Additional Chalcogen Attached Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/488)
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Patent number: 5585486Abstract: Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is (CR.sub.5 R.sub.6).sub.n, (CR.sub.5 R.sub.6).sub.n,-aryl, (CR.sub.5 R.sub.6).sub.n -heteroaryl, X-(CR.sub.5 R.sub.6).sub.n, X-(CR.sub.5 R.sub.6).sub.n -aryl or X-(CR.sub.5 R.sub.6).sub.n -heteroaryl wherein aryl and heteroaryl may be optionally substituted;X is 0 or NR.sub.5 ;R.sub.5 and R.sub.6 are independently H or lower alkyl;R.sub.2 is H, halo, lower alkyl or (CR.sub.5 R.sub.6).sub.n -aryl;R.sub.3 and R.sub.4 are independently H or alkyl;A is a D or L isomer of an amino acid selected from the group consisting of alanine, valine, leucine, isoleucine, proline, phenylalanine, glycine, tyrosine, methionine, asparagine, glutamine, aspartic acid, glutamic acid, lysine, arginine, histidine and .beta.-thienylalanine;Z is CH.sub.2 or O; andn is 0-4;pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1.beta.Type: GrantFiled: May 12, 1995Date of Patent: December 17, 1996Assignee: Sterling Winthrop Inc.Inventors: Roland E. Dolle, Todd L. Graybill, Gary J. Speier, Catherine P. Prouty, Stanley J. Schmidt
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Patent number: 5463083Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i,e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. Also disclosed is a method to treat disorders mediated by PAF and/or leukotrienes that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, to a patient in need of such therapy.Type: GrantFiled: January 6, 1994Date of Patent: October 31, 1995Assignee: Cytomed, Inc.Inventors: Tesfaye Biftu, Xiong Cai, Sajjet Hussion, Gurmit Grewal, T. Y. Shen
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Patent number: 5457237Abstract: Certain dihydroxyindanone compounds, and their pharmaceutically-acceptable salts, are inhibitors of tyrosine kinase enzymes, and so are useful for the control of tyrosine kinase dependent diseases (e.g., cancer, atherosclerosis).Type: GrantFiled: November 23, 1993Date of Patent: October 10, 1995Assignee: Pfizer Inc.Inventor: Robert L. Dow
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Patent number: 5439925Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function. Use is in human and veterinary medicine and in cosmetics.Type: GrantFiled: December 16, 1993Date of Patent: August 8, 1995Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)Inventors: Jean-Michel Bernardon, Willliam R. Pilgrim
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Patent number: 5434151Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.Type: GrantFiled: August 24, 1992Date of Patent: July 18, 1995Assignee: CytoMed, Inc.Inventors: Xiong Cai, Sajjat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
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Patent number: 5359080Abstract: There is disclosed an acylacetamide-type yellow coupler having an acyl group represented by formula (I) and a silver halide color photographic material containing same. ##STR1## wherein R.sub.1 represents a monovalent group, Q represents a group of non-metallic atoms required to form together with the C a substituted or unsubstituted 3- to 5-membered cyclic hydrocarbon group or a substituted or unsubstituted 3- to 5-membered heterocyclic group having in the group at least one hetero atom selected from a group consisting of N, 0, S, and P, provided that R.sub.1 is not a hydrogen atom and does not bond to Q to form a ring.Type: GrantFiled: February 12, 1993Date of Patent: October 25, 1994Assignee: Fuji Photo Film Co., Ltd.Inventors: Yoshio Shimura, Hidetoshi Kobayashi, Yasuhiro Yoshioka
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Patent number: 5358938Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl terahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiphenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.Type: GrantFiled: July 13, 1992Date of Patent: October 25, 1994Assignee: CytoMed, Inc.Inventors: Xiong Cai, Saijat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
