The Additional Cyclo Is Five-membered Consisting Of Nitrogen And Carbon (e.g., Imidazobenzodiazepinones, Etc.) Patents (Class 540/498)
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Patent number: 8946410Abstract: The present invention provides a method to obtain radiofluorinated compounds useful for in vivo imaging GABAA receptors. The method of the invention is high-yielding and may conveniently be carried out on an automated synthesizer such as Fastlabâ„¢. A further aspect of the invention is a cassette suitable for carrying out the automated method of synthesis of the invention. Novel precursor compounds useful in the method of the invention are also provided, as are a number of novel compounds obtained by the method of the invention.Type: GrantFiled: October 8, 2010Date of Patent: February 3, 2015Assignee: GE Healthcare LimitedInventors: John Woodcraft, L Clare Jones, Alessandra Gaeta, John William Trigg, Alexander Paul Jones, Stuart Plant, Alexander Jackson
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Publication number: 20140228562Abstract: The use of 7-chloro-3-(5-dimethylaminomethyl-[1,2,4]oxadiazol-3-yl)-5methyl-4,5-dihydro-imidazol[1,5,-a][1,4]benzodiazepine-6-one or its pharmaceutically acceptable salt for treating various types of insomnia.Type: ApplicationFiled: April 3, 2014Publication date: August 14, 2014Applicant: EVOTEC INTERNATIONAL GMBHInventors: John Alan Kemp, Ian Michael Hunneyball, Timothy Tasker
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Publication number: 20140171422Abstract: Provided are a compound represented by general formula (I), or the pharmaceutically acceptable salt thereof, (wherein Ra represents a hydrogen atom or the like, R1 and R2 may be the same or different, and each represents a hydrogen atom, optionally substituted lower alkyl or cycloalkyl, or R1 and R2 are combined together with the adjacent nitrogen atom thereto to form nitrogen-containing heterocyclic group, and Z represents a bicyclic heterocyclic group in which optionally substituted two six-membered rings are fused to each other, or the like) and the like.Type: ApplicationFiled: May 10, 2012Publication date: June 19, 2014Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Nobumasa Otsubo, Shuko Okazaki, Yukihito Tsukumo, Kyoichiro Iida, Masayoshi Nakoji
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Patent number: 8710046Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.Type: GrantFiled: June 30, 2010Date of Patent: April 29, 2014Assignee: Albany Molecular Research, Inc.Inventors: Peter R. Guzzo, David D. Manning, William Earley
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Publication number: 20140107106Abstract: In part, the present invention is directed to antibacterial compounds.Type: ApplicationFiled: April 25, 2013Publication date: April 17, 2014Applicant: Affinium Pharmaceuticals, Inc.Inventor: Affinium Pharmaceuticals, Inc.
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Publication number: 20140011961Abstract: The present invention relates to a solid precursor in the form of an organic salt, the solid precursor having a solid support, a method for manufacturing same, and an application thereof. The solid precursor of the present invention enables omission of the [18F]fluoride refining process using additional cartridge, and the use of excessive phase-transfer catalyst, and can easily remove remaining substance after reaction through the solid support inside the precursor. The solid precursor of the present invention is very appropriate for an automated synthesis device as an all-in-one system that can carry out overall process of [18F]fluorosis reaction, when used by charging in a cartridge.Type: ApplicationFiled: December 13, 2011Publication date: January 9, 2014Inventors: Dae-Yoon Chi, Byoung-Se Lee, Jae-Hak Lee, So-Young Chu, Woon-Jung Jung, Hye-Rim Kwon
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Publication number: 20130345202Abstract: Soluble complexes of flumazenil, methods for the preparation thereof, pharmaceutical compositions including same and use of the compositions for alleviating or counteracting the various types of hypersomnia, drowsiness, residual effects associated with the administration of sleep/hypnotic drugs, alcohol intoxication or hepatic encephalopathy.Type: ApplicationFiled: August 23, 2013Publication date: December 26, 2013Inventor: Shimon Amselem
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Publication number: 20130137680Abstract: The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5 and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: December 1, 2010Publication date: May 30, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephen James Boyer, Jennifer Burke, Xin Guo, Thomas Martin Kirrane, JR., Roger John Snow, Yunlong Zhang
