Additional Hetero Ring Which Is Unsaturated Patents (Class 544/328)
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Patent number: 8921336Abstract: The present invention provides novel heteroaryl compounds of formula (I) having a pyrimidine-containing core that is linked to a 4-trifluoromethoxyphenyl group via an amine linker. Such compounds are useful for the treatment of cancers.Type: GrantFiled: November 28, 2008Date of Patent: December 30, 2014Assignees: Dana-Farber Cancer Institute, Inc., The Scripps Research InstituteInventors: Nathanael Gray, Jianming Zhang, Barun Okram, Xianming Deng, Jae Won Chang
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Publication number: 20140378488Abstract: Provided are derivatives substituted by urea associated with 4-substituted-(3-substituted-1H-pyrazole-5-amino)-pyrimidine-2-amino of formula (I), wherein these compounds may selectively regulate or inhibit an information transmission process controlled by natural or variant tyrosine kinase. Also provided are preparation methods and uses of the compounds.Type: ApplicationFiled: September 5, 2011Publication date: December 25, 2014Applicant: ZHEJIANG HISUN PHARMACEUTICAL CO., LTD.Inventors: Yili Ding, Xuan Yang, Qingyan Yan, Hua Bai, Lifeng Cai, Kenneth Smith, Jian Chai
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Publication number: 20140371065Abstract: The present invention relates to fungicidal pyrimidine compounds I, to their use and to methods for combating phytopathogenic fungi. The present invention also relates to seeds treated with at least one such compound. Furthermore the invention relates to processes for preparing compounds of formula I.Type: ApplicationFiled: January 30, 2013Publication date: December 18, 2014Applicant: BASF SEInventors: Wassilios Grammenos, Ian Robert Craig, Nadege Boudet, Bernd Mueller, Jochen Dietz, Erica May Wilson Lauterwasser, Jan Klaas Lohmann, Jurith Montag
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Publication number: 20140364408Abstract: The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula (I): or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.Type: ApplicationFiled: July 29, 2012Publication date: December 11, 2014Applicant: KARYOPHARM THERAPEUTICS INC.Inventors: Vincent P. Sandanayaka, Sharon Shacham, Dilara McCauley, Sharon Shechter
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Patent number: 8906914Abstract: Certain ethylene diamine compounds of Formula (I) 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, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). Methods of synthesizing such compounds are also disclosed.Type: GrantFiled: August 17, 2010Date of Patent: December 9, 2014Assignee: Janssen Pharmaceutica NVInventors: Natalie A. Hawryluk, J. Guy Breitenbucher, William M. Jones, Alison L. Chambers, John M. Keith, Mark Seierstad
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Patent number: 8895565Abstract: Provided is a compound represented by general formula (6) and pharmaceutically acceptable salts thereof. (In the formula, R1 is a hydrogen atom or a C1-6 alkyl group; R2 is a hydrogen atom or a C1-6 alkyl group; R3 is a hydrogen atom, a halogen atom, a C1-6 alkyl group, or a C1-6 haloalkyl group.Type: GrantFiled: February 8, 2010Date of Patent: November 25, 2014Inventor: Tetsuya Nishio
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Patent number: 8895747Abstract: Methods for the synthesis of N-substituted pyridinium compounds by using an N-heteroaryl substituted pyridinium salt (Zincke salt) and reacting it with a nucleophilic amine are provided. Novel purine-substituted pyridyl compounds, which may be useful reagents in the above reaction, are also disclosed.Type: GrantFiled: January 27, 2012Date of Patent: November 25, 2014Assignee: Roche Diagnostics Operations, Inc.Inventors: Dieter Heindl, Heribert Maerz, Axel Schmidt
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Publication number: 20140343029Abstract: The invention provides novel imidazole amine compounds according to Formula (I) and Formula (II) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: ApplicationFiled: September 12, 2012Publication date: November 20, 2014Applicant: MERCK PATENT GMBHInventors: Ruoxi Lan, Bayard R. Huck, Xiaoling Chen, Yufang Xiao, Lizbeth Celeste Deselm, Hui Qiu, Constantin Neagu, Donald Bankston, Christopher Charles Victor Jones
