Tricyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/557)
  • Patent number: 7407949
    Abstract: 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: Grant
    Filed: February 12, 2004
    Date of Patent: August 5, 2008
    Assignee: Ferring B.V.
    Inventors: Peter Hudson, Andrzej Roman Batt, Celine Marguerite Simone Heeney, Andrew John Baxter, Michael Bryan Roe, Peter Andrew Robson
  • Publication number: 20080161557
    Abstract: The invention belongs to the field of organic chemistry and relates to a new process for the purification of olanzapine comprising preparation of acid addition salts of olanzapine and transformation thereof into a pharmaceutically acceptable pure and discoloured final product. The present invention also relates to new processes for the preparation of pure olanzapine.
    Type: Application
    Filed: March 17, 2005
    Publication date: July 3, 2008
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Tomaz Mesar, Anton Copar, Hubert Sturm, Johannes Ludescher
  • Patent number: 7384934
    Abstract: Described herein are compounds of formula (I) wherein: is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, S, and O; Alk is (C1-4) alkylene or hydroxy substituted (C1-4) alkylene; X is oxygen or sulfur; R1 is hydrogen, (C1-6) fluroalkyl, (C3-6) cycloalkyl, or (C1-4) alkyl, wherein the (C1-4) alkyl is unsubstituted or substituted with hydroxy, methoxy, ethoxy, OCH2CH2OH, or —CN; R2 is H, halogen, (C1-6) fluoroalkyl, (C1-6) cycloalkyl, OR4, SR4, NO2, CN, COR4, C(O)OR4, CONR5R6, NR5R6, SO2NR5R6, NR5COR4, NR5SO2R4, optionally substituted aromatic, or (C1-6) alkyl, wherein (C1-6) alkyl is unsubstituted or substituted with a hydroxy group; R3 is hydrogen (C1-6) fluoroalkyl, (C2-6) alkenyl, Ar, (C1-4)alkyl-Ar, or (C1-4) alkyl wherein (C1-4) alkyly is unsubstituted or substituted with a phenyl; R4 is hydrogen, (C1-6) alkyl, (C1-6) fluoroalkyl, or optionally substituted aromatic; R5 and R6 are independently hydrogen, (C1-6) alkyl, or optionally
    Type: Grant
    Filed: July 28, 2003
    Date of Patent: June 10, 2008
    Assignee: Eli Lilly and Company
    Inventors: Thomas Daniel Aicher, Zhaogen Chen, Yvan LeHuerou, Fionna Mitchell Martin, Marta Maria Pineiro-Nunez, Vincent Patrick Rocco, Kevin Michael Ruley, John Mehnert Schaus, Patrick Gianpietro Spinazze, David Edward Tupper
  • Patent number: 7329747
    Abstract: Olanzapine and salts thereof are made by a process that utilizes an N-formyl olanzapine intermediate of formula (4) or a salt thereof
    Type: Grant
    Filed: January 27, 2005
    Date of Patent: February 12, 2008
    Assignee: Synthon IP Inc.
    Inventors: Rolf Keltjens, Theodorus H. A. Peters
  • Patent number: 7326701
    Abstract: An agent for increasing the sugar-transporting capacity and an agent for preventing and/or treating diabetes, diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic macroangiopathy, impaired glucose tolerance or adiposis, which contains a lactam compound or a pharmaceutically acceptable salt thereof as the active ingredient.
    Type: Grant
    Filed: April 6, 2006
    Date of Patent: February 5, 2008
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yukio Iino, Takao Ikenoue, Nobuo Kondo, Hiroyuki Matsueda, Toshihiro Hatanaka, Ryusuke Hirama, Yoko Masuzawa, Fumio Ohta, Akiyo Yamazaki, Seiji Niwa, Takashi Yamamoto
  • Patent number: 7323459
    Abstract: The invention is directed to a series of novel crystalline olanzapine forms, in particular hydrated and solvated crystalline forms of olanzapine, methods of use in pharmaceutical compositions, and method of treating psychiatric disorders using the crystalline forms. One series of the crystalline forms are hydrates, i.e. water containing crystals, wherein water may be present in a ratio of about 2:1.5 to a ratio of about 1:3 olanzapine:water, while another includes solvates such as an isobutanol solvate. The olanzapine crystalline forms include Forms H, G, Y, X, K, S, Q, Z, and J.
    Type: Grant
    Filed: December 24, 2003
    Date of Patent: January 29, 2008
    Assignee: Teva Pharmaceutical Industries Ltd.
