Bicyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 544/376)
  • Patent number: 4544667
    Abstract: Novel 2-sulfamoylbenzo[b]furans and derivatives thereof are shown to be useful for the treatment of elevated intraocular pressure in compositions including opthalmic drops and inserts.
    Type: Grant
    Filed: February 9, 1984
    Date of Patent: October 1, 1985
    Assignee: Merck & Co., Inc.
    Inventors: Kenneth L. Shepard, Samuel L. Graham
  • Patent number: 4540801
    Abstract: The present invention relates to 5-fluoro-PGI.sub.2 derivatives of Formula I. These compounds are useful for the treatment of platelet dysfunction. Also disclosed is the process for preparing them and the appropriate intermediates.
    Type: Grant
    Filed: July 13, 1983
    Date of Patent: September 10, 1985
    Assignee: G. D. Searle & Co.
    Inventors: Leonard N. Nysted, Raphael Pappo
  • Patent number: 4529729
    Abstract: Piperazine and homopiperazine compounds of the formula: ##STR1## in which: A is a hydrocarbon radical from C.sub.3 to C.sub.5, in a straight or branched chain, which may contain one or two double bonds, and optionally substituted by one or more OH;B is CH or a nitrogen atom;m is 2 or 3;X--Y-- represents --CH.dbd.CH--(CR'R").sub.n - in which n is zero or 1, and R' and R" are hydrogen or methyl;Z is oxygen or sulfur,R is hydrogen, alkyl from C.sub.1 to C.sub.5, cycloalkyl from C.sub.3 to C.sub.7, or phenyl optionally substituted by fluorine, chlorine or alkyl from C.sub.1 to C.sub.5, andT is hydrogen, fluorine, chlorine or alkyl from C.sub.1 to C.sub.5.These compounds and physiologically tolerable acid addition salts thereof may be used as medicines especially in the treatment of all kinds of tissular hypoxia.
    Type: Grant
    Filed: June 20, 1984
    Date of Patent: July 16, 1985
    Assignee: Adir
    Inventors: Gilbert Regnier, Michel Laubie, Jacques Duhault
  • Patent number: 4515793
    Abstract: A compound of the formula ##STR1## in which A is ##STR2## n is 1, 2 or 3, and R is phenyl optionally substituted with halogen, alkyl, phenyl, cyano, hydroxy, alkoxy, mercapto, sulfinyl, sulfonyl, amino, nitro, trifluoromethyl and/or naphthyl radicals; or a furan, thiophene, pyridine, benzofuran, dibenzothiophene or thianthrene radical,or a pharmacologically acceptable salt thereof, for treating schistosomiasis.
    Type: Grant
    Filed: July 27, 1983
    Date of Patent: May 7, 1985
    Assignee: Edna McConnell Clark Foundation
    Inventors: Leslie M. Werbel, Norman Colbry, William Turner, Donald F. Worth
  • Patent number: 4507292
    Abstract: Aryl N-oxalyl-N-methyl-carbamates of the general formula ##STR1## in which X represents an alkoxy, alkenoxy, alkinoxy, aryloxy, alkylthio, alkenylthio, alkinylthio or arylthio radical, each of which may be optionally substituted, or represents a radical of the general formula --N R.sup.3 R.sup.4, wherein R.sup.3 and R.sup.4 are identical or different and represent a hydrogen atom or an alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl or aryl radical, each of which may be optionally substituted,or the radicals R.sup.3 and R.sup.4, together with the N atom to which they are bonded, form an optionally substituted heterocyclic ring, andR.sup.1 represents an aryl radical which is optionally substituted,are novel and find use as pesticides, especially for combating insects, acarids and nematodes.
    Type: Grant
    Filed: January 27, 1983
    Date of Patent: March 26, 1985
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gerhard Heywang, Engelbert Kuhle, Wolfgang Behrenz, Ingeborg Hammann, Bernhard Homeyer
  • Patent number: 4496565
    Abstract: Compounds of formula (I): ##STR1## a pharmaceutically acceptable salt or solvate thereof having anti-hypertensive activity, a process for their preparation and their use as pharmaceuticals.
    Type: Grant
    Filed: October 17, 1983
    Date of Patent: January 29, 1985
    Assignee: Beecham Group p.l.c.
    Inventors: John M. Evans, Valerie A. Ashwood
  • Patent number: 4487774
    Abstract: Amino derivatives of isochromans are described. These compounds exhibit antipsychotic and hypotensive activity.
