Double Bonded Divalent Sulfur Patents (Class 544/160)
  • Patent number: 6211176
    Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: July 1, 1999
    Date of Patent: April 3, 2001
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Patent number: 6147117
    Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: July 13, 1999
    Date of Patent: November 14, 2000
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 6143747
    Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: ##STR1## or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.
    Type: Grant
    Filed: February 26, 1998
    Date of Patent: November 7, 2000
    Assignee: G. D. Searle & Co.
    Inventors: John N. Freskos, Daniel P. Getman, John J. Talley, James A. Sikorski
  • Patent number: 6107337
    Abstract: A compound of the formula ##STR1## wherein n, X, R.sup.3, R.sup.4 and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, restenosis, periodontal disease, epidermolysis bullosa, scleritis, bone resorption, loosening of artificial joint implants, atherosclerosis, multiple sclerosis, occular angiogenisis and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF.
    Type: Grant
    Filed: August 6, 1998
    Date of Patent: August 22, 2000
    Assignee: Pfizer Inc.
    Inventor: Ralph P. Robinson
  • Patent number: 6057322
    Abstract: Compounds of the formula I ##STR1## and the pharmaceutically tolerated salts thereof, are described. A process for their preparation and their use as medicaments in cardiovascular diseases are also described.
    Type: Grant
    Filed: July 30, 1997
    Date of Patent: May 2, 2000
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
  • Patent number: 6057337
    Abstract: A 1,2-di-substituted piperidine derivative or a salt thereof expressed by the following Formula (I): ##STR1## wherein one of A and B is a hydrocarbon group of C.sub.1-30 expressed by R.sup.1 and the other is --(CH.sub.2)n-NR.sup.2 R.sup.3 ; Y is --CO--, --CONR.sup.5 -- or --COO--; Z is --O--, --OCO--, --OCONR.sup.6 -- or --NR.sup.6 --; R.sup.2 and R.sup.3 individually represent a hydrogen a lower alkyl, a phenyl or a benzyl group, or together represent a heterocycle having 3-7 members; --NR.sup.5 --(CH.sub.2)n-NR.sup.2 R.sup.3 and --NR.sup.6 --(CH.sub.2)n-NR.sup.2 R.sup.3 of --(Y).sub.1 --A and --Z--B may be the following Group W: ##STR2## wherein ring E is a heterocycle of 6 or 7 members including two nitrogen atoms and R.sup.2 is a hydrogen, a lower alkyl, a phenyl or a benzyl group; R.sup.
    Type: Grant
    Filed: January 29, 1999
    Date of Patent: May 2, 2000
    Assignee: Shiseido Co., Ltd.
    Inventors: Koji Kobayashi, Hirotada Fukunishi, Kenichi Umishio, Akihiro Ishino
  • Patent number: 6037472
    Abstract: Compounds of formula (I) ##STR1## and their pharmaceutically acceptable salts inhibit matrix metalloproteases, such as stromelysin, gelatinase, matrilysin and collagenase, and are useful in the treatment of mammals having disease-states alleviated by the inhibition of such matrix metalloproteases.
    Type: Grant
    Filed: November 22, 1994
    Date of Patent: March 14, 2000
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Arlindo Lucas Castelhano, Steven Lee Bender, Judith Gail Deal, Stephen Horne, Teng J. Liak, Zhengyu Yuan
  • Patent number: 6022873
    Abstract: Compounds of formula (I) ##STR1## wherein n, V, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the specification are matrix metalloproteinase inhibitors.
    Type: Grant
    Filed: July 23, 1998
    Date of Patent: February 8, 2000
    Assignee: British Biotech Pharmaceuticals Limited
    Inventors: Raymond Paul Beckett, Fionna Mitchell Martin, Andrew Miller, Richard Simon Todd, Mark Whittaker
  • Patent number: 6013649
    Abstract: This invention is directed to proteinase (protease) inhibitors, and more particularly to thiol sulfone inhibitors for matrix metalloproteinase 13(MMP-13), compositions of proteinase inhibitors, intermediates for the syntheses of proteinase inhibitors, processes for the preparation of proteinase inhibitors and processes for treating pathological conditions associated with pathological matrix metalloproteinase activity related to MMP-13.
    Type: Grant
    Filed: July 22, 1997
    Date of Patent: January 11, 2000
    Assignee: Monsanto Company
    Inventors: John N. Freskos, S. Zaheer Abbas, Gary A. DeCrescenzo, Daniel P. Getman, Robert M. Heintz, Brent V. Mischke, Joseph J. McDonald
  • Patent number: 5965588
    Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: March 26, 1998
    Date of Patent: October 12, 1999
    Assignee: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5935997
    Abstract: The present invention relates to O-thiocarbamoyl-aminoalkanol compound represented by the following structural formula (VI), (VIII) and (IX) which are a racemic or enantiomerically enriched and pharmaceulically acceptable salts thereof to treat diseases of the central nervous system: ##STR1## wherein Ar is a phenyl group as described as follows: ##STR2## wherein R is a member selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, halogen selected from F, Cl, Br, and I, alkoxy containing 1 to 3 carbon atoms, thioalkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, or taifluorocarbon, and x is an integer from 1 to 3, with the proviso that R is the same or different when x is 2 or 3. R.sub.1 and R.sub.2 may be the same or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, aryl, 3 to 7-membered aliphatic cyclic compounds and R.sub.1 and R.sub.
