Nitrogen Of The Hetero Ring Is Shared By An Additional Cyclo Of The Tetracyclo Ring System Patents (Class 540/494)
-
Patent number: 9617270Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VII). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.Type: GrantFiled: February 13, 2015Date of Patent: April 11, 2017Assignee: IMMUNOGEN, INC.Inventors: Wei Li, Michael Louis Miller, Ravi V. J. Chari
-
Publication number: 20150099874Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VII). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.Type: ApplicationFiled: October 10, 2014Publication date: April 9, 2015Inventors: Wei Li, Michael Louis Miller, Nathan Elliott Fishkin, Ravi V.J. Chari
-
Publication number: 20150030616Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: ApplicationFiled: June 26, 2014Publication date: January 29, 2015Inventors: Wei Li, Nathan Elliott Fishkin, Robert Yongxin Zhao, Michael Louis Miller, Ravi V.J. Chari
-
Patent number: 8889669Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VII). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.Type: GrantFiled: March 14, 2013Date of Patent: November 18, 2014Assignee: ImmunoGen, Inc.Inventors: Wei Li, Michael Louis Miller, Nathan Elliott Fishkin, Ravi V. J. Chari
-
Patent number: 8846906Abstract: The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.Type: GrantFiled: September 14, 2012Date of Patent: September 30, 2014Assignee: Arena Pharmaceuticals, Inc.Inventors: Jeffrey Smith, Brian Smith
-
Patent number: 8835626Abstract: The present invention relates to compounds of the formula (1) which are suitable for use in electronic devices, in particular organic electroluminescent devices.Type: GrantFiled: February 25, 2011Date of Patent: September 16, 2014Assignee: Merck Patent GmbHInventors: Amir Hossain Parham, Christof Pflumm, Teresa Mujica-Fernaud
-
Patent number: 8809320Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: GrantFiled: February 22, 2013Date of Patent: August 19, 2014Assignee: ImmunoGen, Inc.Inventors: Wei Li, Nathan Elliott Fishkin, Robert Yongxin Zhao, Michael Louis Miller, Ravi V. J. Chari
-
Patent number: 8802667Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: GrantFiled: March 14, 2013Date of Patent: August 12, 2014Assignee: ImmunoGen, Inc.Inventors: Wei Li, Nathan Elliott Fishkin, Robert Yongxin Zhao, Michael Louis Miller, Ravi V. J. Chari
-
Patent number: 8765740Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VII). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.Type: GrantFiled: February 15, 2012Date of Patent: July 1, 2014Assignee: ImmunoGen, Inc.Inventors: Wei Li, Michael Miller, Nathan Fishkin, Ravi V. J. Chari
-
Patent number: 8759339Abstract: The present invention provides a compound of general formula A, useful as potential antitumour agents against five human cancer cell lines. The present invention further provides a process for the preparation of pyrrolo[2,1-c][1,4]naphthodiazepine linked substituted piperazine conjugates attached through different alkane spacers of general formula A. (Formula I) General formula A. Where R=R?=(Formula II). n=1-9 and R?=methyl, ethyl, acetyl, benzyl, piperinoyl, 4-fluorophenyl, 4-chlorophenyl, 4-methoxyphenyl, pyridyl, pyrimidyl.Type: GrantFiled: January 10, 2012Date of Patent: June 24, 2014Assignee: Council of Scientific & Industrial ResearchInventors: Ahmed Kamal, Jayanti Naga Srirama Chandra Murty, Arutla Viswanath
-
Publication number: 20130338148Abstract: Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: ApplicationFiled: August 21, 2013Publication date: December 19, 2013Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Gabriella Traquandi, Maria Gabriella Brasca, Roberto D'Alessio, Paolo Polucci, Fulvia Roletto, Anna Vulpetti, Paolo Pevarello, Achille Panzeri, Francesca Quartieri, Ron Ferguson, Paola Vianello, Daniele Fancelli
-
Publication number: 20130317211Abstract: The present invention provides a compound of general formula A, useful as potential antitumour agents against five human cancer cell lines. The present invention further provides a process for the preparation of pyrrolo[2,1-c][1,4]naphthodiazepine linked substituted piperazine conjugates attached through different alkane spacers of general formula A. (Formula I) General formula A. Where R=R?=(Formula II).Type: ApplicationFiled: January 10, 2012Publication date: November 28, 2013Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Ahmed Kamal, Jayanti Naga Srirama Chandra Murty, Arutla Viswanath