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Publication number: 20130137659Abstract: Provided herein are compounds of formula (I):Type: ApplicationFiled: January 25, 2013Publication date: May 30, 2013Applicant: SANOFIInventor: SANOFI
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Publication number: 20130012492Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: ApplicationFiled: June 29, 2012Publication date: January 10, 2013Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
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Publication number: 20120295892Abstract: Described herein are ?3 or ?2 or ?2/?3 GABAergic receptor subtype selective ligands, pharmaceutical compositions, and methods of use of such ligands and compositions in treatment of anxiety disorders, epilepsy and schizophrenia with reduced sedative and ataxic side effects. In embodiments, such as ?3 or ?2 or ?2/?3 GABAergic receptor subtype selective ligands lack ester linkages and may be thus relatively insensitive to hydrolysis by esterases.Type: ApplicationFiled: April 27, 2012Publication date: November 22, 2012Applicant: UWM RESEARCH FOUNDATION, INC.Inventors: James M. Cook, Terry S. Clayton, Hiteshkumar D. Jain, Sundari K. Rallipalli, Yun Teng Johnson, Jie Yang, Michael Ming-Jin Poe, Ojas A. Namjoshi, Zhi-jian Wang
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Publication number: 20120270857Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: June 30, 2010Publication date: October 25, 2012Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Peter R. Guzzo, David D. Manning, William Earley
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Publication number: 20120190843Abstract: The present invention provides a method to obtain radiofluorinated compounds useful for in vivo imaging GABAA receptors. The method of the invention is high-yielding and may conveniently be carried out on an automated synthesizer such as Fastlabâ„¢. A further aspect of the invention is a cassette suitable for carrying out the automated method of synthesis of the invention. Novel precursor compounds useful in the method of the invention are also provided, as are a number of novel compounds obtained by the method of the invention.Type: ApplicationFiled: October 8, 2010Publication date: July 26, 2012Inventors: John Woodcraft, L. Clare Jones, Alessandra Gaeta, John William Trigg, Alexander Paul Jones, Stuart Plant, Alexander Jackson
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Publication number: 20120189547Abstract: The present invention provides radiofluorinated compounds useful for in vivo imaging GABAA receptors. Also provided by the present invention is a method of synthesis for the radiofluorinated compounds of the invention, in particular an automated method of synthesis. A further aspect of the invention is a cassette suitable for carrying out the automated method of synthesis of the invention.Type: ApplicationFiled: October 8, 2010Publication date: July 26, 2012Inventors: John Woodcraft, Clare L. Jones, Alessandra Gaeta, William John Trigg, Paul Alexander Jones, Stuart Plant
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Patent number: 8088759Abstract: The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides novel 1,4-benzodiazepine-2,5-dione compounds, and methods of using novel 1,4-benzodiazepine-2,5-dione compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, and the like.Type: GrantFiled: November 1, 2006Date of Patent: January 3, 2012Assignee: The Regents of the University of MichiganInventor: Gary D. Glick
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Patent number: 7998954Abstract: The invention provides a pyrimidodiazepinone derivative represented by the general formula (I) [wherein n represents 1 or 2, Z represents a hydrogen atom or the like, R1 and R2 may be the same or different, and each represents a hydrogen atom or the like, A represents a bond, (CH2)m (wherein m represents an integer of 1 to 4), optionally substituted phenylene, optionally substituted pyridinediyl, or C?O, R3 represents a hydrogen atom, optionally substituted lower alkyl, or the like, and R4 represents a hydrogen atom or the like], or a pharmaceutically acceptable salt thereof or the like.Type: GrantFiled: June 2, 2008Date of Patent: August 16, 2011Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Nobumasa Otsubo, Yukihito Tsukumo, Kenji Uchida, Kyoichiro Iida, Hitoshi Arai, Shuko Okazaki, Takamichi Imaizumi
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Publication number: 20110196149Abstract: A method for the fluoridation of an iodonium salt with a fluoride ion source which can be carried out in an aqueous reaction solvent.Type: ApplicationFiled: April 18, 2011Publication date: August 11, 2011Applicant: GE HEALTHCARE LIMITEDInventors: HARRY JOHN WADSWORTH, PETER ANTHONY DEVENISH