    Type: Grant
    Filed: April 21, 1982
    Date of Patent: December 11, 1984
    Assignee: The Upjohn Company
    Inventor: John M. McCall
  • Patent number: 4486428
    Abstract: Bicyclic fused benzenoid compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, where M is O, CH.sub.2 or NR.sub.6 ; R.sub.6 is hydrogen, formyl, carbobenzyloxy or certain carboalkoxyalkyl, alkanoyl, alkyl, aralkyl or aralkylcarbonyl groups;A' is:(1) A where one of A and B is hydrogen such that when A is hydrogen, B is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 1 or 2; when B is hydrogen, A is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 0 or 1, when taken together A and OR.sub.1 form a lactone or certain derivatives thereof;(2) A' is ##STR2## (3) A' is Q.sub.3 ; Q is CO.sub.2 R.sub.7, COR.sub.8, C(OH)R.sub.8 R.sub.9, CN, CONR.sub.12 R.sub.13, CH.sub.2 NR.sub.12 R.sub.13, CH.sub.2 NHCOR.sub.14, CH.sub.2 NHSO.sub.2 R.sub.17 or 5-tetrazoyl;Q.sub.3 is ##STR3## 5-tetrazolyl, CH.sub.2 CONHCOR.sub.7, COOH or certain ester, amide, carboximido or sulfonimido derivatives thereof, CONHOH, CONHCONH.sub.2, or COCH.sub.2 Q.sub.4 where Q.sub.
    Type: Grant
    Filed: January 13, 1983
    Date of Patent: December 4, 1984
    Assignee: Pfizer Inc.
    Inventors: James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
  • Patent number: 4474783
    Abstract: A compound having the formula ##STR1## in which R is hydrogen or alkyl having 1 to 4 carbon atoms; R.sub.1 is hydrogen, alkyl having 1 to 5 carbon atoms, cycloalkylmethyl in which the cycloalkyl group has from 3 to 6 carbon atoms, 2-hydroxyethyl, alkoxycarbonyl in which the alkoxy group has 1 or 2 carbon atoms, 2-carboxypropyl, N-benzyl-2-carbamoyl propyl, phenyl, phenyl substituted by methoxy, trifluoromethyl or acetyl, benzyl, benzyl substituted by halogen, benzoyl, benzoyl substituted by three methoxy groups, 3,5-dimethoxy-4-acetoxy or 3,5-dimethoxy-4-ethoxycarbonyloxy, cinnamoyl, cinnamoyl in which the phenyl ring is substituted with trifluoromethyl or by one or more methoxy groups, phenoxyacetyl, phenoxyacetyl in which the phenyl ring is substituted with halogen or methoxy, and ##STR2## in which m is 2 or 3 and R.sub.2 and R.sub.
    Type: Grant
    Filed: September 25, 1981
    Date of Patent: October 2, 1984
    Assignee: Innothera
    Inventors: Max F. Robba, Michel E. Aurousseau
  • Patent number: 4469694
    Abstract: 2-(1-Piperazinyl)-2,4,6-cycloheptatrien-1-one derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives are disclosed. The derivatives exhibit dopamine-receptor stimulating activity in a mammal and are useful for treating hyperprolactinemia, galactorrhea, amenorrhea, impotence, Parkinsonism, diabetes, acromegaly, hypertension and other central nervous system disorders.
    Type: Grant
    Filed: February 25, 1980
    Date of Patent: September 4, 1984
    Assignee: Ayerst, McKenna & Harrison Inc.
    Inventors: Jehan F. Bagli, Tibor Bogri, Katherine Voith
  • Patent number: 4463185
    Abstract: The present invention provides novel 1-(6-hydroxy-4- or 7-methoxy or 4,7-dimethoxy-5-benzofuranyl)-4-substituted-1,3-butanediones which are useful as intermediates in the synthesis of khellin and related anti-atherosclerotic furochromones.
    Type: Grant
    Filed: July 30, 1982
    Date of Patent: July 31, 1984
    Assignee: The Upjohn Company
    Inventor: Ronald B. Gammill
  • Patent number: 4447620
    Abstract: The present invention provides novel imidazolyl-benzothiophenes and derivatives thereof which are useful as thromboxane A.sub.2 (TXA.sub.2) synthetase inhibitors and as such represent potent pharmacological agents.
    Type: Grant
    Filed: October 12, 1982
    Date of Patent: May 8, 1984
    Assignee: The Upjohn Company
    Inventors: John C. Sih, Chiu-Hong Lin
  • Patent number: 4447622
    Abstract: The laevo and dextro forms of dl-3,4-trans-2,2-disubstituted-3,4-diarylchromans and similar derivatives thereof have substantially double the post-coital anti-fertility activity of the known racemic compound. The resolution of such known compound into the l- and d-isomeric forms may be carried out using di-p-toluoyl-l-tartaric acid monohydrate or di-p-toluoyl-d-tartaric acid.
