Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 546/284.1)
-
Patent number: 7829585Abstract: The present invention provides an antifungal agent that has superior antifungal action and is also superior in terms of physical properties, safety and metabolic stability. The present invention discloses a compound represented by the formula (I): (wherein X represents an oxygen atom, a sulfur atom or —NH—, R1 represents a hydrogen atom, a halogen atom, a cyano group, an amino group or a substituent, and R2 and R3 independently represent a hydrogen atom, a halogen atom, a hydroxyl group or a substituent, except for a case in which R2 and R3 are both hydrogen atoms), and an antifungal agent containing the above compound.Type: GrantFiled: March 29, 2006Date of Patent: November 9, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Kazutaka Nakamoto, Satoshi Inoue, Keigo Tanaka, Toru Haneda
-
Publication number: 20100267947Abstract: This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists.Type: ApplicationFiled: June 30, 2010Publication date: October 21, 2010Applicant: SCHERING CORPORATIONInventors: Tiruvettipuram K. Thiruvengadam, Anantha R. Sudhakar, Ngiap Kie Lim, Daw-long Kwok, George G. Wu, Tao Wang, Mingsheng Huang, Michael D. Green
-
Publication number: 20100249094Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: ApplicationFiled: March 10, 2010Publication date: September 30, 2010Inventors: Kap-Sun Yeung, Kyle E. Parcella, John A. Bender, Brett R. Beno, Katharine A. Grant-Young, Ying Han, Piyasena Hewawasam, John F. Kadow, Andrew Nickel
-
Publication number: 20100249176Abstract: The present invention is directed to heterocycle amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels 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 T-type calcium channels are involved.Type: ApplicationFiled: October 23, 2008Publication date: September 30, 2010Inventors: James C. Barrow, Thomas S. Reger, Youheng Shu, Zhi-Qiang Yang
-
Patent number: 7772256Abstract: The present invention relates to novel 2-heteroaryl substituted benzothiophene and benzofuran derivatives, precursors thereof, and therapeutic uses of such compounds, having the structural formula (Ia) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel 2-heteroaryl substituted benzothiophene and benzofuran derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents.Type: GrantFiled: March 5, 2008Date of Patent: August 10, 2010Assignee: Astrazeneca ABInventors: Erwan Arzel, Britt-Marie Swahn, David Wensbo
-
Publication number: 20100179137Abstract: [Solving Means] The present inventors have conducted extensive studies on an EP4 receptor agonist, and as a result, found that a novel pyridone compound characterized in that the 1-position in the pyridone ring is substituted with a group having an acidic group such as a carboxyl group and the 6-position is bonded with an aromatic ring group via lower alkyl, lower alkylene, ether, or thioether, has an excellent EP4 receptor agonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor agonistic action and a blood flow increasing action in the hindlimb of a rat, it is useful as a pharmaceutical, in particular, an agent for treating peripheral arterial occlusive disease.Type: ApplicationFiled: June 6, 2008Publication date: July 15, 2010Inventors: Takashi Kamikubo, Fukushi Hirayama, Masanori Miura, Yuriko Komiya, Takao Okuda, Keisuke Maki
-
Patent number: 7754739Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: GrantFiled: May 9, 2008Date of Patent: July 13, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Mark Miller, Brian Bear, Jinglan Zhou, Jason McCartney, Peter Grootenhuis
-
Patent number: 7741345Abstract: The invention is related to compounds of Formula I: or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: GrantFiled: July 19, 2007Date of Patent: June 22, 2010Assignee: Gilead Sciences, Inc.Inventors: Carina E. Cannizzaro, James M. Chen, Manoj C. Desai, Michael L. Mitchell, Sundaramoorthi Swaminathan, Lianhong Xu
-
Publication number: 20100137298Abstract: The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.Type: ApplicationFiled: June 13, 2008Publication date: June 3, 2010Applicant: WyethInventors: Jeremy Ian Levin, Thomas Saltmarsh Rush, III, Frank Lovering, Yonghan Hu, Jianchang Li, Wei Li, Jun Jun Wu, Rajeev Hotchandani, Jason Shaoyun Xiang, Xuemei Du, Derek Cecil Cole, Steve Yikkai Tam
-