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Publication number: 20110082111Abstract: Compounds of the following formula are provided for use with kinases: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: December 7, 2010Publication date: April 7, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Sheldon X. Cao, Victoria Feher, Takashi Ichikawa, Benjamin Jones, Stephen W. KALDOR, Andre A. KIRYANOV, Betty Lam, Yan Liu, Christopher McBride, Srinivasa Reddy Natala, Zhe Nie, Jeffrey A. Stafford
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Publication number: 20100137281Abstract: The present invention aims to provide a compound having superior pharmacological action, physicochemical properties and the like, which is useful for the prophylaxis or treatment s of circulatory diseases such as hypertension, cardiac diseases, arteriosclerosis, renal diseases, cerebral apoplexy and the like and/or metabolic diseases such as hyperlipidemia, obesity, diabetes and the like, central nervous disorders such as cerebral infarction and the like, mental diseases such as dementia, depression and the like, and the like. A compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: May 20, 2008Publication date: June 3, 2010Applicant: Takeda Pharmaceutical Company LimitedInventors: Takanobu Kuroita, Hideyuki Igawa, Hiroki Sakamoto, Kouhei Asano, Minoru Sasaki
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Publication number: 20100130479Abstract: The present invention provides molecules and methods for the prevention and/or treatment of memory deficit related conditions and/or enhancement of cognition. In a preferred embodiment, the invention includes compounds, salts and prodrugs thereof for the prevention and/or treatment of these conditions.Type: ApplicationFiled: August 31, 2009Publication date: May 27, 2010Inventors: James M. Cook, Terry Clayton, Yun Teng Johnson, Sundari Rallapalli, Dongmei Han
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Patent number: 7595395Abstract: The present invention provides molecules and methods for the prevention and/or treatment of memory deficit related conditions and/or enhancement of cognizance. In a preferred embodiment, the invention includes compounds, salts and prodrugs thereof for the prevention and/or treatment of these conditions.Type: GrantFiled: May 16, 2006Date of Patent: September 29, 2009Assignee: WiSys Technology FoundationInventors: James M. Cook, Dongmei Han, Terry Clayton
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Publication number: 20090221535Abstract: The present invention is directed to compounds of Formula I: I (where A1, A2, B1, B2, B3, B4, D1, D2, T, U, V, W, X, Y, Z. R4, R5a?, R5b, R5c, R6, m and n are defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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 CGRP is involved.Type: ApplicationFiled: September 9, 2005Publication date: September 3, 2009Inventors: Ian M. Bell, Steven N. Gallicchio, C. Blair Zartman, Cory R. Theberge, Xufang Zhang
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Patent number: 7528126Abstract: A compound of formula (I) and salts and solvates thereof, wherein: R10 is a nitrogen protecting group and R11 is either OH or O—R12, wherein R12 is an oxygen protecting group, or R10 and R11 together form a double bond between N10 and C11; and R10? and R11? are selected from the same options as R10 and R11 respectively.Type: GrantFiled: March 9, 2005Date of Patent: May 5, 2009Assignee: Spirogen LimitedInventors: Philip Wilson Howard, Stephen John Gregson, Peter William Taylor, David Edwin Thurston, Tsveta Stefanova Hadjivassileva
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Publication number: 20080234254Abstract: The present invention relates to a benzamide derivative comprising a head, spacer and cap group wherein the spacer includes a benzene ring substituted with an additional spacer and wherein the additional spacer is an unsaturated group.Type: ApplicationFiled: June 7, 2005Publication date: September 25, 2008Applicant: UNIVERSITY OF LEEDSInventors: Ronald Grigg, Andrew Cook
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Patent number: 7323458Abstract: The invention concerns a benzodiazepin derivative of formula (I) and their use for treating dyslipidemia, atherosclerosis, diabetes and its complications.Type: GrantFiled: July 4, 2000Date of Patent: January 29, 2008Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Jean-Jacques Berthelon, Daniel Guerrier, Michel Brunet, Jean-Jacques Zeiller, Francis Contard, Fréderic Ausseil
