Patents Examined by Philip I. Datlow
  • Benzodiazepine derivatives
    Patent number: 5521175
    Abstract: Compounds of Formula (I), and salts and prodrugs thereof, wherein R.sup.1 represents C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl; R.sup.2 optionally substituted phenyl or R.sup.2 represents a group (A) where W is CH.sub.2 or NR.sup.10, and W.sup.1 is CH.sub.2, or W and W.sup.1 each represent 0; R.sup.3 is C.sub.1-6 alkyl, halo or NR.sup.13 R.sup.14 ; R.sup.4 is H, C.sub.1-4 alkyl, optionally substituted phenyl or optionally substituted benzyl; R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are H or C.sub.1-4 alkyl; or any two of R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 together form a chain (CH.sub.2).sub.t, and any other two of R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 optionally form a chain (CH.sub.2).sub.s where s and t are independently 1, 2 or 3; m is 2, 3, 4, 5, 6, 7, 8 or 9; n is 0, 1, 2, 3 or 4; and x is 0, 1, 2 or 3; are CCK and/or gastrin antagonists useful in therapy.
    Type: Grant
    Filed: January 26, 1995
    Date of Patent: May 28, 1996
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jose L. Castro Pineiro, Mark S. Chambers, Victor G. Matassa
  • Tricyclic benzazepine vasopressin antagonists
    Patent number: 5521173
    Abstract: Tricyclic diazepines of the Formula I: ##STR1## wherein A, B, D, E, F, Y, and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.
    Type: Grant
    Filed: January 17, 1995
    Date of Patent: May 28, 1996
    Assignee: American Home Products Corporation
    Inventors: Aranapakam M. Venkatesan, Jay D. Albright, George T. Grosu
  • Synthesis of pyridooxazinyl-indoles
    Patent number: 5519131
    Abstract: This application relates to a process for the preparation of indolylpyridooxazines of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification which comprises cyclizing compound of the formula ##STR2## in the presence of a strong base such as sodium hydride or potassium t-butoxide.
    Type: Grant
    Filed: October 20, 1993
    Date of Patent: May 21, 1996
    Assignee: Hoechst Marion Roussel Inc.
    Inventors: Richard C. Effland, Larry Davis, Gordon E. Olsen
  • Tricyclic diazepine vasopressin antagonists and oxytocin antagonists
    Patent number: 5516774
    Abstract: Tricyclic diazepines of the formula: ##STR1## wherein A, B, D, E, F, Y and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.
    Type: Grant
    Filed: June 13, 1994
    Date of Patent: May 14, 1996
    Assignee: American Cyanamid Company
    Inventors: Jay D. Albright, Marvin F. Reich, Fuk-Wah Sum, Efren G. Delos Santos
  • Tricyclic 2,3,4,5-tetrahydro-1H-3-benzapines
    Patent number: 5512562
    Abstract: Tricyclic benzazepines having the general formula ##STR1## wherein A together with the .alpha.- and .beta.-marked carbon atoms is a cyclopentene, cyclohexene, furan, dihydrofuran, pyran, dihydropyran, thiophene, oxazole, pyrrole, pyrroline, tetrahydropyridine or dioxole ring, R.sup.1 is H or alkyl, R.sup.2 and R.sup.3 independently are H, alkoxy, halogen, nitro, cyano or hydroxy, or R.sup.2 and R.sup.3 together may form a furan, dihydrofuran, cyclopentene or dioxole ring and R.sup.4 is H, alkoxy, nitro, cyano, hydroxy or halogen, or a pharmaceutically acceptable salt thereof, are useful in treatment of certain disorders in the central nervous system, e.g., psychosis, pain, depression, sleep disturbances, dyskinesia, Parkinson's disease, stroke.
    Type: Grant
    Filed: February 24, 1994
    Date of Patent: April 30, 1996
    Assignee: Novo Nordisk A/S
    Inventors: Rolf Hohlweg, Erik B. Nielsen
  • Tricyclic compounds having affinity for the 5-HT1A receptor
    Patent number: 5512566
    Abstract: Compounds represented by the general formula I: ##STR1## are disclosed as useful in treating diseases of the central nervous system.
    Type: Grant
    Filed: October 25, 1993
    Date of Patent: April 30, 1996
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Ellen W. Baxter, Allen B. Reitz
  • Tricyclic benzazepine vasopressin antagonists
    Patent number: 5512563
    Abstract: Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.
    Type: Grant
    Filed: June 13, 1994
    Date of Patent: April 30, 1996
    Assignee: American Cyanamid Company
    Inventors: Jay D. Albright, Fuk-Wah Sum, Xuemei Du
  • Benzo-fused lactams
    Patent number: 5504080
    Abstract: Compounds of the formula ##STR1## wherein A is ##STR2## are useful as ACE and NEP inhibitors and those wherein A is ##STR3## are useful as ACE inhibitors. Methods of preparation and intermediates are also disclosed.
