Three Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/278)
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Publication number: 20130059867Abstract: An objective of the present invention is to improve the solubility of 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid. The present invention provides 342-fluoro-5-(2,3-difluoro-6-methoxybenzyl-oxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid choline salt has excellent solubility and storage stability.Type: ApplicationFiled: February 9, 2011Publication date: March 7, 2013Applicant: Kissei Pharmaceutical Co., Ltd.Inventors: Kazumichi Jo, Hideki Takeuchi
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Publication number: 20130059866Abstract: The invention relates to novel piperidino-dihydrothienopyrimidine sulfoxides of formula I, wherein Ring A is a 6-membered aromatic ring which may optionally comprise one or two nitrogen atoms and wherein R is Cl and wherein R may be located either in the para-, meta- or ortho-position of Ring A, wherein S* is a sulphur atom that represents a chiral center, and all pharmaceutically acceptable salts, enantiomers and racemates, hydrates and solvates thereof and the use of these compounds for the treatment of inflammatory or allergic diseases of the respiratory tract such as COPD or asthma.Type: ApplicationFiled: February 23, 2012Publication date: March 7, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Horst Dollinger, Rogelio Perez Frutos, Soojin Kim, Jason Alan Mulder, Peter Nickolaus, Nitinchandra D. Patel, Pascale Pouzet, Chris Hugh Senanayake, Thomas Gabriel Tampone, Xudong Wei, Ulrike Werthmann, Bing-Shiou Yang
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Publication number: 20130058980Abstract: Compounds that modulate, for example, that inhibit, syk kinase, and, optionally other kinases. The compounds can be used to treat a variety of disorders, including inflammatory disorders and autoimmune disorders.Type: ApplicationFiled: November 2, 2010Publication date: March 7, 2013Inventors: Ketan Desai, Renee Desai
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Publication number: 20130053370Abstract: The present invention relates to a thieno[3,2-d]pyrimidine derivative of formula (I), or a pharmaceutically acceptable salt, hydrate or solvate thereof, which has an excellent inhibitory activity on protein kinases, and a pharmaceutical composition comprising the same is effective in preventing or treating abnormal cell growth diseases.Type: ApplicationFiled: January 31, 2011Publication date: February 28, 2013Applicants: HANMI SCIENCE CO., LTD., CATHOLIC UNIVERSITY INDUSTRY ACADEMIC COOPERATION FOUNDATION, KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Jung Beom Son, Seung Hyun Jung, Wha ll Choi, Young Hee Jung, Jae Yul Choi, Ji Yeon Song, Kyu Hang Lee, Jae Chul Lee, Eun Young Kim, Young Gil Ahn, Maeng Sup Kim, Hwan Geun Choi, Tae Bo Sim, Young Jin Ham, Dong-sik Park, Hwan Kim, Dong-Wook Kim
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Patent number: 8377944Abstract: This invention provides thienopyrimidine derivatives of the formula, wherein R1 stands for hydrogen atom, an alkyl group or the like; R2 stands for a hydrogen atom, an alkyl or amino group or the like, R3 stands for an alkyl, alkenyl or alkylthio group or the like or a group Y—X—; or R2 and R3 may together form tetramethylene group; X standing for a direct bond or linking group such as CH2, CH(OH), S, O, NH; Y standing for a substituted or unsubstituted aromatic carbocyclic, aromatic heterocylic, cycloalkyl or saturated heterocyclic group or the like; Z stands for S or O, and n is 0 or an integer of 1 to 4, or salts thereof, which exhibit an inhibitory effect on PDE9, and are therefore useful for prevention or treatment of overactive bladder syndrome, pollakiuria, urinary incontinence, dysuria associated with prostatic hyperplasia, urolithiasis, Alzheimer's disease, chronic obstructive pulmonary disease, myocardial infarction, thrombosis, diabetes and the like.Type: GrantFiled: August 14, 2012Date of Patent: February 19, 2013Assignee: ASKA Pharmaceutical Co., Ltd.Inventors: Kotaro Gotanda, Atsushi Shinbo, Youichi Nakano, Hideo Kobayashi, Makoto Okada, Akira Asagarasu
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Patent number: 8377949Abstract: Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving Chymase.Type: GrantFiled: August 12, 2008Date of Patent: February 19, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Xin Guo, Ho Yin Lo, Chuk Chui Man, Hidenori Takahashi
