Nitrogen Or Chalcogen Attached Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/72)
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Publication number: 20110213003Abstract: This invention provides compounds of formula (I): wherein X1, X2, X3, R2, R4b, R1, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: February 25, 2011Publication date: September 1, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
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Publication number: 20110213156Abstract: A compound represented by the following general formula (I): [wherein R1 and R2 represent an alkyl group, X represents —S—, —O— or —NH—, Y represents C or N, R3 represents hydrogen atom or a C1-10 alkyl group, Z represents —CO—N(R5)— (R5 represents hydrogen atom or a C1-6 alkyl group) or —C(R6)?C(R7)—CO—NH— (R6 and R7 represent hydrogen atom or a C1-6 alkyl group), Ar represents an aryldiyl group or a heteroaryldiyl group, and R4 represents —COOH, —OCH2—COOH, —CH2—COOH, or —CH2—CH2—COOH], 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: Hideaki Muratake, Masayuki Noguchi, Koichi Shudo
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Publication number: 20110207945Abstract: Provided is a process for the preparation of enantiomerically pure 1-substituted-3-aminoalcohols, particularly of (S)-(?)- and (R)-(+)-3-N-methylamino-1-(2-thienyl)-1-propanol, by asymmetrically hydrogenating salts of a carboxylic acids with an aminoketone of formula (II), wherein R1 is selected from the group consisting of 2-thienyl, 2-furanyl and phenyl, each optionally substituted with one or more halogen atoms and/or one or more C1-4-alkoxy groups, and wherein R2 is C1-4-alkyl or phenyl, each optionally substituted with one or more halogen atoms and/or one or more C1-4-alkyl or C1-4-alkoxy groups, and wherein the corresponding aminoalcohols are obtained by subsequent hydrolysis of their salts. Furthermore provided are salts of a carboxylic acid with said aminoketones and the aminoalcohols obtained by asymmetrically hydrogenating said aminoketones, respectively.Type: ApplicationFiled: March 8, 2011Publication date: August 25, 2011Inventors: Dominique Michel, Hanspeter Mettler, John McGarrity
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Novel 1, 2-Disubstituted Amido-anthraquinone Derivatives, Preparation Method and application thereof
Publication number: 20110207739Abstract: A series of novel 1,2-disubstituted amido-anthraquinone derivatives, and the preparation method and application of said derivatives. Said application includes said derivatives with therapeutically effective amount being prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.Type: ApplicationFiled: February 25, 2010Publication date: August 25, 2011Inventor: Hsu-Shan HUANG -
Publication number: 20110178101Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: January 18, 2011Publication date: July 21, 2011Inventors: Paul R. Fatheree, Robert Murray McKinnell
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Publication number: 20110160207Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.Type: ApplicationFiled: March 2, 2011Publication date: June 30, 2011Inventors: Stephen T. Wrobleski, Jagabandhu Das, T.G. Murali Dhar, Alaric J. Dyckman, John Hynes, Katerina Leftheris, James Lin, Shuqun Lin
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Patent number: 7964735Abstract: Novel 3-acylaminobenzanilides of the formula (I) wherein R1 represents phenyl which may be substituted or a 5-member or 6-member heterocyclic ring group, which may be substituted, containing at least one hetero-atom selected from the group consisting of N, O, and S; R2 represents halogen, C1-6 alkyl, or C1-6 haloalkyl; R3 represents C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 haloalkylthio, C1-6 haloalkylsulfinyl, or C1-6 haloalkylsulfonyl; R4 represents halogen, C1-6 alkyl, or C1-6 haloalkyl; X represents halogen, C1-6 alkyl, or C1-6 haloalkyl; and n represents 0 or 1 and the compounds are used as insecticides, and a use of the new compounds as insecticides.Type: GrantFiled: July 21, 2006Date of Patent: June 21, 2011Assignee: Bayer Cropscience AGInventors: Akihiko Yanagi, Yukiyoshi Watanabe, Katsuaki Wada, Tetsuya Murata, Jun Mihara, Katsuhiko Shibuya, Eiichi Shimojo, Akira Emoto
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Publication number: 20110144189Abstract: The present invention relates to compounds having the formula: salts thereof; compositions comprising one or more of the compounds and/or salts thereof; methods of using; and methods of making.Type: ApplicationFiled: December 7, 2010Publication date: June 16, 2011Applicant: CYTOKINE PHARMASCIENCES, INC.Inventor: Thais SIELECKI-DZURDZ
