Polycyclo Ring System Having At Least Three Cyclos And Having The Hetero Ring As One Of The Cyclos Patents (Class 549/12)
  • Patent number: 5118701
    Abstract: Novel tricyclic compound represented by formula (I): ##STR1## possess a TXA.sub.2 biosynthesis inhibiting activity and/or a TXA.sub.2 receptor antagonizing activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.
    Type: Grant
    Filed: November 14, 1990
    Date of Patent: June 2, 1992
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
  • Patent number: 5071853
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: February 27, 1990
    Date of Patent: December 10, 1991
    Inventors: Christopher F. Bigge, Sheryl J. Hays, Graham Johnson, Perry M. Novak, Daniel F. Ortwine
  • Patent number: 5036067
    Abstract: Compounds having the formula I: ##STR1## are inhibitors of the 5-lipoxygenase enzyme. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.
    Type: Grant
    Filed: March 14, 1990
    Date of Patent: July 30, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Yves Girard, Pierre Hamel, Daniel Delorme
  • Patent number: 5026877
    Abstract: Disclosed are new 1,3-dioxenones having the formulae ##STR1## in an optically pure state, a process for preparing same and the use thereof.
    Type: Grant
    Filed: May 10, 1989
    Date of Patent: June 25, 1991
    Assignee: Studiengesellschaft Kohle mbH
    Inventors: Kurt Schaffner, Martin Demuth
  • Patent number: 5006664
    Abstract: Novel aminoalkylthiodibenzothiepins and related compounds, physiologically tolerable acid addition salts thereof, a method of preparing same, pharmaceutical and veterinary preparations including same and methods of treating by administering same are disclosed. These compounds are useful as antidepressant, analgetic, and anticonvulsant agents.
    Type: Grant
    Filed: December 20, 1989
    Date of Patent: April 9, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Helen H. Ong, Vernon B. Anderson, James A. Profitt
  • Patent number: 4996316
    Abstract: A process for the preparation of tertiary N,N-dimethylamines by the reaction of primary amines, formaldehyde, and hydrogen under pressure and at elevated temperature in the presence of a nickel-containing hydrogenation catalyst in the liquid phase. The hydrogenation catalyst is suspended in a solvent, the nickel concentration is 0.1 to 10% by weight, based on the primary amine. The starting materials are separate from each other, brought to 80.degree. to 150.degree. C. and 1 to 15 MPa and fed into the catalyst suspension simultaneously with stirring and reacted in one step to form the tertiary N,N-dimethylamines.
    Type: Grant
    Filed: December 24, 1988
    Date of Patent: February 26, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Jurgen Weber, Detlef Kampmann, Claus Kniep
  • Patent number: 4963683
    Abstract: A process for synthesizing polyoxa tetracyclics which involves the ozonolysis of a single-ring-structure vinyl silane with resulting direct formation of the desired multiple ring matrial. The polyoxa tetracyclic compounds have the formula ##STR1## The vinyl silanes have the structure ##STR2## The vinyl silanes are new chemical compounds as are corresponding primary ozonide and dioxetane intermediates. In a preferred embodiment, this invention provides a total synthesis of the antimalarial artemisinin.
    Type: Grant
    Filed: February 15, 1989
    Date of Patent: October 16, 1990
    Assignee: SRI International
    Inventors: Mitchell A. Avery, Clive Jennings-White
  • Patent number: 4891433
    Abstract: A novel process for the preparation of 2-(10,11-dihydro-10-oxodibenzo[b, f]thiepin-2-yl)propionic acid which shows high anti-inflammatory and analgetic action is disclosed. The process starts from a propiophenone derivative having the formula (II): ##STR1## wherein R.sup.1 is hydrogen or a lower alkyl group, which is once converted into a haloacetal compound via a halo-ketone compound, and then converted into the desired dibenzothiepin derivative through a combination of rearrangement, hydrolysis and ring closure in variable sequences.
    Type: Grant
    Filed: September 30, 1987
    Date of Patent: January 2, 1990
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Mitsuo Masaki, Hiromitsu Takeda, Naoya Moritoh, Toshihiro Takahashi
  • Patent number: 4885404
    Abstract: Disclosed is a process for the production of acids of the formula ##STR1## wherein R is 2-fluoro-4-(1,1'-biphenyl), 4-(2-methylpropyl)phenyl, 6-methoxy-2-napthyl, 3-benzophenyl, 4-(2-thienylcarbonyl)-phenyl or 7-chlorocarbazole-3-yl which comprises contacting an organometallic compound of the formula R--M--R.sub.
