Ring Sulfur In The Bicyclo Ring System Patents (Class 546/114)
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Publication number: 20110207767Abstract: This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.Type: ApplicationFiled: November 3, 2009Publication date: August 25, 2011Inventors: Patrick Henry Beusker, Rudy Gerardus Elisabeth Coumans, Ronald Christiaan Elgrtsma, Wiro Michaël Petrus Bernardus Menge, Johannes Albertus Frederikus Joosten, Henri Johannes Spijker, Franciscus Marinus Hendrikus De Groot
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Patent number: 8003662Abstract: Compounds of Formula I and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula I and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: GrantFiled: January 30, 2007Date of Patent: August 23, 2011Assignee: Array BioPharma, Inc.Inventors: James F. Blake, Steven Boyd, Jason De Meese, John J. Gaudino, Allison L. Marlow, Jeongbeob Seo, Allen A. Thomas, Hongqi Tian
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Publication number: 20110201632Abstract: The present invention is directed to 2,5-disubstituted piperidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: ApplicationFiled: October 15, 2009Publication date: August 18, 2011Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, Izzat T. Raheem, Anthony J. Roecker, John D. Schreier
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Publication number: 20110201814Abstract: A method for producing a solid preparation containing a compound represented by the formula (I) below or a pharmacologically acceptable salt thereof, which comprises a step wherein a composition containing the compound represented by the general formula (I) below or a pharmacologically acceptable salt thereof is mixed, while applying mechanical stress to the composition. The compound of the formula (I) is as follows: The method results in improved dissolvability of the compound of the formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: December 6, 2007Publication date: August 18, 2011Applicants: Daiichi Sankyo Company Limited, Ube Industries, Ltd.Inventor: Tomoyuki Watanabe
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Patent number: 7999106Abstract: Processes for the preparation of clopidogrel hydrogen sulfate of polymorphic form I are described which include use of specific solvents and process measures to avoid formation of undesired by-products.Type: GrantFiled: April 19, 2005Date of Patent: August 16, 2011Assignee: KRKA, Tovarna Zdravil, D.D., Novo MestoInventors: Haifang Mao, Hongguang Qian, Chen Chen
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Patent number: 7994322Abstract: Disclosed herein are the improved processes for the preparation of different forms of (S)-(+)-Clopidogrel besylate, pharmaceutical compositions containing them and their use in medicine.Type: GrantFiled: August 28, 2006Date of Patent: August 9, 2011Assignee: Cadila Healthcare LimitedInventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Bipin Pandey, Mayank Ghanshyambhai Dave, Parind Narendra Dholakia
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Patent number: 7994321Abstract: There are provided compounds of the formula wherein R1, R2, R3, X, Y, Q, Ring A and Ring B are as described. The compounds exhibit activity as anticancer agents.Type: GrantFiled: July 20, 2007Date of Patent: August 9, 2011Assignee: Hoffmann-La Roche Inc.Inventors: David Joseph Bartkovitz, Yi Chen, Xin-Jie Chu, Kin-Chun Luk
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Patent number: 7994192Abstract: Novel bicyclic heteroaromatic compounds are provided that are inhibitors of bacterial methionyl tRNA synthetase (MetRS). Compounds of the invention generally have a left hand side chroman group or left hand side tetrahydroquinoline group and a right hand side thienopyridone group. Also disclosed are methods for their preparation and their use in therapy as antibacterial agents, particularly as anti-Clostridium difficile agents.Type: GrantFiled: September 11, 2007Date of Patent: August 9, 2011Assignee: Crestone, Inc.Inventors: Joseph Guiles, Xicheng Sun, Nebojsa Janjic, Sarah Strong
