutz
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Publication number: 20130053346Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.Type: ApplicationFiled: August 23, 2012Publication date: February 28, 2013Applicant: Endo Pharmaceuticals IncInventors: Aranapakam Venkatesan, Roger Astbury Smith, Subramanya Hosahalli, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
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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: 20130045980Abstract: Disclosed are imidazopyridazinyl compounds of Formula (I): (I), or pharmaceutically salts and prodrugs thereof, wherein R3 is C2-4alkenyl or a cyclic group, and R1 and R2 are defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: April 27, 2011Publication date: February 21, 2013Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Upender Velaparthi, Peiying Liu, James Aaron Balog
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Publication number: 20130040955Abstract: The invention relates to novel pyrazolopyrimidinones according to formula (I). wherein X is CRe or unsubstituted N, D is optionally substituted cyclopentyl, cyclohexyl, tetrahydrofuranyl, tetrahydropyranyl or 2-, 3- or 4-pyridyl, Ra, Rb, Rc, Rd, Re are either H or optional substituents, m=1 or 2 and n is 0, 1 or 2. The new compounds are for use as the active entity of medicaments or for the manufacture of medicaments respectively, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. Such conditions may for example be associated with Alzheimer's disease, schizophrenia and other diseases. The new compounds are also for example for the manufacture of medicaments and/or for use in the treatment of these diseases, in particular for cognitive impairment associated with such disease. The compounds of the invention show PDE9 inhibiting properties.Type: ApplicationFiled: February 9, 2012Publication date: February 14, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Niklas HEINE, Riccardo GIOVANNINI
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Publication number: 20130035324Abstract: Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the heterocyclic entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.Type: ApplicationFiled: August 17, 2010Publication date: February 7, 2013Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Simon Fraser Campbell
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Publication number: 20130029982Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: July 18, 2012Publication date: January 31, 2013Applicants: INTELLIKINE, LLC, INFINITY PHARMACEUTICALS, INC.Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
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Publication number: 20130023523Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein B, R1, R2, R4, 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 wee-1 and methods of treating diseases such as cancer.Type: ApplicationFiled: July 19, 2012Publication date: January 24, 2013Applicant: ABBOTT LABORATORIESInventors: Gui-Dong Zhu, Jane Gong, Andrew S. Judd, Virajkumar B. Ghandi, Alexander R. Shoemaker, Thomas D. Penning, Michael R. Michaelides, Chunqiu Lai, Keith W. Woods
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Patent number: 8354405Abstract: The invention relates to the 6-cycloamino-3-(pyridin-4-yl)imidazo[I,2-b]pyridazine derivatives corresponding to general formula (I): Wherein R2, R3, R7, R8, A, L and B are as defined herein. Also disclosed are the preparative methods and therapeutic use thereof.Type: GrantFiled: December 24, 2009Date of Patent: January 15, 2013Assignee: SanofiInventors: Antonio Almario Garcia, Matthieu Barrague, Philippe Burnier, Cécile Enguehard, Zhongli Gao, Pascal George, Alain Gueiffier, Adrien Tak Li, Frédéric Puech, Roy Vaz, Qiuxia Zhao
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Publication number: 20130012516Abstract: The invention relates to the 6-cycloamino-3-(pyridin-4-yl)imidazo[I,2-b]pyridazine derivatives corresponding to general formula (I): Wherein R2, R3, R7, R8, A, L and B are as defined herein. Also disclosed are the preparative methods and therapeutic use thereof.Type: ApplicationFiled: September 14, 2012Publication date: January 10, 2013Applicant: SANOFIInventors: Antonio ALMARIO GARCIA, Matthieu BARRAGUE, Philippe BURNIER, Cécile ENGUEHARD, Zhongli GAO, Pascal GEORGE, Alain GUEIFFIER, Adrien Tak LI, Frédéric PUACH, Roy VAZ, Qiuxia ZHAO
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Publication number: 20130012511Abstract: The invention relates to compounds having the structure of Formula (I) and pharmaceutically acceptable salts thereof, which are soluble guanylate cyclase activators. The compounds are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The compounds are useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, pulmonary hypertension, angina pectoris, thromboses, restenosis, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver.Type: ApplicationFiled: March 22, 2011Publication date: January 10, 2013Inventors: Darby Schmidt, Subharekha Raghavan, John Stelmach, Jian Guo, Jonathan Groeper, Linda Brockunier, Keith Rosauer, Hong Shen, Rui Liang, Fa-Xiang Ding
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Patent number: 8343973Abstract: 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: GrantFiled: December 18, 2009Date of Patent: January 1, 2013Assignee: EnVivo Pharmaceuticals, Inc.Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Patent number: 8338412Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: May 13, 2011Date of Patent: December 25, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Guy W. Bemis, Francesco G. Salituro, John P. Duffy, John E. Cochran, Edmund M. Harrington, Mark A. Murcko, Keith P. Wilson, Michael Su, Vincent P. Galullo
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Publication number: 20120322784Abstract: The present invention relates to compounds of formula I, wherein the groups R1, LP, LQ, X1, X2, X3, Ar and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: ApplicationFiled: December 16, 2011Publication date: December 20, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank HIMMELSBACH, Matthias ECKHARDT, Niklas HEINE, Elke LANGKOPF, Bernd NOSSE