Patent number: 7723380Abstract: The invention is related to compounds of Formula I: or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: GrantFiled: July 19, 2007Date of Patent: May 25, 2010Assignee: Gilead Sciences, Inc.Inventors: Carina E. Cannizzaro, James M. Chen, Manoj C. Desai, Michael L. Mitchell, Sundaramoorthi Swaminathan, Lianhong Xu, Zheng-Yu Yang
-
Publication number: 20100125073Abstract: The present invention relates to benzofuran and benzothiophene derivatives and compositions containing such compounds for the production of medicaments for the treatment of cancers of the central nervous system as monotherapy or combination with other agents.Type: ApplicationFiled: August 28, 2007Publication date: May 20, 2010Inventors: Olaf Weber, Verena Voehringer, Hans-Georg Lerchen, Frank-Thorsten Hafner, Joerg Keldenich, Karl-Heinz Schlemmer, Ursula Krenz, Bernd Riedl
-
Publication number: 20100123123Abstract: A thin-film transistor comprises a semiconducting layer comprising a semiconducting material selected from Formula (I) or (II): wherein X, R1, R2, R3, R4, R5 a, b, and n are as described herein. Semiconducting compositions of Formula (I) or (II) are also described.Type: ApplicationFiled: November 19, 2008Publication date: May 20, 2010Applicant: Xerox CorporationInventors: Yuning Li, Yiliang Wu, Ping Liu, Paul F. Smith
-
Publication number: 20100120760Abstract: A compound of the formula (I): as defined herein, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing a compound of the formula (I) for use in inhibiting hepatitis C virus polymerase and/or of treating or preventing an illness due to hepatitis C virus,Type: ApplicationFiled: March 25, 2008Publication date: May 13, 2010Applicant: ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGInventors: Uwe Koch, Angela Claire Mackay, Frank Narjes, Ian Stansfield
-
Publication number: 20100121062Abstract: A method of performing a chemical reaction includes reacting a compound selected from the group consisting of an organohalide and an organo-pseudohalide, and a protected organoboronic acid represented by formula (I) in a reaction mixture: R1—B-T ??(I); where R1 represents an organic group, T represents a conformationally rigid protecting group, and B represents boron having sp3 hybridization. When unprotected, the corresponding organoboronic acid is unstable by the boronic acid neat stability test. The reaction mixture further includes a base having a pKB of at least 1 and a palladium catalyst. The method further includes forming a cross-coupled product in the reaction mixture.Type: ApplicationFiled: September 25, 2009Publication date: May 13, 2010Applicant: The Board of Trustees of the University of IllinoisInventors: Martin D. Burke, David M. Knapp, Eric P. Gillis
-
Patent number: 7713999Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt thereof, wherein: the dotted line represents an optional single bond; ?represents an optional double bond, n is 0-2; Q is cycloalkyl, optionally substituted by R13 and R14; R13 and R14 are independently selected from (C1-C6)alkyl, (C3-C8)cycloalkyl, —OH, (C1-C6)alkoxy, R27-aryl(C1-C6)alkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, halogen and haloalkyl; or R13 and R14 together form a spirocyclic or a heterospirocyclic ring of 3-6 atoms, Het is a mono- or bi-cyclic optionally substituted heteroaryl group; and B is a bond, alkylene, or optionally substituted alkenylene or alkynylene, wherein the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administerinType: GrantFiled: April 10, 2007Date of Patent: May 11, 2010Assignee: Schering CorporationInventors: Samuel Chackalamannil, Martin C. Clasby, William J. Greenlee, Yuguang Wang, Yan Xia, Enrico P. Veltri, Mariappan V. Chelliah
-
Patent number: 7709505Abstract: Compound of formula (I) wherein A is selected from pyridin-2-yl or thiazol-2-yl and R1, R2 and R3 are as described in the specification and their use in the treatment or prevention of a disease or medical conditions mediated through glucokinase.Type: GrantFiled: November 13, 2003Date of Patent: May 4, 2010Assignee: AstraZeneca ABInventors: Darren McKerrecher, John Wall Rayner
-
Publication number: 20100093806Abstract: PDE4 inhibition is achieved by novel compounds, e.g., aminoindazole and aminobenzofuran analogs. The compounds of the present invention are of Formulas I and II: wherein R1, R2, R3, R4, R7 and R8 are as defined herein.Type: ApplicationFiled: December 17, 2009Publication date: April 15, 2010Inventors: Richard A. SCHUMACHER, Allen T. Hopper, Ashok Tehim
