The Nitrogen Is Double Or Triple Bonded Directly To Carbon Patents (Class 548/505)
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Publication number: 20150065487Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: November 11, 2014Publication date: March 5, 2015Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fred Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
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Publication number: 20150031722Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: October 6, 2014Publication date: January 29, 2015Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
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Publication number: 20140275569Abstract: The present application provides methods for decarboxylation of amino acids via imine formation with a catalyst under superheated conditions in either a microwave or oil bath.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Inventors: Richard W. Morrison, Douglas Michael Jackson
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Patent number: 8748411Abstract: Chemical compounds derived by in silico molecular modelling, having a well defined structure suitable for the blocking of the phosphorylation event, through the specific interaction of the chemical with the Casein Kinase 2 enzyme substrate phosphorylation domain or it's neighbourhood. This invention comprises also the pharmaceutical compositions containing such compounds, and their use in the preparation of medicines or agents for the treatment of diseases or conditions related with neoplasic processes.Type: GrantFiled: May 5, 2006Date of Patent: June 10, 2014Assignee: Centro de Ingenieria Genetica y BiotechnologiaInventors: Rolando Eduardo Rodriguez Fernandez, Roberto Vera Alvarez, Ania De La Nuez Veulens, Yuliet Mazola Reyes, Silvio Ernesto Perea Rodriguez, Boris Ernesto Acevedo Castro, Alexis Musacchio Lasa, Raimundo Ubieta Gómez
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Publication number: 20140155431Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: December 19, 2013Publication date: June 5, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
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Publication number: 20130252955Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.Type: ApplicationFiled: May 16, 2013Publication date: September 26, 2013Applicant: Kissei Pharmaceutical Co., Ltd.Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
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Patent number: 8470877Abstract: 2-Phenylethylamino substituted carboxamide derivatives and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies are presented.Type: GrantFiled: January 26, 2012Date of Patent: June 25, 2013Assignee: Newron Pharmaceuticals S.p.A.Inventors: Florian Thaler, Mauro Napoletano, Cibele Sabido-David, Ermanno Moriggi, Carla Caccia, Laura Faravelli, Alessandra Restivo, Patricia Salvati
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Publication number: 20130131084Abstract: The present invention relates to the use of derivatives of indoles having a general formula (I) as follow: for the manufacture of a pharmaceutical composition intended for the treatment of cancer.Type: ApplicationFiled: August 17, 2012Publication date: May 23, 2013Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Catherine GUILLOU, Frank Kozielski, Christophe Labriere, Francoise Gueritte, Sergey Tcherniuk, Dimitrios Skoufias, Claude Thal, Henri-Philippe Husson
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Publication number: 20130060047Abstract: Disclosed are novel methods for the synthesis of N-substituted indol-3-yl-alkylamide compounds which act as P2X7R antagonists, said methods involving the rearrangement of an oxime intermediate.Type: ApplicationFiled: March 4, 2011Publication date: March 7, 2013Applicant: AFFECTIS PHARMACEUTICALS AGInventor: Michael Bos
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Patent number: 8367665Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification.Type: GrantFiled: April 16, 2009Date of Patent: February 5, 2013Assignee: Karo Bio ABInventors: Patrik Rhönnstad, Elisabet Kallin, Theresa Apelqvist, Mattias Wennerstål, Aiping Cheng