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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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Patent number: 7935696Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.Type: GrantFiled: October 25, 2007Date of Patent: May 3, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Stephen T. Wrobleski, Jagabandhu Das, T. G. Murali Dhar, Alaric J. Dyckman, John Hynes, Katerina Leftheris, James Lin, Shuqun Lin
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Publication number: 20110092496Abstract: A compound represented by the formula (I) (wherein R1, R2, R3 and R4 are as defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.Type: ApplicationFiled: November 29, 2010Publication date: April 21, 2011Applicant: Nissan Chemical Industries, Ltd.Inventors: Katsuaki MIYAJI, Kazufumi Yanagihara, Yukihiro Shigeta, Shunsuke Iwamoto, Masato Horikawa, Yutaka Hirokawa, Shingo Owada, Satoshi Nakano, Hirofumi Ota, Norihisa Ishiwata
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Patent number: 7928250Abstract: A compound of formula 10 is useful in making duloxetine.Type: GrantFiled: December 20, 2007Date of Patent: April 19, 2011Assignee: Synthon BVInventors: Karel Pospisilik, Bohumil Dymacek
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Patent number: 7880020Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the formula (1) wherein: A is an aryl group; Q1 is an aryl leader group having a backbone of at least 2 carbon atoms; J is an amide linkage selected from: —NR1C(?O)— and —C(?O)NR1—; R1 is an amido substituent; and, Q2 is an acid leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. 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 HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psorias.Type: GrantFiled: June 3, 2009Date of Patent: February 1, 2011Assignee: Topotarget UK LimitedInventors: Clare J Watkins, Maria Rosario Romero-Martin, Kathryn G Moore, James Ritchie, Paul W Finn, Ivars Kalvinsh, Einars Loza, Igor Starchenkov, Klara Dikovska, Rasma M Bokaldere, Vija Gailite, Maxim Vorona, Victor Andrianov, Daina Lolya, Valentina Semenikhina, Andris Amolins, C. John Harris, James E S Duffy
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Publication number: 20110021771Abstract: This invention relates to compounds and methods for the inhibition of HDAC enzymatic activity. More particularly, the invention provides for compounds of formula (I), (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein L, M, n, R, W, X and Y are as defined in the specification.Type: ApplicationFiled: November 3, 2008Publication date: January 27, 2011Applicant: METHYLGENE INC.Inventors: Tammy Mallais, Oscar Moradei, Alain Ajamian, Pierre Tessier, David Smil, Sylvie Frechette, Roger Machaalani, Silvana Leit, Patrick Beaulieu, Robert Déziel, John Mancuso
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Publication number: 20110021528Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: ApplicationFiled: October 1, 2010Publication date: January 27, 2011Applicant: PHARMACYCLICS, INC.Inventors: Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
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Publication number: 20110009457Abstract: The invention relates to a composition comprising at least one aminobenzamide compound or a salt thereof for controlling animal parasites, veterinary pharmaceutical compositions comprising at least one aminobenzamide of formula (I) for preventing infection with diseases transmitted through parasites, its use for the preparation of a veterinary pharmaceutical for controlling animal parasites, and a method for preventing infection with diseases transmitted through parasites.Type: ApplicationFiled: December 9, 2008Publication date: January 13, 2011Applicant: BAYER CROPSCIENCE AGInventors: Ulrich Görgens, Katsuaki Wada, Yukiyoshi Watanabe, Jun Mihara, Koichi Araki
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Publication number: 20100297542Abstract: Compounds of the formula (I), wherein X is a single bond, CRaRb O, S, NRC, NCORC, CO, SO or SO2; L, L1, L2, L3, L4, L5, L6, L7 and L8 are for example hydrogen, R1 or COT; T denotes T1 or O-T2; T1 and T2 for example are hydrogen, C1-C20alkyl, C3-C12cycloalkyl, C2-C20alkenyl, C5-C12cycloalkenyl, C6-C14aryl, C3-C12heteroaryl, C1-C20alkyl substituted by one or more D, C2-C20alkyl interrupted by one or more E, C2-C20alkyl substituted by one or more D and interrupted by one or more E or Q; R1, R2, R3, R4, Ra, Rb and Rc are T1; D is for example R5, OR5, SR5 or Q1; E is for example O, S, COO or Q2; R5 and R6 for example are hydrogen, C1-C12alkyl or phenyl; Q is for example C6-C12bicycloalkyl, C6-C12bicycloalkenyl or C6-C12tricycloalkyl; Q1 is for example, C6-C14aryl or C3-C12heteroaryl; Q2 is for example C6-C14arylene or C3-C12heteroarylene; Y is an anion; and M is a cation; provided that at least one of L, L1, L2, L3, L4, L5, L6, L7 and L8 is other than hydrogen; and provided that (i) at least one of T1 or T2 is a gType: ApplicationFiled: September 29, 2008Publication date: November 25, 2010Applicant: BASF SEInventors: Pascal Hayoz, Hitoshi Yamato