-
Publication number: 20100081658Abstract: Compounds having the formula I wherein R1, R2a, R2b, R2c, R3, Y and p are as defined herein and C2-C3 is a single or double bond are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: September 25, 2009Publication date: April 1, 2010Inventors: Elbert Chin, Jim Li, Francisco Xavier Talamas, Beihan Wang
-
Patent number: 7687631Abstract: This application discloses a novel process for the preparation of phosphonate esters useful as intermediates in the preparation of himbacine analogs, themselves useful as thrombin receptor antagonists. The chemistry taught herein can be exemplified by the following scheme: wherein R9 is selected from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms, and R11 is selected independently for each occurrence from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms and hydrogen, X2 is Cl, Br, or I; X3 is selected from Cl and Br; and PdLn is a supported palladium metal catalyst or a soluble heterogeneous palladium catalyst. The L-derivatizing reagent is a moiety which converts the alcohol functional group of compound 137D to any leaving group which can be displaced by a triorgano-phosphite phosphonating agent.Type: GrantFiled: June 29, 2007Date of Patent: March 30, 2010Assignee: Schering CorporationInventors: Kelvin H. Yong, Ilia A. Zavialov, Jianguo Yin, Xiaoyong Fu, Tiruvettipuram K. Thiruvengadam
-
Publication number: 20100062937Abstract: Benzanilides of the formula: in which X represents hydrogen, halogen, nitro, C1-6 alkylthio, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl or C1-6 alkylsulfonyloxy; Y represents halogen or C1-6 alkyl; R1 represents C1-6 alkyl, C1-6 alkylthio C1-6 alkyl, C1-6 alkylsulfinyl-C1-6 alkyl or C1-6 alkylsulfonyl-C1-6 alkyl; R2 represents hydrogen, C1-6 alkyl or C1-6 haloalkyl; R3 represents hydrogen or hydroxy; W represents CH or N; and Q represents optionally substituted phenyl or optionally substituted pyridyl wherein the substituent is at least one group selected from the group consisting of halogen, C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 haloalkylthio, C1-6 haloalkylsulfinyl and C1-6 haloalkylsulfoxy; provided that when R3 is hydroxy, R2 is not C1-6 alkyl, or when R2 is C1-6 haloalkyl, R3 is hydroxy, W is CH, and the substituents of Q are two or more C1-6 haloalkyl. Insecticides comprising the benzanilides are herein provided.Type: ApplicationFiled: June 2, 2006Publication date: March 11, 2010Applicant: BAYER CROPSCIENCE AGInventors: Katsuaki Wada, Tetsuya Murata, Katsuhiko Shibuya, Eiichi Shimojo
-
Publication number: 20100056796Abstract: The present invention relates to novel derivatives that are suitable as precursors to compounds that are useful for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. The compounds deriving from these precursors are useful in methods of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease by positron emission tomography (PET) as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents. Furthermore, the present invention also discloses the precursor compounds in crystalline form.Type: ApplicationFiled: August 20, 2009Publication date: March 4, 2010Applicant: ASTRAZENECA ABInventors: Seth Bjõrk, Peter Johnstrõm, Nils Anders Nilsson, Katinka Ruda, Per Magnus Schou, Britt-Marie Swahn, Vern Delisser
-
Publication number: 20100004208Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.Type: ApplicationFiled: February 2, 2007Publication date: January 7, 2010Applicant: BIONOMICS LIMITEDInventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn, Gabriel Kremmidiotis
-
Patent number: 7632861Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.Type: GrantFiled: November 7, 2008Date of Patent: December 15, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Joanne J. Bronson, Andrew P. Degnan, William D. Schmitz
-