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Publication number: 20140336171Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: July 24, 2014Publication date: November 13, 2014Inventors: Luc Farmer, Gabriel Martinez-Botella, Albert Pierce, Francesco Salituro, Jian Wang, Marion W. Wannamaker, Tiansheng Wang
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Publication number: 20140336377Abstract: The present invention relates to arylamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.Type: ApplicationFiled: October 18, 2011Publication date: November 13, 2014Applicant: RAQUALIA PHARMA INC.Inventors: Tatsuya Yamagishi, Kiyoshi Kawamura, Yoshimasa Arano, Mikio Morita
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Publication number: 20140336503Abstract: The present invention provides biomarkers that find use as imaging agents within nuclear medicine applications (e.g., PET imaging and SPECT imaging). In particular, the present invention provides methods for identifying and characterizing osteoclast activation within subjects with radiolabeled cathepsin K inhibitors.Type: ApplicationFiled: April 30, 2014Publication date: November 13, 2014Applicant: The Regents of the University of MichiganInventors: Michael R. Kilbourn, Kenneth Kozloff, Melissa E. Rodnick
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Publication number: 20140336374Abstract: The present invention relates to a process for the production of novel antagonists for CCR2 (CC chemokine receptor 2) and intermediates thereof.Type: ApplicationFiled: July 29, 2014Publication date: November 13, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Heiner EBEL, Sara FRATTINI, Riccardo GIOVANNINI, Christoph HOENKE, Thomas TRIESELMANN, Patrick TIELMANN
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Publication number: 20140336379Abstract: An organic light-emitting device containing a compound represented by the following general formula in a light light-emitting layer has a high light-emission efficiency. The ring containing Y1, Y2 and Y3 represent a triazine ring or a pyrimidine ring; Z1, Z2 and R1 to R8 represent a hydrogen atom or a substituent; and at least one of R1 to R8 represents a diarylamino group or a carbazolyl group. The compound represented by the general formula (1) contains at least two carbazole structures in the molecule thereof.Type: ApplicationFiled: November 30, 2012Publication date: November 13, 2014Inventors: Chihaya Adachi, Takuma Yasuda, Saeyoun Lee, Hiroko Nomura, Tetsuya Nakagawa
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Patent number: 8883785Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.Type: GrantFiled: January 20, 2011Date of Patent: November 11, 2014Assignee: CHDI Foundation, Inc.Inventors: Celia Dominguez, Leticia M. Toledo-Sherman, Dirk Winkler, Frederick Brookfield, Paula C. De Aguiar Pena
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Publication number: 20140329822Abstract: The invention relates to a N-piperidin-4-yl derivative having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same and to the use of said N-piperidin-4-yl derivatives for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, or for the treatment of uterine fibroids or other menstrual-related disorders.Type: ApplicationFiled: September 14, 2012Publication date: November 6, 2014Inventors: Ines Huisman, Marcelis Van Der Stelt, Wouter Wiedenhof, Charles Anthony Graham Baker-Glenn, Wesley Peter Blackaby, Naimisha Trivedi
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Patent number: 8877745Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) wherein HET is a group selected from among formulas (IIa) (IIb) (IIc) (IId) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases.Type: GrantFiled: May 10, 2011Date of Patent: November 4, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Stefan Scheuerer
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Publication number: 20140323465Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: July 14, 2014Publication date: October 30, 2014Inventors: Deqiang Niu, Russell C. Petter, Juswinder Singh, Arthur F. Kluge, Lixin Qiao
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Publication number: 20140315934Abstract: Compounds of formula (I) and their use as pharmaceutical.Type: ApplicationFiled: December 17, 2012Publication date: October 23, 2014Inventors: Marion Hitchcock, Anne Mengel, Anja Richter, Hans Briem, Knut Eis, Vera Pütter, Gerhard Siemeister, Stefan Prechtl, Amaury Ernesto Fernandez-Montalvan, Christian Stegmann, Simon Holton, Mark Jean Gnoth, Cornelia Preuße
