Polycyclo Ring System Patents (Class 562/427)
  • Patent number: 4970336
    Abstract: This invention relates to methods of preparing and purifying .alpha.-substituted acetic acids, which comprise treating an .alpha.aromatic-substituted acetic acid represented by a specific general formula with a weak alkali while shielding light, or subjecting an .alpha.-aromatic-substituted acetonitrile represented by a specific general formula to acid hydrolysis, followed by treatment with a weak alkali while shielding light; and treating the alkali salt of .alpha.-substituted acetic acid thus formed with a decolorizing agent.
    Type: Grant
    Filed: May 31, 1989
    Date of Patent: November 13, 1990
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Yoshikazu Yoshioka, Isao Hashiba, Suketoshi Tsukamoto
  • Patent number: 4965279
    Abstract: Novel cyclopropyl aza prostaglandin analogs are disclosed having the formula ##STR1## wherein A can be carbonyl, sulfonyl or a single bond. These compounds are useful, for example, as thromboxane antagonists.
    Type: Grant
    Filed: November 18, 1988
    Date of Patent: October 23, 1990
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Raj N. Misra, David M. Floyd, Steven E. Hall
  • Patent number: 4962224
    Abstract: Disclosed herein are N-naphthoylglycines and methods of their preparation. The N-naphthoylglycines are novel aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.
    Type: Grant
    Filed: August 22, 1989
    Date of Patent: October 9, 1990
    Assignee: American Home Products Corporation
    Inventors: Jay E. Wrobel, Kazimir Sestanj
  • Patent number: 4960792
    Abstract: 2-Acylaminoalkyl-3-[1-(carboxycycloalkylcarbamoyl)cycloalkyl]propanoic acid derivatives (which may also be viewed as glutaramide derivatives) are useful in the treatment of hypertension, heart failure and renal insufficiency, based upon their inhibition of zinc-dependant, neutral endopiptidase.
    Type: Grant
    Filed: May 8, 1989
    Date of Patent: October 2, 1990
    Assignee: Pfizer Inc.
    Inventors: John C. Danilewicz, Keith James
  • Patent number: 4959383
    Abstract: Phenylsulfone alkenoic acids and derivatives thereof are provided which have the structure ##STR1## wherein Ar represents an aryl group including phenyl or naphthyl which may or may not include one or more substituents, X is COOR wherein R is hydrogen, alkali metal or lower alkyl or X is 5-tetrazolyl or ##STR2## wherein R' is lower alkyl or aryl; n is 2, 3 or 4 and m is 2, 3 or 4. These compounds are cardiovascular agents which exhibit thromboxane antagonist activity and thus are useful in the treatment of thrombotic and vasospastic disease.
    Type: Grant
    Filed: October 31, 1988
    Date of Patent: September 25, 1990
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Steven E. Hall
  • Patent number: 4948810
    Abstract: Novel phenoxyacetic acid derivative of the formula: ##STR1## wherein R is a substituted or unsubstituted phenyl group, naphthyl group or a sulfur-containing 5-membered hetero-monocyclic group, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are hydrogen atom, a lower alkyl group, a phenyl-lower alkyl group or phenyl group, R.sup.5 is hydrogen atom or a lower alkyl group, R.sup.6 is carboxyl group, a protected carboxyl group, hydroxy group or a di(lower alkyl)-amino group, Ring A is a substituted or unsubstituted phenylene group, m is 0 or 1 and n is an integer 0 to 5, provided that, when m is 0,(1) at least either one of R.sup.1 to R.sup.4 is or/are a phenyl-lower alkyl group or phenyl group,(2) at least either one of R.sup.1 to R.sup.4 is or/are a lower alkyl group, and R.sup.6 is hydroxy group, or(3) all of R.sup.1 to R.sup.4 are hydrogen atom, and Ring A is a substituted phenylene group,or a pharmaceutically acceptable salt thereof are disclosed.
    Type: Grant
    Filed: February 6, 1989
    Date of Patent: August 14, 1990
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Takeo Iwakuma, Takayuki Kawaguchi, Toyoharu Yamashita, Yasuhiko Sasaki, Tamotu Shimazaki
  • Patent number: 4945106
    Abstract: Prostaglandin analogues exhibiting activity at thromboxane receptor sites have been prepared.
    Type: Grant
    Filed: July 6, 1989
    Date of Patent: July 31, 1990
    Assignee: National Research Development Corporation
    Inventors: Robert L. Jones, Norman H. Wilson
  • Patent number: 4933367
    Abstract: This invention relates to carboxylic acid derivatives and their use thereof. The compounds are useful in treatment of various diseases such as diabetes, prediabetic conditions, adipositas ailments or atherosclerosis.
