Carbocyclic Ring Bonded Directly At 2-position Patents (Class 544/289)
  • Patent number: 6806274
    Abstract: 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: Grant
    Filed: January 7, 2002
    Date of Patent: October 19, 2004
    Assignee: AstraZeneca UK Limited
    Inventors: Graham C Crawley, Laurent F A Hennequin, Darren McKerrecher, Patrick Ple, Jeffrey Philip Poyser, Christine M P Lambert
  • Patent number: 6596727
    Abstract: 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: Grant
    Filed: March 15, 1996
    Date of Patent: July 22, 2003
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang Schaper, Rainer Preuss, Gerhard Salbeck, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lümmen, Werner Bonin
  • Publication number: 20030036066
    Abstract: 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: Application
    Filed: September 10, 2001
    Publication date: February 20, 2003
    Applicant: University Technologies International Inc.
    Inventors: Richard T. Pon, Shuyan Yu
  • Patent number: 6429311
    Abstract: 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: Grant
    Filed: February 1, 2001
    Date of Patent: August 6, 2002
    Assignee: Sepracor Inc.
    Inventor: Yun Gao
  • Patent number: 6316455
    Abstract: 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: Grant
    Filed: November 24, 1999
    Date of Patent: November 13, 2001
    Assignee: Newcastle University Ventures Limited
    Inventors: Roger John Griffin, Alan Hilary Calvert, Nicola Jane Curtin, David Richard Newell, Bernard Thomas Golding
  • Patent number: 6274383
    Abstract: 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: Grant
    Filed: December 15, 1997
    Date of Patent: August 14, 2001
    Assignee: Sepracor Inc.
    Inventor: Yun Gao
  • Patent number: 6204267
    Abstract: 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: Grant
    Filed: May 1, 1998
    Date of Patent: March 20, 2001
    Assignee: Sugen, Inc.
    Inventors: Peng C. Tang, Gerald McMahon, Heinz Weinberger, Bernhard Kutscher, Harald App
  • Patent number: 6184377
    Abstract: 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: Grant
    Filed: December 15, 1997
    Date of Patent: February 6, 2001
    Assignee: Sepracor Inc.
    Inventor: Yun Gao
  • Patent number: 5972929
    Abstract: 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: Grant
    Filed: August 20, 1998
    Date of Patent: October 26, 1999
    Assignee: Shiseido Co., Ltd.
    Inventors: Koji Kobayashi, Hirotada Fukunishi, Tsunao Magara
  • Patent number: 5948775
    Abstract: 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: Grant
    Filed: March 12, 1998
    Date of Patent: September 7, 1999
    Assignee: American Home Products Corporation
    Inventors: Marci Catherine Koko, Arthur Attilio Santilli
  • Patent number: 5922866
    Abstract: 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: Grant
    Filed: February 25, 1998
    Date of Patent: July 13, 1999
    Assignee: Otsuka Pharmaceutical Factory, Inc.
    Inventors: Kazuyoshi Miyata, Yasuhisa Kurogi, Yasuhiro Sakai, Yoshihiko Tsuda
  • Patent number: 5922711
    Abstract: 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: Grant
    Filed: September 19, 1997
    Date of Patent: July 13, 1999
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Teruo Oku, Hiroshi Kayakiri, Shigeki Satoh, Yoshito Abe, Yuki Sawada, Takayuki Inoue, Hirokazu Tanaka
  • Patent number: 5885996
    Abstract: 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: Grant
    Filed: September 4, 1997
    Date of Patent: March 23, 1999
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Stephen E. Webber, Ted M. Bleckman, John Attard, Terrence R. Jones, Michael D. Varney
  • Patent number: 5811429
    Abstract: 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: Grant
    Filed: December 9, 1996
    Date of Patent: September 22, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Richard Connell, Siegfried Goldmann, Ulrich Muller, Stefan Lohmer, Hilmar Bischoff, Dirk Denzer, Rudi Grutzmann, Stefan Wohlfeil
  • Patent number: 5753664
    Abstract: 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: Grant
    Filed: March 13, 1996
    Date of Patent: May 19, 1998
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tetsuya Aono, Shogo Marui, Fumio Itoh, Masuo Yamaoka, Masafumi Nakao
  • Patent number: 5747497
    Abstract: 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: Grant
    Filed: November 8, 1995
    Date of Patent: May 5, 1998
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: James Francis Bereznak, Zen-Yu Chang, Thomas Paul Selby, Charlene Gross Sternberg
  • Patent number: 5721238
    Abstract: 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: Grant
    Filed: January 11, 1996
    Date of Patent: February 24, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Fred Robert Heiker, Ulrich Niewohner, Wolfgang Hartwig, Helmuth Schutz, Erwin Bischoff, Elisabeth Perzborn, Matthias Schramm
  • Patent number: 5707992
    Abstract: 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: Grant
    Filed: April 7, 1995
    Date of Patent: January 13, 1998
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Stephen E. Webber, Ted M. Bleckman, John Attard, Terence R. Jones, Michael D. Varney
  • Patent number: 5675006
    Abstract: 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: Grant
    Filed: May 30, 1995
    Date of Patent: October 7, 1997
    Assignee: Brantford Chemicals Inc.