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Publication number: 20140315926Abstract: The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I) which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: July 1, 2014Publication date: October 23, 2014Inventor: Peter FEY
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Patent number: 8865723Abstract: Provided herein are methods of improving cognitive ability or memory in a subject that has suffered a brain injury or spinal cord injury by administering a selective PDE4 B inhibitor.Type: GrantFiled: March 13, 2013Date of Patent: October 21, 2014Assignee: Tetra Discovery Partners LLCInventors: Mark E. Gurney, Coleen M. Atkins, David J. Adaikkalasamy, W. Dalton Dietrich
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Patent number: 8865724Abstract: Disclosed is a derivative of 2-methyl-4-amino-5-(substituted-1H-1,2,3-triazol)methylpyrimidine of general formula I and microbicidal activity thereof. In the formula, R1 represents hydrogen, I; X represents O or NH; Y represents phenyl of substituted phenyl, benzoyl or substituted benzoyl, phenyloxyacetyl or substituted phenyloxyacetyl; the substituents on the phenyl rings which Y involves are: H, halogen, nitro, cyano, CF3, C1˜4 alkyl, methoxyl, C1˜2 carboxyl or carboxylic ester groups; any position of phenyl rings can be mono- or multi-substituted by identical or different substituents. The compound has a significant inhibition effect on cucumber bacterial angular leaf spot, tomato bacterial leaf spot, cucumber brown blot, cucumber downy mildew, rice sheath blight, Gibberella saubinetii, Alternaria solani, Botrytis cinerea, Alternaria alternate and Colletotrichum orbiculare and it can be used as an effective ingredient of microbicides.Type: GrantFiled: March 11, 2014Date of Patent: October 21, 2014Assignee: Central China Normal UniversityInventors: Hongwu He, Junbo He, Fang Wang, Xiaoguo Wang, Xiaosong Tan, Hao Peng
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Publication number: 20140309421Abstract: The present invention relates to processes and intermediates for the preparation of compounds useful as inhibitors of Janus kinases (JAK).Type: ApplicationFiled: June 25, 2014Publication date: October 16, 2014Inventors: Gerald J. Tanoury, Young Chun Jung, Derek Magdziak, Adam Looker, Billie J. Kline, Václav Jurcík, Beatriz Dominguez Olmo
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Publication number: 20140309211Abstract: Substituted 5-(pyrazin-2-yl)-1H-pyrazolo[3,4-b]pyridine, 5-(pyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridine and pyrazolo[3,4-b]pyridine derivatives according to formula I, II and VII, and methods for making same, which are inhibitors of constitutively activated Tyrosine Kinase-Like (TKL), CMGC protein kinases family members and can be useful in the treatment of Parkinson's disease, Alzheimer's disease, Down's Syndrome, Huntington's disease, other neurodegenerative and central nervous system disorders, cancer, metabolic disorders and inflammatory diseases. Also disclosed are pharmaceutical compositions including the compounds and methods of inhibiting wild type and/or mutated protein kinase activities of these families and the treatment of disorders associated therewith using compounds and pharmaceutical compositions including the compounds.Type: ApplicationFiled: May 29, 2014Publication date: October 16, 2014Applicant: ARRIEN PHARMACEUTICALS LLCInventors: Hariprasad Vankayalapati, Rajendra P. Appalaneni, Y. Venkata Krishna Reddy
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Publication number: 20140303139Abstract: The present disclosure provides substituted pyrimidine compounds of Formula (I), and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A1, X, A2, W1, W2, E, Z, and R4 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.Type: ApplicationFiled: August 31, 2012Publication date: October 9, 2014Inventors: Chiyou Ni, Laykea Tafesse, Jiangcho Yao, Mark Youngman, Minnie Park, Bin Shao
