Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/48)
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Patent number: 4485107Abstract: Novel [[bis(aryl)methylene]-1-piperidinyl]alkyl-pyrimidinones, wherein the pyrimidinone-ring is embraced within a bicyclic system, being useful compounds in the treatment of psychosomatic disorders.Type: GrantFiled: July 27, 1983Date of Patent: November 27, 1984Assignee: Janssen Pharmaceutica N.V.Inventors: Ludo E. J. Kennis, Jan Vandenberk, Josephus C. Mertens
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Patent number: 4451650Abstract: There are disclosed certain 2H-pyrido[4,3-b][1,4]oxazines and 2H-pyrido[4,3-b][1,4]thiazines which possess biological activity. The compounds have the structure: ##STR1## wherein n has a value of 1,2 or 3; X is oxygen or sulfur; R.sub.1 is a lower alkyl group, e.g., an alkyl group containing up to six carbon atoms such as methyl, ethyl, propyl, butyl, etc.; R.sub.2 is a member selected from the group consisting of hydrogen, alkyl radicals having from about one to about 12 carbon atoms, preferably from about one to about six carbon atoms; alkenyl radicals having from about two to about 15 carbon atoms; preferably from about two to about 10 carbon atoms; cycloalkyl radicals having from about three to about 20 carbon atoms, preferably from about three to about 15 carbon atoms; aryl, aralkyl and alkaryl radicals having from about six to about 20 carbon atoms, preferably from about six to about 15 carbon atoms; a halogen radical, e.g.Type: GrantFiled: October 26, 1982Date of Patent: May 29, 1984Assignee: Southern Research InstituteInventors: Carroll G. Temple, Jr., John A. Montgomery, Robert D. Elliott, Glynn P. Wheeler
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Patent number: 4443451Abstract: Novel 5H-thiazolo- and 5H-1,3,4-thiadiazolo[3,2-a]pyrimidin-5-one and 3,4-dihydro-2H,6H-pyrimido[2,1-b] [1,3]-thiazin-6-one derivatives, which compounds are useful psychotropic agents.Type: GrantFiled: April 21, 1982Date of Patent: April 17, 1984Assignee: Janssen Pharmaceutica N.V.Inventors: Ludo E. J. Kennis, Josephus C. Mertens
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Patent number: 4437877Abstract: A herbicidal composition which comprises as an active ingredient a compound of the formula: ##STR1## wherein X is a chlorine atom or a bromine atom, Y is --CH.sub.2 --, --S-- or --SO.sub.2 -- and R is a C.sub.1 -C.sub.4 alkyl group, an allyl group or a propargyl group, and an inert carrier.Type: GrantFiled: June 10, 1982Date of Patent: March 20, 1984Assignee: Sumitomo Chemical Company, LimitedInventors: Eiki Nagano, Shunichi Hashimoto, Ryo Yoshida, Hiroshi Matsumoto, Katsuzo Kamoshita
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Patent number: 4414388Abstract: Antiallergy and antiulcer agents having the formula (I), ##STR1## and their pharmaceutically acceptable salts, wherein R.sub.1 and R.sub.2 taken separately are each hydrogen or lower alkyl; and R.sub.1 and R.sub.2 taken together are alkylene of 3-9 carbon atoms or phenylalkylene of 9-11 carbon atoms, with the proviso that the ring so formed is between 5- and 8-membered; acids of the formula (II), ##STR2## wherein R.sub.1 and R.sub.2 are as defined above and R.sub.3 is hydrogen, which are useful as intermediates for compounds of the formula (I), but in many instances also possess the same useful biological activity as do formula I compounds; and intermediates of the formula II wherein R.sub.1 and R.sub.2 are defined as above, and R.sub.3 is alkyl of 1 to 4 carbon atoms, carbalkoxy of 2 to 5 carbon atoms, carbophenoxy or carbobenzoxy, are also described.Type: GrantFiled: December 14, 1981Date of Patent: November 8, 1983Assignee: Pfizer Inc.Inventor: Saul B. Kadin
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Patent number: 4394505Abstract: Novel 5-fluorouracil derivatives of the following general formula ##STR1## wherein R.sup.1 is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.6 -C.sub.10 aryl, C.sub.7 -C.sub.10 aralkyl, C.sub.1 -C.sub.12 alkanoyl, C.sub.2 -C.sub.6 alkoxycarbonyl, C.sub.1 -C.sub.5 alkanoyloxymethyl, carbamoyl or tri-C.sub.1 -C.sub.5 alkylsilyl;R.sup.2 is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.6 -C.sub.10 aryl or C.sub.7 -C.sub.10 aralkyl;X is hydrogen, halogen or C.sub.2 -C.sub.6 alkoxycarbonyl;Y is O, NR' (R' is hydrogen or C.sub.1 -C.sub.5 alkyl), S, SO or SO.sub.2 ; andn is an integer of 1-3.which are orally administrable anti-tumor agents.Type: GrantFiled: April 16, 1982Date of Patent: July 19, 1983Assignee: Shionogi & Co., Ltd.Inventors: Susumu Kamata, Wataru Nagata
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Patent number: 4376769Abstract: Disclosed herein are novel tetrahydro imidazo thiazoles, tetrahydro imidazo thiazines, hexahydro imidazo thiazepines and hexahydro imidazo thiazocines, intermediates for the preparation thereof, methods of using the compounds as anti-inflammatory agents and methods of using an intermediate thereof as anti-secretory agents to relieve the symptoms of gastric distress.Type: GrantFiled: June 19, 1981Date of Patent: March 15, 1983Assignee: Schering CorporationInventor: Sherlock Margaret H.
