Chalcogen Bonded Directly To The Tricyclo-carbocyclic Ring System Patents (Class 546/204)
  • 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: 5039681
    Abstract: A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from one selected among substituted or unsubstituted benzene, pyridine, pyrazine, indole, anthraquinone, quinoline, substituted or unsubstituted phthalimide, homophthalimide, pyridinecarboxylic acid imide, pyridine N-oxide, pyrazinedicarboxylic acid imide, naphthalenedicarboxylic acid imide, substituted or unsubstituted quinazolinedione, 1,8-naphthalimide, bicyclo [2.2.2] oct-5-ene-2,3-dicarboxylic acid imide and pyromerylimide,X denotes a group of the formula --(CH.sub.2).sub.n --, a group of the formula --O(CH.sub.2).sub.n --, a group of the formula --S(CH.sub.2).sub.n --, a group of the formula --NH(CH.sub.2).sub.n --, a group of the formula --SO.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR2## a group of the formula ##STR3## a group of the formula ##STR4## a group of the formula --CH.sub.2 NH(CH.sub.2).sub.
    Type: Grant
    Filed: February 14, 1990
    Date of Patent: August 13, 1991
    Assignee: Eisai Co., Ltd.
    Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
  • Patent number: 5037821
    Abstract: A method is provided for inhibiting loss of cognitive function, including memory, which may or may not be associated with Alzheimer's disease, in a mammalian species by administering a benzazepine-type or a pyrimidine-type calcium channel blocker such as diltiazem, SQ 31,765, SQ 32,324, SQ 33,351, SQ 33,537 or SQ 32,547 alone or in combination with an ACE inhibitor, such as captopril or SQ 29,852, over a prolonged period of treatment.
    Type: Grant
    Filed: March 27, 1989
    Date of Patent: August 6, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Zola P. Horovitz
  • Patent number: 5021480
    Abstract: Compounds which contain azo linkages as well as a hindered amine light stabilizer moiety of low basicity function as free radical polymerization initiators and provide a polymer containing a hindered amine stabilizer chemically bonded to said polymer. The low basicity of the instant compounds prevents interaction with acid catalysts used in some polymerization systems.
    Type: Grant
    Filed: February 14, 1990
    Date of Patent: June 4, 1991
    Assignee: Ciba-Geigy Corporation
    Inventor: Ramanathan Ravichandran
  • Patent number: 5010105
    Abstract: Compounds of Formula (I) and (II): ##STR1## are HMG-CoA reductase inhibitors.
    Type: Grant
    Filed: May 9, 1990
    Date of Patent: April 23, 1991
    Assignee: Merck & Co., Inc.
    Inventor: Ta J. Lee
  • Patent number: 4996215
    Abstract: A new piperidine compound is pharmacologically effective for treatment of the arrythmia and is defined by the formula: ##STR1## in which R.sup.1 is a lower alkyl or a tolyl, R.sup.2 is hydrogen, hydroxyl, a lower alkoxy or a lower alkyl, R.sup.3 is hydrogen, a lower alkyl, a lower alkenyl, a cycloalkyl or a cycloalkylalkyl, X is --CO--, --CH.sub.2 -- or --CHOH--, g is an integer of 1 to 3, h is an integer of 1 to 3, Y is hydrogen, a lower alkyl, a lower alkenyl, cyano, --CH.sub.2 COOR, R being hydrogen or a lower alkyl, a cycloalkyl, a cycloalkylalkyl, ##STR2## l being 1 or 2, --A--B, A being --(CH.sub.2).sub.
    Type: Grant
    Filed: September 15, 1989
    Date of Patent: February 26, 1991
    Assignee: Eisai Co., Ltd.
    Inventors: Hitoshi Oinuma, Motosuke Yamanaka, Kazutoshi Miyake, Tomonori Hoshiko, Norio Minami, Tadao Shoji, Yoshiharu Daiku, Kohei Sawada, Kenichi Nomoto
  • Patent number: 4994463
    Abstract: Novel tricyclic compounds having a TXA.sub.2 antagonizing activity represented by formula (I): ##STR1## possess a potent antagonizing action against thromboxane A.sub.2 and also an antiallergic and/or antihistaminic activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.