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Patent number: 7829501Abstract: Conventional many fungicidal compositions have had practical problems such that either a preventive effect or a curing effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired.Type: GrantFiled: August 10, 2005Date of Patent: November 9, 2010Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Yuji Nakamura, Shigeru Mitani, Tetsuo Yoneda
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Publication number: 20100280036Abstract: The present invention relates to the use of compounds of the general Formula (I): wherein in Formula (I), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R1 is H, alkyl, cycloalkyl, aryl or heteroaryl; R2 is H, alkyl, cycloalkyl, aryl or heteroaryl; A1 and A2 each independently represent an optionally substituted C1-C20-alkyl group which may contain one or more group(s) Z, or a monocyclic or polycyclic optionally substituted aromatic or non-aromatic ring system which may contain one or more group(s) X, and in case of a polycyclic ring system, said system contains at least one aromatic ring; Z is selected from the group consisting of S, O, N, NR4, CO, CO2, CS, SO or SO2 X is selected from the group consisting of S, O, N, NR4, SO or SO2;Type: ApplicationFiled: December 28, 2007Publication date: November 4, 2010Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
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Publication number: 20100273835Abstract: The invention provides compounds of general formula (I) or a pharmaceutically acceptable salt, polymorph or solvate thereof, including all tautomers and stereoisomers thereof, wherein K, W, X; Y and Z are described throughout the description and claims. The compounds of the present invention are useful as inhibitors of prolyl endopeptidase (PEP, EC 3.4.21.26) and/or IL-6.Type: ApplicationFiled: July 10, 2008Publication date: October 28, 2010Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Andre J. Niestroj, Ingo Schulz
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Publication number: 20100261675Abstract: Conventional many fungicidal compositions have had practical problems such that either a preventive effect or a curing effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired.Type: ApplicationFiled: June 24, 2010Publication date: October 14, 2010Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Yuji Nakamura, Shigeru Mitani, Tetsuo Yoneda
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Publication number: 20100260778Abstract: Small-molecule inhibitors of Botulinum toxin, including BoNTA, BoNTD and BoNTE are provided, as well as methods of using the inhibitors.Type: ApplicationFiled: September 20, 2006Publication date: October 14, 2010Inventors: Yuan-Ping Pang, Charles B. Millard, Jewn Giew Park, Jing Tang, James J. Schmidt
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Publication number: 20100261760Abstract: The disclosure provides EP2 receptor agonist compounds and methods for using the compounds for treating conditions which can be alleviated by agonism of an EP2 receptor.Type: ApplicationFiled: June 22, 2010Publication date: October 14, 2010Applicant: Asterand UK LimitedInventors: Alexander William Oxford, Richard John Davis, Robert Alexander Coleman, Kenneth Lyle Clark, David Edward Clark, Neil Victor Harris, Garry Fenton, George Hynd, Keith Alfred James Stuttle, Jonathan Mark Sutton, Mark Richard Ashton, Edward Andrew Boyd, Shirley Ann Brunton
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Patent number: 7803800Abstract: New inhibitors of histone deacetylases having antitumor activity, and the process of preparation thereof are herein described. These compounds belong to the structural formula (I) where R1 is a linear or branched chain containing at least two conjugated double bonds, A is an optionally substituted phenyl or pyridyl ring, Ar is an aryl or heteroaryl group, and R3 is hydrogen or alkoxyalkyl. The application also describes the use of said compounds in the treatment of diseases associated to the deregulation of histone deacetylases activity, such as tumors, as well as the relevant pharmaceutical compositions for administration to patients requiring said treatment.Type: GrantFiled: September 30, 2005Date of Patent: September 28, 2010Assignee: DAC S.R.L.Inventors: Saverio Minucci, Pier Giuseppe Pelicci, Antonello Mai, Marco Ballarini, Gaetano Gargiulo, Silvio Massa
