Patents Examined by Y. N. Gupta
  • Patent number: 5256655
    Abstract: Compounds of the formula [I] and salts thereof, which are useful for treatment of liver disorders, ##STR1## wherein X is oxygen or sulfur; andA is straight C.sub.3 -C.sub.4 alkylene which can be substituted by one or more lower alkyl groups.
    Type: Grant
    Filed: October 30, 1992
    Date of Patent: October 26, 1993
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Takakazu Morita, Shiro Mita, Yoichi Kawashima
  • Patent number: 5254558
    Abstract: The present invention relates to certain novel substituted heterocycles which are 1-pyrimidinylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these substituted heterocycles, processes for preparing the substituted heterocycles, pharmaceutical compositions containing such substituted heterocycles and methods for their use.
    Type: Grant
    Filed: August 14, 1992
    Date of Patent: October 19, 1993
    Assignee: Imperial Chemical Industries PLC
    Inventors: Peter R. Bernstein, Philip D. Edwards, Royston M. Thomas, Chris A. Veale, Peter Warner, Donald J. Wolanin
  • Patent number: 5254548
    Abstract: A compound having an aryltriazine structure selected from those of formula (I): ##STR1## for which the meaning of the substituents Ar, R.sub.1, R.sub.5, R.sub.6, and R.sub.6 ' is given in the description.The compound of the invention is useful as medicinal product for disorders associated with a cholinergic dysfunction.
    Type: Grant
    Filed: January 14, 1992
    Date of Patent: October 19, 1993
    Assignee: Adir et Compagnie
    Inventors: Camille-Georges Wermuth, Jean-Jacques Bourguignon, Isabelle Morin, Pierre Renard, Michelle Devissaguet, Jean-Francois R. de La Faverie, Gerard Adam
  • Patent number: 5254745
    Abstract: Polyoxyalkylene polyols initiated with melamine and coinitiated with toluene diamine and oxyalkylated with one or more alkylene oxides have relatively low viscosity and are suitable for preparing polyurethane foams.
    Type: Grant
    Filed: November 12, 1991
    Date of Patent: October 19, 1993
    Assignee: BASF Corporation
    Inventor: Joachim Jahme
  • Patent number: 5254682
    Abstract: Compounds of the formula: ##STR1## are disclosed. These compounds inhibit the angiotensinogen-cleaving action of the natural proteolytic enzyme, renin, and are useful in treating, preventing or managing renin-associated hypertension, hyperaldosteronism, congestive heart failure, and glaucoma.
    Type: Grant
    Filed: June 11, 1991
    Date of Patent: October 19, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Daljit S. Dhanoa, Arthur A. Patchett, William J. Greenlee, William H. Parsons, Thomas A. Halgren, Ann E. Weber, Lihu Yang
  • Patent number: 5250687
    Abstract: 1,3,5-TRINITROHEXAHYDRO-1,3,5-TRIAZINE (RDX) is prepared in a new simplif and efficient manner which provides near quantitative yield. Our process is based upon the nitration of 3,7-DIACETYL 1,3,5,7 TETRAAZA[3.3.1.]BICYCLONONANE (DAPT).
    Type: Grant
    Filed: August 28, 1992
    Date of Patent: October 5, 1993
    Assignee: The United States of America as represented by the Secretary of the Army
    Inventors: William J. Lukasavage, Steven Nicolich, Norman Slagg
  • Patent number: 5250505
    Abstract: Cyclohexenone oxime ethers I ##STR1## where R.sup.1 is C.sub.1 -C.sub.6 -alkyl, A is unsubstituted or substituted C.sub.3 -C.sub.6 -alkynylene, Z is unsubstituted or substituted phenyl an unsubstituted or substituted 6-membered or 7-membered saturated or monounsaturated or diunsaturated heterocyclic structure having one or two hetero atoms selected from the group consisting of oxygen and sulfer, and their agriculturally useful salts and esters of C.sub.1 -C.sub.10 -carboxylic acids and inorganic acids, are suitable as herbicides.
