The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/253)
  • Patent number: 5684028
    Abstract: Novel compounds of the formula ##STR1## wherein the, substituents are defined as in the specification and their non-toxic, pharmaceutically acceptable salts which inhibit the effects of angiotensin II in warm-blooded animals.
    Type: Grant
    Filed: October 9, 1996
    Date of Patent: November 4, 1997
    Assignee: Roussel UCLAF
    Inventors: Jean Claude Caille, Alain Corbier, Michel Fortin, Gilles Hamon, Simone Jouquey, Jean Paul Vevert
  • Patent number: 5684024
    Abstract: Substituted pyrazole dimers are useful in prophylaxis and treatment of influenza virus infections.
    Type: Grant
    Filed: May 13, 1996
    Date of Patent: November 4, 1997
    Assignee: Viropharma Incorporated
    Inventors: Guy D. Diana, Dorothy C. Young, Tandy D. Goldstein, Theodore J. Nitz, John Swestock, William P. Gorczyca
  • Patent number: 5684029
    Abstract: The invention relates to benzimidazoles of general formula ##STR1## wherein R.sub.1 to R.sub.4 are as defined herein, the 1-, 3-isomer mixtures thereof and the addition salts thereof. The new compounds are useful, in particular, as angiotensin antagonists.
    Type: Grant
    Filed: February 20, 1996
    Date of Patent: November 4, 1997
    Assignee: Karl Thomae GmbH
    Inventors: Berthold Narr, Norbert Hauel, Jacques Van Meel, Wolfgang Wienen, Michael Entzeroth, Uwe Ries
  • Patent number: 5681844
    Abstract: This invention relates to compounds which inhibit thrombin or factor Xa. The compounds contain an aldehyde functionality and a methionine sulfone or S-substituted cysteine sulfone residue. The compounds and their pharmaceutical compositions are useful for preventing thrombosis in mammals which are suspected of having a condition characterized by abnormal thrombosis.
    Type: Grant
    Filed: April 28, 1994
    Date of Patent: October 28, 1997
    Assignee: Corvas International, Inc.
    Inventors: Matthew M. Abelman, Robert J. Ardecky, Ruth F. Nutt
  • Patent number: 5675024
    Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification have retinoid-like biological activity.
    Type: Grant
    Filed: November 22, 1995
    Date of Patent: October 7, 1997
    Assignee: Allergan
    Inventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
  • Patent number: 5674879
    Abstract: Conformationally restricted compounds are described which are therapeutically effective as angiotensin II antagonists for the treatment of circulatory disorders.
    Type: Grant
    Filed: March 3, 1995
    Date of Patent: October 7, 1997
    Assignee: G.D. Searle & Co.
    Inventors: Robert E. Manning, Horng-Chih Huang
  • Patent number: 5674905
    Abstract: Compounds of formula (I), wherein A is selected from (a), (b), (c), (d), (e), (f) and B is selected from (g), (h), and (i), wherein W is a carbonyl, sulphonyl or sulphinyl group, and X is a carbonyl, sulphonyl or sulphinyl group or --C(O)--CH.sub.2 -- (in which the carbonyl group is bonded to Y), provided that at least one of W and X contains carbonyl, Y is R.sub.9 --O-- or R.sub.9 --N(R.sub.10)--, Z is selected from (i), (ii), (iii), (iv) or Z is absent and W is H, with a number of provisions and phamaceutically acceptable salts thereof are ligands at CCK and/or gastrin receptors.
    Type: Grant
    Filed: December 19, 1994
    Date of Patent: October 7, 1997
    Assignee: James Black Foundation Limited
    Inventors: Sarkis Barret Kalindjian, Caroline Minli Rachel Low, Michael John Pether, Jonathan Michael Richard Davies, David John Dunstone, Iain Mair McDonald
  • Patent number: 5663171
    Abstract: The present invention is directed to certain compounds of the general structural formula: ##STR1## wherein R.sub.1, R.sub.1a, R.sub.2a, R.sub.3, R.sub.3a, R.sub.4, R.sub.5, R.sub.6, A, W, and n are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.
    Type: Grant
    Filed: March 3, 1995
    Date of Patent: September 2, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Meng Hsin Chen, Gregori J. Morriello, Ravi Nargund, Arthur A. Patchett, Lihu Yang
  • Patent number: 5658935
    Abstract: The invention concerns heterocyclic compounds of the general formula (I) in which A, B, R, R.sup.2, R.sup.3, W, Y, Z.sup.1, Z.sup.2 and r are as defined in the description, methods of preparing them and their use as inhibitors of thrombocyte aggregation, the metastization of carcinoma cells and the binding of osteoclasts on bone surfaces.
