The Additional Cyclo Consists Of Two Nitrogens And Three Carbons (e.g., Imidazobenzodiazepines, Etc.) Patents (Class 540/562)
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Patent number: 12083126Abstract: Pharmaceutical compositions and methods for inducing conscious sedation using such compositions are described, the compositions including a benzodiazepine-based compound, an NMDA antagonist, and optionally a ?-blocker, antiemetic, an NSAID, and/or an antihistamine medication. Compositions may be incorporated into vehicles for extended release. Methods for fabricating the compositions and using them for anesthesiological applications are also described.Type: GrantFiled: April 29, 2022Date of Patent: September 10, 2024Assignee: MELT PHARMACEUTICALS, INC.Inventor: Dennis Elias Saadeh
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Patent number: 9156842Abstract: The invention concerns a new process for preparing 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]-propionic acid methyl ester or 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]propionic acid methyl ester benzene sulfonate (P) which comprises reacting 3-[(S)-7-bromo-2-((R and/or S)-2-hydroxy-propylamino)-5-pyridin-2-yl-3H-benzo[e][1,4]diazepin-3-yl]-propionic acid methyl ester of formula (EM) with an oxidizing agent and optionally treating the reaction product under acidic conditions, such as to produce the compound of formula (F) or the compound (P), and new compounds useful as starting material or as intermediate for performing that process.Type: GrantFiled: September 15, 2010Date of Patent: October 13, 2015Assignee: PAION UK LIMITEDInventors: Gary Stuart Tilbrook, Andreas Schumacher, René Emmenegger
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Patent number: 9006233Abstract: 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: GrantFiled: April 27, 2012Date of Patent: April 14, 2015Assignee: 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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Patent number: 8981083Abstract: The invention features compositions and methods for treating or preventing a neoplasia. More specifically, the invention provides compositions and methods for disrupting the interaction of a BET family polypeptide comprising a bromodomain with chromatin (e.g., disrupting a bromodomain interaction with an acetyl-lysine modification present on a histone N-terminal tail).Type: GrantFiled: May 16, 2011Date of Patent: March 17, 2015Assignee: Dana Farber Cancer Institute, Inc.Inventors: James Elliott Bradner, Jun Qi
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Patent number: 8835424Abstract: In preferred embodiments, the present invention provides methods of treatment and pharmaceutical compositions for the suppression, alleviation and prevention of the often chronic, severe and debilitating pain that can accompany inflammatory diseases and neuropathic insults, pain that is often unresponsive to conventional analgesic treatment. The preferred embodiments of the present invention further relate to methods of treatment and pharmaceutical compositions using benzodiazepine derivatives that provide suppression, alleviation and prevention of neuropathic pain, migraine-related pain and inflammatory pain with reduced sedative and ataxic side effects.Type: GrantFiled: May 13, 2010Date of Patent: September 16, 2014Assignee: Wisconsin Alumni Research FoundationInventors: James Cook, Shengming Huang, Rahul Edwankar, Ojas A. Namjoshi, Zhi-Jian Wang
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Publication number: 20140228320Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I):Type: ApplicationFiled: April 15, 2014Publication date: August 14, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Takahiko TANIGUCHI, Masato YOSHIKAWA, Kasei MIURA, Tomoaki HASUI, Eiji HONDA, Keisuke IMAMURA, Makoto KAMATA, Haruhi KAMISAKI, John F. QUINN, Joseph RAKER, Fatoumata CAMARA, Yi WANG
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Publication number: 20140081018Abstract: Disclosed is the synthesis of [18F]flumazenil that is useful in imaging epileptic lesions by PET (positron emission tomography). A method for preparing [18F]flumazenil by reacting a diaryliodonium salt precursor with the positron-emitting radionuclide fluorine-18. [18F]flumazenil can be prepared from the diaryliodonium salt precursor in the presence of kryptofix2.2.2./potassium carbonate(K2.2.2./K2CO3) and TEMPO in dimethylformamide (DMF) at a high yield.Type: ApplicationFiled: November 22, 2013Publication date: March 20, 2014Applicant: BIO IMAGING KOREA CO., LTD.Inventors: Byung Chul Lee, Byung Seok Moon, Ji Sun Kim