    Inventors: Ben Zion Dolitzky, Judith Aronhime, Dov Diller
  • Patent number: 7309699
    Abstract: Compounds of formula (I) wherein A is N or N+—O?; n is 0, 1, or 2; Y is O, S, —NH—, and —N-alkyl-; Ar1 is both 6-membered aromatic rings; Ar2 is 5- or 6-membered aromatic rings with a —NR8R9 group, as defined herein. The compounds are useful in treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands. Also disclosed are pharmaceutical compositions having compounds of formula (I) and methods for using such compounds and compositions.
    Type: Grant
    Filed: December 17, 2004
    Date of Patent: December 18, 2007
    Assignee: Abbott Laboratories
    Inventors: Jianguo Ji, Tao Li, Ying Wang
  • Patent number: 7297789
    Abstract: A process for the preparation of polymorph Form I of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine, or olanzapine.
    Type: Grant
    Filed: May 30, 2003
    Date of Patent: November 20, 2007
    Assignee: Sandoz, Inc.
    Inventors: Hiren V. Patel, Anup K. Ray, Pramod B. Patel, Mahendra R. Patel
  • Patent number: 7244843
    Abstract: The present invention provides modulators of serotonin receptors, pharmaceutical compositions containing such modulators and methods for treating various diseases, conditions and disorders associated with modulation of serotonin receptors such as, for example: metabolic diseases, which includes but is not limited to obesity, diabetes, diabetic complications, atherosclerosis, impared glucose tolerance and dyslipidemia; central nervous system diseases which includes but is not limited to, anxiety, depression, obsessive compulsive disorder, panic disorder, psychosis, schizophrenia, sleep disorder, sexual disorder and social phobias; cephalic pain; migraine; and gastrointestinal disorders using such compounds and compositions.
    Type: Grant
    Filed: October 5, 2004
    Date of Patent: July 17, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: Dean A. Wacker, Jeffrey G. Varnes
  • Patent number: 7223752
    Abstract: A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1–C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1–C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1–C6) lower alkoxy, (C1–C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1–C6) lower alkyl], —CON[(C1–C6) lower alkyl]2; or (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1–C6) lower alkyl, halogen or (C1–C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1–C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1–C6) lower alkoxy, or (C1–C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1–C6) lower alkyl], —CON[(C1–C6) lower alkyl]2; or (2) a 5-membered aromatic (unsaturat
    Type: Grant
    Filed: November 4, 2004
    Date of Patent: May 29, 2007
    Assignee: Wyeth
    Inventors: Amedeo Arturo Failli, John P. Dusza, Thomas Joseph Caggiano, Jay Scott Shumsky, Kevin A. Memoli, Eugene J. Trybulski
  • Patent number: 7214664
    Abstract: Dipeptide, and tripeptide and tetrapeptide ester derivatives of bioactive agents are provided wherein the parent agents are substrates effluxed by the P-gp transporter. The derivatives are useful in treating the same condition as the bioactive agent. Also disclosed is a method for preparing a bioactive agent for targeted delivery by nutrient or peptide transporters comprising linking the agent to one or more groups of the formula —X—Y(n)-Z(n?)-Z?(n?)-R; wherein each X, Y, Z, and Z? is independently Met, Val, Thr, Tyr, Trp, Ser, Ala or Gly; R is independently H or an amino-protecting group; n=1, and each, n?, or n? is independently 0 or 1.
    Type: Grant
    Filed: November 22, 2005
    Date of Patent: May 8, 2007
    Assignee: The Curators of the University of Missouri
    Inventors: Ashim K. Mitra, Soumyajit Majumdar, Ritesh Jain, Yasser Nashed
  • Patent number: 7214673
    Abstract: Described herein are antipyschotic compounds of formula (I) wherein, A is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, O, and S; Alk is (C1-4) alkylene optionally substituted with OH, methoxy, ethoxy, or F; Ar is optionally substituted phenyl, naphthyl, monocyclic heteroaromatic, or bicyclic heteroaromatic; R1 is hydrogen or (C1-4) alkyl optionally substituted with OH, OR3, or OCH2CH2OH, wherein R3 is (C1-2) alkyl; R2 is H, (C1-6) alkyl, halogen, fluorinated (C1-6) alkyl, OR4, SR4, NO2, CN, COR4, CONR5R6, SO2NR5R6, NR5R6, NR5COR4, NR5SO2R4, or optionally substituted phenyl, wherein R4 is hydrogen, (C1-6) alkyl, fluorinated (C1-6) alkyl, or optionally substituted phenyl, R5 and R6 are independently hydrogen, (C1-6) alkyl, or optionally substituted phenyl; Z is one or two substituents independently selected from hydrogen, halogen, (C1-6) alkyl, fluorinated (C1-6) alkyl, OR7, SR7, NO2, CN, COR7, CONR8R9, SO2NR8R9, NR8SO2R
    Type: Grant
    Filed: March 17, 2003
    Date of Patent: May 8, 2007
    Assignee: Eli Lilly and Company
    Inventors: Thomas Daniel Aicher, Zhaogen Chen, Joseph Herman Krushinski, Jr., Yvan Le Huerou, Marta Maria Pineiro-Nunez, Kevin Michael Ruley, John Mehnert Schaus, Dennis Charles Thompson, David Edward Tupper, Ying Chen, Margaret Mary Faul, Vincent Patrick Rocco
  • Patent number: 7153850
    Abstract: An agent for increasing the sugar-transporting capacity and an agent for preventing and/or treating diabetes, diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic macroangiopathy, impaired glucose tolerance or adiposis, which contains a lactam compound or a pharmaceutically acceptable salt thereof as the active ingredient.