    Type: Grant
    Filed: March 6, 1987
    Date of Patent: December 5, 1989
    Assignee: The Upjohn Company
    Inventor: Peter G. M. Wuts
  • Patent number: 4882351
    Abstract: Novel tricyclic compounds having a TXA.sub.2 -antagonizing activity represented by formula (I): ##STR1## which strongly antagonize an action of thromboxane A.sub.2 and are expected to have preventive and therapeutic effects on ischemica diseases, cerebro-vascular diseases, etc.
    Type: Grant
    Filed: October 11, 1988
    Date of Patent: November 21, 1989
    Assignee: Roussel Uclaf
    Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
  • Patent number: 4775683
    Abstract: Novel aminoalkylthiodibenzothiepins and related compounds, physiologically tolerable acid addition salts thereof, a method of preparing same, pharmaceutical and veterinary preparations including same and methods of treating by administering same are disclosed. These compounds are useful as antidepressant, analgetic, and anticonvulsant agents.
    Type: Grant
    Filed: February 13, 1987
    Date of Patent: October 4, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Helen H. Ong, Vernon B. Anderson, James A. Profitt
  • Patent number: 4775682
    Abstract: Novel aminoalkylthiodibenzothiepins and related compounds, physiologically tolerable acid addition salts thereof, a method of preparing same, pharmaceutical and veterinary preparations including same and methods of treating by administering same are disclosed. These compounds are useful as antidepressant, analgetic, and anticonvulsant agents.
    Type: Grant
    Filed: February 13, 1987
    Date of Patent: October 4, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Helen H. Ong, Vernon B. Anderson, James A. Profitt
  • Patent number: 4766143
    Abstract: Novel aminoalkylthiodibenzothiepins and related compounds, physiologically tolerable acid addition salts thereof, a method of preparing same, pharmaceutical and veterinary preparations including same and methods of treating by administering same are disclosed. These compounds are useful as antidepressant, analgetic, and anticonvulsant agents.
    Type: Grant
    Filed: February 12, 1987
    Date of Patent: August 23, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Helen H. Ong, Vernon B. Anderson, James A. Profitt
  • Patent number: 4730054
    Abstract: The present invention relates to imidazolyl thieno-benzothiepin derivatives of the Formula I: ##STR1## and acid addition salts thereof with pharmaceutically acceptable inorganic and organic acids, wherein R is a hydrogen or a chlorine atom. The invention also relates to processes for the preparation of these compounds. These compounds demonstrate substantial in vitro and in vivo antimycotic properties of the kind useful for the treatment of dermal and vaginal mycoses.The new compounds can be prepared by reacting 4,9-dihydrothieno(2,3-c)-2-benzothiepin-4-ol or its 6-chloro derivative with imidazole or a reactive derivative thereof, such as 1,1'-carbonyl-diimidazole or 1,1'-thionyldiimidazole; or by first converting the respective thieno-benzothiepin-4-ol into its alkane- or arenesulfonate ester, followed by reaction with imidazole.
    Type: Grant
    Filed: December 1, 1986
    Date of Patent: March 8, 1988
    Assignee: SPOFA, Spojene Podinky Pro Zdravotnickou Vyrobu
    Inventors: Jan Leiner, Vladislava Hola, Miroslav Rajsner, Iva Matunova
  • Patent number: 4701538
    Abstract: A composition comprising a cyclic oligomer of the formula ##STR1## wherein X is selected from the group consisting of alkylene of two to twelve carbon atoms, inclusive, alkylidene of one to twelve carbon atoms, inclusive, cycloalkylene of four to twelve carbon atoms, inclusive cycloalkylidene of four to twelve carbon atoms, inclusive, --S--, --O--, --S--S--, ##STR2## a is zero or 1; n and m are the same or different and are integers of one to about fifteen;R is alkylene of two to eight carbon atoms, inclusive or alkylidene of one to eight carbon atoms, inclusive, phenylene or a single bond.R.sup.1 and R.sup.2 are the same or different and are alkyl or one to four carbon atoms, inclusive or halo;b and c are the same or different and are integers of zero to four; andR.sub.3 and R.sub.4 are the same or different and are alkyl of one to eight carbon atoms, inclusive, phenyl, hydrogen or R.sub.3 and R.sub.4 are taken together to form an alkylene of two to eight carbon atoms inclusive.