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Patent number: 8642588Abstract: The invention relates to esylate salts of the compound of formula (I): Methods of preparing the salts, and their use as medicaments, in particular for sedative or hypnotic, anxiolytic, muscle relaxant, or anticonvulsant purposes is also described.Type: GrantFiled: July 10, 2007Date of Patent: February 4, 2014Assignee: PAION UK LimitedInventors: Gary Stuart Tilbrook, Louisa Jane Cubitt
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Patent number: 8557981Abstract: The present invention refers to a process for the preparation of 4H-imidazo[1,5-a][1,4]benzodiazepines, in particular Midazolam, through an efficient and selective decarboxylation reaction of the derivative compound of the 5-aminomethyl-1-phenyl-1H-imidazole-4-carboxylic acid of formula (II) avoiding the formation of the 6H-imidazo[1,5-a][1,4]benzodiazepines by-products and the ensuing process for the isomerization of a 4H-imidazo[1,5-a][1,4]benzodiazepine product.Type: GrantFiled: May 3, 2011Date of Patent: October 15, 2013Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.Inventors: Andrea Castellin, Michele Maggini, Paola Donnola
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Publication number: 20130172328Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I):Type: ApplicationFiled: June 22, 2011Publication date: July 4, 2013Applicant: CROSSWING INC.Inventors: Takahiko Taniguchi, Masato Yoshikawa, Kasei Miura, Tomoaki Hasui, Eiji Honda, Keisuke Imamura, Makoto Kamata, Haruhi Kamisaki, John F. Quinn, Joseph Raker, Fatoumata Camara, Yi Wang
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Patent number: 8455479Abstract: The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising compounds of Formula I and methods of treating or preventing one or more conditions that may be regulated or normalized via inhibition of dipeptidyl peptidase IV (DPP-IV).Type: GrantFiled: January 23, 2009Date of Patent: June 4, 2013Assignee: Panacea Biotec LimitedInventors: Rajesh Jain, Sanjay Trehan, Jagattaran Das, Nishan Singh, Gurmeet Kaur Nanda, Sitaram Kumar Magadi, Sudhir Kumar Sharma
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Publication number: 20130023524Abstract: Tricyclic indazole compound and its pharmaceutically acceptable salts of acid addition, use thereof, method and intermediates for preparing them, and a pharmaceutical composition containing them. The tricyclic indazole compound has the following general Formula (I): in which R1, R2, L1, L2, X1, X2, X3, X4, X5, Y, W, m, and n have the meanings stated in the description.Type: ApplicationFiled: March 4, 2011Publication date: January 24, 2013Applicant: AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.Inventors: Maria Alessandra Alisi, Nicola Cazzolla, Guido Furlotti, Beatrice Garrone, Gabriele Magaro', Giorgina Mangano
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Publication number: 20120330007Abstract: The invention concerns a new process for preparing 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]-propionic acid methyl ester or 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]propionic acid methyl ester benzene sulfonate (P) which comprises reacting 3-[(S)-7-bromo-2-((R and/or S)-2-hydroxy-propylamino)-5-pyridin-2-yl-3H-benzo[e][1,4]diazepin-3-yl]-propionic acid methyl ester of formula (EM) with an oxidizing agent and optionally treating the reaction product under acidic conditions, such as to produce the compound of formula (F) or the compound (P), and new compounds useful as starting material or as intermediate for performing that process.Type: ApplicationFiled: September 15, 2010Publication date: December 27, 2012Applicant: PAION UK LimitedInventors: Gary Stuart Tilbrook, Andreas Schumacher, René Emmengger
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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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Patent number: 8278297Abstract: In one aspect, the invention provides compounds of Formula I or pharmaceutically acceptable salts thereof. In another aspect, the invention provides methods for treatment of diseases or disorders mediated by a protein kinase, comprising administering a therapeutically effective amount of a compound of this invention.Type: GrantFiled: December 23, 2010Date of Patent: October 2, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Steven Durrant