    Type: Grant
    Filed: December 8, 1988
    Date of Patent: February 19, 1991
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii, Hidee Ishii, Kenji Ohmori
  • Patent number: 4972009
    Abstract: Compounds possessing both a hindered amine moiety, such as a derivative of 2,2,6,6-tetramethylpiperidine, and a nitrone moiety are valuable stabilizers for protecting polymer compositions against the deleterious effects of actinic light and from the adverse effects of high temperature polymer processing environments. Additionally, the instant compounds present the opportunity for grafting onto preformed polymer backbones.
    Type: Grant
    Filed: August 18, 1989
    Date of Patent: November 20, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Joseph Suhadolnik, Ramanathan Ravichandran
  • Patent number: 4963538
    Abstract: Novel HMG-CoA reductase inhibitors are useful as antihypercholesterolemic agents and are represented by structural formulae (I) or (II): ##STR1## wherein position 5 of the polyhydronaphthyl ring is singly or doubly bonded to oxygen or incorporated into a C.sub.3-7 carbocyclic ring.
    Type: Grant
    Filed: March 13, 1989
    Date of Patent: October 16, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, George D. Hartman
  • Patent number: 4962102
    Abstract: Fungicidal 4-halogeno-5-nitrothiazoles of the formula ##STR1## in which Hal represents halogen,A represents O, S, SO, SO.sub.2 or N-R.sup.1,whereinR and R.sup.1 each independently is hydrogen or an organic radical, or together withN form a heterocyclic ring,with the exception that R is not hydrogen if A represents SO or SO.sub.2.Compounds of the formula ##STR2## in which Hal' and Hal.sup.1' independently of one another represent chlorine, iodine or fluorine, with the proviso that the two Hals may not simultaneously be chlorine,are also effective in protecting industrial materials against microbes.
    Type: Grant
    Filed: July 12, 1989
    Date of Patent: October 9, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gunther Beck, Wilheim Brandes, Stefan Dutzmann, Wilfried Paulus
  • Patent number: 4950756
    Abstract: 1-Nitroanthraquinone-2-carboxylic acid of the formula I ##STR1## is prepared by treating novel 2-substituted 1-nitroanthraquinones of the general formula II ##STR2## where R is --CH.dbd.CH--R.sup.1 or --CH.sub.2 --CHO, where R.sup.1 is C.sub.1 -C.sub.5 -dialkylamino or a cyclic 5- or 6-membered amine which may contain further hetero atoms, with oxidizing agents free of heavy metal.
    Type: Grant
    Filed: October 30, 1989
    Date of Patent: August 21, 1990
    Assignee: BASF Aktiengesellschaft
    Inventors: Jochem Henkelmann, Helmut Hoch, Thomas-Michael Kahl, Gerhard Kilpper, Walter Maier
  • Patent number: 4942169
    Abstract: A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from one selected among substituted or unsubstituted benzene, pyridine, pyrazine, indole, anthraquinone, quinoline, substituted or unsubstituted phthalimide, homophthalimide, pyridinecarboxylic acid imide, pyridine N-oxide, pyrazinedicarboxylic acid imide, naphthalenedicarboxylic acid imide, substituted or unsubstituted quinazolinedione, 1,8-naphthalimide, bicyclo [2.2.2.] oct-5-ene-2,3-dicarboxylic acid imide and pyromerylimide,X denotes a group of the formula --(CH.sub.2).sub.n --, a group of the formula --O(CH.sub.2).sub.n --, a group of the formula --S(CH.sub.2).sub.n --, a group of the formula --NH(CH.sub.2).sub.n --, a group of the formula --SO.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR2## a group of the formula ##STR3## a group of the formula ##STR4## a group of the formula --CH.sub.2 NH(CH.sub.2).sub.
