Carbocyclic Ring Bonded Directly At 2-position Patents (Class 544/289)
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Patent number: 6806274Abstract: The invention concerns quinazoline derivatives of Formula (I) wherein Q1 includes a quinazoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X1— wherein X1 includes a direct bond and O and Q3 includes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of R2 and R3 is hydrogen or (1-6C)alkyl; Z includes O, S and NH; and Q2 includes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions in a warm-blooded animal.Type: GrantFiled: January 7, 2002Date of Patent: October 19, 2004Assignee: AstraZeneca UK LimitedInventors: Graham C Crawley, Laurent F A Hennequin, Darren McKerrecher, Patrick Ple, Jeffrey Philip Poyser, Christine M P Lambert
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Substituted pyrimidines, processes for their preparation, and their use as pesticides and fungicides
Patent number: 6596727Abstract: Substituted 4-amino- and 4-alkoxy-cycloalkylpyrimidines, processes for their preparation, and their use as pesticides and fungicides The invention relates to compounds of the formula in which R1, R2, R3 and Q are as defined in the description, X is NH or oxygen and E is a bond or a 1- to 4-membered carbon chain, to a process for their preparation, to agents containing them, and to their use in the control of pests and as fungicides.Type: GrantFiled: March 15, 1996Date of Patent: July 22, 2003Assignee: Hoechst AktiengesellschaftInventors: Wolfgang Schaper, Rainer Preuss, Gerhard Salbeck, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lümmen, Werner Bonin -
Publication number: 20030036066Abstract: A novel approach for combining the ease of cleavage of carboxylic acid linker arms with the single phosphoramidite coupling chemistry of the universal supports useful in oligonucleotide synthesis. There is disclosed a new class of phosphoramidite reagents, linker phosphoramidites, which contain a bifunctional linker arm with a protected nucleoside linked through a 3′-ester bond on one end and a reactive phosphoramidite group or other phosphate precursor group on the other end—see FIGS. 2 and 3. The phosphoramidite group on the linker phosphoramidite may be activated under the same conditions and has similar reactivity as conventional nucleoside-3′-phosphoramidite reagents lacking the intermediate linker arm. The 3′-ester linkage contained within the linker phosphoramidite has similar properties to the linkages on prederivatized supports.Type: ApplicationFiled: September 10, 2001Publication date: February 20, 2003Applicant: University Technologies International Inc.Inventors: Richard T. Pon, Shuyan Yu
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Patent number: 6429311Abstract: The present invention is directed to certain N-amino- and N-hydroxy-quinazolinone compounds and synthetic methods for synthesis thereof, which compounds may find use in combinatorial libraries. More specifically, the invention is directed to the synthesis of 3-hydroxy- and 3-amino-4 (1H)-quinazolinones via the reaction of an appropriate 2-aminobenzamide compound with a carboxylic acid or acyl halide at ambient temperature performed on a solid support or in solution.Type: GrantFiled: February 1, 2001Date of Patent: August 6, 2002Assignee: Sepracor Inc.Inventor: Yun Gao
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Patent number: 6316455Abstract: A range of 3-oxybenzamide compounds and related quinazolinone compounds are disclosed which can act as potent inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase or PARP enzyme (EC 2.4.2.30), and which thereby can provide useful therapeutic compounds for use in conjunction with DNA-damaging cytotoxic drugs or radiotherapy to potentiate the effects of the latter. The coumpounds disclosed include 3-benzyloxybenzamides, 3-oxybenzamides in which a chain of 5 or more methylene groups terminate in a halogen atom or in a purin-9-yl moiety, certain benzoxazole-4-carboxamide compounds and certain quinazolinone compounds. In formula X and Y together may form a bride —X—Y— that represents the grouping (a), (b) or (c) wherein R5 is H, alkyl, aryl or aralkyl.Type: GrantFiled: November 24, 1999Date of Patent: November 13, 2001Assignee: Newcastle University Ventures LimitedInventors: Roger John Griffin, Alan Hilary Calvert, Nicola Jane Curtin, David Richard Newell, Bernard Thomas Golding
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Patent number: 6274383Abstract: Synthetic methods for solution and solid-phase synthesis of combinatorial libraries of dihydro-quinazolinones, including synthesis of 2,3-dihydro-3-alkoxy-4(1H)-quinazolinones or 2,3-dihydro-3-hydroxy-4(1H)-quinazolinones via the Lewis-acid catalyzed reaction of an appropriate 2-aminobenzamide with an aldehyde at ambient temperature performed on a solid support or in solution.Type: GrantFiled: December 15, 1997Date of Patent: August 14, 2001Assignee: Sepracor Inc.Inventor: Yun Gao