    Type: Grant
    Filed: September 22, 1993
    Date of Patent: April 2, 1996
    Assignee: Bristol-Myers Squibb Co.
    Inventor: Donald S. Karanewsky
  • Process for preparing intermediates for the synthesis of D1 antagonists
    Patent number: 5502186
    Abstract: Disclosed are a process and intermediates of the formula ##STR1## wherein R is --CH.sub.3 or --C(O)--OR.sup.1, and R.sup.1 is C.sub.1 -C.sub.6 alkyl or --CH.sub.2 C.sub.6 H.sub.5 ; or the formula ##STR2## wherein: R.sup.2 is H or OH, R is --C(O)OR.sup.1 and R.sup.1 is C.sub.1 -C.sub.6 alkyl or --CH.sub.2 C.sub.6 H.sub.5, or where R.sup.2 is H, R can also be CH.sub.3 ; for preparing benzazepine intermediates of the formula ##STR3## The benzazepine intermediates are useful for preparing benzazepines having activity as selective D1 receptor antagonists.
    Type: Grant
    Filed: May 23, 1995
    Date of Patent: March 26, 1996
    Assignee: Schering Corporation
    Inventors: Donald Hou, Richard W. Draper, Gary M. Lee, Janet L. Mas
  • Synthesis of 4,10-dinitro-2,6,8,12-tetraoxa-4,10-diazatetracyclo[5.5.0.05,903,11]dode cane
    Patent number: 5498711
    Abstract: 4,10-dinitro-2,6,8,12-tetraoxa-4,10-diazatetracyclo[5.5.0.0.sup.5,9 0.sup.3,11 ]dodecane is synthesized by reacting a diacyl-2,3,5,6-tetraoxypiperazine or tetraoxadiazaisowurtzitane derivative, a strong acid, and a nitrate source, such that an exothermic reaction occurs which proceeds at a temperature above ambient temperature. The reaction product is precipitated by cooling. It may be purified by washing with methanol and/or sodium bicarbonate and by simmering in nitric acid.
    Type: Grant
    Filed: August 2, 1993
    Date of Patent: March 12, 1996
    Assignee: Thiokol Corporation
    Inventors: Thomas K. Highsmith, W. Wayne Edwards, Robert B. Wardle
  • Triphenodioxazine dyes
    Patent number: 5498712
    Abstract: A water-soluble triphenodioxazine dye having a chloro or bromo atom at one of the 6- and 13-positions and a group of Formula (1) at the remaining 6- or 13-position: ##STR1## wherein: R.sup.1 is H, OH or CH.sub.3 ; andR.sup.2 is C.sub.1-3 -alkyl, hydroxy-C.sub.1-3 -alkyl or --CH.sub.2 --(C.sub.1-4 -alkyl).The dyes are useful for the coloration of textile materials.
    Type: Grant
    Filed: May 13, 1993
    Date of Patent: March 12, 1996
    Assignee: Zeneca Limited
    Inventor: Gordon A. Thomson
  • Ophthalmic use of S-timolol hemihydrate
    Patent number: 5496820
    Abstract: A novel composition and method for making compositions containing S-timolol hemihydrate having the formula: ##STR1## wherein the compositions are useful as pharmaceutical agents for topical administration to an eye for treating glaucoma and/or lowering intraocular pressure.
    Type: Grant
    Filed: July 27, 1993
    Date of Patent: March 5, 1996
    Inventor: Markku Pera/ lampi
  • Derivatives of thieno-triazolo-diazepine and therapeutic compositions containing them
    Patent number: 5492906
    Abstract: The invention relates to thieno-triazolo-diazepine derivatives of the formula: ##STR1## wherein Y stands for oxygen or sulphur and R stands for various substituents, to a preparation process of said compounds and to therapeutic compositions containing the same. The compounds are particularly interesting as anti-asthmatic, anti-allergic and gastro-intestinal protectors.
    Type: Grant
    Filed: February 18, 1992
    Date of Patent: February 20, 1996
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Pierre Braquet, Andre Esanu, Jean-Pierre Laurent, Alain Rolland
  • Derivatives of cyclic ethers and sulfides for the treatment of atherosclerosis
    Patent number: 5491152
    Abstract: The present invention provides compounds of Formula I, ##STR1## or a pharmaceutically acceptable salt forms thereof, which are inhibitors of acyl-Coenzyme A: cholesterol O-acyltransferase (ACAT), pharmaceutical compositions containing such compounds, processes for the preparation of such compounds, and the use of such compounds as antihypercholesterolemic and/or antiatherosclerotic agents.