    Type: Grant
    Filed: January 17, 1996
    Date of Patent: August 19, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Otmar Klingler, Gerhard Zoller, Bernd Jablonka, Melitta Just, Gerhard Breipohl, Jochen Knolle, Wolfgang Konig
  • Patent number: 5658939
    Abstract: This invention relates to compounds which inhibit thrombin or factor Xa. The compounds contain an aldehyde functionality and a methionine sulfone or S-substituted cysteine sulfone residue. The compounds and their pharmaceutical compositions are useful for preventing thrombosis in mammals which are suspected of having a condition characterized by abnormal thrombosis.
    Type: Grant
    Filed: April 18, 1995
    Date of Patent: August 19, 1997
    Assignee: Corvas International Inc.
    Inventors: Matthew Mark Abelman, Robert John Ardecky, Ruth Foelsche Nutt
  • Patent number: 5656619
    Abstract: Abstract of the Disclosure: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 12, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5650511
    Abstract: Derivatives of 9-deazaguanine are prepared by reacting an aldehyde or ketone with a dialkylaminomalonate to form the corresponding enamine. The enamine is then reacted with a base to form a cyclic pyrrole. The cyclic pyrrole is reacted with an urea compound to provide a protected guanidino compound. The guanidino is converted to the desired 9-deazaguanine derivative by reacting with trifluoracetic acid or with an alkoxide or hydroxide followed by neutralization with an acid.
    Type: Grant
    Filed: December 12, 1995
    Date of Patent: July 22, 1997
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Arthur J. Elliott, David A. Walsh
  • Patent number: 5648387
    Abstract: Dialkyl ethers lower Lp(a) and triglycerides, and elevate HDL-cholesterol, and are thereby useful for treating vascular diseases and noninsulin-dependent diabetes mellitus.
    Type: Grant
    Filed: March 24, 1995
    Date of Patent: July 15, 1997
    Assignee: Warner-Lambert Company
    Inventors: Charles Larry Bisgaier, Paul Leroy Creger, Alan Robert Saltiel, Sherrie Rae Tafuri
  • Patent number: 5646171
    Abstract: An angiotensin II antagonist of the formula: ##STR1## in which: R.sub.p.sup.1 represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or C.sub.1 -C.sub.6 alkanoyl; R.sub.p.sup.2 represents a single bond, C.sub.1 -C.sub.4 alkylene or C.sub.1 -C.sub.4 alkylidene; R.sub.p.sup.3 and R.sub.p.sup.4 are independently selected from the group consisting of hydrogen and C.sub.1 -C.sub.6 alkyl; R.sub.p.sup.5 represents hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl, naphthyl, benzyl, diphenylmethyl, naphthylmethyl, alkanoyloxyalkyl, cycloalkanecarbonyloxyalkyl, alkoxycarbonyloxyalkyl, cycloalkyloxycarbonyloxyalkyl, (5-phenyl-2-oxo-1,3-dioxolen-4-yl)methyl, (5-alkyl-2-oxo-1,3-dioxolen-4-yl)methyl or phthalaidyl; R.sub.p.sup.6 represents a carboxy or a tetrazol-5-yl; and X.sub.p represents an oxygen or sulfur, and pharmaceutically acceptable salts thereof. The compounds have hypotensive activity and can thus be used for the treatment and prophylaxis of hypertension.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: July 8, 1997
    Assignee: Sankyo Company, Limited
    Inventors: Hiroaki Yanagisawa, Yoshiya Amemiya, Yasuo Shimoji, Takuro Kanazaki, Hiroyuki Koike, Toshio Sada
  • Patent number: 5646295
    Abstract: The invention concerns diazapentalene derivatives of formula I ##STR1## in which X and Y represent leaving groups which are less nucleophilic than thiol compounds, as thiol-specific fluorochromes for the detection of compounds containing thiol groups, in particular in cells.
    Type: Grant
    Filed: January 31, 1996
    Date of Patent: July 8, 1997
    Assignee: Boehringer Mannheim GmbH
    Inventors: Rudolf Gompper, Manfred Kubbies, Axel Schmidt, Bernhard Virnekas
  • Patent number: 5646170
    Abstract: Pharmaceutically useful compounds having ACAT inhibitory activity of the formula ##STR1## wherein n is 0, 1, or 2, for X other than tetrazole and n=2 then R.sub.2 .dbd.R.sub.3 .dbd.H; R.sub.1 is phenyl, substituted phenyl, naphthyl, substituted naphthyl, a heteroaromatic group or a hydrocarbon group having from one to 18 carbon atoms; R.sub.2 and R.sub.3 are hydrogen, halo, hydroxy, alkyl, alkenyl, cycloalkyl, phenyl, substituted phenyl, a heteroaryl, or form a spiroalkyl group; X is a heteromonocyclic 5-membered ring containing one to four heteroatoms, said heteroatoms being nitrogen, oxygen or sulfur, and combination thereof; and R.sub.4 is a hydrocarbon group having from one to 20 carbon atoms are described as well as methods of their manufacture.