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Patent number: 6204267Abstract: The present invention is directed in part towards methods of modulating the function of serine/threonine protein kinases with quinazoline-based compounds. The methods incorporate cells that express a serine/threonine protein kinase, such as RAF. In addition, the invention describes methods of preventing and treating serine/threonine protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to quinazoline compounds and pharmaceutical compositions comprising these compounds.Type: GrantFiled: May 1, 1998Date of Patent: March 20, 2001Assignee: Sugen, Inc.Inventors: Peng C. Tang, Gerald McMahon, Heinz Weinberger, Bernhard Kutscher, Harald App
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Patent number: 6184377Abstract: The present invention is directed to certain N-amino- and N-hydroxy-quinazolinone compounds and synthetic methods for synthesis thereof, which compounds may find use in combinatorial libraries. More specifically, the invention is directed to the synthesis of 3-hydroxy- and 3-amino-4(1H)-quinazolinones via the reaction of an appropriate 2-aminobenzamide compound with a carboxylic acid or acyl halide at ambient temperature performed on a solid support or in solution.Type: GrantFiled: December 15, 1997Date of Patent: February 6, 2001Assignee: Sepracor Inc.Inventor: Yun Gao
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Patent number: 5972929Abstract: A quinazolinone derivative or a salt thereof expressed by the following Formula (I); ##STR1## wherein each of A and B is R.sup.1 or --(CH.sub.2).sub.n -NR.sup.2 R.sup.3 ; wherein R.sup.1 represents a hydrocarbon group of C.sub.10-30 ; wherein R.sup.2 and R.sup.3 individually represent a hydrogen atom, a lower alkyl group, a phenyl group, or a benzyl group, or together represent a heterocyclic ring having 3-7 members; and n represents an integer of 1-5; wherein when A is R.sup.1, B is --(CH.sub.2).sub.n -NR.sup.2 R.sup.3 and when A is --(CH.sub.2).sub.n -NR.sup.2 R.sup.3, B is R.sup.1 ; and wherein R.sup.4 is selected from the group consisting of a hydrogen atom, a halogen atom, a lower alkyl group, a lower acyl group, a nitro group, a cyano group, an amino group, a lower alkoxycarbonyl group, a lower alkylamino group, a lower alkoxy group, a lower acyloxy group, a carbamoyl group, a lower alkylcarbamoyl group, and a lower acylamino group.Type: GrantFiled: August 20, 1998Date of Patent: October 26, 1999Assignee: Shiseido Co., Ltd.Inventors: Koji Kobayashi, Hirotada Fukunishi, Tsunao Magara
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Patent number: 5948775Abstract: This invention relates to 2- or 3-(substituted aminoalkoxyphenyl)quinazolin-4-ones which are partial estrogen agonists and are useful in treating osteoporosis, prostatic hypertrophy, breast cancer and endometrial cancer.Type: GrantFiled: March 12, 1998Date of Patent: September 7, 1999Assignee: American Home Products CorporationInventors: Marci Catherine Koko, Arthur Attilio Santilli
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Patent number: 5922866Abstract: The present invention provides a novel process for preparing a series of quinazolin-4-one derivatives in high yields with reduced amounts of byproducts, the process comprising reacting, in the presence of a base, a trialkylsilyl halide with a compound represented by the formula ##STR1## wherein; R.sup.5 is a phenyl group which may have 1 to 3 substituents each selected from a lower alkyl group, a lower alkoxy group or a halogen atom, a lower alkyl group, a phenyl-lower alkyl group which may have a halogen atom as a substituent on the phenyl ring, a lower alkenyl group, a lower alkoxy-lower alkyl group or a lower alkynyl group; R.sup.6 is a lower alkyl group, a halogen-substituted lower alkyl group, a lower alkoxycarbonyl group or a phenyl group which may have, as a substituent, a lower alkyl group or a group of the formula ##STR2## wherein A is an oxygen atom or a single bond, Z is a lower alkylene group, R.sup.7 is a lower alkyl group and R.sup.Type: GrantFiled: February 25, 1998Date of Patent: July 13, 1999Assignee: Otsuka Pharmaceutical Factory, Inc.Inventors: Kazuyoshi Miyata, Yasuhisa Kurogi, Yasuhiro Sakai, Yoshihiko Tsuda