-
Publication number: 20130306955Abstract: A specific nitrogen-containing heterocyclic compound having a urea structure, an electron transporting material containing the nitrogen-containing heterocyclic compound, and an organic electroluminescence device including a light emitting layer and an electron transporting layer between a cathode and an anode in which the electron transporting layer includes the electron transporting material or the nitrogen-containing heterocyclic derivative. An organic EL device exhibiting high emission efficiency even at low voltage and a material for organic EL devices are described.Type: ApplicationFiled: February 1, 2012Publication date: November 21, 2013Applicant: IDEMITSU KOSAN CO., LTD.Inventors: Sayaka Mizutani, Takayasu Sado, Hiroki Ishida
-
Publication number: 20130302357Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: ApplicationFiled: March 14, 2013Publication date: November 14, 2013Inventors: Wei Li, Nathan Elliott Fishkin, Robert Yongxin Zhao, Michael Louis Miller, Ravi V.J. Chari
-
Patent number: 8431716Abstract: The invention relates to special (methyl)acrylaic monomers and concerns more particularly an enhanced process for preparing solutions of alkylimiozolidone (meth)acrylates in water solutions of alkylimidazolidone (meth)acrylates in a light (meth)acrylate.Type: GrantFiled: April 8, 2009Date of Patent: April 30, 2013Assignee: Arkema FranceInventors: Alain Riondel, Jean-Michel Paul
-
Patent number: 8426402Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: GrantFiled: February 4, 2010Date of Patent: April 23, 2013Assignee: ImmunoGen, Inc.Inventors: Wei Li, Nathan Fishkin, Robert Zhao, Michael Miller, Ravi Chari
-
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
-
Publication number: 20120283248Abstract: Compounds having inverse agonist functional selectivity for GABAA receptors containing the ?5 subunit for use as a medicament in the treatment of cognitive impairments in subjects suffering from Down syndrome. The use of these compounds is disclosed. Pharmaceutical compositions for such treatment can comprise these compounds or suitable pharmaceutically acceptable salt thereof, a polyethoxylated castor oil and dimethyl sulfoxide (DMSO). Methods are disclosed for enhancing cognitive function, or treating or lessening the severity of cognitive impairments, in subjects suffering from Down syndrome by administering to a subject in need thereof a pharmaceutically effective amount of one or more of these compounds.Type: ApplicationFiled: August 24, 2010Publication date: November 8, 2012Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE - CNRSInventors: Marie-Claude Potier, Robert Dodd, Benoît Delatour, Jérôme Braudeau, Yann Herault
-
Publication number: 20120244171Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VII). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.Type: ApplicationFiled: February 15, 2012Publication date: September 27, 2012Applicant: ImmunoGen, Inc.Inventors: Wei Li, Michael Miller, Nathan Fishkin, Ravi V.J. Chari
-
Publication number: 20120070409Abstract: The present invention relates to a tetracyclic fused heterocyclic compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.Type: ApplicationFiled: February 3, 2011Publication date: March 22, 2012Applicant: Japan Tobacco Inc.Inventors: Takahiro Oka, Kazutaka Ikegashira, Shintaro Hirashima, Hiroshi Yamanaka, Satoru Noji, Yasushi Niwa, Yoko Matsumoto, Toshihiro Sato, Izuru Ando, Yukihiro Nomura
-
Publication number: 20100203007Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: ApplicationFiled: February 4, 2010Publication date: August 12, 2010Applicant: Immunogen Inc.Inventors: Wei Li, Nathan Fishkin, Robert Zhao, Michael Miller, Ravi Chari
-
Patent number: 7659263Abstract: The present invention relates to a thienopyrrole compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound as an active ingredient. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.Type: GrantFiled: November 10, 2005Date of Patent: February 9, 2010Assignee: Japan Tobacco Inc.Inventors: Ryo Mizojiri, Takahiro Oka, Kenta Aoki, Satoru Noji, Yoko Matsumoto, Toshihiro Sato, Izuru Ando, Yasushi Niwa
-