    Type: Grant
    Filed: March 12, 1987
    Date of Patent: June 12, 1990
    Assignee: Boehringer Mannheim GmbH
    Inventors: Hans P. Wolff, Ernst-Christian Witte, Hans-Frieder Kuhnle
  • Patent number: 4929641
    Abstract: Novel mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating hypertension are disclosed.
    Type: Grant
    Filed: May 11, 1988
    Date of Patent: May 29, 1990
    Assignee: Schering Corporation
    Inventors: Martin F. Haslanger, Bernard R. Neustadt, Elizabeth M. Smith
  • Patent number: 4925595
    Abstract: Liquid detergent compositions which are stable on storage and contain fluorescent whitening agents from the class of the disulfonated distyrylbiphenyl and distyrylphenyl compounds; they do not produce bleach spots on direct contact with textile fabric. Some of the fluorescent whitening agents used are novel.
    Type: Grant
    Filed: June 27, 1988
    Date of Patent: May 15, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Heinz Hefti, Dieter Reinehr, Kurt Weber, Claude Eckhardt
  • Patent number: 4906766
    Abstract: Disclosed herein are N-[[6-methoxy-5-(trifluoromethyl)-1-naphthalenyl][substituted imino]methyl]-N-methylglycines and methods for their preparation. The N-methylglycines are new aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.
    Type: Grant
    Filed: March 20, 1989
    Date of Patent: March 6, 1990
    Assignee: American Home Products Corporation
    Inventors: Jay E. Wrobel, Kazimir Sestanj
  • Patent number: 4904819
    Abstract: Bicyclic sulfonamide derivatives represented by the formula: ##STR1## (wherein R.sub.1 is hydrogen or lower alkyl; R.sub.2 is lower alkyl, aralkyl, or aryl which may be substituted by lower alkyl, alkoxy, acetoxy, hydroxy, halogen, nitro or phenyl; and the wavy line indicates R or S configuration or their mixture) or their salt being used as antithrombotic, antivasoconstricting, and antibronchoconstricting drugs and the process therefor.
    Type: Grant
    Filed: April 28, 1988
    Date of Patent: February 27, 1990
    Assignee: Shionogi & Co., Ltd.
    Inventors: Sanji Hagishita, Kaoru Seno
  • Patent number: 4897397
    Abstract: Certain aryl-alkynoic, alkenoic and alkanoic acids and derivatives and their use in treating inflammation, allergy and hyperproliferative skin disease are disclosed.
    Type: Grant
    Filed: December 16, 1988
    Date of Patent: January 30, 1990
    Assignee: Schering Corporation
    Inventors: Neng Y. Shih, David J. Blythin
  • Patent number: 4894181
    Abstract: Carbocyclic compounds of the formula I ##STR1## wherein Q is a benzene or cyclohexane ring or a naphthalene system, X is in each case --CH.sub.2 --(CH.sub.2).sub.p -- where it is also possible for one or two non-adjacent CH.sub.2 groups to be replaced by --O--, --S--, --CO--, --O--CO--, --CO--O-- or --CH.dbd.CH--,p is 0, 1 or 2,A.sup.1 and A.sup.2 independently of one another are each a 1,4-phenylene group which is unsubstituted or monosubstituted or polysubstituted by halogen atoms and/or CH.sub.3 groups and/or CN groups and in which it would also be possible for one or more CH groups to be replaced by N atoms, a 1,4-cyclohexylene group wherein it would also be possible for one or two non-adjacent CH.sub.2 groups to be replaced by --O-- and/or --S--, a piperidine-1,4-diyl group or a 1,4-bicyclo[2.2.2]octylene group,Z is --CO--O--, --O--CO--, --O--, --CH.sub.2 --, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CHCN--CH.sub.2 --, --CH.sub.2 --CHCN--, --CH.dbd.CH--, --CH.dbd.N--, --N.dbd.CH--, --NO.
    Type: Grant
    Filed: May 16, 1988
    Date of Patent: January 16, 1990
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Klaus Praefcke, Bernd Kohne, Eike Poetsch
  • Patent number: 4889951
    Abstract: Perfluoroalkylaromatic compounds containing at least two carbons in the perfluoroalkyl group are prepared by reacting an aromatic bromide or iodide with a potassium perfluoroalkanoate corresponding to the formula KOOC(CF.sub.2).sub.n CF.sub.3 wherein n is an integer of at least one in the presence of cuprous iodide and a dipolar aprotic solvent.