    Type: Grant
    Filed: June 2, 2003
    Date of Patent: December 26, 2006
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yukio Iino, Takao Ikenoue, Nobuo Kondo, Hiroyuki Matsueda, Toshihiro Hatanaka, Ryusuke Hirama, Yoko Masuzawa, Fumio Ohta, Akiyo Yamazaki, Seiji Niwa, Takashi Yamamoto
  • Patent number: 7053083
    Abstract: The present invention provides compounds of the general formulas: wherein Y is NR or —(CH2)n; R is H or alkyl “Z” represents optionally substituted phenyl or a 6-membered aromatic ring having one nitrogen atom; “W” represents a optionally substituted phenyl or 5-membered aromatic ring having one nitrogen atom; “X” represents an optionally substituted 5-membered aromatic ring having one sulfur atom; as well as methods and pharmaceutical compositions utilizing these compounds for the inducing temporary delay of urination or treatment of disorders remedied by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, or bleeding and coagulation disorders.
    Type: Grant
    Filed: April 11, 2002
    Date of Patent: May 30, 2006
    Assignee: Wyeth
    Inventors: Amedeo Arturo Failli, Jay Scott Shumsky, Thomas Joseph Caggiano, John P. Dusza, Kevin A. Memoli
  • Patent number: 7053082
    Abstract: The invention relates to new 2,3-benzodiazepine derivatives of general Formula (I), (wherein R1 stands for methyl, formyl, carboxy, cyano, —CH?NOH, —CH?NNHCONH2 or —NR5R6, wherein R5 and R6 independently from each other represent hydrogen or lower alkyl or together with the nitrogen atom, they are attached to, form a 5- or 6-membered, saturated or unsaturated heterocyclic ring optionally containing one or more further nitrogen, sulfur and/or oxygen atom(s); R2 is nitro or amino; R3 stands for hydrogen, lower alkanoyl or CO—NR7R8, wherein R7 and R8 independently from each other stand for hydrogen, lower alkoxy, lower alkyl or lower cycloalkyl or together with the nitrogen atom, they are attached to, form a 5- or 6-membered, saturated or unsaturated heterocyclic ring optionally containing one or more further nitrogen, sulfur and/or oxygen atom(s); R4 is hydrogen or lower alkyl; the dotted lines have the following meaning: if R3 and R4 are not present, the bond between positions C8 and C9 is a single bond and th
    Type: Grant
    Filed: July 4, 2000
    Date of Patent: May 30, 2006
    Assignee: EGIS Gyogyszergyar Rt.
    Inventors: Zoltan Greff, Geza Szabo, Jozsef Barkoczy, Zoltan Ratkai, Gabor Blasko, Gyula Simig, Gabor Gigler, Bernadett Martonné Marko, György Levay, Karoly Tihanyi, Andras Egyed, Annamaria Simo
  • Patent number: 7022698
    Abstract: Pharmaceutical compositions containing Form III, Form IV, Form V olanzapine and/or pharmaceutically acceptable salts thereof. The pharmaceutical compositions are useful for the treatment of psychotic conditions, mild anxiety and gastrointestinal conditions. In particular, the compositions are useful for treating schizophrenia and related disorders, acute mania, Bipolar I Disorder, psychotic mood disorder and psychosis in patients with Alzheimer's disease.
    Type: Grant
    Filed: December 27, 2001
    Date of Patent: April 4, 2006
    Assignee: U & I Pharmaceuticals, Ltd.