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Patent number: 8252787Abstract: In one aspect, the invention provides compounds of Formula I or pharmaceutically acceptable salts thereof. In another aspect, the invention provides methods for treatment of diseases or disorders mediated by a protein kinase, comprising administering a therapeutically effective amount of a compound of this invention.Type: GrantFiled: December 23, 2010Date of Patent: August 28, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Steven Durrant
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Publication number: 20120184536Abstract: The present invention encompasses compositions comprising UGT inhibitors. Additionally, the invention encompasses methods of reducing the glucuronidation of a compound using a UGT inhibitor.Type: ApplicationFiled: February 27, 2012Publication date: July 19, 2012Applicant: The Board of Trustees of the University of ArkansasInventor: Anna Radominska-Pandya
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Patent number: 8202858Abstract: The present invention concerns compounds inter alia according to general formula 1a. Compounds according to the invention are vasopressin V1a receptor antagonists. Pharmaceutical compositions of the compounds are useful as treatment of dysmenorrhoea.Type: GrantFiled: August 24, 2005Date of Patent: June 19, 2012Assignee: Vantia LimitedInventors: Andrzej Roman Batt, Martin Lee Stockley, Michael Bryan Roe, Celine Marguerite Simone Heeney, Andrew John Baxter, Peter Hudson, Rachel Handy
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Patent number: 8119629Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.Type: GrantFiled: September 29, 2008Date of Patent: February 21, 2012Assignee: Bristol-Meyers Squibb CompanyInventor: Ronald J. Mattson
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Publication number: 20110319394Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia. The compound is represented by the formula (I): wherein the symbols are defined in the specification.Type: ApplicationFiled: June 22, 2011Publication date: December 29, 2011Inventors: Takahiko TANIGUCHI, Masato YOSHIKAWA, Kasei MIURA, Tomoaki HASUI, Eiji HONDA, Keisuke IMAMURA, Makoto KAMATA, Haruhi KAMISAKI, John F. QUINN, Joseph RAKER, Fatoumata CAMARA, Yi WANG
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Patent number: 8063032Abstract: Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.Type: GrantFiled: February 11, 2010Date of Patent: November 22, 2011Assignee: Sunovion Pharmaceuticals Inc.Inventors: Milan Chytil, Qun Kevin Fang, Kerry L. Spear
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Publication number: 20110224195Abstract: The present invention is directed to substituted six-membered heterocyclic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as obesity and diabetes, particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: August 18, 2008Publication date: September 15, 2011Inventors: Tesfaye Biftu, Danqing Feng, Ann E. Weber, Jason M. Cox, Xiaoxia Qian, Jinyou Xu
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Patent number: 7947678Abstract: Compounds of formula I: (where variables R2, R7, D, W, X, Y and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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: GrantFiled: July 25, 2006Date of Patent: May 24, 2011Assignee: Merck Sharp & Dohme Corp.Inventor: Theresa M. Williams
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Publication number: 20100311732Abstract: The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising compounds of Formula I and methods of treating or preventing one or more conditions that may be regulated or normalized via inhibition of dipeptidyl peptidase IV (DPP-IV).Type: ApplicationFiled: January 23, 2009Publication date: December 9, 2010Inventors: Rajesh Jain, Sanjay Trehan, Jagattaran Das, Nishan Singh, Gurmeet Kaur Nanda, Sitaram Kumar Magadi, Sudhir Kumar Sharma
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Publication number: 20100298287Abstract: There is provided a compound of the formula (I?): wherein X is a nitrogen or CRx, Rx is a hydrogen, etc., R1 is an optionally substituted hydrocarbon group, etc., R2 is an optionally substituted hydrocarbon group, etc., ring A is 5- to -8-membered heterocyclic ring, etc., and each of Y1, Y2 and Y3 is an optionally substituted carbon or a nitrogen, etc.; or ‘a salt thereof or a prodrug thereof, which have CRF receptor antagonistic activity and use thereof.Type: ApplicationFiled: January 21, 2009Publication date: November 25, 2010Inventors: Kazuyoshi Aso, Katsumi Kobayashi, Takafumi Takai, Takuto Kojima, Kazuyuki Tokumaru, Michiyo Mochizuki, Yasutaka Hoashi