    Type: Grant
    Filed: April 25, 1988
    Date of Patent: December 26, 1989
    Assignee: Ethyl Corporation
    Inventor: Robert I. Davidson
  • Patent number: 4885385
    Abstract: Water-soluble triphendioxazine compounds having fiber-reactive dye properties conforming to the general formula ##STR1## where: B is --O-- or --S-- or --NH-- or (C.sub.1 -C.sub.6)-alkylamino;R* is hydrogen or optionally substituted alkyl or aryl;W and W.sup.1 are each a bivalent, aliphatic or optionally alkyl-substituted cycloaliphatic or aliphatic-cycloaliphatic radical, which aliphatic radicals can be interrupted by --O--, --S--, sulfonyl, carbonyl, 1,4-piperidino, amino, alkylamino and/or alkanoylamino groups, orthe grouping --B--W.sup.1 --N(R*) and/or --N(R*)--W--B-- each represent the bivalent radical of a five- or six-membered saturated heterocycle which contains two nitrogen atoms, orthe grouping --B--W.sup.1 -- and/or --W--B-- each represent the bivalent radical of a five- or six=-membered saturated heterocycle which contains two nitrogen atoms and which is bonded by one of the two nitrogen atoms via an alkylene group of 2 to 4 carbon atoms to the grouping --N(R*)--CO--G.sup.
    Type: Grant
    Filed: July 28, 1988
    Date of Patent: December 5, 1989
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hartmut Springer, Walter Helmling, Gunther Schwaiger
  • Patent number: 4879309
    Abstract: Novel mercapto-acylamino acids useful as analgesic, as well as in the treatment of hypertension and congestive heart failure and combinations of mercapto acylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating hypertension and congestive heart failure are disclosed.
    Type: Grant
    Filed: January 30, 1989
    Date of Patent: November 7, 1989
    Assignee: Schering Corporation
    Inventors: Ronald J. Doll, Bernard R. Neustadt
  • Patent number: 4868331
    Abstract: Antithrombotic, antiatherosclerotic and antiischaemic compounds of the formula ##STR1## in which R.sup.1 is ##STR2## or SO.sub.2 R.sup.4, R.sup.3 is aryl, substituted aryl, heteroaryl, aralkyl or the group ##STR3## R.sup.4 is aryl or substituted aryl, R.sup.2 is OH, alkoxy, phenoxy, benzoxy or NR.sup.5 R.sup.6, andR.sup.5 and R.sup.6 each independently is hydrogen or alkyl, orone of the radicals R.sup.5 or R.sup.6 is benzyl,and physiologically acceptable salts thereof with mono- and divalent cations.
    Type: Grant
    Filed: June 29, 1987
    Date of Patent: September 19, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Niewohner, Franz-Peter Hoever, Bodo Junge, Elisabeth Perzborn, Friedel Seuter, Volker-Bernd Fiedler
  • Patent number: 4868332
    Abstract: An aminomethyl-5,6,7,8-tetrahydronaphthyl-oxyacetic acid derivative of the formula ##STR1## in which R.sup.3 is aryl or substituted aryl,R.sup.2 is hydroxyl, alkoxy, phenoxy, benzoxy or NR.sup.4 R.sup.5, andR.sup.4 and R.sup.5 each independently is hydrogen or alkyl, or one of the radicals R.sup.4 or R.sup.5 is benzyl,and physiologically acceptable salts thereof with monovalent or divalent cations which have antithrombotic, antiatherosclerotic and antiischaemic activities.
    Type: Grant
    Filed: November 23, 1987
    Date of Patent: September 19, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Niewohner, Franz-Peter Hoever, Folker Lieb, Ulrich Rosentreter, Elisabeth Perzborn, Volker-Bernd Fiedler, Friedel Seuter
  • Patent number: 4864058
    Abstract: A process for preparing optically active naphtho[1,2-b][1,4]thiazepin-4(5H)-ones comprising resolution of rac-.beta.-[(2-amino-1-naphthalenyl)thio]-.alpha.-hydroxy-4-methoxybenzene propanoic acid and converting the optically active acids so obtained into final products is described. The end product naphtho[1,2-b][1,4]thiazepin-4(5H)-ones have activity as calcium channel blockers and accordingly are useful as agents for lowering blood pressure, and as agents for treating ischemia.
    Type: Grant
    Filed: May 10, 1988
    Date of Patent: September 5, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Erno Mohacsi
  • Patent number: 4861913
    Abstract: Bicyclic sulfonamido derivatives represented by the formula: ##STR1## wherein R.sub.1 is a hydrogen or lower alkyl; R.sub.2 is an alkyl, substituted or unsubstituted aryl, aralkyl or heterocycle; R.sub.3 is a hydrogen or methyl; X is an alkylene or alkenylene which may be substituted by a fluorine atom or atoms an may contain an oxygen, sulfur and/or phenylene in the chain; Y is straight or branched alkylene or alkenylene, oxygen, or sulfur; m is 0 or 1; and n is 0, 1 or 2, or their salt, said derivatives being useful as antithrombotic, anti-vasoconstricting, and anti-bronchoconstricting drugs.