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Patent number: 5922711Abstract: A compound of the formula: ##STR1## wherein --X.sup.3 .dbd.X.sup.2 --X.sup.1 .dbd.N-- is a group of the formula: ##STR2## R.sup.1 is hydrogen or halogen, R.sup.2 is halogen,R.sup.3 is hydrogen, nitro, amino optionally having at least one substituent or a heterocyclic group optionally having at least one substituent,R.sup.4 and R.sup.5 are each hydrogen, or halogen,R.sup.6 and R.sup.8 are each hydrogen, halogen, lower alkyl, hydroxy, lower alkylthio, amino optionally substituted with lower alkyl, or lower alkoxy optionally substituted with a substituent selected from the group consisting of hydroxy, lower alkoxy, amino, lower alkylamino and aryl optionally substituted with lower alkoxy,R.sup.7 is hydrogen or lower alkyl,A is lower alkylene, andQ is O or N--R.sup.9 is hydrogen or acyl,provided that R.sup.3 is not hydrogen when X.sup.1 is C--R.sup.6, in which R.sup.6 is hydrogen, andpharmaceutically acceptable salts thereof.Type: GrantFiled: September 19, 1997Date of Patent: July 13, 1999Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Teruo Oku, Hiroshi Kayakiri, Shigeki Satoh, Yoshito Abe, Yuki Sawada, Takayuki Inoue, Hirokazu Tanaka
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Patent number: 5885996Abstract: Quinazoline compounds which demonstrate antiproliferative activity, such as antitumor activity, processes of preparing these compounds, pharmaceutical compositions containing these compounds, and the use of these compounds. These compounds inhibit the growth and proliferation of the cells of higher organisms and microorganisms, such as bacteria, yeasts and fungi. Preferred quinazoline compounds are capable of inhibiting the enzyme thymidylate synthase. Effects derived from the inhibition of the enzyme thymidylate synthase include those discussed above.Type: GrantFiled: September 4, 1997Date of Patent: March 23, 1999Assignee: Agouron Pharmaceuticals, Inc.Inventors: Stephen E. Webber, Ted M. Bleckman, John Attard, Terrence R. Jones, Michael D. Varney
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Patent number: 5811429Abstract: The bicyclic heterocyclic compounds are prepared by reaction of correspondingly substituted carboxylic acids with amines, in particular with phenylglycinolamine. The bicyclic heterocyclic compounds according to the invention are suitable as active compounds in medicaments, in particular in medicaments having an antiatherosclerotic action.Type: GrantFiled: December 9, 1996Date of Patent: September 22, 1998Assignee: Bayer AktiengesellschaftInventors: Richard Connell, Siegfried Goldmann, Ulrich Muller, Stefan Lohmer, Hilmar Bischoff, Dirk Denzer, Rudi Grutzmann, Stefan Wohlfeil
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Patent number: 5753664Abstract: A novel compound of the formula:A--Z--Ar.sup.1 1'CO--Ar.sup.2wherein A is a condensed pyrimidinone or condensed pyridazinone ring; Ar.sup.1 and Ar.sup.2 are independently a ring; Z is a divalent group, or a salt thereof which have an excellent antitumor activity.Type: GrantFiled: March 13, 1996Date of Patent: May 19, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Tetsuya Aono, Shogo Marui, Fumio Itoh, Masuo Yamaoka, Masafumi Nakao
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Patent number: 5747497Abstract: This invention pertains to compounds of Formulae I, II and III, as defined in the disclosure and claims, including all geometric and stereoisomers, N-oxides, agriculturally suitable salts thereof, agricultural compositions containing them and their use as fungicides.Type: GrantFiled: November 8, 1995Date of Patent: May 5, 1998Assignee: E. I. du Pont de Nemours and CompanyInventors: James Francis Bereznak, Zen-Yu Chang, Thomas Paul Selby, Charlene Gross Sternberg
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Patent number: 5721238Abstract: 2,8-Disubstituted quinazolinones are prepared by first subjecting the quinazolinone basic skeleton to condensation by customary reactions and then introducing the desired substituents into the 8-position. The compounds are suitable as active compounds in medicaments, in particular for the treatment of inflammations, thromboembolic diseases and cardiovascular diseases.Type: GrantFiled: January 11, 1996Date of Patent: February 24, 1998Assignee: Bayer AktiengesellschaftInventors: Fred Robert Heiker, Ulrich Niewohner, Wolfgang Hartwig, Helmuth Schutz, Erwin Bischoff, Elisabeth Perzborn, Matthias Schramm
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Patent number: 5707992Abstract: Quinazoline compounds which demonstrate antiproliferative activity, such as antitumor activity, processes of preparing these compounds, pharmaceutical compositions containing these compounds, and the use of these compounds. These compounds inhibit the growth and proliferation of the cells of higher organisms and microorganisms, such as bacteria, yeasts and fungi. Preferred quinazoline compounds are capable of inhibiting the enzyme thymidylate synthase. Effects derived from the inhibition of the enzyme thymidylate synthase include those discussed above.Type: GrantFiled: April 7, 1995Date of Patent: January 13, 1998Assignee: Agouron Pharmaceuticals, Inc.Inventors: Stephen E. Webber, Ted M. Bleckman, John Attard, Terence R. Jones, Michael D. Varney