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Publication number: 20100234417Abstract: A hetero-dimeric or hetero-oligomeric receptor, comprising at least one thyrotropin releasing hormone receptor subunit associated with at least one orexin receptor subunit.Type: ApplicationFiled: November 9, 2007Publication date: September 16, 2010Applicant: DIMERIX BIOSCIENCE PTY LTD.Inventors: Kevin Donald George Pfleger, Ruth Marie Seeber, Heng See Boon, Karin Ann Eidne
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Patent number: 7776852Abstract: Provided is a process for producing highly pure midazolam and salts thereof, and a pharmaceutical composition containing the highly pure midazolam and/or a salt thereof.Type: GrantFiled: September 11, 2007Date of Patent: August 17, 2010Assignee: CHEMAGIS Ltd.Inventors: Sonia Krivonos, Yana Sery
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Publication number: 20100204214Abstract: Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.Type: ApplicationFiled: February 11, 2010Publication date: August 12, 2010Inventors: Milan Chytil, Sharon R. Engel, Qun Kevin Fang, Kerry L. Spear
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Patent number: 7700588Abstract: Compositions of midazolam, a benzodiazapine, in concentrations of 35-100 mg/ml are disclosed for the treatment of anxiety, epilepsy and epileptic seizures, invasive surgical procedures and diagnostic procedures and sedation. These compositions are particularly characterized by a solubilizer such an propylene glycol. Preferably, the compositions are aqueous solutions for intranasal administration.Type: GrantFiled: January 13, 2005Date of Patent: April 20, 2010Inventor: Franciscus Wilhelmus Henricus Maria Merkus
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Publication number: 20100081647Abstract: The invention relates to besylate salts of the compound of formula (I): Methods of preparing the salts, and their use as medicaments, in particular for sedative or hypnotic, anxiolytic, muscle relaxant, or anticonvulsant purposes is also described.Type: ApplicationFiled: July 10, 2007Publication date: April 1, 2010Applicant: PAION UK LimitedInventors: Gary Stuart Tilbrook, Louisa Jane Cubitt
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Publication number: 20100075955Abstract: The invention relates to esylate salts of the compound of formula (I): Methods of preparing the salts, and their use as medicaments, in particular for sedative or hypnotic, anxiolytic, muscle relaxant, or anticonvulsant purposes is also described.Type: ApplicationFiled: July 10, 2007Publication date: March 25, 2010Inventors: Gary Stuart Tilbrook, Louisa Jane Cubitt
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Patent number: 7625888Abstract: The present invention is directed to novel fused triazole derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: August 19, 2005Date of Patent: December 1, 2009Assignee: Merck & Co., Inc.Inventors: Ann E. Weber, Wallace T. Ashton
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Patent number: 7618958Abstract: The present invention provides compositions and methods of using stereospecific benzodiazepine derivatives, their salts and prodrugs for the treatment of anxiolytic or convulsant disorders having the side effects of reduced alcohol craving in human alcoholics and a concomitant reduced sedative, hypnotic, muscle relaxant and ataxic side-effects. The invention further provides pharmaceutical compositions for treatment of anxiolytic and convulsant disorders in subjects in need thereof, comprising a compound, prodrug or a salt having a chemical structure represented by any one of Formula I-XXI and a pharmaceutically-acceptable carrier.Type: GrantFiled: June 30, 2005Date of Patent: November 17, 2009Assignee: WISYS Technology Foundation, Inc.Inventors: James M. Cook, Hao Zhou, Shengming Huang, P.V.V. Srirama Sarma, Chunchun Zhang
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Publication number: 20090093466Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.Type: ApplicationFiled: September 29, 2008Publication date: April 9, 2009Inventor: Ronald J. Mattson
