Additional Nitrogen Containing Hetero Ring (e.g., Thiazetidine, Etc.) Patents (Class 544/111)
  • Patent number: 4427687
    Abstract: Carbamoyl-oxime compound of the formula ##STR1## wherein A, R.sup.3, R.sup.4 and R.sup.5 are as hereinafter set forth, a process for their preparation, pesticidal compositions containing one or more of these compounds as the active ingredient, methods of use of such compositions for the control of pests, particularly insects, mites, nematodes and molluscs, and intermediates for the production of such compounds are described.
    Type: Grant
    Filed: April 24, 1981
    Date of Patent: January 24, 1984
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Christoph Luthy, Paul Winternitz
  • Patent number: 4416817
    Abstract: Novel 3-methoxy-2-oxoazetidine derivatives, which are shown by the following formula ##STR1## wherein R.sub.1 is amino, acylated amino or protected amino, are of value as intermediates for the synthesis of useful compounds represented by the formula ##STR2## wherein R.sub.1 has the same meaning as defined above, as drugs in the treatment of bacterial infections.
    Type: Grant
    Filed: November 18, 1981
    Date of Patent: November 22, 1983
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Taisuke Matsuo, Michihiko Ochiai
  • Patent number: 4397848
    Abstract: The present invention provides pharmaceutical compositions containing N-substituted aziridine-2-carboxylic acid derivatives of the general formula: ##STR1## wherein X is a carboxyl, a cyano, an alkoxycarbonyl or an optionally substituted carbamoyl radical, R is a hydrogen atom, or an optionally substituted aliphatic hydrocarbon radical or cycloalkyl or cycloalkenyl radical, and R.sub.1 is a hydrogen atom or an alkyl or phenyl radical; and the pharmacologically acceptable salts thereof, in admixture with a pharmaceutical diluent or carrier. The present invention also provides, as new compounds, N-substituted aziridine-2-carboxylic acid derivatives of general formula (I') but with the proviso that when X is a carbamoyl or alkoxycarbonyl radical and R.sub.1 is a hydrogen atom, R is not a methyl, ethyl, isopropyl or benzyl radical; and the pharmacologically acceptable salts thereof, and also provides processes for the preparation of these new compounds.
    Type: Grant
    Filed: February 20, 1981
    Date of Patent: August 9, 1983
    Assignee: Boehringer Mannheim GmbH
    Inventors: Elmar Bosies, Wolfgang Kampe, Max Thiel, Uwe Bicker, Dietmar Boerner
  • Patent number: 4385179
    Abstract: The present invention refers to a new process for preparing N-2,3,4,5-substituted-1H-pyrrol-1-yl)-6-substituted amino-3-pyridazineamine, known as antihypertensive agents. The process is characterized in that a suitable 3,6-dihalogenopyridazine is reacted with hydrazine hydrate or other hydrazine derivatives of formula NH.sub.2 NHR, the obtained compound is reacted with a suitable dicarbonyl compound yielding first an alcandione-bis-[6-halogen-3-pyridazininyl]hydrazone, and then a 6-halogen-3-pyrrolylpyridazineamine derivative which is in turn reacted with an amine to yield the desired compounds.
    Type: Grant
    Filed: December 18, 1981
    Date of Patent: May 24, 1983
    Assignee: Gruppo Lepetit S.p.A.
    Inventor: Elvio Bellasio
  • Patent number: 4374244
    Abstract: Quaternary ammonium polymers having formula ##STR1## wherein R' and R" may be the same or different alkyl groups of from 1 to 18 carbon atoms, optionally substituted by from 1 to 2 hydroxyl groups or, when taken together, with N form a saturated or unsaturated ring of from 5 to 7 atoms, or when taken together with N and an oxygen atom form the N-morpholino group; wherein Z is --CH.sub.2 CH.dbd.CHCH.sub.2 -- when Z' is --CH.sub.2 CHOHCH.sub.2 -- or Z is --CH.sub.2 CHOHCH.sub.2 -- when Z' is --CH.sub.2 CH.dbd.CHCH.sub.2 --; wherein X is a halogen of atomic weight greater than 30; wherein Y and Y' may be either the same or different and may be either X or -NR'R"; and wherein n is an integer of from 2 to 20.
    Type: Grant
    Filed: November 17, 1980
    Date of Patent: February 15, 1983
    Assignee: Kewanee Industries, Inc.
    Inventors: Harold A. Green, John J. Merianos, Alfonso N. Petrocci
  • Patent number: 4374271
    Abstract: N-Amino substituted aniline and 1,3-phenylenediamine compounds having 1 or 2 nitro groups on the aromatic ring. The compounds are useful as herbicides and as intermediates for preparing herbicides.