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Patent number: 8853398Abstract: The present invention relates to a process for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate of the formula (I) and to a process for purifying the crude product of the compound of the formula (I) for use as pharmaceutically active compound, where, for purification, methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate sulphinyldimethane (1:1), i.e. a compound of the formula (II), is isolated as intermediate or is generated as intermediate in this purification process, if appropriate present in a mixture.Type: GrantFiled: July 18, 2013Date of Patent: October 7, 2014Assignee: Bayer Intellectual Property GmbHInventors: Franz-Josef Mais, Joachim Rehse, Winfried Joentgen, Konrad Siegel
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Publication number: 20140296201Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A compound is represented by Structural Formula (IA) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.Type: ApplicationFiled: June 16, 2014Publication date: October 2, 2014Inventors: Paul S. Charifson, Michael P. Clark, Upul K. Bandarage, Randy S. Bethiel, John J. Court, Hongbo Deng, Ioana Davies, John P. Duffy, Luc J. Farmer, Huai Gao, Wenxin Gu, Dylan H. Jacobs, Joseph M. Kennedy, Mark W. Ledeboer, Brian Ledford, Francois Maltais, Emanuele Perola, Tiansheng Wang, M. Woods Wannamaker, Randal Byrn, Yi Zhou, Chao Lin, Min Jiang, Steven Jones, Ursula A. Germann, Francesco G. Salituro, Ann Dak-Yee Kwong
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Publication number: 20140296204Abstract: The invention is directed to substituted heteroaryl derivatives. Specifically, the invention is directed to compounds according to Formula Q: wherein D, L, M, W, X, Y, and Z are defined herein. The compounds of the invention are inhibitors of DNA methyltransferase (DNMT) activity—including DNMT1, DNMT3a, or DNMT3b—and are useful in the treatment of cancer and hyperproliferative diseases. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting DNMT activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: October 23, 2012Publication date: October 2, 2014Inventors: Thomas Francis Hendrickson, Koc-Kan Ho, Michael David Saunders, Brian John Stevens, Krzysztof Swierczek, Kevin Bret Wright
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Publication number: 20140288067Abstract: Provided herein are compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, R1, R2a, R2b, R2c, R2d, are as defined herein, and Ring HET is a 6-membered monocyclic heteroaryl ring system of formula: wherein L2, R13, G8, G10, G11, and G12 are as defined herein. Compounds of the present invention are useful for inhibiting CARM1 activity. Methods of using the compounds for treating CARM1-mediated disorders are also described.Type: ApplicationFiled: March 14, 2014Publication date: September 25, 2014Applicant: Epizyme, Inc.Inventors: Richard Chesworth, Oscar Miguel Moradei, Gideon Shapiro, Lei Jin, Robert E. Babine
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Publication number: 20140288303Abstract: The present invention relates to a process for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate of the formula (I) and to a process for purifying the crude product of the compound of the formula (I) for use as pharmaceutically active compound, where, for purification, methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate sulphinyldimethane (1:1), i.e. a compound of the formula (II), is isolated as intermediate or is generated as intermediate in this purification process, if appropriate present in a mixture.Type: ApplicationFiled: June 4, 2014Publication date: September 25, 2014Applicant: Bayer Intellectual Property GmbHInventors: Franz-Josef MAIS, Joachim Rehse, Winfried Joentgen, Konrad Siegel
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Publication number: 20140274701Abstract: Novel 4-amino-6-(heterocyclic)picolinic acids and their derivatives and 6-amino-2-(heterocyclic)pyrimidine-4-carboxylates and their derivatives are useful to control undesirable vegetation.Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Applicant: Dow AgroSciences LLCInventors: Joseph D. Eckelbarger, Jeffrey B. Epp, Lindsey G. Fischer, Christian T. Lowe, Jeff Petkus, Joshua Roth, Norbert M. Satchivi, Paul R. Schmitzer, Thomas L. Siddall