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Patent number: 4361700Abstract: Derivatives of pyridopyrimidinone of the following formulae: ##STR1## wherein Y is C.dbd.S, C.dbd.O, SO.sub.2, or CH.sub.2 ;Z is C--H, N, S or O;R.sub.1 is hydrogen, hydroxyl, halogen, lower alkyl or R.sub.3 ;R.sub.2 is hydrogen, aliphatic hydrocarbon, substituted aliphatic hydrocarbon or carbocyclic aryl-aliphatic hydrocarbon, wherein the substituent of the aliphatic hydrocarbon may be hydroxyl, halogen, alkoxy, carboxylic acid ester, or lower alkyl amine;R.sub.3 is ##STR2## wherein A is carbon, nitrogen, oxygen, or sulfur; R.sub.Type: GrantFiled: May 20, 1980Date of Patent: November 30, 1982Assignee: James S. WaldronInventors: William P. Purcell, Richard D. Gilliom, Harlie A. Parish, Jr.
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Patent number: 4315767Abstract: Triazolone herbicides of the formula: ##STR1## where V is hydrogen, fluorine, chlorine, bromine, methyl or OR where R is alkyl of 1-4 carbon atoms;X is hydrogen, fluorine, chlorine, bromine, cyano, methyl, methoxy, or nitro;Y is hydrogen, fluorine, chlorine, bromine, or methyl;n, m is 0, 1, 2, 3 or 4;Q is oxygen or sulfur;Z is oxygen, S(O).sub.p or NR';p is 0, 1 or 2 andR' is alkyl of 1-3 carbon atoms with the provisos that(1) n+m=2, 3, or 4; and(2) if n+m=2 or 4 then Y, X.noteq.Hand when Z is S(O)p, n is 1, 2, 3 or 4.Type: GrantFiled: December 14, 1979Date of Patent: February 16, 1982Assignee: E. I. Du Pont de Nemours and CompanyInventor: Anthony D. Wolf
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Patent number: 4187303Abstract: Thienothiazine derivatives of the formula ##STR1## wherein A, R.sub.1 and R.sub.2 are as hereinafter set forth, and their tautomers are described. The thienothiazine derivatives are useful as anti-inflammatory, analgesic, antirheumatic and antithrombotic agents.Type: GrantFiled: August 15, 1978Date of Patent: February 5, 1980Assignee: Hoffmann-La Roche Inc.Inventors: Otto Hromatka, Dieter Binder, Paul Zeller, Rudolf Pfister
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Patent number: 4181799Abstract: The compound 5(6H), 8(8aH)-dioxo-1H,3H-thiazolo[4,3-c] [1,4]thiazine is useful as an inhibitor of Angiotensin I converting enzyme.Type: GrantFiled: November 13, 1978Date of Patent: January 1, 1980Assignee: Morton-Norwich Products, Inc.Inventor: Ralph L. White, Jr.