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Patent number: 7151097Abstract: Compounds of Formula (I) are described herein. The compounds have been shown to act as cannabinoid receptor ligands and are therefore useful in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals.Type: GrantFiled: October 22, 2004Date of Patent: December 19, 2006Assignee: Pfizer Inc.Inventors: Philip A. Carpino, Robert L. Dow, David A. Griffith
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Patent number: 7084135Abstract: A family of imidazole compounds useful for inhibiting the activity of prenyl transferases.Type: GrantFiled: December 30, 1999Date of Patent: August 1, 2006Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques, SASInventors: Thomas D. Gordon, Barry A. Morgan
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Patent number: 6979683Abstract: The invention relates to benzimidazole derivatives of general formula (I) in which X represents a nitrogen atom or a carbon atom; and when X represents a nitrogen atom R3 represents in particular a hydrogen atom or a (C1-C4)alkyl group, R4 represents in particular a hydrogen atom; a (C1-C6)alkyl; (C3-C7)cycloalkyl; 4-piperidyl; —(CH2)p—NR5R6; —(CH2)p—CONR5R6; —CO—(CH2)p—NR5R6; —(CH2)p-phenyl; —(CH2)p-morpholinyl; —(CH2)p-pyrrolidinyl; —(CH2)p-tetrahydroisoquinoline; —(CH2)p-heteroaryl; heteroarylcarbonyl; phenylcarbonyl; (C1-C6)alkylcarbonyl; —(CH2)p—COOR?; or phenylsulphonyl group; and when X represents a carbon atom R3 represents a hydrogen atom; a group —NR5R6; —NHCOR7; —CONHR5; —COR7; —NHCONH2; —OH or —CH2OH, R4 represents in particular a hydrogen atom; an optionally substituted group —(CH2)p-phenyl; a group —(CH2)p-heteroaryl; or a group —(CH2)tNR7R8. Preparation process and therapeutic application.Type: GrantFiled: November 21, 2001Date of Patent: December 27, 2005Assignee: Sanofi-SynthelaboInventors: Francis Barth, Daniel Bichon, Frank Bolkenius, Viviane Van Dorsselaer
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Patent number: 6838455Abstract: Disclosed are compounds which inhibit ?-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits ?-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: December 23, 2002Date of Patent: January 4, 2005Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: James E. Audia, Warren J. Porter, Richard C. Thompson, Stephen C. Wilkie, Douglas R. Stack, Qing Shi
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Patent number: 6774125Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: October 7, 2002Date of Patent: August 10, 2004Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & CompanyInventors: James E. Audia, Richard C. Thompson, Stephen C. Wilkie, Thomas C. Britton, Warren J. Porter, George W. Huffman, Lee H. Latimer
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Publication number: 20040116410Abstract: The invention is novel compounds of formula (I) which exhibit an improved therapeutic index and improved metabolic stability which are useful in the treatment and/or prevention of herpes viral infections. Novel intermediates useful in the synthesis of the final compounds are also part of the invention.Type: ApplicationFiled: February 18, 2003Publication date: June 17, 2004Inventors: Hidetsura Cho, Rocco Dean Gogliotti, Harriet Wall Hamilton, Alexei Krasutsky, Takeshi Nakamura, Hiroki Tada, Peter Craig Weber
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Patent number: 6696438Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: December 12, 2002Date of Patent: February 24, 2004Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & CompanyInventors: James E. Audia, Bruce A. Dressman, Qing Shi
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Publication number: 20040029866Abstract: The invention relates to benzimidazole derivatives of general formula (I) 1Type: ApplicationFiled: May 23, 2003Publication date: February 12, 2004Inventors: Francis Barth, Daniel Bichon, Frank Bolkenius, Viviane Van Dorsselaer
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Patent number: 6686349Abstract: The invention relates to novel tetracyclic pyrroloquinolone derivatives of the formula (I) or (II): wherein all variables are as herein defined, pharmaceutical compositions containing the compounds and their use for the treatment of sexual dysfunction.Type: GrantFiled: November 12, 2002Date of Patent: February 3, 2004Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Weiqin Jiang, Zhihua Sui
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Patent number: 6683075Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: January 6, 2003Date of Patent: January 27, 2004Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
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Patent number: 6653303Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: January 6, 2003Date of Patent: November 25, 2003Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
