Plural Hetero Rings Patents (Class 549/414)
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Patent number: 6028092Abstract: This invention relates to novel formulations of salts of certain benzopyran compounds, to compositions containing them and their use in the treatment of certain disorders.Type: GrantFiled: June 17, 1998Date of Patent: February 22, 2000Assignee: SmithKline Beecham p.l.cInventors: Christopher John Banton, Phillip Christopher Buxton
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Patent number: 5990313Abstract: Disclosed is a process for the preparation of 3-alkyltetrahydrofurans by a two-step process wherein 2,3-dihydrofuran is reacted with an acetal to form an intermediate compound which may be converted to a 3-alkyltetrahydrofuran by contacting the intermediate with hydrogen in the presence of a catalytic amount of a Group VIII noble metal or rhenium, water and a strong acid.Type: GrantFiled: September 29, 1998Date of Patent: November 23, 1999Assignee: Eastman Chemical CompanyInventor: William Anthony Beavers
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Aryl- and hetaryl-sulfonamide derivatives, their preparation and their use as endothelin antagonists
Patent number: 5962682Abstract: Compounds of formula (I) ##STR1## wherein R.sup.1 signifies phenyl, substituted phenyl or heterocyclyl; R.sup.2 signifies phenyl or substituted phenyl; R.sup.3 signifies hydrogen, lower-alkyl, cyano, carboxy, esterified carboxy, phenyl, substituted phenyl, heterocyclyl or a residue --CONR.sup.5 R.sup.6 or --NR.sup.5 COR.sup.7 ; R.sup.4 signifies hydrogen or lower-alkyl; R.sup.5 signifies hydrogen or a residue R.sup.7, and R.sup.6 signifies --(CH.sub.2).sub.m R.sup.7 ; or R.sup.5 and R.sup.6 together with the N atom associated with them signify a heterocyclic residue; R.sup.7 signifies phenyl, substituted phenyl, cycloalkyl, heterocyclyl, lower-alkyl, cyano-lower-alkyl, hydroxy-lower-alkyl, di-lower-alkylamino-lower-alkyl, carboxy-lower-alkyl, lower-alkoxycarbonyl-lower-alkyl, lower-alkoxycarbonylamino-lower-alkyl or phenyl-lower-alkoxycarbonyl; R.sup.a signifies hydrogen, lower-alkyl or hydroxy; R.sup.b signifies hydrogen or lower-alkyl; Z signifies hydroxy, amino or a residue --OR.sup.8, --OC(O)NHR.sup.Type: GrantFiled: August 18, 1997Date of Patent: October 5, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz -
Patent number: 5962499Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.Type: GrantFiled: March 23, 1998Date of Patent: October 5, 1999Assignee: Merck & Co., Inc.Inventors: Peter T. Meinke, Thomas Shih, Michael H. Fisher
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Patent number: 5942532Abstract: The invention relates to benzimidazole antibacterial compounds of the Formula I: ##STR1## as described herein, pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhibiting the action of a bacterial histidine protein kinase and are useful as anti-infective agents against a variety of bacterial organisms, including organisms which are resistant to other known antibiotics.Type: GrantFiled: September 5, 1997Date of Patent: August 24, 1999Assignee: Ortho Pharmaceutical CorporationInventors: Kwasi Adomako Ohemeng, Van Nhatton Nguyen
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Patent number: 5908581Abstract: A red fluorescent material includes a compound of the formula: ##STR1## wherein: R.sub.1, and R.sub.2 are individually alkyl of from 1 to 20 carbon atoms, aryl, carbocyclic and other heterocyclic systems; andR.sub.3, and R.sub.4 are individually alkyl of from 1 to 10 carbon atoms, and a branched or unbranched 5 or 6 member substituent ring connecting with R.sub.1, R.sub.2 respectively; andR.sub.5 is alkyl of from 2-20 carbon atoms; sterically hindered aryl and heteroaryl; andR.sub.6 is alkyl of from 1 to 10 carbon atoms, and a 5 or 6-member carbocyclic ring connecting with R.sub.5.Type: GrantFiled: April 7, 1997Date of Patent: June 1, 1999Assignee: Eastman Kodak CompanyInventors: Chin H. Chen, Kevin P. Klubek, Jianmin Shi
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Patent number: 5883106Abstract: Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having the following formula I: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Ar.sup.1 is a heterocyclic moiety which is selected from imidazolyl, pyrrolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, indolyl, indazolyl and benzimidazolyl, which is bonded to X.sup.1 through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, and C.sub.1-4 alkyl; X.sup.1 is a direct bond or C.sub.1-4 alkylene; Ar.sup.2 is phenylene optionally substituted with halo, hydroxy, cyano, and amino X.sup.2 is --A--X-- or --X--A-- wherein A is a direct bond or C.sub.1-4 alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar.sup.3 is phenylene, pyridylene, thienylene, furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino and C.sub.1-4 alkyl; R.sup.1 and R.sup.2 are each C.sub.Type: GrantFiled: February 6, 1998Date of Patent: March 16, 1999Assignee: Pfizer Inc.Inventors: Rodney W. Stevens, Takashi Mano, Kazunari Nakao, Yoshiyuki Okumura