    Type: Grant
    Filed: March 10, 1989
    Date of Patent: July 17, 1990
    Assignee: Eisai Co., Ltd.
    Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
  • Patent number: 4937259
    Abstract: Compounds of Formula (I) and (II): ##STR1## are HMG-CoA reductase inhibitors.
    Type: Grant
    Filed: June 9, 1989
    Date of Patent: June 26, 1990
    Assignee: Merck & Co., Inc.
    Inventor: Ta Jyh Lee
  • Patent number: 4912222
    Abstract: 4-Dibenzocycloheptenyl, 4-dibenzocycloheptyl, and 4-dibenzoxepinylpiperidine compounds possessing antihistaminic activity.
    Type: Grant
    Filed: June 17, 1988
    Date of Patent: March 27, 1990
    Assignee: Fisons Corporation
    Inventors: Ronald C. Griffith, James J. Napier
  • Patent number: 4904688
    Abstract: The present invention deals with dibenzo-oxocin-, dibenzo-thiocin-, dibenzo-azocin- and dibenzocyclo-octenamine derivatives suitable for use as antipsychotic compounds without extra-pyrimidal side-effects.
    Type: Grant
    Filed: March 8, 1989
    Date of Patent: February 27, 1990
    Assignee: Akzo N.V.
    Inventors: Duncan R. Rae, James Cairns
  • Patent number: 4902787
    Abstract: A method of producing a UV lightfast disperse dyestuff comprising selecting a disperse dyestuff having predetermined chromophoric groups, selecting a photostabilizer compound, designing a hybrid disperse dye molecular structure which contains the chromophoric groups of the selected disperse dyestuff and also contains the molecular structural features of the selected photostabilizer compound, and synthesizing the thus designed hybrid disperse dyestuff molecule. Such a method produces a hybrid dye molecule which is a UV lightfast analog of a disperse dyestuff having predetermined chromophoric groups, said hybrid dye molecule containing in its molecular structure the chromophoric groups of the selected disperse dyestuff and also containing the molecular structural features of a photostabilizer compound.
    Type: Grant
    Filed: April 21, 1988
    Date of Patent: February 20, 1990
    Assignee: North Carolina State University
    Inventor: Harold S. Freeman
  • Patent number: 4898607
    Abstract: 1,5-substituted imidazole derivatives of formula I ##STR1## the stereochemically isomeric forms thereof, and the salts thereof, have useful herbicidal properties. The substituents R.sup.1, R.sup.2, R.sup.3, R.sup.4, X.sup.1, X.sup.2, X.sup.3, A, L and m have the meanings defined herein.
    Type: Grant
    Filed: August 18, 1988
    Date of Patent: February 6, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Henry Szczepanski, Lourens Wals
  • Patent number: 4894451
    Abstract: The disclosure describes unsymmetrical 1,4-bis-(aminoalkylamino)-anthracene-9,10-diones useful in the treatment of neoplasms. Also described is a process of preparing same starting from 1,4-dimethoxyanthracene-9,10-dione which is reacted with an aminoalkylamine. The reaction product is treated with a dialkylaminoethylamine or a N-heteroethylamine to give the unsymmetrical compound.
    Type: Grant
    Filed: July 19, 1988
    Date of Patent: January 16, 1990
    Assignee: The University of Vermont
    Inventors: A. Paul Krapcho, Miles P. Hacker, John J. Landi, Jr., J. J. McCormack, Kenneth J. Shaw
  • Patent number: 4891376
    Abstract: A compound which is a pyrimidinylamino derivative of piperidine of formula (I) ##STR1## in which: X is a (CH.sub.2).sub.2, CH.dbd.CH or CH.sub.2 --CO group;Y is a CH.dbd.CH gruop or sulphur;n is 2, 3 or 4;R.sub.1 is hydrogen or a halogen;R.sub.2 is hydrogen or a (C.sub.1-4) alkyl group; andR.sub.3 is hydrogen or a hydroxy group;or a pharmaceutically acceptable acid addition salt thereof.