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Patent number: 5962450Abstract: The invention is concerned with basically-substituted imidazodiazepines of general formula I. These compounds can be used as anxiolytic and/or anticonvulsant and/or muscle relaxant and/or sedative-hypnotic active substances.Type: GrantFiled: November 25, 1997Date of Patent: October 5, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Buttelmann, Thierry Godel
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Patent number: 5817808Abstract: The object of the present invention is to provide an improved process for preparing benzodiazepine-3-alkyl carboxylate of formula(I) and its pharmaceutically acceptable salts and esters. ##STR1## wherein R.sup.1 is methyl, ethyl or isopropyl;R.sup.2 and R.sup.3 are each independently hydrogen or C.sub.1 -C.sub.6 lower alkyl;R.sup.4 is hydrogen, halogen or trifluoromethyl;carbon atom denoted as c has the S-- or R, S-- configuration.Type: GrantFiled: September 8, 1997Date of Patent: October 6, 1998Assignee: Dong Kook Pharmaceutical Company, Inc.Inventors: Yong Hae Kim, Jin Kyu Park, Kwon Kim, Hee Sock Park
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Patent number: 5786352Abstract: Novel compounds of the following general formula or salts thereof. ##STR1## wherein Ring M is a heterocyclic ring having --N.dbd.C<, --CO--N< or --CS--N< as the partial structure --X . . . Y<; R.sup.a and R.sup.b are bonded to each other to form Ring A, or they are the same or different and represent, independently, a hydrogen atom or a substituent on the Ring M; Ring A and Ring B represent, independently, an optionally substituted homocyclic or heterocyclic ring, and at least one of them is optionally substituted heterocyclic ring; Ring C is optionally substituted homocyclic or heterocyclic ring; Ring Z is an optionally substituted ring; and n represents an integer of from 1 to 6, or a salt thereof, which has an excellent tachykinin receptor antagonistic effect, and their production, and pharmaceutical compositions.Type: GrantFiled: March 25, 1996Date of Patent: July 28, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideaki Natsugari, Takenori Ishimaru, Takayuki Doi, Yoshinori Ikeura, Chiharu Kimura
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Patent number: 5716951Abstract: A tricylic benzodiazepine derivative that acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII.sub.b III.sub.a receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.Type: GrantFiled: May 8, 1995Date of Patent: February 10, 1998Assignee: Genentech, Inc.Inventors: Brent K. Blackburn, Kirk Robarge, Todd C. Somers
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Patent number: 5705890Abstract: A tricylic benzodiazepine derivative that acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII.sub.b III.sub.a receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.Type: GrantFiled: September 26, 1994Date of Patent: January 6, 1998Assignee: Genentech, Inc.Inventors: Brent K. Blackburn, Kirk Robarge, Todd C. Somers
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Patent number: 5670640Abstract: A process for the manufacture of compounds of formula ##STR1##Type: GrantFiled: December 9, 1996Date of Patent: September 23, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Mark Rogers-Evans, Paul Spurr
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Patent number: 5665718Abstract: The invention relates to compounds of the formula ##STR1## wherein A together with the two carbon atoms denoted by .alpha. and .beta. is one of the residues ##STR2## Q is one of the residues ##STR3## R.sup.1 and R.sup.2 each independently are hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower hydroxyalkyl, lower alkoxy-lower alkyl, (C.sub.3 -C.sub.6)-cycloalkyl, (C.sub.3 -C.sub.6)-cycloalkyl-lower alkyl, amino-lower alkyl, lower alkylamino-lower alkyl, di-lower alkylamino-lower alkyl or aryl-lower alkyl or together with the nitrogen atom are a 5- to 8-membered membered heterocycle optionally containing a further hetero atom or a fused benzene ring,R.sup.3 is hydrogen and R.sup.4 is lower alkyl or R.sup.3 and R.sup.4 together are dimethylene or trimethylene andR.sup.5 and R.sup.6 each independently are hydrogen, halogen, trifluoromethyl, lower alkoxy or nitro,the compounds of formula I having the (S) configuration with reference to the carbon atom denoted by .gamma. when R.sup.3 and R.sup.Type: GrantFiled: January 16, 1996Date of Patent: September 9, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Thierry Godel, Walter Hunkeler, Heinz Stadler, Ulrich Widmer