    Inventors: Yusuf K. Hamied, Rajendra N. Kankan, Dharmaraj R. Rao
  • Patent number: 7015214
    Abstract: The present invention relates to 1,3-benzodiazepin-2-ones and 1,3-benzoxazepin-2-ones of formula I: or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.
    Type: Grant
    Filed: March 27, 2002
    Date of Patent: March 21, 2006
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventor: Donna M Bilder
  • Patent number: 6916925
    Abstract: Dye labeled imidazonaphthyridine, imidazopyridine and imidazoquinoline compounds having immune response modulating activity are disclosed. The compounds arc useful, inter alia, for determining the binding and/or receptor sites of the molecules.
    Type: Grant
    Filed: July 22, 2003
    Date of Patent: July 12, 2005
    Assignee: 3M Innovative Properties Co.
    Inventors: Michael J. Rice, Mark A. Tomai, Ai-Ping Wei
  • Patent number: 6916923
    Abstract: Disclosed is a novel method for synthesizing pyrazolobenzodiazepines of formula I using intermediates of formula Pyrazolobenzodiazepines of formula I are useful in the treatment and control of solid tumors.
    Type: Grant
    Filed: April 19, 2004
    Date of Patent: July 12, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Qingjie Ding, Jin-Jun Liu, Giacomo Pizzolato, Peter Michael Wovkulich
  • Patent number: 6906062
    Abstract: Crystalline Form I of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepine characterised by x-ray powder diffraction peaks at approximately 9.94, 8.53, 8.19, 6.86, 6.35, 5.47, 4.83, 4.71, 4.53, 4.22, 4.08, 3.82, 3.75, 3.69, 3.50, 3.34, 3.11, 2.94, 2.82, 2.76, 2.59, 2.34, 2.03, 1.92 d (interplanar spacing) values; infrared absorbance bands at approximately 1456, 1365, 905, 757, 662 & 604 cm?3 and having stable colour at ambient conditions of storage; and the process of its preparation comprising at least two repetitive steps of crystallization from one or more organic solvent by dissolving 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepine in said solvent and allowing crystallization to occur; wherein in at least one step the solution is purified by treating with a solid adsorbent material and filtering; and wherein in the last step the crystalline material is subjected to drying.
    Type: Grant
    Filed: December 23, 2002
    Date of Patent: June 14, 2005
    Assignee: Sun Pharmaceutical Industries Limited
    Inventors: Vijay Chhangamal Chhabada, Rajeev Budhdev Rehani, Rajamamannar Thennati
  • Patent number: 6903091
    Abstract: A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1-C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen or (C1-C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, or (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 5-membered aromatic (unsaturated) hete
    Type: Grant
    Filed: April 11, 2002
    Date of Patent: June 7, 2005
    Assignee: Wyeth
    Inventors: Amedeo A. Failli, Thomas J. Caggiano, Jay S. Shumsky, Eugene J. Trybulski, Kevin A. Memoli, John P. Dusza
  • Patent number: 6887867
    Abstract: Substituted benzodiazepine compositions are provided which are active as non-NMDA ionotropic excitatory amino acid (EAA) receptor antagonists. The compounds are generally 7- or 8-mono substituted 5H-2,3-benzodiazepines. The compositions are useful for treating disorders associated with excessive activation of the non-NMDA subtype of the ionotropic EAA receptor. The compounds further are useful as testing agents to identify and characterize other compounds for the treatment of these disorders. The compounds are useful therapeutically as sedatives or for the treatment of neurosychopharmacological disorders such as stroke, ischemia and epilepsy. The compositions may be provided in combination with a suitable carrier for oral or parenteral administration. The compounds may be administered orally or parenterally for the treatment of a variety of disorders associated with non-NMDA EEA receptor function.
    Type: Grant
    Filed: June 15, 2001
    Date of Patent: May 3, 2005
    Assignee: Transgenomic, Inc.
    Inventors: Xue-Feng Pei, Baoqing Li, Maria-Luisa Maccecchini
  • Patent number: 6887838
    Abstract: Formulation components such as bleach boosting compounds selected from the group consisting of bleach boosters comprising quaternary imine cations, zwitterions, polyions having a net charge of from about +3 to about 3 and mixtures thereof, bleaching species comprising oxariridinium cations, zwitterions, polyions having a net charge of from about +3 to about ?3 and mixtures thereof, and mixtures thereof are disclosed. The bleach boosting compounds increase bleaching effectiveness even in lower temperature solutions and provides improved stability toward unwanted boosting compound decomposition. The bleach boosting compounds are ideally suited for inclusion into bleaching compositions including those with detersive surfactants and enzymes. Also provided is a method for laundering a fabric employing the bleach compounds, a laundry additive product employing the bleach boosting compounds.