    Type: Grant
    Filed: September 8, 1988
    Date of Patent: January 2, 1990
    Assignee: Synthelabo
    Inventors: Philippe Manoury, Alfred Saarmets
  • Patent number: 4863522
    Abstract: A composition comprising(a) a dianthraquinonyl pigment of formula I ##STR1## (b) a compound of formula II ##STR2## wherein X.sup..sym. is H.sup..sym. or a group of formula M.sup.n.sym. /n or N.sup..sym. (R)(R.sub.1)(R.sub.2)(R.sub.3), M.sup.n.sym. is a monovalent metal cation of valency n, n is 1, 2 or 3, each of R, R.sub.1, R.sub.2 and R.sub.3 independently is hydrogen, C.sub.1 -C.sub.18 alkyl, C.sub.5 -C.sub.6 cycloalkyl, phenyl or phenyl which is substituted by C.sub.1 -C.sub.18 alkyl, or R.sub.2 and R.sub.3, together with the linking nitrogen atom, are a pyrrolidine, imidazolidine, piperidine, piperazine or morpholine radical, or R.sub.1, R.sub.2 and R.sub.3, together with the linking nitrogen atom, are a pyrrole, pyridine, picoline, pyrazine, quinoline or isoquinoline radical, r and t are each independently of the other 0 or 1, with the proviso that at least one of r and t must be 1.
    Type: Grant
    Filed: December 22, 1987
    Date of Patent: September 5, 1989
    Assignee: Ciba-Geigy Corporation
    Inventors: Max Jost, Edward E. Jaffe, Philippe Bugnon
  • Patent number: 4849431
    Abstract: A novel piperidine derivative or a pharmacologically acceptable salt thereof is used in the treatment and prevention of dementias and sequelae of cerebrovascular diseases. These compounds also exhibit strong, highly selective anticholinesterase activity and may be orally or parenterally administered.
    Type: Grant
    Filed: December 24, 1986
    Date of Patent: July 18, 1989
    Assignee: Eisai Co., Ltd.
    Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
  • Patent number: 4792551
    Abstract: Compounds useful for treating inflammation, pain and swelling, represented by the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: Y and Z are each independently halo, alkyl or alkoxy;l and m are each independently integers of 0-4;b is an integer of 2-12; andX is selected from the group consisting of:--NR.sup.1 R.sup.2, --NR.sup.1 (CH.sub.2 CH.sub.2 OH), ##STR2## in which R.sup.1 and R.sup.2 are independently H, alkyl or cycloalkyl;R.sup.3 is H, alkyl or CH.sub.2 CH.sub.2 OH; andn is an integer of 3-7.
    Type: Grant
    Filed: July 15, 1983
    Date of Patent: December 20, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Peter H. Nelson, Stefan H. Unger, Thomas R. Thieme
  • Patent number: 4782092
    Abstract: Chemical compounds are provided that are novel 5,8-dichloro-4-hydroxy-1-[(aminoalkyl)amino]-9,10-anthracenediones (I), as well as a method for their production, pharmaceutical compositions comprising the compounds, and methods of treatment using the compounds in dosage form. Compounds of the invention have pharmacological properties and are useful antimicrobial agents and antitumor agents.
    Type: Grant
    Filed: July 3, 1986
    Date of Patent: November 1, 1988
    Assignee: Mid-America Cancer Center
    Inventors: Robert K. Zee-Cheng, Chia C. Cheng
  • Patent number: 4772615
    Abstract: Analogs of nipecotic acid are the novel compounds of the present invention. The analogs are GABA uptake inhibitors for use to treat epilepsy and, thus, the invention is also pharmaceutical compositions and methods of use therefor.
    Type: Grant
    Filed: October 14, 1987
    Date of Patent: September 20, 1988
    Assignee: Warner-Lambert Company
    Inventor: Michael R. Pavia
  • Patent number: 4758577
    Abstract: Novel 4-(5H-dibenzo[a,d]cyclohepten-5-yl)piperidine compounds are disclosed. The compounds have the property of inhibiting calcium induced contraction of the smooth muscle.