    Type: Grant
    Filed: September 22, 1981
    Date of Patent: May 8, 1984
    Assignee: Council of Scientific and Industrial Research Rafi Marg
    Inventors: Mohammad Salman, Suprabhat Ray, Ved P. Kamboj, Nitya Anand
  • Patent number: 4436921
    Abstract: A 1-(4-aminobenzyl)-2,3-dioxopiperazine derivative represented by the formula: ##STR1## and an acid addition salt thereof have excellent carcinostatic activity but a low toxicity. Therefore, said compounds are useful as medicines and also as intermediates.
    Type: Grant
    Filed: July 16, 1980
    Date of Patent: March 13, 1984
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Takako Hori, Chosaku Yoshida, Yasuo Kiba, Ryuko Takeno, Joji Nakano, Jun Nitta, Sumiko Kishimoto, Shohachi Murakami, Hisatsugu Tsuda, Isamu Saikawa
  • Patent number: 4435397
    Abstract: 4-(3-Aryloxy-2-hydroxypropyl)piperazines bearing a carbamyl group in the 1-position are .beta.-adrenergic blockers. A typical example is 1-carbamyl-4-{3-[2-allyl-3-(2-carbethoxyaminoethyl)phenoxy]-2-hydroxypropy l}piperazine.
    Type: Grant
    Filed: March 26, 1981
    Date of Patent: March 6, 1984
    Assignee: Nippon Shinyaku Co., Ltd.
    Inventors: Shingo Matsumura, Hiroshi Enomoto, Yoshiaki Aoyagi, Haruo Tanaka
  • Patent number: 4430341
    Abstract: Water soluble quaternary ammonium salt compounds exhibit outstanding insecticidal and miticidal activity coupled with reduced mammalian toxicity and acceptable phytotoxicity.
    Type: Grant
    Filed: August 24, 1977
    Date of Patent: February 7, 1984
    Assignee: Union Carbide Corporation
    Inventor: Barbara W. Kaplan
  • Patent number: 4426380
    Abstract: The invention relates to novel furans, especially benzofuranones of the general formula ##STR1## in which R.sub.1 represents hydrogen or an aliphatic radical, R.sub.2 represents an amino group di-substituted by a divalent hydrocarbon radical, and the aromatic ring A may be additionally substituted, and their salts and/or isomers, processes for the manufacture of compounds of the formula (I) and their salts and isomers, pharmaceutical preparations containing these compounds, and their use as the active ingredients of medicaments as anti-inflammatory agents, analgesics or light-screening agents and/or for the manufacture of pharmaceutical preparations.
    Type: Grant
    Filed: October 21, 1982
    Date of Patent: January 17, 1984
    Assignee: Ciba-Geigy Corporation
    Inventors: Paul Wenk, Werner Breitenstein, Marcus Baumann
  • 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: 4383995
    Abstract: This invention relates to the derivatives of the following formula: ##STR1## in which R, R', R.sub.1, R.sub.2 are hydrogen atoms or hydrocarbonated radicals, and X is an oxo, hydroxy, imino or aminal radical.These compounds have anti-fibrillating activity.
    Type: Grant
    Filed: November 4, 1981
    Date of Patent: May 17, 1983
    Inventors: Bernard Delbarre, Louis Mavoungou-Gomes
  • Patent number: 4382935
    Abstract: The drug contains an active substance consisting of 1-(3'-benzofuryl)-4-benzylpiperazine. In order to prepare the compound, a reaction is carried out with reflux between 3-coumaranone and N-benzylpiperazine in the presence of acetic acid and in an aromatic solvent.
    Type: Grant
    Filed: January 29, 1981
    Date of Patent: May 10, 1983
    Assignees: Andre Buzas, Jean-Marie Melon, Laboratoires Sauba S.A., Universite d'Orleans
    Inventors: Andre Buzas, Jean-Marie Melon, Gilbert Lavielle, Andre Champagnac
  • Patent number: 4374990
    Abstract: A compound having the general formula or an acid addition salt thereof ##STR1## in which formula R.sub.1 is selected from the group consisting of(A) an at least mononuclear heterocyclic group having 4 to 10 carbon atoms in the ring system bound to the group ##STR2## through a carbon atom and containing at least one oxygen, nitrogen or sulphur atom,(B) substitution products of (A) containing at least one substituent selected from the group consisting of halogen, trifluoromethyl, hydroxy, alkoxy of 1 to 3 carbon atoms, unsubstituted amino, amino substituted by up to two alkyl groups each having 1 to 3 carbon atoms and alkyl groups having 1 to 6 carbon atoms,X is oxygen, sulphur or an NH-group,Y is an alkylene group having 1 to 3 carbon atoms in the chain, or an alkylene group having 1 to 3 carbon atoms in the chain substituted by (a) up to 3 alkyl groups each having up to 3 carbon atoms and a total of not more than 8 carbon atoms, or (b) substituted by one or two phenyl groups,R.sub.