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Publication number: 20110190502Abstract: A process for the preparation of (S)-Clopidogrel free base or a pharmaceutically acceptable salt thereof by the racemization of the undesired (R)-Clopidogrel in the presence of a suitable base followed by resolution with camphor sulfonate salt and further treatment with an inorganic acid to yield the title compound.Type: ApplicationFiled: October 23, 2009Publication date: August 4, 2011Applicant: SANDOZ AGInventors: Shreerang Joshi, Sachin Bhuta, Raji Nair, Sanjukumar Salunke
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Publication number: 20110190334Abstract: The present invention relates to compounds of Formula I where R1a, R1b, X, R2a, R2b, W, R3, R4, and R5 are as defined herein as well as pharmaceutically acceptable salts thereof. The compounds have been shown to act as MEK inhibitors which may be useful in the treatment of hyperproliferative diseases, like cancer and inflammation.Type: ApplicationFiled: November 3, 2010Publication date: August 4, 2011Applicant: NOVARTIS AGInventors: Mark G. Bock, Dinesh Chikkanna, Clive McCarthy, Henrik Moebitz, Chetan Pandit
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Patent number: 7989625Abstract: The invention relates to novel thienopyridine derivatives of formula (I), wherein R1, R2, R3, R4 and Y have the meaning cited in claim 1, are HSP90-inhibitors and can be used for producing a medicament for treating illnesses, wherein the inhibition, regulation and/or modulation of HSP90 plays a roll.Type: GrantFiled: May 11, 2006Date of Patent: August 2, 2011Assignee: Merck Patent GmbHInventors: Hans-Michael Eggenweiler, Michael Wolf
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Publication number: 20110184177Abstract: The invention relates to compounds of the formula I: in which R1, R2, X, A, B, D and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.Type: ApplicationFiled: April 4, 2011Publication date: July 28, 2011Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Stephanie Hachtel, Juergen Dedio, Holger Heitsch, Werngard Czechtizky, Sven Grueneberg, Stephen J. Shimshock, Raymond W. Kosley, JR., Carolina L. Lanter, Hui Li, Rosy Sher, Aleksandra Weichsel
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Publication number: 20110184014Abstract: The present invention relates to new mGluR1 and mGluR5 receptor subtype preferring ligands of formula (I); wherein Y represents a substituent selected from hydrogen, methyl, fluoro, chloro, bromo, methoxy; Z is hydrogen or methyl; R is an optionally substituted heteroaryl, and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of pathological conditions which require the modulation of mGluR1 and mGluR5 receptors such as neurological disorders, psychiatric disorders, acute and chronic pain and neuromuscular dysfunctions of the lower urinary tract.Type: ApplicationFiled: December 19, 2006Publication date: July 28, 2011Inventors: Katalin Nogradi, Gyorgy Keseru, Attila Bielik, Tamas Gati, Krisztina Gal, Monika Vastag, Amrita Agnes Bobok
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Publication number: 20110182812Abstract: Imaging agents of formulas (I)-(V) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formulas (I)-(V) capable of binding to tau proteins and ?-amyloid peptides are presented herein. The invention also relates to methods of imaging A? and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formulas (I)-(V) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders.Type: ApplicationFiled: February 25, 2011Publication date: July 28, 2011Applicant: SIEMENS MEDICAL SOLUTIONS USA, INC.Inventors: Anna Katrin Szardenings, Wei Zhang, Hartmuth C. Kolb, Daniel Kurt Cashion, Gang Chen, Dhanalakshmi Kasi, Changhui Liu, Anjana Sinha, Eric Wang, Chul Yu, Umesh B. Gangadharmath, Joseph C. Walsh
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Patent number: 7985859Abstract: The invention relates to processes for the preparation of clopidogrel and salts thereof. The inventors have developed a process for preparing racemic clopidogrel by racemizing R(?) clopidogrel. The process includes the step of reacting R(?) clopidogrel with a powered anhydrous base in one or more solvents.Type: GrantFiled: May 29, 2008Date of Patent: July 26, 2011Assignee: Wockhardt Ltd.Inventors: Jagdish Shukla, Anjum Reyaz Khan, Arvind Merwade, Mohammad Jaweed Mukarram Siddiqui, Yatendra Kumar
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Publication number: 20110178070Abstract: The invention relates to PI3K/mTOR inhibiting compounds consisting of the formula: wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: June 23, 2009Publication date: July 21, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Xianchang Gong, Bohan Jin, Massaki Hirose, Feng Zhou, Qing Dong