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Patent number: 5234946Abstract: The substituted alkylamine derivatives represented by formula (I) ##STR1## wherein R.sup.1 represents (a) substituted or unsubstituted C.sub.2-6 alkenyl group, (b) substituted or unsubstituted C.sub.3-6 cycloalkenyl group, (c) substituted or unsubstituted C.sub.2-6 alkynyl group, (d) substituted or unsubstituted aryl group, (e) substituted or unsubstituted heterocyclic group, (f) fused heterocyclic group which may be substituted, or (g) group represented by the formula Ru.sup.11 -Ar wherein R.sup.11 is a heterocyclic group and Ar is a 5- or 6-membered aromatic ring which may contain a hetero N, O or S atom, and which may be substituted; ##STR2## represents a 5- or 6-membered aromatic ring which may contain a hetero N, O or S atom, and may be substituted by R.sup.7,X and Y are linking groups,R.sup.2 is H or lower alkyl,R.sup.3 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl or lower cycloalkyl,R.sup.4 and R.sup.5 are independently hydrogen or halogen atoms,R.sup.Type: GrantFiled: August 30, 1991Date of Patent: August 10, 1993Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Hiroshi Takezawa, Masahiro Hayashi, Yoshikazu Iwasawa, Masaaki Hosoi, Yoshiaki Iida, Yoshimi Tsuchiya, Masahiro Horie, Toshio Kamei
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Patent number: 5235068Abstract: Acylaromatic compounds ##STR1## (Q: aromatic compound residue; R: straight, branched or cyclic aliphatic group, aromatic group or araliphatic group) are prepared in high yield by a reaction, in the presence of a boron trifluoride complex catalyst, of an aromatic compound with ##STR2## (X: H, Cl, Br; Y: Cl, Br) or with RCOOH in the presence of (XYCHCO).sub.2 O.Type: GrantFiled: July 21, 1992Date of Patent: August 10, 1993Assignee: Sumitomo Chemical Company, LimitedInventors: Masayoshi Minai, Michitada Kondo, Yuji Ueda, Seiichi Kai, Takayuki Higashii
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Patent number: 5206389Abstract: These acrylates are those of formulae: ##STR1## where R=C.sub.1 -C.sub.12 alkyl, C.sub.5 -C.sub.12 cycloalkyl, aryl, arylalkyl or alkylaryl; Y=C.sub.1 -C.sub.12 alkyl, C.sub.6 -C.sub.12 aryl, heterocyclic radical whose ring contains from 5 to 10 members and whose heteroatom is chosen from N, O and S, an alkylaryl in which the alkyl part contains from 1 to 4 carbon atoms, Y not being able to denote 1,4-phenylene when R denotes methyl; and Z=hydrocarbon radical containing at least 2 C forming with O and the 2 adjacent Cs a ring containing from 4 to 8 members.To prepare them, an acrylate of formula CH.sub.2 .dbd.CH--COOR is reacted with a dialdehyde OHC--Y--CHO in the presence of an effective quantity of at least one functionalisation catalyst.The invention also relates to the preparation of new polymers and copolymers from the said acrylates.Type: GrantFiled: June 27, 1991Date of Patent: April 27, 1993Assignee: AtochemInventors: Marie-Christine Berthe, Paul Caubere, Yves Fort
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Patent number: 5189187Abstract: A clerodane-type diterpene derivative, which has antibacterial and antitumor activities, as well as chemically equivalent tautomers thereof and a process for producing said derivative using a microorganism belonging to the genus Streptomyces.Type: GrantFiled: June 24, 1992Date of Patent: February 23, 1993Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Hirofumi Nakano, Shozo Kawada, Yoichi Uosaki, Yutaka Saito, Katsushige Gomi, Toshiaki Iwazaki
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Patent number: 5183818Abstract: The present invention provides compounds having the structureY-Het-[Q.sub.1 ]-X-[Q.sub.2 ]-Zwhich inhibit the catalytic action of lipoxygenase enzymes, particularly 5-lipoxygenase, and thereby reduce the biosynthesis of leukotrienes B.sub.4, C.sub.4, D.sub.4, and E.sub.4.In the generic formula given above, X is oxygen or sulfur and Het is a heteroaryl group selected from the group consisting of furyl, thienyl, 2-, 3-, and 4-pyridyl, 2- and 3-benzo[b]furyl, 2- and 3-benzo[b]thienyl and thienothienyl.Y is one or two substituents independently selected from hydrogen, hydroxy, halogen, cyano, alkyl, haloalkyl, alkoxy, alkylthio, alkoxyaryl), alkylthioaryl, arylalkoxy, arylalkylthio, aryloxy, arylthio, alkylamido, cycloalkyl, alkanoyl, alkoxycarbonyl, amino, alkylamino, dialkylamino, and the following groups wherein R, at each occurrence, is independently selected from hydrogen and alkyl of from one to six carbon atoms: --CRROR, --NRC(O)R, --NRC(O)OR, and --C(O)NRR.The group Q.sub.Type: GrantFiled: August 27, 1991Date of Patent: February 2, 1993Assignee: Abbott LaboratoriesInventors: Dee W. Brooks, Andrew O. Stewart, Jonathan G. Martin
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Patent number: 5166369Abstract: Novel compounds are disclosed of the derivatives of furan having the formula ##STR1## wherein R.sub.4 consists essentially of hydrogen and C.sub.1 -C.sub.6 alkyl, and W is either carbonyl or carbinol and N is from 3-5.Type: GrantFiled: August 21, 1990Date of Patent: November 24, 1992Assignee: American Cyanamid CompanyInventor: Middleton B. Floyd, Jr.
