Acyclic Nitrogen Bonded Directly To A -c(=x)- Group, Wherein X Is Chalcogen Patents (Class 546/309)
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Publication number: 20120004228Abstract: There is provided compounds of formula I, wherein Y, ring A, Da, Db, D2, D3, L1, Y1, L2, Y2, L3 and Y3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.Type: ApplicationFiled: March 12, 2010Publication date: January 5, 2012Applicant: BIOLIPOX ABInventors: Peter Nilsson, Benjamin Pelcman, Martins Katkevics
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Publication number: 20110319627Abstract: Described herein are novel methods of preparing a compound of Formula II or a pharmaceutically acceptable salt thereof. In some embodiments, the method is for preparing betrixaban or a pharmaceutically acceptable salt thereof. Also described are compositions comprising substantially pure betrixaban free base or salt thereof.Type: ApplicationFiled: December 15, 2010Publication date: December 29, 2011Inventors: Anjali Pandey, Emilia P. T. Leitao, Jose Rato, Zhiguo Jake Song
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Publication number: 20110319454Abstract: The invention provides well defined compounds having FPRL-1 agonist or antagonist activity. As such, the compounds of the invention are useful for treating a variety of ocular disorders.Type: ApplicationFiled: June 24, 2011Publication date: December 29, 2011Applicant: ALLERGAN, INC.Inventors: Richard L. Beard, John E. Donello, Vidyasagar Voligonda, Michael E. Garst
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Patent number: 8084615Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.Type: GrantFiled: October 30, 2007Date of Patent: December 27, 2011Assignees: University of Washington, Novartis Vaccines and Diagnostics, Inc.Inventors: Niels H. Andersen, Jason Bowman, Alice L. Erwin, Eric A. Harwood, Toni Kline, Khisimuzi E. Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
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Publication number: 20110301179Abstract: A compound (particularly useful for inhibiting cancer) according to formula I: or a pharmaceutically acceptable salt thereof, wherein: x is 0 or 1; R1-R6 are each independently H, —CN, —NO2, —NO, —OH, halogen, hydroxyalkyl, carboxyl, substituted carboxyl, aminocarbonyl, alkoxy, carbonyl or substituted carbonyl; R7 is H, alkyl, alkyl amino, aminoacyl, hydroxyacyl, heteroaryl, heterocycloalkyl, alkyl heteroaryl or alkyl heterocycloalkyl; R8 is H or alkyl; A is O or N; and Ar is an aryl, substituted aryl, heteroaryl, or substituted heteroaryl, provided that if R7 is H then Ar is aryl substituted with alkyl amino.Type: ApplicationFiled: October 21, 2009Publication date: December 8, 2011Inventors: Xiangshu Xiao, Bingbing Li
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Publication number: 20110295018Abstract: The invention relates to a process for the synthesis of the diamine of formula (1) an important intermediate in the synthesis of dabiagtran etexilate.Type: ApplicationFiled: June 12, 2009Publication date: December 1, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ingo Heddesheimer, Ulrich Scholz
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Publication number: 20110263556Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.Type: ApplicationFiled: October 20, 2010Publication date: October 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Henri DOODS, Raimund KUELZER, Roland PFAU, Dirk STENKAMP, Robert ROENN, Benjamin PELCMAN
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Patent number: 8034819Abstract: A compound, or a pharmaceutically acceptable salt thereof, represented by the formula (1), (wherein, the carbon atom marked with an * is in the R-configuration, R1 represents a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1-C6 alkyl group, or a C1-C6 alkoxy group, R2 represents a C3-C6 cycloalkylsulfanyl group, a C3-C6 cycloalkylsulfinyl group, or a C3-C6 cycloalkylsulfonyl group, and A represents a substituted or unsubstituted heteroaryl group).Type: GrantFiled: March 6, 2008Date of Patent: October 11, 2011Assignees: Kyorin Pharmaceutical Co., Ltd., Teijin Pharma LimitedInventors: Yasumichi Fukuda, Yoshikazu Asahina, Masanori Takadoi, Kohei Ohata, Tomohiro Ide, Fumiyoshi Kobayashi, Shinji Kobayashi, Kanji Komatsu, Masanori Yamamoto
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Patent number: 8030518Abstract: This invention is directed to compounds of formula I, where G is —O—, —S—, —C(g1)(g2)-, or —NH—, and n=1, 2, or 3. Such compounds modulate potassium channels. The compounds are useful for the treatment and prevention of diseases and disorders which are affected by modulation of potassium ion channels. One such condition is seizure disorders.Type: GrantFiled: November 28, 2007Date of Patent: October 4, 2011Assignee: Valeant Pharmaceuticals InternationalInventors: Huanming Chen, Jianlan Song, Jean-Michel Vernier, Jim Zhen Wu