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Patent number: 5869662Abstract: Benzopyran compounds represented by the formulas: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, and R.sub.10 are selected from hydrogen, a stable organic radical, a heterocyclic group, halogen, a nitrogen-substituted group, and a nitrogen-substituted ring compound.Type: GrantFiled: July 17, 1997Date of Patent: February 9, 1999Assignee: Vision-Ease Lens, Inc.Inventor: Frank J. Hughes
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Patent number: 5849216Abstract: Compounds of the formula (I)R.sup.1 --(A.sup.1).sub.a (--M.sup.1).sub.b --(--A.sup.2).sub.c (--M.sup.2).sub.d (--A.sup.3).sub.e (--M.sup.3).sub.f (--A.sup.4).sub.g --H(I)in which the symbols and indices have the following meanings:R.sup.1 is B or a straight-chain or branched alkyl radical having 1 to 22 carbon atoms (with or without an asymmetrical carbon atom) in which, in addition, it is possible for one or two non-adjacent --CH.sub.2 -- groups to be replaced by --O--, --S--, --CO--, --CO--O--, --O--CO--, --CO--S--, --S--CO--, --O--CO--O--, --CH.dbd.CH--, --C.tbd.C--, .DELTA. or --Si(CH.sub.3).sub.2 --, and in which, in addition, one or more hydrogen atoms of the alkyl radical may be substituted by F, Cl, Br or CN, or is a chiral group, for example an epoxide, a dioxolane or a cyclic lactone,--(A.sup.1).sub.a (--M.sup.1).sub.b --(--A.sup.2).sub.c (--M.sup.2).sub.d (--A.sup.3).sub.e (--M.sup.3).sub.f (--A.sup.4).sub.Type: GrantFiled: May 31, 1995Date of Patent: December 15, 1998Assignee: Hoechst AktiengesellschaftInventors: Gerd Illian, Anke Kaltbeitzel, Rainer Wingen, Hubert Schlosser
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Patent number: 5849550Abstract: A method for producing lysocellin in bead form comprises:(a) cultivating a lysocellin-producing microorganism in an aqueous nutrient-containing fermentation broth under lysocellin-producing conditions;(b) adding a base or inorganic phosphate to the fermentation broth within about the first 24 hours of the beginning of the fermentation in an amount sufficient to ensure that the lysocellin is produced in the form of a cation salt of lysocellin;(c) providing a lipid to the fermentation broth such that the lipid is present in the broth in a sufficient amount to form discrete beads with the lysocellin in the fermentation broth; and(d) separating the beads from the broth.Type: GrantFiled: June 30, 1995Date of Patent: December 15, 1998Assignee: Mallinckrodt Veterinary, Inc.Inventors: Donald R. Hahn, James R. McMullen, Vikram P. Mehrotra
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Patent number: 5847160Abstract: Compounds of the formula ##STR1## wherein R.sub.1 -R.sub.5 X, Y, A, B are as defined in the specification, have retinoid-like biological activity.Type: GrantFiled: September 4, 1997Date of Patent: December 8, 1998Assignee: AllerganInventors: Tae K. Song, Roshantha A. Chandraratna
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Patent number: 5844000Abstract: This invention relates to novel propenone oxime ethers, methods of preparing them and pharmaceutical compositions containing them. The compounds have the formula: ##STR1## wherein R.sup.1 is H, or glucuronide;R.sup.2 and R.sup.3 are independently H or methyl;R.sup.4 is 0, or glucuronide, andn is 0 or 1, provided that when R.sup.1 is H, n is 1.Type: GrantFiled: June 12, 1997Date of Patent: December 1, 1998Assignee: SanofiInventors: William Brian, Brian Folk, Juan Shi, Gerard Fabre, Claude Tronquet
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Patent number: 5834467Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.Type: GrantFiled: June 7, 1995Date of Patent: November 10, 1998Assignee: Agouron Pharmaceuticals, Inc.Inventors: Vincent J. Kalish, Bruce A. Dressman, James E. Fritz, Marlys Hammond, William J. Hornback, Stephen W. Kaldor, John E. Munroe, Siegfried Heinz Reich, John H. Tatlock, Timothy A. Shepherd, Michael J. Rodriquez