    Type: Grant
    Filed: May 3, 1995
    Date of Patent: July 8, 1997
    Assignee: Warner-Lambert Company
    Inventors: Helen Tsenwhei Lee, Patrick Michael O'Brien, Joseph Armand Picard, Claude Forsey Purchase, Jr., Bruce David Roth, Drago Robert Sliskovic, Andrew David White
  • Patent number: 5641778
    Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is a 2-R.sub.A -3-R.sub.B -phenyl radical, a 2-R.sub.A -4-R.sub.C -phenyl radical, a 2-R.sub.A -pyridin-3-yl radical, a 3-R.sub.A -pyridin-2-yl radical or a 1-R.sub.D -indol-3-yl radical, wherein one of the radicals R.sub.A and R.sub.B is an aliphatic or heterocycloaliphatic-aliphatic radical or free or aliphatically, araliphatically or heteroaraliphatically etherified hydroxy and the other is hydrogen, an aliphatic radical or free or esterified or amidated carboxy, R.sub.C is hydrogen, an aliphatic radical, free or aliphatically, araliphatically, heteroaraliphatically or heteroarylaliphatically etherified hydroxy or an unsubstituted or heteroaliphatically substituted amino group, and R.sub.D is an aliphatic, araliphatic or heteroaliphatic radical, one of the radicals X.sub.1 and X.sub.2 is carbonyl and the other is methylene, R.sub.2 is an aliphatic radical, R.sub.3 is unsubstituted or aliphatically substituted amino, R.sub.
    Type: Grant
    Filed: December 6, 1995
    Date of Patent: June 24, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Jurgen Klaus Maibaum, Pascal Rigollier, Peter Herold, Nissim Claude Cohen, Richard Goschke, Stefan Stutz
  • Patent number: 5637722
    Abstract: "Esters" are synthesized by reacting a nucleophile with a propargyl xanthate advantageously having the formula (I):R.sub.3 --C.tbd.C--CR.sub.1 R.sub.2 --S--CS--Y--R (I)in the presence of at least one acid, Bronsted or otherwise, and at a temperature ranging from 0.degree. to 300.degree. C.; the subject reaction is particularly applicable to a wide variety of chiral organic syntheses.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: June 10, 1997
    Assignee: Rhone-Poulenc Chimie
    Inventors: Jean Boivin, Eric B. Henriet, Samir Z. Zard
  • Patent number: 5629432
    Abstract: This appliciation discloses a process for preparing a lactone of general formula (I), where R is an optionally substituted phenyl group or an optionally substituted mono- or bicyclic heteroaryl radical which process comprises reacting an anion of a malonate of formula (II) with an ethylene compound of formula (III) Y--CH.sub.2 --CH.sub.2 OZ, to give a compound of formula (IV) and hydrolysing the compound of formula (IV) to give a lactone of formula (I). The lactones are of use as intermediates for preparing 5-HT.sub.1A binding agents.
    Type: Grant
    Filed: May 16, 1995
    Date of Patent: May 13, 1997
    Assignee: John Wyeth & Brother, Ltd.
    Inventor: Robin G. Shepherd
  • Patent number: 5629331
    Abstract: The present invention relates to a process for the preparation of the 2-n.butyl-3-[[2'-(tetrazol-5-yl)biphenyl-4-yl]methyl]-1,3-diazaspiro [4.4]-non-1-en-4-one by reaction of the corresponding nitrile with an alkaline azide and triethylamine hydrochloride, recovering the 2-n.butyl-3-[[2'-(tetrazol-5-yl)biphenyl-4-yl]methyl]-1,3-diazaspiro[4.4]n on-1-en-4-one in form of one of its alkaline salts in aqueous solution, by neutralization of said alkaline salt and crystallization of the 2-n.butyl-3-[[2'-(tetrazol-5-yl)-biphenyl-4-yl]methyl]-1,3-diazaspiro[4.4] non-1-en-4-one thus precipitated either in a solvent containing less than 10% of water or in a solvent containing more than 10% of water in order to obtain two differents crystalline forms. Furthermore a novel crystalline form of 2-n.butyl-3-[[2'-(tetrazol-5-yl)biphenyl-4-yl]methyl]-1,3-diazaspiro[4.4] non-1-en-4-one and pharmaceutical compositions containing it are described.