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Publication number: 20090069306Abstract: Provided is a process for producing highly pure midazolam and salts thereof, and a pharmaceutical composition containing the highly pure midazolam and/or a salt thereof.Type: ApplicationFiled: September 11, 2007Publication date: March 12, 2009Applicant: CHEMAGIS LTD.Inventors: Sonia KRIVONOS, Yana SERY
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Patent number: 7485635Abstract: The present invention provides a compound of formula (I): wherein all variables are as defined herein, pharmaceutical formulations containing the same, processes for preparing the same and their use therapy.Type: GrantFiled: December 5, 2006Date of Patent: February 3, 2009Assignee: CeNes LimitedInventors: Paul L. Feldman, David Kendall Jung, Istvan Kaldor, Gregory J. Pacofsky, Jeffrey A. Stafford, Jeffrey H. Tidwell
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Patent number: 7459414Abstract: Compounds of formula wherein the substituents have the meanings given in claim 1, and agronomically tolerable salts, isomers and enantiomers of those compounds, are suitable for use as herbicides.Type: GrantFiled: March 18, 2005Date of Patent: December 2, 2008Assignee: Syngenta Crop Protection, Inc.Inventors: Thomas Maetzke, André Stoller, Sebastian Wendeborn, Henry Szczepanski
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Patent number: 7435730Abstract: The present invention provides a compound of formula (I): wherein all variables are as defined herein, pharmaceutical formulations containing the same, processes for preparing the same and their use therapy.Type: GrantFiled: January 5, 2007Date of Patent: October 14, 2008Assignee: CeNeS LimitedInventors: Paul L. Feldman, David Kendall Jung, Istvan Kaldor, Gregory J. Pacofsky, Jeffrey A. Stafford, Jeffrey H. Tidwell
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Patent number: 7407949Abstract: Novel compounds according to general formula 1, wherein G1 is NR5R6 or a fused polycyclic group that are specific OT receptor agonists and/or V1a receptor antagonists. Pharmaceutical compositions comprising such compounds are useful in the treatment of, inter alia, primary dysmenorrhoea.Type: GrantFiled: February 12, 2004Date of Patent: August 5, 2008Assignee: Ferring B.V.Inventors: Peter Hudson, Andrzej Roman Batt, Celine Marguerite Simone Heeney, Andrew John Baxter, Michael Bryan Roe, Peter Andrew Robson
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Patent number: 7238685Abstract: The invention relates to novel benzo-fused heterocycles and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as endothelin receptor antagonists.Type: GrantFiled: July 31, 2002Date of Patent: July 3, 2007Assignee: Actelion Pharmaceuticals Ltd.Inventors: Martin Bolli, Christoph Boss, Martine Clozel, Walter Fischli, Thomas Weller, Judith Marfurt
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Patent number: 7119196Abstract: Orally active benzodiazepine derivatives and their salts are disclosed. These compounds and their salts have anxiolytic and anticonvulsant activity with reduced sedative/hypnotic/muscle relaxant/ataxic effects.Type: GrantFiled: March 28, 2003Date of Patent: October 10, 2006Assignee: Wisys Technology Foundation, Inc.Inventors: James M. Cook, Qi Huang, Xiaohui He, Xioayan Li, Jianming Yu, Dongmei Han, Snjezana Lelas, John F. McElroy
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Patent number: 7105509Abstract: A novel class of 1,4- and 1,5-benzodiazepines of formula (I) is disclosed.Type: GrantFiled: May 21, 2001Date of Patent: September 12, 2006Assignee: Merck Sharp & Dohme LimitedInventors: Jose Luis Castro Pineiro, Ian Churcher, Alexander Richard Guiblin, Timothy Harrison, Sonia Kerrard, Andrew Madin, Alan John Nadin, Andrew Pate Owens, Timothy Jason Sparey, Martin Richard Teall, Susannah Williams
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Patent number: 6894005Abstract: Compounds of formula wherein the substituents have the meanings given in claim 1, and agronomically tolerable salts, isomers and enantiomer of those compounds, are suitable for use as herbicides.Type: GrantFiled: September 5, 2000Date of Patent: May 17, 2005Assignee: Syngenta Crop Protection, Inc.Inventors: Thomas Maetzke, André Stoller, Sebastian Wendeborn, Henry Szczepanski
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Patent number: 6784292Abstract: The invention relates to a method for the preparation of compound of formula (1). The invention further relates to the previously unknown compounds of formulas (5 and 6) as intermediates in the production of benzodiazepines of formula (1).Type: GrantFiled: August 21, 2003Date of Patent: August 31, 2004Assignee: Schering AGInventors: Eric Winter, Matthias Schneider, Ulf Tilstam