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Patent number: 5767297Abstract: A taxoid derivative wherein sugar is combined with any one of paclitaxel, docetaxel and 10-deacetyl-bacatin III via a spacer. A method of producing the taxoid derivative comprises protecting hydroxyl groups at specific position of paclitaxel or docetaxel by protective compound followed by reacting with tetrabenzyl acetyloxyglucoside, and then carrying out debenzyl and detriethylsilyl reactions. A method of producing the taxoid derivative comprises reacting paclitaxel or docetaxel with tetrabenzyl acetyloxyglucoside, and then carrying out debenzyl reaction.Type: GrantFiled: June 3, 1997Date of Patent: June 16, 1998Assignees: Ensuiko Sugar Refining Co., Ltd., Tadakatsu MANDAI, Kaken Pharmaceutical Co., Ltd.Inventors: Tadakatsu Mandai, Hiroshi Okumoto, Koji Hara, Katsuhiko Mikuni, Kozo Hara, Hiroki Hamada
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Patent number: 5760072Abstract: A paclitaxel prodrug has a paclitaxel portion coupled to a cleavable N-(aliphatic or aromatic)-O-glycosyl carbamate spacer group, and can be administered orally, topically or by injection to provide an anti-tumor effect, the prodrug being activated by a hydrolizing enzyme, an endogeneous enzyme or an exogeneous enzyme.Type: GrantFiled: September 30, 1996Date of Patent: June 2, 1998Assignee: Pharmachemie B.V.Inventors: Hendricus B. A. de Bont, Ruben G. G. Leenders, Johan W. Scheeren, Hidde J. Haisma, Dick de Vos
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Patent number: 5718845Abstract: Nonlinear optical compounds which contain a heteroaromatic ring and may further comprise a tricyanovinyl group attached to the heteroaromatic ring.Type: GrantFiled: January 18, 1995Date of Patent: February 17, 1998Assignee: Enichem S.p.A.Inventors: Kevin J. Drost, Pushkara Rao Varanasi, Kwan-Yue Alex Jen, Michael Anthony Drzewinski
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Patent number: 5719179Abstract: Disclosed is Compound GEX1 of formula (I), having excellent antitumor activity: ##STR1## wherein R.sup.1 represents hydroxy or ##STR2## R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen or hydroxy; R.sup.5 represents hydroxyl or lower alkoxy; provided that when R.sup.1 is hydroxy and R.sup.5 is methoxy, then at least one of R.sup.2, R.sup.3 and R.sup.4 is the group except for hydrogen, and pharmaceutically acceptable salts thereof.Type: GrantFiled: December 24, 1996Date of Patent: February 17, 1998Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Tamio Mizukami, Yasushi Sakai, Tetsuo Yoshida, Youichi Uosaki, Keiko Ochiai, Shiro Akinaga
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Patent number: 5708178Abstract: Novel acceptor-donor-acceptor and donor-acceptor-donor compounds for use in forming a thermally-stable electro-optic waveguide are disclosed. Also disclosed is a thermally stable waveguide material containing thermally stable acceptor-donor-acceptor or donor-acceptor-donor guest dipole compounds in a temperature-resistant polymer matrix. The waveguide has selected regions in which the net dipoles of the guest molecules are oriented, for electro-optic switching when an electric field is placed across these regions.Type: GrantFiled: September 20, 1996Date of Patent: January 13, 1998Assignee: Lockheed Martin CorporationInventors: Susan P. Ermer, Doris S. Y. Leung, Steven M. Lovejoy
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Patent number: 5674894Abstract: The current invention discloses novel amidine derivatives with nitric oxide donating property that can inhibit platelet aggregation and promote vasodilation in a single compound.Type: GrantFiled: May 15, 1995Date of Patent: October 7, 1997Assignee: G.D. Searle & Co.Inventors: Mark G. Currie, Foe S. Tjoeng, Mark E. Zupec
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Patent number: 5648376Abstract: An immunosuppressant compound is produced having the structure: ##STR1## or a mirror image thereof, wherein X.sub.1 is 2,2-dimethylvinyl and X.sub.2 and X.sub.3 together are .dbd.CH.sub.2 ; or X.sub.1 is 2,2-dimethyloxiranyl, and X.sub.2 and X.sub.3 together are --0--CH.sub.2 --; or X.sub.1 is 1,2-dihydroxy-2-methyl-propyl, X.sub.2 is --CH.sub.2 OH, and X.sub.3 is OH; or X.sub.1 is 2-hydroxy-2-methylpropyl, X.sub.2 is H, and X.sub.3 is CH.sub.2 OH; or X.sub.1 is COOR, and X.sub.2 and X.sub.3 together are .dbd.O, where R is a lower alkyl, phenyl, or benzyl group; or X.sub.1 is 2-methylpropyl, X.sub.2 is H, and X.sub.3 is CH.sub.3. The compound can be produced by culturing Fusarium subglutinans f. sp. tripterygii ATCC 74358 isolated from the stems of Tripterygium wilfordii. A pharmaceutical composition for immunosuppression therapy is prepared containing the compound and a pharmaceutically acceptable vehicle.Type: GrantFiled: January 19, 1995Date of Patent: July 15, 1997Assignee: Pharmagenesis, Inc.Inventors: Gary A. Strobel, Nathan B. Pliam