    Type: Grant
    Filed: May 8, 1991
    Date of Patent: October 5, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Juergen Kast, Norbert Meyer, Ulf Misslitz, Albrecht Harreus, Thomas Kuekenhoehner, Harald Bang, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
  • Patent number: 5250548
    Abstract: Compounds are disclosed having the formula: ##STR1## The compounds of the invention are angiotensin II receptor antagonists.
    Type: Grant
    Filed: March 2, 1992
    Date of Patent: October 5, 1993
    Assignee: Abbott Laboratories
    Inventors: Martin Winn, Biswanath De, Thomas M. Zydowsky, Daniel J. Kerkman, John F. DeBernardis, Saul H. Rosenberg, Kazumi Shiosaki, Fatima Z. Basha, Andrew S. Tasker, Thomas W. von Geldern, Jeffrey A. Kester, Steven Boyd, Diane M. Yamamoto, Anthony K. L. Fung
  • Patent number: 5250534
    Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is H, C.sub.1 -C.sub.3 alkyl, C.sub.3 -C.sub.5 cycloalkyl or C.sub.1 -C.sub.3 perfluoroalkyl; R.sup.2 is H, C.sub.1 -C.sub.6 alkyl optionally substituted by OH, C.sub.1 -C.sub.3 alkoxy or C.sub.3 -C.sub.6 cycloalkyl, or C.sub.1 -C.sub.3 perfluoroalkyl; R.sup.3 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.6 perfluoroalkyl or (C.sub.3 -C.sub.6 cycloalkyl)C.sub.1 -C.sub.6 alkyl; R.sup.4 taken together with the nitrogen atom to which it is attached completes a pyrrolidinyl, piperidino, morpholino, or 4-N-(R.sup.6)-piperazinyl group; R.sup.5 is H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.3 alkoxy, NR.sup.7 R.sup.8, or CONR.sup.7 R.sup.8 ; R.sup.6 is H, C.sub.1 -C.sub.6 alkyl, (C.sub.1 -C.sub.3 alkoxy) C.sub.2 - C.sub.6 alkyl, hydroxy C.sub.2 -C.sub.6 alkyl, (R.sup.7 R.sup.8 N)C.sub.2 -C.sub.6 alkyl, (R.sup.7 R.sup.8 NCO)C.sub.1 -C.sub.6 alkyl, CONR.sup.7 R.sup.8, CSNR.sup.7 R.sup.
    Type: Grant
    Filed: May 14, 1992
    Date of Patent: October 5, 1993
    Assignee: Pfizer Inc.
    Inventors: Andrew S. Bell, David Brown, Nicholas K. Terrett
  • Patent number: 5248679
    Abstract: The invention relates to novel cholecystokinin antagonists of the formula ##STR1## wherein R.sup.1 is aryl which may have suitable substituent(s), X is --O-- or ##STR2## in which R.sup.3 is hydrogen or lower alkyl, A is bond; or methylene, ethylene, trimethylene, tetramethylene, pentamethylene or hexamethylene, each of which may have lower alkyl group(s), andR.sup.2 is heterocyclic(C.sub.3 -C.sub.6) alkenoyl or heterocycliciccarbonyl, or a pharmaceutically acceptable salt thereof, useful as a cholecystokinin antagonist.
    Type: Grant
    Filed: July 27, 1992
    Date of Patent: September 28, 1993
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Yoshinari Sato, Teruaki Matuo, Takatomo Ogahara
  • Patent number: 5248692
    Abstract: Novel DC-89 derivatives as shown below have an excellent anti-tumor activity, and thus are useful as anti-tumor agent ##STR1## wherein L represents chlorine or bromine; R represents ##STR2## (wherein n represents an integer of 4 to 7) or ##STR3## (wherein Y represents oxygen or N--M).