    Type: Grant
    Filed: May 26, 2004
    Date of Patent: May 3, 2005
    Assignee: Procter & Gamble Company
    Inventors: Robert Richard Dykstra, Gregory Scot Miracle
  • Patent number: 6858605
    Abstract: The invention relates to new 2,3-benzodiazepine derivatives of formula (I), isomers and acid addition salts thereof and to pharmaceutical compositions containing the same, as well as to pharmaceutical compositions and methods of using the same suitable for treating conditions associated with muscle spasms, epilepsy, acute and chronic forms of neurodegenerative diseases as well as preventing, treating or alleviating the symptoms of acute and chronic inflammatory disorders.
    Type: Grant
    Filed: February 4, 2003
    Date of Patent: February 22, 2005
    Assignee: IVAX Drug Research Institute, Ltd.
    Inventors: Sándor Sólyom, Gizella Ábrahám, Tamás Hámori, Pál Berzsenyi, Ferenc Andrási, István Kurucz
  • Patent number: 6858599
    Abstract: This invention relates to tricyclic compounds having spiro union represented by the following formula (I) or its salt which is useful as a drug, and in particular, as an inhibitor for activated blood coagulation factor X, which can be administered orally and which exhibits strong anticoagulation action. The invention also relates to a pharmacophore which was derived from the compound and is useful in molecular designing of the FXa inhibitor.
    Type: Grant
    Filed: December 27, 2001
    Date of Patent: February 22, 2005
    Assignee: Mochida Pharmaceutical Co., Ltd.
    Inventors: Hidemitsu Nishida, Fumihiko Saitoh, Kousuke Harada, Ikuya Shiromizu, Takafumi Mukaihira
  • Patent number: 6838558
    Abstract: Disclosed are novel pyrazolobenzodiazepines having the formula These compounds are useful in the preparation of the pyrazolobenzodiazepines of formula I, which are useful in the treatment and control of solid tumors.
    Type: Grant
    Filed: April 15, 2002
    Date of Patent: January 4, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Qingjie Ding, Jin-Jun Liu, Giacomo Pizzolato, Chung-Chen Wei, Peter Michael Wovkulich
  • Publication number: 20040198721
    Abstract: The invention is directed to a series of novel crystalline olanzapine forms, in particular hydrated and solvated crystalline forms of olanzapine, methods of use in pharmaceutical compositions, and method of treating psychiatric disorders using the crystalline forms. One series of the crystalline forms are hydrates, i.e. water containing crystals, wherein water may be present in a ratio of about 2:1.5 to a ratio of about 1:3 olanzapine:water, while another includes solvates such as an isobutanol solvate. The olanzapine crystalline forms include Forms H, G, Y, X, K, S, Q, Z, and J.
    Type: Application
    Filed: December 24, 2003
    Publication date: October 7, 2004
    Inventors: Ben Zion Dolitzky, Judith Aronhime, Dov Diller
  • Patent number: 6800656
    Abstract: The present invention provides a compound of the formula and pharmaceutically acceptable salts having useful antiviral activity against viruses of the herpes family. Wherein: X=O, (CH2)m, S, SO, SO2, NH, NR8; Y=O, (CH2)m, S, SO, SO2, NH, NR8 or a chemical bond; Z=NH, O, NR8, S, SO, SO2; The remaining substituents are described in the specification.
    Type: Grant
    Filed: July 5, 2002
    Date of Patent: October 5, 2004
    Assignee: Warner Lambert Company
    Inventors: Richard John Booth, Vara Prasad Venkata Nagendra Josyula, Annette Lynn Meyer, Bruce Allan Steinbaugh
  • Publication number: 20040152693
    Abstract: The invention relates to new 2,3-benzodiazepine derivatives of formula (I), isomers and acid addition salts thereof and to pharmaceutical compositions containing the same, as well as to pharmaceutical compositions and methods of using the same suitable for treating conditions associated with muscle spasms, epilepsy, acute and chronic forms of neurodegenerative diseases as well as preventing, treating or alleviating the symptoms of acute and chronic inflammatory disorders.
    Type: Application
    Filed: February 4, 2003
    Publication date: August 5, 2004
    Inventors: Sandor Solyom, Gizella Abraham, Tamas Hamori, Pal Berzsenyi, Ferenc Andrasi, Istvan Kurucz
  • Patent number: 6740753
    Abstract: A novel crystal form the pharmaceutical compound olanzapine, processes for its preparation and its pharmaceutical use are disclosed.