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Patent number: 5646147Abstract: Acaricidal, insecticidal and nematicidal substituted (hetero)arylalkyl ketone oxime O-ethers, processes for their preparation, agents containing them, and their use as pesticides.The invention relates to compounds of the formula ##STR1## in which Ar.sup.1 and Ar.sup.2 are aryl or heteroaryl, each of which is optionally substituted, and R is an optionally substituted aliphatic or alicyclic radical, to processes for their preparation, and to agents containing these compounds, and to their use for controlling animal pests.Type: GrantFiled: April 20, 1994Date of Patent: July 8, 1997Assignee: Hoechst AktiengesellschaftInventors: Birgit Kuhn, Gerhard Salbeck, deceased, Uwe Doller, Stefan Schnatterer, Hans-Herbert Schubert, Werner Knauf, Anna Waltersdorfer, Manfred Kern
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Patent number: 5597932Abstract: The invention is drawn to a compound having the following formula ##STR1## in which X.sup.1 and X.sup.2, which may be the same or different, represent hydrogen or a hydroxy-protecting group, X.sup.4 is hydrogen, A is selected from --COOAlkyl and CH.sub.2 OH, and B is a hydroxy group, or A and B, when taken together, represent an oxo group. These compounds are useful as intermediates in the production of 19-nor vitamin D derivatives.Type: GrantFiled: May 16, 1995Date of Patent: January 28, 1997Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Heinrich K. Schnoes, Kato L. Perlman, Rolf E. Swenson
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Patent number: 5594026Abstract: Two further crystalline polymorphic forms of the anti-infective agent mupirocin have been identified. Processes for the preparation thereof and the use thereof are described.Type: GrantFiled: April 18, 1995Date of Patent: January 14, 1997Assignee: SmithKline Beecham Group p.l.c.Inventors: Michael J. Greenway, Sarah D. Salt, Christopher E. Valder, Alan D. Curzons
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Patent number: 5565129Abstract: The polycarbonates of the present invention include those of sucrose series having a specific cyclic structure, those of oligosaccharide and monosaccharide series other than the sucrose series, those derived from specific saccharides having no cyclic structure, those having a skeletal structure of pentaerythritol, neopentyl glycol or trimethylolmethane, and specific dicarbonates.The lubricating oil and electrical insulating oil of the invention contain the above-mentioned polycarbonates.The polycarbonates of the invention are excellent in compatibility with Freon R-134a (HFC) as well as in lubricating properties, detergency and electrical insulating properties, and are capable of providing lubricating oil for refrigerator, automotive engine oil, automotive gear oil, lubricating oil for rolling and lubricating oil for fiber, especially lubricating oil for which electrical insulating properties are required, and electrical insulating oil.Type: GrantFiled: June 1, 1995Date of Patent: October 15, 1996Assignee: Mitsui Petrochemical Industries, Ltd.Inventors: Masahide Tanaka, Tadaaki Fujimoto, Tetsuo Hayashi, Takashi Hayashi, Kazunori Takahata
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Patent number: 5543534Abstract: Compounds of Formula 1 ##STR1## wherein X is S or O; R.sub.1 -R.sub.5, m, o, X, Y, A, B are as defined in the specification.Type: GrantFiled: December 29, 1994Date of Patent: August 6, 1996Assignee: AllerganInventors: Vidyasagar Vuligonda, Min Teng, Richard L. Beard, Alan T. Johnson, Yuan Lin, Roshantha A. Chandraratna
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Patent number: 5536745Abstract: Conformationally restricted aryl and heteroaryl ketones derived from monic acid have useful antibacterial properties.Type: GrantFiled: January 23, 1995Date of Patent: July 16, 1996Assignee: SmithKline Beecham p.l.c.Inventor: Neil D. Pearson
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Patent number: 5536850Abstract: The present invention relates to a novel substance DC114-A1 represented by the following formula (I): ##STR1##Type: GrantFiled: March 1, 1995Date of Patent: July 16, 1996Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Hirofumi Nakano, Noboru Fujii, Tamio Mizukami, Youichi Uosaki, Katsunori Kita, Eiji Kobayashi