    Type: Grant
    Filed: April 4, 1979
    Date of Patent: February 15, 1983
    Assignee: United States Borax & Chemical Corporation
    Inventors: Don L. Hunter, William G. Woods, James D. Stone, Cecil W. LeFevre
  • Patent number: 4362728
    Abstract: Compounds useful for inhibiting gastric acid secretion and for the treatment of peptic ulcers caused or exacerbated by gastric acidity having the following formula (I): ##STR1## in which R.sup.1 and R.sup.2, are H, C.sub.1-10 alkyl, C.sub.3-8 cycloalkyl or cycloalkylalkyl in which the alkyl part is C.sub.1-6 and the cycloalkyl part is C.sub.3-8, each of the alkyl, cycloalkyl and cycloalkylalkyls being optionally substituted by one or more halogens selected from F, Cl and Br, provided that at least one of R.sup.1 and R.sup.2 is a halogen substituted alkyl, cycloalkyl or cycloalkylalkyl and provided that there is no halogen substituent on the carbon directly attached to the nitrogen; and X, m, Y, n and R.sup.3 are as described in the specification; and the pharmaceutically-acceptable acid-addition salts thereof.
    Type: Grant
    Filed: November 12, 1980
    Date of Patent: December 7, 1982
    Assignees: ICI Americas Inc., Imperial Chemical Industries Ltd.
    Inventors: Tobias O. Yellin, Philip N. Edwards, Michael S. Large
  • Patent number: 4349378
    Abstract: Sulphonanilides of formula ##STR1## and salts thereof, wherein R.sup.1 represents alkyl or certain other groups;R represents alkylene or alkenylene;A represents --COR.sup.12 or a carbonyl derivative or addition compound thereof, where R.sup.12 represents hydrogen, alkyl or certain other groups; andR.sup.2 -R.sup.6 represent hydrogen, alkyl, halogen or certain other groups;are pesticides and plant growth regulants, especially herbicides and fungicides.
    Type: Grant
    Filed: December 14, 1978
    Date of Patent: September 14, 1982
    Assignee: FBC Limited
    Inventors: Geoffrey R. Cliff, Russell G. Hunt, Albert Percival
  • Patent number: 4348406
    Abstract: Compounds of the formula: ##STR1## and their pharmaceutically acceptable acid addition salts, useful as anthelmintics are disclosed.
    Type: Grant
    Filed: October 20, 1980
    Date of Patent: September 7, 1982
    Assignee: Schering Corporation
    Inventor: M. Mehdi Nafissi-Varchei
  • Patent number: 4348330
    Abstract: A process for the production of a sulphinate of formula ##STR1## which comprises reacting a compound of formula ##STR2## or a mixture of the compounds of formulae (2a) and (2b) with a compound of formulaY--SO.sub.2 --M (3)in an organic solvent in the presence of a mineral acid or organic acid and, optionally, also of water, wherein Ar.sub.1 and Ar.sub.2 are the same or different and each represents an unsubstituted or substituted aromatic carbocyclic radical.R.sub.1, R.sub.2, R.sub.3 and R.sub.4 independently of one another represent hydrogen, C.sub.1 -C.sub.12 -alkyl, C.sub.2 -C.sub.8 -alkoxyalkyl, cycloalkyl, aralkyl, aryl, or substituted alkyl, cycloalkyl, aralkyl or aryl, or each of the pairs of substituents (R.sub.1 and R.sub.2) and (R.sub.3 and R.sub.4), together with the nitrogen atom to which said pair is attached, independently, represents a heterocyclic ring, or one of several of the substituents R.sub.1, R.sub.2, R.sub.3 and R.sub.4 with the nitrogen and an adajcent carbon atom of the residue Ar.
    Type: Grant
    Filed: February 6, 1981
    Date of Patent: September 7, 1982
    Assignee: Ciba-Geigy Corporation
    Inventors: Malcolm C. Clark, John B. Henshall
  • Patent number: 4344893
    Abstract: Novel compounds are described which are substituted benzophenone hydrazones. They have pesticidal activity, especially against insects and acarids, and pesticidal compositions and methods are described. Methods of making the compounds, and novel intermediates, are also described.
    Type: Grant
    Filed: February 25, 1980
    Date of Patent: August 17, 1982
    Assignee: The Boots Company Limited
    Inventors: Leonard G. Copping, John C. Kerry, Thomas I. Watkins, Robert J. Willis, Bryan H. Palmer
  • Patent number: 4342756
    Abstract: Compounds are described of the formula ##STR1## (and their salts and solvates) in which: X is cis or trans --CH.dbd.CH--;R.sup.1 is C.sub.1-7 alkyl terminated by --COOR.sup.3 where R.sup.3 is H, C.sub.1-6 alkyl or C.sub.7-10 aralkyl;Y is a saturated heterocyclic amino group having 5-8 ring members; andR.sup.2 is C.sub.2-4 alkanoyl, C.sub.3-6 alkenyl (optionally substituted), C.sub.1-12 alkyl, or substituted or unsubstituted phenylalkyl, biphenylalkyl or naphthylalkyl.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic and anti-asthmatic agents.