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Publication number: 20120302576Abstract: The present invention relates to compounds and pharmaceutically acceptable salts, esters and prodrugs of Formula (I) or (II): which are useful as AMPK modulators effective in treating diabetes, obesity and cancer in a subject.Type: ApplicationFiled: August 9, 2012Publication date: November 29, 2012Inventors: Neal C. Birnberg, Hong Liu, Qing Ping Weng, Haibo Shang, Pan Yin, Sharanappa B. Rajur, Hwa-Ok Kim, Paresh D. Salgaonkar, Norton P. Peet
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Patent number: 8129427Abstract: 2-Phenylethylamino substituted carboxamide derivatives and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies are presented.Type: GrantFiled: September 9, 2010Date of Patent: March 6, 2012Assignee: Newron Pharmaceuticals S.p.A.Inventors: Florian Thaler, Mauro Napoletano, Cibele Sabido-David, Ermanno Moriggi, Carla Caccia, Laura Faravelli, Alessandra Restivo, Patricia Salvati
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Publication number: 20110230454Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.Type: ApplicationFiled: May 26, 2011Publication date: September 22, 2011Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
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Publication number: 20110201555Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity. wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 , R10 and R11 are as defined in the specification.Type: ApplicationFiled: September 18, 2009Publication date: August 18, 2011Inventors: Patrik Rhönnstad, Theresa Apelqvist, Mattias Wennerstål, Aiping Cheng, Sandra Gordon
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Publication number: 20110190294Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification.Type: ApplicationFiled: April 16, 2009Publication date: August 4, 2011Inventors: Patrik Rhönnstad, Elisabet Kallin, Theresa Apelqvist, Mattias Wennerstål, Aiping Cheng
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Publication number: 20110183928Abstract: The present application relates to novel 3-cyanoalkyl- and 3-hydroxyalkyl-substituted indole derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of cardiovascular diseases.Type: ApplicationFiled: June 18, 2009Publication date: July 28, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Kai Thede, Elisabeth Woltering, Peter Kolkhof, Carsten Schmeck, Elisabeth Pook, Alexander Hillisch, Lars Bärfacker, Klemens Lustig, Dieter Lang, Martin Radtke, Rolf Grosser, Astrid Brüns, Michael Gerisch
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Publication number: 20110112037Abstract: The invention provides a method of predicting a three dimensional structural representation of a target protein of unknown structure, or part thereof, comprising: providing the coordinates of the turkey ?1-AR structure listed in Table A, Table B, Table C or Table D, optionally varied by a root mean square deviation of residue backbone atoms of not more than 1.235 A, or selected coordinates thereof; and predicting the three-dimensional structural representation of the target protein, or part thereof, by modelling the structural representation on all or the selected coordinates of the turkey ?1-AR. The invention also provides the use of the turkey ?1-AR coordinates to select or design one or more binding partners of ?1-AR.Type: ApplicationFiled: March 5, 2008Publication date: May 12, 2011Applicant: Heptares Therapeutics Limited BioParkInventors: Antony Johannes Warne, Maria Josefa Serrano-Vega, Rouslan Moukhametzianov, Patricia C. Edwards, Richard Henderson, Andrew G.W. Leslie, Christopher Gordon Tate, Gebhard F.X. Schertler
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Publication number: 20110021785Abstract: The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: ApplicationFiled: January 20, 2010Publication date: January 27, 2011Inventors: James C. Lanter, Zhihua Sui, James J. Fiordeliso, Weiqin Jiang, Xuqing Zhang
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Patent number: 7855227Abstract: 2-Phenylethylamino substituted carboxamide derivatives of formula (I); wherein J, W, R0, R1, R2, R3, and R4 have the meanings as defined in the specification and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them as active ingredient and their use as sodium and/or calcium channel modulators useful in preventing alleviating and curing a wide range of pathologies, including neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urology, and gastrointestinal diseases where the above mechanisms have been described as playing a pathological role, are described.Type: GrantFiled: November 29, 2006Date of Patent: December 21, 2010Assignee: Newron Pharmaceuticals S.p.A.Inventors: Florian Thaler, Mauro Napoletano, Cibele Sabido-David, Ermanno Moriggi, Carla Caccia, Laura Faravelli, Alessandra Restivo, Patricia Salvati