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Patent number: 5532359Abstract: Benzodiazepine derivatives are disclosed that act as potent inhibitors of ras farnesyl:protein transferase. Pharmaceutical compositions containing these benzodiazepines are provided for treatment of diseases for which inhibition of the ras farnesyl:protein transferase is indicated.Type: GrantFiled: October 25, 1994Date of Patent: July 2, 1996Assignees: Genentech, Inc., Board of Regents, The University of Texas SystemInventors: James C. Marsters, Jr., Michael S. Brown, Craig W. Crowley, Joseph L. Goldstein, Guy L. James, Robert S. McDowell, David Oare, Thomas E. Rawson, Mark Reynolds, Todd C. Somers
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Patent number: 5493020Abstract: A trycylic benzodiazepine derivative which acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII.sub.b III.sub.a receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.Type: GrantFiled: July 29, 1993Date of Patent: February 20, 1996Assignee: Genentech, Inc.Inventors: Brent K. Blackburn, Kirk Robarge, Todd C. Somers
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Patent number: 5468854Abstract: Conjugates of fluorescent labels with specific, selective, and high affinity ligands for receptors have been synthesized and used to directly measure binding to receptors. In the examples, fluorescein conjugates of the high-affinity benzodiazepine receptor ligands Ro 15-1788 and Ro 7-1986 were synthesized. The binding of these fluorescent ligands (BD 621, BD 623 and BD 607) to benzodiazepine receptors was characterized by direct fluorescence measurement. Both the equilibrium dissociation constants (K.sub.D) of BD 621 and BD 607 and the maximum number of binding sites (B.sub.max) estimated by fluorescence monitoring were consistent with values obtained by using radioligand binding techniques. The binding of BD 621 and BD 607 assessed by fluorescence measurement was reversible, abolished by photoaffinity labeling with Ro 15-4513, and unaffected by a variety of substances that do not bind to benzodiazepine receptors.Type: GrantFiled: July 22, 1993Date of Patent: November 21, 1995Assignee: Pharmaceutical Discovery CorporationInventors: R. Tyler McCabe, Brian R. de Costa
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Patent number: 5247079Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein Y is a nitrogen atom or carbon atom bearing Z, Z is selected from the group consisting of hydrogen, halogen, --C.ident.N, --N.sub.3 and --C(Hal).sub.3, Hal is a halogen, X is cycloalkyl of 3 to 6 carbon atoms or hydrogen with the proviso that when X is hydrogen, Y must be nitrogen, R is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, phenyl and substituted phenyl and their non-toxic, pharmaceutically acceptable acid addition salts, a process and intermediate for preparing them, having tranquillizing properties.Type: GrantFiled: October 23, 1991Date of Patent: September 21, 1993Assignee: Roussel UclafInventors: Charles J. R. Hedgecock, Stuart D. Jones
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Patent number: 5210209Abstract: The invention provides a method for the production of a pyrazolo(1,5-a)benzimidazole of the general formula (A): ##STR1## wherein R is a substituted or unsubstituted alkyl or aryl group, andR.sup.1 -R.sup.4 =R, H, halogen, OR, COOR, CONHR, SO.sub.2, NO.sub.2 NHR, NR.sub.2, or CN, andX is hydogen or a reactive group releasable on coupling with an oxidized color developer, wherein the invention provides reacting a 2-amino or 2-mercapto substituted benzimidazole to form a triazepinone or a thiadiazino derivative respectively, ring contracting said triazepinone or thiadiazino derivative to give the corresponding 2-methylpyrazolobenzimidazole product, and subsequently removing the substituents at the -3 or -4 positions to provide a compound of the general formula (1).Type: GrantFiled: June 3, 1991Date of Patent: May 11, 1993Assignee: Eastman Kodak CompanyInventor: Michael W. Crawley
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Patent number: 5109013Abstract: Novel compounds of the formula: ##STR1## wherein R and R.sup.1 are C.sub.1 -C.sub.6 alkyl or cycloalkyl and R.sup.2 and R.sup.3 are independently selected from C.sub.1 -C.sub.6 alkyl or aryl or --NR.sup.2 R.sup.3 forms a heterocyclic group which may be further substituted are disclosed. These compounds were found to possess muscle relaxant properties.Type: GrantFiled: June 6, 1990Date of Patent: April 28, 1992Assignee: A. H. Robins Company, IncorporatedInventors: Albert D. Cale, Jr., Thomas W. Gero
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Patent number: 5096695Abstract: Radioiodine 5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine derivatives and their use as brain imaging agents.Type: GrantFiled: June 25, 1990Date of Patent: March 17, 1992Assignee: Hoffmann-LaRoche Inc.Inventors: Heinz Carmann, Walter Hunkeler