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Patent number: 5112382Abstract: Compounds of the formula ##STR1## wherein A is selected from the group consisting of (1) phenyl, (2) naphthyl, (3) phenyl substituted with one or more halo, cyano, (C.sub.1 -C.sub.4) alkyl, nitro, (C.sub.1 -C.sub.4)haloalkyl, and (C.sub.1 -C.sub.4)thioalkyl, (4) naphthyl substituted with one or more halo, cyano, (C.sub.1 -C.sub.4)alkyl,nitro,(C.sub.1 -C.sub.4), and (C.sub.1 -C.sub.4) thioalkyl, (5) thiophene, (6) furan, (7) thiophene substituted with one or more substituents selected from halo and nitro, and (8) furan substituted with one or more substituents selected from halo and nitro;R disclose as microbicidally and fungicidally active.Type: GrantFiled: May 24, 1990Date of Patent: May 12, 1992Assignee: Rohm and Haas CompanyInventor: Adam C. Hsu
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Patent number: 5091426Abstract: A method of preventing epileptic seizures in a human or lower animal subject susceptible to said seizures, comprising systemically administering to said subject a safe and effective amount of a compound of the formula: ##STR1## wherein (a) X is halo or nil, and Y is a substituent selected from the group consisting of unsubstituted or halogen-substituted methyl, halo, nitro, amino, and methoxy; and(b) R is R.sup.1 C(O)OH, R.sup.1 C(O)N(R.sup.2).sub.2, or R.sup.1 N(R.sup.2).sub.2 ; whereR.sup.1 is C.sub.1 -C.sub.3 alkylene which is unsubstituted or substituted with C.sub.1 -C.sub.2 alkyl; andeach R.sup.2 is, independently, hydrogen or lower alkyl; orboth R.sup.2 groups are connected to form a saturated 5- or 6-membered heterocycle containing 1 or 2 heteroatoms, wherein one of which is nitrogen and the other is selected from oxygen and nitrogen and said heterocycle is unsubstituted or substituted with lower alkyl or hydroxy-substituted lower alkyl;or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: June 23, 1989Date of Patent: February 25, 1992Assignee: Norwich Eaton Pharmaceuticals, Inc.Inventor: Stanford S. Pelosi, Jr.
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Patent number: 5055471Abstract: This invention relates to derivatives of propanoic acid of the formula ##STR1## Useful as fungicides, insecticides and miticides, to processes for preparing them, to compositions containing them, and to methods of using them to combat fungi, especially fungal infections of plants, and to kill or control insects and mites.Type: GrantFiled: November 15, 1989Date of Patent: October 8, 1991Assignee: Imperial Chemical Industries PLCInventors: Paul J. de Fraine, Anne Martin
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Patent number: 5053400Abstract: The invention relates to carbacyclin derivatives of Formula I ##STR1## wherein the various substituents are defined herein, including, inter alia,if R.sub.2 means a hydrogen atom,their salts with physiologically compatible bases, their cyclodextrin clathrates, processes for their preparation, and their use as medicinal agents.Type: GrantFiled: March 22, 1989Date of Patent: October 1, 1991Assignee: Schering AktiengesellschaftInventors: Helmut Vorbruggen, Ulrich Klar, Bob Nieuweboer, Claus-Steffen Sturzebecher
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Patent number: 5039685Abstract: Novel O-alkylated oximes of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are optionally substituted aromatic or heteroaromatic rings, R.sup.3 is hydrogen or lower alkyl, R.sup.4 is a nitrogen containing, substituted ring or an amino group carrying a substituted ring, and n and m independently are 0, 1 or 2, are potent inhibitors of GABA reuptake from the synaptic cleft.Type: GrantFiled: May 10, 1989Date of Patent: August 13, 1991Assignee: Novo Nordisk A/SInventors: Lars J. S. Knutsen, Knud E. Andersen, Anker S. Jorgensen, Ursula Sonnewald
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Patent number: 5010104Abstract: Novel tricyclic compounds having a TXA.sub.2 -antagonizing activity represented by formul (I): ##STR1## which strongly antagonize an action of thromboxane A.sub.2 and are expected to have preventive and therapeutic effects on ischemica diseases, cerebro-vascular diseases, etc.Type: GrantFiled: June 29, 1989Date of Patent: April 23, 1991Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
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Patent number: 5008290Abstract: The invention relates to new sulphonamidoethyl compounds having valuable pharmacological properties, particularly anti-thrombotic properties, and which are also thromboxane antagonists.Type: GrantFiled: March 3, 1989Date of Patent: April 16, 1991Assignee: Dr. Karl Thomae GmbHInventors: Armin Heckel, Josef Nickl, Erich Muller, Berthold Narr, Johannes Weisenberger, Wolfgang Eisert, Thomas Muller