    Type: Grant
    Filed: November 12, 1985
    Date of Patent: October 20, 1987
    Assignee: General Electric Company
    Inventors: Niles R. Rosenquist, Kenneth F. Miller
  • Patent number: 4678788
    Abstract: N-substituted 2-chloro-7-fluoro-10-piperazino-10,11-dihydrodibenzo(b,f)thiepins are disclosed of the general formula I, ##STR1## in which R represents an aminocarbonyl, amino-oximinomethyl, 1,3-dioxolan-2-yl or 1,3-dioxan-2-yl, group and their addition salts with convenient organic and inorganic acids. These compounds are highly potent antidopaminergic, non-cataleptic neuroleptics of use in the treatment of schizophrenia. According to recent pharmacological assay results, the subject compounds are expected to be substantially free of the usual undesired extrapyramidal side effects. They can be obtained by common preparative methods from the respective starting compounds of formula III, IV or V, or also by appropriate interconversion reactions of other compounds of formula I.
    Type: Grant
    Filed: January 24, 1986
    Date of Patent: July 7, 1987
    Assignee: SPOFA, Spojene Podniky Pro Zdravotnickou Vyrobu
    Inventors: Miroslav Protiva, Jiri Jilek, Irena Cervena, Antonin Dlabac, Martin Valchar, Josef Pomykacek
  • Patent number: 4668695
    Abstract: Novel aminoalkylthiodibenzothiepins and related compounds, physiologically tolerable acid addition salts thereof, a method of preparing same, pharmaceutical and veterinary preparations including same and methods of treating by administering same are disclosed. These compounds are useful as antidepressant, analgetic, and anticonvulsant agents.
    Type: Grant
    Filed: October 28, 1983
    Date of Patent: May 26, 1987
    Assignee: Hoechst Roussel Pharmaceuticals Inc.
    Inventors: Helen H. Ong, Vernon B. Anderson, James A. Profitt
  • Patent number: 4645758
    Abstract: The invention concerns:Novel dibenz/b,e/oxepin and dibenz/b,e/thiepin compounds having the general formula: ##STR1## wherein X is O or S,R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and are each selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, lower alkoxy, lower alkylthio, lower alkylsulphinyl, lower alkylsulponyl, halogen, trifluoromethyl, trifluoromethylthio, lower dialkylsulphonamido, nitro, hydroxy, cyano, carbamyl, carboxy, lower alkoxycarbonyl, amino, N-lower alkylamino, N,N-diloweralkylamino, lower acylamido, lower alkanesulfonamido and lower acyl and, when on adjacent carbon atoms at the positions 2 and 3 and/or 8 and 9, two of the substituents R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4 taken together may form a methylenedioxy group;R.sup.5 and R.sup.
    Type: Grant
    Filed: January 17, 1986
    Date of Patent: February 24, 1987
    Inventors: Nils-Erik Willman, Bengt C. H. Sjogren, Lennart G. Nordh, Gustav L. Persson, Goran H. Sjoholm
  • Patent number: 4622403
    Abstract: Novel dibenz[b,f]thiepin derivatives are employed in the treatment and control of allergic conditions such as allergic asthma.
    Type: Grant
    Filed: October 11, 1983
    Date of Patent: November 11, 1986
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Haydn Williams, Joshua Rokach
  • Patent number: 4604128
    Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein: m is an integer selected from 1 to 4;n is zero or an integer selected from 1 to 4;X are selected from halogen, nitro, cyano, alkyl, substituted alkyl, hydroxy, alkoxy, alkylthio, sulfamoyl, substituted sulfamoyl, amino, substituted amino, the group --(CH.sub.2).sub.p C(.dbd.A)Z in which p is zero or one A is oxygen or sulfur, and Z is hydrogen, hydroxy, alkoxy, alkylthio, alkyl, substituted alkyl, amino or substituted amino, the group --NHC(.dbd.B)NR.sup.7 R.sup.8 in which B is oxygen or sulfur and R.sup.7 and R.sup.8 are hydrogen or alkyl;R.sup.1 is selected from hydrogen, acyl and an inorganic or organic cation;R.sup.2 is selected from alkyl, substituted alkyl, alkenyl, haloalkenyl, alkynyl and haloalkynyl;R.sup.3 is selected from alkyl, fluoroalkyl, alkenyl, alkynyl, and phenyl; andR.sup.4 is selected from hydrogen, halogen, alkyl, cyano and alkoxycarbonyl.