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Patent number: 5525745Abstract: The invention describes intermediates for use in the synthesis of 1.alpha.-hydroxy-19-nor-vitamin D compounds. The intermediates have the following formula: ##STR1## The disclosed process includes (a) the construction of a 5,8-diol-6-yne intermediate by joining ring-A and ring-C/D portions of the desired end product via the condensation of an acetylenic derivative containing the C/D-ring portion of the desired end product with a cyclic dihydroxy ketone representing the A-ring of the desired end product; (b) the partial reduction of the 6,7 acetylenic triple bond linkage between the A and C/D ring portions to obtain a 5,8-diol-6-ene intermediate; and (c) the reductive removal of the 5,8-oxygen functions to generate the required 5,7-diene end product from which the desired 7-trans(7E)-isomer is purified directly, or after optional double bond isomerization of the 7-cis(7Z)-isomer employing a novel thiophenol-promoted isomerization step.Type: GrantFiled: March 27, 1995Date of Patent: June 11, 1996Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Heinrich K. Schnoes, Fariba Aria
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Patent number: 5514708Abstract: The present invention is based upon the discovery that the methanol extract of the bryozoan Myriapora truncata showed potent cytotoxicity against L1210 murine leukemia cells (99% inhibition at 50 .mu.g/mL). Fractionation and purification of active components from this extract, guided by a cytotoxicity assay, resulted in the isolation of a novel, highly cytotoxic polyketide-derived metabolite MT-332 (Compound 3) and its equilibrium isomer (Compound 4), along with two less active compounds, MT-381 (Compound 1) and MT-381-B (Compound 2). The equilibrium mixture of Compounds 3 and 4 showed 88% inhibition at 0.2 .mu.g/mL against L1210 cells.Type: GrantFiled: February 18, 1994Date of Patent: May 7, 1996Assignee: PharmaMar, S.A.Inventors: Kenneth L. Rinehart, Jie-Fei Cheng, Jong-Soo Lee
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Patent number: 5496943Abstract: Disclosed is a novel heterocyclic compound selected from the group consisting of the compounds [IV] to [VII], [IX] and [X]. The heterocyclic compound is useful for reactive materials in chemical industry. A process for producing the heterocyclic compound is also disclosed.Type: GrantFiled: March 13, 1992Date of Patent: March 5, 1996Assignee: Nippon Paint Co., Ltd.Inventors: Otohiko Tsuge, Taizo Hatta, Satoshi Urano, Noriyuki Tsuboniwa, Ryuzo Mizuguchi
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Patent number: 5482966Abstract: The invention concerns oxime derivatives of the formula I ##STR1## wherein R.sup.4 includes hydrogen, carboxy, carbamoyl, amino, cyano, trifluoromethyl, (1-4C)alkylamino, di-(1-4C)alkylamino and (1-4C)alkyl;R.sup.5 includes hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, (2-5C)alkanoyl, halogeno-(2-4C)alkyl and hydroxy-(2-4C)alkyl;Ar.sup.1 is phenylene or a heteroaryl diradical;A.sup.1 is a direct link to X.sup.1, or A.sup.1 is (1-4C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene or a heteroaryl diradical;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which together with the carbon atom to which A.sup.2 and A.sup.3 are attached define a ring having 5 or 6 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.Type: GrantFiled: June 13, 1994Date of Patent: January 9, 1996Assignees: Zeneca Limited, Zeneca Pharma S.A.Inventors: Thomas G. C. Bird, Patrick Ple
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Patent number: 5457125Abstract: The invention concerns oxime derivatives of the formula I ##STR1## wherein R.sup.4 is hydrogen, (1-4C)alkyl, halogeno-(2-4C)alkyl, hydroxy-(2-4C)alkyl, cyano-(1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl;R.sup.5 is hydrogen, (1-4C)alkyl, halogeno-(2-4C)alkyl, hydroxy-(2-4C)alkyl, cyano-(1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl, or a heteroaryl moiety selected from pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, furyl, thienyl, oxazolyl and thiazolyl;A.sup.4 is (1-4C)alkylene;Ar.sup.1 is phenylene, pyridinediyl or pyrimidinediyl;A.sup.1 is a direct link to X.sup.1, or A.sup.1 is (1-4C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene, pyridinediyl, pyrimidinediyl, thiophenediyl, furandiyl or thiazolediyl;R.sup.1 is hydrogen, (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- wherein each of A.sup.2 and A.sup.3 is independently (1-3C)alkylene and X.sup.Type: GrantFiled: August 19, 1994Date of Patent: October 10, 1995Assignees: Zeneca Limited, Zeneca Pharma S.A.Inventors: Philip N. Edwards, Michael S. Large