    Type: Grant
    Filed: November 5, 1986
    Date of Patent: August 29, 1989
    Assignee: Shionogi & Co., Ltd.
    Inventors: Masayuki Narisada, Mitsuaki Ohtani, Fumihiko Watanabe, Sanji Hagishita, Kaoru Seno, Susumu Kamata, Nobuhiro Haga, Tatsuo Tsuri, Tadahiko Tsushima, Kenji Kawada
  • Patent number: 4853412
    Abstract: Disclosed herein are N-[[6-methoxy-5-(trifluoromethyl)-1-naphthalenyl][substituted imino]methyl]-N-methylglycines and methods for their preparation. The N-methylglycines are new aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.
    Type: Grant
    Filed: December 23, 1987
    Date of Patent: August 1, 1989
    Assignee: American Home Products Corporation
    Inventors: Jay E. Wrobel, Kazimir Sestanj
  • Patent number: 4849563
    Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 s an alkyl of 1-6 carbon atoms, benzyl, phenyl, or phenyl substituted by halogen, alkoxy of 1 to 4 carbon atoms, alkyl of 1 to 4 carbon atoms, amino, or carbonyl substituents, or --RN(R').sub.2 wherein R and R' are each independently an alkyl of 1 to 4 carbon atoms; R.sub.2 is an aromatic substituent selected from the group consisting of phenyl, benzyl, and naphthyl, and A is an aromatic substitution selected from the group consisting of hydrogen, alkyl of 1-4 carbon atoms, alkoxy of 1-4 carbon atoms, halogen, --NO.sub.2, --NH.sub.2, --COOH, and --NHCOCH.sub.3. The compounds have been found to be alkylating agents having antineoplastic activity for use in inhibiting the growth of tumors.
    Type: Grant
    Filed: December 28, 1987
    Date of Patent: July 18, 1989
    Assignee: Yale University
    Inventors: Alan C. Sartorelli, Krishnamurthy Shyam, Robert T. Hrubiec
  • Patent number: 4843062
    Abstract: Disclosed herein are N-acyl-N-napthoylglycines and methods of their preparation. The N-acyl-N-napthoylglycines are novel aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.
    Type: Grant
    Filed: December 23, 1987
    Date of Patent: June 27, 1989
    Assignee: American Home Products Corporation
    Inventors: Kazimir Sestanj, Jay E. Wrobel, Joseph M. Kelly
  • Patent number: 4837234
    Abstract: Novel compounds have a formula (I) ##STR1## wherein ##STR2## represents a bicyclo [2,2,1] hept-2Z-ene, bicyclo [2,2,1] heptane, 7-oxa-bicyclo [2,2,1] hept-2Z-ene, 7-oxa-bicyclo [2,2,1] heptane, bicyclo [2,2,2] oct-2Z-ene or bicyclo [2,2,2] octane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group ANR.sup.2 R, a 6,6-dimethyl-bicyclo [3,1,1] heptane substituted at the 2-position by the group R.sup.1 and at the 3-position by the group ANR.sup.2 R or at the 2-position by the group ANR.sup.2 R and at the 3-position by the group R.sup.1, a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R.sup.1 and at the 5-position by the group ANR.sup.2 R or a 1-hydroxycyclopentane substituted at the 2-position by the group R.sup.1 and at the 2-position by the group ANR.sup.2 R, R.sup.
    Type: Grant
    Filed: July 22, 1986
    Date of Patent: June 6, 1989
    Assignee: National Research Development Corporation
    Inventors: Robert L. Jones, Norman H. Wilson
  • Patent number: 4801609
    Abstract: Novel mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic peptides useful for treating hypertension are disclosed.
    Type: Grant
    Filed: March 27, 1987
    Date of Patent: January 31, 1989
    Assignee: Schering Corporation
    Inventors: Martin F. Haslanger, Bernard R. Neustadt, Elizabeth M. Smith
  • Patent number: 4792550
    Abstract: A novel 13-aza-14-oxo-TXA.sub.2 analogue of general formula: ##STR1## wherein symbol A represents --CH.sub.2 CH.sub.2 --(CH.sub.2).sub.m --, cis--CH.dbd.CH--(CH.sub.2).sub.m --, --CH.sub.2 O--(CH.sub.2).sub.m --, --S--(CH.sub.2).sub.m -- ##STR2## R.sup.2 represents a bond or a straight or branched alkylene or alkenylene group of from 1 to 10 carbon atom(s) unsubstituted or substituted;R.sup.3 represents(i) a phenyl, phenoxy or phenylthio group unsubstituted or substituted,(ii) a straight or branched alkyl, alkenyl or alkynyl group of from 1 to 6 carbon atom(s) unsubstituted or substituted,(iii) a cycloalkyl, cycloalkyloxy or cycloalkylthio group of from 4 to 7 carbon atoms unsubstituted or substituted,(iv) a naphthyl, indolyl or indanyl group, or(v) an amino group unsubstituted or substitutedR.sup.4 represents a hydrogen atom or a methyl group.