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Patent number: 4980371Abstract: Furan ketone derivatives thereof having antiretrovirus activity and effective in a method of treatment of a retrovirus infection, have the formula ##STR1## wherein Y is a bond, oxygen or divalent sulfur; n is 0 or 1; R is a straight or branched C.sub.8-20 alkyl chain or a straight or branched C.sub.8-20 alkenyl chain having from 1 to 4 double bonds; and R.sub.1 is C.sub.1-6 alkyl.Type: GrantFiled: November 27, 1989Date of Patent: December 25, 1990Assignee: Merrell Dow PharmaceuticalsInventors: Roger A. Parker, Sai P. Sunkara
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Patent number: 4977185Abstract: Novel furan ketone derivatives having antiretrovirus activity and effective in a method of treatment of a retrovirus infection, have the formula ##STR1## wherein Y represents a bond, oxygen or divalent sulfur; Ar represents phenyl or naphthylenyl; n is 0 or 1; m is an integer of from 4 to 10; and R.sub.1 represents C.sub.1-6 alkyl.Type: GrantFiled: November 27, 1989Date of Patent: December 11, 1990Assignee: Merrell Dow PharmaceuticalsInventors: Roger A. Parker, Sai P. Sunkara
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Patent number: 4977283Abstract: A process for the oxidation of 5-hydroxymethylfurfural which comprises oxidizing 5-hydroxymethylfurfural in an aqueous medium with oxygen in the presence of a catalyst which contains at least one metal of the platinum group.Type: GrantFiled: July 27, 1989Date of Patent: December 11, 1990Assignee: Hoechst AktiengesellschaftInventors: Ernst I. Leupold, Matthias Wiesner, Merten Schlingmann, Knut Rapp
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Patent number: 4973715Abstract: This invention relates to novel furan polyols, which are characterized in that they are the product of reaction of a strain selected from the group or consisting of a polyalcohol, a monoamine or polyamine, said polyalcohol or said amine possibly containing a furan cycle and mixtures thereof with a chain extension agent constituted by an organic epoxide, with the proviso that this organic epoxide is a furannic oxiran when this polyalcohol does not contain a furan cycle with the exclusion of 2,5(bis-hydroxy)furan as sole strain, when the chain extension agent does not contain any furan cycle. These furan polyols are used for the preparation of polyurethane foams having improved properties.Type: GrantFiled: August 22, 1988Date of Patent: November 27, 1990Assignee: Centre Scientifique et Technique du BattmentInventors: Gabriel Roux, Janine Rivero, Alessandro Gandini
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Patent number: 4927835Abstract: Compounds of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof, wherein: R.sup.1 is cycloalkyl of 5 to 7 carbon atoms; aryl of 6 to 10 carbon atoms unsubstituted or substituted by straight or branched chain alkyl of 1 to 4 carbon atoms, halo or trifluoromethyl; or ##STR2## wherein A is oxygen, sulfur or NR.sup.5, wherein R.sup.5 is hydrogen, straight or branched chain alkyl of 1 to 4 carbon atoms or halo, and R.sup.6 is hydrogen, straight or branched chain alkyl of 1 to 4 carbon atoms or halo;R.sup.2 is straight or branched chain alkyl of 1 to 4 carbon atoms or cycloalkyl of 5 to 7 carbon atoms; andR.sup.3 and R.sup.4 are the same or different and each is hydrogen; straight or branched chain alkyl of 1 to 8 carbon atoms unsubstituted or substituted by hydroxy, acyloxy of 2 to 5 carbon atoms, carboxyl or carbamoyl;are useful for treating pain, inflammation and fever in humans and animals.Type: GrantFiled: March 1, 1989Date of Patent: May 22, 1990Assignee: Nippon Shinyaku Co., Ltd.Inventors: Masahiro Kise, Yoshihiko Yoshimoto, Hiroshi Fujisawa, Yasuo Sasaki, Shoji Yasufuku
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Patent number: 4885311Abstract: Esters and amides of 13-trans-retinoic acid are disclosed which are used for the treatment of acne and skin diseases.Type: GrantFiled: June 29, 1987Date of Patent: December 5, 1989Assignee: Molecular Design InternationalInventors: Harlie A. Parish, William P. Purcell