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Patent number: 5436266Abstract: Crystalline calcium pseudomonate or a hydrate thereof, in particular the dihydrate. Processes for the preparation of these salts and their use in human and veterinary medicine and as a growth promoter in animals are described.Type: GrantFiled: February 28, 1994Date of Patent: July 25, 1995Assignee: Beecham Group p.l.c.Inventors: Geoffrey H. Baker, Merle Beal
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Patent number: 5412116Abstract: A process for the conversion of glycoside substituted taxanes to taxol and related compounds that can serve as precursors to taxol. The process includes the oxidation of glycoside substituted taxanes to convert the glycoside to the hydroxyl group. The oxidation can occur in the presence of an acid or followed by treatment with acid. Application of the process to 7-xylosyl taxol ("XT") yields taxol; application to other glycoside substituted taxanes forms compounds that can serve as precursors for taxol. The process includes the formation of certain new taxol related intermediate compounds having a hemialdal at the C-7 site on the taxane ring, which hemialdal can then be converted to taxol or taxol precursors. Since glycoside substituted taxanes are isolated with taxol from naturally occurring biomass, their conversion to taxol using the process of the present invention significantly improves the total yield of taxol from natural sources.Type: GrantFiled: October 7, 1993Date of Patent: May 2, 1995Assignee: Hauser Chemical Research, Inc.Inventors: Christopher K. Murray, Jeffrey T. Beckvermit, David T. Bailey, S. Kent Peterson
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Patent number: 5405968Abstract: Methine dyes with a polyketo group I ##STR1## where A is ##STR2## R.sup.1 is a 5- or 6-membered cycloaliphatic radical which contains one or two hetero atoms from the group --NR.sup.4 --, --O-- and --S-- and which may be fused to an isoaromatic or heteroaromatic group, R.sup.2 and R.sup.3 are identical or different C.sub.1 -C.sub.10 -alkyl groups or together one of the radicals R.sup.1, and m and n are identical or different integers from 0 to 3, are useful as drugs, for producing singlet oxygen, as sensitizers in electrophotographic layers and for photopolymerizations and as laser light sensitive dyes in optical recording media; also novel triketo- and tetraketomethine dyes.Type: GrantFiled: September 27, 1993Date of Patent: April 11, 1995Assignee: BASF AktiengesellschaftInventors: Bernhard Albert, Knut Kessel, Hans-Dieter Martin, Stefan Silber
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Patent number: 5395854Abstract: Ortho-substituted phenyl-acetamides I ##STR1## (R.sup.1 =H, alkyl, cycloalkyl, alkenyl, alkynyl, phenylalkynyl, alkoxyalkyl, alkoxycarbonyl, phenyl, phenylalkyl, phenylalkenyl or phenoxyalkyl, 5- or 6-membered heterocycle with 1-3 hetero atoms to which a benzene ring or a 5- or 6-membered heterocycle can be fused; R.sup.2 and R.sup.3 =H, CN, halogen, alkyl, alkoxy; R.sub.4 and R.sup.5 =H, alkyl and R.sup.4 or R.sup.5 =alkoxy; Y=O, S, SO, SO.sub.2, N=N, O--CO, CO--O, CO--O--CH.sub.2, alkylene or haloalkylene, alkenylene, alkynylene, oxy- alkylene, thio-alkylene, alkyleneoxy, carbonylalkylene or alkylenecarbonyl, W=alkoxyimino, alkoxymethylene or alkylthiomethylene), excepting compounds where R.sup.1 is hydrogen, phenyl or 2,2-dimethyl-3-(2,2-dichlorovinyl)cyclopropyl, R.sup.2 to R.sup.5 are each hydrogen, Y is carbonyloxymethylene and W is methoxymethylene or methylthiomethylene, are suitable as fungicides and for controlling pests.Type: GrantFiled: September 22, 1993Date of Patent: March 7, 1995Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Eberhard Ammermann, Gisela Lorenz, Hubert Sauter, Klaus Oberdorf, Uwe Kardorff, Christoph Kuenast
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Patent number: 5376680Abstract: The invention concerns oxime derivatives of the formula I ##STR1## wherein R.sup.4 is hydrogen, (1-4C)alkyl, halogeno-(2-4C)alkyl, hydroxy-(2-4C)alkyl, cyano-(1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl; R.sup.5 is hydrogen, (1-4C)alkyl, halogeno-(2-4C)alkyl, hydroxy-(2-4C)alkyl, cyano-(1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl, or a heteroaryl moiety selected from pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, furyl, thienyl, oxazolyl and thiazolyl;A.sup.4 is (1-4C)alkylene;Ar.sup.1 is phenylene, pyridinediyl or pyrimidinediyl;A.sup.1 is a direct link to X.sup.1 or A.sup.1 is (1-4C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene, pyridinediyl, pyrimidinediyl, thiophenediyl, furandiyl or thiazolediyl;R.sup.1 is hydrogen, (1-4C)alkyl, (3-C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- wherein each of A.sup.2 and A.sup.3 is independently (1-3C)alkylene and X.sup.Type: GrantFiled: May 11, 1993Date of Patent: December 27, 1994Assignees: Zeneca Limited, Zeneca Pharma, S.A.Inventors: Philip N. Edwards, Michael S. Large