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Publication number: 20130040957Abstract: The present invention is concerned with deuterium-enriched pyrimidine compounds of formula I, their derivatives, enantiomers, diastereomers, solvates and pharmaceutical salts thereof, and their uses in the treatment, prevention and modulation of various diseases including chronic liver diseases, liver cirrhosis, liver fibrosis, hepatocellular carcinoma, liver cancer, renal cell carcinoma, kidney cancer, colorectal cancer, brain cancer, breast cancer, blood cancer, lung cancer, thyroid cancer, ovarian cancer, pancreas cancer, prostate cancer, stomach cancer, testicular cancer, uterus cancer, intestinal cancer, skin cancer, and other forms of cancer, carcinoid tumors, teratocarcinoma, tumor progression, metastasis and fibrosis in the neuroendocrine neoplasia, fibrotic processes as well as a disease state modulated directly or indirectly with 5-HT receptors, 5-HT1, 5-HT1A, 5-HT2 receptors, 5-HT2A and 5-HT2B receptors, dopamine receptors and multiple kinase pathways.Type: ApplicationFiled: October 12, 2012Publication date: February 14, 2013Inventor: Daljit Singh Dhanoa
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Publication number: 20130040975Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: ApplicationFiled: August 10, 2012Publication date: February 14, 2013Applicant: NEUROCRINE BIOSCIENCES, INC.Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Jinghua Yu, Willy Moree, Warren Wade, Liren Zhao, Yun-fei Zhu, Martin Rowbottom, Neil Ashweek
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Publication number: 20130035347Abstract: The present invention relates to novel aromatic bicyclic derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the CXCR4 receptor.Type: ApplicationFiled: August 2, 2012Publication date: February 7, 2013Inventors: Vidyasagar Vuligonda, Richard L. Beard, Thong Vu, John E. Donello, Gerard Rodrigues, Veena Viswanath, Michael E. Garst
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Publication number: 20130029984Abstract: 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, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
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Publication number: 20130029942Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof that are effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: ApplicationFiled: October 4, 2012Publication date: January 31, 2013Applicant: Myrexis, Inc.Inventor: Myrexis, Inc.
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Publication number: 20130030011Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.Type: ApplicationFiled: January 26, 2012Publication date: January 31, 2013Inventors: KENNETH M. BOY, Jason M. Guernon, John E. Macor, Richard E. Olson, Jianliang Shi, Lorin A. Thompson, III, Yong-Jin Wu, Li Xu, Yunhui Zhang, Dmitry S. Zuev
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Publication number: 20130029969Abstract: Provided is a compound useful for the prophylaxis or treatment of cancer. The present invention relates to a compound represented by formula (I): wherein each symbol in the formula is as defined in the specification, or a salt thereof or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.Type: ApplicationFiled: February 16, 2011Publication date: January 31, 2013Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Misaki Homma, Toru Miyazaki, Yuya Oguro, Osamu Kurasawa
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Publication number: 20130018038Abstract: The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, and R3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. 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 PERK 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: March 23, 2011Publication date: January 17, 2013Inventors: Jeffrey Michael Axten, Seth Wilson Grant, Dirk A. Heerding, Jesus Rual Medina, Stuart Paul Romeril, Jun Tang
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Publication number: 20130018044Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.Type: ApplicationFiled: December 21, 2010Publication date: January 17, 2013Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michel Pawlotsky
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Publication number: 20130018057Abstract: A series of quinoline and quinoxaline derivatives, substituted by a fused bicyclic pyridine or pyrimidine moiety attached via an alkylene chain optionally linked to a heteroatom, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.Type: ApplicationFiled: November 11, 2010Publication date: January 17, 2013Applicant: UCB PHARMA S.A.Inventors: Roland Bürli, Alan Findlay Haughan, Mîzio Matteucci, Andrew Pate Owens, Gilles Raphy, Andrew Sharpe
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Patent number: 8354531Abstract: Dihydrothienopyrimidines of formula 1 and the pharmacologically acceptable salts, enantiomers, racemates, hydrates, or solvates thereof, which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.Type: GrantFiled: April 2, 2010Date of Patent: January 15, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Christoph Hoenke, Birgit Jung, Domnic Martyres, Peter Nickolaus, Pascale Pouzet