    Inventors: Khashayar Karimian, Keshava Murthy, Darren Hall
  • Patent number: 5580872
    Abstract: 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: Grant
    Filed: September 30, 1994
    Date of Patent: December 3, 1996
    Assignee: Abbott Laboratories
    Inventors: Daniel T. Chu, Qun Li, Curt S. Cooper, Anthony K. L. Fung, Cheuk M. Lee, Jacob J. Plattner
  • Patent number: 5576322
    Abstract: 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: Grant
    Filed: February 18, 1994
    Date of Patent: November 19, 1996
    Assignee: 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
  • Patent number: 5571815
    Abstract: 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: Grant
    Filed: March 11, 1993
    Date of Patent: November 5, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang Schaper, Rainer Preuss, Gerhard Salbeck, deceased, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter L ummen, Werner Bonin
  • Patent number: 5550229
    Abstract: 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: Grant
    Filed: June 21, 1994
    Date of Patent: August 27, 1996
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Tameo Iwasaki, Kazuhiko Kondo, Hiroshi Ohmizu
  • Patent number: 5536723
    Abstract: 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: Grant
    Filed: October 6, 1994
    Date of Patent: July 16, 1996
    Assignee: Brigham & Women's Hospital
    Inventors: Joseph Loscalzo, John Cooke
  • Patent number: 5482941
    Abstract: 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: Grant
    Filed: May 6, 1994
    Date of Patent: January 9, 1996
    Assignee: Pfizer Inc.
    Inventor: Nicholas K. Terrett
  • Patent number: 5470975
    Abstract: 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: Grant
    Filed: January 11, 1994
    Date of Patent: November 28, 1995
    Assignee: E.R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 5430148
    Abstract: 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: Grant
    Filed: March 31, 1992
    Date of Patent: July 4, 1995
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Stephen E. Webber, Ted M. Bleckman, John Attard, Terence R. Jones, Michael D. Varney
  • Patent number: 5401745
    Abstract: 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: Grant
    Filed: March 19, 1993
    Date of Patent: March 28, 1995
    Assignee: 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.
  • Patent number: 5395838
    Abstract: 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: Grant
    Filed: July 13, 1993
    Date of Patent: March 7, 1995
    Assignees: Imperial Chemical Industries PLC, National Research Development Corporation
    Inventors: Andrew J. Barker, Leslie R. Hughes, Peter R. Marsham, John Oldfield, Stephen J. Pegg
  • Patent number: 5389600
    Abstract: 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: Grant
    Filed: May 21, 1993
    Date of Patent: February 14, 1995
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Thomas P. Selby
  • Patent number: 5385894
    Abstract: Novel disubstituted 6-aminoquinazolinones of the Formula (I), are useful as angiotensin II antagonists: ##STR1##
    Type: Grant
    Filed: April 4, 1994
    Date of Patent: January 31, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Stephen E. de Laszlo, Tomasz W. Glinka, William J. Greenlee, Prasun K. Chakravarty, Arthur A. Patchett
  • Patent number: 5316906
    Abstract: 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: Grant
    Filed: August 23, 1991
    Date of Patent: May 31, 1994
    Assignee: 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
  • Patent number: 5264439
    Abstract: Substituted heterocycles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I are useful as angiotensin II antagonists.
    Type: Grant
    Filed: August 13, 1991
    Date of Patent: November 23, 1993
    Assignee: Merck & Co., Inc.
    Inventors: William J. Greenlee, David Hangauer, Arthur A. Patchett, Thomas F. Walsh, Kenneth J. Fitch, Daljit S. Dhanoa, Ralph A. Rivero
  • Patent number: 5240928
    Abstract: Novel substituted quinazolinones of the formula (I), which are useful as angiotensin II antagonists, are disclosed.