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Patent number: 8334379Abstract: A process for producing an imidazo[1,2-b]pyridazine compound represented by the formula (2): wherein R1, R2 and R3 are the same or different and each represents a hydrogen atom, a halogen atom, an alkyl group which may be substituted with a halogen atom or atoms, an alkenyl group which may be substituted with a halogen atom or atoms, or an alkoxy group which may be substituted with a halogen atom or atoms, which comprises reacting a 2,3-dihydropyridazine compound represented by the formula (1): wherein R1, R2 and R3 are the same meanings as defined above, with a phosphorus oxyhalide in the presence of an organic base which is in an amount of 0.5 mole or more relative to 1 mole of the 2,3-dihydropyridazine compound and 1 mole or less relative to 1 mole of the phosphorus oxyhalide.Type: GrantFiled: August 22, 2006Date of Patent: December 18, 2012Assignee: Sumitomo Chemical Company, LimitedInventors: Ichiro Komoto, Kazuaki Sasaki, Tomohiko Gotou
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Publication number: 20120316380Abstract: The present invention is related to pyrazolo piperidine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).Type: ApplicationFiled: February 17, 2011Publication date: December 13, 2012Applicant: GENKYOTEX SAInventors: Patrick Page, Benoît Laleu, Francesca Gaggini, Mike Orchard
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Patent number: 8324241Abstract: Disclosed are triazolopyridine compounds of Formula (I), including pharmaceutically acceptable salts thereof. Also, disclosed are methods of using the compound in the treatment of obesity, dyslipidemia, diabetes and atherosclerosis, and to pharmaceutical compositions comprising at least one compound of Formula (I) or a stereoisomer or pharmaceutically acceptable salt thereof.Type: GrantFiled: April 7, 2009Date of Patent: December 4, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Yanting Huang, Chongqing Sun, R. Michael Lawrence, William R. Ewing, Huji Turdi
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Patent number: 8324212Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: GrantFiled: February 22, 2011Date of Patent: December 4, 2012Assignee: Bristol-Myers Squibb CompanyInventors: John F. Kadow, Richard Pracitto
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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: 20120302748Abstract: The disclosure relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. Also provided are pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. Provided are methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1B1 and allelic variants thereof. Finally, provided is a method for determining the efficacy of a compound as described herein in treating cancer.Type: ApplicationFiled: February 28, 2012Publication date: November 29, 2012Applicant: THE UNIVERSITY COURT OF THE UNIVERSITY OF DUNDEEInventors: Steven Albert Everett, Saraj Ulhaq
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Publication number: 20120296089Abstract: Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.Type: ApplicationFiled: July 6, 2012Publication date: November 22, 2012Applicant: Pharmacyclics, Inc.Inventors: Lee Honigberg, Erik J. Verner, Joseph J. Buggy, David J. Loury, Wei Chen
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Publication number: 20120283241Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazopyridazines inhibit protein kinase activity thereby making them useful as anticancer agents.Type: ApplicationFiled: July 19, 2012Publication date: November 8, 2012Inventors: Brian E. Fink, Libing Chen, Ashvinikumar V. Gavai, Liqi He, Soong-Hoon Kim, Andrew James Nation, Yufen Zhao, Litai H. Zhang
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Publication number: 20120277225Abstract: Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.Type: ApplicationFiled: July 6, 2012Publication date: November 1, 2012Applicant: Pharmacyclics, Inc.Inventors: Lee Honigberg, Erik J. Verner, Joseph J. Buggy, David J. Loury, Wei Chen
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Patent number: 8299076Abstract: Disclosed are crystalline forms of 2-(2-fluoro-4-iodophenylamino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxamide useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.Type: GrantFiled: May 17, 2006Date of Patent: October 30, 2012Assignees: Array Biopharma Inc., Astrazeneca ABInventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, Jim Blake, Richard Anthony Storey, Rebecca Jane Booth, John David Pittam, John Leonard, Mark Richard Fielding
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Publication number: 20120270879Abstract: Disclosed are CCR1 receptor antagonists of the formula (I) wherein Ar1, Ar2, R1-R3, X and L are disclosed herein. Also disclosed are compositions, methods of making and using compounds of the formula (I).Type: ApplicationFiled: October 21, 2010Publication date: October 25, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Brian Nicholas Cook, Daniel Kuzmich
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Patent number: 8293948Abstract: A reagent for organic synthesis with which a chemical reaction can be conducted in a liquid phase and unnecessary compound(s) can be easily separated at low cost from the liquid phase after completion of the reaction. The reagent for organic synthesis reversibly changes from a liquid-phase state to a solid-phase state with changes in solution composition and/or solution temperature, and is for use in organic synthesis reactions. This reagent for organic syntheses facilitates process development. With the reagent, research on and development of, e.g., medicines through, e.g., compound library synthesis, etc. can be accelerated. It can hence contribute to technical innovations in the biochemical industry and chemical industry.Type: GrantFiled: January 9, 2012Date of Patent: October 23, 2012Assignee: Jitsubo Co., Ltd.Inventors: Kazuhiro Chiba, Shokaku Kim, Yusuke Kono