    Type: Grant
    Filed: April 29, 1981
    Date of Patent: August 3, 1982
    Assignee: Glaxo Group Limited
    Inventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, John Bradshaw, Norman F. Hayes
  • Patent number: 4323677
    Abstract: N-amides of 2-benzothiazolinone have been found to be effective in regulating the growth of leguminous plants.
    Type: Grant
    Filed: June 25, 1979
    Date of Patent: April 6, 1982
    Assignee: Monsanto Company
    Inventor: John J. D'Amico
  • Patent number: 4321194
    Abstract: Aziridine-2-carboxylic acid derivatives of the formula ##STR1## wherein X is a carboxyl, nitrile, alkoxycarbonyl or carbamoyl group, andR and R.sup.1 are various organic radicals, or pharmacologically acceptable salts thereof, exhibit marked immunostimulant activity, especially in conjunction with added chemotherapeutic agents such as a penicillin, a cephalosporin, a nitrofuran or chloramphenicol. Those compounds are new where X is a cyano group or an alkoxycarbonyl radical and R.sub.1 is a hydrogen atom, but R' is not an unsubstituted alkyl radical or an alkyl radical substituted by hydroxyl, alkoxy, dialkylamino, phenyl, 4-chlorophenyl or 4-methoxyphenyl or a vinyl radical substituted by a phenyl or methyl radical, or a cycloalkyl radical, a phenyl a 4-chlorophenyl, a 4-methoxyphenyl, an s-triazinyl or a pyridinyl radical; or where X is a carbamoyl group and R.sub.
    Type: Grant
    Filed: July 23, 1979
    Date of Patent: March 23, 1982
    Assignee: Boehringer Mannheim GmbH
    Inventors: Elmar Bosies, Herbert Berger, Wolfgang Kampe, Uwe Bicker, Alfred Grafe
  • Patent number: 4316036
    Abstract: A benzopyranothiazole of the formula ##STR1## wherein each of R.sub.1 and R.sub.2 independently represents hydrogen, alkyl of not more than 12 carbon atoms which is unsubstituted or substituted by halogen, hydroxyl, cyano or lower alkoxy, or represents cycloalkyl, phenyl, benzyl, or phenyl or benzyl which is substituted by halogen, lower alkyl or lower alkoxy, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached represent a 5- or 6-membered heterocyclic radical or a N-carbazolyl radical, Q represents hydrogen, lower alkyl, benzyl or groups of the formulae (1a) or (1b) ##STR2## each of X, X.sub.1 and X.sub.2 represents hydrogen, halogen, lower alkyl or lower alkoxy, each of Y.sub.1, Y.sub.2, Y'.sub.1 and Y'.sub.
    Type: Grant
    Filed: September 11, 1978
    Date of Patent: February 16, 1982
    Assignee: Ciba-Geigy Corporation
    Inventor: Jean C. Petitpierre
  • Patent number: 4309345
    Abstract: Hydrogenated 1-aminoalkyl indeno- or -naphth[1,2-d]azepines, e.g. those of the formula ##STR1## Am'=NH.sub.2, (alkyl, alkenyl, alkynyl, hydroxyalkyl, cycloalkyl, or benzyl)amino, its N-lower alkyl derivatives; alkyleneimino morpholino or piperazinoR.sub.o-3 =H, OH, alkyl, alkoxy, halo or CF.sub.3R.sub.4,5 =H or alkyl; X=H.sub.2 or 0 m=1 or 2; q=0 or 1and salts thereof are potassium-sparing diuretic agents.
    Type: Grant
    Filed: January 10, 1979
    Date of Patent: January 5, 1982
    Assignee: Ciba-Geigy Corporation
    Inventor: Norbert Gruenfeld
  • Patent number: 4309559
    Abstract: Sulphonanilides of formula ##STR1## and salts thereof, wherein R.sup.1 represents alkyl or certain other groups;R represents alkylene or alkenylene;A represents --COOH, --COO alkyl, --CSSH, CN or certain related groups; orR-A represents a group of formula ##STR2## where R.sup.14 represents hydrogen, alkyl or aryl, B represents oxygen or ##STR3## R.sup.15 represents hydrogen or alkyl, and n represents 0, 1 or 2; and R.sup.2 -R.sup.6 represent hydrogen; alkyl, halogen or certain other groups,are pesticides and plant growth regulants, especially herbicides and fungicides.