Patent number: 7026311Abstract: The invention relates to compounds of the formula I and their tautomeric forms, possible enantiomeric and diastereomeric forms and their prodrugs, and to their preparation and use, where A, B, R1 and X1 have the meanings given in the description.Type: GrantFiled: January 10, 2002Date of Patent: April 11, 2006Assignee: Abbott GmbH & Co., KGInventors: Wilfried Lubisch, Roland Grandel, Wilfried Braje, Thomas Subkowski, Reinhold Mueller, Wolfgang Wernet, Karla Drescher
-
Patent number: 6777406Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein is R1, R6a, R6b, R7, R8, R9, X, b, m, and n are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: December 19, 2001Date of Patent: August 17, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventors: John M. Fevig, Ian S. Mitchell, Taekyu Lee, Wenting Chen, Joseph Cacciola
-
Publication number: 20040092502Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) 1Type: ApplicationFiled: December 19, 2001Publication date: May 13, 2004Inventors: John M. Fevig, Ian S. Mitchell, Taekyu Lee, Wenting Chen, Joseph Cacciola
-
Publication number: 20030144268Abstract: The invention relates to novel tetracyclic pyrroloquinolone derivatives of the formula (I) or (II): 1Type: ApplicationFiled: November 12, 2002Publication date: July 31, 2003Inventors: Weiqin Jiang, Zhihua Sui
-
Publication number: 20030139394Abstract: The invention relates to compounds of the formula I 1Type: ApplicationFiled: January 10, 2002Publication date: July 24, 2003Inventors: Wilfried Lubisch, Roland Grandel, Wilfried Braje, Thomas Subkowski, Reinhold Mueller, Wolfgang Wernet, Karla Drescher
-
Patent number: 6562806Abstract: A compound with formula (I) where R10 is a therapeutically removable nitrogen protecting group; R2 and R3 are independently selected from: H, R, OH, OR, ═O, ═CH—R, ═CH2, CH2—CO2R, CH2—CO2H, CH2—SO2R, O—SO2—R, CO2R, COR and CN; R6, R7 and R9 are independently selected from H, R, OH, OR, halo, amino, nitro, Me3Sn; X is S, O or NH; R11 is either H or R; and where there is optionally a double bond between C1 and C2 or C2 and C3; and R8 is selected from H, R, OH, OR, halo, amino, nitro, Me3Sn, or R7 and R8 together form a group —O—(CH2)p—O—, where p is 1 or 2. Such compounds may be used in methods of ADEPT, GDEPT, NPEPT or PDT.Type: GrantFiled: February 26, 2001Date of Patent: May 13, 2003Assignee: Spirogen LimitedInventors: David Edwin Thurston, Philip Wilson Howard
-
Patent number: 6552017Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: June 15, 2000Date of Patent: April 22, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Michael Guang Yang, Simon Haydar, Wenting Chen, Christopher D. Mc Clung, Emilie J. B. Calvello, David M. Zawrotny
-
Patent number: 6515122Abstract: The present invention relates to novel tetracyclic benzimidazole derivative compounds of the following formula: wherein R1 to R10 have the meanings described in here. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing tetracyclic benzimidazole derivative compounds.Type: GrantFiled: September 24, 1999Date of Patent: February 4, 2003Assignee: Lion Bioscience AGInventors: Hengyuan Lang, Yazhong Pei
-
Patent number: 6482821Abstract: Vitronectin receptor antagonists, their preparation and their use The present invention relates to compounds of the formula I, A—B—D—E—F—G (I) in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: February 8, 2001Date of Patent: November 19, 2002Assignees: Hoechst Aktiengellschaft, Genentech, Inc.Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Karlheinz Scheunemann, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
-
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
-
Patent number: 5554632Abstract: The present patent application discloses compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.3, R.sup.4, R.sup.6 and R.sup.7 each have the meanings set forth in the specification.The compounds are useful for the treatment of various central nervous system disorders such as epilepsy and other convulsive disorders, anxiety, sleep disorders and memory disorders.Type: GrantFiled: December 9, 1994Date of Patent: September 10, 1996Assignees: NeuroSearch A/S, Meiji Seika Kaisha, Ltd.Inventors: Lene Teuber, Oskar Axelsson, Frank Watjen
-