    Type: Grant
    Filed: April 5, 1984
    Date of Patent: July 19, 1988
    Assignee: Merck & Co., Inc.
    Inventor: Steven D. Young
  • Patent number: 4731470
    Abstract: The invention relates to novel [(5,6-dichloro-3-oxo-2,9a-alkano--2,3,9,9a-tetrahydro-1H-fluoren-7-yl)oxy] alkanoic acids and alkanimidamides, their derivatives, and their salts. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections including that due to AIDS virus, various brain concussions and elevated intracranial pressure.
    Type: Grant
    Filed: November 3, 1986
    Date of Patent: March 15, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Adolph M. Pietruszkiewicz, Otto W. Woltersdorf, Jr., Edward J. Cragoe, Jr.
  • Patent number: 4731447
    Abstract: A process for the preparation of piperidylidene-dihydro-dibenzo[a,d]cycloheptene or aza-derivatives thereof and intermediates in such process are disclosed.
    Type: Grant
    Filed: March 12, 1986
    Date of Patent: March 15, 1988
    Assignee: Schering Corporation
    Inventors: Doris P. Schumacher, Bruce L. Murphy, Jon E. Clark
  • Patent number: 4731471
    Abstract: The invention relates to novel [(5,6-dichloro-3-oxo-2,3,9,9a-tetrahydrofluoren-7-yl)]alkanoic acids and alkanimidamides bearing novel functional 9a-substituents, their derivatives and their salts. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, the neurological problems caused by AIDS, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections, various brain concussions and elevated intracranial pressure.
    Type: Grant
    Filed: November 3, 1986
    Date of Patent: March 15, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr., Adolph M. Pietruszkiewicz
  • Patent number: 4727072
    Abstract: Propylamines of the formula (I): ##STR1## and isomers thereof, particularly those enantiomers and racemates relative to the chiral carbon indicated by an asterisk (*). The propylamines can be used for the treatment of hypertension or angina in humans. A is pyrrolidine, piperidine or morpholine and B is an aromatic heterocycle, aromatic carbocycle or saturated carbocycle.
    Type: Grant
    Filed: February 12, 1986
    Date of Patent: February 23, 1988
    Assignee: McNeilab, Inc.
    Inventors: Philip P. Grous, Richard J. Mohrbacher
  • Patent number: 4683330
    Abstract: A compound of the formula ##STR1## and intermediates useful in preparing same.
    Type: Grant
    Filed: January 11, 1985
    Date of Patent: July 28, 1987
    Assignee: The Upjohn Company
    Inventor: Paul A. Aristoff
  • Patent number: 4668814
    Abstract: A compound of the formula ##STR1## and intermediates useful in preparing same.
    Type: Grant
    Filed: January 11, 1985
    Date of Patent: May 26, 1987
    Assignee: The Upjohn Company
    Inventor: Paul A. Aristoff
  • Patent number: 4658061
    Abstract: Fluorenes bearing a 9-aminoalkyl substituent are useful antiarrhythmic agents. Pharmaceutical formulations containing such compounds are provided, as well as a method of treatment.
    Type: Grant
    Filed: December 24, 1984
    Date of Patent: April 14, 1987
    Assignee: Eli Lilly and Company
    Inventors: William B. Lacefield, Richard L. Simon
  • Patent number: 4650810
    Abstract: Compounds are disclosed of general formula (I): ##STR1## wherein R.sub.1, R.sub.3, R.sub.4, R.sub.6 and R.sub.7, which may be the same or different, each represents a hydrogen atom or an alkyl group;R.sub.2 represents a hydrogen atom or an alkyl, aryl, aralkyl, cycloalkyl or alkenyl group;or R.sub.1 and R.sub.2, together with the nitrogen atom to which they are attached, form a saturated monocyclic 5 to 7-membered ring which may optionally contain a further hetero function;R.sub.5 represents a hydrogen atom or an alkyl or alkenyl group;or R.sub.4 and R.sub.5 together form an aralkylidene group;Alk represents an alkylene chain containing two or three carbon atoms which may be unsubstituted or substituted by not more than two C.sub.1-3 alkyl groups; andX represents an oxygen or sulphur atom; and physiologically acceptable salts, solvates and bioprecursors thereof.