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Patent number: 8354415Abstract: Compounds of formula (I) are A2B wherein R1 and R2 are independently selected from hydrogen, or optionally substituted CrC6 alkyl, C1-C6alkoxy-(C1-C6)-alkyl, C3-C8 cycloalkyl, aryl, heteroaryl, aryl-(C1-C6)-alkyl, or heteroaryl-(C1-C6)-alkyl; or R?1 and R2 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R3 and R4 are independently selected from hydrogen, or optionally substituted C1-C6 alkyl, C1-C6 alkoxy-(C1-C6)-alkyl, C3-C8 cycloalkyl, aryl, heteroaryl, aryl-(C1-C6)-alkyl, or heteroaryl-C1-C6)-alkyl; or R3 and R4 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R5 and R6 are independently selected from hydrogen, C1-C6 alkyl, aryl, aryl-(C1-C6)-alkyl, —NHR7—N(—R8)—R9, —NH—(C?O)—R10, —(C?O)—NH—R11, —(C?O)—O—R12, or halo; and R7, R8, R9, R10, R?11, and R12 are independently selected from C1-C6 alkyl, aryl, aryl-(C1-C6)-alkyl and heteroaryl.Type: GrantFiled: September 19, 2008Date of Patent: January 15, 2013Assignee: Vernalis (R&D) Ltd.Inventors: Allan Jordan, Simon Bedford, Klenke Burkhard, Ian Yule, Karine Poullennec
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Publication number: 20130012703Abstract: Disclosed are a 2,4,7-substituted thieno[3,2-d]pyrimidine compound having a protein kinase inhibition activity, a pharmaceutically acceptable salt, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth comprising the compound as an effective ingredient. Since the novel 2,4,7-substituted thieno[3,2-d]pyrimidine compound exhibits superior inhibition activity against various protein kinases involved in growth factor signal transduction, it is useful as an agent for preventing or treating diseases caused by abnormal cell growth.Type: ApplicationFiled: October 22, 2010Publication date: January 10, 2013Inventors: Tae Bo Sim, Jung Mi Hah, Hwan Geun Choi, Young Jin Ham, Jung Hun Lee, Dong Sik Park, Hwan Kim
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Publication number: 20120329808Abstract: The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.Type: ApplicationFiled: July 5, 2007Publication date: December 27, 2012Applicant: Array Biopharma Inc.Inventors: Ian S. Mitchell, James F. Blake, Rui Xu, Nicholas C. Kallan, Dengming Xiao, Keith Lee Spencer, Josef R. Bencsik
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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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Publication number: 20120322797Abstract: Compounds, compositions and methods are provided that comprise selective ?-glucuronidase inhibitors for both aerobic and anaerobic bacteria, especially enteric bacteria normally associated with the gastrointestinal tract. The compounds, compositions and methods can be for inhibiting bacterial ?-glucuronidases and for improving efficacy of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds by attenuating the side effects caused by reactivation by bacterial ?-glucuronidases of glucuronidated metabolites of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds.Type: ApplicationFiled: December 9, 2010Publication date: December 20, 2012Applicants: THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL, NORTH CAROLINA CENTRAL UNIVERSITY, ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITYInventors: Matthew R. Redinbo, Sridhar Mani, Alfred Williams, John Scott, Li-An Yeh, Bret David Wallace, Kimberly Terry Lane
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Publication number: 20120316184Abstract: Compounds of formula (I) wherein G1 represents together with the two ring atoms of the pyrimidine ring to which it is attached, a 5- to 6-membered aromatic heterocyclic ring system which contains one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the other substituents are as defined in claim 1, are suitable for use as micro-biocides.Type: ApplicationFiled: February 18, 2011Publication date: December 13, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Martin Pouliot, David Guillaume Claude Francois Lefranc, Laura Quaranta, Clemens Lamberth, Nityakalyani Srinivas
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Patent number: 8329701Abstract: The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula (I): Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.Type: GrantFiled: July 5, 2007Date of Patent: December 11, 2012Assignee: Array Biopharma Inc.Inventors: Ian S. Mitchell, James F. Blake, Rui Xu, Nicholas C. Kallan, Dengming Xiao, Keith Lee Spencer, Josef R. Bencsik
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Publication number: 20120309773Abstract: The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for suppressing an immune response or treating cancer or a hematologic malignancy using compounds of formula I.Type: ApplicationFiled: December 22, 2010Publication date: December 6, 2012Inventors: Yarlagadda S. Babu, Pravin L. Kotian