Publication number: 20090306055Abstract: The present invention is directed to compounds represented by the formula (1): B-D-Z (1), wherein B represent the following formula (B-1), A represents an optionally substituted imidazole or pyrazole group; E represents the following formula (1a): X represents an oxygen atom, the formula: SOu, or the formula: N—R9; Y represents a carbon atom or a nitrogen atom; D represents an oxygen atom, a sulfur atom or the formula (1a); Z represents (a chroman-2-yl group, a chroman-4-yl group, a 2,3-dihydrobenzofuran-2-yl group, a 2,3-dihydrobenzofuran-3-yl group, etc.) which is substituted with NHR10 or OR11)] or pharmaceutically acceptable salts thereof, and to antioxidants, therapeutic agents for kidney diseases or cerebrovascular disorder, and retinal oxidative damage inhibitors, which include the compounds as the active ingredient.Type: ApplicationFiled: May 15, 2009Publication date: December 10, 2009Applicant: NIPPON SODA CO., LTD.Inventors: Nobuhiro Umeda, Nobuo Mochizuki, Seiichi Uchida, Mitsumasa Takada, Seiichi Ikeyama, Shiro Tsubokura, Yasuyuki Shiinoki, Fumie Shirato, Hiroko Moroe
-
Publication number: 20090306112Abstract: The invention is related to compounds of Formula I or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: July 19, 2007Publication date: December 10, 2009Applicant: Gilead Sciences, Inc.Inventors: Carina E. Cannizzaro, James M. Chen, Manoj C. Desai, Michael L. Mitchell, Sundaramoorthi Swaminathan, Lianhong Xu, Zheng-Yu Yang
-
Publication number: 20090281321Abstract: This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center.Type: ApplicationFiled: July 17, 2009Publication date: November 12, 2009Inventors: George Wu, Anantha R. Sudhakar, Tao Wang, Ji Xie, Frank Xing Chen, Marc Poirier, Mingsheng Huang, Vijay Sabesan, Daw-long Kwok, Jian Cui, Xiaojing Yang, Tiruvettipuram K. Thiruvengadam, Jing Liao, Ilia A. Zavialov, Hoa N. Nguyen, Ngiap Kie Lim
-
Publication number: 20090281138Abstract: The invention provides compounds of formula wherein R1, R3, L1, L2, G1, G2, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.Type: ApplicationFiled: November 14, 2008Publication date: November 12, 2009Applicant: AstraZeneca ABInventors: Johan Bylund, Marie E. Ek, Annika Kers, Gunnar Nordvall, Liselotte Ohberg, Jenny Viklund, Stefan Von Berg, Jorg Holenz, Katja Narhi, Daniel Sohn, Martin H. Johansson
-
Publication number: 20090274650Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: ApplicationFiled: February 12, 2009Publication date: November 5, 2009Inventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger, Ronald George Sherrill
-
Patent number: 7605158Abstract: The present invention provides a carbamoyl-type benzofuran derivative of the formula [1]: wherein Ring Z is a group of the formula: etc.; A is a single bond, and the like; Y is a cycloalkanediyl group, etc.; R4 and R5 are the same or different and each is an optionally substituted lower alkyl group, etc.; R1 is a halogen atom, etc.; Ring B of the formula: is an optionally substituted benzene ring; and R3 is a hydrogen atom. etc., or a pharmaceutically acceptable salt thereof, which is useful as an FXa inhibitor.Type: GrantFiled: September 24, 2004Date of Patent: October 20, 2009Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Takayuki Kawaguchi, Hidenori Akatsuka, Masamichi Morimoto, Tatsuya Watanabe, Toru Iijima, Jun Murakami
-
Publication number: 20090221644Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.Type: ApplicationFiled: June 29, 2006Publication date: September 3, 2009Inventors: Stuart Edward Bradley, Matthew Colin Thor Fyfe, Lisa Sarah Bertram, William Gattrell, Martin James Procter, Chrystelle Marie Rasamison, Colin Peter Sambrook-Smith, Vilasben Kanji Shah, David French Stonehouse, Simon Andrew Swain, Gerard Hugh Thomas
-
Publication number: 20090209511Abstract: The present invention provides a benzofuran derivative of the formula [1]: wherein x is a group of the formula: —N? or —CH?; Y is an optionally substituted amino group, an optionally substituted cycloalkyl group or an optionally substituted saturated heterocyclic group; A is a single bond, a carbon chain optionally having a double bond within or at the end(s) of the chain, or an oxygen atom; R1 is a hydrogen atom or a halogen atom; Ring B is an optionally substituted benzene ring; and R3 is a hydrogen atom, or a pharmaceutically acceptable salt thereof, which is useful as a medicament, especially as an activated blood coagulation factor X inhibitor.Type: ApplicationFiled: March 24, 2009Publication date: August 20, 2009Inventors: Takayuki Kawaguchi, Hidenori Akatsuka, Toru Iijima, Yasunori Tsuboi, Takashi Mitsui, Jun Murakami
-
Publication number: 20090192315Abstract: Methods for the synthesis of heterocyclic compounds including N-(3,5-dichloropyrid-4-yl)-4-difluoromethoxy-8-methanesulfonamido-dibenzo[b,d]furan-1-carboxamide and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: December 24, 2008Publication date: July 30, 2009Applicant: FOREST LABORATORIES HOLDINGS LIMITEDInventors: Gian-Luca Araldi, Melanie Ronsheim, Nhut Diep, Shao Hong Zhou