    Type: Grant
    Filed: September 10, 1985
    Date of Patent: August 5, 1986
    Assignee: ICI Australia Limited
    Inventors: Keith G. Watson, John D. Wishart, Graeme J. Farquharson, Graham J. Bird, Lindsay E. Cross
  • Patent number: 4536507
    Abstract: Prostaglandin antagonists are disclosed which are 7- and 8-substituted-dizenzo[b,f]thiepins of the structural formula: ##STR1##
    Type: Grant
    Filed: July 8, 1982
    Date of Patent: August 20, 1985
    Assignees: Merck & Co., Inc., Merck Frosst Canada, Inc.
    Inventors: Joshua Rokach, Clarence S. Rooney, Edward J. Cragoe, Jr.
  • Patent number: 4535171
    Abstract: Novel dibenzo[b,f]thiepin-3-carboxaldehydes and derivatives are prepared and employed in the treatment and control of allergic conditions such as allergic asthma.
    Type: Grant
    Filed: October 11, 1983
    Date of Patent: August 13, 1985
    Assignee: Merck Frosst Canada, Inc.
    Inventor: Joshua Rokach
  • Patent number: 4496447
    Abstract: Compounds of the formula ##STR1## wherein A, X, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4, n and m are defined hereinbelow are effective photoinitiators especially for the photopolymerization of ethylenically unsaturated compounds and for the curing of printing inks.
    Type: Grant
    Filed: December 21, 1982
    Date of Patent: January 29, 1985
    Assignee: Merck Patent Gesellschaft mit beschraenkter Haftung
    Inventors: Jurgen Eichler, Claus Herz, Karl-Heinz Neisius, Gregor Wehner
  • Patent number: 4435579
    Abstract: The present invention is concerned with an improved process for the production of highly active optical isomers of (-) 7 or 8 fluorodibenzo[b,f]thiepin-3-carboxylic acid-5-oxide having the structural formula ##STR1## in which the fluoro substituent replaces a hydrogen in the 7 or 8 position. The two active isomers represented by formula II are S(-)7-fluorodibenzo[b,f]thiepin-3-carboxylic acid-5-oxide and R(-)8-fluorodibenzo[b,f]thiepin-3-carboxylic acid-5-oxide. It is especially concerned with the resolution of the racemic 7 or 8 fluorodibenzo[b,f]thiepin-3-carboxylic acid-5-oxide by first forming and separating diastereomers of said racemic carboxylic acids by salt formation with ephedrine followed by crystallization and regeneration of the desired (-) isomers and recycling of the (+) isomer by racemization of the regenerated isomer. The compounds obtained in high yield by this process are highly active prostaglandin antagonists which are useful in treating a variety of conditions such as allergic asthma.
    Type: Grant
    Filed: July 12, 1982
    Date of Patent: March 6, 1984
    Assignee: Merck & Co., Inc.
    Inventors: Patrice C. Belanger, Haydn W. R. Williams, Joshua Rokach
  • Patent number: 4424213
    Abstract: Novel heterobicyclic compounds of Formula I, processes for preparing same and pesticidal compositions and methods are described.
    Type: Grant
    Filed: November 2, 1981
    Date of Patent: January 3, 1984
    Assignee: SDS Biotech Corporation
    Inventors: Thomas A. Magee, Robert D. Battershell, Lawrence E. Limpel, Andrew W. Ho, Arthur W. Friedman, H. Glenn Corkins, William W. Brand, Russell Buchman, Louis Storace, Edmond R. Osgood
  • Patent number: 4424355
    Abstract: The present invention is concerned with an improved process for the production of highly active optical isomers of (-) 7 or 8 fluorodibenzo?b,f!thiepin-3-carboxylic acid-5-oxide having the structural formula ##STR1## in which the fluoro substituent replaces a hydrogen in the 7 or 8 position. The two active isomers represented by formula II are S(-)7-fluorodibenzo?b,f!thiepin-3-carboxylic acid-5-oxide and R(-)8-fluorodibenzo?b,f!thiepin-3-carboxylic acid-5-oxide. It is especially concerned with the resolution of the racemic 7 or 8 fluorodibenzo?b,f!thiepin-3-carboxylic acid-5-oxide by first forming and separating diastereomers of said racemic carboxylic acids by salt formation with brucine or ephedrine followed by crystallization and regeneration of the desired (-) isomers and recycling of the (+) isomer by racemization of the regenerated isomer.
    Type: Grant
    Filed: February 24, 1982
    Date of Patent: January 3, 1984
    Assignee: Merck & Co., Inc.