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Publication number: 20120309739Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: ApplicationFiled: November 3, 2010Publication date: December 6, 2012Applicant: ALMAC DISCOVERY LIMITEDInventors: Mark Peter Bell, Colin Roderick O'Dowd, James Samuel Shane Rountree, Graham Peter Trevitt, Timothy Harrison, Mary Melissa McFarland
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Publication number: 20120308588Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, a, R4, R5, and R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: May 18, 2012Publication date: December 6, 2012Applicant: THERAVANCE, INC.Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
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Patent number: 8324222Abstract: The present application relates to novel, cyclically substituted furopyrimidine derivatives, methods for their production, their use for the treatment and/or prophylaxis of diseases and their use for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular diseases.Type: GrantFiled: December 8, 2006Date of Patent: December 4, 2012Assignee: Bayer Intellectual Property GmbHInventors: Thomas Lampe, Eva-Maria Becker, Raimund Kast, Hartmut Beck, Mario Jeske, Joachim Schuhmacher, Friederike Stoll, Martina Klein, Metin Akbaba, Andreas Knorr, Johannes-Peter Stasch, Lars Bärfacker, Alexander Hillisch, Gunter Karig, Mark Meininghaus, Karl-Heinz Schlemmer, Rudolf Schohe-Loop
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Patent number: 8324223Abstract: This application concerns certain 4-cyanophenylamino-substituted bicyclic heterocycles of formula I where the dashed line represents a double bond that may be located either between A and C(V) or between C(V) and D, where A is S or C(Z); D is S or C(W); provided that one and only one of A and D is S; where T is NH, O, or S; and where other substituents are defined herein. These compounds are non-nucleoside reverse transcriptase inhibitors and have potential as anti-HIV treatment.Type: GrantFiled: May 11, 2012Date of Patent: December 4, 2012Assignee: Ardea Biosciences, Inc.Inventors: Jean-Luc Girardet, Zhi Hong, Stephanie Shaw, Yung-hyo Koh
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Patent number: 8324227Abstract: The present invention discloses novel compounds of the Formula (1), containing thieno-[2,3-d]pyrimidin-4(3H)-one moieties and pharmaceutically acceptable salts thereof, methods for preparing these compounds, the use of these compounds in prevention and treatment of fungal infections, and pharmaceutical preparations containing these novel compounds.Type: GrantFiled: September 5, 2008Date of Patent: December 4, 2012Assignee: FDC LimitedInventors: Hanumant Bapurao Borate, Suleman Riyajsaheb Maujan, Sangmesher Prabhakar Sawargave, Sheerang Vidhyadhar Joshi, Sharangi Vaiude, Mohan Anand Chandavarkar
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Publication number: 20120302567Abstract: The present invention relates to a novel bicyclic heteroaryl derivative, a pharmaceutically acceptable salt thereof, a hydrate thereof, and a solvate thereof having an improved inhibitory activity for protein kinases, and a pharmaceutical composition for preventing or treating an abnormal cell growth disorder comprising same as an active ingredient.Type: ApplicationFiled: January 28, 2011Publication date: November 29, 2012Applicants: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY, HANMI PHARM. CO. LTD.Inventors: Seung Hyun Jung, Young Hee Jung, Wha Il Choi, Jung Beom Son, Eun Ju Jeon, In Ho Yang, Tae Hun Song, Mi Kyoung Lee, Myoung Sil Ko, Young Gil Ahn, Maeng Sup Kim, Young Jin Ham, Tae Bo Sim, Hwan Geun Choi, Jung Mi Han, Dong-sik Park, Hwan Kim
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Publication number: 20120295924Abstract: The present invention is related to novel thienopyrimidinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.Type: ApplicationFiled: March 23, 2010Publication date: November 22, 2012Applicant: Glenmark Pharmaceuticals S.A.Inventors: Sukeerthi Kumar, Abraham Thomas, Nayan Taterao Waghmare, Sanjay Margal, Neelima Khairatkar-Joshi, Indranil Mukhopadhyay
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Publication number: 20120289474Abstract: The compounds of Formula (1), in which A, R1, R2, R3 and R5 have the meanings as given in the description, are novel effective inhibitors of type 4 and 5 phosphodiesterase.Type: ApplicationFiled: December 15, 2010Publication date: November 15, 2012Applicant: NYCOMED GMBHInventors: Dieter Flockerzi, Thomas Stengel, Alexander Mann, Harald Ohmer, Ulrich Kautz, Steffen Weinbrenner, Stefan Fischer, Christof Zitt, Armin Hatzelmann, Torsten Dunkern, Christian Hesslinger, Thomas Maier, Hermann Tenor, Clemens Braun, Raimund Külzer, Degenhard Marx