    Type: Grant
    Filed: October 26, 1979
    Date of Patent: February 22, 1983
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Rolf-Ortwin Weber, Alfons Soder, Istvan Boksay
  • Patent number: 4367237
    Abstract: Prostaglandin analogues of the general formula: ##STR1## [wherein the ring A represents: ##STR2## the ring B represents: ##STR3## (wherein R.sup.6 represents hydrogen, methyl or ethyl, and r is zero, one or two), Y represents ethylene, cis- or trans-vinylene or ethynylene, Z represents a grouping of the formula: --(CH.sub.2).sub.m --, --(CH.sub.2).sub.3 --CHR.sup.7 --, --(CH.sub.2).sub.2 --CHR.sup.7 --CH.sub.2 --, --CH.sub.2 --CHR.sup.7 --(CH.sub.2).sub.2 --, --CHR.sup.7 --(CH.sub.2).sub.3 --, or trans--(CH.sub.2).sub.2 --CH.dbd.CH-- (wherein m is 3, 4 or 5, and R.sup.7 represents methyl or ethyl), R.sup.1 represents a grouping of the formula: --COOR.sup.8, ##STR4## or --CH.sub.2 OR.sup.11 (wherein R.sup.8 represents hydrogen, alkyl, aralkyl, cycloalkyl which is unsubstituted or substituted by at least one alkyl group, or R.sup.
    Type: Grant
    Filed: November 27, 1979
    Date of Patent: January 4, 1983
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Hirohisa Wakatsuka, Katsuichi Shimoji, Sadahiko Iguchi, Yoshitaka Konishi, Hisashi Suga, Yasuyuki Miyata, Yoichi Iguchi, Hajimu Miyake, Masaki Hayashi
  • Patent number: 4362740
    Abstract: New spiro compounds of the formula: ##STR1## wherein n is an integer of 1 to 4, and X is halogen, lower alkyl, nitro, amino which may be substituted, hydroxyl which may be substituted, acyl, carboxyl, lower alkoxycarbonyl, carbamoyl which may be substituted, sulfamoyl which may be substituted, lower alkylthio or lower alkylsulfonyl, or two of X at the 5- and 6-positions together form --CH.dbd.CH--CH.dbd.CH--, exhibit inhibitory activity to thrombocyte aggregation and are useful for the prophylaxis or treatment of cardiovascular disturbance such as thrombosis.
    Type: Grant
    Filed: September 19, 1980
    Date of Patent: December 7, 1982
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Isuke Imada, Hirosada Sugihara, Mitsuru Kawada
  • Patent number: 4358450
    Abstract: Compounds of general formula ##STR1## wherein R.sup.1 represents a member selected from the group consisting of (a) an unsubstituted at most binuclear aryl group having from 6 to 10 carbon atoms, such groups substituted by from 1 to 3 equal or different radicals selected from the group consisting of alkyl, halogenoalkyl, alkoxy, dialkylamino each having up to 4 carbon atoms in the alkyl moiety, halogen phenyl, carboxyl, cyano, nitro and hydroxy groups,(b) a 5- to 6-membered heteroaromatic ring wherein the heteroatom is selected from nitrogen, oxygen and sulfur atoms and such rings anellated to a benzene nucleus;R.sup.2 represents a member selected from the group consisting of hydrogen, alkyl having up to 3 carbon atoms, phenyl, cycloalkyl having up to 6 carbon atoms in the ring and cycloalkyl bearing a hydrocarbon bridging radical having up to 2 carbon atoms;R.sup.3 represents hydrogen, hydroxy or acyloxy;R.sup.4 and R.sup.
    Type: Grant
    Filed: August 6, 1979
    Date of Patent: November 9, 1982
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ulrich Gebert, Ernold Granzer, Heinz-Gunter Greve, Werner Thorwart
  • Patent number: 4352808
    Abstract: 3-Aralkyloxy-2,3-dihydro-2-(imidazolylmethyl(benzo(b)thiophenes and related derivatives having antifungal, antibacterial, and antiprotozoal activity are prepared by the reaction of the corresponding 2,3-dihydro-3-hydroxy-2-(imidazolylmethyl)benzo(b)thiophene or related derivative and an aralkyl halide.Preferred compounds are those where the aralkyl function is a hetercyclic aromatic, particularly 2-chloro-3-thenyl, and where the benzene nucleus is substituted by chlorine or fluorine.Pharmaceutical formulations comprising compounds of this invention are described, as well as the method for their use in treating microbial infections.