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Patent number: 8022079Abstract: Novel compounds having the general formula (I) below: are useful in a wide variety of applications in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively are formulated into cosmetic compositions.Type: GrantFiled: September 18, 2009Date of Patent: September 20, 2011Assignee: Galderma Research & DevelopmentInventors: Laurence Clary, Etienne Thoreau, Michel Rivier, Jerome Aubert, Laurent Chantalat, Johannes Voegel
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Publication number: 20110224225Abstract: Compounds of general Formula (I): wherein R1, R2, R3, Ra, A, B and x are as defined herein are inhibitors of protein kinases in particular members of the cyclin-dependent kinase family and/or the glycogen synthase kinase 3 family and are useful in preventing and/or treating any type of pain, inflammatory disorders, cancer, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases, metabolic disorders, renal diseases, neurologic and neuropsychiatric diseases and neurodegenerative diseases.Type: ApplicationFiled: March 10, 2011Publication date: September 15, 2011Inventors: Lutz Zeitlmann, Andre Niestroj, Ulrich Heiser
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Publication number: 20110224266Abstract: A composition is provided having the formula where R1 in each occurrence is independently H or a C1-C4 hydrocarbon; R3 is H, and R4 is a moiety capable of crossing the blood brain barrier selected from the group consisting of: an amino acid, a peptide, transferrin, gluconate, lactate, citrate, malate, fumarate, benzoate, salicylate, pyruvate and propionate. The composition includes 4-aminopyridine and a transporter species which allows for improved transport of the aminopyridine across the blood brain barrier thereby reducing systemic side effects of aminopyridine administration.Type: ApplicationFiled: January 24, 2011Publication date: September 15, 2011Inventor: Landon C.G. Miller
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Patent number: 8013241Abstract: Disclosed is a novel ionic liquid gel electrolyte having high photoelectric conversion efficiency. Also disclosed are a novel dye-sensitized photoelectric conversion device using such an ionic liquid gel electrolyte, and a solar cell composed of such a dye-sensitized photoelectric conversion device. Specifically disclosed is an ionic liquid gel electrolyte obtained by gelling a liquid electrolyte by using an ionic organic oligomer gelling agent represented by the general formulae (1) and (2) below. Also specifically disclosed are a dye-sensitized photoelectric conversion device, wherein the ionic liquid gel electrolyte is arranged between a counter electrode and a dye-absorbed semiconductor substrate which is arranged in contact with a transparent conductive substrate, and a solar cell.Type: GrantFiled: October 16, 2006Date of Patent: September 6, 2011Assignee: National Institute of Advanced Industrial Science and TechnologyInventors: Nagatoshi Koumura, Koujirou Hara, Zhong-Sheng Wang, Masaru Yoshida, Nobuyuki Tamaoki
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Publication number: 20110213157Abstract: A compound represented by the following general formula (I): [wherein R1 represents hydrogen atom or a C1-6 alkyl group, A and B represent —(CH2)2—, —(CH2)3— or —(CH2)4—, X represents —N(R2)—CO— (R2 represents hydrogen atom or a C1-6 alkyl group), —CO—N(R3)— (R3 represents hydrogen atom or a C1-6 alkyl group), —C(R4)?C(R5)— (R4 and R5 represent hydrogen atom or a C1-6 alkyl group), or —N(R6)—SO2— (R6 represents hydrogen atom or a C1-6 alkyl group), and Ar represents an aryldiyl group or a heteroaryldiyl group], which has a retinoid action and is useful as an active ingredient of a medicament.Type: ApplicationFiled: August 14, 2008Publication date: September 1, 2011Applicant: RESEARCH FOUNDATION ITSUU LABORATORYInventors: Yohei Amano, Masayuki Noguchi, Koichi Shudo
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Patent number: 8003799Abstract: Compounds of general formula (I): in which n, G, Q1, Q2, X1, X2, Y and Z are as defined in the description, process for preparing these compounds, fungicidal compositions comprising these compounds, processes for treating plants by applying these compounds or compositions.Type: GrantFiled: January 5, 2001Date of Patent: August 23, 2011Assignee: Bayer SASInventors: Francisco Nieto-Roman, Jean-Pierre Vors, Alain Villier, Helene Lachaise, Adeline Mousques, Benoit Hartmann, Pierre Hutin, Jose Lorenzo Molina, Benoit Muller