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Publication number: 20120289522Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: ApplicationFiled: October 1, 2010Publication date: November 15, 2012Inventors: Thomas J. Seiders, Lucy Zhao, Jeannie Arruda, Bowei Wang, Brian Andrew Stearns, Yen Pham Truong, Jill Melissa Scott, John Howard Hutchinson, Ryan Clark, Heather Renee Coate, Nicholas Simon Stock, Deborah Volkots
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Publication number: 20120277424Abstract: Disclosed are a 2,7-substituted thieno[3,2-d]pyrimidine compound having a protein kinase inhibition activity, a pharmaceutically acceptable salt, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth comprising the compound as an effective ingredient. Since the novel 2,7-substituted thieno[3,2-d]pyrimidine compound exhibits superior inhibition activity against various protein kinases involved in growth factor signal transduction, it is useful as an agent for preventing or treating diseases caused by abnormal cell growth.Type: ApplicationFiled: October 15, 2010Publication date: November 1, 2012Applicant: Korea Institute of Science and TechnologyInventors: Tae Bo Sim, Hwan Geun Choi, Jung Mi Hah, Young Jin Ham, Eun Jin Jun, Jung Hun Lee, Hwan Kim
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Publication number: 20120270855Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.Type: ApplicationFiled: April 25, 2012Publication date: October 25, 2012Inventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
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Patent number: 8293729Abstract: New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein R1, R2, R3, n, p, q, and Ar are as defined herein, including stereoisomers, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising a compound of this invention, as well as methods relating to the use thereof in a patient in need thereof.Type: GrantFiled: June 23, 2010Date of Patent: October 23, 2012Assignees: Boehringer Ingelheim International GmbH, Neurocrine Biosciences Inc.Inventors: Brian Dyck, Joe A. Tran, Junko Tamiya, Florence Jovic, Troy Vickers, Chen Chen, Nicole Harriott, Timothy Coon, Neil J. Ashweek
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Patent number: 8293754Abstract: This invention provides thienopyrimidine derivatives of the formula, wherein R1 stands for hydrogen atom, an alkyl group or the like; R2 stands for a hydrogen atom, an alkyl or amino group or the like, R3 stands for an alkyl, alkenyl or alkylthio group or the like or a group Y—X—; or R2 and R3 may together form tetramethylene group; X standing for a direct bond or linking group such as CH2, CH(OH), S, O, NH; Y standing for a substituted or unsubstituted aromatic carbocycylic, aromatic heterocylic, cycloalkyl or saturated heterocyclic group or the like; Z stands for S or O, and n is 0 or an integer of 1 to 4, or salts thereof, which exhibit an inhibitory effect on PDE9, and are therefore useful for prevention or treatment of overactive bladder syndrome, pollakiuria, urinary incontinence, dysuria associated with prostatic hyperplasia, urolithiasis, Alzheimer's disease, chronic obstructive pulmonary disease, myocardial infarction, thrombosis, diabetes and the like.Type: GrantFiled: June 13, 2006Date of Patent: October 23, 2012Assignee: Aska Pharmaceutical Co., Ltd.Inventors: Kotaro Gotanda, Atsushi Shinbo, Youichi Nakano, Hideo Kobayashi, Makoto Okada, Akira Asagarasu
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Patent number: 8293769Abstract: Benzoxazole and benzothiazole compounds and their oxides, esters, prodrugs, solvates, and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF 1R.Type: GrantFiled: May 20, 2008Date of Patent: October 23, 2012Assignee: Novartis AGInventors: Simon C. Ng, Keith B. Pfister, Martin Sendzik, James Sutton, Allan S. Wagman, Marion Wiesmann
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Publication number: 20120264768Abstract: Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed.Type: ApplicationFiled: February 2, 2012Publication date: October 18, 2012Inventor: Aleem Gangjee
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Publication number: 20120264760Abstract: One aspect of the present invention relates to compounds, and pharmaceutically acceptable salts and prodrugs thereof, that are useful as inhibitors of IMPDH. The invention also provides pharmaceutical compositions comprising the compounds of the invention which selectively inhibit parasitic IMPDH. In certain embodiments, the present invention relates to selective inhibition of C. parvum inosine-5?-monophosphate-dehydrogenase over human inosine-5?-monophosphate-dehydrogenase (IMPDH type I and type II). These compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.Type: ApplicationFiled: June 6, 2012Publication date: October 18, 2012Applicants: University of Georgia Research Foundation, Inc., Brandeis UniversityInventors: Lizbeth K. Hedstrom, Boris Striepen