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Publication number: 20100240911Abstract: A process for the preparation of a compound of formula: and/or an addition salt of a proton acid, which process comprises the following steps: (a) reacting a mixture comprising (i) a methyl ketone of formula IV and (ii) a compound of formula: H2N—R2??V and/or an addition salt of proton acid, and (iii) formaldehyde or a source of formaldehyde, in the presence of a solvent, and optionally a proton acid, to afford a ?-amino ketone of formula II, and/or an addition salt of a proton acid, and (b) reducing the carbonyl group of said ?-amino acid, the first step is carried out at a pressure above 1.5 bar.Type: ApplicationFiled: May 28, 2010Publication date: September 23, 2010Inventor: Dominique Michel
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Publication number: 20100240717Abstract: The invention relates to thiophene derivatives of formula (I)/their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents wherein: A represents *—CO—CH?CH—, *—CO—CH2CH2—, *—CO—CH2—NH—, wherein the sterisks indicate the bond that is linked to the thiophene group of Formula (I), and R1-R3 are as defined in the claims.Type: ApplicationFiled: January 10, 2007Publication date: September 23, 2010Applicant: ACTELION PHARMACEUTICALS LTD.Inventors: Martin Boli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jörg Velker
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Publication number: 20100217008Abstract: The present invention relates to a new method for the production of valsartan, a valine derivative having the chemical N name is (S)—N-(1-carboxy-2-methylprop-1-yl)-N-pentanoyl-N-[2?-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]amine, and pharmacologically acceptable salts thereof. Furthermore the invention relates to new intermediate compounds which are suitable for the production of valsartan and new methods for the production of intermediate compounds which are suitable for the production of valsartan.Type: ApplicationFiled: December 11, 2007Publication date: August 26, 2010Applicant: ratiopharm GmbHInventors: Jiri Stohandl, Pavel Bobal, Jaroslav Frantisek
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Publication number: 20100216849Abstract: This invention relates to novel biphenylcarboxamides of the formula (I) in which R, Z, X, Y, m, n and A are as defined in the disclosure, to a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.Type: ApplicationFiled: April 30, 2010Publication date: August 26, 2010Inventors: Ralf Dunkel, Hans-Ludwig Elbe, Heiko Rieck, Ulrike Wachendorff-Neumann, Peter Dahmen, Peter Lösel, Karl-Heinz Kuck, Astrid Mauler-Machnik, Jörg Nico Greul
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Publication number: 20100204487Abstract: The invention encompasses a process for making a thiophene carboxamide derivative, which is an EP4 antagonist useful for treating pain and inflammation.Type: ApplicationFiled: August 5, 2008Publication date: August 12, 2010Inventor: Ian DAVIES
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Publication number: 20100190779Abstract: Compounds of formula I: wherein X, R2, R3, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.Type: ApplicationFiled: July 31, 2008Publication date: July 29, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Pierre L. Beaulieu, Paul J. Edwards, Martin Poirier, Jean Rancourt, Timothy A. Stammers
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Patent number: 7759501Abstract: The present invention provides a process for producing an N-monoalkyl-3-hydroxy-3-(2-thienyl)propanamine represented by General Formula (2): wherein R is C1-4 alkyl, comprising the step of reducing (Z)-N-monoalkyl-3-oxo-3-(2-thienyl)propenamine represented by General Formula (1): wherein R is as defined above. According to the present invention, an N-monoalkyl-3-hydroxy-3-(2-thienyl)propanamine which is for use as an intermediate for various pharmaceuticals can be produced in an industrially inexpensive and easy manner.Type: GrantFiled: July 15, 2003Date of Patent: July 20, 2010Assignee: Sumitomo Seika Chemicals Co., Ltd.Inventors: Kenji Kogami, Noriyuki Hayashizaka, Syuzo Satake, Ichiro Fuseya, Hirokazu Kagano