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Publication number: 20140274695Abstract: 4-Amino-6-(heterocyclic)picolinic acids and their derivatives; 6-amino-2-(heterocyclic)pyrimidine-4-carboxylates and their derivatives; and methods of using the same as herbicides.Type: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Applicant: Dow AgroSciences LLCInventors: Joseph D. Eckelbarger, Jeffrey B. Epp, Stephen Craig Fields, Lindsey G. Fischer, Natalie C. Giampietro, Katherine A. Guenthenspberger, Christian T. Lowe, Jeff Petkus, Joshua Roth, Norbert M. Satchivi, Paul R. Schmitzer, Thomas L. Siddall, Nick X. Wang
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Publication number: 20140274703Abstract: 4-amino-6-(pyridyl and 2-substitutedphenyl)-picolinic acids and their derivatives; 6-amino-2-(pyridyl and 2-substitutedphenyl)-pyrimidine-4-carboxylates and their derivatives; and methods of using the same as herbicides.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: Dow AgroSciences LLCInventors: Joseph D. ECKELBARGER, Jeffrey B. EPP, Lindsey G. FISCHER, Natalie C. GIAMPIETRO, Jeremy KISTER, Jeffrey PETKUS, Joshua ROTH, Norbert M. SATCHIVI, Paul R. SCHMITZER, Thomas L. SIDDALL, Carla N. YERKES
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Publication number: 20140271543Abstract: New pyridin-2(1H)-one derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).Type: ApplicationFiled: July 23, 2012Publication date: September 18, 2014Applicant: ALMIRALL, S.A.Inventors: Paul Robert Eastwood, Jordi Bach Taña, Lluis Miquel Pages Santacana
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Patent number: 8835440Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.Type: GrantFiled: July 24, 2013Date of Patent: September 16, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Thomas Trieselmann, Patrick Tielmann, Stefan Scheuerer, Silke Hobbie, Frank Buettner
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Publication number: 20140256703Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: ApplicationFiled: March 13, 2013Publication date: September 11, 2014Inventors: Juan-Miguel Jimenez, Philip Collier, Andrew Miller
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Publication number: 20140256708Abstract: The present invention is directed to substituted azetidinecompounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: ApplicationFiled: October 1, 2012Publication date: September 11, 2014Inventors: Christopher D. Cox, Douglas C. Beshore, June J. Kim, Scott D. Kuduk, Carol A. McVean, Thomas Reger, Justin T. Sheen
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Patent number: 8829006Abstract: The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R1, R2, R3 and R4 are defined as mentioned in the description, the tautomers thereof, the isomers thereof, the diastereomers thereof, the enantiomers thereof, the hydrates thereof, the mixtures thereof and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, the use thereof and processes for the preparation thereof.Type: GrantFiled: November 21, 2008Date of Patent: September 9, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Dirk Gottschling, Georg Dahmann, Henri Doods, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Schaenzle, Dirk Stenkamp
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Patent number: 8829007Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A compound is represented by Structural Formula (IA) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.Type: GrantFiled: December 6, 2013Date of Patent: September 9, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Paul S. Charifson, Michael P. Clark, Upul K. Bandarage, Randy S. Bethiel, John J. Court, Hongbo Deng, Ioana Davies, John P. Duffy, Luc J. Farmer, Huai Gao, Wenxin Gu, Dylan H. Jacobs, Joseph M. Kennedy, Mark W. Ledeboer, Brian Ledford, Francois Maltais, Emanuele Perola, Tiansheng Wang, M. Woods Wannamaker, Randal Bym, Yi Zhou, Chao Lin, Min Jiang, Steven Jones, Ursula A. Germann, Francesco G. Salituro, Ann Dak-Yee Kwong
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Publication number: 20140249138Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: February 18, 2014Publication date: September 4, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Francesco Salituro, Luc Farmer, Randy Bethiel, Edmund Harrington, Jeremy Green, John Court, Jon Come, David Lauffer, Alex Aronov, Hayley Binch, Dean Boyall, Jean-Damien Charrier, Simon Everitt, Damien Fraysse, Michael Mortimore, Francoise Pierard, Daniel Robinson, Jian Wang, Joanne Pinder, Tiansheng Wang, Albert Pierce