Patent number: 5536717Abstract: There are disclosed various compounds of the formula below, ##STR1## where the parameters X, Y, R.sub.1 and R.sub.2 are as defined in the specification which are useful as antidepressant and analgesic agents.Type: GrantFiled: November 22, 1993Date of Patent: July 16, 1996Assignee: Hoechst Marion Roussel Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
-
Patent number: 5439905Abstract: Thienodiazepine compounds of the formula ##STR1## wherein each symbol is as defined in the specification, their pharmaceutically acceptable salts, and pharmaceutical compositions containing said compound.Since the compounds possess excellent antagonistic actions on cholecystokinin and gastrin, and exhibit potent and durable suppressive actions on pancreatic enzyme secretion and gastric acid secretion, they are useful as medicaments acting on the central nervous system and the peripheral nervous system, as well as prophylactic and therapeutic medicines for pancreatic disorders and gastrointestinal ulcers. Furthermore, they are expected to exhibit anti-dementia actions based on their antagonistic actions on cholecystokinin, and are useful as an anti-dementia.Type: GrantFiled: May 27, 1993Date of Patent: August 8, 1995Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Yoichi Naka, Keiichiro Haga, Masahiro Hosoya
-
Patent number: 5015738Abstract: Novel benzo[b]pyrrolo[3,2,1-jk]benzodiazepines, intermediates and processes for the preparation thereof, and methods for alleviating pain utilizing the compounds or compositions thereof are disclosed.Type: GrantFiled: September 21, 1990Date of Patent: May 14, 1991Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Edward J. Glamkowski, Barbara E. Kurys
-
Patent number: 4914201Abstract: There are disclosed compounds having the formula ##STR1## where X is H, halogen, --OH, --OCH.sub.3, --NO.sub.2 or --CF.sub.3 ; Y is H, Cl or Br; Z is H, halogen, --OH or --OCH.sub.3 ; and R is H, loweralkyl, --CH.sub.2 OH or diloweralkylaminomethyl, which compounds are useful as analgesic agents.Type: GrantFiled: October 30, 1989Date of Patent: April 3, 1990Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: John J. Tegeler, Eileen M. Gardenhire, Grover C. Helsley
-
Patent number: 4897392Abstract: There are disclosed compounds having the formula ##STR1## where X is H, halogen, --OH,--OCH.sub.3,--NO.sub.2 or --CF.sub.3 ; Y is H, Cl or Br; Z is H, halogen, --OH or --OCH.sub.3 ; and R is H, loweralkyl, --CH.sub.2 OH or diloweralkylaminomethyl, which compounds are useful as analgesic agents.Type: GrantFiled: July 3, 1989Date of Patent: January 30, 1990Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: John J. Tegeler, Eileen M. Gardenhire, Grover C. Helsley
-
Patent number: 4868176Abstract: A compound selected from the group consisting a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of phenyl, cycloalkyl of 4 to 6 carbon atoms and ##STR2## R.sub.4 and R.sub.5 are individually hydrogen or alkyl of 1 to 5 carbon atoms, R.sub.6 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, phenyl, halogen, alkoxycarbonyl of 2 to 5 carbon atoms, cyano, amido and mono- and dialkylamido of 1 to 5 alkyl carbon atoms, R.sub.2 and R.sub.3 are individually selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and cycloalkyl of 3 to 5 carbon atoms or taken together form alkylene of 3 to 5 carbon atoms, X and Y are individually selected form the group consisting of hydrogen, halogen, --NO.sub.2, azido, --CN, --CF.sub.Type: GrantFiled: August 26, 1988Date of Patent: September 19, 1989Assignee: Roussel UclafInventors: Colin R. Gardner, John R. Hedgecock
-
Patent number: 4829066Abstract: This invention relates to substituted pyridooxazinone pyridazinone and pyrazolone compounds, which are useful as cardiotonic agents for the treatment of congestive heart failure. This invention also relates to methods for increasing cardiac contractility using said compounds, and pharmaceutical compositions including said compound.Type: GrantFiled: May 8, 1987Date of Patent: May 9, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Alfred P. Spada, William L. Studt, Henry F. Campbell, Donald E. Kuhla
-