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Patent number: 7982040Abstract: The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.Type: GrantFiled: December 24, 2008Date of Patent: July 19, 2011Assignee: Nanotherapeutics, Inc.Inventors: Dale S. Dhanoa, Oren Becker, Silvia Noiman, Pradyumna Mohanty, Dongli Chen, Mercedes Lobera, Laurence Wu, Yael Marantz, Boaz Inbal, Alexander Heifetz, Shay Bar-Haim, Sharon Shacham
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Patent number: 7977351Abstract: The present invention provides a compound represented by the formula: wherein the variables R1, b, R6, Y, Z, X, R and a are defined in the specification. Said compound may be used in a method for treating diseases related to unregulated tyrosine kinase signal transduction, wherein said disease is selected from the group consisting of cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders, and metabolic diseases.Type: GrantFiled: March 16, 2007Date of Patent: July 12, 2011Assignee: Allergan, Inc.Inventors: Sougato Boral, Xialing Guo, Shimiao Wang, Julie A. Wurster, Thomas C. Malone
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Publication number: 20110166354Abstract: The present application relates to a method for producing an optically active ?-amino acid derivative, comprising steps of reacting an ?-haloester derivative represented by the general formula (1): of which alcohol part of the ester group is an optically active alcohol derivative, with an amine compound; then deprotecting the obtained compound; further carrying out an ester exchange reaction. According to the present invention method, it is possible to easily produce an optically active ?-amino acid ester derivative which is useful as an intermediate for drugs with high selectivity.Type: ApplicationFiled: June 2, 2009Publication date: July 7, 2011Inventors: Shohei Yamamoto, Akio Fujii, Masaru Mitsuda
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Patent number: 7973051Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R3 have the significance given in claim 1 and which can be used in the form of pharmaceutical compositions.Type: GrantFiled: November 10, 2008Date of Patent: July 5, 2011Assignee: Hoffman-La Roche Inc.Inventors: Paul Hebeisen, Eric A. Kitas, Rudolf E. Minder, Peter Mohr, Hans Peter Wessel
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Patent number: 7973050Abstract: Novel compounds in enantiomeric excess that are inhibitors of bacterial methionyl synthetase (MetRS) are disclosed. Also disclosed are methods for their preparation and their use in therapy as antibacterial agents, and in particular their use in therapy for Clostridium difficile infection.Type: GrantFiled: September 11, 2007Date of Patent: July 5, 2011Assignee: Crestone, Inc.Inventors: Joseph Guiles, Xicheng Sun, Nebojsa Janjic, Sarah Strong, Albert Charles Gyorkos
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Publication number: 20110159563Abstract: Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.Type: ApplicationFiled: March 2, 2011Publication date: June 30, 2011Inventors: Genesis M. Bacani, Diego Broggini, Eugene Y. Cheung, Christa C. Chrovian, Xiaohu Deng, Anne M. Fourie, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Jimmy T. Liang, Susanne Lochner, Neelakandha S. Mani, Alejandro Santillán, JR., Kathleen Sappey, Kia Sepassi, Virginia M. Tanis, Alvah T. Wickboldt, John J. M. Wiener, Hartmut Zinser
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Publication number: 20110152301Abstract: The present invention describes novel methods of identifying compounds which inhibit HIV particle formation and Rev-dependent HIV production. The present invention also provides methods and compounds for inhibiting HIV particle formation and or treating patients infected with HIV.Type: ApplicationFiled: December 22, 2010Publication date: June 23, 2011Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: David Rekosh, Marie-Louise Hammarskjöld