-
Patent number: 7563900Abstract: The present invention relates to a method of preparing N-(3,5-dichloropyrid-4-yl)-4-difluoromethoxy-8-methanesulfonamido-dibenzo[b,d]furan-1-carboxamide and pharmaceutically acceptable salts thereof, such as its sodium salt, and novel intermediate compounds useful in the synthesis of the aforementioned compound.Type: GrantFiled: October 13, 2005Date of Patent: July 21, 2009Assignee: Glenmark Pharmaceuticals S.A.Inventors: Balasubramanian Gopalan, Laxmikant A. Gharat, Batchu Chandrasekhar, Bijukumar G. Pillai
-
Publication number: 20090182143Abstract: The present invention relates to novel heterocyclic compounds, their analogs, their tautomers, their regioisomers, their stereoisomers, their enantiomers, their diastereomers, their polymorphs, their pharmaceutically acceptable salts, their appropriate N-oxides, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. The present invention more particularly relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the Formula (1), their analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxide, pharmaceutically acceptable solvates and the pharmaceutical compositions containing them.Type: ApplicationFiled: June 2, 2008Publication date: July 16, 2009Applicant: GLENMARK PHARMACEUTICALS, S.A.Inventors: Balasubramanian Gopalan, Laxmikant A. Gharat, Aftab D. Lakdawala, Usha Karunakaran
-
Publication number: 20090167162Abstract: A new class of dibenzothiophene and/or dibenzofuran-containing compounds are provided. The new compounds may be useful in organic light emitting devices, particularly as the host of an emissive layer having a host and an emissive dopant, or as a material in an enhancement layer.Type: ApplicationFiled: September 11, 2008Publication date: July 2, 2009Applicant: Universal Display CorporationInventors: Chun Lin, Alexey Dyatkin, Zeinab Elshenawy, Walter Yeager
-
Publication number: 20090170903Abstract: The invention provides inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are new ester derivatives, methods of preparing such compounds, compositions containing them, and therapeutic uses thereof.Type: ApplicationFiled: December 15, 2008Publication date: July 2, 2009Applicant: Chiesi Farmaceutici S.p.A.Inventors: Elisabetta ARMANI, Gabriele AMARI, Gino VILLETTI
-
Publication number: 20090149493Abstract: The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, s, t, R1, R2, A and Z have defined meanings.Type: ApplicationFiled: March 19, 2007Publication date: June 11, 2009Inventors: Jean Fernand Armand Lacrampe, Christophe Meyer, Bruno Schoentjes, Delphine Yvonne Raymonde Lardeau, Alain Philippe Poncelet, Luc Van Hijfte
-
Publication number: 20090143408Abstract: Methods of inhibiting cytochrome P450 2D6 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450 2D6. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 2D6 enzymes.Type: ApplicationFiled: November 26, 2008Publication date: June 4, 2009Applicant: Sequoia Pharmaceuticals, Inc.Inventors: Michael EISSENSTAT, Dehui Duan, Ji-Hye Kang
-
Publication number: 20090143593Abstract: Methods for the synthesis of heterocyclic compounds including N-(3,5-dichloropyrid-4-yl)-4-difluoromethoxy-8-methanesulfonamido-dibenzo[b,d]furan-1-carboxamide and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: February 12, 2009Publication date: June 4, 2009Applicant: FOREST LABORATORIES HOLDINGS LIMITEDInventors: Gian-Luca Araldi, Melanie Ronsheim, Nhut Diep, Shao Hong Zhou
-
Patent number: 7541471Abstract: The present invention relates to an improved process for preparing himbacine analogs. The compounds are useful as thrombin receptor antagonists. The improved process may allow for at least one of easier purification by crystallization, easier scalability, and improved process yield on the desired enantiomer.Type: GrantFiled: January 12, 2006Date of Patent: June 2, 2009Assignee: Schering CorporationInventors: Tiruvettipuram K Thiruvengadam, Tao Wang, Jing Liao, John S Chiu, David Jieh-Shyh Tsai, Hong-Chang Lee, Wenxue Wu, Xiaoyong Fu
-