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Publication number: 20100317863Abstract: Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.Type: ApplicationFiled: July 21, 2008Publication date: December 16, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Daniel Kuzmich, John Robinson Regan
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Publication number: 20100292187Abstract: The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity.Type: ApplicationFiled: June 14, 2010Publication date: November 18, 2010Applicant: PTC THERAPEUTICS, INC.Inventors: Gary M. Karp, Peter Seongwoo Hwang, James J. Takasugi, Hongyu Ren, Richard Gerald Wilde, Anthony A. Turpoff, Alexander Arefolov, Guangming Chen, Jeffrey A. Campbell, Chunshi Li, Steven Paget, Nanjing Zhang, Xiaoyan Zhang, Jin Zhu
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Publication number: 20100056521Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.Type: ApplicationFiled: April 10, 2008Publication date: March 4, 2010Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
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Patent number: 7662849Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.Type: GrantFiled: June 4, 2004Date of Patent: February 16, 2010Assignee: ViroBay, Inc.Inventors: John W. Patterson, Soon H. Woo
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Publication number: 20090306170Abstract: The present invention relates to a novel process for the synthesis of 1-((5-methoxy-1H-indol-3-yl)methyleneamino)-3-pentyl-guanidine, commonly known as tegaserod, which is used as a gastroprokinetic, and salts thereof. The present invention also relates to tegaserod and salts thereof having an HPLC purity of about 95% or more. The present invention further relates to pharmaceutical compositions comprising tegaserod or a salt thereof, second medical uses of tegaserod or a salt thereof, and methods of treating or preventing irritable bowel syndrome using tegaserod or a salt thereof.Type: ApplicationFiled: November 9, 2007Publication date: December 10, 2009Applicant: GENERICS UK LIMITEDInventors: Abhay Gaitonde, Bindu Mnaojkumar, Sandeep Sonawane
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Publication number: 20090306396Abstract: The present invention relates to novel compounds having a xanthine oxidase inhibitory effect and an uricosuric effect and pharmaceutical compositions comprising the same as an active ingredient. That is, the present invention relates nitrogen-containing heterocyclic compounds represented by the following general formula (I): wherein Y1 represents N or C(R4); Y2 represents N or C(R5); R4 and R5 independently represent an alkyl group, a hydrogen atom etc.; one of R1 and R2 represents an optionally substituted aryl group, an alkoxy group or an optionally substituted heterocyclic group; the other of R1 and R2 represents a haloalkyl group, a cyano group, a halogen atom etc.; and R3 represents a 5-tetrazolyl group or a carboxy group, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising the same as an active ingredient.Type: ApplicationFiled: October 3, 2006Publication date: December 10, 2009Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Takahiro Toyoshima, Toshinobu Sasaki, Chikara Hoshino, Masakazu Takeda
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Publication number: 20090215730Abstract: Chemical compounds derived by in silico molecular modelling, having a well defined structure suitable for the blocking of the phosphorylation event, through the specific interaction of the chemical with the Casein Kinase 2 enzyme substrate phosphorylation domain or it's neighbourhood. This invention comprises also the pharmaceutical compositions containing such compounds, and their use in the preparation of medicines or agents for the treatment of diseases or conditions related with neoplasic processes.Type: ApplicationFiled: May 5, 2006Publication date: August 27, 2009Inventors: Rolando Eduardo Rodriguez Fernandez, Roberto Vera Alvarez, Ania De La Nuez Veulens, Yuliet Mazola Reyes, Silvio Ernesto Perea Rodriguez, Boris Ernesto Acevedo Castro, Alexis Musacchio Lasa, Raimundo Ubieta Gomez