    Type: Grant
    Filed: March 6, 1991
    Date of Patent: August 31, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Eric E. Allen, Stephen E. de Laszlo, Prasun K. Chakravarty, William J. Greenlee, Arthur A. Patchett, Thomas F. Walsh
  • Patent number: 5236927
    Abstract: 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: Grant
    Filed: December 12, 1990
    Date of Patent: August 17, 1993
    Assignee: National Research Development Corporation
    Inventors: Terence R. Jones, Ann L. Jackman, David R. Newell
  • Patent number: 5223501
    Abstract: Novel substituted fused pyrimidinones of formula (I) are useful as angiotensin II antagonists.
    Type: Grant
    Filed: May 10, 1991
    Date of Patent: June 29, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Prasun K. Chakravarty, Nathan B. Mantlo, William J. Greenlee, Arthur A. Patchett, Dooseop Kim
  • Patent number: 5208239
    Abstract: 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: Grant
    Filed: October 31, 1991
    Date of Patent: May 4, 1993
    Assignee: Imperial Chemical Industries PLC
    Inventors: Michael J. Robson, Paul A. Worthington
  • Patent number: 5147875
    Abstract: This invention relates to quinazolinone derivatives which have bronchodilator activity. A compound of the invention is 2-(2-propoxyphenyl)quinazolin-4(3H)-one.
    Type: Grant
    Filed: November 30, 1989
    Date of Patent: September 15, 1992
    Assignee: Sanshin Kogyo Kabishiki Kaisha
    Inventors: William J. Coates, Lawrence I. Kruse
  • Patent number: 5081124
    Abstract: 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: Grant
    Filed: September 5, 1990
    Date of Patent: January 14, 1992
    Assignee: Imperial Chemical Industries PLC
    Inventor: Leslie R. Hughes
  • Patent number: 5053411
    Abstract: 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: Grant
    Filed: April 20, 1989
    Date of Patent: October 1, 1991
    Assignee: Anaquest, Inc.
    Inventors: Jerome R. Bagley, Nhora L. Lalinde, Bao-Shan Huang, H. Kenneth Spencer
  • Patent number: 5051506
    Abstract: 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: Grant
    Filed: March 4, 1988
    Date of Patent: September 24, 1991
    Assignee: Displaytech, Inc.
    Inventors: Michael D. Wand, David M. Walba
  • Patent number: 5025001
    Abstract: 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: Grant
    Filed: March 24, 1989
    Date of Patent: June 18, 1991
    Assignee: Brigham and Women's Hospital
    Inventors: Joseph Loscalzo, John Cooke
  • Patent number: 4992550
    Abstract: 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: Grant
    Filed: April 6, 1989
    Date of Patent: February 12, 1991
    Assignee: Imperial Chemical Industries PLC
    Inventor: Leslie R. Hughes
  • Patent number: 4981856
    Abstract: 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: Grant
    Filed: April 12, 1990
    Date of Patent: January 1, 1991
    Assignee: Imperial Chemical Industries PLC
    Inventor: Leslie R. Hughes
  • Patent number: 4920224
    Abstract: 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: Grant
    Filed: March 13, 1989
    Date of Patent: April 24, 1990
    Assignee: Pfizer Inc.
    Inventor: Edward A. Glazer
  • Patent number: 4908448
    Abstract: 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: Grant
    Filed: August 4, 1989
    Date of Patent: March 13, 1990
    Assignee: BASF Aktiengesellschaft
    Inventors: Reinhard Aldag, Peter Neumann, Andreas Boettcher, Thomas Bluemel, Friedrich Seitz
  • Patent number: 4849518
    Abstract: 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: Grant
    Filed: March 24, 1988
    Date of Patent: July 18, 1989
    Assignee: Pfizer Inc.
    Inventor: Edward A. Glazer
  • Patent number: 4788204
    Abstract: 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: Grant
    Filed: May 28, 1986
    Date of Patent: November 29, 1988
    Assignee: Rhone-Poulenc Sante
    Inventors: Jesus Benavides, Marie-Christine Dubroeucq, Gerard LeFur, Christian Renault
  • Patent number: 4788199
    Abstract: 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: Grant
    Filed: March 11, 1988
    Date of Patent: November 29, 1988
    Assignee: Rhone-Poulenc Sante
    Inventors: Jesus Benavides, Marie-Christine Dubroeucq, Gerard Le Fur, Christian Renault
  • Patent number: 4766211
    Abstract: 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: Grant
    Filed: August 27, 1986
    Date of Patent: August 23, 1988
    Assignee: Ciba-Geigy Corporation
    Inventors: Rudolf Zink, Ian J. Fletcher