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Publication number: 20120264751Abstract: Pyrrole pyrazole compounds of formula I, compositions including these compounds and methods of their use are provided. Preferred compounds of formula I have activity as protein kinase inhibitors, including as inhibitors of PAK4.Type: ApplicationFiled: October 6, 2011Publication date: October 18, 2012Inventors: Junhu ZHANG, Chuangxing Guo, Djamal Bouzida, Liming Dong, Haitao Li, Joseph Timothy Marakovits, Anle Yang, Yufeng Hong
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Publication number: 20120252667Abstract: Insecticidal 4-Amino-thieno[2,3-d]-pyrimidine compounds and methods of their use to control pests that damage plants and crops and parasites that harm animals. The present invention relates to new insecticidal 4-Amino-thieno[2,3-d]-pyrimidine compounds and new methods of their use. The new 4-Amino-thieno[2,3-d]-pyrimidine derivatives have the general formula I: wherein X, R1, R2, R3 and A are defined as in the description. The invention relates also to their enantiomer, diastereomer or agriculturally or veterinary acceptable salt thereof. The invention relates also to agricultural and veterinary compositions comprising such compounds. The invention relates further also to different insecticidal methods applying such compounds and compositions.Type: ApplicationFiled: July 29, 2010Publication date: October 4, 2012Inventors: Mark David Soll, Charles Meng, Matthias Pohlman, Ernst Baumann, Ralph Paulini
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Publication number: 20120238544Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.Type: ApplicationFiled: April 25, 2012Publication date: September 20, 2012Inventors: James P. Edwards, Daneile K. Neff, Deborah M. Smith, Jennifer D. Venable
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Patent number: 8263764Abstract: The invention relates to cyclic hydrazone compounds, compositions including the cyclic hydrazone compounds and methods of using and methods of making thereof. The compounds (and compositions) are useful, inter alia, in modulating IL-12 production and processes mediated by IL-12.Type: GrantFiled: December 23, 2010Date of Patent: September 11, 2012Assignee: Synta Pharmaceuticals Corp.Inventors: Zachary Demko, Lijun Sun, Howard P. Ng
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Publication number: 20120214792Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.Type: ApplicationFiled: April 25, 2012Publication date: August 23, 2012Inventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
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Publication number: 20120214795Abstract: The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. Specially, the present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or salt thereof, and a medicament containing the compound or a prodrug thereof, which is an Smo inhibitor or an agent for the prophylaxis or treatment of cancer.Type: ApplicationFiled: August 25, 2010Publication date: August 23, 2012Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Hiroshi Banno, Toshio Tanaka, Satoshi Sasaki
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Publication number: 20120208829Abstract: 2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: ApplicationFiled: August 22, 2011Publication date: August 16, 2012Applicant: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Scott M. Capitosti, Jianjun Xu, Bertrand L. Chenard, Manuka Ghosh, Charles A. Blum
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Patent number: 8242123Abstract: The present invention relates to new insecticidal methods of using 4-Amino-5-chloro-thieno[2,3-d]-pyrimidine compounds of formula (I) wherein R1, R2, R3 and A are defined as in the description. The present invention relates to insecticidal methods of applying such compounds of formula (I), and to new derivatives of compounds of formula (I).Type: GrantFiled: May 15, 2007Date of Patent: August 14, 2012Assignee: Merial LimitedInventors: Ernst Baumann, Henricus Maria Martinus Bastiaans, Wolfgang von Deyn, Michael Puhl, Michael Rack, Douglas D. Anspaugh, Deborah L. Culbertson, Hassan Oloumi-Sadeghi
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Publication number: 20120202690Abstract: The present invention relates to substituted heterobicyclic carboxylic acid derivatives, as well as N-oxides and agriculturally acceptable salts thereof, and their use in controlling plant growth, particularly undesirable plant growth, in crops of useful plants. The invention extends to herbicidal compositions comprising such compounds, N-oxides and/or salts as well as mixtures of the same with one or more further active ingredients and/or a safener.Type: ApplicationFiled: October 8, 2010Publication date: August 9, 2012Applicant: SYNGENTA LIMITEDInventors: William Guy Whittingham, Caroline Louise Winn, Julie Evelyne Blanc, Shuji Hachisu, Matthew Brian Hotson, Harry Glithro