Additional Hetero Atom In The Additional Cyclo Of The Tricyclo Ring System Patents (Class 540/497)
  • Patent number: 5401737
    Abstract: The invention relates to a compound of the formula ##STR1## wherein R.sup.1 is aryl which may have suitable substituent(s), X is --O-- or ##STR2## in which R.sup.3 is hydrogen or lower alkyl, A is a bond or lower alkylene which may have lower alkyl group(s), andR.sup.2 is arylcarbamoyl which may have halogen or lower alkoxy,or a pharmaceutically acceptable salt thereof, useful as a cholecystokinin antagonist.
    Type: Grant
    Filed: July 23, 1993
    Date of Patent: March 28, 1995
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Yoshinari Sato, Teruaki Matuo, Takatomo Ogahara
  • Patent number: 5322842
    Abstract: Tricyclic compounds of the formula: ##STR1## wherein R.sup.1 1 is hydrogen or an organic group,R.sup.2 is aryl which may have suitable substituent(s),R.sup.3 is hydrogen or an acyl group andA is lower alkylene,and pharmaceutically acceptable salts thereof which are useful as a medicament.
    Type: Grant
    Filed: February 19, 1993
    Date of Patent: June 21, 1994
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Yoshinari Sato, Teruaki Matuo, Takatomo Ogahara
  • Patent number: 5308842
    Abstract: Conformationally constrained tricyclic derivatives of the thienodiazocine and thienothiadiazocine classes of compounds and ring homologs thereof are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma associated therewith.
    Type: Grant
    Filed: May 10, 1993
    Date of Patent: May 3, 1994
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello
  • Patent number: 5248679
    Abstract: The invention relates to novel cholecystokinin antagonists of the formula ##STR1## wherein R.sup.1 is aryl which may have suitable substituent(s), X is --O-- or ##STR2## in which R.sup.3 is hydrogen or lower alkyl, A is bond; or methylene, ethylene, trimethylene, tetramethylene, pentamethylene or hexamethylene, each of which may have lower alkyl group(s), andR.sup.2 is heterocyclic(C.sub.3 -C.sub.6) alkenoyl or heterocycliciccarbonyl, or a pharmaceutically acceptable salt thereof, useful as a cholecystokinin antagonist.
    Type: Grant
    Filed: July 27, 1992
    Date of Patent: September 28, 1993
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Yoshinari Sato, Teruaki Matuo, Takatomo Ogahara
  • Patent number: 5218117
    Abstract: The invention relates to novel compounds of the general formula (I), ##STR1## The compounds of the invention antagonize the effects of constrictive mediators, e.g. histamine, acetylcholine or serotonin; they show an antiallergic action and possess an antiinflammatory effect. Thus, these compounds can therapeutically be used as bronchodilators as well as antiallergic or antiinflammatory drugs, particularly in the treatment of bronchial asthma.
    Type: Grant
    Filed: September 25, 1992
    Date of Patent: June 8, 1993
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.
    Inventors: Kalman Takacs, Iloma Kiss nee Ajzert, Istvan Hermecz, Janos Ori, Maria H. Pap, Zsolt Bencze, Peter Szekely Kormoczy, Maria Szabo, Judit Szeredy, Csaba Vertesi, Lorand Debreczeni, Jozsef Gaal, Zoltan Kapui
  • Patent number: 5155101
    Abstract: The invention relates to a compound of the formula: ##STR1## wherein R.sup.1 is aryl which may have suitable substituents(s), X is --O-- or ##STR2## in which R.sup.3 is hydrogen or lower alkyl, A is a bond or lower alkylene which may have lower alkyl group(s), andR.sup.2 is hydrogen; heterocyclic(lower)alkenoyl which may have carboxy or protected carboxy; heterocycliccarbonyl which may have N,N-di(lower)alkylamino(lower)alkyl, hydroxyimino(lower)alkyl, aryliminio(lower)alkyl, acyl or hydroxy(lower)alkylheterocyclic(lower)alkyl; aroyl which may have 1 to 3 substituent(s) selected from the group consisting of halogen, amino and mono(or di or tri)halo(lower)alkyl; arylcarbamoyl which may have halogen or lower alkoxy; arylamino(lower)alkanoyl; or ar(lower)alkanoyl which may have amino or protected amino,or a pharmaceutically acceptable salt thereof, useful as a cholecystokinin antagonist.
    Type: Grant
    Filed: November 15, 1990
    Date of Patent: October 13, 1992
    Assignee: Fujisawa Pharmaceutical Company, Ltd.