    Type: Grant
    Filed: October 17, 1995
    Date of Patent: May 13, 1997
    Assignee: Sanofi
    Inventors: Antoine Caron, Dominique Chantreux, Colette Bouloumie
  • Patent number: 5627283
    Abstract: Amidinophenylalanine derivatives of the formula I ##STR1## the synthesis of these compounds, the use thereof and pharmaceutical agents which contain these compounds are described.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: May 6, 1997
    Assignee: Behringwerke Aktiengesellschaft
    Inventors: Werner St uber, Gerhard Dickneite, Rainer Koschinsky, Cenek Kolar
  • Patent number: 5620998
    Abstract: The invention relates to N-acyl-N-heterocyclylalkylamino acids of the formula ##STR1## wherein Y.sub.1 is O, S or N(R) and R is hydrogen or C.sub.1 -C.sub.7 alkyl;X.sub.1 is --CO-- or --S(O).sub.m -- and the index m is 0, 1 or 2;one of the variables X.sub.2 and X.sub.4 is C.sub.1 -C.sub.4 alkylene and the other of the variables X.sub.2 and X.sub.4 is a bond; or each of the variables X.sub.2 and X.sub.4 is a bond;X.sub.3 is C.sub.3 -C.sub.7 cycloalkylidene or the structural element --C(X.sub.a)(X.sub.b)-- and X.sub.a is hydrogen or C.sub.1 -C.sub.7 alkyl and X.sub.b is C.sub.1 -C.sub.7 alkyl;and the rings A, B and C, with the exception of the substituents indicated in the formula, and also aromatic substituents are, independently of one another, unsubstituted or mono- or poly-substituted by substituents selected from the group consisting of halogen, C.sub.1 -C.sub.7 alkyl, C.sub.1 -C.sub.7 alkoxy, C.sub.2 -C.sub.7 alkenyloxy, phenoxy, benzyloxy, trifluoromethyl and S(O).sub.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: April 15, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Tibur Schmidlin, Paul Zbinden, Peter B uhlmayer
  • Patent number: 5618975
    Abstract: Biphenyl derivatives and processes for the preparation of biphenyl derivatives are described. A compound of formula (I) is disclosed ##STR1## in which the substituent X is --CHO or --CH(OR.sup.1)OR.sup.2, where R.sup.1 and R.sup.2 independently of one another are (C.sub.1 -C.sub.6)-alkyl or R.sup.1 and R.sup.2 together are an alkylene group (--CH.sub.2).sub.n --, where n is 2, 3 4 or 5 and R is --F, --Cl, --NO.sub.2, --(CH.sub.2).sub.m --COOR.sup.3, --(CH.sub.2).sub.m --CONHR.sup.3, --(CH.sub.2).sub.m --CN, --SO.sub.2 NH--COOR.sup.3, --SO.sub.2 NH--CO--NHR.sup.3, --SO.sub.2 NH--SO.sub.2 --R.sup.3, --NHSO.sub.2 R.sup.3, ##STR2## --PO.sub.3 R.sup.3, --NH--SO.sub.2 --CF.sub.3, --SO.sub.2 NR.sup.4 where R.sup.3 is hydrogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.3 -C.sub.6)cycloalkyl, or (C.sub.1 -C.sub.6)-alkyl-(C.sub.3 -C.sub.6)cycloalkyl and R.sup.4 is a group .dbd.C--N(CH.sub.3).sub.2, and m is 0, 1, 2, 3, or 4.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: April 8, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Adalbert Wagner, Neerja Bhatnagar, Jean Buendia, Christine Griffoul
  • Patent number: 5618793
    Abstract: Compounds of the formula ##STR1## wherein R.sub.3, R.sub.4, J, K, Z, and Het are as set forth herein are described.The compounds of formula I are useful as agents in the treatment of fungal infections.
    Type: Grant
    Filed: August 1, 1995
    Date of Patent: April 8, 1997
    Assignee: Schering Corporation
    Inventors: Alan B. Cooper, Anil K. Saksena, Raymond Lovey, Viyyoor Girijavallabhan, Ashit Ganguly
  • Patent number: 5616721
    Abstract: Disclosed herein is a process for preparing a compound of structure (I): ##STR1## which comprises cyclization of a compound of structure (II) ##STR2##
    Type: Grant
    Filed: May 26, 1995
    Date of Patent: April 1, 1997
    Assignee: SmithKline Beecham plc
    Inventors: Graham Johnson, Neil Smith, Graham R. Geen, Inderjit S. Mann, Vance Novack
  • Patent number: 5616599
    Abstract: Compounds of the following formula (I) or the formula (I).sub.p : ##STR1## wherein R.sup.1 is alkyl or alkenyl; R.sup.2 and R.sup.3 are hydrogen, alkyl, alkenyl, cycloalkyl, aralkyl, aryl, or aryl fused to cycloalkyl; R.sup.4 is hydrogen, alkyl, alkanoyl, alkenoyl, arylcarbonyl, alkoxycarbonyl, tetrahydropyranyl, tetrahydrothiopyranyl, tetrahydrothienyl, tetrahydrofuryl, a group of formula --SiR.sup.a R.sup.b R.sup.c, in which R.sup.a, R.sup.b and R.sup.c are alkyl or aryl, alkoxymethyl, (alkoxyalkoxy)methyl, haloalkoxymethyl, aralkyl, aryl or alkanoyloxymethoxycarbonyl; R.sup.5 is carboxy or --CONR.sup.8 R.sup.9, wherein R.sup.8 and R.sup.9 hydrogens or alkyl, or R.sup.8 and R.sup.9 together form alkylene; R.sup.6 is hydrogen, alkyl, alkoxy or halogen; R.sup.7 is carboxy or tetrazol-5-yl; R.sub.p.sup.1 is hydrogen, alkyl, cycloalkyl or alkanoyl; R.sub.p.sup.2 is a single bond, alkylene or alkylidene; R.sub.p.sup.3 and R.sub.p.sup.4 are each hydrogen or alkyl; R.sub.p.sup.6 is carboxy or tetrazol-5-yl; and X.