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Patent number: 5371222Abstract: A fungicidal composition for agricultural use, which comprises a compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen, lower alkyl or cyclo(lower)alkyl; R.sup.3 is lower alkyl or cyclo(lower)alkyl; R.sup.4 and R.sup.5 are each hydrogen, lower alkyl, lower alkoxy, halogen-substituted lower alkyl, lower alkyl-substituted silyl, halogen or nitro; A represents an unsaturated hydrocarbon group, a halogen-substituted unsaturated hydrocarbon group, a phenyl group or a heterocyclic group, among which the phenyl group and the heterocyclic group may be optionally substituted with not more than three substituents; and Z is --CH.sub.2 --, --CH(OH)--, --CO--, --O--, --S--, --NR-- (R being hydrogen or lower alkyl), --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 SO--, --OCH.sub.2 --, --SCH.sub.2 -- or --SOCH.sub.2 --.Type: GrantFiled: October 16, 1992Date of Patent: December 6, 1994Assignee: Shionogi Seiyaku Kabushiki KaishaInventors: Yoshio Hayase, Takahiro Kataoka, Hideyuki Takenaka, Mitsuhiro Ichinari, Michio Masuko, Toshio Takahashi, Norihiko Tanimoto
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Patent number: 5371223Abstract: A fungicidal composition for agricultural use, which comprises a compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen, lower alkyl or cyclo(lower)alkyl; R.sup.3 is lower alkyl or cyclo(lower)alkyl; R.sup.4 and R.sup.5 are each hydrogen, lower alkyl, lower alkoxy, halogen-substituted lower alkyl, lower alkyl-substituted silyl, halogen or nitro; A represents an unsaturated hydrocarbon group, a halogen-substituted unsaturated hydrocarbon group, a phenyl group or a heterocyclic group, among which the phenyl group and the heterocyclic group may be optionally substituted with not more than three substituents; and Z is --CH.sub.2 --, --CH(OH)--, --CO--, --O--, --S--, --NR-- (R being hydrogen or lower alkyl), --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 SO--, --OCH.sub.2 --, --SCH.sub.2 -- or --SOCH.sub.2 --.Type: GrantFiled: October 8, 1993Date of Patent: December 6, 1994Assignee: Shionogi Seiyaku Kabushiki KaishaInventors: Yoshio Hayase, Takahiro Kataoka, Hideyuki Takenaka, Mitsuhiro Ichinari, Michio Masuko, Toshio Takahashi, Norihiko Tanimoto
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Patent number: 5360815Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.Type: GrantFiled: June 23, 1993Date of Patent: November 1, 1994Assignee: Merck Frosst Canada, Inc.Inventors: Rejean Fortin, Yves Girard, Erich Grimm, John Hutchinson, John Scheigetz
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Patent number: 5352831Abstract: Oligomeric cyanoguanidines of formula I ##STR1## wherein, for example, R.sup.1 and R.sup.2 are each phenyl, R is 1,4-phenylene and n is an integer from 1 to 20, are suitable latent hardeners for epoxy resins. They are readily soluble in solvents suitable for the application of epoxy resins, and the cured products obtained therewith have a high glass transition temperature.Type: GrantFiled: July 14, 1992Date of Patent: October 4, 1994Assignee: Ciba-Geigy CorporationInventors: Peter Flury, Martin Roth, Sameer H. Eldin
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Patent number: 5350764Abstract: An acidic polycyclic ether antibiotic, having structure established by X-ray crystallography, is formed by fermentation of a novel microorganism, Actinomadura sp. ATCC 55027. This novel antibiotic is useful as an anticoccidial in poultry, in the prevention and treatment of swine dysentery and as a growth promotant in cattle and swine.Type: GrantFiled: March 12, 1993Date of Patent: September 27, 1994Assignee: Pfizer Inc.Inventors: John P. Dirlam, Hiroshi Maeda, Junsuke Tone
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Patent number: 5308852Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis and allograft rejection and in preventing the formation of atherosclerotic plaques.Type: GrantFiled: August 27, 1992Date of Patent: May 3, 1994Assignee: Merck Frosst Canada, Inc.Inventors: Yves Girard, Daniel Delorme, Rejean Fortin, Daniel Dube, Pierre Hamel, Carol Lepine, Yves Ducharme