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Patent number: 6511974Abstract: This invention relates to new compounds selected from those of the general formula (I), or a pharmaceutically acceptable salt, ester or prodrug form thereof: wherein D, E and G are N or CH, which serve as vasopressin agonists and are useful in treating disorders such as diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, and the inability to temporarily delay urination and pharmaceutical compositions and methods for same.Type: GrantFiled: July 24, 1998Date of Patent: January 28, 2003Assignee: WyethInventors: John P. Dusza, Peter S. Chan, Jay D. Albright, Jehan F. Bagli, Amedeo A. Failli, Mark A. Ashwell, Albert J. Molinari, Thomas J. Caggiano, Eugene J. Trybulski
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Patent number: 6512114Abstract: The present invention provides a process for the synthesis of Midazolam I from a compound of formula II, using thermodynamic, basic workup conditions. Additional steps to isolate the pure bulk product follow.Type: GrantFiled: June 30, 1999Date of Patent: January 28, 2003Assignee: Abbott LaboratoriesInventors: Madhup K. Dhaon, Grant L. Esser, Deborah A. Davis, Ashok V. Bhatia
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Patent number: 6482819Abstract: 2,3-Benzodiazepines of formula (I), their stereoisomers and acid addition salts, wherein the variables have the meaning given in the specification, and pharmaceutical compositions containing them which are suitable for treating conditions associated with muscle spasms, epilepsy as well as acute and chronic forms of neurodegenerative diseases are disclosed.Type: GrantFiled: April 10, 2000Date of Patent: November 19, 2002Assignee: Gyogyszerkutato Intezet Kft.Inventors: Gizella Ábrahám, Emese Csuzdi, Sándor Sólyom, Pál Berzsenyi, István Tarnawa, Ferenc Andrási, István Ling, Tamás Hámori, Katalin Horváth, Imre Moravcsik, István Pallagi, Antal Simay
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Patent number: 6413956Abstract: Disclosed are compounds of Formula I: or the pharmaceutically acceptable salts thereof where, R1, R2, and W are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.Type: GrantFiled: May 5, 2000Date of Patent: July 2, 2002Assignee: Neurogen CorporationInventors: Pamela A. Albaugh, Kevin S. Currie, Dan Rosewater, Guolin Cai
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Patent number: 6323197Abstract: The invention concerns compounds of formula (I), in which R1, R2, R3 and R4 mean hydrogen or different substituents; X means hydrogen or halogen; Y means C1-6 alkoxy or X and Y together mean —O—(CH2)n—O—; n means 1, 2 or 3; and A together with nitrogen forms a saturated or unsaturated five-member heterocycle which can contain between 1 and 3 nitrogen atoms and/or an oxygen atom and/or one or two carbonyl groups. Owing to their non-competitive inhibiting of the AMPA receptors, these compounds can be used as medicaments for treating diseases of the central nervous system.Type: GrantFiled: November 5, 1998Date of Patent: November 27, 2001Assignee: Schering AktiengesellschaftInventors: Ernese Csuzdi, Tamas Hámori, Gizella Ábrahám, Sändor Sólyom, István Tarnawa, Pál Berzsenyi, Ferenc Andrási, István Ling, Antal Simay, Melinda Gál, Katalin Horváth, Eszter Szentkuti, Márta Szöllosy, István Pallagi
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Patent number: RE47475Abstract: In preferred embodiments, the present invention provides methods of treatment and pharmaceutical compositions for the suppression, alleviation and prevention of the often chronic, severe and debilitating pain that can accompany inflammatory diseases and neuropathic insults, pain that is often unresponsive to conventional analgesic treatment. The preferred embodiments of the present invention further relate to methods of treatment and pharmaceutical compositions using benzodiazepine derivatives that provide suppression, alleviation and prevention of neuropathic pain, migraine-related pain and inflammatory pain with reduced sedative and ataxic side effects.Type: GrantFiled: September 16, 2016Date of Patent: July 2, 2019Assignee: WISYS TECHNOLOGY FOUNDATION, INC.Inventors: James M. Cook, Shengming Huang, Rahul Edwankar, Ojas A. Namjoshi, Zhi-Jian Wang, Qi Huang, Xiaohui He, Xiaoyan Li, Jianming Yu, Dongmei Han