    Type: Grant
    Filed: December 19, 2001
    Date of Patent: May 25, 2004
    Assignee: Geneva Pharmaceuticals, Inc.
    Inventors: Julian Davies, James Edward Gano
  • Publication number: 20040058914
    Abstract: A pharmaceutical agent containing an NK-1 receptor antagonist, an NK-2 receptor antagonist and/or an anti-cholinergic drug in combination is provided, which is useful as a prophylactic or therapeutic agent of urinary frequency, urinary incontinence, asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, osteoarthritis, pain, cough, irritable bowel syndrome, emesis, depression, anxiety, manic depressive psychosis or schizophrenia.
    Type: Application
    Filed: June 23, 2003
    Publication date: March 25, 2004
    Inventors: Takayuki Doi, Tadatoshi Hashimoto, Izumi Kamo
  • Publication number: 20040048854
    Abstract: A process for the preparation of polymorph Form I of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine, or olanzapine.
    Type: Application
    Filed: May 30, 2003
    Publication date: March 11, 2004
    Inventors: Hiren V. Patel, Anup K. Ray, Pramod B. Patel, Mahendra R. Patel
  • Publication number: 20040048847
    Abstract: An agent for increasing the sugar-transporting capacity and an agent for preventing and/or treating diabetes, diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic macroangiopathy, impaired glucose tolerance or adiposis, which contains a lactam compound or a pharmaceutically acceptable salt thereof as the active ingredient.
    Type: Application
    Filed: June 2, 2003
    Publication date: March 11, 2004
    Applicant: AJINOMOTO CO. INC
    Inventors: Yukio Iino, Takao Ikenoue, Nobuo Kondo, Hiroyuki Matsueda, Toshihiro Hatanaka, Ryusuke Hirama, Yoko Masuzawa, Fumio Ohta, Akiyo Yamazaki
  • Publication number: 20040038962
    Abstract: Compounds according to general formulae (1 and 2), wherein G1 is an azepine derivative and G2 is a group according to general formulae (9-11) are new. Compounds according to the invention are vasopressin V2 receptor agonists. Pharmaceutical compositions of the compounds are useful as antidiuretic agents.
    Type: Application
    Filed: June 13, 2003
    Publication date: February 26, 2004
    Inventors: Doreen Ashworth, Gary R W Pitt, Peter Hudson, Christopher Yea, Richard J Franklin, Graeme Semple, David Paul Jenkins
  • Patent number: 6620807
    Abstract: The present invention provides benzoheterocyclic carboxyamides, particularly pyridobenzodiazepine and pyridobenzoxazepine carboxyamides, of the general formula: wherein: W is O or NH, optionally substituted, as well as methods and pharmaceutical compositions utilizing these compounds for providing a temporary delay of urination or for the treatment of disorder which may be remedied or alleviated by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding or coagulation disorders.
    Type: Grant
    Filed: February 1, 2000
    Date of Patent: September 16, 2003
    Assignee: Wyeth
    Inventors: Robert J. Steffan, Amedeo A. Failli
  • Patent number: 6617321
    Abstract: The invention provides a pharmaceutically acceptable oleaginous or cholesterol microsphere formulation or olanzapine or olanzapine pamoate or solvates thereof. The invention further provides novel olanzapine pamoate salts or solvates thereof.
    Type: Grant
    Filed: May 1, 2002
    Date of Patent: September 9, 2003
    Assignee: Eli Lilly and Company
    Inventors: Douglas J. Allen, Kurt D. Dekemper, Thomas H. Ferguson, Stuart J. Garvin, Linda C. Murray, Norman D. Brooks, Charles A. Bunnell, Snehlata S. Mascarenhas, Sharon L. Shinkle, Barry A. Hendriksen, David E. Tupper, Manuel V. Sanchez-Felix
  • Publication number: 20030125322
    Abstract: Crystalline Form I of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepine characterised by x-ray powder diffraction peaks at approximately 9.94, 8.53, 8.19, 6.86, 6.35, 5.47, 4.83, 4.71, 4.53, 4.22, 4.08, 3.82, 3.75, 3.69, 3.50, 3.34, 3.11, 2.94, 2.82, 2.76, 2.59, 2.34, 2.03, 1.92 d (interplanar spacing) values; infrared absorbance bands at approximately 1456, 1365, 905, 757, 662 & 604 cm−3 and having stable colour at ambient conditions of storage; and the process of its preparation comprising at least two repetitive steps of crystallization from one or more organic solvent by dissolving 2-methyl-4 -(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepine in said solvent and allowing crystallization to occur; wherein in at least one step the solution is purified by treating with a solid adsorbent material and filtering; and wherein in the last step the crystalline material is subjected to drying.