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Publication number: 20090118350Abstract: Pharmacogenetics was used to evaluate the effect of polymorphisms in select candidate genes on the response of patients with chronic constipation to tegaserod (Zelmac®/Zelnorm®). The analysis identified twelve single nucleotide polymorphisms (SNPs) in six genes (HTR4, HTR3B, MLN, AQP3, SLC12A2, SCNN1A) that were associated with at least a 60% response rate to tegaserod and an odds ratios of 5 or greater (compared to placebo) after 4 weeks of treatment. The identified genes display a wide range of different functions, including serotonin signaling, secretion and motility, all of which are important in maintaining the normal function of the gastrointestinal tract. Thus, these data imply that chronic constipation may result from a variety of pathophysiological mechanisms related to variants in the above identified genes, all of which respond well to treatment with tegaserod.Type: ApplicationFiled: January 3, 2006Publication date: May 7, 2009Inventor: LeeAnne McLean
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Publication number: 20090092782Abstract: An indole compound represented by general formula (I): Wherein R1 and R2 each represent a hydrogen atom, a hydrocarbon group having 1 to 30 carbon atoms or a substituent represented by general formula (II); R3 and R4 each represent an alkyl group having 1 to 10 carbon atoms, an alkoxy group having 1 to 10 carbon atoms or an aryl group having 6 to 30 carbon atoms; R5, R6, R7, and R8 each represent a hydrogen atom, a hydrocarbon group having 1 to 30 carbon atoms, a halogen atom, a hydroxyl group, a nitro group, a cyano group, NHR or NR?R?; R, R?, and R? each represent an alkyl group having 1 to 10 carbon atoms, or R? and R? are taken together to form a ring; or R5 and R6, or R6 and R7, or R7 and R8 may be taken together to form a ring; Anq? represents a q-valent anion; q represents 1 or 2; and p represents a coefficient necessary to maintain charge neutrality.Type: ApplicationFiled: July 19, 2006Publication date: April 9, 2009Applicant: ADEKA CORPORATIONInventor: Satoshi Yanagisawa
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Publication number: 20090048303Abstract: The present invention relates therefore first to new indole-2-carboxamidine derivatives of formula (I)—wherein the meaning of X is hydrogen or halogen atom, C1-C4 alkyl, C1-C4 alkoxy, trifluoromethyl group, Y, V and Z independently are hydrogen or halogen atom, hydroxy, cyano, C1-C4 alkylsulfonamido optionally substituted by a halogen atom or halogen atoms, C1-C4 alkanoylamido optionally substituted by a halogen atom or halogen atoms, trifluoromethyl, trifluoromethoxy, C1-C4 alkyl, C1-C4 alkoxy group, or the neighboring V and Z groups in given case together with one or more identical or different additional hetero atom and —CH? and/or —CH2— groups can form an optionally substituted 4-7 membered homo- or heterocyclic ring, preferably benzene, dioxolane ring, A, B and C independently are substituted carbon atom or one of them is nitrogen atom, and the salts thereof.Type: ApplicationFiled: July 21, 2005Publication date: February 19, 2009Inventors: Istvan Borza, Csilla Horvath, Sandor Farkas, Jozsef Nagy, Sandor Kolok
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Publication number: 20090042875Abstract: The present invention relates to substituted heterocyclic compounds and compositions comprising a substituted heterocyclic compound. The present invention also relates to methods for preventing or treating various diseases and disorders by administering to a subject in need thereof one or more substituted heterocyclic compounds. In particular, the invention relates to methods for preventing or treating cancer or an inflammatory disorder by administering to a subject in need thereof one or more substituted heterocyclic compounds. The present invention further relates to articles of manufacture and kits comprising one or more substituted heterocyclic compounds.Type: ApplicationFiled: September 29, 2008Publication date: February 12, 2009Inventors: George W. Muller, Hon-Wah Man
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Patent number: 7288553Abstract: The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: GrantFiled: April 1, 2005Date of Patent: October 30, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: James C. Lanter, Zhihua Sui, James J. Fiordeliso, Weiqin Jiang, Xuqing Zhang