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Patent number: 4870100Abstract: 2-benzylfuryl compounds of the general formula I ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are identical or different substituents and are each hydrogen, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, haloalkylthio, alkenyl or haloalkenyl, each of not more than 6 carbon atoms, n being 1, 2 or 3 where R.sup.3 is not hydrogen, and R.sup.4 and R.sup.5 are each hydrogen or alkyl of not more than 6 carbon atoms, R is --CHO or CHR.sup.6 OA, R.sup.6 is hydrogen, cyano, alkyl, alkenyl, haloalkenyl or alkynyl, each of not more than 6 carbon atoms, or carboxamide, and A is either hydrogen or a radical of an acid typical for pyrethroids, with the proviso that R.sup.2 is not hydrogen, chlorine, bromine, methyl or methoxy when R.sup.1 is hydrogen or methyl and R.sup.3 and A are each hydrogen, and furthermore with the proviso that R.sup.1 and R.sup.2 are not methyl when A is a radical of tetramethylcyclopropanecarboxylic acid, and finally with the proviso that R.sup.2 is not methyl, chlorine, bromine or methoxy and R.Type: GrantFiled: December 11, 1986Date of Patent: September 26, 1989Assignee: BASF AktiengesellschaftInventors: Bernd Wolf, Hans Theobald, Rainer Becker, Norbert Goetz, Walter Himmele, Rudolf Kropp
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Patent number: 4870076Abstract: The invention relates to new sulphonamido-ethyl compounds having the following structure: ##STR1## wherein R.sub.1 is substituted or unsubstituted phenyl, benzyl, nitrophenyl, acetamidophenyl or thienyl, R.sub.2 is hydroxycarbonyl or alkoxycarbonyl bonded via alkylene or alkenylene, or a 4,5-dihydro-pyridazin-3-one-6-yl or pyridazin-3-on-6-yl group optionally substituted on a ring carbon by C.sub.1 -C.sub.3 alkyl and X is substituted or unsubstituted imino, oxygen or sulphur, which compounds may be used to prevent arteriosclerosis or tumor metastasis, and are antitrombotic and thromboxane antagonists.Type: GrantFiled: September 3, 1987Date of Patent: September 26, 1989Assignee: Karl Thomae GmbHInventors: Armin Heckel, Josef Nickl, Erich Muller, Berthold Narr, Johannes Weisenberger, Wolfgang Eisert, Thomas Muller
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Patent number: 4820823Abstract: In accordance with a process of the present invention, .alpha.-keto acids of the general formula RCOCOOH wherein R is aryl, alkenyl or heterocyclic group, can be obtained through one-step carbonylation reaction of an organic halogenide of the general formula RX wherein R is the same as above and X is a halogen atom, with carbon monoxide and water in the presence of a basic compound and a palladium containing catalyst.Type: GrantFiled: February 21, 1986Date of Patent: April 11, 1989Assignee: Director-General of Agency of Industrial Science and TechnologyInventors: Masato Tanaka, Toshiaki Kobayashi, Toshiyasu Sakakura
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Patent number: 4812585Abstract: 2-Acylfuran derivatives ##STR1## (R: alkyl, phenyl, etc.; R.sub.1 : H, alkyl) are prepared in high yield by reaction, in the presence of a boron trifluoride complex catalyst, of a furan compound ##STR2## (X: H, Cl, Br; Y: Cl, Br) or with RCOOH in the presence of (XYCHCO).sub.2 O.Type: GrantFiled: October 15, 1987Date of Patent: March 14, 1989Assignee: Sumitomo Chemical Company, LimitedInventors: Michitada Kondo, Masayoshi Minai, Seiichi Kai, Takayuki Higashii, Yuji Ueda
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Patent number: 4792606Abstract: A process for the preparation of a dimeric aromatic acyl cyanide of the formula ##STR1## in which Ar is optionally substituted phenyl, naphthyl or hetaryl,comprising reaction an acyl halide of the formulaAr--CO--Halin whichHal is fluorine, chlorine or bromine, with an alkali metal cyanide in a two-phase system comprising water and a water-immiscible or only sparingly water-miscible aliphatic ketone, and in the presence of a phase-transfer catalyst. The products are known intermediates for pesticides.Type: GrantFiled: July 16, 1987Date of Patent: December 20, 1988Assignee: Bayer AktiengesellschaftInventors: Reinhard Lantzsch, Hermann-Dieter Krall
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Patent number: 4746350Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein: Y is selected from phenyl, furyl, thienyl and pyrrolyl rings (each optionally substituted by group X), optionally branched alkylene or alkylenethio(oxy)alkylene;X which may be the same or different are independently selected from halogen, nitro, alkyl, substituted alkyl, hydroxy, alkoxy, carboxy, alkoxycarbonyl, alkylthio, sulfamoyl, substituted sulfamoyl, amino, substituted amino and alkanoyl;R.sup.1 is selected from hydrogen, acyl and an inorganic or organic cation;R.sup.2 is selected from alkyl, substituted alkyl, alkenyl, haloalkenyl and alkynyl;R.sup.3 is selected from alkyl; andR.sup.4 is selected from hydrogen, alkyl, and alkoxycarbonyl.Type: GrantFiled: April 14, 1986Date of Patent: May 24, 1988Assignee: Imperial Chemical Industries PLCInventor: Keith G. Watson