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Publication number: 20110190256Abstract: Compounds which modulate the CB2 receptor are disclosed. The compounds are useful for treating CB2 receptor-mediated diseases such as pain.Type: ApplicationFiled: February 19, 2009Publication date: August 4, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, Monika Ermann, Innocent Mushi
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Publication number: 20110190282Abstract: The invention relates to compounds of general formula (I) wherein W, D, E, G, J, L, R1, R2, R3, R4, R5 and Y are as defined herein, and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for treating diseases associated with deregulated angiogenesis, such as cancer and skin and eye diseases.Type: ApplicationFiled: August 27, 2009Publication date: August 4, 2011Applicant: LEO PHARMA A/SInventors: Jakob Felding, Xifu Liang, Anne Marie Horneman, Tina Dahlerup Poulsen, Jens Christian Højland Larsen
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Publication number: 20110184032Abstract: The invention provides novel compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation.Type: ApplicationFiled: July 27, 2009Publication date: July 28, 2011Applicant: MERCK PATENT GMBHInventors: Andreas Goutopoulos, Henry Yu, Benny C. Askew, Jr., Lesley Liu-Bujalski
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Patent number: 7985862Abstract: The present invention aims to provide an iminopyridine derivative compound having an ?1D adrenergic receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like. The present invention provides a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.Type: GrantFiled: February 7, 2011Date of Patent: July 26, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Masato Yoshida, Nobuki Sakauchi
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Patent number: 7985863Abstract: The present invention aims to provide an iminopyridine derivative compound having an ?1D adrenergic receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like. The present invention provides a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.Type: GrantFiled: February 7, 2011Date of Patent: July 26, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Masato Yoshida, Nobuki Sakauchi
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Publication number: 20110178087Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreatic carcinomas), and mesotheliomas.Type: ApplicationFiled: March 30, 2011Publication date: July 21, 2011Applicant: Compass Pharmaceuticals LLC.Inventors: David Kanne, John Ward, Gary Look, X. Michael Wang, Diva Chan, Tina Lee, Donald R. James, Richard Gless, John Schullek, Charles Vacin
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Patent number: 7982044Abstract: The present invention aims to provide an iminopyridine derivative compound having an ?1D adrenergic receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like. The present invention provides a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.Type: GrantFiled: February 7, 2011Date of Patent: July 19, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Masato Yoshida, Nobuki Sakauchi
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Patent number: 7977367Abstract: The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R1, R2, R3, and R4 are as described herein.Type: GrantFiled: September 9, 2009Date of Patent: July 12, 2011Assignee: Pfizer IncInventors: John William Benbow, Jihong Lou, Jeffrey Allen Pfefferkorn, Meihua Mike Tu
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Publication number: 20110166161Abstract: This invention relates to novel heterocyclic carboxamide derivatives and salts thereof. More particularly, it relates to novel heterocyclic carboxamide derivatives and salts thereof which act as a ROCK inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of ROCK-related disease.Type: ApplicationFiled: September 17, 2009Publication date: July 7, 2011Applicant: Astellas Pharma Inc.Inventors: Takeshi Terasawa, Shinji Shigenaga, Shinji Itoh, Jun Maeda, Hideyuki Watanabe, Satoshi Kubo, Noe Iahii
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Publication number: 20110160163Abstract: 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 inhibitors of ZAP70. 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: ApplicationFiled: March 1, 2011Publication date: June 30, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: John Cochran, Vincent Galullo, Guy W. Bemis