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Patent number: 5286745Abstract: The invention provides antibiotics designated LL-E19020 Epsilon and LL-E19020 Epsilon.sub.1 which are derived from the microorganism Streptomyces lydicus ssp. tanzanius NRRL 18036.Type: GrantFiled: September 9, 1991Date of Patent: February 15, 1994Assignee: American Cyanamid CompanyInventors: Guy T. Carter, Joseph J. Goodman
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Patent number: 5252599Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.Type: GrantFiled: August 27, 1992Date of Patent: October 12, 1993Assignee: Merck Frosst Canada, Inc.Inventors: Yves Girard, Rejean Fortin, Daniel Delorme, Daniel Dube, Pierre Hamel, Yves Ducharme, John W. Gillard
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Patent number: 5234900Abstract: The present invention relates to novel oxabicyclo ether derivative compounds, compositions containing these ether derivative compounds, and methods of using these compounds or compositions to control the growth of undesired vegetation. More particularly, the present invention relates to a variety of compounds, compositions, and methods of using them which are herbicidally active on a wide variety of weed species and exhibit safety to rice, cereals or broadleaf crops.Type: GrantFiled: March 11, 1992Date of Patent: August 10, 1993Assignee: E. I. Du Pont de Nemours and CompanyInventors: James E. Powell, Jr., Wendy S. Taylor
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Patent number: 5228896Abstract: Cyclohexenone oxime ethers of the formula I ##STR1## (R.sup.1 =C.sub.1 -C.sub.6 -alkyl; A=substituted or unsubstituted alkylene or alkenylene;Z=a 5-membered or 6-membered heteroaromatic structure;X=substituted or unsubstituted amino, nitro, cyano, halogen, alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl and phenyl;n=0 to 3, or 1 to 4 where Z is halogen-substituted pyridyl; andR.sup.Type: GrantFiled: May 8, 1991Date of Patent: July 20, 1993Assignee: BASF AktiengesellschaftInventors: Ulf Misslitz, Norbert Meyer, Juergen Kast, Norbert Goetz, Albrecht Harreus, Thomas Kuekenhoehner, Bruno Wuerzer, Helmut Walter, Karl-Otto Westphalen, Matthias Gerber
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Patent number: 5223616Abstract: A heterocyclic compound which is useful for dyeing or printing hydrophobic fiber materials and which has the following formula (I), ##STR1##wherein A.sub.1, A.sub.2, A.sub.3 and A.sub.4 are each hydrogen, halogen, alkyl, alkoxy or alkenyl, X.sub.1 is --O-- or the like, R.sub.1 is a methylene or the like, X.sub.2 is a direct linkage or a divalent group of --O--, --S--, --SO--, --SO.sub.2 --, ##STR2## in which R.sub.3 is a hydrogen atom or a C.sub.1-4 alkyl group, ##STR3## in which R.sub.3 is as defined above, T and u are each independently hydrogen or a C.sub.1-4 alkyl, l is O or an integer of 1 to 3, Q is an unsubstituted or substituted 5-, 6- or 7-membered saturated or unsaturated heterocyclic residue, Y is hydrogen, C.sub.1-4 alkyl, a C.sub.1-4 alkoxy group or the like.Type: GrantFiled: November 4, 1991Date of Patent: June 29, 1993Assignee: Sumitomo Chemical Company, Ltd.Inventors: Jun Yamamoto, Junichi Sekihachi, Yosuke Yamamoto, Kazuhiro Machiguchi, Yutaka Kayane
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Patent number: 5216167Abstract: Phenylacetic acid benzylamides having the following general structure ##STR1## wherein the substituents are defined herein, are disclosed, which compounds are hypoglcemic agents.Type: GrantFiled: June 21, 1990Date of Patent: June 1, 1993Assignee: Dr. Karl Thomae GmbHInventors: Wolfgang Grell, Rudolf Hurnaus, Gerhart Griss, deceased, Robert Sauter, Manfred Reiffen, Eckhard Rupprecht
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Patent number: 5190573Abstract: Cyclohexenone oxime ethers ##STR1## where R.sup.1 is alkyl;A is substituted or unsubstituted alkylene or alkenylene, where methylene is replaced by an oxygen atom, a sulfur atom, a sulfoxyl group, a sulfonyl group or --NR.sup.a --,Z is phenyl or a 5- or 6-membered heteroaromatic structure;X is substituted or unsubstituted amino, nitro, cyano, halogen, alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, substituted or unsubstituted benzyloxycarbony or phenyl;n is 0 to 3, or 1 to 5 where X is halogen;R.sup.Type: GrantFiled: May 8, 1991Date of Patent: March 2, 1993Assignee: BASF AktiengesellschaftInventors: Ulf Misslitz, Norbert Meyer, Juergen Kast, Norbert Goetz, Albrecht Harreus, Bruno Wuerzer, Helmut Walter, Karl-Otto Westphalen, Matthias Gerber