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Patent number: 7250440Abstract: This invention provides estrogen receptor modulators of formula I, having the structure where R1, R2, R3, and R4 are as defined in the specification, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 9, 2004Date of Patent: July 31, 2007Assignee: WyethInventors: Richard Eric Mewshaw, Stephen Marc Bowen, Eric Steven Manas
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Patent number: 7129264Abstract: The present invention provides compounds of Formula (I): or a stereoisomer or pharmaceutically acceptable salt or hydrate form thereof, wherein the variables A, B, L1, L2, X1, X2, X3, X4 and W 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: April 14, 2004Date of Patent: October 31, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Joanne M. Smallheer, Mimi L. Quan, Shuaige Wang, Gregory S. Bisacchi
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Patent number: 7125906Abstract: The invention relates to the use of a compound of Formula (I), for the manufacture of a medicament to inhibit and/or reverse and/or alleviate symptoms of angiogenesis and/or any disease state associated with angiogenesis: wherein: X, p, q, R1, R2, R3, R4, and R5 are as defined in the description. The invention also related to use of compounds of Formula (I) as medicaments and also to novel compounds of Formula (I). The invention further provides pharmaceutical compositions of compounds of Formula (I) and processes for the synthesis of compounds of Formula (I).Type: GrantFiled: March 31, 2003Date of Patent: October 24, 2006Assignee: AstraZeneca ABInventor: Jean-Claude Arnould
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Patent number: 6995262Abstract: The invention relates to a novel polymethine dyes containing at least one acylsulfonamido group of the formula (I) in which n, Y, A and R have the meaning given in the claims, and at least one compound of the formulae (a) to (n) given in the claims. The polymethine dyes according to the invention are suitable for use as dyes and/or labels, in particular for staining or labeling biomolecules.Type: GrantFiled: July 24, 2000Date of Patent: February 7, 2006Assignee: Bayer CropScience AGInventors: Geert Deroover, Michael Missfeldt, Lydia Simon
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Patent number: 6809098Abstract: The present invention relates to compounds of formula I which are antagonists of gonadotropin releasing hormone (GnRH) activity. The invention also relates to pharmaceutical formulations, the use of a compound of the present invention in the manufacture of a medicament, a method of therapeutic treatment using such a compound and processes for producing the compounds.Type: GrantFiled: August 21, 2002Date of Patent: October 26, 2004Assignee: AstraZeneca ABInventors: Michael Wardleworth, Alexander Graham Dossetter, Christopher Thomas Halsall
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Patent number: 6727270Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.Type: GrantFiled: February 13, 2003Date of Patent: April 27, 2004Assignee: WyethInventors: Michael Gerard Kelly, Ping Zhou
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Patent number: 6699862Abstract: Novel indolyl-2-phenyl bisamidines are described which are DNA methyltransferase inhibiting agents, and pharmaceutical compositions containing them are used as antiproliferative agents for treating a disease, especially a neoplastic disease, characterized by abnormally rapid proliferation of tissue involved in said disease; said indolyl-2-phenyl bisamidines comprising a and a pharmaceutically acceptable salt thereof, wherein: R1 is hydrogen or (C1-C3)alkyl; R3, R4, R5, R8, R9, and R10 are hydrogen or (C1-C3)alkyl, or R3 and R4 may be taken together, or R8 and R9 may be taken together with the nitrogen atoms to which they are attached, to form an imidazolinyl group; R14 is —H; —NHC(═O)(CH2)mR20; —(CH2)mR20; —CH(CH3)R20; —(CH2)m(C6H3)—R17; —(CH2)m(C6H3)—R20; —(CH2)m(heterocyclyl)—R17; —(CH2)m(heterocyclyl)—R20; —CH2CH═CHR20; —(CH2)mC(═O)NH—CHR20R21; or —(CH2)mC(═O)NH—CH2&mType: GrantFiled: March 24, 2000Date of Patent: March 2, 2004Assignee: Pfizer Inc.Inventors: Steven W. Goldstein, Banauara L. Mylari, Jose R. Perez, Edward A. Glazer