    Type: Grant
    Filed: January 26, 1995
    Date of Patent: April 1, 1997
    Assignee: Sankyo Company, Limited
    Inventors: Hiroaki Yanagisawa, Koichi Fujimoto, Yoshiya Amemiya, Yasuo Shimoji, Takuro Kanazaki, Hiroyuki Koike, Toshio Sada
  • Patent number: 5612370
    Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein a, b and d are all carbon atoms or one of a, b and d is a nitrogen atom or --N(O)-- and the others are carbon atoms; Y is a single bond, --CH.sub.2 --, --C(O)--, --O--, --S-- or --N(R.sup.8)--; and R.sup.1 to R.sup.7 are as defined herein. These compounds have potassium channel activating activity and are useful, therefore for example, as cardiovascular agents.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 18, 1997
    Assignee: Bristol-Myers Squibb Company
    Inventor: Karnail S. Atwal
  • Patent number: 5612360
    Abstract: This invention provides novel heterocyclic derivatives, their pharmaceutical formulations, and their use for antagonizing angiotensin II receptors in mammals.
    Type: Grant
    Filed: April 20, 1993
    Date of Patent: March 18, 1997
    Assignee: Eli Lilly and Company
    Inventors: Donald B. Boyd, Sherryl L. Lifer, Winston S. Marshall, Alan D. Palkowitz, William Pfeifer, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, K. Jeff Thrasher, Venkatraghavan Vasudevan, Celia A. Whitesitt
  • Patent number: 5605920
    Abstract: Disclosed are herbicidal tetrazolinone derivatives, selective in paddy fields of the formula ##STR1## wherein X represents C.sub.1-4 alkyl,n represents 1, 2, 3 or 4,R.sup.1 and R.sup.2 each independently represents C.sub.1-6 alkyl, C.sub.2-4 alkenyl, C.sub.2-6 alkynyl, C.sub.3-8 cycloalkyl, aryl which may optionally be substituted (wherein the substituent is at least one radical selected from the group consisting of halogen, C.sub.1-4 alkyl, C.sub.1-2 haloalkyl, C.sub.1-2 haloalkoxy, C.sub.1-2 haloalkylthio, acyl, nitro and cyano) or aralkyl optionally substituted by halogen orR.sup.1 and R.sup.2 form, together with the N-atom to which they are bonded, a cyclic ring which may be substituted. Also, disclosed are novel intermediates useful in the preparation of the compounds of formula (I).
    Type: Grant
    Filed: March 20, 1996
    Date of Patent: February 25, 1997
    Assignee: Nihon Bayer Agrochem K.K.
    Inventors: Toshio Goto, Yoshinori Kitagawa, Seishi Ito, Katsuhiko Shibuya, Tatsuya Yamaoka, Chieko Ueno, Yoshiko Kyo
  • Patent number: 5602161
    Abstract: The tetrazolylphenyl pivalate of the the following general formula or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sup.1 and R.sup.2 each represents a hydrogen atom, a lower alkyl group or other substituents; an elastase-inhibitory composition, a composition for preventing and treating emphysema and a composition for preventing and treating endotoxin-induced lung disorders each comprising the foregoing tetrazolylphenyl pivalate derivative or a non-toxic or acid-addition salt thereof.
    Type: Grant
    Filed: March 6, 1995
    Date of Patent: February 11, 1997
    Assignee: Wakamoto Pharmaceutical Co., Ltd.