    Type: Grant
    Filed: December 12, 1980
    Date of Patent: October 5, 1982
    Assignee: Schering Corporation
    Inventors: Dinanath F. Rane, John J. Wright, Russell E. Pike
  • Patent number: 4339450
    Abstract: Derivatives of 1-aminopropan-2-o1 which are useful in the treatment and control of cardiac disorders in warm-blooded mammals. The process of manufacture and pharmaceutical compositions.
    Type: Grant
    Filed: December 22, 1980
    Date of Patent: July 13, 1982
    Assignee: Sanofi
    Inventors: Jean P. Mafrand, Jean Courregelongue
  • Patent number: 4337338
    Abstract: The present invention provides 2,5-inter-o-phenylene-3,4-dinor-5,9.alpha.-epoxy-6-iodo-PGF.sub.1 amides. These compounds are intermediates for preparing 2,5-inter-o-phenylene-3,4-dinor-prostacyclin analogs, which are useful for pharmacological purposes, e.g., as antithrombotic agents.
    Type: Grant
    Filed: July 3, 1980
    Date of Patent: June 29, 1982
    Assignee: The Upjohn Company
    Inventors: Udo F. Axen, John C. Sih
  • Patent number: 4337203
    Abstract: The present invention provides 2,5-inter-o-phenylene-3,4-dinor-5,9.alpha.-epoxy-PGF.sub.1 amides. These compounds are useful for a wide variety of pharmacological and therapeutical purposes, e.g., as antithrombotic agents.
    Type: Grant
    Filed: July 3, 1980
    Date of Patent: June 29, 1982
    Assignee: The Upjohn Company
    Inventors: Udo F. Axen, John C. Sih
  • Patent number: 4334067
    Abstract: A flavan compound represented by the formula (I) ##STR1## wherein R, R.sub.1, R.sub.2 and R.sub.3 are as defined above, and the pharmaceutically acceptable acid addition salt thereof, which are useful as pharmaceutical agent having anti-convulsive, anti-ulcer, anti-arrythmic and diuretic activities.
    Type: Grant
    Filed: October 29, 1980
    Date of Patent: June 8, 1982
    Assignee: Maruko Seiyaku Co., Ltd.
    Inventors: Sachio Ohno, Mitsuaki Nagasaka, Kazuo Kato
  • Patent number: 4329357
    Abstract: 2,3-Dihydro-1-benzothiepin-4-carboxamides, e.g. those of the formula ##STR1## Am=arylamino or N-alkyl-N-arylamino substituted by R X=HO, alkoxy, alkanoyloxy or alkyleneiminoR=alkyl, alkoxy, alkylmercapto, halo, CF.sub.3, CN, or NO.sub.2n=0-2or their salts with therapeutically useful bases, exhibit anti-inflammatory effects.
    Type: Grant
    Filed: February 9, 1981
    Date of Patent: May 11, 1982
    Assignee: Ciba-Geigy Corporation
    Inventor: Melvin H. Rosen
  • Patent number: 4328227
    Abstract: Compounds of general formula ##STR1## wherein R.sup.
    Type: Grant
    Filed: May 19, 1980
    Date of Patent: May 4, 1982
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gebert Ulrich, Werner Thorwart, Jaromir Komarek, Carl Cartheuser, Kurt Popendiker, Heinz-Gunther Greve
  • Patent number: 4321270
    Abstract: The invention relates to chroman derivatives of the general formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, substituted phenyl, phenyl, phenyl-lower alkyl, substituted phenyl-lower alkyl or lower alkyl-amino-lower alkyl;R.sub.2 is ##STR2## R.sub.3, R.sub.4, R.sub.5 and R.sub.6 each is independently selected from hydrogen, hydroxy, amino, -o-acyl, -o-lower alkyl; ##STR3## halogen, lower alkyl, or halo substituted lower alkyl; and salts and hydrates thereof.These compounds are useful as anti-inflammatory agents; for inhibition of blood platelet aggregation, as antiallergy and as antihypertensive agents.
    Type: Grant
    Filed: January 29, 1981
    Date of Patent: March 23, 1982
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Joseph E. Sundeen
  • Patent number: 4320128
    Abstract: Compounds of the formula (II): ##STR1## and pharmaceutically acceptable acid-addition salts thereof wherein Ar is a pyridyl or optionally substituted phenyl group of the sub-formula --C.sub.6 H.sub.3 R.sub.1 R.sub.2 wherein R.sub.1 is a hydrogen, fluorine, chlorine or bromine atom or a lower alkyl, lower alkoxyl, lower acyl, lower acyloxyl or lower alkoxycarbonyl group; and R.sub.2 is a hydrogen, fluorine or chlorine atom or a lower alkyl or lower alkoxy group having useful anti-hypertension activity, their preparation, and pharmaceutical compositions containing them.