Patent number: 4723003Abstract: The invention relates to benzopyrrolobenzodiazepines and quinobenzodiazepines of the formula ##STR1## where X and Y may be the same or different and each is hydrogen, halogen, CF.sub.3, lower alkyl, lower alkoxy, lower alkylthio and lower alkylsulfonyl, p and q are independently 1 or 2; R.sub.1 is hydrogen when R.sub.2 is bonded to R.sub.3 to form a --(CH.sub.2).sub.m --CH.sub.2 -- group or a --CH.dbd.CH-- group; R.sub.3 is hydrogen when R.sub.1 is bonded to R.sub.2 to form a --(CH.sub.2).sub.m --CH.sub.2 -- group or a --CH.dbd.CH-- group; m is 1 or 2; R.sub.4 is NR.sub.5 R.sub.6 wherein R.sub.5 is hydrogen or lower alkyl and R.sub.6 is hydrogen, lower alkyl or a group of the formula (CH.sub.2).sub.n NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are lower alkyl, and n is 2 or 3, ##STR2## wherein R.sub.9 is lower alkyl, ##STR3## wherein R.sub.10 is CH.sub.2 CH.sub.2 OH, lower alkyl, phenyl, phenyl substituted by halogen, CF.sub.Type: GrantFiled: November 12, 1986Date of Patent: February 2, 1988Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
-
Patent number: 4696925Abstract: Products of Aspergillus alliaceus fermentation having cholecystokinin (CCK) antagonist activity, their preparation and use are disclosed.Type: GrantFiled: January 25, 1985Date of Patent: September 29, 1987Assignee: Merck & Co., Inc.Inventors: David R. Houck, Edward S. Inamine, Michael A. Goetz
-
Patent number: 4670433Abstract: New oxadiazolyl imidazobenzodiazepine derivatives having the formula ##STR1## wherein R.sup.3 has the formula ##STR2## wherein R" is hydrogen, C.sub.1-6 alkyl C.sub.1-6 alkoxymethyl or C.sub.3-6 - cycloalkyl;R.sup.4 is hydrogen;R.sup.5 is C.sub.1-6 alkyl or R.sup.4 and R.sup.5 together form a 2-4 membered alkylene bridge; and R.sup.A is C.sub.1-6 alkyl, C.sub.1-6 alkoxy, or C.sub.1-3 trifluoroalkyl, pharmaceutical compositions thereof, and method of treating therewith, are disclosed.The compounds and pharmaceutical compositions are useful in the amelioration, mitigation, or elimination of central nervous system disorders related to benzodiazepine receptors and especially as anticonvulsants, anxiolytics, hypnotics, and nootropics.Type: GrantFiled: March 6, 1986Date of Patent: June 2, 1987Assignee: A/S FerrosanInventors: Frank Watjen, Mogens Engelstoft, John B. Hansen, Leif H. Jensen
-
Patent number: 4663453Abstract: The invention relates to benzopyrrolobenzodiazepines and quinobenzodiazepines of the formula ##STR1## where X and Y may be the same or different and each is hydrogen, halogen, CF.sub.3, lower alkyl, lower alkoxy, lower alkylthio and lower alkylsulfonyl, p and q are independently 1 or 2; R.sub.1 is hydrogen when R.sub.2 is bonded to R.sub.3 to form a --(CH.sub.2).sub.m --CH.sub.2 -- group or a --CH.dbd.CH-- group; R.sub.3 is hydrogen when R.sub.1 is bonded to R.sub.2 to form a --(CH.sub.2).sub.m --CH.sub.2 -- group or a --CH.dbd.CH-- group; m is 1 or 2; R.sub.4 is NR.sub.5 R.sub.6 wherein R.sub.5 is hydrogen or lower alkyl and R.sub.6 is hydrogen, lower alkyl or a group of the formula (CH.sub.2).sub.n NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are lower alkyl, and n is 2 or 3, ##STR2## wherein R.sub.9 is lower alkyl, ##STR3## wherein R.sub.10 is CH.sub.2 CH.sub.2 OH, lower alkyl, phenyl, phenyl substituted by halogen, CF.sub.Type: GrantFiled: August 28, 1985Date of Patent: May 5, 1987Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
-
Patent number: 4616010Abstract: Compounds which are imidazodiazepine derivatives of the formula ##STR1## wherein A together with the carbon atoms denoted by .alpha. and .beta. signifies the group ##STR2## one of R.sup.1 and R.sup.2 signifies hydrogen and the other signifies hydrogen, halogen or trifluoromethyl, R.sup.3 and R.sup.4 each signify hydrogen or halogen and n signifies the number 2 or 3, the compounds having the (S)- or (R,S)-configuration with reference to the carbon atom denoted by .gamma., and their pharmaceutically acceptable acid addition salts have been discovered which possess anxiolytic, anticonvulsant, muscle relaxant and sedative-hypnotic properties. They can be prepared into compositions, including pharmaceutically acceptable ones, using suitable inert carriers.Type: GrantFiled: February 20, 1986Date of Patent: October 7, 1986Assignee: Hoffmann-La Roche Inc.Inventors: Walter Hunkeler, Emilio Kyburz
-
Patent number: RE39680Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: February 16, 2006Date of Patent: June 5, 2007Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Michael Guang Yang, Simon Haydar, Wenting Chen, Christopher D. McClung, Emile J. B. Calvello, David M. Zawrotny, Parthasarathl Rajagopalan