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Patent number: 7964612Abstract: The present invention provides for compounds of Formula I, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, and R7 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as therapeutic agents in the treatment of TGF?-mediated conditions, including cancer and fibrotic disorders. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.Type: GrantFiled: October 12, 2007Date of Patent: June 21, 2011Assignee: Graceway Pharmaceuticals, LLCInventors: Stephen D. Barrett, James B. Kramer, Mark L Boys, Huifen Chen
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Publication number: 20110144104Abstract: The present invention relates to pyrrolidinyl-alkyl-amide derivatives of formula (I) or (IA) wherein the variables are as defined herein, to their preparation and to their therapeutic use as CCR3 receptor ligands.Type: ApplicationFiled: January 26, 2011Publication date: June 16, 2011Applicant: SANOFI-AVENTISInventors: Agnes BEHR, Sandor BATORI, Veronika BARTANE BODOR, Zoltan SZLAVIK, Imre BATA, Katalin URBAN-SZABO, Zoltan KAPUI, Endre MIKUS
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Publication number: 20110144343Abstract: A process for the preparation of compounds of formula (I) or a salt thereof wherein X1, X2, X3, X4, Rx, u, R2, R1g, z, and A1 are as defined in the specification is disclosed.Type: ApplicationFiled: December 15, 2010Publication date: June 16, 2011Applicant: ABBOTT LABORATORIESInventors: Yu-Ming Pu, Alan Christesen, Steven Cullen, Yi-Yin Ku
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Patent number: 7960550Abstract: Processes for the preparation of Methyl (+)-(S)-(2-chlorophenyl)-(6,7dihydro-4H-thieno[3,2-c]pyridin-5-yl)acetate [Clopidogrel base, (I)] and their various pharmaceutically acceptable salts.Type: GrantFiled: January 8, 2007Date of Patent: June 14, 2011Assignee: Cadila Healthcare LimitedInventors: Parind Narendra Dholakia, Mayank Ghanshyambhai Dave, Pankaj Ramanbhai Patel
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Publication number: 20110135603Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. 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: October 15, 2010Publication date: June 9, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Tiansheng Wang, Alexander Aronov, Mark Cornebise, Francois Maltais, Mark Ledeboer, Arnaud Le Tiran, Valerie Marone, David Messesrsmith, Kevin Cottrell, Jon H. Come, Gabriel Martinez Botella
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Patent number: 7956068Abstract: The present invention relates to compounds of formula (I) wherein c, X, Y, R2, R3, R4 and R6 are as defined herein, compositions and uses thereof for treating human immunodeficiency virus (HIV) infection. In particular, the present invention provides novel inhibitors of HIV integrase, pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HIV infection.Type: GrantFiled: November 3, 2008Date of Patent: June 7, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Rebekah J. Carson, Lee Fader, Stephen Kawai, Serge R. Landry, Youla S. Tsantrizos, Christian Brochu, Sebastien Morin, Mathieu Parisien, Bruno Simoneau
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Publication number: 20110124675Abstract: The present invention provides the prasugrel bisulfate of formula (II) and pharmaceutical composition and use thereof. Prasugrel bisulfate of the present invention has good stability, oral absorbability, metabolic activity and platelet aggregation inhibition effect, and low toxicity, and is therefore a promising anticoagulant for preventing or treating diseases associated with thrombosis or embolism.Type: ApplicationFiled: July 31, 2008Publication date: May 26, 2011Inventor: Zhiquan Zhao
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Publication number: 20110124674Abstract: Disclosed are a compound of a formula (I) and its pharmaceutically-acceptable salt: wherein Q is CH or N; R1a, R1b, R1c and R1d are independently a C1-6 alkyl, a halo-C1-6 alkyl, etc.; R2 is a hydrogen atom, etc.; R3 is independently a hydrogen atom, a C1-6 alkyl, etc., or two R3's, taken together, form a bridge such as methylene, etc.; R4a and R4b are independently a hydrogen atom, a C1-6 alkyl, etc.; Z is a bicyclic aromatic hetero ring, etc.; Ar is a benzene ring, etc.; m1 and m2 are independently 0, 1 or 2; n is an integer of from 1 to 4. The compound and its salt act as a melanin concentrating hormone receptor antagonist, and are useful as a preventive or remedy for central system disorders, cardiovascular disorders, metabolic disorders, etc.Type: ApplicationFiled: July 14, 2009Publication date: May 26, 2011Inventors: Hiroyuki Kishino, Nagaaki Sato, Takao Suzuki