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Patent number: 5675006Abstract: Novel methods for the synthesis of substituted ureas and guanidines including Terazosin, Prazosin, Doxazosin, Tiodazosin, Trimazosin, Quinasin and Bunazosin (exemplary of 2-amino substituted Quinazolines), Meobentine and Bethanidine and novel intermediates suitable for use in such methods of synthesis are taught.Type: GrantFiled: May 30, 1995Date of Patent: October 7, 1997Assignee: Brantford Chemicals Inc.Inventors: Khashayar Karimian, Keshava Murthy, Darren Hall
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Patent number: 5580872Abstract: Antibacterial compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, preferred examples of which include those compounds whereinA is .dbd.CR.sup.6 --;R.sup.1 is cycloalkyl of from three to eight carbon atoms or substituted phenyl;R.sup.2 is selected from the group consisting of ##STR2## R.sup.3 is halogen; R.sup.4 is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group;R.sup.5 is hydrogen, loweralkyl, halo(loweralkyl), or --NR.sup.13 R.sup.14 ; andR.sup.6 is halogen, loweralkyl, halo(loweralkyl), hydroxy-substituted loweralkyl, loweralkoxy(loweralkyl), loweralkoxy, or amino(loweralkyl),as well as pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.Type: GrantFiled: September 30, 1994Date of Patent: December 3, 1996Assignee: Abbott LaboratoriesInventors: Daniel T. Chu, Qun Li, Curt S. Cooper, Anthony K. L. Fung, Cheuk M. Lee, Jacob J. Plattner
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Patent number: 5576322Abstract: The invention is directed to certain 2,4-diaminoquinazoline compounds, their pharmaceutically acceptable salts, the pharmaceutical compositions comprising those compounds and their therapeutic methods of use. The compounds possess anti-ischemic activity.Type: GrantFiled: February 18, 1994Date of Patent: November 19, 1996Assignee: Eisai Co., Ltd.Inventors: Yasutaka Takase, Nobuhisa Watanabe, Makoto Matsui, Hironori Ikuta, Teiji Kimura, Takao Saeki, Hideyuki Adachi, Tadakazu Tokumura, Hisatoshi Mochida, Yasunori Akita, Shigeru Souda
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Patent number: 5571815Abstract: The invention relates to compounds of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and Q are as defined in the description, X is NH or oxygen and E is a bond or a 1- to 4-membered carbon chain, to a process for their preparation, to agents containing them, and to their use in the control of pests and as fungicides.Type: GrantFiled: March 11, 1993Date of Patent: November 5, 1996Assignee: Hoechst AktiengesellschaftInventors: Wolfgang Schaper, Rainer Preuss, Gerhard Salbeck, deceased, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter L ummen, Werner Bonin
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Patent number: 5550229Abstract: Novel process for preparing azetidinone compound of the formula [III]: ##STR1## wherein R.sup.1 is H or lower alkyl, R.sup.2 and R.sup.3 combine together with the adjacent nitrogen to form heterocyclic group, and R.sup.4 is protected or unprotected hydroxy-substituted lower alkyl, which comprises reacting an alkanamide compound of the formula [I]: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are the same as defined above, with a compound of the formula [II]: ##STR3## wherein L.sup.1 is a leaving group and R.sup.4 is the same as defined above, in the presence of a base, said compound [III] being useful as synthetic intermediate for 1-methylcarbapenem derivative having excellent antibacterial activity.Type: GrantFiled: June 21, 1994Date of Patent: August 27, 1996Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Tameo Iwasaki, Kazuhiko Kondo, Hiroshi Ohmizu
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Patent number: 5536723Abstract: The invention relates to novel S-nitroso derivatives of ACE inhibitors and to pharmaceutical compositions comprising the S-nitrosothiol derivatives of the invention together with a pharmaceutically acceptable carrier.The invention also relates to methods for treating various pathophysiological conditions including acute myocardial infarction, left ventricular dysfunction without overt heart failure, hypertension, pulmonary hypertension, congestive heart failure, angina pectoris, vascular thrombosis, Raynauds syndrome, scleroderma, toxemia of pregnancy, acute renal failure, diabetic nephropathy, and renal artery stenosis, and to methods of inhibiting ACE and effecting vasodilation comprising administering the S-nitrosothiol derivatives of the ACE inhibitors of the invention to an animal.Type: GrantFiled: October 6, 1994Date of Patent: July 16, 1996Assignee: Brigham & Women's HospitalInventors: Joseph Loscalzo, John Cooke