    Type: Grant
    Filed: January 26, 1983
    Date of Patent: March 17, 1987
    Assignee: Glaxo Group Limited
    Inventors: David E. Bays, Colin F. Webb, Michael D. Dowle
  • Patent number: 4647557
    Abstract: This invention relates to novel heterocyclic derivatives bearing an amino group and to processes for making said compounds.More particularly this invention provides novel heterocyclic compounds the hetero ring of which has two hetero atoms, the same or different, substituted with a free or substituted amino group.These compounds are useful as active ingredients of drugs.
    Type: Grant
    Filed: December 23, 1983
    Date of Patent: March 3, 1987
    Inventors: Gerard Moinet, Michel Schaeffer, Pierre Bessin, Jacqueline Bonnet
  • Patent number: 4609664
    Abstract: Piperidylidene derivatives of formula ##STR1## wherein n is 2 or 3, R.sub.1 comprises a tricyclic nucleus and R.sub.2 is hydrogen or an acid residue, useful in the treatment and prophylaxis of asthmatic conditions.
    Type: Grant
    Filed: July 16, 1984
    Date of Patent: September 2, 1986
    Assignee: Sandoz Ltd.
    Inventor: Klaus Hasspacher
  • Patent number: 4605673
    Abstract: The invention is concerned with 7H-dibenzo(a,c)-cyclohepten-5-one-(7) derivatives of general formula I ##STR1## wherein R.sup.1 and R.sup.2 can be the same or different, a hydrogen atom, an alkyl radical containing 1 to 3 carbon atoms, or, together with the nitrogen atom to which they are attached form a heterocyclic ring containing 3 to 6 carbon atoms,n is 2 or 3R.sup.3 is a hydrogen atom or a halogen atom andX is either a methylene radical or an oxygen atomand the pharmacologically acceptable salts thereof with inorganic and organic acids.The invention is furthermore concerned with analogous processes for the preparation thereof and their application for controlling psychic diseases and gastric and/or intestinal ulcers.
    Type: Grant
    Filed: December 19, 1983
    Date of Patent: August 12, 1986
    Assignee: Warner-Lambert Company
    Inventors: Gerhard Satzinger, Edgar Fritschi, Manfred Herrmann
  • Patent number: 4604396
    Abstract: The invention relates to novel [(2,3,9,9a-tetrahydro-3-oxo-9a-substituted-1H-fluoren-yl)oxy]ethanimidamid es and [(2,3,9,9a-tetrahydro-3-oxo-9a-substituted-1H-fluoren-7-yl)oxy]ethanimidic acid hydrazides, their derivatives and their salts. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections, various brain concussions and elevated intracranial pressure.
    Type: Grant
    Filed: September 26, 1985
    Date of Patent: August 5, 1986
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
  • Patent number: 4599409
    Abstract: The present invention relates to new bisamidine derivatives of polycyclic compounds such as 5,10-dioxo-4,5,9,10-tetrahydro-4,9-dioxapyrene-6(5H)-phenanthridone and 5,10-dioxo-4,5,9,10-tetrahydro-4,9-dioxapyrenephenanthridine and to a process for their preparation. The polycyclic bisamidines according to the invention are distinguished by valuable chemotherapeutic properties, such as, for example, an action against amoebas and trichomonads.
    Type: Grant
    Filed: February 15, 1984
    Date of Patent: July 8, 1986
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Balbir S. Bajwa, deceased, Dipak K. Chatterjee, Bimal N. Ganguli, Jurgen Reden, Noel J. de Souza
  • Patent number: 4459306
    Abstract: This invention relates to novel tricyclic ethers, pharmaceutically acceptable addition salts and optical isomers therefrom. The compounds described herein are useful as psychotropic agents in the treatment of depression and anxiety. Also included herein are methods of preparing said compounds, pharmaceutical compositions including them and methods of treating human or animal beings by administering these pharmaceutical compositions.