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Patent number: 7947692Abstract: There are presented compounds of the formula or a pharmaceutically acceptable salt thereof, which are active adenosine A2B receptor antagonists and useful in the treatment of diabetes, diabetic retinopathy, asthma and diarrhea.Type: GrantFiled: May 11, 2007Date of Patent: May 24, 2011Assignee: Hoffmann-La Roche Inc.Inventors: John A. Brinkman, Adrian Wai-Hing Cheung, Fariborz Firooznia, Kevin Richard Guertin, Nicholas Marcopulos, Lida Qi, Jagdish Kumar Racha, Ramakanth Sarabu, Jenny Tan, Jefferson Wright Tilley
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Publication number: 20110118303Abstract: The present invention relates to compounds derived from taurine with non-steroidal anti inflammatory activity. In a first embodiment, the present invention relates to compounds derived from taurine, in which taurine is bound directly by means of an amide bond or through an spacing group, to a compound selected from the group of non-steroidal anti inflammatory compounds, cited as derived from taurine presenting the Formula (I): in which R means the component with non-steroidal anti inflammatory activity. In a second embodiment, the invention provides a process for obtaining the compounds of Formula (I) by reaction of taurine with a compound belonging to the group of non-steroidal anti inflammatory (NSAIs), in order to obtain a compound derived from taurine by direct bond or through a spacing group of the taurine to the NSAI. The invention also relates to the pharmaceutical compositions comprising at least one compound derived from taurine presenting non-steroidal anti inflammatory activity.Type: ApplicationFiled: April 9, 2009Publication date: May 19, 2011Applicants: EMS S.A., Universidade Estadual Paulista Julio De Mesquita Filho - UNESPInventors: Ednir de Oliveira Vizioli, Chung Man Chin, Renato Farina Menegon, Lorena Blau, Jean Leandro Dos Santos, Maria do Carmo Longo
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Publication number: 20110118467Abstract: The present invention relates to a process for the preparation of clopidogrel and, more particularly, to an improved process for the preparation of clopidogrel hydrogen sulfate crystalline Form I by addition of dilute sulfuric acid to a solution of clopidogrel free base in butyl acetate.Type: ApplicationFiled: June 11, 2009Publication date: May 19, 2011Applicant: ZACH SYSTEM S.P.A.Inventors: Giorgio Soriato, Roberto Brescello, Daniele Urbani, Livius Cotarca
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Patent number: 7943637Abstract: Novel thienopyridine derivatives of the formula (I), in which R1, R2, R3 and Y have the meanings indicated in claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: GrantFiled: February 10, 2006Date of Patent: May 17, 2011Assignee: Merck Patent GmbHInventors: Hans-Michael Eggenweiler, Michael Wolf
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Patent number: 7939527Abstract: Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.Type: GrantFiled: April 9, 2009Date of Patent: May 10, 2011Assignee: Janssen Pharmaceutica NVInventors: Genesis M. Bacani, Diego Broggini, Eugene Y. Cheung, Christa C. Chrovian, Xiaohu Deng, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Jimmy T. Liang, Susanne Lochner, Neelakandha S. Mani, Alejandro Santillán, Jr., Kathleen Sappey, Kia Sepassi, Virginia M. Tanis, Alvah T. Wickboldt, John J. M. Wiener, Hartmut Zinser
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Patent number: 7935824Abstract: The invention relates a compound represented by the formula (1): Q1-Q2-C(?O)—N(R1)-Q3-N(R2)-T1-Q4??(1) wherein R1 and R2 represent H or the like; Q1 represents an aromatic ring, heterocyclic ring or the like; Q2 represents a single bond, aromatic ring, heterocyclic ring or the like; Q3 represents a group or the like, Q4 represents an aromatic ring, heterocyclic ring or the like; and T1 represents —CO— or —SO2—, and a medicine which comprises the compound and is useful for thrombosis and embolism.Type: GrantFiled: May 13, 2009Date of Patent: May 3, 2011Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Toshiharu Yoshino, Tsutomu Nagata, Noriyasu Haginoya, Kenji Yoshikawa, Hideyuki Kanno, Masatoshi Nagamochi