    Type: Grant
    Filed: December 14, 1978
    Date of Patent: January 5, 1982
    Assignee: FBC Limited
    Inventor: Geoffrey R. Cliff
  • Patent number: 4305949
    Abstract: A series of N-(2-thiazolyl)amides has been prepared, including their pharmaceutically acceptable acid addition salts as well as pharmaceutical compositions containing same. These compounds are useful in therapy as anti-inflammatory agents in addition to being useful as immunoregulatory agents for modulating various body immune responses. Preferred member compounds include N-(2-thiazolyl)-.alpha.-methylaminoacetamide, N-(2-thiazolyl)-.alpha.-benzylaminoacetamide, N-(2-thiazolyl)-.alpha.-(p-fluorobenzylamino)acetamide, N-(2-thiazolyl)-.alpha.-(2-thenylamino)acetamide and N-(4-methyl-2-thiazolyl)-.alpha.-amino-.beta.-phenylpropionamide, and their hydrohalide acid addition salts. Three different methods of preparation are provided and these are all described in some detail, including the various synthetic routes leading to the required novel intermediates and/or starting materials.
    Type: Grant
    Filed: January 29, 1980
    Date of Patent: December 15, 1981
    Assignee: Pfizer Inc.
    Inventors: Charles A. Harbert, Joseph G. Lombardino
  • Patent number: 4301280
    Abstract: There is described a process for preparing an enamine of formula (IX): ##STR1## where R.sup.2 is a carboxylic acid protecting group and R.sup.3 is the residue of a carboxylic acid derived acyl group and where R.sup.5 and R.sup.6 are the same or different C.sub.1-4 alkyl or C.sub.7-10 aralkyl groups; or taken together with the adjacent nitrogen atom form a heterocyclic ring containing from 4 to 8 carbon atoms and optionally a further heteroatom selected from oxygen and nitrogen; by reacting a compound of formula (XII): ##STR2## with an amine of formula HNR.sup.5 R.sup.6, the reactant of formula (XII) being prepared by reaction of an appropriate enol derivative with a phosphorus reagent. The enamines of formula (IX) are useful in the preparation of 3-hydroxycephalosporins.
    Type: Grant
    Filed: May 1, 1980
    Date of Patent: November 17, 1981
    Assignee: Lilly Industries Limited
    Inventors: John R. Corfield, Derek Johnson, Clifford G. Taylor
  • Patent number: 4293462
    Abstract: The invention concerns a process for the manufacture of 7.beta.-amino-3-cephem-3-ol-4-carboxylic acid compounds by ring closure of esters of 2-[4-(substituted-thio)-3-acylamino-2-oxoazetidin-1-yl]-3-substituted-amin o-crotonic acids and solvolyzing the enamino group in the resulting 7.beta.-acylamino-3-substituted-amino-cephem-4-carboxylic acid esters.
    Type: Grant
    Filed: December 10, 1979
    Date of Patent: October 6, 1981
    Assignee: Ciba-Geigy Corporation
    Inventors: Robert B. Woodward, Hans Bickel
  • Patent number: 4282212
    Abstract: 1-(N-Acyl-carbamoyl)-2-cyanoaziridines of the formula ##STR1## wherein X is oxygen or sulphur,Z is hydrogen or an organic radical, andY is a carbonyl, sulphonyl, sulphinyl, sulphenyl, phosphoryl or phosphonyl radical,and salts thereof, exhibit immune-stimulating and cancerostatic activities.
    Type: Grant
    Filed: September 30, 1977
    Date of Patent: August 4, 1981
    Assignee: Boehringer Mannheim GmbH
    Inventors: Herbert Berger, Rudi Gall, Wolfgang Kampe, Uwe Bicker, Gottfried Hebold
  • Patent number: 4256896
    Abstract: A naphtholactam dyestuff of the general formula (1) ##STR1## in which R represents C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -alkenyl, C.sub.6 -C.sub.9 -cycloalkyl, C.sub.6 -C.sub.9 -aralkyl, aryl or, preferably, hydrogen, X represents --COOH, --COO.sup..crclbar. cation.sup..sym., a modified carboxyl group, the radical --SO.sub.2 --T or a heterocyclic radical, T denoting alkyl, alkenyl or, preferably, aryl, M represents hydrogen or a cation, Y represents a free or modified carboxyl group, Z is C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, Cl, Br, NO.sub.2, phenyl sulphonyl C.sub.1 -C.sub.4 -alkyl-S, C.sub.1 -C.sub.4 -alkyl sulphonyl, cyano, CONH.sub.2, CONH-C.sub.1 -C.sub.4 -alkyl, and CON(C.sub.1 -C.sub.4 -alkyl).sub.2, n represents 0, 1 or 2, A represents a heterocyclic radical or --CN and B and C can carry further non-ionic substituents.The new dyestuffs give brilliant yellow and red shades on polyester and polyamide fibers.