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Patent number: 6541505Abstract: This invention is directed to an (aminoiminomethyl or aminomethyl)benzoheteroaryl compound of formula I which is useful for inhibiting the activity of Factor Xa by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.Type: GrantFiled: June 30, 2000Date of Patent: April 1, 2003Assignee: Aventis Pharmaceuticals Inc.Inventors: William P. Dankulich, Daniel G. McGarry, Christopher Burns, Timothy F. Gallagher, Francis A. Volz
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Patent number: 6541632Abstract: A carbocyclic or heterocyclic compound, ammonia and an oxygen-containing gas are subjected to fluid catalytic reaction in vapor phase in the presence of a catalyst containing alkali metal to produce an aromatic or heterocyclic nitrile. The use of the catalyst containing a specific amount of alkali metal enables the stable production of the aromatic or heterocyclic nitrile in high yields with little change with time even when water is present in the reaction system. The use of the catalyst containing the alkali metal also enables the recycle and reuse of unreacted ammonia which is usually accompanied by water, thereby reducing production costs.Type: GrantFiled: June 19, 2002Date of Patent: April 1, 2003Assignee: Mitsubishi Gas Chemical Company, Inc.Inventors: Hideaki Ogino, Takashi Okawa, Shuji Ebata, Yoshinori Kanamori
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Patent number: 6303782Abstract: A process is described for preparing an aromatic compound substituted by a tertiary nitrile of Formula (1.0.0): comprising treating a substituted aromatic compound of Formula (2.0.0): with a secondary nitrile of Formula (3.0.0): in the presence of a base having a pKa numerical value in the range of from about 17 to about 30, provided that the difference in pKa numerical values between said base and the corresponding tertiary nitrile of Formula (3.0.0) is no more than about 6; in an aprotic solvent having a dielectric constant (∈) of less than about 20; and at a reaction temperature in the range of from about 0° C. to about 120° C.; whereby there is formed said tertiary-nitrile-substituted aromatic compound final product of Formula (1.0.0); wherein the constituent parts W1, W2, W3, W4, and W5; and the substituent moieties R1, R2, R3, R4, R5, R6, and R7 in the compounds of Formulas (1.0.0), (2.0.0) and (3.0.Type: GrantFiled: March 1, 2000Date of Patent: October 16, 2001Assignee: Pfizer IncInventor: Stéphane Caron
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Patent number: 6258852Abstract: Disclosed are methods for treating or preventing inflammatory bowel disease (IBD) using aryl nitrone compounds. Pharmaceutical compositions containing aryl nitrone compounds which are useful for the treatment or prophylaxis of IBD are also disclosed.Type: GrantFiled: May 8, 2000Date of Patent: July 10, 2001Assignee: Centaur Pharmaceuticals, Inc.Inventors: William D. Flitter, William A. Garland, Beverly Greenwood Van-Meerveld, Ian Irwin
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Patent number: 5969112Abstract: A flocculating dye reduces bleed between two inks when they are applied side by side. A first ink comprises the flocculating dye which flocculates the dispersant-pigment of the second ink.Type: GrantFiled: April 3, 1998Date of Patent: October 19, 1999Assignee: Lexmark International, Inc.Inventors: James F. Feeman, Jing X. Sun
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Patent number: 5922582Abstract: The present invention relates to compound 0089-D having excellent antitumor activity and antimicrobial activity, represented by the general formula (I): ##STR1## or pharmaceutically acceptable salts thereof.Type: GrantFiled: April 3, 1998Date of Patent: July 13, 1999Assignee: HIGETA SHOYU Co., Ltd.Inventors: Akira Nemoto, Yasushi Tanaka, Hisayuki Komaki, Yuzuru Mikami, Katsukiyo Yazawa, Jun'ichi Kobayashi
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Patent number: 5814633Abstract: Iminooxymephyleneanilides of the formula I ##STR1## where the index and the substituents have the following meanings: n is 0, 1, 2, 3 or 4;R is nitro, cyano, halogen, unsubst. or subst. alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy or an unsubst. or subst. bridge bonded to two adjacent ring atoms;X is a direct bond or CH.sub.2, O or NR.sup.a ;R.sup.a is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl;R.sup.1 is hydrogen,unsubst. or subst. alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, alkylcarbonyl or alkoxycarbonyl;R.sup.2 is alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl, or in the case where X is NR.sup.a, additionally hydrogen;R.sup.3 is hydrogen, cyano, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio or cycloalkyl;R.sup.4 is a 6- to 10-membered mono- or bicyclic, substituted heteroaromatic ring system,and process and intermediates for their preparation and their use.Type: GrantFiled: May 20, 1997Date of Patent: September 29, 1998Assignee: BASF AktiengesellschaftInventors: Bernd Muller, Hubert Sauter, Franz Rohl, Eberhard Ammermann, Gisela Lorenz, Norbert Gotz