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Publication number: 20100173981Abstract: Disclosed herein is a compound according to one of the formulas or a pharmaceutically acceptable salt thereof, medicaments for the treatment of glaucoma or ocular hypertension and compositions related thereto, as further elaborated herein.Type: ApplicationFiled: January 30, 2008Publication date: July 8, 2010Applicant: Allergan, Inc.Inventors: Brent A. Johnson, David W. Old, Yariv Donde, Robert M. Burk
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Patent number: 7745483Abstract: Novel 2-halofuryl/thienyl-3-carboxamides of the formula (I) in which A, Hal, R, M and Z are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.Type: GrantFiled: January 22, 2005Date of Patent: June 29, 2010Assignee: Bayer CropScience AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Benoit Hartmann, Peter Dahmen, Karl-Heinz Kuck, Ulrike Wachendorff-Neumann
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Publication number: 20100144785Abstract: The present invention relates N-(aromatic, 6-membered, fused, (hetero)aryl-methylene)-N-cycloalkyl carboxamide derivatives, their thiocarboxamide or N-substituted carboximidamide analogues, all of formula (I) wherein A represents a carbo-linked 5-membered heterocyclyl group; T represents O, S, N—Rc, N—ORd, N—NRcRd or N—CN; Z1 to Z3 and B represents an aromatic, 6-membered, fused, (hetero)aryl; their process of preparation; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: July 31, 2008Publication date: June 10, 2010Applicant: Bayer SASInventors: Philippe Desbordes, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Benoit Hartmann, Philippe Rinolfi, Arounarith Tuch
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Publication number: 20100137336Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: July 10, 2008Publication date: June 3, 2010Inventor: Christelle Boléa
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Publication number: 20100137347Abstract: Disclosed herein is a compound of the formula (I). Therapeutic methods, compositions, and medicaments, related thereto are also disclosed.Type: ApplicationFiled: January 21, 2008Publication date: June 3, 2010Applicant: ALLERGAN, INC.Inventors: Yariv Donde, Jeremiah H. Nguyen
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Publication number: 20100137291Abstract: The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent.Type: ApplicationFiled: December 11, 2009Publication date: June 3, 2010Inventors: Richard A. EARL, Maiko EZAWA, Xinqin FANG, David S. GARVEY, Ricky D. GASTON, Subhash P. KHANAPURE, L. Gordon LETTS, Chia-En LIN, Ramani R. RANATUNGA, Stewart K. RICHARDSON, Joseph D. SCHROEDER, Cheri A. STEVENSON, Shiow-Jyi WEY
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Publication number: 20100137599Abstract: The present invention relates to a process for the preparation of 1,4-butanediol mononitrate as intermediate for large scale preparation of high purity nitrooxybutyl ester of pharmaceutically active compounds.Type: ApplicationFiled: June 18, 2008Publication date: June 3, 2010Applicant: NICOX S.A.Inventors: Achim Hack, Gunter Weingarner, Matthias Kramer
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Publication number: 20100137417Abstract: The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have glucagon receptor antagonist or inverse agonist activity, as well as methods of using these compounds and intermediates and methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising N compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.Type: ApplicationFiled: February 9, 2006Publication date: June 3, 2010Inventors: Mark Donald Chappell, Scott Eugene Conner, Allie Edward Tripp, Guoxin Zhu
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Publication number: 20100113477Abstract: The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl-naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided.Type: ApplicationFiled: October 20, 2009Publication date: May 6, 2010Inventors: Joel S. Freundlich, James C. Sacchettini, Inna V. Kriger, Thomas R. Ioerger, Vijay Gawandi
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Publication number: 20100087494Abstract: A compound of general formula (I): A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: ApplicationFiled: February 21, 2008Publication date: April 8, 2010Inventors: Pierre-Yves Coqueron, Rudiger Fischer, Oliver Gaertzen, Marie-Claire Grosjean-Cournoyer, Benoit Hartmann, Klaus Kunz, Darren Mansfield, Amos Mattes, Oswald Ort, Philippe Desbordes