    Type: Grant
    Filed: September 29, 1978
    Date of Patent: March 17, 1981
    Assignee: Ciba-Geigy Aktiengesellschaft
    Inventors: Hansrudolf Schwander, Christian Zickendraht
  • Patent number: 4256742
    Abstract: Polycyclic aziridines, such as 0-[2-(dimethylamino)ethyl]oxime of 1a,10b-dihydrodibenzo-[3,4,6,7]cyclohept[1,2-b]-N-methylazirin-6(1H)-one, useful for alleviating depression in mammals.
    Type: Grant
    Filed: June 27, 1979
    Date of Patent: March 17, 1981
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Michael J. Haire
  • Patent number: 4252804
    Abstract: Compounds of the formula I ##STR1## wherein m and n are 0, 1 or 2, X represents oxygen, imino, benzylimino, or morpholinoethylimino, Y represents CO, CONH, COO or SO.sub.2, and NR.sub.1 R.sub.2 represents a dimethylamino, diethylamino, dipropylamino, dibutylamino, allylamino, isobutenylamino, cyclopentylamino, cyclohexylamino, cycloheptylamino, cyclooctylamino, N-methyl N-cyclopentylamino, N-methyl N-cyclohexylamino, N-allyl N-cyclohexylamino, adamantylamino, diethoxyethylamino, dimethylaminoethylamino, dimethylaminopropylamino, N-methyl N-dimethylaminopropyl-amino, benzylamino, 3,4,5-trimethoxybenzylamino, phenethylamino, p-chlorophenethylamino, tetrahydrofurfurylamino, tetrahydropyranylmethylamino, pyrrolidino, isoxazolidinyl, piperidino, 4-hydroxypiperidino, 4-m-chlorophenyl-4-hydroxypiperidino, homopiperidino, 1,2,3,6-tetrahydropyridyl, morpholino, 2-methylmorpholino, 2,6-dimethylmorpholino, 2-morpholinoethylamino, thiamorpholino, piperazino, 4-methylpiperazino, 4-(.alpha.
    Type: Grant
    Filed: January 13, 1978
    Date of Patent: February 24, 1981
    Assignee: Metabio-Joullie
    Inventors: Maurice Joullie, Gabriel Maillard, Lucien Lakah, Christian J. M. Warolin
  • Patent number: 4239894
    Abstract: An organic compound of the general formula ##STR1## where R.sup.1 and R.sup.2 are cyano, formyl, substituted or unsubstituted alkanoyl or aroyl, a carboxylic acid ester group, substituted or unsubstituted carbamoyl or sulfamoyl, alkylsulfonyl, arylsulfonyl or alkylsulfinyl, orR.sup.1 and R.sup.2 together may be a cyclic radical,R.sup.2 may also be alkyl, aryl or hetaryl,R.sup.3 is hydrogen, substituted or unsubstituted alkyl, aryl or hetaryl,X is CH, CR.sup.5 or N,R.sup.4 is a radical of the formula ##STR2## R.sup.5 to R.sup.10 are substituents conventionally present in dyes. The compounds may be used as dyes for synthetic and natural fibers and give very fast dyeings.
    Type: Grant
    Filed: June 29, 1978
    Date of Patent: December 16, 1980
    Assignee: BASF Aktiengesellschaft
    Inventors: Guenther Seybold, Heinz Eilingsfeld
  • Patent number: 4237134
    Abstract: New substituted derivatives of thiazolidine-, thiazane- and related carboxylic acids which have the general formula ##STR1## are useful as angiostensin converting enzyme inhibitors.
    Type: Grant
    Filed: June 28, 1979
    Date of Patent: December 2, 1980
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Miguel A. Ondetti
  • Patent number: 4228074
    Abstract: .beta.-Lactam compounds of the formula (I) ##STR1## (wherein R represents an esterified carboxyl group, --NR.sup.1 R.sup.2 R.sup.3 represents the residue of a nitrogen base, and R.sup.4 represents a hydrogen atom, a hydroxyl group or acylated or etherified hydroxyl group or the residue of a sulphur nucleophile) are disclosed, together with processes for their preparation. The compounds are valuable intermediates for the preparation or purification of further .beta.-lactam compounds having .beta.-lactamase inhibitory activity.
    Type: Grant
    Filed: September 8, 1977
    Date of Patent: October 14, 1980
    Assignee: Glaxo Laboratories Limited
    Inventors: Peter C. Cherry, Christopher E. Newall, Nigel S. Watson
  • Patent number: 4224244
    Abstract: Novel 9-phenyl 5,6-dimethyl-nona-2,4,6,8-tetraenoic acid, tetraenal or tetraenol derivatives useful as anti-tumor agents.