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Patent number: 5756531Abstract: The present invention provides a class of substituted indole and indene iminoxy derivatives of the formula ##STR1## which inhibit leukotriene biosynthesis and are useful in the treatment of allergic and inflammatory disease states.Type: GrantFiled: April 30, 1996Date of Patent: May 26, 1998Assignee: Abbott LaboratoriesInventors: Clint D. W. Brooks, Richard A. Craig, David E. Gunn, Teodozyji Kolasa, Jimmie L. Moore, Andrew O. Stewart
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Patent number: 5750558Abstract: Described herein are compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein L is selected from the group consisting of ##STR2## R.sup.2 is selected from (a) ##STR3## R.sup.3 is selected from optionally substituted phenyl, and optionally substituted pyridyl; Y is selected from halogen, alkyl, haloalkyl, alkoxy, pyridylmethoxy, thiazolylmethoxy, benzothiazolylmethoxy, quinolylmethoxy, and optionally substituted quinolylmethoxy; W is selected from hydrogen, alkyl, hydroxyalkyl, and hydroxy; A is absent or is selected from optionally substituted alkylene optionally substituted cycloalkylene, optionally substituted cycloalkylene wherein one or two of the carbon atoms is replaced with one or two heteroatoms independently selected from O, S, and N, and ##STR4## and X is absent or is alkylene; Z is selected from (a) hydrogen, (b) COM wherein M is selected from (b-1) a pharmaceutically acceptable metabolically cleavable group, (b-2)--OR.sup.10,(b-3)--O(CH.sub.2).sub.w --CH(OR.sup.Type: GrantFiled: June 6, 1996Date of Patent: May 12, 1998Assignee: Abbott LaboratoriesInventors: Clint D. W. Brooks, Teodozyj Kolasa, Wendy Lee, Andrew O. Stewart
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Patent number: 5705506Abstract: The present invention relates to a pharmaceutical composition for rectal administration in solid dosage form which comprises a compound acting as a 5HT-1 like receptor agonist in the form of its free base or a physiologically acceptable hard fat base carrier having a hydroxyl value of more than 15 in the method for the treament of a mammal suffering from a susceptible to conditions associated with cephalic pain.Type: GrantFiled: December 29, 1994Date of Patent: January 6, 1998Assignee: Laboratoires Glaxo SAInventors: Nadine Merlet, Isabelle Richard, Isabelle Thielemans
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Patent number: 5698364Abstract: Dye-donor element for thermal dye transfer comprising at least one magenta dye having extremely low side absorption in the blue and red regions of the spectrum, said dye corresponding to the general formula (I) : ##STR1## wherein R.sup.1 is H, (cyclo)alkyl, or aryl; X represents the atoms completing a heterocycle; Z is an electron-withdrawing group; Y is an electron-withdrawing group or --N(R.sup.2)R.sup.3 ; R.sup.2 and R.sup.3 together represent the atoms completing a heterocycle; or R.sup.2 and R.sup.3 together represent .dbd.C(R.sup.4)R.sup.5, or each of R.sup.2 and R.sup.3 represents (same or different) (cyclo) alkyl, aryl, or an electron-withdrawing group; each of R.sup.4 and R.sup.5 (same or different) represents H, (cyclo)alkyl, aryl, a heterocycle, SO.sub.2 R.sup.6, COR.sup.6, CSR.sup.6, POR.sup.6 R.sup.7, OR.sup.8, NR.sup.8 R.sup.9, SR.sup.8, or R.sup.4 and R.sup.5 together represent the atoms completing an aliphatic ring or a heterocycle, each of R.sup.6 and R.sup.Type: GrantFiled: June 6, 1995Date of Patent: December 16, 1997Assignee: Agfa-Gevaert, N.V.Inventors: Wilhelmus Janssens, Luc Vanmaele
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Patent number: 5696148Abstract: The present invention relates to therapeutically active indole compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system related to the metabotropic glutamate receptor system.Type: GrantFiled: November 18, 1996Date of Patent: December 9, 1997Assignee: Novo Nordisk A/SInventors: Jane Marie Lundbech, Anders Kanstrup