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Patent number: 4180662Abstract: Anti-inflammatory, analgesic, anti-rheumatic and anti-thrombotic thienothiazine derivatives having the formula ##STR1## wherein A together with the two carbon atoms forms the group ##STR2## and the dotted line indicates the double bond present in the first and last thieno structures above, R.sup.1 is lower alkyl, R.sup.2 is the radical of an aromatic heterocycle with 1 to 4 hetero atoms optionally substituted by one or two lower alkyl groups, or a phenyl radical optionally substituted by halogen, hydroxy, lower alkyl, trifluoromethyl or lower alkoxy, R.sup.3 is halogen and R.sup.3' is hydrogen or halogen,and pharmaceutically acceptable salts thereof are described.Type: GrantFiled: August 31, 1978Date of Patent: December 25, 1979Assignee: Hoffmann-La Roche Inc.Inventors: Rudolf Pfister, Paul Zeller, Dieter Binder, Otto Hromatka
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Patent number: 4179276Abstract: This invention relates to novel 2-aryl-1H-imidazo-[5,1-c][1,4]thiazine-1,3(2H)-diones, to agricultural compositions containing them and to the method of use of these compounds as pre- or postemergence herbicides for general control of undesirable vegetation. The invention also includes novel intermediate compounds for making the novel compounds.Type: GrantFiled: March 27, 1978Date of Patent: December 18, 1979Assignee: E. I. Du Pont de Nemours and CompanyInventor: Jiin-Duey Cheng
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Patent number: 4119777Abstract: A thiazine derivative, which forms a color on contact with an electron accepting material, represented by the formula (II): ##STR1## wherein A.sub.1 and A.sub.2, which may be the same or different, each represents an aryl group or a heterocyclic group and A.sub.1 and A.sub.2 may combine together to form a heterocyclic ring or a fluorene ring, the ring B represents an aromatic hydrocarbon ring or a heterocyclic ring, and Y represents a hydrogen atom, an aliphatic group, an aryl group, a heterocyclic group, an amino group, an amido group, an oxy group or a thio group, but at least one of A.sub.1 and A.sub.2 or the ring formed by the combination of A.sub.1 and A.sub.2 represents an electron donating aryl group or an electron donating heterocyclic group, and a process for preparing the thiazine derivatives represented by the formula (II) by oxidizing a thioamide derivative represented by the formula (I): ##STR2## wherein A.sub.1, A.sub.2, B and Y are as above described.Type: GrantFiled: December 17, 1976Date of Patent: October 10, 1978Assignee: Fuji Photo Film Co., Ltd.Inventors: Hideo Usui, Sadao Ishige, Keiso Saeki
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Patent number: 4090020Abstract: Thienothiazine derivatives of the formula ##STR1## wherein R.sub.1 is lower alkyl; R.sub.2 is an unsubstituted aromatic heterocyclic radical which contains from 1 to 4 hetero atoms or one which is substituted by one or two lower alkyl groups, or is an unsubstituted phenyl radical or one substituted by halogen, hydroxy, lower alkyl, nitro, trifluoromethyl or lower alkoxy; and R.sub.3 and R.sub.4, independently, are hydrogen or lower alkyl,Prepared inter alia, from novel intermediates, are described. The end products are useful as anti-inflammatory, analgesic and anti-rheumatic agents.Type: GrantFiled: February 9, 1977Date of Patent: May 16, 1978Assignee: Hoffmann-La Roche Inc.Inventors: Dieter Binder, Otto Hromatka, Rudolf Pfister, Paul Zeller
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Patent number: 4076709Abstract: The present invention relates to compounds of the formula ##STR1## wherein A together with the two carbon atoms to which it is attached forms the group ##STR2## AND THE BROKEN LINE REPRESENTS THE DOUBLE BOND IN GROUP (A); R.sub.1 represents a lower alkyl group; R.sub.2 represents the residue of an aromatic heterocyclic ring containing from 1 to 4 hetero atoms, which may be substituted by one or two lower alkyl groups, or a phenyl group which may be substituted by halogen, hydroxy, lower alkyl, trifluoromethyl or lower alkoxy and R.sub.3 and R.sub.4 each represent a hydrogen atom or a lower alkyl group.Also provided are methods for their preparation. The thienothiazine derivatives provided by this invention have anti-flammatory, analgesic and antirheumatic activity.Type: GrantFiled: August 21, 1975Date of Patent: February 28, 1978Assignee: Hoffmann-La Roche Inc.Inventors: Otto Hromatka, Dieter Binder, Rudolf Pfister, Paul Zeller