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Publication number: 20140249137Abstract: The present invention relates to compounds useful as inhibitors of treating tuberculosis.Type: ApplicationFiled: October 31, 2013Publication date: September 4, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Tiansheng Wang, Brian Hanzelka, Ute Muh, Guy Bemis, Harmon J. Zuccola
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Publication number: 20140249133Abstract: Compounds of formula (I) which are inhibitors of Bub1 kinase, processes for their production and their use as pharmaceuticals.Type: ApplicationFiled: October 4, 2012Publication date: September 4, 2014Inventors: Marion Hitchcock, Anne Mengel, Vera Pütter, Gerhard Siemeister, Antje Margret Wengner, Hans Briem, Knut Eis, Volker Schulze, Amaury Ernesto Fernandez-Montalvan, Stefan Prechtl, Simon Holton, Jörg Fanghänel, Philip Lienau, Cornelia Preusse, Mark Jean Gnoth
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Publication number: 20140249134Abstract: The present invention is directed to substituted triazolyl compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: ApplicationFiled: October 3, 2012Publication date: September 4, 2014Inventors: Christopher D. Cox, Vadim Y. Dudkin, June J. Kim, Scott D. Kuduk, Carol A. McVean, Thomas Reger, Justin T. Sheen, Thomas Steele
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Publication number: 20140242120Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein Y, L, A, W1, W2, and R?1 are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: May 8, 2014Publication date: August 28, 2014Applicant: Synta Pharmaceuticals Corp.Inventors: Shoujun Chen, Lijun Sun, Yu Xie
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Publication number: 20140228386Abstract: The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds of the present invention have been found to be useful as 17?-hydroxylase/C17,20-lyase inhibitors.Type: ApplicationFiled: April 27, 2012Publication date: August 14, 2014Applicant: NOVARTIS AGInventors: Mark Gary Bock, Christoph Gaul, Venkateshwar Rao Gummadi, Saumitra Sengupta
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Publication number: 20140228358Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.Type: ApplicationFiled: September 21, 2012Publication date: August 14, 2014Inventors: Jason Brubaker, Joshua T. Close, Joon Jung, Michelle Martinez, Catherine White, Kevin Wilson, Jonathan R. Young, Hongjun Zhang
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Patent number: 8802847Abstract: The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I) which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.Type: GrantFiled: November 26, 2012Date of Patent: August 12, 2014Assignee: Bayer Intellectual Property GmbHInventor: Peter Fey
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Publication number: 20140221366Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: ApplicationFiled: June 11, 2012Publication date: August 7, 2014Applicant: MERCK PATENT GMBHInventors: Timo Heinrich, Nadia Brugger, Kristopher Josephson
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Publication number: 20140221336Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: February 5, 2014Publication date: August 7, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Marion W. Wannamaker, Francesco Salituro, Albert Pierce, Alex Aronov, Gabriel Martinez-Botella, Jian Wang, Luc Farmer, Mark Ledeboer, Tiansheng Wang, Randy Bethiel, Brian Ledford, Emilie Porter Huck
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Patent number: 8796314Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, CY, X1, X2, and X3 are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: GrantFiled: January 28, 2010Date of Patent: August 5, 2014Assignee: Millennium Pharmaceuticals, Inc.Inventors: Zhan Shi, Irache Visiers, Tricia J. Vos, Stepan Vyskocil
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Patent number: 8796453Abstract: The present invention relates to processes and intermediates for the preparation of compounds useful as inhibitors of Janus kinases (JAK).Type: GrantFiled: July 12, 2013Date of Patent: August 5, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Gerald J. Tanoury, Young Chun Jung, Derek Magdziak, Adam Looker, Billie J. Kline, Václav Jurcík, Beatriz Dominguez Olmo