    Type: Grant
    Filed: June 11, 1985
    Date of Patent: December 20, 1988
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Hajimu Miyake, Tadao Okegawa, Akiyoshi Kawasaki
  • Patent number: 4788319
    Abstract: A novel isocarbacyclin which is a compound represented by the following formula ##STR1## wherein R.sup.1 represents a hydrogen atom, or a C.sub.1 -C.sub.4 alkyl or alkenyl group; R.sup.2 and R.sup.3 are identical or different and each represents a hydrogen atom, a tri(C.sub.1 -C.sub.7)hydrocarbon-silyl group or a group forming an acetal linkage together with the oxygen atom of the hydroxyl group; R.sup.4 represents a hydrogen atom, a methyl group or a vinyl group; R.sup.5 represents an unsubstituted linear or branched C.sub.3 -C.sub.8 alkyl group which may be interrupted by an oxygen atom, a substituted linear or branched C.sub.1 -C.sub.5 group in which the substituent is a C.sub.1 -C.sub.6 alkoxy group or a phenyl, phenoxy or C.sub.3 -C.sub.10 cycloalkyl group which may be substituted further, a phenyl group which may be substituted, a phenoxy group which may be substituted, or a C.sub.3 -C.sub.
    Type: Grant
    Filed: May 1, 1987
    Date of Patent: November 29, 1988
    Assignee: Teijin Limited
    Inventors: Atsuo Hazato, Toshio Tanaka, Noriaki Okamura, Kiyoshi Bannai, Kurozumi, Seizi, Suzuki, Masaaki, Noyori, Ryoji
  • Patent number: 4783548
    Abstract: A process for preparing a 3,4-dihydro 2-naphthanoic acid or an ester thereof comprises heating an alpha-vinyl cinnamic acid or a (C.sub.1 -C.sub.12)alkyl, (C.sub.6 -C.sub.12)aryl, (C.sub.6 -C.sub.12)aralkyl or (C.sub.6 -C.sub.12)alkylaryl ester thereof at a temperature effective to cyclize said acid or ester thereof and obtain the corresponding 3,4-dihydro 2-naphthanoic acid or ester thereof. The alpha-vinyl cinnamic acid or ester thereof may be obtained by contacting crotonic anhydride and a benzaldehyde substituted with halo or (C.sub.1 -C.sub.12)alkyl, acyl, acyloxy, carboxy, carbalkoxy, alkylthiol or alkoxy.A process for preparing 2-naphthanoic acid or an ester thereof comprises the above steps to prepare a 3,4-dihydro-2-naphthanoic acid, and dehydrogenating said 3,4-dihydro 2-naphthanoic acid or ester thereof to obtain the 2-naphthanoic acid.
    Type: Grant
    Filed: September 16, 1987
    Date of Patent: November 8, 1988
    Assignee: Eastman Kodak Company
    Inventor: Joseph R. Zoeller
  • Patent number: 4780469
    Abstract: A (fused) benz(thio)amide of the formula: ##STR1## wherein B represents(i) a carbocyclic ring of from 4 to 8 members being unreplaced or replaced one, two or three of optional carbon atom(s) by oxygen, nitrogen and/or sulphur atom(s) or(ii) a divalent group of the formula: ##STR2## R.sup.1 represents a group of formula: ##STR3## (iv) a straight or branched alkyl, alkenyl, or alkynyl of from 1 to 20 carbon atoms,R.sup.4 represents(i) when B represents a closed ring, a group of the formula: ##STR4## (ii) when B does not represent a ring, a group of formula: ##STR5## with the proviso that compounds of formula: ##STR6## wherein A' is a vinylene or an ethylene group optionally substituted by straight or branched alkyl groups of from 1 to 4 carbon atom(s);R.sup.4' is--(CH.sub.2).sub.n --COOR.sup.8andR.sup.1' is(i) a group of the formula: ##STR7## or (ii) a group of the formula: ##STR8## are excluded, wherein A, R.sup.2, R.sup.3, R.sup.5, R.sup.6, R.sup.7, R.sup.8, U, n, m, p, q, R.sup.5', and R.sup.