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Publication number: 20110160211Abstract: A compound having a hypoglycemic effect is provided. The compound and a pharmaceutically acceptable salt thereof are useful for the treatment or prevention of diabetes, obesity, and the like. The compound is represented by the general formula (1): (wherein R1 and R2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1 to C6 alkyl group, a C1 to C6 alkoxy group, a C1 to C6 alkylsulfanyl group, a C1 to C6 alkylsulfinyl group, a C1 to C6 alkylsulfonyl group, or a C1 to C6 alkoxy-C1 to C6 alkylsulfonyl group, and A is a substituted or unsubstituted heteroaryl group).Type: ApplicationFiled: April 27, 2009Publication date: June 30, 2011Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Masanori Takadoi, Masanori Yamamoto
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Patent number: 7968577Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g.Type: GrantFiled: October 31, 2007Date of Patent: June 28, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Bingwei Vera Yang, Lidia M. Doweyko, Wayne Vaccaro, Tram N. Huynh, David R. Tortolani, T. G. Murali Dhar
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Patent number: 7968560Abstract: Novel compounds having the general formula (I) below: are useful in a wide variety of applications in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively are formulated into cosmetic compositions.Type: GrantFiled: September 21, 2009Date of Patent: June 28, 2011Assignee: Galderma Research & DevelopmentInventors: Laurence Clary, Etienne Thoreau, Michel Rivier, Jerome Aubert, Laurent Chantalat, Johannes Voegel
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Publication number: 20110152175Abstract: The invention provides dendrimeric compounds of the formula 1 comprising amino acids, wherein n is an integer of 1-4, T is an alkylidene —(CH2)2CONH(CH2)2- group, R2 is an —NH2 group or a moiety of a primary organic amine, and P is an amino acid and/or peptide moiety, wherein at least one hydrogen atom of at least one amino group is optionally replaced by a protective group, and a hyperbranched core compound of the formula 3, wherein T and R2 are as defined above. The invention provides also a process for the preparation of a dendrimeric compound and a hyperbranched core, wherein the process employs addition reactions of alkyl acrylate and a basic amino acid, and use of a hyperbranched core for the preparation of a dendrimeric compound comprising amino acids. The invention provides also use of dendrimeric compounds for the preparation of the medicament for inhibiting growth of bacterial cells, fungi and tumor cells.Type: ApplicationFiled: September 18, 2009Publication date: June 23, 2011Applicant: Instytut Chemii Organicznej Polska Akademia NaukInventors: Zofia Lipkowska, Piotr Polcyn, Andrzej Wojciech Lipkowski
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Publication number: 20110152323Abstract: The present invention discloses a group of histone deacetylase inhibitors and use thereof. The histone deacetylase inhibitors are useful in the treatment of malignant tumors and the diseases associated with differentiation and proliferation.Type: ApplicationFiled: June 9, 2009Publication date: June 23, 2011Applicants: JIANGSU GOWORTH INVESTMENT CO. LTD, SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRYInventors: Jianqi Li, Juan Feng, Wangping Cai
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Publication number: 20110130431Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: February 8, 2011Publication date: June 2, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Angela BERRY, Pier Francesco CIRILLO, Eugene Richard HICKEY, Doris RIETHER, David THOMSON, Renee M. ZINDELL, Nigel BLUMIRE, Chandana CHOWDHURY, Monika ERMANN, James Edward JENKINS, Innocent MUSHI, Christopher Francis PALMER, Malcolm TAYLOR
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Publication number: 20110124875Abstract: The present invention aims to provide an iminopyridine derivative compound having an ?1D adrenergic receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like. The present invention provides a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: February 7, 2011Publication date: May 26, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masato YOSHIDA, Nobuki Sakauchi
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Publication number: 20110124874Abstract: The present invention aims to provide an iminopyridine derivative compound having an ?1D adrenergic receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like. The present invention provides a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: February 7, 2011Publication date: May 26, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masato YOSHIDA, Nobuki Sakauchi