    Type: Grant
    Filed: April 6, 1981
    Date of Patent: July 10, 1984
    Assignee: Science Union et Cie
    Inventors: Charles Malen, Jean-Claude Poignant
  • Patent number: 4452745
    Abstract: Fluorenes bearing a 9-aminoalkyl substituent are useful antiarrhythmic agents. Pharmaceutical formulations containing such compounds are provided, as well as a method of treatment.
    Type: Grant
    Filed: September 29, 1982
    Date of Patent: June 5, 1984
    Assignee: Eli Lilly and Company
    Inventors: William B. Lacefield, Richard L. Simon
  • Patent number: 4447368
    Abstract: Aromatic aminosulphonic acids which have a reduced content of discoloring by-products are obtained when aromatic amines are reacted with a sulphonating agent in a reaction medium at least some of which consists of tetramethylene sulphone.
    Type: Grant
    Filed: March 31, 1982
    Date of Patent: May 8, 1984
    Assignee: Siemens-Allis, Inc.
    Inventors: Herbert Emde, Heinz U. Blank, Peter Schnegg
  • Patent number: 4435336
    Abstract: Aminoarylsulphonic acids which have a relatively high purity and a relatively low content of aminoaryldisulphonic acids can be obtained, if they are prepared, from the corresponding arylammonium hydrogen sulphates, by an improved version of the so-called baking process, wherein the reaction is carried out under pressure at a temperature of at least 140.degree. C. and, at least partially, in the presence of water.
    Type: Grant
    Filed: March 31, 1982
    Date of Patent: March 6, 1984
    Assignee: Bayer Aktiengesellschaft
    Inventors: Herbert Emde, Heinz U. Blank, Peter Schnegg
  • Patent number: 4426387
    Abstract: The invention concerns compounds of formula ##STR1## and acid addition and quaternary ammonium salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula ##STR2## in which Q is O,S,--CR.sup.7 .dbd.CR.sup.8 --, --N.dbd.CR.sup.8 -- and --N.dbd.N--; R.sup.4, R.sup.5 and R.sup.6, and R.sup.7 and R.sup.8 when present, each represent hydrogen or defined substituents and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.8 when adjacent, together with the carbon atoms to which they are attached also represent a fused five or six membered carbocyclic or heterocyclic ring optionally carrying one or more defined substituents; R is an optionally substituted aryl or heteroaryl radical or a cycloalkyl radical containing 5 to 7 carbon atoms; R.sup.1, R.sup.2, R.sup.3 and R.sup.9 are each hydrogen or a lower alkyl group; n is 0 or 1; X is .dbd.O, .dbd.S or .dbd.NH; Y is --O-- or a direct bond and Z is --CO-- or --CH.sub.
    Type: Grant
    Filed: April 7, 1982
    Date of Patent: January 17, 1984
    Assignee: John Wyeth & Brother Ltd.
    Inventors: John L. Archibald, Terrence J. Ward
  • Patent number: 4399141
    Abstract: 5-Substituted-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imines, derivatives and pharmaceutically acceptable salts thereof are useful as anticonvulsants.
    Type: Grant
    Filed: June 12, 1981
    Date of Patent: August 16, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Paul Anderson, Marcia E. Christy, Ben E. Evans
  • Patent number: 4374984
    Abstract: Compounds of the formula ##STR1## wherein the substituents A, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, n and m are defined hereinbeloware effective photoinitiators, especially for the photopolymerization of ethylenically unsaturated compounds and for the curing of printing inks.