    Type: Grant
    Filed: August 20, 1985
    Date of Patent: October 25, 1988
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Masaaki Toda, Tumoru Miyamoto, Yoshinobu Arai
  • Patent number: 4777289
    Abstract: A process for the preparation of alkylthioalkanoate salts by reaction of an alkali metal alkylmercaptide with a lactone in the presence of an aprotic polar organic solvent. Preferably, the alkali metal mercaptide is prepared by reaction of an alkylmercaptan and an alkali metal phenate.
    Type: Grant
    Filed: May 8, 1986
    Date of Patent: October 11, 1988
    Assignee: Monsanto Company
    Inventor: Dennis A. Ruest
  • Patent number: 4752616
    Abstract: Arylthioalkylphenylcarboxylic acids are provided which have the structure ##STR1## wherein Ar represents an aryl group including phenyl or naphthyl which may or may not include one or more substituents, A is ##STR2## R is hydrogen, alkali metal or lower alkyl, m is 0, 1, 2, or 3, n is 0, 1, or 2, p is 1 to 5, q, is 0, 1, 2, or 3, r is 0, 1, 2, or 3. These compounds are cardiovascular agents which exhibit thromboxane antagonist activity and thus are useful in the treatment of thrombotic disease.
    Type: Grant
    Filed: June 29, 1987
    Date of Patent: June 21, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Steven E. Hall, Philip D. Stein
  • Patent number: 4751240
    Abstract: A phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined phenolic nucleus including a phenyl-hydroxynaphthyl; hydroxyphenyl-naphthyl; phenyl-hydroxyindanyl, phenyl-hydroxybenzothienyl or mono-hydroxyphenyl-ethylene or vinylene nucleus; wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages, wherein R.sup.1 is hydrogen, or alkyl, alkenyl, alkynyl, cycloalkyl, halogenoalkyl, alkoxyalkyl, halogenoalkoxyalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 --or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --(PO)R.sup.2 13 , --S--, --SO--or --SO.sub.2 --, wherein R.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene; wherein R.sup.12 is hydrogen or alkyl, and wherein R.sup.22 is hydrogen, cyano or nitro; or a salt thereof when appropriate.
    Type: Grant
    Filed: April 24, 1985
    Date of Patent: June 14, 1988
    Assignee: Imperial Chemical Industries PLC
    Inventors: Jean Bowler, Graham C. Crawley, Philip N. Edwards, Alasdair T. Glen, Michael S. Large, Brian S. Tait
  • Patent number: 4746350
    Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein: Y is selected from phenyl, furyl, thienyl and pyrrolyl rings (each optionally substituted by group X), optionally branched alkylene or alkylenethio(oxy)alkylene;X which may be the same or different are independently selected from halogen, nitro, alkyl, substituted alkyl, hydroxy, alkoxy, carboxy, alkoxycarbonyl, alkylthio, sulfamoyl, substituted sulfamoyl, amino, substituted amino and alkanoyl;R.sup.1 is selected from hydrogen, acyl and an inorganic or organic cation;R.sup.2 is selected from alkyl, substituted alkyl, alkenyl, haloalkenyl and alkynyl;R.sup.3 is selected from alkyl; andR.sup.4 is selected from hydrogen, alkyl, and alkoxycarbonyl.
    Type: Grant
    Filed: April 14, 1986
    Date of Patent: May 24, 1988
    Assignee: Imperial Chemical Industries PLC
    Inventor: Keith G. Watson
  • Patent number: 4736055
    Abstract: Oxime sulfonates of formula I ##STR1## wherein Y is a polymerizable unsaturated group or epoxide group or an --OH, --NHR.sup.5, --COOH, COOR.sup.6, --COCl, --CH.sub.2 Hal, --SO.sub.2 Cl or --NCO group, Z is an (x+y)-valent connecting member, R.sup.1 and R.sup.2 are monovalent organic radicals, m is 0 or 1, x is 1 or 2 and y is 1 or 2, can be converted into polymers which can be thermally or photochemically dissociated to form free sulfonic acid groups. Said polymers can therefore be used as photoresists which can be developed with aqueous alkalis.
    Type: Grant
    Filed: April 11, 1986
    Date of Patent: April 5, 1988
    Assignee: Ciba-Geigy Corporation
    Inventors: Kurt Dietliker, Werner Rutsch, Godwin Berner, Max Hunziker, Christopher G. Demmer
  • Patent number: 4734435
    Abstract: Disclosed herein are N-[[6-methoxy-5-(trifluoromethyl)-1-naphthalenyl]-thioxomethyl]-N-methylgl ycine S-oxide (tolrestat S-oxide) and the amide thereof and methods of their preparation. The S-oxides are new aldose reductase inhibitors useful for the treatment of prevention of diabetic complications.