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Patent number: 4736055Abstract: Oxime sulfonates of formula I ##STR1## wherein Y is a polymerizable unsaturated group or epoxide group or an --OH, --NHR.sup.5, --COOH, COOR.sup.6, --COCl, --CH.sub.2 Hal, --SO.sub.2 Cl or --NCO group, Z is an (x+y)-valent connecting member, R.sup.1 and R.sup.2 are monovalent organic radicals, m is 0 or 1, x is 1 or 2 and y is 1 or 2, can be converted into polymers which can be thermally or photochemically dissociated to form free sulfonic acid groups. Said polymers can therefore be used as photoresists which can be developed with aqueous alkalis.Type: GrantFiled: April 11, 1986Date of Patent: April 5, 1988Assignee: Ciba-Geigy CorporationInventors: Kurt Dietliker, Werner Rutsch, Godwin Berner, Max Hunziker, Christopher G. Demmer
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Patent number: 4680306Abstract: Spiro-imidazolones are disclosed which are useful as aldose reductase inhibitors and as therapeutic agents for the treatment of complications arising from diabetes. Pharmaceutical compositions containing the spiro compounds and a method of treating diabetic complications are also disclosed.Type: GrantFiled: March 14, 1986Date of Patent: July 14, 1987Assignee: Pfizer Inc.Inventor: Christopher A. Lipinski
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Patent number: 4677120Abstract: Esters and amides of 13-cis-retinoic acid are disclosed which are used for the treatment of acne and skin diseases.Type: GrantFiled: July 31, 1985Date of Patent: June 30, 1987Assignee: Molecular Design InternationalInventors: Harlie A. Parish, William P. Purcell
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Patent number: 4665174Abstract: A process for preparing cyclopentenone derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl or lower alkenyl, R.sup.2 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, substituted or unsubstituted aryl or substituted or unsubstituted ar(lower)alkyl and A is the residue of a nucleophilic agent from which a hydrogen atom is excluded, which comprises reacting a 3-hydroxy-4-cyclopentenone compound of the formula: ##STR2## wherein R.sup.1 and R.sup.2 are each as defined above with a nucleophilic agent of the formulaA--H (III)wherein A is as defined above.The cyclopentenone derivatives of the formula (I) are useful as pharmaceuticals, agricultural chemicals, perfumes and as intermediates for the preparation of agricultural chemicals, pharmaceuticals and perfumes.Type: GrantFiled: May 11, 1982Date of Patent: May 12, 1987Assignee: Sumitomo Chemical Company, LimitedInventors: Masayoshi Minai, Tadashi Katsura
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Patent number: 4643849Abstract: This invention relates to amine derivatives and salts thereof. These compounds have an anti-ulcer activity which is effective to human beings and animals. This disclosure relates to such compounds, a process for the preparation thereof and an anti-ulcer agent containing the same.Type: GrantFiled: November 14, 1983Date of Patent: February 17, 1987Assignee: Toyama Chemical Co., Ltd.Inventors: Shiro Hirai, Hiroshi Hirano, Hirotoshi Arai, Yasuo Kiba, Hisanari Shibata, Yoshikazu Kusayanagi, Minako Yotsuji, Kazuhiko Hashiba, Kikuko Tanada
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Patent number: 4636575Abstract: Compounds of formula II and X ##STR1## wherein X is O, S, SO.sub.2, methylene, isopropylidene or NCOR.sub.7 where R.sub.7 is alkyl or phenyl, Y is a direct bond or methylene, n is 1 or 2, R.sub.4 is alkyl, phenyl, naphthyl, cycloalkyl, aralkyl, camphoryl, CF.sub.3, CCl.sub.3, F or NH.sub.2 ; or is alkylene, phenylene or naphthylene, R.sub.5 is hydrogen or halogen, R.sub.6 is hydrogen, alkyl, phenyl or cyano, R.sub.8 is substituted phenyl, substituted naphthyl, anthryl or phenanthryl, R.sub.9 is alkyl R.sub.10 is alkyl or substituted phenyl, and R.sub.11 is alkyl, substituted phenyl, naphthyl, camphoryl, alkylene, phenylene or naphthylene, are latent curing catalysts for acid-curable stoving lacquers. They are distinguished by satisfactory solubility in the acid-curable resin systems, can be stored virtually indefinitely in the dark and, when exposed to shortwave light, make it possible to cure the resins by acid catalysts at a relatively low temperature.Type: GrantFiled: December 17, 1984Date of Patent: January 13, 1987Assignee: Ciba-Geigy CorporationInventor: Rudolf Kirchmayr