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Patent number: 5482941Abstract: Compounds of formula: ##STR1## and pharmaceutically acceptable salts thereof whereinR.sup.1 is H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or CONR.sup.5 R.sup.6 ;R.sup.2 is H or- C.sub.1 -C.sub.4 alkyl;R.sup.3 is C.sub.2 -C.sub.4 alkyl;R.sup.4 is H, C.sub.2 -C.sub.4 alkanoyl optionally substituted with NR.sup.7 R.sup.8, (hydroxy)C.sub.2 -C.sub.4 alkyl optionally substituted with NR.sup.7 R.sup.8, CH.dbd.CHCO.sub.2 R.sup.9, CH.dbd.CHCONR.sup.7 R.sup.8, CH.sub.2 CH.sub.2 CO.sub.2 R.sup.9, CH.sub.2 CH.sub.2 CONR.sup.7 R.sup.8, SO.sub.2 NR.sup.7 R.sup.8, SO.sub.2 NH(CH.sub.2).sub.n NR.sup.7 R.sup.8 or imidazolyl;R.sup.5 and R.sup.6 are each independently H or C.sub.1 -C.sub.4 alkyl;R.sup.7 and R.sup.8 are each independently H or C.sub.1 -C.sub.4 alkyl, or together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino, morpholino or 4-(NR.sup.10)-1-piperazinyl group wherein any of said groups is optionally substituted with CONR.sup.5 R.sup.6 ;R.sup.9 is H or C.sub.1 -C.sub.Type: GrantFiled: May 6, 1994Date of Patent: January 9, 1996Assignee: Pfizer Inc.Inventor: Nicholas K. Terrett
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Patent number: 5470975Abstract: Novel A-II receptor antagonists have the formula ##STR1## and its isomer ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are as defined herein.Type: GrantFiled: January 11, 1994Date of Patent: November 28, 1995Assignee: E.R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 5430148Abstract: Quinazoline compounds which demonstrate antiproliferative activity, such as antitumor activity, processes of preparing these compounds, pharmaceutical compositions containing these compounds, and the use of these compounds. These compounds inhibit the growth and proliferation of the cells of higher organisms and microorganisms, such as bacteria, yeasts and fungi. Preferred quinazoline compounds are capable of inhibiting the enzyme thymidylate synthase. Effects derived from the inhibition of the enzyme thymidylate synthase include those discussed above.Type: GrantFiled: March 31, 1992Date of Patent: July 4, 1995Assignee: Agouron Pharmaceuticals, Inc.Inventors: Stephen E. Webber, Ted M. Bleckman, John Attard, Terence R. Jones, Michael D. Varney
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Patent number: 5401745Abstract: Phenoxyphenylacetic acids and derivatives of general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebal and cardiac ischemia, myocardial infarction, inflammatory diseases, Raynaud's disease, and endotoxic shock, and asthma.Type: GrantFiled: March 19, 1993Date of Patent: March 28, 1995Assignee: Merck & Co., Inc.Inventors: Scott W. Bagley, Prasun K. Chakravarty, Anna Chen, Daljit S. Dhanoa, Kenneth J. Fitch, William J. Greenlee, Elizabeth M. Naylor, James R. Tata, Thomas F. Walsh, David L. Williams, Jr.
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Patent number: 5395838Abstract: The invention relates to quinazoline derivatives, or pharmaceutically-acceptable salts thereof, which possess anti-tumour activity; to processes for their manufacture; and to pharmaceutical compositions containing them.The invention provides a quinazoline of the formula: ##STR1## wherein R.sup.1 is hydrogen or amino, or alkyl or alkoxy each of up to 6 carbon atoms; or R.sup.1 is substituted alkyl or alkoxy each of up to 3 carbon atoms;R.sup.2 is hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, halogenoalkyl or cyanoalkyl each of up to 6 carbon atoms;Ar is phenylene or heterocyclene;L is a group of the formula --CO.NH--, --NH.CO--, --CO.NR.sup.3 --, --NR.sup.3.CO--, --CH.dbd.CH--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 S--, --SCH.sub.2 --, --CO.CH.sub.2 --, --CH.sub.2.CO-- or --CO.O--, wherein R.sup.3 is alkyl of up to 6 carbon atoms; andY is aryl or heteroaryl or a hydrogenated derivative thereof; orY is a group of the formula --A--Y.sup.Type: GrantFiled: July 13, 1993Date of Patent: March 7, 1995Assignees: Imperial Chemical Industries PLC, National Research Development CorporationInventors: Andrew J. Barker, Leslie R. Hughes, Peter R. Marsham, John Oldfield, Stephen J. Pegg
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Patent number: 5389600Abstract: The invention relates to certain substituted fused compounds of Formula I ##STR1## which are useful as herbicides, and their agriculturally suitable compositions, as well as methods for their use as general or selective preemergent or postemergent herbicides or as plant growth regulants.Type: GrantFiled: May 21, 1993Date of Patent: February 14, 1995Assignee: E. I. du Pont de Nemours and CompanyInventor: Thomas P. Selby
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Patent number: 5385894Abstract: Novel disubstituted 6-aminoquinazolinones of the Formula (I), are useful as angiotensin II antagonists: ##STR1##Type: GrantFiled: April 4, 1994Date of Patent: January 31, 1995Assignee: Merck & Co., Inc.Inventors: Stephen E. de Laszlo, Tomasz W. Glinka, William J. Greenlee, Prasun K. Chakravarty, Arthur A. Patchett