    Inventors: Kenji Naito, Ryoki Takahashi, Daisuke Morizono, Mitsuji Agata, Hatsunori Toyofuku, Makoto Maeda
  • Patent number: 5599830
    Abstract: The invention relates to the products: ##STR1## in which: R.sub.1 =alkyl, alkenyl, alkynyl, alkylthio,R.sub.2B, R.sub.3B representing:hydrogen, mercapto, formyl, acyl, carboxy nitro, cyano,--PO.sub.3 (R).sub.2, R representing hydrogen, alkyl, aryl, amino or carbamoyl,the R.sub.4B radicals; ##STR2## n=0 to 2 X'=arylR.sub.4B either represents --(CH.sub.2).sub.m1 --S(O).sub.m2 --X--R.sub.10, m1=0 to 4, m2=0 to 2either m1 is different from 0, X--R.sub.10 represents amino, or whatever m1 is, X represents a single bond or --NH--, --NH--CO--, --NH--CO--NH--,R.sub.10 =alkyl, alkenyl or aryl, or hydrogen, alkyl, alkenyl, alkynyl, acyl or amino,--S--S--R.sub.4B ', R.sub.4B ' represents R.sub.4B except for amino and alkoxy, and one of R.sub.2B and R.sub.3B represents --OR.sub.4B : ##STR3## m=0 to 2, Y.sub.B ---Y.sub.1B --B--Y.sub.2B,Y.sub.1B =aryl,B=a single bond or --CO--, --O--, --NH--CO--, --CO--NH--, --O--O--(CH.sub.2).sub.p --,p=1 to 3,Y.sub.
    Type: Grant
    Filed: January 9, 1995
    Date of Patent: February 4, 1997
    Assignee: Roussel Uclaf
    Inventors: Jean C. Caille, Alain Corbier, Michel Fortin, Gilles Hamon, Simone Jouquey, Jean P. Vevert
  • Patent number: 5597929
    Abstract: There is disclosed a process for producing a 2-(tetrazol-5-yl)-4-oxo-4H-benzopyran of general formula (1): ##STR1## which comprises reacting a hydroxyacetophenone of general formula (2): ##STR2## with a tetrazole compound of general formula (3): ##STR3## in the presence of a base in a solvent composed mainly of at least one selected from hydrocarbons, halogenated hydrocarbons and alcohols, and then treating the reaction mixture under acidic conditions.
    Type: Grant
    Filed: February 23, 1996
    Date of Patent: January 28, 1997
    Assignee: Sumitomo Chemical Co., Ltd.
    Inventors: Hideki Ushio, Takayuki Higashii
  • Patent number: 5596103
    Abstract: This invention comprises a process for preparing benzopyran derivatives represented by formula (I) ##STR1## in which, R.sup.1 is C.sub.1-20 alkyl, C.sub.2-20 alkenyl, C.sub.2-20 alkynyl, or a group of structure (i), (ii) or (iii).
    Type: Grant
    Filed: May 26, 1995
    Date of Patent: January 21, 1997
    Assignee: SmithKline Beecham Plc
    Inventors: Graham Johnson, Neil Smith, Graham R. Geen, Inderjit S. Mann, Vance Novack
  • Patent number: 5594016
    Abstract: Naphthalene derivatives represented by the formula (I): ##STR1## wherein the symbol ##STR2## --X-- represents --O-- or --S--, .dbd.Y-- represents .dbd.N-- or .dbd.CR.sup.5 --, R.sup.1, C.sup.2, R.sup.3, R.sup.4 and R.sup.5 represent hydrogen, halogen, alkyl and the like,R.sup.6 represents hydrogen, alkyl, aryl and the like,n represents an integer of 0 to 3, --- represents a single bond or a double bond, which are useful for reducing blood sugar and blood lipid levels are provided.
    Type: Grant
    Filed: October 23, 1995
    Date of Patent: January 14, 1997
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Hiroaki Ueno, Takayuki Oe, Ichiro Suehiro, Fumiko Nakamura
  • Patent number: 5589501
    Abstract: A pharmaceutical compound of the formula ##STR1## in which m is 0, 1 or 2, n and q are each 0 or 1 to 5, and p is 0 or 1, X is --CO.sub.2 H or tetrazolyl,Y is --CH.dbd.CH--, andZ is(i) phenyl, naphthyl or thienyl, said phenyl, naphthyl and thienyl being optionally substituted,(ii) --CHR.sup.1 R.sup.2 where R.sup.1 and R.sup.2 are each phenyl, naphthyl or thienyl, said phenyl, naphthyl and thienyl being optionally substituted,(iii) .dbd.CR.sup.1 R.sup.2 where R.sup.1 and R.sup.2 are each phenyl, naphthyl or thienyl, said phenyl, naphthyl and thienyl being optionally substituted, or(iv) ##STR2## where r is 0 or 1 to 3 and the phenyl rings are optionally substituted; provided that when Z is phenyl and m is 1, p is 1; and salts and esters thereof.
    Type: Grant
    Filed: November 22, 1994
    Date of Patent: December 31, 1996
    Assignees: Eli Lilly and Company, Universite Louis Pasteur, Lilly, S.A.
    Inventors: Jesus E. Carrera, Almudena R. Esteban, Andr e Mann, Ang ele Schoenfelder, Darryle D. Schoepp, Concepcion P. Tercero, Camille-Georges Wermuth
  • Patent number: 5587483
    Abstract: A process for preparing substituted benzopyran derivatives which comprises a final step cyclisation of the corresponding open-chain intermediates.