    Type: Grant
    Filed: May 9, 1979
    Date of Patent: September 23, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Werner Bollag, Rudolf Ruegg, Gottlieb Ryser
  • Patent number: 4208325
    Abstract: The invention provides a novel process for opening the ring of 2-R-6-(1'-R.sup.1 -oxycarbonyl-2'-methyl-prop-1'-enyl)-1-oxa-3,6-diaza-4S,5R-bicyclo[3,2,0]h ept-2-en-7-one by treatment with a sulfonic acid salt thereby forming R.sup.1 2-(2'R-R-oxy-3'S-amino-4'-oxo)azetidinyl-3-methyl-2-butenoate sulfonic acid salts which can provide oxapenicillins by two different routes depending on the substituent desired on the carboxamido group of the 1-oxapenicillins. In the alternate processes, new intermediates are also provided.
    Type: Grant
    Filed: November 30, 1977
    Date of Patent: June 17, 1980
    Assignee: Queen's University at Kingston
    Inventor: Saul Wolfe
  • Patent number: 4207234
    Abstract: New antimicrobial azetidinone derivatives and their salt of the formula: ##STR1## wherein R.sub.1 is amino or acylamino, and A is selected from a variety of groups.
    Type: Grant
    Filed: December 7, 1977
    Date of Patent: June 10, 1980
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takashi Kamiya, Yoshihisa Saito, Masashi Hashimoto, Osamu Nakaguti, Teruo Oku, Youichi Shiokawa, Takao Takaya, Tadaaki Komori, Tsutomu Teraji, Keiji Hemmi, Hisashi Takasugi
  • Patent number: 4202839
    Abstract: N-Amino substituted aniline and 1,3-phenylenediamine compounds having 1 or 2 nitro groups on the aromatic ring. The compounds are useful as herbicides and as intermediates for preparing herbicides.
    Type: Grant
    Filed: December 26, 1978
    Date of Patent: May 13, 1980
    Assignee: United States Borax & Chemical Corporation
    Inventors: Don L. Hunter, William G. Woods, James D. Stone, Cecil W. LeFevre
  • Patent number: 4191689
    Abstract: This invention relates to certain 3,3-di(4'-OP-carbocyclic aryl)-2,3-dihydrobenz[d]isothiazole-1,1-dioxides (and-2,3-dihydronaphtho[1,8-de]-1,2-thiazine-1,1-dioxides) and to the preparation thereof by reacting (a) at least 2 equivalents of (i) a 4'-OP-carbocyclic aryllithium compound wherein P is a protecting group compatible with organometallic reagents or (ii) a 4'-OP-carbocyclic arylMgE compound wherein P is a protecting group compatible with organometallic reagents and E is chloro, bromo or iodo and (b) 1 equivalent of a compound selected from a 3-chlorobenz[d] isothiazole-1,1-dioxide and a 3-chloronaphtho[1,8-de]-1,2-thiazine-1,1-dioxide to give the corresponding 3,3-di(4'-OP-carbocyclic aryl)-2,3-dihydrobenz[d]isothiazole-1,1-dioxide or the corresponding 3,3-di(4'-OP-carbocyclic aryl)-2,3-dihydronaphtho[1,8-de]-1,2-thiazine-1,1-dioxide, which compounds are useful in the synthesis of phenol and 1-naphthol sulfam(na)-phthaleins employed, for example, as photographic optical filter agents and filter agent
    Type: Grant
    Filed: September 23, 1977
    Date of Patent: March 4, 1980
    Assignee: Polaroid Corporation
    Inventors: Stanley M. Bloom, Alan L. Borror, James W. Foley
  • Patent number: 4189588
    Abstract: Novel triazolo- or imidazo-benzotriazepines are prepared from 1,3,4-benzotriazepine-2-thiones which in turn are prepared from a 2-aminobenzophenone.
    Type: Grant
    Filed: October 16, 1978
    Date of Patent: February 19, 1980
    Assignee: The Dow Chemical Company
    Inventors: Thomas C. Britton, Donald L. Trepanier
  • Patent number: 4183946
    Abstract: Substituted 2-vinyl chromones are disclosed, wherein the chromone ring has an alkyl or alkenyl substituent at the 3-position, and a styryl substituent at the 2-position. The compounds exhibit anti-allergy activity and can be used to treat allergic conditions.
    Type: Grant
    Filed: July 24, 1978
    Date of Patent: January 15, 1980
    Assignee: Carlo Erba S.p.A.
    Inventors: Gianfederico Doria, Ciriaco Romeo, Francesco Lauria, Maria L. Corno, Piernicola Giraldi, Marcello Tibolla
  • Patent number: 4181655
    Abstract: Novel compounds of general formula ##STR1## (where R.sup.1 and R.sup.2, which may be the same or different, are hydrogen atoms or alkyl groups; and R.sup.3 and R.sup.4, which may be the same or different, represent alkyl groups which may carry substituents, R.sup.4 alternatively representing a hydrogen atom; or R.sup.3 and R.sup.4 together with the intervening N represent a heterocyclic group or an acid-addition salt thereof) are provided, together with a process for their preparation. The new compounds are useful as antidepressants.