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Patent number: 5316906Abstract: Novel fluorescent precipitating substrates made from a class of fluorophores, generally including quinazolinones (quinazolones), benzimidazoles, benzothiazoles, benzoxazoles, quinolines, indolines, and phenanthridines, having the general formula: ##STR1## where carbon atoms of --C.sup.1 .dbd.C.sup.2 -- are further joined so as to complete a first 5- or 6-membered aromatic ring which may contain at least one of the hetero atoms N, O or S,where carbon atoms of --C.sup.4 --N.dbd.C.sup.3 -- are further joined so as to complete a second 5- or 6-membered aromatic ring that contains at least the nitrogen between C.sup.3 and C.sup.4 and may contain at least one additional hetero atom N, O or S,where the first and second aromatic rings may be joined by a 5- or 6-membered bridging ring that contains at least the C.sup.2 from the first aromatic ring and the C.sup.Type: GrantFiled: August 23, 1991Date of Patent: May 31, 1994Assignee: Molecular Probes, Inc.Inventors: Richard P. Haugland, Yu-zhong Zhang, Stephen T. Yue, Ewald Terpetschnig, Nels A. Olson, John J. Naleway, Karen D. Larison, Zhijian Huang
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Patent number: 5264439Abstract: Substituted heterocycles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I are useful as angiotensin II antagonists.Type: GrantFiled: August 13, 1991Date of Patent: November 23, 1993Assignee: Merck & Co., Inc.Inventors: William J. Greenlee, David Hangauer, Arthur A. Patchett, Thomas F. Walsh, Kenneth J. Fitch, Daljit S. Dhanoa, Ralph A. Rivero
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Patent number: 5240928Abstract: Novel substituted quinazolinones of the formula (I), which are useful as angiotensin II antagonists, are disclosed.Type: GrantFiled: March 6, 1991Date of Patent: August 31, 1993Assignee: Merck & Co., Inc.Inventors: Eric E. Allen, Stephen E. de Laszlo, Prasun K. Chakravarty, William J. Greenlee, Arthur A. Patchett, Thomas F. Walsh
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Patent number: 5236927Abstract: A compound of formula I: ##STR1## wherein R is hydrogen; oran alkyl, alkenyl or alkynyl group of up to 6 carbon atoms; nis O; 1 or 2; Z represents --CH.dbd.CH-- or --S--; each X independently represents halogeno, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, nitro or trifluoromethyl; and Y represents a group of formula: ##STR2## or a pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: December 12, 1990Date of Patent: August 17, 1993Assignee: National Research Development CorporationInventors: Terence R. Jones, Ann L. Jackman, David R. Newell
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Patent number: 5223501Abstract: Novel substituted fused pyrimidinones of formula (I) are useful as angiotensin II antagonists.Type: GrantFiled: May 10, 1991Date of Patent: June 29, 1993Assignee: Merck & Co., Inc.Inventors: Prasun K. Chakravarty, Nathan B. Mantlo, William J. Greenlee, Arthur A. Patchett, Dooseop Kim
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Patent number: 5208239Abstract: Fungicidal compounds having the formula (I): ##STR1## wherein R.sup.1 is an optionally substituted phenyl group, C.sub.3-6 cycloalkyl optionally substituted by alkyl or alkyl; R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are independently hydrogen, C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, C.sub.1-4 alkoxy or N'R"; Z is a linking group and is --C.tbd.C--, --CR.sup.8 .dbd.CR.sup.10 -- or --CR.sup.8 R.sup.9 --CR.sup.10 R.sup.11 --; R.sup.8, R.sup.9, R.sup.10, R.sup.11, R' and R" are independently hydrogen or C.sub.1-4 alkyl; provided that when R is alkyl Z is not --CR.sup.8 R.sup.9 --CR.sup.10 R.sup.11 --; and acid addition salts or metal complexes thereof; and processes for preparing then, compositions comprising them and methods of using them to combat fungi.Type: GrantFiled: October 31, 1991Date of Patent: May 4, 1993Assignee: Imperial Chemical Industries PLCInventors: Michael J. Robson, Paul A. Worthington
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Patent number: 5147875Abstract: This invention relates to quinazolinone derivatives which have bronchodilator activity. A compound of the invention is 2-(2-propoxyphenyl)quinazolin-4(3H)-one.Type: GrantFiled: November 30, 1989Date of Patent: September 15, 1992Assignee: Sanshin Kogyo Kabishiki KaishaInventors: William J. Coates, Lawrence I. Kruse
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Patent number: 5081124Abstract: A quinazoline of the formula: ##STR1## wherein R.sup.1 is alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkylthio, aryl, aryloxy, arylalkyl, halogeno, hydroxy, mercapto, pyridylthio, pyrimidinylthio, or substituted alkyl or alkoxy;wherein R.sup.2 is hydrogen, alkyl, alkenyl, alkynyl, substituted alkyl or alkanoyl;wherein Ar is phenylene, naphthylene or heterocyclene which is unsubstituted or bears one or more substituents and wherein R.sup.3 is such that R.sup.3 --NH.sub.2 is an amino acid;or a pharmaceutically-acceptable salt or ester thereof. The compounds possess anti-tumor activity.Type: GrantFiled: September 5, 1990Date of Patent: January 14, 1992Assignee: Imperial Chemical Industries PLCInventor: Leslie R. Hughes