    Type: Grant
    Filed: May 26, 1995
    Date of Patent: December 24, 1996
    Assignee: SmithKline Beecham PLC
    Inventors: Graham Johnson, Neil Smith, Graham R. Geen, Inderjit S. Mann, Vance Novack
  • Patent number: 5587390
    Abstract: Imidazole derivatives having A II antagonist activity, of Formula I, the processes for the preparation thereof, pharmaceutical compositions containing them and the use thereof as therapeutic agents. The described compounds having A II antagonist activity can be used in various cardiovascular disorders.
    Type: Grant
    Filed: March 17, 1995
    Date of Patent: December 24, 1996
    Assignee: Istituto Luso Farmaco D'Italia S.p.A.
    Inventors: Aldo Salimbeni, Fabio Paleari, Jacques Mizrahi, Carlo Scolastico
  • Patent number: 5578634
    Abstract: A class of novel 1H-indole-3-acetic acid hydrazides is disclosed together with the use of such indole compounds for inhibiting sPLA.sub.2 mediated release of fatty acids (e.g., arachidonic acid) for treatment of conditions such as septic shock.
    Type: Grant
    Filed: May 12, 1995
    Date of Patent: November 26, 1996
    Assignee: Eli Lilly and Company
    Inventors: Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim, Robert B. Hermann, Richard W. Schevitz
  • Patent number: 5578733
    Abstract: Disclosed is a method for removing a protective group of an N-protected tetrazolyl compound which comprises reacting said N-protected tetrazolyl compound with a mineral acid under substantially anhydrous conditions in the presence of an alcohol, insuring a high reaction yield of the object tetrazolyl compound.
    Type: Grant
    Filed: January 27, 1995
    Date of Patent: November 26, 1996
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Yasushi Shida, Kokichi Yoshida
  • Patent number: 5571813
    Abstract: Pharmaceutical compounds which are azolo-fused pyrimidine compounds having the formula ##STR1## in which .dbd.
    Type: Grant
    Filed: June 6, 1994
    Date of Patent: November 5, 1996
    Assignee: Beiersdorf-Lilly GmbH
    Inventors: Gerd R uhter, Theo Schotten, Wolfgang Stenzel, Michael Paal
  • Patent number: 5569768
    Abstract: This invention provides novel heterocyclic derivatives, their pharmaceutical formulations, and their use for antagonizing angiotensin II receptors in mammals.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: October 29, 1996
    Assignee: Eli Lilly and Company
    Inventors: Donald B. Boyd, Sherryl L. Lifer, Winston S. Marshall, Alan D. Palkowitz, William Pfeifer, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, K. Jeff Thrasher, Venkatraghavan Vasudevan, Celia A. Whitesitt
  • Patent number: 5567725
    Abstract: Cyclohexanol esters of the formula I ##STR1## are described in which the radicals have the given meaning. The compounds are pharmacologically active and may therefore be used as pharmaceuticals, in particular for treating diabetes and other diseases which are characterized by an elevated secretion of glucose from the liver or by an elevated activity of the glucose-6-phosphatase system.
    Type: Grant
    Filed: February 14, 1995
    Date of Patent: October 22, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Horst Hemmerle, Gerrit Schubert, Peter Below, Andreas Herling, Hans-J org Burger
  • Patent number: 5565485
    Abstract: Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, inflammatory diseases including Raynaud's disease and asthma.
    Type: Grant
    Filed: August 22, 1994
    Date of Patent: October 15, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Scott W. Bagley, Theodore P. Broten, Prasun K. Chakravarty, Daljit S. Dhanoa, Kenneth J. Fitch, William J. Greenlee, Nancy J. Kevin, Douglas J. Pettibone, Ralph A. Rivero, Thomas F. Walsh, David L. Williams, Jr., Richard B. Toupence, Jay M. Matthews
  • Patent number: 5563278
    Abstract: This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their use for antagonizing angiotensin II receptors in mammals.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: October 8, 1996
    Assignee: Eli Lilly and Company
    Inventors: Sherryl L. Lifer, Winston S. Marshall, Fariborz Mohamadi, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, Celia A. Whitesitt
  • Patent number: 5561113
    Abstract: A compound of formula (I): ##STR1## in which: R represents naphthyl, 5,6,7,8-tetrahydronaphthyl, 1,2,3,4-tetrahydronaphthyl, thienyl, optionally substituted phenyl or (C.sub.3 -C.sub.7)cycloalkyl,n represents an integer such that 1.ltoreq.n.ltoreq.8, their enantiomers, diastereoisomers and epimers as well as their addition salts with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as antagonists of substance P.