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Publication number: 20110105571Abstract: A compound of the formula (I) wherein the variables X1, X2, B, D, R1 to R7 including R3?, p, y, q, and z, are as defined or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed.Type: ApplicationFiled: January 6, 2011Publication date: May 5, 2011Applicant: ELI LILLY AND COMPANYInventors: Mark Donald Chappell, Charles Howard Mitch, Steven James Quimby, Miles Goodman Siegel
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Publication number: 20110105530Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: June 25, 2009Publication date: May 5, 2011Inventors: Natalie Dales, Zaihui Zhang, Jianmin Fu, Duanjie Hou, Shaoyi Sun, Vishnumurthy Kodumuru, Natalia Pokrovskaia
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Patent number: 7935715Abstract: Compound of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: July 23, 2007Date of Patent: May 3, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Angela Berry, Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, David S. Thomson, Monika Ermann, James Edward Jenkins, Innocent Mushi, Malcolm Taylor, Christopher Francis Palmer, Nigel Blumire
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Publication number: 20110098325Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain pyridine benzamide and pyrazine benzamide compounds (referred to herein as PDBA and PZBA compounds) which, inter alia, inhibit protein kinase D (PKD) (e.g., PKD1, PKD2, PKD3). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PKD, and in the treatment of diseases and conditions that are mediated by PKD, that are ameliorated by the inhibition of PKD, etc., including proliferative conditions such as cancer, etc.Type: ApplicationFiled: December 14, 2007Publication date: April 28, 2011Applicant: CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Tony Michael Raynham, Timothy Robin Hammonds, Mark David Charles, Grégoire Alexandre Pave, Caroline Heather Foxton, Wesley Peter Blackaby, Adrian Philip Stevens, Chukuemeka Tennyson Ekwuru
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Patent number: 7928123Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: September 13, 2007Date of Patent: April 19, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Angela Berry, Pier Francesco Cirillo, Doris Riether, David Thomson, Renee M. Zindell, Nigel Blumire, Chandana Chowdhury, Monika Ermann, James Edward Jenkins, Innocent Mushi, Christopher Francis Palmer, Malcolm Taylor
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Publication number: 20110082299Abstract: A method for the manufacture of dabigatran of formula VIII, in which the product of a reaction of 4-ethylamino-3-nitrobenzoic acid chloride with ethyl-3-(pyridin-2-ylamino)propanoate, is converted to the hydrochloride using a hydrogen chloride solution producing the compound of formula III-HCl, in which the nitro group is reduced by means of a reaction with sodium dithionite, and the resulting compound of formula IV is subjected to a reaction with [(4-cyanophenyl)amino] acetic acid and oxalic acid, the product of this reaction VI-oxal is then subjected to hydrolysis and a reaction with ammonium carbonate to produce the intermediate of formula VII-HCl, which is then converted to dabigatran by means of a reaction with hexyl chloroformate.Type: ApplicationFiled: March 10, 2009Publication date: April 7, 2011Inventors: Josef Jirman, Jindrich Richter, Petr Lustig
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Publication number: 20110065717Abstract: The present invention relates to novel substituted sulfoximine derivatives of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation.Type: ApplicationFiled: August 4, 2008Publication date: March 17, 2011Applicant: CADILA HEALTHCARE LIMITEDInventors: Vrajesh B. Pandya, Pankaj Ramanbhai Patel
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Publication number: 20110052552Abstract: Compositions containing neurogenic agents for inhibition of neuron death and inducing proliferation of neural cells are disclosedType: ApplicationFiled: November 4, 2010Publication date: March 3, 2011Inventors: Judith KELLEHER-ANDERSSON, Karl K. Johe