    Inventors: Yoshinari Sato, Teruaki Matuo, Takatomo Ogahara
  • Patent number: 5082839
    Abstract: The invention relates to new thieno-triazolo-1,4-diazepino-2-carboxylic acid amides of formula I ##STR1## wherein R.sub.1 represents hydrogen, a C.sub.1-C.sub.4 straight-chained or branched alkyl which can optionally be substituted by halogen, preferably C1 or Br, or by hydroxy, cyclopropyl, C.sub.1 -C.sub.3 alkoxy, preferably methoxy, or halogen, preferably chlorine or bromine;R.sub.2 and R.sub.3, each independently, represent hydrogen, a C.sub.1 -C.sub.4 straight-chained or branched alkyl, C.sub.1 -C.sub.4 hydroxyalkyl or the two groups R.sub.2 and R.sub.3 together with the nitrogen atom represent a 5-, 6- or 7-membered ring which optionally contains a nitrogen, oxygen or sulfur atom as a further heteroatom, the second nitrogen atom optionally being substituted by a C.sub.1 -C.sub.4 alkyl, preferably a methyl group;R.sub.
    Type: Grant
    Filed: June 15, 1990
    Date of Patent: January 21, 1992
    Assignee: Boehringer Ingelheim GmbH
    Inventors: Karl-Heinz Weber, Albrecht Harreus, Jorge Casals-Stenzel, Gojko Muacevic, Wolfgang Troger, Gerhard Walther
  • Patent number: 5008263
    Abstract: Platelet activating factor antagonists of formula (I), (II) or (III): ##STR1## where A is optionally substituted benzene, pyridine, naphthalene, quinoline, thiophene, benzothiophene, pyrazole or isothiazole,X is O, S or NHY is 1,4 phenylene or a group of formula ##STR2## R.sup.1 is H or optionally substituted C.sub.1 -C.sub.4 alkyl, R.sup.2 and R.sup.3 are H or C.sub.1 -C.sub.4 alkyl,B is an optionally fused 5- or 6-membered ring containing nitrogen atoms,Het is an optionally substituted 5-membered heterocyclic ring containing nitrogen or a pyridine ring, the ring optionally being fused to benzene or nitrogen-containing heterocyclic ring.
    Type: Grant
    Filed: March 20, 1990
    Date of Patent: April 16, 1991
    Assignee: Pfizer Inc.
    Inventors: Kelvin Cooper, Michael J. Fray
  • Patent number: 4992437
    Abstract: Thienodiazepine compounds of the general formula ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and respectively stand for a hydrogen atom, a halogen, an alkyl or an aralkyl, or mean a group wherein R.sup.1 and R.sup.2 combinedly together form a ring; R.sup.3 stands for an oxygen atom, R.sup.4 stands for a hydrogen atom, an alkyl, an alkenyl or a group of the formula --(CH.sub.2).sub.m COOR.sup.6 (wherein R.sup.6 l stands for a hydrogen atom, an alkyl, an alkenyl or an aralkyl and m stands for an integer of 1-6), or R.sup.3 and R.sup.4 stand for a group wherein R.sup.3 and R.sup.4 combinedly together form a group of the formula .dbd.N--N.dbd.C(R.sup.5)-- [wherein R.sup.5 stands for a hydrogen atom, an alkyl, an alkenyl, an aralkyl or a group of the formula --(CH.sub.2).sub.n COOR.sup.7 (wherein R.sup.
    Type: Grant
    Filed: August 9, 1989
    Date of Patent: February 12, 1991
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Yoichi Naka, Yukio Hitotsuyanagi, Keiichiro Haga, Masahiro Hosoya
  • Patent number: 4981847
    Abstract: Tricyclo benzodiazepines are cholecystokinin antagonists.
    Type: Grant
    Filed: August 21, 1989
    Date of Patent: January 1, 1991
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Yoshinari Sato, Teruaki Matuo, Takatomo Ogahara
  • Patent number: 4939137
    Abstract: The synthesis of ring-fused thienopyrimidinedione derivatives is described. The novel ring-fused thienopyrimidinedione derivatives are generally vasodilating agents and antihypertensive agents and as such are useful as cardiovascular agents.
    Type: Grant
    Filed: June 28, 1989
    Date of Patent: July 3, 1990
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Ronald K. Russell, Richard A. Rampulla
  • Patent number: 4642343
    Abstract: Aromatic azepinones and thiones having the formula ##STR1## wherein: A is benzene, naphthalene, quinoline or pyridine;B is oxygen or sulfur;E is oxygen, sulfur or ##STR2## n is 1, 2 or 3; Z is an amino or a heterocyclic nitrogen containing radical;R is hydrogen, loweralkyl, cycloalkyl or phenylloweralkyl;and having antihistaminic utility, a process for the preparation thereof and chemical intermediates therefor are disclosed.
    Type: Grant
    Filed: March 3, 1986
    Date of Patent: February 10, 1987
    Assignee: A. H. Robins Company, Incorporated
    Inventor: Albert D. Cale, Jr.