    Type: Grant
    Filed: April 26, 1995
    Date of Patent: October 1, 1996
    Assignee: Adir ET Compagnie
    Inventors: Jean-Luc Fauchere, Nathalie Kucharczyk-Gentric, Joseph Paladino, Jacqueline Bonnet, Emmanuel Canet, Graham Birrell
  • Patent number: 5559111
    Abstract: .delta.-Amino-.gamma.-hydroxy-.omega.-aryl-alkanoic acid amides of formula I ##STR1## and the salts thereof, have renin-inhibiting properties and can be used as antihypertensive medicinal active ingredients.
    Type: Grant
    Filed: April 4, 1995
    Date of Patent: September 24, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Richard G oschke, J urgen K. Maibaum, Walter Schilling, Stefan Stutz, Pascal Rigollier, Yasuchika Yamaguchi, Nissim C. Cohen, Peter Herold
  • Patent number: 5554633
    Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; X and Y are each H or together form a group=O; Z is O, S or NR.sup.9, where R.sup.9 is H or C.sub.1-6 alkyl; R.sup.1 represents H or C.sub.1-6 alkyl; R.sup.2 represents C.sub.1-6 alkyl substituted by CONR.sup.7 (CH.sub.2).sub.p R.sup.8 (where R.sup.7 is H or C.sub.1-6 alkyl, R.sup.8 is optionally substituted heteroaryl and p is 0, 1, 2, 3, 4, 5 or 6); R.sup.3 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkynyl; R.sup.4 represents H, C.sub.1-6 alkyl or optionally substitute phenyl; R.sup.5 represents optionally substituted phenyl; R.sup.6 is H or C.sub.1-6 alkyl; and q is 0, 1, 2 or 3; are tachykinin antagonists useful in therapy.
    Type: Grant
    Filed: January 27, 1995
    Date of Patent: September 10, 1996
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventor: Martin R. Teall
  • Patent number: 5554627
    Abstract: Compounds of formula (I), wherein Q.sup.1 represents an aryl group; the dotted line represents an optional covalent bond; one of X and Y represents H and the other represents hydroxy or C.sub.1-6 alkoxy, or X and Y together form a group .dbd.O or .dbd.NOR.sup.5 where R.sup.5 is H or C.sub.1-6 alkyl; Z represents O, S or NR.sup.2, where R.sup.2 is H or C.sub.1-6 alkyl; W represents a bond or a saturated or unsaturated hydrocarbon chain of 1, 2, 3, 4, 5 or 6 carbon atoms; R.sup.1 represents H or C.sub.1-6 alkyl. R.sup.3 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; R.sup.4 represents an optionally substituted phenyl group; and R.sup.6 represents a specified amino group or an optionally substituted aromatic or non-aromatic azacyclic or azabicyclic group; and salts and prodrugs are tachykinin receptor antagonists.
    Type: Grant
    Filed: April 27, 1995
    Date of Patent: September 10, 1996
    Assignee: Merck, Sharp & Dohme Ltd.
    Inventors: Richard T. Lewis, Angus M. MacLeod, Kevin J. Merchant
  • Patent number: 5545651
    Abstract: Novel substituted imidazoles of Formula (I), which are useful as angiotensin II antagonists, are disclosed: ##STR1##
    Type: Grant
    Filed: November 28, 1994
    Date of Patent: August 13, 1996
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: John J. V. Duncia, Carol L. Ensinger, Richard E. Olson, Mimi L. Quan, Joseph B. Santella, III, Mary K. Vanatten
  • Patent number: RE35321
    Abstract: A tetrazoleacetic acid derivative represented by the following general formula (I): ##STR1## .[.[in Formula (I),.]. .Iadd.wherein .Iaddend.R.sub.1 represents a hydrogen atom or an alkyl group; R.sub.2 represents a hydrogen atom, an alkyl group, an aralkyl group, a halogen atom, a haloalkyl group, a hydroxyl group, an alkoxy group, an alkoxyalkyl group, an amino group, an aryl group, an alkyl or aryl thio group, an alkyl or aryl carbonylamino group, an alkyl or aryl sulfonylamino group, an alkyl or aryl aminosulfonyl group, an alkyl or aryl sulfonyl group or an alkyl or aryl sulfinyl group; and X represents --O-- or --S--.[.].]. except for [5-(2-thienyl)tetrazol-1-yl] acetic acid, [5-(2-furyl)tetrazol-1-yl) acetic acid.Iadd., (5-(5-bromo-2-furyl)tetrazol-1-yl)acetic acid, (5-(5-phenylthio-2-furyl)tetrazol-1-yl)acetic acid, (5-(5-phenylsulfonyl-2-furyl)tetrazol-1-yl)acetic acid .Iaddend.
    Type: Grant
    Filed: September 25, 1992
    Date of Patent: August 27, 1996
    Assignee: Wakamoto Pharmaceutical Co., Ltd.
    Inventors: Sinji Inukai, Mitsuzi Agata, Manami Umezawa, Yoshihiro Horio, Yasuhiro Ootake, Shohei Sawaki, Masayoshi Goto