    Type: Grant
    Filed: March 17, 1980
    Date of Patent: March 16, 1982
    Assignee: Beecham Group Limited
    Inventor: Charles S. Fake
  • Patent number: 4313877
    Abstract: The present invention provides novel thromboxane analogs and intermediates. Particularly, the present invention provides novel 11a-methano-TXA.sub.2 amides.
    Type: Grant
    Filed: January 28, 1980
    Date of Patent: February 2, 1982
    Assignee: The Upjohn Company
    Inventor: Gordon L. Bundy
  • Patent number: 4312810
    Abstract: This invention relates to certain structural and pharmacological analogs of prostacyclin (PGI.sub.2) and 5,6-dehydroprostacyclin (PGI.sub.1) and 5,9.alpha.-epoxy-9-deoxy-PGF.sub.1, wherein between the position beta to the carboxy (C-2) and C-5 there is substituted an inter-o-phenylene for the ethylene chain. These novel 2,5-inter-o-phenylene-3,4-dinor-prostaglandin or prostacyclin-type compounds are useful for certain of the same pharmacological purposes as prostacyclin, particularly being smooth muscle stimulators, blood pressure depressors and platelet aggregation inhibitors. Also provided are novel intermediates therefor, namely corresponding interphenylene-containing PGF.sub.2.alpha. and 5-halo-PGI.sub.1 and 6-halo-5,9.alpha.-epoxy-9-deoxy-PGF.sub.1 compounds.
    Type: Grant
    Filed: July 31, 1979
    Date of Patent: January 26, 1982
    Assignee: The Upjohn Company
    Inventors: Udo F. Axen, John C. Sih
  • Patent number: 4302466
    Abstract: 2,3-Dihydro-2,2-dimethyl-7-benzofuranyl N-carboxylated-N-methyl-carbamates of the formula ##STR1## in which R is alkoxy with 1-10 C atoms, alkenoxy or alkynoxy with 5-7 C atoms each optionally substituted by halogen or by a radical of the formula--X--R.sup.1 or --NR.sup.2 R.sup.3 ; or NR.sup.2 R.sup.3 ;X is an oxygen or sulphur atom or a sulphoxide or sulphone group,R.sup.1 is hydrogen or alkyl with 1-4 C atoms,R.sup.2 and R.sup.3 independently is hydrogen, alkyl radical with 1-18 C atoms, alkenyl with up to 8 C atoms, or together are ##STR2## and W is hydrogen or alkyl wth 1-4 C atoms,which possess arthropodicidal and nematocidal properties.
    Type: Grant
    Filed: July 2, 1980
    Date of Patent: November 24, 1981
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gerhard Heywang, Alfons Hartmann, Ingeborg Hammann, Bernhard Homeyer
  • Patent number: 4299959
    Abstract: A fluorescent pigment consisting of N-substituted iminocoumarins of the general formula I, ##STR1## wherein X.sub.1 is a cyano group, a carboxamido group or an aryl or a heteroaryl radical linked directly or through a --CO or --SO.sub.2 group,X.sub.2 is an amino group, hydroxy group or an alkoxy group and when it is an amino group, may carry an optionally substituted alkylene or alkylidene group bound in ortho position to the nitrogen atom and in para position with respect to the coumarin oxygen atom,X.sub.3 is a hydrogen atom, a halogen atom or a cyano group andX.sub.4 is a functionally converted carboxyl groups. The new dyestuffs dye polyester fiber in orange or red shades with good fastness.
    Type: Grant
    Filed: January 31, 1979
    Date of Patent: November 10, 1981
    Assignee: Ciba-Geigy Corporation
    Inventor: Nalin B. Desai
  • Patent number: 4288437
    Abstract: Compounds of the formula ##STR1## wherein Ar is phenyl; mono- or di-substituted phenyl, where the substituents are one to two halogens, one to two alkyls of 1 to 3 carbon atoms, or one amino, nitro, cyano or trifluoromethyl; or pyridinyl;R is hydrogen, chlorine, methyl or methoxy;R.sub.1 is hydrogen or methyl;R.sub.2 is hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, methyl-(cycloalkyl of 3 to 8 carbon atoms) or --A--R.sub.4,where A is alkylene of 2 to 3 carbon atoms, and R.sub.4 is hydroxyl, methylamino, dimethylamino, N-methyl-ethylamino, diethylamino, pyrrolidino, piperidino, hexamethyleneimino, morpholino or 4-methyl-1-piperazinyl; orR.sub.1 and R.sub.