    Type: Grant
    Filed: November 25, 1986
    Date of Patent: March 29, 1988
    Assignee: American Home Products Corp.
    Inventors: Eckhardt S. Ferdinandi, Michael S. Malamas, Kazimir Sestanj, Surendra N. Sehgal
  • Patent number: 4723013
    Abstract: Certain 4,8-disubstituted-2,6-naphthalene dicarboxylic acid monomers and a method for their preparation. These monomers are useful for the preparation of polymers, which polymers may be used to prepare high strength fibers.
    Type: Grant
    Filed: April 7, 1987
    Date of Patent: February 2, 1988
    Assignee: The United States of America as represented by the Secretary of the Air Force
    Inventors: Tsu-Tzu Tsai, Fred E. Arnold
  • Patent number: 4705882
    Abstract: Herein disclosed are N-naphthoylglycine derivatives having aldose reductase inhibiting activity. The derivatives are useful for treating diabetic complications.
    Type: Grant
    Filed: March 28, 1986
    Date of Patent: November 10, 1987
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventors: Kazimir Sestanj, Nedumparambil A. Abraham, Francesco Bellini, Adi Treasurywala
  • Patent number: 4692512
    Abstract: alpha-L-Aspartyl-D-phenylglycine esters and amides are disclosed to be useful as high intensity sweeteners. These compounds can be used to sweeten a variety of foods, beverages and other oral products.
    Type: Grant
    Filed: December 20, 1985
    Date of Patent: September 8, 1987
    Assignee: The Procter & Gamble Company
    Inventor: John M. Janusz
  • Patent number: 4666941
    Abstract: New polysubstituted derivatives of naphtalene.These derivatives correspond to the following formula: ##STR1## in which: R.sub.1 to R.sub.4 is H or CH.sub.3R.sub.5 is ##STR2## or (iv) the radical: 2-oxazolinyl m is 0 or 1R.sub.8 is H, alkyl, OR.sub.11, R.sub.11 being H, alkyl or ##STR3## R.sub.13 being alkyl or aryl or R.sub.8 is ##STR4## when m=1, r' and r" representing H, alkyl mono or polyhydroxyalkyl, aryl or a heterocycle when they are taken together, R.sub.9 is H or alkyl, R.sub.10 is H, alkyl and the acetals of the said compounds, ##STR5## --OR.sub.14, R.sub.14 being H, alkyl, mono or polyhydroxyalkyl, aryl or aralkyl a rest of a sugar or represents ##STR6## P being 0, 1, 2, or 3 R.sub.6 represents a hydrogen atom or a lower alkyl radical,R.sub.7 represents H, alkyl, halogen, hydroxyl, sulfydryl, alkoxy, alkylthio, acyloxy, acylthio, acylamino or primary, secondary or tertiary amino and the salts of the said compounds.These compounds find an application in the cosmetic and pharmaceutical fields.
    Type: Grant
    Filed: November 28, 1984
    Date of Patent: May 19, 1987
    Assignee: Groupement Economique dit: Centre International de Recherces Dermatologiques C.I.R.D.
    Inventors: Braham Shroot, Jacques Eustache, Martine Bouclier
  • Patent number: 4661628
    Abstract: A new process for the optical resolution of racemic mixtures of .alpha.-naphthyl-propionic acids of formula ##STR1## This process comprises reacting a racemic mixture of a compound of formula ##STR2## with an optically active substance of formula R.sub.4 --NH.sub.2 (III), said substance being a .beta.-aminoalcohol, thus forming a pair of diastereoisomeric amides which are resolved into the single diastereoisomers by fractional crystallization. The obtained single diastereoisomeric amide is then hydrolyzed to give the desired optically active .alpha.-naphthyl-propionic acid of formula ##STR3## In the above compound I.fwdarw.III and VI, R.sub.1 is (C.sub.1-6)alkyl, R.sub.2 stands for hydrogen, halogen, mercapto, (C.sub.1-6)alkylthio, phenylthio, benzylthio, (C.sub.1-6)alkylsulfonyl, benzenesulfonyl, benzenesulfonyl substituted by halogen or (C.sub.1-4)alkyl, R.sub.3 is a reactive group and R.sub.4 is the residue of a primary or secondary alcohol.
    Type: Grant
    Filed: November 5, 1984
    Date of Patent: April 28, 1987
    Assignee: Alfa Chemicals Italiana S.p.A.