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Patent number: 5053411Abstract: This invention pertains to novel substituted N-aryl-N-[4-(1-heterocyclicalkyl)piperidinyl]amides useful as analgesics, and methods of administering analgesia, which comprises the systemic administration to mammals of such compounds, and pharmaceutical compositions containing such compounds, wherein the novel compounds have the general formula: ##STR1## including optically active isomeric forms, and the pharmaceutically acceptable acid addition salts thereof, wherein R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are defined in the disclosure.Type: GrantFiled: April 20, 1989Date of Patent: October 1, 1991Assignee: Anaquest, Inc.Inventors: Jerome R. Bagley, Nhora L. Lalinde, Bao-Shan Huang, H. Kenneth Spencer
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Patent number: 5051506Abstract: Chiral, nonracemic compounds of the general formula: ##STR1## wherein m and n are either both zero, both equal one or n is equal to one and m is equal to zero, X and Y and Z are halogens, R' is an alkyl or alkoxy group having three to fifteen carbons, R is an alkyl group having one to fifteen carbons, and Ar is a 4,4'-substituted phenylvenzoate, 4,4'-substituted biphenylbenzoate, 5,4-substituted 2-phenylpyrimidine or 4,4'-substituted biphenyl core, and wherein * indicates a chiral center, which are useful as ferroelectric liquid crystal components having high polarization are described.Type: GrantFiled: March 4, 1988Date of Patent: September 24, 1991Assignee: Displaytech, Inc.Inventors: Michael D. Wand, David M. Walba
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Patent number: 5025001Abstract: The invention relates to novel S-nitroso derivatives of ACE inhibitors and to pharmaceutical compositions comprising the S-nitrosothiol derivatives of the invention together with a pharmaceutically acceptable carrier.The invention also relates to methods for treating various pathophysiological conditions including acute myocardial infarction, left ventricular dysfunction without overt heart failure, hypertension, pulmonary hypertension, congestive heart failure, angina pectoris, vascular thrombosis, Raynauds syndrome, scleroderma, toxemia of pregnancy, acute renal failure, diabetic nephropathy, and renal artery stenosis, and to methods of inhibiting ACE and effecting vasodilation comprising administering the S-nitrosothiol derivatives of the ACE inhibitors of the invention to an animal.Type: GrantFiled: March 24, 1989Date of Patent: June 18, 1991Assignee: Brigham and Women's HospitalInventors: Joseph Loscalzo, John Cooke
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Patent number: 4992550Abstract: A quinazoline of the formula: ##STR1## wherein R.sup.1 is alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkylthio, aryl, aryloxy, arylalkyl, halogeno, hydroxy, mercapto, pyridylthio, pyrimidinylthio, or substituted alkyl or alkoxy;wherein R.sup.2 is hydrogen, alkyl, alkenyl, alkynyl, substituted alkyl or alkanoyl;wherein Ar is phenylene, naphthylene or heterocyclene which is unsubstituted or bears one or more substituents and wherein R.sup.3 is such that R.sup.3 --NH.sub.2 is an amino acid;or a pharmaceutically-acceptable salt or ester thereof. The compounds possess anti-tumour activity.Type: GrantFiled: April 6, 1989Date of Patent: February 12, 1991Assignee: Imperial Chemical Industries PLCInventor: Leslie R. Hughes
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Patent number: 4981856Abstract: A quinazoline of the formula: ##STR1## wherein R.sup.1 is alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkylthio, aryl, aryloxy, arylthio, arylalkyl, halogeno, hydroxy or mercapto, or substituted alkyl or alkoxy;wherein R.sup.2 is hydrogen, alkyl, alkenyl or alkynyl, or substituted alkyl or alkanoyl;wherein Ar is phenylene, naphthylene or heterocyclene which is unsubstituted or bears one or more substituents;wherein R.sup.3 is such that R.sup.3 --NH.sub.2 is an amino acid;wherein R.sup.4 is hydrogen or alkyl;wherein R.sup.5 is hydrogen or alkyl; andwherein each of R.sup.6, R.sup.7 and R.sup.8 is hydrogen, hydroxy, alkyl, alkoxy, alkylthio, alkylamino, dialkylamino, phenyl, halogeno, nitro, cyano or amino, or substituted alkyl, alkoxy or alkylthio;provided that at least one of R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 is other than hydrogen;or a pharmaceutically-acceptable salt or ester thereof. The compounds possess anti-tumour activity.Type: GrantFiled: April 12, 1990Date of Patent: January 1, 1991Assignee: Imperial Chemical Industries PLCInventor: Leslie R. Hughes