Publication number: 20090131468Abstract: The invention provides compounds of formula wherein R1, R2, R3, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.Type: ApplicationFiled: November 14, 2008Publication date: May 21, 2009Applicant: AstraZeneca ABInventors: Johan Bylund, Marie E. Ek, Annika Kers, Gunnar Nordvall, Liselotte Ohberg, Jenny Viklund, Stefan Von Berg, Jorg Holenz, Katja Narhi, Daniel Sohn, Martin H. Johansson
-
Publication number: 20090124613Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.Type: ApplicationFiled: November 7, 2008Publication date: May 14, 2009Inventors: Joanne J. Bronson, Andrew P. Degnan, William D. Schmitz
-
Patent number: 7531537Abstract: The present invention provides a benzofuran derivative of the formula [1]: wherein x is a group of the formula: —N? or —CH?; Y is an optionally substituted amino group, an optionally substituted cycloalkyl group or an optionally substituted saturated heterocyclic group; A is a single bond, a carbon chain optionally having a double bond within or at the end(s) of the chain, or an oxygen atom; R1 is a hydrogen atom or a halogen atom; Ring B is an optionally substituted benzene ring; and R3 is a hydrogen atom, or a pharmaceutically acceptable salt thereof, which is useful as a medicament, especially as an activated blood coagulation factor X inhibitor.Type: GrantFiled: March 27, 2003Date of Patent: May 12, 2009Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Takayuki Kawaguchi, Hidenori Akatsuka, Toru Iijima, Yasunori Tsuboi, Takashi Mitsui, Jun Murakami
-
Publication number: 20090105279Abstract: The invention is related to compounds of Formula I: or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: July 19, 2007Publication date: April 23, 2009Inventors: Carina E. Cannizzaro, James M. Chen, Manoj C. Desai, Michael L. Mitchell, Sundaramoorthi Swaminathan, Lianhong Xu, Zheng-Yu Yang
-
Publication number: 20090093485Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).Type: ApplicationFiled: October 26, 2005Publication date: April 9, 2009Applicant: ASTRAZENECA ABInventors: Hakan Bladh, Krister Henriksson, Vijaykumar Hulikal, Matti Lepisto
-
Patent number: 7511150Abstract: Methods for the synthesis of heterocyclic compounds including N-(3,5-dichloropyrid-4-yl)-4-difluoromethoxy-8-methanesulfonamido-dibenzo[b,d]furan-1-carboxamide and pharmaceutically acceptable salts thereof.Type: GrantFiled: July 3, 2007Date of Patent: March 31, 2009Assignee: Forest Laboratories Holdings LimitedInventors: Gian-Luca Araldi, Melanie Ronsheim, Nhut Diep, Shao Hong Zhou
-
Publication number: 20090076088Abstract: A series of compounds represented by the structural formulas and pharmaceutically acceptable isomers, salts, solvates and polymorphs thereof are disclosed. Also disclosed are pharmaceutical compositions containing said compounds and their use as thrombin receptor antagonists and binders to cannabinoid receptors.Type: ApplicationFiled: October 30, 2008Publication date: March 19, 2009Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yan Xia
-
Publication number: 20090069383Abstract: A series of compounds represented by the structural formulas and pharmaceutically acceptable isomers, salts, solvates and polymorphs thereof are disclosed. Also disclosed are pharmaceutical compositions containing said compounds and their use as thrombin receptor antagonists and binders to cannabinoid receptors.Type: ApplicationFiled: October 30, 2008Publication date: March 12, 2009Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yan Xia
-
Publication number: 20090062348Abstract: The present invention provides an antifungal agent that has superior antifungal action and is also superior in terms of physical properties, safety and metabolic stability. The present invention discloses a compound represented by the formula (I): (wherein X represents an oxygen atom, a sulfur atom or —NH—, R1 represents a hydrogen atom, a halogen atom, a cyano group, an amino group or a substituent, and R2 and R3 independently represent a hydrogen atom, a halogen atom, a hydroxyl group or a substituent, except for a case in which R2 and R3 are both hydrogen atoms), and an antifungal agent containing the above compound.Type: ApplicationFiled: March 29, 2006Publication date: March 5, 2009Inventors: Kazutaka Nakamoto, Satoshi Inoue, Keigo Tanaka, Toru Haneda
-
Patent number: 7498349Abstract: Aromatic compounds exemplified by exhibit antimicrobial activity.Type: GrantFiled: August 1, 2003Date of Patent: March 3, 2009Assignee: Genesoft Pharmaceuticals, Inc.Inventors: Roland W. Burli, Eldon E. Baird, Jacob A. Kaizerman, Dustin L. McMinn