    Type: Grant
    Filed: March 23, 1994
    Date of Patent: February 13, 1996
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventors: Richard G. Wilde, Soo S. Ko, Jeffrey T. Billheimer
  • Substituted N-cycloalkylmethyl-1H-pyrazolo(3,4-b)quinolin-4 amines and compositions and methods of use thereof
    Patent number: 5488055
    Abstract: Substituted N-cycloalkylmethyl-1H-pyrazolo[3,4-b]quinolin-4-amines, pharmaceutical compositions containing them and methods for a) effecting c-GMP-phosphodiesterase inhibition, b) treating heart failure and/or hypertension, c) reversing or reducing nitrate-induced tolerance and d) treating angina pectoris, congestive heart disease and myocardial infarction utilizing them.
    Type: Grant
    Filed: March 10, 1995
    Date of Patent: January 30, 1996
    Assignee: Sanofi Winthrop Inc.
    Inventors: Virendra Kumar, John A. Dority, Jr.
  • Intermediates for preparing antifolate compounds
    Patent number: 5486614
    Abstract: This invention relates to intermediates, and processes thereto, for the preparation of tetrahydropyrido[2,3-d]pyrimidines which are useful for the treatment of susceptable neoplasms. The intermediates have the following formula II; ##STR1## wherein the R, R.sup.1 and A groups are as defined in the specification.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: January 23, 1996
    Assignee: Eli Lilly and Company
    Inventors: Charles J. Barnett, Thomas M. Wilson
  • Quinazoline derivatives as acetylcholinesterase inhibitors
    Patent number: 5486512
    Abstract: A method of treating cognitive deficiencies is described by administering a quinazoline derivative of the general formula ##STR1## wherein A represents ##STR2## in which n is 1-10, P is a bond or (CH.sub.2).sub.m in which m is 0-10, and M is .dbd.O, .dbd.S, .dbd.NR, .dbd.CRR', ##STR3## novel compounds of the above are also described as well as methods of manufacture and pharmaceutical compositions.
    Type: Grant
    Filed: March 17, 1994
    Date of Patent: January 23, 1996
    Assignee: Warner-Lambert Company
    Inventor: Vlad E. Gregor
  • Dioxazine blue dye compound having vinylsulfone type fiber reactive groups
    Patent number: 5486607
    Abstract: A dioxazine compound represented by the following formula in the free acid form, ##STR1## wherein V is a direct linkage or ##STR2## in which R.sub.3 is hydrogen or alkyl, X is a direct linkage or an aliphatic, araliphatic or aromatic bridging group, Y is phenylene or naphthylene, Z is a so-called vinylsulfone type fiber reactive group, and R.sub.1 and R.sub.2 are each hydrogen or alkyl, which is useful for dyeing or printing fiber materials to give a dyed or printed product of a blue color superior in fastness properties with superior build-up property.
    Type: Grant
    Filed: January 27, 1995
    Date of Patent: January 23, 1996
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Tetsuya Miyamoto, Miyao Takahashi, Takahiko Fujisaki, Naoki Harada, Yutaka Kayane, Takashi Omura
  • Phthalocyanine photosensitizers for photodynamic therapy and methods for their use
    Patent number: 5484778
    Abstract: The present invention relates to a series of novel phthalocyanine compositions (or compounds) suitable for use as photosensitizers for photodynamic therapy. Specifically, the invention relates to a series of new aluminum (Al) germanium (Ge), gallium (Ga), tin (Sn) and/or silicon (Si) phthalocyanines having substituted amine or quaternary ammonium axial ligands attached to the central metal, and the use of these new phthalocyanine compositions for the treatment of cancer through photosensitization. Moreover, the present invention is directed to the methods of preparing these compositions for use in photodynamic therapy.
    Type: Grant
    Filed: September 2, 1993
    Date of Patent: January 16, 1996
    Assignee: University Hospitals of Cleveland
    Inventors: Malcolm E. Kenney, Nancy L. Oleinick, Boris D. Rihter, Ying-Syi Li
  • Imidazo[4,5-C]quinoline amines
    Patent number: 5482936
    Abstract: Compounds and pharmaceutically acceptable salts thereof formally derived by bridging the 1- and 2-positions of 1H-imidazo[4,5-c]quinolin-4-amines. Also, methods of using such compounds and pharmaceutical formulations containing such compounds. Said compounds are useful to induce interferon biosynthesis in an animal.
    Type: Grant
    Filed: January 12, 1995
    Date of Patent: January 9, 1996
    Assignee: Minnesota Mining and Manufacturing Company
    Inventor: Kyle J. Lindstrom