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Publication number: 20110098471Abstract: The present invention provides a novel antimicrobial drug comprising an oxazolidinone derivative of the formula (I): or a pharmaceutically acceptable salt or solvate thereof; wherein ring A is ring B is a benzene ring optionally substituted with lower alkyl; ring C is an optionally substituted six-membered heterocycle containing at least one nitrogen atom and one to three double bond(s) in the ling wherein the atom at the point of attachment to ring B is a carbon atom; ring D is an optionally substituted five-membered ring containing one or two double bond(s) in the ring; A1 and A2 are independently nitrogen or carbon; m is 0 or 1; R represents H, —NHC(?O)RA, —NHC(?S)RA, —NH-het1, —O-het1, —S-het1, —S(?O)-het1, —S(?O)2-het1, het2, —CONHRA, —OH, lower alkyl, lower alkoxy or lower alkenyl; and het1 and het2 are independently a heterocyclic group; with the proviso that the fused ring C-D is notType: ApplicationFiled: June 23, 2009Publication date: April 28, 2011Inventors: Issei Katoh, Toshiaki Aoki, Hideyuki Suzuki, Iwao Utsunomiya, Norikazu Kuroda, Tsutomu Iwaki
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Publication number: 20110098293Abstract: This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and opthalmological diseases, disorders and conditions.Type: ApplicationFiled: February 27, 2009Publication date: April 28, 2011Inventors: Michael Mannion, Stephane Raeppel, Stephen William Claridge, Frederic Gaudette, Lijie Zhan, Ljubomir Isakovic, Oscar Mario Saavedra, Tetsuyuki Uno, Masashi Kishida, Arkadii Vaisburg
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Patent number: 7932391Abstract: The present invention disclosed a preparation method of Clopidogrel (X=2?Cl) and its analogues of methyl tetrahydrothienopyridine acetate (I) by using halogen phenyl acetonitrile (VIII) as starting material and tetrahydrothienopyridine acetonitrile (IV), tetrahydrothienopyridine acetate (V) as key intermediates, and further using kinetic resolution to prepare the optical active Clopidogrel and compounds of methyl tetrahydrothenopridine acetate of formula (XII). The Clopidogrel of present invention is a novel high effective and safety drug for inhibition of platelet aggregation. This invention applied systematic technique of racemization of unwanted optical active enantiomer, recover recycle and reuse of resolution agent etc., with greater economic advantages and suitable for commercial scale industrial production. Wherein: X represents atoms of hydrogen, fluorine, chlorine, bromine or iodine, M represents an alkali metal ion.Type: GrantFiled: September 7, 2006Date of Patent: April 26, 2011Assignees: Zhejiang Hauhai Pharmaceutical Co., Ltd., Chengdu Organic Chemicals Co., Ltd., Chinese Academy of SciencesInventors: Lixin Wang, Yi Tang, Yi Chen, Fang Tian
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Patent number: 7932390Abstract: There are provided compounds of the formula wherein R1, R2, R3, X, ring A and ring B are as described. The compounds exhibit anticancer properties.Type: GrantFiled: June 18, 2007Date of Patent: April 26, 2011Assignee: Hoffman-La Roche Inc.Inventors: Yi Chen, Kin-Chun Luk, Pamela Loreen Rossman, Sung-Sau So
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Publication number: 20110087028Abstract: The present invention relates to a method for preparing Clopidogrel and its derivatives. More particularly, the present invention is a method for preparation of (S)-2-Clopidogrel and its derivatives, which are active inhibitors of platelet aggregation, from an optically active (S)-2-chlorophenyl glycine alkyl ester through hydrolysis of racemic 2-chlorophenylglycine alkyl esters using an enzyme. The present invention employs a simple procedure to prepare Clopidogrel and its derivatives. Because no chiral resolving agents are used except for a small amount of enzyme, the cost of preparation can be reduced. In addition, the present invention is suitable for synthesizing highly optical-active Clopidogrel and its derivatives on a large scale by using optically active (S)-2-chlorophenylglycine alkyl ester obtained in high yield as an intermediate, and is also environmentally friendly since no highly toxic reagents are employed.Type: ApplicationFiled: June 9, 2009Publication date: April 14, 2011Applicant: ENZYTECH LTD.Inventors: Soon Ook Hwang, Young Jin Kim