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Publication number: 20110053939Abstract: Pharmaceutical compositions comprising at least one compound of e.g. the formulas (Ie) and a pharmaceutically acceptable carrier which is useful in a medicine wherein the symbols and substituents have the following meaning—X— is e.g. and Y is e.g. or the pharmaceutically acceptable salts, esters or amides and prodrugs of the above identified compounds can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.Type: ApplicationFiled: November 8, 2010Publication date: March 3, 2011Applicant: REVOTAR BIOPHARMACEUTICALS AGInventors: Ewald M. AYDT, Remo Kranich
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MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
Publication number: 20110053958Abstract: The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.Type: ApplicationFiled: March 17, 2009Publication date: March 3, 2011Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Thuy-Anh Tran, Weichao Chen, Bryan A. Kramer, Abu J.M. Sadeque, Anna Shifrina, Young-Jun Shin, Pureza Vallar, Ning Zou -
Publication number: 20110039846Abstract: The present invention aims to provide an iminopyridine derivative compound having an ?1D adrenergic receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like. The present invention provides a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: April 22, 2009Publication date: February 17, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masato Yoshida, Nobuki Sakauchi, Ayumu Sato
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Publication number: 20110039892Abstract: The present invention aims to provide a compound having a superior selective ?1D adrenergic receptor antagonistic action and useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like. The present invention provides a compound represented by the formula (I) wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: April 21, 2009Publication date: February 17, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masato Yoshida, Yasuhisa Kohara, Nobuki Sakauchi, Ayumu Sato
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Patent number: 7888374Abstract: The present invention relates to compounds that are inhibitors of c-jun N-terminal kinase 1, 2, or 3 (JNK1, JNK2, or JNK3), compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by the activation of JNK1, JNK2 and JNK3.Type: GrantFiled: January 23, 2006Date of Patent: February 15, 2011Assignee: Abbott LaboratoriesInventors: Gang Liu, Hing L. Sham, Bruce G. Szczepankiewicz, Zhili Xin, Hongyu Zhao, Michael D. Serby, Bo Liu, Mei Liu
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Publication number: 20110034464Abstract: The present invention aims to provide an iminopyridine derivative compound having an ?1D adrenergic receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like. The present invention provides a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: October 7, 2010Publication date: February 10, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masato YOSHIDA, Nobuki Sakauchi, Ayumu Sato
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Patent number: 7884079Abstract: A composition is provided having the formula where R1 and R2 are each independently H or a C1-C4 hydrocarbon; R3 is H, and R4 is a moiety capable of crossing the blood brain barrier selected from the group consisting of: an amino acid, a peptide, transferrin, gluconate, lactate, citrate, malate, fumarate, benzoate, salicylate, pyruvate and propionate. The composition includes 4-aminopyridine and a transporter species which allows for improved transport of the aminopyridine across the blood brain barrier thereby reducing systemic side effects of aminopyridine administration.Type: GrantFiled: December 27, 2004Date of Patent: February 8, 2011Inventor: Landon C. G. Miller
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Publication number: 20110021562Abstract: The invention provides methods of treating Friedreich's ataxia using histone deacetylase inhibitors.Type: ApplicationFiled: May 4, 2010Publication date: January 27, 2011Applicant: THE SCRIPPS RESEARCH INSTUTEInventors: KAI JENSSEN, DAVID M. HERMAN, JOEL M. GOTTESFELD, RYAN BURNETT, C. JAMES CHOU
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Publication number: 20110009454Abstract: Disclosed is a composition for agricultural use, which is used for controlling or preventing plant diseases caused by plant pathogens. The composition for agricultural use contains a compound represented by formula (1), a salt thereof or a hydrate of the compound or the salt. (1) [In the formula, Z represents an oxygen atom, a sulfur atom or NRZ; and E represents a furyl group, a thienyl group, a pyrrolyl group, a tetrazolyl group, a thiazolyl group, a pyrazolyl group, a phenyl group or the like.Type: ApplicationFiled: February 27, 2009Publication date: January 13, 2011Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Yuichi Matsuzaki, Takashi Komori, Tohru Inoue