    Type: Grant
    Filed: July 28, 1980
    Date of Patent: September 8, 1981
    Assignee: Boehringer Ingelheim GmbH
    Inventors: Wolfhard Engel, Gunter Trummlitz, Ernst Seeger, Joachim Kahling
  • Patent number: 4285966
    Abstract: The present invention relates to 15-epi-derivatives of prostacyclin and its analogs, to a process for their preparation and to pharmaceutical and veterinary compositions containing them.
    Type: Grant
    Filed: October 30, 1978
    Date of Patent: August 25, 1981
    Assignee: Farmitalia Carlo Erba, S.p.A.
    Inventors: Carmelo Gandolfi, Carlo Passarotti, Alessandro Andreoni, Angelo Fumagalli, Franco Faustini, Roberto Cesarani
  • Patent number: 4284644
    Abstract: Novel spiro compounds of the formula: ##STR1## wherein Ring A represents a benzene ring or a naphthalene ring, said rings being unsubstituted or substituted by at least one of lower alkyl, nitro, halogen, amino which may optionally be substituted, hydroxyl which may optionally be substituted, acyl, sulfamoyl, carboxyl, lower alkoxycarbonyl, carbamoyl which may optionally be substituted, ureido which may optionally be substituted, thioureido which may optionally be substituted, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, aminomethyl which may optionally be substituted, cyano and phenyl, have gastric secretion inhibitive, anti-inflammatory and analgesic activities, and are of value as drugs.
    Type: Grant
    Filed: January 25, 1980
    Date of Patent: August 18, 1981
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirosada Sugihara, Masazumi Watanabe, Mitsuru Kawada, Isuke Imada
  • Patent number: 4281014
    Abstract: Insecticidal compositions containing N-aminosulfenyl derivatives of carbofuran are stabilized against spontaneous decomposition by incorporating an epoxide compound therein.
    Type: Grant
    Filed: June 4, 1980
    Date of Patent: July 28, 1981
    Assignee: FMC Corporation
    Inventor: Jerome Yaffe
  • Patent number: 4279905
    Abstract: Novel, 3-amino-1-benzoxepin-5 (2H)-one derivatives and methods for their production are disclosed. These derivatives correspond to the Formula I: ##STR1## wherein: R.sub.1 and R.sub.2 independently of one another arehydrogen,C.sub.1 -C.sub.5 alkyl,C.sub.1 -C.sub.5 alkyl substituted with a terminal phenyl, or a phenyl containing one or two halogens, methyl or methoxy groups, a 3,4-methylenedioxy or a 3,4-ethylenedioxy group,C.sub.2 -C.sub.5 alkyl substituted with terminal hydroxy or methoxy or,C.sub.3 -C.sub.4 alkenyl; orone of R.sub.1 and R.sub.2 are hydrogen or a C.sub.1 -C.sub.5 alkyl and the other is a C.sub.2 -C.sub.5 alkyl substituted with a terminal NR.sub.5 R.sub.6 ;R.sub.5 and R.sub.6 independently of one another are hydrogen or C.sub.1 -C.sub.5 alkyl; orR.sub.5 and R.sub.6 are together a 5 to 7 member ring, orR.sub.5 and R.sub.6 are together a 5 to 7 member ring having heterogeneous oxygen, sulfur or nitrogen;R.sub.1 and R.sub.2 are together a 5 to 7 member ring, orR.sub.1 and R.sub.
    Type: Grant
    Filed: July 28, 1980
    Date of Patent: July 21, 1981
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Heinrich-Wilhelm Ohlendorf, Klaus-Ullrich Wolf, Wilhelm Kaupmann
  • Patent number: 4279904
    Abstract: Novel 3-amino-1-benzoxepine derivatives and methods for their production are disclosed. These derivatives correspond to the Formula I ##STR1## wherein: R.sub.1 and R.sub.2 independently of one another arehydrogen,C.sub.1 -C.sub.5 alkyl,C.sub.1 -C.sub.5 alkyl substituted with a terminal phenyl, or a phenyl containing one or two halogens, methyl or methoxy groups, a 3,4-methylenedioxy or a 3,4-ethylenedioxy group,C.sub.2 -C.sub.5 alkyl substituted with terminal hydroxy or methoxy or,C.sub.3 -C.sub.4 alkenyl; orone of R.sub.1 and R.sub.2 are hydrogen or a C.sub.1 -C.sub.5 alkyl and the other is a C.sub.2 -C.sub.5 alkyl substituted with a terminal NR.sub.7 R.sub.8 ;R.sub.7 and R.sub.8 independently of one another are hydrogen or C.sub.1 -C.sub.5 alkyl; orR.sub.7 and R.sub.8 are together a 5 to 7 member ring or said ring having heterogeneous oxygen, sulfur or nitrogen, orR.sub.1 and R.sub.2 are together a 5 to 7 member ring or said ring having heterogeneous oxygen, sulfur or NR.sub.9 ;R.sub.