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Publication number: 20100081702Abstract: Object The present invention provides a pharmaceutical composition for prophylaxis or treatment of hepatitis. Solution A pharmaceutical composition for prophylaxis or treatment of hepatitis, comprising a compound represented by the general formula (I): wherein R1 represents a C1-C4 alkyl group, R2 and R3 which are the same or different represent a hydrogen atom, a C1-C4 alkyl group, or a C1-C4 alkoxy group, X represents a sulfur atom or a nitrogen atom substituted by a methyl group, and n represents an integer of 3 or 4, or a pharmacologically acceptable salt thereof as an active ingredient.Type: ApplicationFiled: November 23, 2009Publication date: April 1, 2010Inventors: Takaichi Shimozato, Takashi Kagari, Hiromi Doi
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Publication number: 20100081652Abstract: Disclosed is an extracellular matrix genetranscription inhibitor composition or the like characterized by containing a cinnamoyl compound represented by the formula (I) below: and an inert carrier.Type: ApplicationFiled: March 2, 2006Publication date: April 1, 2010Inventors: Hiroaki Shiraki, Kiyoshi Higashi, Yoshitaka Tomigahara, Junya Takahashi
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Publication number: 20100081807Abstract: The invention relates to a method for producing 5-chloro-N-({5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophenecarboxamide starting from 5-chlorothiophene-2-carbonyl chloride, (2S)-3-amino-propane-1,2-diol and 4-(4-aminophenyl)-3-morpholinone.Type: ApplicationFiled: September 9, 2009Publication date: April 1, 2010Applicant: Bayer Healthcare AGInventor: Christian R. Thomas
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Publication number: 20100073847Abstract: A compound having the formula below. X is hydroxyl, a sulfonic ester or salt thereof, a phosphonate or salt thereof, a carboxylate or salt thereof, or a boronic ester or salt thereof. The value n is an integer greater than or equal to 2. A polymer made by polymerizing the compound. A method of: reacting NH2—(CH2—CH2—O)n—CH2—CH2—OH with thiophene acid chloride to form a (SC4H3)—CO—NH—(CH2—CH2—O)n—CH2—CH2—OH amide; reacting the amide with a vinyl sulfonic ester, a vinyl phosphonate, a vinyl carboxylate, or a vinyl boronic ester to form an intermediate; and converting the intermediate to a salt form.Type: ApplicationFiled: September 22, 2009Publication date: March 25, 2010Applicant: The Government of the United States of America, as represented by the Secretary of the NavyInventors: Brett D. Martin, Banahalli R. Ratna, Jawad Naciri, Michael A. Markowitz
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Publication number: 20100075946Abstract: The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.Type: ApplicationFiled: June 20, 2006Publication date: March 25, 2010Applicant: Actelion Pharmaceuticals Ltd.Inventors: Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Jörg Velker
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Publication number: 20100063044Abstract: The present invention relates to aniline derivatives of formula I: wherein R1, R2, R3, R4, Z and q are as defined herein; or salts thereof and their use.Type: ApplicationFiled: August 17, 2009Publication date: March 11, 2010Applicant: H. Lundbeck A/SInventors: Christian Wenzel Tornoe, Mario Rottlãnder, Daniel Rodriguez Greve, Nikolay Khanzhin, Andreas Ritzén, William Patrick Watson
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Patent number: 7666866Abstract: This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt of the compound) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: November 15, 2005Date of Patent: February 23, 2010Assignee: Eli Lilly and CompanyInventors: Jeffry Bernard Franciskovich, David Kent Herron, Valentine Joseph Klimkowski, Angela Lynn Marquart, John Joseph Masters, David Mendel, Andrew Michael Ratz, Gerald Floyd Smith, Michael Robert Wiley, Ying Kwong Yee
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Patent number: 7645799Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: GrantFiled: November 7, 2008Date of Patent: January 12, 2010Assignee: Bristol-Myers Squibb CompanyInventors: James R. Corte, Mimi L. Quan, Joanne M. Smallheer, Donald J. P. Pinto
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Patent number: 7638553Abstract: Objects of the present invention are the compounds of formula (I), their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.Type: GrantFiled: June 13, 2005Date of Patent: December 29, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Georg Fertig, Frank Herting, Matthias Koerner, Manfred Kubbies, Anja Limberg, Ulrike Reiff, Ulrich Tibes