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Patent number: 4920224Abstract: Variously substituted trans-3-[3-(3-hydroxypiperid-2-yl)-2-oxopropyl]quinazolin-4(3H)-ones, a method of controlling or preventing coccidiosis in poultry therewith, intermediates therefor, and a process for the preparation of certain intermediates therefor.Type: GrantFiled: March 13, 1989Date of Patent: April 24, 1990Assignee: Pfizer Inc.Inventor: Edward A. Glazer
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Patent number: 4908448Abstract: Novel photopolymerizable recording materials suitable in particular for producing photoresist layers and lithographic printing plates are composed of one or more photopolymerizable, olefinically unsaturated organic compounds, optionally a polymeric binder, a photopolymerization initiator, a color-forming system composed of a color former and a photooxidant, novel 4-quinazolone compounds as sensitizers and optionally further additive and/or auxiliary substances.Type: GrantFiled: August 4, 1989Date of Patent: March 13, 1990Assignee: BASF AktiengesellschaftInventors: Reinhard Aldag, Peter Neumann, Andreas Boettcher, Thomas Bluemel, Friedrich Seitz
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Patent number: 4849518Abstract: Variously substituted trans-3-[3-(3-hydroxypiperid-2-yl)-2-oxopropyl]quinazoline-4(3H)-ones, a method of controlling or preventing coccidiosis in poultry therewith, intermediates therefor, and a process for the preparation of certain intermediates thereof.Type: GrantFiled: March 24, 1988Date of Patent: July 18, 1989Assignee: Pfizer Inc.Inventor: Edward A. Glazer
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Patent number: 4788204Abstract: Amides of formula: ##STR1## in which A is ##STR2## V and W are H, halogen, alkyl (1-3C), alkoxy (1-3C), NO.sub.2 or CF.sub.3, Z is bound in the ortho or para position with respect toB and is phenyl, optionally substituted, thienyl or pyridyl, the chain X-(CH.sub.2).sub.n --(CHR).sub.m --CO--NR.sub.1 R.sub.2 is bound in the ortho or para position with respect to B,R is H or alkyl (1-3C),R.sub.1 and R.sub.2 are alkyl (1-6C), cycloalkyl (3-6C), phenyl, phenylalkyl, cycloalkylalkyl, alkenyl (3-6C),R.sub.1 and R.sub.2 can also form, with the nitrogen atom to which they are attached, a pyrrolidine, piperidine, morpholine or thiomorpholine ring,X is >CH--R.sub.3, >N--R.sub.4, >SO, >SO.sub.2, >O or >S,R.sub.3 is H, alkyl (1-3C),R.sub.4 is alkyl (1-3C)m=0 or 1 and n=0, 1 or 2,provided that, if X is >SO, >SO.sub.2 or >N--R.sub.4, the sum m+n is equal to at least 1, that, when A and B are N and Z is in the para position with respect to B, X cannot denote the group >CH--R.sub.Type: GrantFiled: May 28, 1986Date of Patent: November 29, 1988Assignee: Rhone-Poulenc SanteInventors: Jesus Benavides, Marie-Christine Dubroeucq, Gerard LeFur, Christian Renault
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Patent number: 4788199Abstract: Amides of formula: ##STR1## in which A is ##STR2## V and W are H, halogen, alkyl (1-3C), alkoxy (1-3C), NO.sub.2 or CF.sub.3, Z is bound in the ortho or para position with respect to B and is phenyl, optionally substituted, thienyl or pyridyl, the chain X--(CH.sub.2).sub.n --(CHR).sub.m --CO--NR.sub.1 R.sub.2 is bound in the ortho or para position with respect to B,R is H or alkyl (1-3C),R.sub.1 and R.sub.2 are alkyl (1-6C), cycloalkyl (3-6C), phenyl, phenylalkyl, cycloalkylalkyl, alkenyl (3-6C),R.sub.1 and R.sub.2 can also form, with the nitrogen atom to which they are attached, a pyrrolidine, piperidine, morpholine or thiomorpholine ring,X is >CH--R.sub.3, >N--R.sub.4, >SO, >SO.sub.2, >O or >S,R.sub.3 is H, alkyl (1-3C),R.sub.4 is alkyl (1-3C)m=0 or 1 and n=0, 1 or 2,provided that, if X is >SO, >SO.sub.2 or >N--R.sub.4 , the sum m+n is equal to at least 1, that, when A and B are N and Z is in the para position with respect to B, X cannot denote the group >CH--R.sub.Type: GrantFiled: March 11, 1988Date of Patent: November 29, 1988Assignee: Rhone-Poulenc SanteInventors: Jesus Benavides, Marie-Christine Dubroeucq, Gerard Le Fur, Christian Renault
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Patent number: 4766211Abstract: Chromogenic quinazolines of formula ##STR1## wherein R is an aryl radical or a heterocyclic radical,Z.sub.1 is oxygen or sulfur,Z.sub.2 is oxygen, sulfur or ##STR2## R' is hydrogen, alkyl which is unsubstituted or substituted by halogen, cyano or lower alkoxy, or is cycloalkyl, phenyl, benzyl, phenethyl or acyl, or --NRR' is a 5- or 6-membered heterocyclic radical,Q is an aliphatic radical which may be interrupted by a further member Z.sub.2,Y is the radical of a couplable compound, and the ringA is unsubstituted or substituted by halogen, cyano, nitro, lower alkyl, lower alkoxy or lower alkoxycarbonyl.These quinazolines are exceedingly fast to sublimation and are particularly suitable color formers in pressure-sensitive or heat-sensitive recording materials and give strong and lightfast yellow and orange colorations.Type: GrantFiled: August 27, 1986Date of Patent: August 23, 1988Assignee: Ciba-Geigy CorporationInventors: Rudolf Zink, Ian J. Fletcher