    Type: Grant
    Filed: July 28, 1980
    Date of Patent: July 21, 1981
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Heinrich-Wilhelm Ohlendorf, Klaus-Ullrich Wolf, Wilhelm Kaupmann, Henning Heinemann
  • Patent number: 4277474
    Abstract: New propanone derivatives, useful for treating allergic diseases, the pharmacologically allowable salts thereof, their manufacturing process and pharmaceutical composition containing at least one of them as the active ingredient.
    Type: Grant
    Filed: September 27, 1979
    Date of Patent: July 7, 1981
    Assignee: Nippon Zoki Pharmaceutical Co., Ltd.
    Inventors: Akihide Kohda, Teikichi Kurosaki
  • Patent number: 4276294
    Abstract: 1-(2-phenyl-3-benzofuryl)-piperazines, e.g. those of the formula ##STR1## R=H, alkyl or halo R', R"=H, alkyl, alkoxy, alkylenedioxy, alkylthio or haloR.degree.=H, alkyl or hydroxyalkyln=2 or 3acyl derivatives, quaternaries and salts thereof are anticonvulsants.
    Type: Grant
    Filed: March 31, 1980
    Date of Patent: June 30, 1981
    Assignee: Ciba-Geigy Corporation
    Inventor: Robert M. Bowman
  • Patent number: 4263299
    Abstract: A compound of formula (I): ##STR1## and pharmaceutically acceptable salts thereof, wherein R is hydrogen or an alkyl group containing up to 6 carbon atoms; X is a bond or oxygen; Y is --(CH.sub.2).sub.n -- where n is 0 or an integer from 1 to 5 wherein one carbon atom not bound to the nitrogen atom may be optionally substituted with a hydroxy group; and Z is hydrogen or halogen; may be used in the prophylaxis and treatment of diseases whose symptoms are controlled by the mediators of the allergic response, for example asthma, hay-fever, rhinitis and allergic eczema.
    Type: Grant
    Filed: October 15, 1979
    Date of Patent: April 21, 1981
    Assignee: Beecham Group Limited
    Inventors: Derek R. Buckle, Harry Smith
  • Patent number: 4251537
    Abstract: Amino chromanols, their preparation and anti-hypertensive compositions containing the compounds in hypotensive amounts with a pharmaceutically acceptable carrier for oral or parenteral administration. Pharmaceutically acceptable salts and O-acyl, particularly O-acetyl, derivatives are described. The compounds exist as racemates and optically active isomers.
    Type: Grant
    Filed: December 18, 1978
    Date of Patent: February 17, 1981
    Assignee: Beecham Group Limited
    Inventor: John M. Evans
  • 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: 4238487
    Abstract: There are disclosed novel compounds described as aminoalkyl benzofuran derivatives in which the aminoalkyl benzofuran is connected to a guanidine moiety or functional equivalent thereof through a linear connecting group. Processes for the preparation of such compounds are also disclosed. The compounds are useful for the suppression of gastric acid secretions in mammals and compositions for such uses are also disclosed.
    Type: Grant
    Filed: October 31, 1979
    Date of Patent: December 9, 1980
    Assignee: Merck & Co., Inc.
    Inventor: John B. Bicking
  • Patent number: 4234726
    Abstract: Compounds of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof wherein the NR.sub.1 R.sub.2 moiety is a 5-, 6-, or 7-membered saturated heterocyclic ring; R.sub.3 is hydrogen, alkyl of 1 to 4 carbon atoms or acyl of 1 to 4 carbon atoms; R.sub.4 is naphthyl or phenyl unsubstituted or substituted by one or two substituents selected from the group consisting of fluorine, chlorine, bromine, methoxyl, benzyloxyl, trifluoromethyl, methyl, cyano, nitro, acetoxyl, amino, methylamino, ethylamino, dimethylamino, diethylamino, acetamide, hydroxyl, methoxycarbonyl, ethoxycarbonyl, carboxamido, sulphonamido, carboxy, trifluoromethylthio, trifluoromethoxyl, methylsulphonyl, trifluomethylsulphonyl and methylthio; R.sub.5 is hydrogen or alkyl of 1 to 4 carbon atoms; R.sub.6 is hydrogen or alkyl of 1 to 4 carbon atoms; X is oxygen and the dotted line represents a single or double bond.
    Type: Grant
    Filed: May 9, 1979
    Date of Patent: November 18, 1980
    Assignee: Beecham Group Limited
    Inventor: Derek V. Gardner