    Type: Grant
    Filed: March 1, 1993
    Date of Patent: September 28, 1993
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Hiromitsu Saito, Akira Asai, Satoru Nagamura, Eiji Kobayashi, Katsushige Gomi
  • Patent number: 5246939
    Abstract: A compound which is a 2-aminopyrimidine carboxamide derivative represented by formula (I) ##STR1## in which X represents hydrogen, fluorine, chlorine, methyl, 1-methylethyl or methoxy, with the proviso that more than one substituent X may be present in which case each X may be the same or different,n represents 2 or 3,m represents 1, in which case p represents 1, or elsem represents 0, in which case p represents 2,q represents 0 or 1, andR.sub.1 represents a hydrogen atom;or a pharmaceutically acceptable acid addition salt thereof.A compound of formula (I) has .alpha..sub.1 -adrenergic receptor antagonist activity and is useful as a therapeutic substance.
    Type: Grant
    Filed: June 26, 1992
    Date of Patent: September 21, 1993
    Assignee: Synthelabo
    Inventors: Pascal George, Christian Maloizel, Benoit Marabout, Jean-Pierre Merly
  • Patent number: 5246929
    Abstract: Thiazine (or oxazine) derivatives of the formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 are both H or form a naphthalene ring together with the benzene ring; R.sup.3 and R.sup.4 are both H, or one of them is halogen and another is H; X is S or O; R.sup.5 and R.sup.6 are each i) H, ii) lower alkyl, iii) cycloalkyl, iv) substituted phenyl, v) naphthyl, vi) lower alkyl which is substituted by substituted or unsubstituted phenyl, or vii) S-containing heterocyclic group; one of Z.sup.1 and Z.sup.2 is O and another is H.sub.2 ; A is lower alkylene; R.sup.7 and R.sup.8 are each i) H, ii) lower alkyl, iii) lower alkenyl, iv) lower alkynyl, or v) lower alkyl which is substituted by substituted or unsubstituted phenyl, or both form together N-containing heterocyclic group; provided that when both of R.sup.1 and R.sup.2 are H, Z.sup.2 is O and either one of R.sup.5 and R.sup.
    Type: Grant
    Filed: January 31, 1991
    Date of Patent: September 21, 1993
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Masakatsu Ozeki, Shin-ichi Kodato, Kousuke Yasuda, Yukitsuka Kudo, Kayoko Maeda
  • Patent number: 5245040
    Abstract: A process for the preparation of 1,3-disubstituted 2-nitroguanidines of the formula I ##STR1## in which R.sub.1 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or a radical --CH.sub.2 B; A is an unsubstituted or mono- to tetrasubstituted aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical, which may contain one or two substituents from the group comprising C.sub.1 -C.sub.3 haloalkyl having 1 to 7 halogen atoms, cyclopropyl, halocyclopropyl having 1 to 3 halogen atoms, C.sub.2 -C.sub.3 alkenyl, C.sub.2 -C.sub.3 alkynyl, C.sub.2 -C.sub.3 haloalkenyl and C.sub.2 -C.sub.3 haloalkynyl having 1 to 4 halogen atoms, C.sub.1 -C.sub.3 haloalkoxy having 1 to 7 halogen atoms, C.sub.1 -C.sub.3 alkylthio, C.sub.1 -C.sub.3 haloalkylthio having 1 to 7 halogen atoms, allyloxy, propargyloxy, allylthio, propargylthio, haloallyloxy, haloallylthio, cyano and nitro and one to four substituents from the group comprising C.sub.1 -C.sub.3 alkyl, C.sub.