    Type: Grant
    Filed: March 4, 1981
    Date of Patent: February 22, 1983
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Jurgen Eichler, Claus Herz, Karl-Heinz Neisius, Gregor Wehner
  • Patent number: 4368205
    Abstract: Disclosed are novel compounds of the formula ##STR1## wherein R.sup.1 is a heterocyclic radical selected from furanyl, thienyl, pyridyl, pyrimidyl, oxazolyl, pyrrolyl, isoxazolyl, thiazolyl, and isothiazolyl, and R.sup.2 is hydrogen, a tetramethylcylopropanecarbonyl group, a 1-(substituted-phenyl)-2-methylpropyl-1-carbonyl group, a 1-(4-ethoxyphenyl)-2-dichlorocyclopropanecarbonyl group, or a substituted-vinyl-cyclopropanecarbonyl group. The compounds wherein R.sup.2 is other than hydrogen are insecticides.
    Type: Grant
    Filed: September 17, 1981
    Date of Patent: January 11, 1983
    Assignee: FMC Corporation
    Inventor: John F. Engel
  • Patent number: 4349689
    Abstract: The present specification provides novel analogs of carbacyclin (CBA.sub.2), 6a-carba-prostacyclin (6a-carba-PGI.sub.2), which have pronounced prostacyclin-like pharmacological activity, e.g., as platelet anti-aggregatory agents. Specifically the novel chemical analogs of CBA.sub.2 are those substituted by fluoro (C-5), alkyl (C-9), interphenylene (C-5), and methano (C-6a,9). Further provided are benzindene analogs of CBA.sub.2 and substituted forms thereof, i.e., 9-deoxy-2',9-methano (or 2',9-metheno)-3-oxa-4,5,6-trinor-3,7-(1',3'-interphenylene)-PGF.sub.1 compounds. Also provided are a variety of novel chemical intermediates, e.g., substituted bicyclo[3.3.0]octane intermediates, and chemical process utilizing such intermediates which are useful in the preparation of the novel CBA.sub.2 analogs.
    Type: Grant
    Filed: December 22, 1980
    Date of Patent: September 14, 1982
    Assignee: The Upjohn Company
    Inventor: Paul A. Aristoff
  • Patent number: 4341904
    Abstract: Novel amino derivatives of 2-hydroxy-6,9-methano-11-amino-5,6,7,8,9,10-hexahydro-benzocyclooctenes, methods for their preparation, and their use as effective analgesic agents is described.
    Type: Grant
    Filed: February 19, 1980
    Date of Patent: July 27, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Patrice C. Belanger, Robert N. Young
  • Patent number: 4329469
    Abstract: An optically impure diastereomeric salt is purified by treating a suspension of the salt in an appropriate solvent or solvent mixture with the required amount of the desired, optically pure, acid or base.
    Type: Grant
    Filed: November 24, 1980
    Date of Patent: May 11, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Torleif Utne, Ronald B. Jobson
  • Patent number: 4323691
    Abstract: Described are compounds of the formula ##STR1## wherein ##STR2## wherein Z is hydrogen or loweralkyl, R.sub.5 and R.sub.6 may be the same or different and are hydrogen, loweralkyl or together are alkylene of 4 or 5 carbon atoms,R.sub.2 is hydrogen, halo, haloloweralkyl, loweralkyl, loweralkoxy, loweralkylthio or ##STR3## wherein R.sub.5 and R.sub.6 are previously defined, R.sub.3 is hydroxy, alkoxy, branched alkoxy, adamantyloxy, morpholino, amino or amino substituted by loweralkyl or alkylene of 4 or 5 carbon atoms,R.sub.4 is hydrogen or loweralkyl, andX.sub.1 and X.sub.2 are hydrogen, loweralkyl, halo or when substituted on adjacent carbon atoms of the benzene ring form a 1,3-butadienylene linkage, Y is oxygen or sulfur, and pharmaceutically acceptable salts thereof. The compounds are effective as diuretic agents in increasing urinary excretion.
    Type: Grant
    Filed: December 1, 1980
    Date of Patent: April 6, 1982
    Assignee: Abbott Laboratories
    Inventors: Carroll W. Ours, Cheuk M. Lee