    Type: Grant
    Filed: May 4, 1977
    Date of Patent: January 1, 1980
    Assignee: Research Institute for Medicine and Chemistry Inc.
    Inventors: Derek H. R. Barton, Robert H. Hesse
  • Patent number: 4176183
    Abstract: Novel naphthyridines having a 3-amino-2-OR-propoxy substituent are disclosed. The compounds have .beta.-adrenergic blocking and immediate onset antihypertensive activities.
    Type: Grant
    Filed: July 17, 1978
    Date of Patent: November 27, 1979
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello
  • Patent number: 4174317
    Abstract: Compounds having the formula ##STR1## wherein A.sub.1 is an alkylene group having 2 to 4 carbon atoms; R.sub.1 is dialkylamino or a nitrogen containing heterocyclic group and R.sub.2 is phenyl, substituted phenyl, naphthyl, or 1,3-benzodioxol-5-yl; have antiinflammatory activity.
    Type: Grant
    Filed: March 24, 1978
    Date of Patent: November 13, 1979
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: John Krapcho, Chester F. Turk
  • Patent number: 4173633
    Abstract: Hydrogenated 1-aminoalkyl-indeno- or naphth[1,2-d]-azepines, e.g. those of the formula ##STR1## Am'=NH.sub.2, (alkyl, alkenyl, alkynyl, hydroxyalkyl, cycloalkyl, or benzyl)amino, its N-lower alkyl derivatives; alkyleneimino morpholino or piperazino;R.sub.o-3 =H, OH, alkyl, alkoxy, halo or CF.sub.3 ;R.sub.4,5 =H or alkyl;X=H.sub.2 or 0;m=1 or 2;q=0 or 1;and salts thereof are potassium-sparing diuretic agents.
    Type: Grant
    Filed: December 2, 1977
    Date of Patent: November 6, 1979
    Assignee: Ciba-Geigy Corporation
    Inventor: Norbert Gruenfeld
  • Patent number: 4166907
    Abstract: Compounds having the formula ##STR1## wherein R.sub.1 is alkyl, cycloalkyl or aryl; R.sub.2 is dialkylamino or a nitrogen containing heterocyclic group; A.sub.1 is a saturated bond or an alkylene group having 1 to 4 carbon atoms; and A.sub.2 is an alkylene group having 2 to 5 carbon atoms; have antiinflammatory activity.
    Type: Grant
    Filed: October 11, 1977
    Date of Patent: September 4, 1979
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: John Krapcho, Chester F. Turk
  • Patent number: 4163784
    Abstract: Heterocyclylcarbonyl derivatives of urea having the formula ##STR1## wherein R is a heterocyclyl group; R.sub.1 is hydrogen, alkyl having up to ten carbon atoms or phenyl; R.sub.2 is R.sub.1, 1-naphthyl and phenylalkyl having 1 to 4 carbon atoms in the alkyl group; and R.sub.1 and R.sub.2 when taken together with the nitrogen to which they are attached are morpholino, thiomorpholino or a 6-8 membered nitrogen containing heterocyclic ring; methods for their preparation and use as agents for dissolving gallstones.
    Type: Grant
    Filed: March 9, 1978
    Date of Patent: August 7, 1979
    Assignee: Pfizer Inc.
    Inventor: Gerald F. Holland
  • Patent number: 4160090
    Abstract: N-Amino substituted aniline and 1,3-phenylenediamine compounds having 1 or 2 nitro groups on the aromatic ring. The compounds are useful as herbicides and as intermediates for preparing herbicides.
    Type: Grant
    Filed: November 7, 1977
    Date of Patent: July 3, 1979
    Assignee: United States Borax & Chemical Corporation
    Inventors: Don L. Hunter, William G. Woods, James D. Stone, Cecil W. LeFevre
  • Patent number: 4148900
    Abstract: Chromone compounds carrying a pyridyl substituent at the 2-position are disclosed, such as, for instance, 6-carboxy-2-(2'-pyridyl)-chromone. The disclosed compounds are useful in the treatment of allergies.
    Type: Grant
    Filed: September 16, 1977
    Date of Patent: April 10, 1979
    Assignee: Carlo Erba S.p.A.
    Inventors: Gianfederico Doria, Piernicola Giraldi, Francesco Lauria, Maria L. Corno, Piero Sberze, Marcello Tibolla
  • Patent number: 4145541
    Abstract: Compounds having the formula ##STR1## wherein X is oxygen or sulfur; R.sub.1 is alkyl, cycloalkyl or aryl; R.sub.2 is a nitrogen containing heterocyclic group; A.sub.1 is a saturated bond or an alkylene group having 1 to 4 carbon atoms; and A.sub.2 is an alkylene group having 2 to 5 carbon atoms; have antiinflammatory activity.