    Inventors: Patrice C. Belanger, Haydn W. R. Williams, Joshua Rokach
  • Patent number: 4394515
    Abstract: Novel 7- and 8-R-10,11-dihydro-11-oxodibenzo[b,f]thiepin derivatives are employed in the treatment and control of allergic conditions such as allergic asthma.
    Type: Grant
    Filed: April 6, 1981
    Date of Patent: July 19, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Joshua Rokach, Clarence S. Rooney, Edward J. Cragoe, Jr.
  • Patent number: 4377702
    Abstract: Acetic acid derivatives having the formula, ##STR1## wherein X represents an oxygen or two hydrogen atoms, Y represents CH or N, A represents an oxygen or sulfur atom, and R represents hydroxy, amino or a lower alkoxy group having 1 to 5 carbon atoms possess excellent antiinfammatory activities.
    Type: Grant
    Filed: September 15, 1980
    Date of Patent: March 22, 1983
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Yasuo Fujimoto, Shigeru Yamabe
  • Patent number: 4356186
    Abstract: Novel acetic acid derivatives of the formula: ##STR1## wherein X is oxygen or sulfur; R.sub.1 is hydrogen or a lower alkyl; R.sub.2 is hydroxy, an alkoxy, an alkenyloxy, a cycloalkyloxy, an aryloxy, a substituted aryloxy, an aryl-lower alkoxy, a substituted aryl-lower alkoxy, an aryl-lower alkenyloxy, a substituted aryl-lower alkenyloxy, an .omega.-disubstituted amino-lower alkoxy, a lower alkoxycrbonyl-lower alkoxy, a lower alkoxy-lower alkoxy, a hydroxy-lower alkoxy-lower alkoxy, an acyl-lower alkoxy, or a group ##STR2## wherein R.sub.3 is hydrogen, hydroxy, a lower alkyl, an aryl-lower alkyl, a hydroxy-lower alkyl, or a carboxy-lower alkyl, R.sub.4 is hydrogen, a lower alkyl or a hydroxy-lower alkyl, or the R.sub.3 and R.sub.4 may combine together with the nitrogen atom to which they are joined to form a heterocyclic group; and the group --CH(R.sub.1)COR.sub.
    Type: Grant
    Filed: March 20, 1981
    Date of Patent: October 26, 1982
    Assignee: Dainippon Pharmaceutical Co., Ltd.
    Inventors: Hitoshi Uno, Mikio Kurokawa, Hideo Nakamura
  • Patent number: 4347254
    Abstract: A compound of the formula: ##STR1## wherein A.sub.1 is a single bond or a C.sub.1 -C.sub.5 alkylene group bonding at the 2-, 2'- or 3-position, A.sub.2 is a C.sub.1 -C.sub.3 alkylene group, A.sub.3 is a C.sub.1 -C.sub.4 alkylene group, X is --O-- or --SO.sub.n -- and B is a carboxy group, a C.sub.2 -C.sub.5 alkoxycarbonyl group, a cyano group, an amino group of the formula: ##STR2## or a carbamoyl group of the formula: ##STR3## which is useful as an antiviral agent with no side effect.
    Type: Grant
    Filed: July 22, 1980
    Date of Patent: August 31, 1982
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Junki Katsube, Hiromi Shimomura, Shun Inokuma, Akihiko Sugie
  • Patent number: 4335122
    Abstract: The invention relates to diuretic dihydro-dibenzoxepines-thiepines and -morphanthridones of the formula ##STR1## wherein R is ##STR2## where R.sup.4 is a hydrogen or an alkyl; R.sup.1 is hydrogen or alkyl; R.sup.2 and R.sup.3 are the same or different and are hydrogen, alkyl or R.sup.2 and R.sup.3 are fused to form a pyrrolidino, morpholino, piperidino or azepino ring substituent; Y is hydrogen, halogen and alkoxy, X is ##STR3## where R.sup.4 is as defined above; m is an integer of 0 or 1; and n is an integer of 2 or 3; and the pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: March 18, 1981
    Date of Patent: June 15, 1982
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Arthur R. McFadden, Daniel E. Aultz
  • Patent number: 4334077
    Abstract: The present invention relates to a process for the preparation of an enantiomer of 7 or 8-fluoro-dibenzo[b,f]thiepin-3-carboxylic acid having a negative rotation and prostaglandin antagonist activity.