    Inventors: Vincenzo Cannata, Giancarlo Tamerlani
  • Patent number: 4647585
    Abstract: Bicycloheptane substituted ether prostaglandin analogs are provided having the structural formula ##STR1## wherein X is O or ##STR2## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
    Type: Grant
    Filed: November 8, 1984
    Date of Patent: March 3, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Melanie J. Loots, Steven E. Hall, Peter W. Sprague
  • Patent number: 4638078
    Abstract: The invention is a compound which comprises an amido alkenoic acid or a water-soluble salt thereof and and arylcyclobutene moiety, wherein the cyclobutene moiety is fused to the aryl radical, and wherein the amide nitrogen is connected to the aryl radical of the arylcyclobutenyl moiety by a direct bond or a bridging member.
    Type: Grant
    Filed: April 25, 1985
    Date of Patent: January 20, 1987
    Assignee: The Dow Chemical Company
    Inventor: Robert A. Kirchhoff
  • Patent number: 4628110
    Abstract: Novel compounds of the following general formula: ##STR1##
    Type: Grant
    Filed: October 30, 1984
    Date of Patent: December 9, 1986
    Assignee: The Upjohn Company
    Inventor: Paul A. Aristoff
  • Patent number: 4604406
    Abstract: Disclosed herein are new aldose reductase inhibitors of the formula ##STR1## wherein n is an integer from 1 to 5 and X is a chalcogen, and methods of preparation. The derivatives are useful for treating or preventing diabetic complications.
    Type: Grant
    Filed: November 16, 1984
    Date of Patent: August 5, 1986
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventors: Francesco Bellini, Kazimir Sestanj
  • Patent number: 4600724
    Abstract: Herein disclosed are N-naphthoylglycine derivatives having aldose reductase inhibiting activity. The derivatives are useful for treating diabetic complications.
    Type: Grant
    Filed: July 17, 1985
    Date of Patent: July 15, 1986
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventors: Kazimir Sestanj, Nedumparambil A. Abraham, Francesco Bellini, Adi Treasurywala
  • Patent number: 4596823
    Abstract: Novel compounds have a formula (I) ##STR1## wherein ##STR2## represents a bicyclo[2,2,1]hept-2Z-ene, bicyclo[2,2,1]heptane, 7-oxabicyclo[2,2,1]hept-2Z-ene, 7-oxabicyclo[2,2,1]heptane, bicyclo[2,2,2]oct-2Z-ene or bicyclo[2,2,2]octane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group C(R.sup.2).dbd.NR, a 6,6-dimethyl-bicyclo[3,1,1]heptane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group C(R.sup.2).dbd.NR or at the 5-position by the group C(R.sup.2).dbd.NR and at the 6-position by the group R.sup.1, a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R.sup.1 and at the 5-position by the group C(R.sup.2).dbd.NR, or a 1-hydroxycyclopentane substituted at the 2-position by the group R.sup.1 and at the 2-position by the group C(R.sup.2).dbd.NR, R.sup.1 is a 6-caboxyhex-2-enyl group or a modification thereof as defined herein, R.sup.
    Type: Grant
    Filed: February 12, 1982
    Date of Patent: June 24, 1986
    Assignee: National Research Development Corporation
    Inventors: Robert L. Jones, Norman H. Wilson
  • Patent number: 4588823
    Abstract: Novel compounds of the following general formula: ##STR1##
    Type: Grant
    Filed: September 27, 1984
    Date of Patent: May 13, 1986
    Assignee: The Upjohn Company
    Inventor: Paul A. Aristoff
  • Patent number: 4577025
    Abstract: A method for the preparation of an ester of .alpha.-thio-.alpha.-aromatic propionic acid derivatives of the formula: ##STR1## wherein R.sup.1 is alkyl, phenyl or benzothiazolyl, R.sup.2 is alkyl and Ar is an aromatic substituent.The method comprises reacting an ester of .alpha.-chloro-.alpha.-thiopropionic acid of the formula: ##STR2## with an aromatic compound of the formula ARH, in the presence of a Lewis acid. The method provides good reactivity and positional selectivity in the Friedel-Crafts reaction. Many esters of the formula (2) are useful as pharmaceuticals, agricultural chemicals, perfumes or their intermediates.
    Type: Grant
    Filed: August 26, 1983
    Date of Patent: March 18, 1986
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Kazutaka Arai, Yoshio Ohara, Yashio Takakuwa, Toyoko Iizumi
  • Patent number: 4568693
    Abstract: Herein disclosed are N-naphthoylglycine derivatives having aldose reductase inhibiting activity. The derivatives are useful for treating diabetic complications.
    Type: Grant
    Filed: September 9, 1983
    Date of Patent: February 4, 1986
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventors: Kazimir Sestanj, Nedumparambil A. Abraham, Francesco Bellini, Adi Treasurywala