    Type: Grant
    Filed: June 30, 1978
    Date of Patent: March 20, 1979
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: John Krapcho, Chester F. Turk
  • Patent number: 4144233
    Abstract: Novel triazolo- or imidazo-benzotriazepines are prepared from 1,3,4-benzotriazepine-2-thiones which in turn are prepared from a 2-aminobenzophenone.
    Type: Grant
    Filed: July 25, 1977
    Date of Patent: March 13, 1979
    Assignee: The Dow Chemical Company
    Inventors: Thomas C. Britton, Donald L. Trepanier
  • Patent number: 4139623
    Abstract: Compounds of the formula ##STR1## WHEREIN Ar.sub.1 and Ar.sub.2 denote an optionally substituted aromatic hydrocarbon radical or a monocyclic, monoazacyclic or diazacyclic radical of aromatic character and Alk represents lower alkylene, or salts thereof, exhibit .beta.-receptor-blocking, blood pressure-lowering and vasodilatory effects and are useful for example in the treatment of arrythmias and angina pectoris, and as blood pressure-lowering agents.
    Type: Grant
    Filed: March 14, 1977
    Date of Patent: February 13, 1979
    Assignee: C-G Corp.
    Inventors: Knut A. Jaeggi, Franz Ostermayer, Herbert Schroter
  • Patent number: 4125532
    Abstract: The reaction of 1-(halo/cyano/sulfonyloxy)alkanoyl-2-(dibenzoxazepine-10-carbonyl)hydrazin es with an amine affords the corresponding 1-(substituted amino)alkanoyl-2-(dibenzoxazepine-10-carbonyl)hydrazines which compounds are useful anti-inflammatory or anti-diarrheal agents.
    Type: Grant
    Filed: July 5, 1977
    Date of Patent: November 14, 1978
    Assignee: G. D. Searle & Co.
    Inventor: Richard A. Mueller
  • Patent number: 4123527
    Abstract: Novel N-tricyclic derivatives of azetidine are disclosed of the general formula ##STR1## where A is a C.sub.1 -C.sub.3 alkylene group, a C.sub.2 -C.sub.3 alkenylene group or a cyclopropylene group, the remaining substituents being defined in the specification. Such compounds are useful for their anti-depressant, anti-convulsant and anxiolytic activities. The compound 1-[5-(10, 11-dihydro-5H-dibenzo [a,d]cyclopheptenyl)]-3-methyl-amino-azetidine is illustrative.
    Type: Grant
    Filed: January 9, 1976
    Date of Patent: October 31, 1978
    Assignee: Carlo Erba, S.p.A.
    Inventors: Piero Melloni, Arturo Della Torre, Francesco Lauria, Norina Passerini, Alessandro Rossi, Raffaele Tommasini
  • Patent number: 4118501
    Abstract: 4-(Sulfamoyl-phenyl)-4-hydroxy-2-imino-thiazolidine-derivatives having salidiuretic activity and a process for their manufacture.
    Type: Grant
    Filed: January 14, 1977
    Date of Patent: October 3, 1978
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hans-Jochen Lang, Roman Muschaweck
  • Patent number: 4115382
    Abstract: Compounds having the formula ##STR1## wherein X is oxygen or sulfur; R.sub.1 is alkyl, cycloalkyl or aryl; R.sub.2 is dialkylamino or a nitrogen containing heterocyclic group; A.sub.1 is a saturated bond or an alkylene group having 1 to 4 carbon atoms; and A.sub.2 is an alkylene group having 2 to 5 carbon atoms; have antiinflammatory activity.
    Type: Grant
    Filed: June 6, 1977
    Date of Patent: September 19, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: John Krapcho, Chester F. Turk
  • Patent number: 4103256
    Abstract: A dye laser comprising a laser dye solution of a compound having the general structure: ##STR1## wherein at least one of the 5, 6 and 8 ring positions is occupied by a nitrogen atom in lieu of the corresponding CR group and X is OH, alkoxy, or amino including amino substituted by at least one of the following: alkyl, aryl, acyl, aracyl, a group which taken together with the nitrogen atom of the amino group forms a heterocyclic ring, or part of one or two 5 or 6 membered aliphatic heterocyclic rings attached to ring A at positions 6 or 8 or both depending on where the N in ring A is located. R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.8 are hydrogen or other groups as defined below. The compounds lase in the blue-green to near ultraviolet region.
    Type: Grant
    Filed: May 25, 1976
    Date of Patent: July 25, 1978
    Assignee: The United States of America as represented by the United States Department of Energy
    Inventors: Peter R. Hammond, Ronald L. Atkins, Ronald A. Henry, Aaron N. Fletcher