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Patent number: 4629802Abstract: A novel process for producing sulfonylureas of the formula I having a herbicidal action and an action regulating plant growth ##STR1## wherein A is an unsubstituted or substituted phenyl, naphthyl, furan, thiophene or pyridine group, E is a nitrogen atom or the methine group, R.sub.a is hydrogen, halogen, C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -haloalkyl, C.sub.1 -C.sub.5 -alkoxy, C.sub.1 -C.sub.5 -haloalkoxy, C.sub.1 -C.sub.5 -alkylthio or C.sub.2 -C.sub.10 -alkoxyalkoxy, and R.sub.b is the same as R.sub.Type: GrantFiled: March 1, 1985Date of Patent: December 16, 1986Assignee: Ciba-Geigy CorporationInventors: Haukur Kristinsson, Werner Topfl
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Patent number: 4622337Abstract: New insecticides are of formula: ##STR1## wherein R.sup.1 represents hydrogen or a methyl group; R.sup.2 represents hydrogen or a halogeno or lower alkyl group; R.sup.3 represents hydrogen or a halogeno or carbo(lower alkoxy) group which contains at least 2 carbon atoms in the lower alkoxy residue when R.sup.2 represents methyl; with the proviso that (a) R.sup.2 and R.sup.3 each represent hydrogen only when R.sup.1 represents methyl, (b) when R.sup.1 and R.sup.3 each represent hydrogen and R.sup.2 represents alkyl, that alkyl group contains at least 2 carbon atoms and (c) when R.sup.3 represents halogeno, R.sup.2 represents hydrogen or halogeno; and R represents a group which forms insecticidal esters with chrysanthemic acid e.g. 5-benzyl-3-furylmethyl, 3-phenoxybenzyl, .alpha.-cyano-3-phenoxybenzyl.Type: GrantFiled: May 22, 1984Date of Patent: November 11, 1986Assignee: National Research Development CorporationInventors: Michael Elliott, Norman F. Janes, David A. Pulman
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Patent number: 4602023Abstract: The present invention provides various novel diphenic acid monoamide compounds, novel pharmaceutical compositions and methods of use thereof, as well as novel methods of synthesis therefor. The novel diphenic acid monoamides of the present invention are leukotriene antagonists, 5-lipoxygenase inhibitors, and mediator release inhibitors providing activity useful for treating asthma, allergies, cardiovascular diseases, migraines, and immunoinflammatory conditions.Type: GrantFiled: June 3, 1985Date of Patent: July 22, 1986Assignee: Warner-Lambert CompanyInventors: John S. Kiely, Suchin Huang
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Patent number: 4590283Abstract: The invention relates to a process for manufacturing 5-hydroxymethylfurfural consisting of bringing a hexose into contact with a catalytic support in the form of a solution of said hexose in a strongly polar aprotic solvent, particularly dimethylsulfoxide, the 5-hydroxymethylfurfural formed being extracted by means of a solvent for the latter also brought into contact with the catalytic support. All of the operations are carried out preferably continuously, particularly by the counter-current principle.Type: GrantFiled: September 14, 1984Date of Patent: May 20, 1986Assignee: Roquette FreresInventors: Antoine Gaset, Luc Rigal, Gilles Paillassa, Jean-Paul Salome, Guy Fleche
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Patent number: 4535092Abstract: Acylanilides of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are substituents defined in claim 1; wherein R.sup.4 is hydrogen or alkyl of up to 4 carbon atoms, or is joined to R.sup.5 as stated below;wherein R.sup.5 is hydrogen, hydroxy, or alkoxy or acyloxy each of up to 15 carbon atoms, or is joined to R.sup.4 to form an oxycarbonyl group such that together with the --N--CO--C-- part of the molecule it forms an oxazolidinedione group;wherein R.sup.6 is alkyl or halogenoalkyl of up to 4 carbon atoms;and wherein R.sup.7 is 5- or 6- membered saturated or unsaturated heterocyclic which contains one, two or three hetero atoms selected from oxygen, nitrogen and sulphur, which heterocyclic may be a single ring or may be fused to a benzo-ring, and which heterocyclic is unsubstituted or bears one or two substituents defined in claim 1;processes for their manufacture and pharmaceutical compositions containing them. The compounds possess antiandrogenic activity.Type: GrantFiled: November 1, 1982Date of Patent: August 13, 1985Assignee: Imperial Chemical Industries PLCInventor: Leslie R. Hughes