    Type: Grant
    Filed: January 28, 1981
    Date of Patent: June 8, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Patrice C. Belanger, Joshua Rokach, Robert N. Young, John Scheigetz
  • Patent number: 4282245
    Abstract: A compound of the formula (I), ##STR1## wherein R.sub.1 represents a halogen atom, or a hydroxy, nitro, amino, trihalogenomethyl or lower alkoxy group having 1 to 5 carbon atoms, and R.sub.2 represents a hydroxy or amino group is an antiinflammatory agent.
    Type: Grant
    Filed: May 23, 1979
    Date of Patent: August 4, 1981
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Yasuo Fujimoto, Shigeru Yamabe
  • Patent number: 4263437
    Abstract: Acetic acid derivatives having the formula, ##STR1## wherein X represents an oxygen or two hydrogen atoms, Y represents CH or N, A represents an oxygen or sulfur atom, and R represents hydroxy, amino or a lower alkoxy group having 1 to 5 carbon atoms possess excellent antiinflammatory activities.
    Type: Grant
    Filed: February 27, 1979
    Date of Patent: April 21, 1981
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Yasuo Fujimoto, Shigeru Yamabe
  • Patent number: 4251526
    Abstract: Novel 2-Benzothiepins, having substituents in the 1-position heretofore unknown, are described. The compounds possess hypotensive and antipsychotic properties; methods and compositions using them are described.
    Type: Grant
    Filed: May 15, 1979
    Date of Patent: February 17, 1981
    Inventor: John M. McCall
  • Patent number: 4247706
    Abstract: A compound of the formula, ##STR1## wherein R represents a hydroxy or amino group is an antiinflammatory and analgesic agent.
    Type: Grant
    Filed: October 12, 1979
    Date of Patent: January 27, 1981
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Yasuo Fujimoto, Shigeru Yamabe
  • Patent number: 4237160
    Abstract: Novel 3-hydroxymethyldibenzo[b,f]thiepin and derivatives are prepared and employed in the treatment and control of allergic conditions such as allergic asthma.
    Type: Grant
    Filed: November 27, 1979
    Date of Patent: December 2, 1980
    Assignee: Merck Sharp & Dohme (I.A.) Corp.
    Inventors: Pierre A. Hamel, Joshua Rokach
  • Patent number: 4207239
    Abstract: Isochromans, isothiochromans, 2-benzoxepins, and 2-benzothiepins are described. These compounds are useful for preparing corresponding amino derivatives that possess antihypertensive and CNS activity.
    Type: Grant
    Filed: January 2, 1979
    Date of Patent: June 10, 1980
    Assignee: The Upjohn Company
    Inventor: John M. McCall
  • Patent number: 4205170
    Abstract: Propionic acid derivatives having the formula ##STR1## wherein X represents an oxygen or two hydrogen atoms, Y represents CH or N, A represents an oxygen or sulfur atom, and R represents hydroxy, amino, or a lower alkoxy group having 1 to 5 carbon atoms are antiinflammatory agents.
    Type: Grant
    Filed: November 28, 1977
    Date of Patent: May 27, 1980
    Assignee: Nippon Chemiphar Company, Limited
    Inventors: Yasuo Fujimoto, Shigeru Yamabe
  • Patent number: 4166062
    Abstract: 1-Alkoxyethanol-isochromas, -isothiochromas, -2-benzoxepins, and -2-benzothiepins are described. These compounds are useful for preparing the corresponding aminoalkoxyalkyl derivatives that possess antihypertensive and CNS activity.
    Type: Grant
    Filed: July 21, 1978
    Date of Patent: August 28, 1979
    Assignee: The Upjohn Company
    Inventors: John M. McCall, Ruth E. TenBrink
  • Patent number: 4166127
    Abstract: Novel benzo [b,f] thiepin derivatives possessing strong anti-flammatory action and presenting few adverse reactions, of the formula (I) ##STR1## wherein R represents a fluorine atom, or a trifluoromethyl or 1-5C lower alkoxy group, and R.sub.3 and R.sub.4 each represent a 1-4C lower alkyl group or R.sub.3 and R.sub.4 together with the adjacent nitrogen atom to which they are attached form a heterocyclic group. Pharmaceutical compositions comprising an anti-inflammatory effective amount of the compound according to formula (I) in the presence of an inert carrier.
    Type: Grant
    Filed: January 16, 1978
    Date of Patent: August 28, 1979
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Shigeru Yamabe, Yasuo Fujimoto, Shoji Ryu, Yoshio Suzuki, Yoshihiro Tanaka, Toru Yamanaka, Kiyosato Nyu