    Type: Application
    Filed: December 23, 2002
    Publication date: July 3, 2003
    Applicant: SUN PARMACEUTICAL INDUSTRIES LIMITED
    Inventors: Vijay Chhangamal Chhabada, Rajeev Budhdev Rehani, Rajamamannar Thennati
  • Publication number: 20030100088
    Abstract: Activated haptens useful for generating immunogens to HIV protease inhibitors, immunogens useful for producing antibodies to HIV protease inhibitors, and antibodies and labeled conjugates useful in immunoassays for HIV protease inhibitors. The novel haptens feature an activated functionality at the central, non-terminal hydroxyl group common to all HIV protease inhibitors, e.g., saquinavir, nelfinavir, indinavir, amprenavir, ritonavir and lopinavir.
    Type: Application
    Filed: July 10, 2002
    Publication date: May 29, 2003
    Inventors: Gerald F. Sigler, Raymond A. Hui, Ina Deras, Richard Terry Root, Mitali Ghoshal, Erasmus J. Huber, Herbert W. Von Der Eltz, Sigrun Metz
  • Patent number: 6562810
    Abstract: The disclosure relates to a novel 8-substituted-9H-1,3-dioxolo-[4,5-h][2,3]benzodiazepine compound of formula I and pharmaceutically acceptable quaternary ammonium salts thereof, a process for preparing the same, a pharmaceutical composition containing a 8-substituted-9H-1,3-dioxolo-[4,5-h][2,3]benzodiazepine compound, and a method of treatment using the pharmaceutical composition. A complete description of the compound of formula I is found in the specification. The compounds of the general formula I possess unique competitive AMPA/kainite antagonist properties making them useful in the treatment of diseases where inhibition of the AMPA/kainite receptors may a favorable effect.
    Type: Grant
    Filed: May 19, 2000
    Date of Patent: May 13, 2003
    Assignee: Egis Gyogyszergyar RT.
    Inventors: László Balázs, József Barkóczy, Imre Domán, András Egyed, Istvän Gacsályi, Gábor Gigler, Zoltán Greff, István Gyertyán, Péter Kótay Nagy, Attila Kovács, György Lávay, Zoltán Rátkai, Péter Seres, Gyula Simig, Annamária Simó, Tamás Szabados, Géza Szabó, Károly Tihanyi, Miklós Végh, Géza Schneider, Judit Cselenyák
  • Publication number: 20030087892
    Abstract: This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V1 and V2 are both H, OMe or F, or one of V1 and V2 is Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N3, NH2, NHBn or NH-acyl and the other is H, or V1 and V2 together are ═O, —O(CH2)pO— or —S(CH2)pS—; W1 is either O or S; X1 and X2 are both H, or together are ═O or ═S; Y is OR5 or NR6R7; R1, R2, R3 and R4 are independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; R5 is selected from H and lower alkyl; R6 and R7 are independently selected from H and lower alkyl, or together are —(CH2)n; n=3, 4, 5, 6; and p is 2 or 3. The compounds are agonists at the vasopressin V2 receptor and are useful as antidiuretics and procoagulants.
    Type: Application
    Filed: May 23, 2002
    Publication date: May 8, 2003
    Inventors: Doreen Mary Ashworth, Gary Robert William Pitt, Peter Hudson, Chritpoher Martyn Yea, Richard Jeremy Franklin
  • Publication number: 20030022889
    Abstract: The present invention provides a method for treating ALS and for providing a neuro-protective effect comprising administering a therapeutically effective of olanzapinc or a pharmaceutically acceptable salt or solvate thereof.
    Type: Application
    Filed: August 27, 2002
    Publication date: January 30, 2003
    Inventors: Franklin P. Bymaster, Gary D. Tollefson
  • Patent number: 6458783
    Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formulas their enantiomers, diastereomers, and pharmaceutically acceptable salts, prodrugs and solvates thereof.