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Patent number: 4518797Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is an acyl group or certain optionally halo-substituted hydrocarbyl groups, and X is --CH.sub.2 CH(OCH.sub.3).sub.2, --CH.sub.2 CHO, --CH.dbd.CHOR.sup.2 in which R.sup.2 is acyl, --CHO,--C(O)Cl, --C(O)Br or --C(O)OR in which R is H, a salt-forming cation, an alkyl group or the residue of a pyrethroid alcohol are new pesticides or intermediates therefore. The compounds are prepared using a multi-step synthesis starting from the natural terpene, 3-carene.Type: GrantFiled: March 15, 1979Date of Patent: May 21, 1985Assignee: Shell Oil CompanyInventor: Steven A. Roman
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Patent number: 4487934Abstract: A method of preparing substituted acylbenzenes is disclosed. The method comprises reacting selected acylhalides or equivalents with a selected poly-substituted benzene in the presence of an acylating catalyst comprising a perfluoro sulfonic acid polymer.Type: GrantFiled: June 6, 1980Date of Patent: December 11, 1984Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Linda L. Setescak
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Patent number: 4467101Abstract: Acylamido-3-cephem-4-carboxylic acid compounds of the formula ##STR1## in which the index n represents an integer of from 1 to 4,the index m represents 0 or 1,X represents oxygen, sulphur or an --NH-- group,W represents a --CO--, --CO--NHSO.sub.2 -- or --SO.sub.2 NH--CO-- group, orX-W together represent a --CO-- or --CO--NHSO.sub.2 -- group,A represents optionally substituted phenylene, thienylene or furylene,Y represents hydrogen, hydroxyl, formyloxy, amino or sulpho optionally present in salt form, andZ represents hydrogen, orY and Z together represent an oxo group or an .dbd.N--O--R.degree. group in which R.degree. represents hydrogen or optionally substituted lower alkyl,R.sub.1 represents hydrogen, lower alkyl, lower alkoxy, halogen or a group of the formula --CH.sub.2 --R.sub.2 in which R.sub.2 is a free, esterified or etherified hydroxy or mercapto group or a quaternary ammonium group, andR.sub.Type: GrantFiled: September 20, 1982Date of Patent: August 21, 1984Assignee: Ciba-Geigy CorporationInventors: Karoly Kocsis, Peter Schneider, Bruno Fechtig, Riccardo Scartazzini
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Patent number: 4459305Abstract: The present invention relates to a cyclopropanecarboxylic acid ester derivative of the general formula I: ##STR1## in which R.sub.1 stands for a hydrogen atom, a methyl group, a halogen atom or a halomethyl group, R.sub.1 ' stands for a halomethyl or haloethyl group, R.sub.2 and R.sub.2 ' are the same or different, each standing for methyl group, a halogen atom or a halomethyl group, provided that if R.sub.1 is a hydrogen atom, R.sub.1 ' is a halomethyl group, and R.sub.2 and R.sub.2 ' are each a methyl group, and R stands for a group of the formula II, III, IV, V or VI: ##STR2## in which R.sub.3 stands for a hydrogen atom or a methyl group, R.sub.4 stands for an allyl, propargyl, benzyl or 2,4-pentadienyl group, X stands for an oxygen or sulfur atom, or a --CH.dbd.CH-- group, R.sub.5 stands for a hydrogen atom, or a cyano, ethynyl, propynyl or trifluoromethyl group, R.sub.6 stands for a hydrogen or halogen atom or a methyl or trifluoromethyl group, n is an integer of 1 to 4, R.sub.Type: GrantFiled: December 4, 1981Date of Patent: July 10, 1984Assignee: Dainippon Sochugiku Kabushiki KaishaInventors: Yoshio Katsuda, Yoshihiro Minamite
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Patent number: 4440781Abstract: A method for producing a psychotropic response, especially for alleviating the symptoms of alcohol withdrawal, comprises administering to a human or animal subject in need thereof a psychotropically effective non-toxic amount of an oxyoctadecanoate. A composition for use in the present method is provided.Type: GrantFiled: June 11, 1982Date of Patent: April 3, 1984Assignee: The Vinoxen Company, Inc.Inventors: Herman P. Benecke, Bob E. Sherwood
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Patent number: 4416826Abstract: Peresters of the formula: ##STR1## wherein R is an alkyl group; and ##STR2## light-absorbing chromophore group; and use thereof as photoinitiators are provided.Type: GrantFiled: October 29, 1980Date of Patent: November 22, 1983Inventor: Douglas C. Neckers
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Patent number: 4411911Abstract: Novel sulfonate derivatives represented by the formulaR.sub.1 SO.sub.3 CH.sub.2 CO(CH.sub.2).sub.n R.sub.2act to inhibit esterases and chymotripsin and are useful as antilipemic agents, anti-inflammatory agents, immunity controlling agents, etc.Type: GrantFiled: January 19, 1981Date of Patent: October 25, 1983Assignee: Taiho Pharmaceutical Company, LimitedInventors: Setsuro Fujii, Toshihiro Hamakawa, Kazuo Ogawa, Yoshiyuki Muranaka, Sadao Hashimoto