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Publication number: 20110085985Abstract: The present invention relates to novel amyloid binding compounds of formula (I) and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET/) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents.Type: ApplicationFiled: May 28, 2009Publication date: April 14, 2011Inventors: James C. Barrow, Scott Harrison, James Mulhearn, Cyrille Sur, David L. Williams, Scott Wolkenberg
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Publication number: 20110082136Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.Type: ApplicationFiled: June 8, 2009Publication date: April 7, 2011Inventors: Michelle Machacek, Gabriela de Almeida, Jonathan B. Grimm, Rachel N. MacCoss, Eric Romeo, Tony Siu, Catherine White, Kevin Wilson
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Publication number: 20110077265Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds having the general formula U1-M-U2 wherein M is a linking group covalently joining R2, R3, R4 or R5 of U1 to an R2, R3, R4 or R5 group of U2; U1 and U2 have the general formula (I) and G, X1, X2, R2, R3, R3?, R4, R4? and R5, are as described herein.Type: ApplicationFiled: April 29, 2008Publication date: March 31, 2011Applicant: Genentech, Inc.Inventors: John A. Flygare, Frederick Cohen, Kurt Deshayes, Michael F. T. Koehler, Lewis J. Gazzard, Lan Wang, Chudi Ndubaku
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Publication number: 20110077154Abstract: The present invention relates to pyridin-4-ylmethyl sulfonamides of formula I wherein Het, Ra, Rc, Rf, m, n, p, R, A and Y are as defined in the claims, to the N-oxides, and salts thereof and their use for combating harmful fungi, and also to compositions and seed comprising at least one such compound. The invention also relates to a process and intermediates for preparing these compounds.Type: ApplicationFiled: May 20, 2009Publication date: March 31, 2011Applicant: BASF SEInventors: Alice Glaettli, Wassilios Grammenos, Bernd Mueller, Jan Klaas Lohmann, Marianna Vrettou
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Publication number: 20110077240Abstract: This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and opthalmological diseases, disorders and conditions.Type: ApplicationFiled: December 9, 2010Publication date: March 31, 2011Inventors: Michael Mannion, Stéphane Raeppel, Stephen William Claridge, Frédéric Gaudette, Lijie Zhan, Ljubomir Isakovic, Oscar Mario Saavedra, Tetsuyuki Uno, Masashi Kishida, Arkadii Vaisburg
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Patent number: 7915417Abstract: Novel amino methylated 2-pyridinones, precursors, intermediates, and derivatives; the methods for the preparation of the same; uses of the same for inhibiting pili formation in bacteria; and pharmaceutical compositions comprising these compounds are described in this application. The present compounds may be employed to inhibit biofilm formation and thereby inhibit adherence of bacteria to a host cell.Type: GrantFiled: August 11, 2008Date of Patent: March 29, 2011Assignee: Washington UniversityInventors: Scott J. Hultgren, Jerome S. Pinkner, Fredrik Almqvist, Nils Pemberton, Veronica Aberg, Andreas Larsson
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Publication number: 20110071147Abstract: Disclosed are novel 4-amino-thieno[3,2-c]pyridine-7-carboxylic acid amides, and their pharmaceutically acceptable salts and esters, that are selective inhibitors of KDR and/or FGFR kinases. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular solid cancerous tumors of the breast, colon, lung and prostate. Also disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer using these compounds.Type: ApplicationFiled: November 23, 2010Publication date: March 24, 2011Inventors: Kin-Chun Luk, Lee Apostle McDermott, Pamela Loreen Rossman, Peter Michael Wovkulich, Zhuming Zhang
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Patent number: 7910740Abstract: The invention relates to compounds of formula wherein hetaryl I, hetaryl II, and R1 are as described herein. Compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease.Type: GrantFiled: May 5, 2008Date of Patent: March 22, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Karlheinz Baumann, Alexander Flohr, Helmut Jacobsen, Synese Jolidon, Thomas Luebbers