    Type: Grant
    Filed: April 21, 2000
    Date of Patent: October 1, 2002
    Assignee: Bristol-Myers Squibb Company
    Inventors: Charles Z. Ding, John T. Hunt, Katerina Leftheris, Rajeev S. Bhide
  • Publication number: 20020128260
    Abstract: The present invention relates to compounds of the general formula (I) 1
    Type: Application
    Filed: February 8, 2002
    Publication date: September 12, 2002
    Inventors: Lone Jeppesen, Per Sauerberg, Anthony Murray, Paul Stanley Bury
  • Patent number: 6440959
    Abstract: Disclosed are novel pyrazolobenzodiazepines having the formula and the pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and R4 are as defined herein. These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer, more particularly, the treatment or control of breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing the compounds of formula I as well as intermediates useful in the preparation of the compounds of formula I.
    Type: Grant
    Filed: April 12, 2000
    Date of Patent: August 27, 2002
    Assignee: Hoffman-La Roche Inc.
    Inventors: Qingjie Ding, Jin-Jun Liu, Vincent Stewart Madison, Giacomo Pizzolato, Chung-Chen Wei, Peter Michael Wovkulich
  • Publication number: 20020035104
    Abstract: Provided are compounds of formula (I) 1
    Type: Application
    Filed: August 16, 2001
    Publication date: March 21, 2002
    Applicant: GENENTECH, INC.
    Inventors: Dean R. Artis, David Y. Jackson, Thomas E. Rawson, Mark E. Reynolds, Daniel P. Sutherlin, Mark S. Stanley
  • Publication number: 20020025958
    Abstract: Substituted benzodiazepine compositions are provided which are active as non-NMDA ionotropic excitatory amino acid (EAA) receptor antagonists. The compounds are generally 7- or 8-mono substituted 5H-2,3-benzodiazepines. The compositions are useful for treating disorders associated with excessive activation of the non-NMDA subtype of the ionotropic EAA receptor. The compounds further are useful as testing agents to identify and characterize other compounds for the treatment of these disorders. The compounds are useful therapeutically as sedatives or for the treatment of neurosychopharmacological disorders such as stroke, ischemia and epilepsy. The compositions may be provided in combination with a suitable carrier for oral or parenteral administration. The compounds may be administered orally or parenterally for the treatment of a variety of disorders associated with non-NMDA EEA receptor function.
    Type: Application
    Filed: June 15, 2001
    Publication date: February 28, 2002
    Inventors: Xue-Feng Pei, Baoqing Li, Maria-Luisa Maccecchini
  • Patent number: 6348458
    Abstract: The invention provides three new polymorphic forms of 2-methyl-4-[4-methyl-1-piperazinyl]-10H-thieno[2,3b][1,5]benzodiazepine (Olanzapine) (Formula A), the process for preparing the new polymorphs and pharmaceutical compositions containing the polymorphs. The new polymorphic forms of olanzapine are useful for the treatment of psychotic conditions, mild anxiety and gastrointestinal conditions.
    Type: Grant
    Filed: March 31, 2000
    Date of Patent: February 19, 2002
    Assignee: U & I Pharmaceuticals Ltd.
    Inventors: Yusuf K. Hamied, Rajendra N. Kankan, Dharmaraj R. Rao
  • Patent number: 6346528
    Abstract: Methods and compositions are disclosed utilizing 2-hydroxymethylolanzapine for the treatment of psychosis in humans. 2-Hydroxymethylolanzapine exhibits a lessened liability toward drug-drug interactions than olanzapine and a more predictable dosing regimen than olanzapine. 2-Hydroxymethylolanzapine is also useful for the treatment of acute mania, mild anxiety states, anxiety disorders, schizophrenia, bipolar disorder, attention deficit hyperactivity disorder, autistic disorder, excessive aggression, substance abuse, depressive signs and symptoms, tic disorder, functional bowel disorder and fungal dermatitis.
    Type: Grant
    Filed: October 17, 2000
    Date of Patent: February 12, 2002
    Assignee: Sepracor Inc.
    Inventor: William E. Yelle
  • Patent number: 6319919
    Abstract: Compounds of the formula wherein the broken line represents an optionally present double bond, and R1-R3, R4, R6 and R9 are as defined herein, and compositions containing these compounds can be used to inhibit acetylcholinesterase activity and treat Alzheimer's Disease.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: November 20, 2001
    Inventors: Bonnie Davis, Madeleine M. Joullie
  • Patent number: RE40033
    Abstract: 2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno-[2,3-b][1,5]benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders of the central nervous system.
    Type: Grant
    Filed: December 18, 2001
    Date of Patent: January 22, 2008
    Assignee: Eli Lilly and Company
    Inventors: Reba Chakrabarti, Terrence Michael Hotten, David Edward Tupper, Jiban Kumar Chakrabarti