    Type: Grant
    Filed: October 16, 1991
    Date of Patent: September 14, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Peter Maienfisch, Odd Kristiansen, Laurenz Gsell
  • Patent number: 5242948
    Abstract: The present invention relates to bisguanidine derivatives of the formula I ##STR1## where R.sup.1 and R.sup.2 are each, independently of one another, hydrogen, alkyl, alkenyl, alkenyl, alkoxyalkyl, haloalkenyl; or cycloalkyl which has 5-12 carbon atoms in the ring and may be substituted, or benzyl which may be substituted, with the proviso that only one of R.sup.1 and R.sup.2 can be hydrogen; orR.sup.1 and R.sup.2 are, together with the atoms which they substitute, a heterocyclic ring which may be substituted;X is CH.sub.2, O, a single bond, NH, N-alkyl or N-benzyl whose phenyl ring may be substituted,n is 5 to 8,and their plant-compatible acid addition salts and their metal complexes and fungicides containing these compounds.
    Type: Grant
    Filed: August 9, 1991
    Date of Patent: September 7, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Thomas Mueller, Matthias Zipplies, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 5242919
    Abstract: Novel 2,3-dihydro-1H-indene derivatives and salts thereof represented by the general formula (1), ##STR1## [wherein R.sup.1 and R.sup.2 are each a hydrogen atom, a lower alkyl group, a phenyl group which may have halogen atoms and/or alkyl groups as the substituents on the phenyl ring; R.sup.3 is a halgoen atom or a lower alkyl group; R.sup.4 is a hydrogen atom, a halogen atom, a phenyl-lower alkyl group, a cycloalkyl-lower alkyl group or the like; R.sup.5 is a hydroxyimino group, an alkylamino group or a group of the formula --NHR.sup.8 (wherein R.sup.8 is a hydrogen atom, a halogen-substituted lower alkanoyl group or the like); R.sup.6 is a hydrogen atom or a phenyl group; and R.sup.7 is a hydrogen atom or a lower alkyl group].
    Type: Grant
    Filed: June 13, 1991
    Date of Patent: September 7, 1993
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Yasuo Oshiro, Hiraki Ueda, Kazuyuki Nakagawa
  • Patent number: 5240956
    Abstract: 2-Heteroaromatic alkanoate esters which are useful as inhibitors of human leukocyate or neutrophil elastase.
    Type: Grant
    Filed: April 13, 1992
    Date of Patent: August 31, 1993
    Assignee: Cortech, Inc.
    Inventors: Gary P. Kirschenheuter, Raymond T. Cunningham, John C. Cheronis
  • Patent number: 5240499
    Abstract: Polymeric, water-soluble triazine compounds which contain both basic and acidic groups in the molecule have out-standing surfactant properties and are suitable for the preparation of dispersions of solids, preferably of dispersions of inorganic and/or organic pigments, in an aqueous or water-dilutable medium. Since these triazine compounds are colorless or only slightly colored, they do not influence the shade of the medium used.
    Type: Grant
    Filed: December 13, 1991
    Date of Patent: August 31, 1993
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Rainer Az, Wolfgang Schwab, Dieter Schnaitmann, Erwin Dietz
  • Patent number: 5238908
    Abstract: This invention relates to glutaramic acids and derivatives exhibiting herbicidal activity having the structure ##STR1## wherein A is a carboxylic acid or a derivative thereof, D is CH or N, and R, R.sup.1, R.sup.2, T, X, Y, and Z are as defined within, compositions containing these compounds and methods of controlling weeds with these compounds.
    Type: Grant
    Filed: August 9, 1990
    Date of Patent: August 24, 1993
    Assignee: Rohm and Haas Company
    Inventors: Barry C. Lange, John W. Ashmore, Jane Wissinger-Cornille
  • Patent number: 5238942
    Abstract: Novel substituted quinazolinones of the formula (I) are useful as angiotensin II antagonists.
    Type: Grant
    Filed: April 16, 1992
    Date of Patent: August 24, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Prasun K. Chakravarty, William J. Greenlee, Nathan B. Mantlo, Arthur A. Patchett, Dooseop Kim, Stephen E. de Laszlo, Tomasz W. Glinka