    Type: Grant
    Filed: January 13, 1998
    Date of Patent: August 10, 1999
    Assignee: Yukong Limited
    Inventors: Yong Moon Choi, Yong Kil Kim
  • Patent number: 5852006
    Abstract: Disclosed are new alkylenediamine derivatives of the following formula which are effective for treatment of dysuria are disclosed: ##STR1## wherein R.sup.1 is hydrogen, alkyl, or a substituted or unsubstituted phenyl, naphthyl or aromatic heterocyclic group; R.sup.2 is a substituted or unsubstituted phenyl, naphthyl or aromatic heterocyclic group; R.sup.3 and R.sup.4 represent hydrogen, alkyl, aralkyl or aryl; or R.sup.3 and R.sup.4 are combined to form one of substituted or unsubstituted 5- to 7-membered heterocyclic groups; X is oxygen, sulfur or imino; Y is oxygen or sulfur; Z is --CH.sub.2 --, --CO-- or --CS--; m is an integer of 0-4; n is an integer of 0-4; r is 0 or 1; and p and q represent an integer of 0-5 provided that p plus q is 1-5.
    Type: Grant
    Filed: October 4, 1996
    Date of Patent: December 22, 1998
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Mitsuo Masaki, Norihisa Miyake, Atsushi Tendo, Hiromitsu Takeda, Michiko Ishida, Haruhiko Shinozaki
  • Patent number: 5814634
    Abstract: The invention provides a compound which has anti-ulcer effect and antibacterial activity against Helicobacter pyroli. This compound is an alkylenediamine derivative or salt which has a general formula of (1): ##STR1## wherein each of R.sub.4, R.sub.5, and R.sub.6 is hydrogen or lower alkyl; n represents an integer of 1 to 6; Y is --CH.sub.2 --, --O--, or --N(R.sub.7)--, wherein R.sub.7 is lower alkyl, aryl, carbamoyl lower alkyl, aralkyl, or a heterocyclic group having 5 to 9 carbon numbers; and, W is a group expressed by formulas 2 or 3: ##STR2## wherein (1) in formula 2: each of R.sub.1 and R.sub.2 is hydrogen, lower alkoxy, alkenyloxy, or a halogen atom; each of R.sub.3 and R.sub.3 is methyl, prenyl, or geranyl; when one of R.sub.3 and R.sub.3 is prenyl or geranyl, the other must be a methyl group; and X is oxygen or sulfur; and (2) in formula 3, R.sub.10 is a lower alkyl, and R.sub.11 is a halogen atom.
    Type: Grant
    Filed: April 17, 1997
    Date of Patent: September 29, 1998
    Assignee: Shiseido Co. Ltd.
    Inventors: Chikao Nishino, Fumitaka Sato, Tomohiro Uetake, Hirotada Fukunishi, Nao Kojima
  • Patent number: 5763604
    Abstract: Sulfonamidocarboxamides of the formula ##STR1## wherein A, M, Q, X and Y have the significance given in the description, as well as hydrates, solvates and salts thereof, which inhibit thrombin-induced blood platelet aggregation and clotting of fibrinogen in plasma, as described. The compounds of formula I can be prepared by amidination of a cyclic amino group standing for grouping X or by C(O)N(Q) amide formation.
    Type: Grant
    Filed: June 4, 1997
    Date of Patent: June 9, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, David Banner, Klaus Gubernator, Kurt Hilpert, Gerard Schmid
  • Patent number: 5760064
    Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: June 6, 1997
    Date of Patent: June 2, 1998
    Assignee: G.D. Searle
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5756498
    Abstract: Sulfonylalkanoylamino hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.In accordance with the present invention, compounds of Formula (I) are disclosed ##STR1## wherein the substituents are as defined in the specification.
    Type: Grant
    Filed: January 11, 1996
    Date of Patent: May 26, 1998
    Assignee: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Patent number: 5639769
    Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: January 17, 1996
    Date of Patent: June 17, 1997
    Assignee: G.D. Searle and Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5614536
    Abstract: Substituted N-aminoalkylmethane sulfanilide of formula (I), their solutions and pharmaceutically acceptable addition salts, their pharmaceutical compositions and their therapeutic use. In formula (I) Y represents hydrogen, cyano, nitro, amino, acetamide or halogen; n is an integer between 2 and 4, R.sup.1 and R.sup.2 equal or different are alkyl-(C1-C4) or they are connected together and with the N-atom thereby forming a 1-pyrrolidinyl, 1-piperidinyl, 1-piperazinyl, 4-methyl-1-piperazinyl, 4-ethylpiperazinyl, 4-propylpiperazinyl, 1-homopiperidinyl or 4-morpholine residue. The products of formula (I) are used as antispasmodic agents.
    Type: Grant
    Filed: January 7, 1994
    Date of Patent: March 25, 1997
    Assignee: Roemmers S.A.I.C.F.
    Inventors: Carlos E. A. Monti, Gustavo E. Aldom a
  • Patent number: 5602119
    Abstract: Succinoylamino hydroxyethylamino sulfamic acid derivative compounds which are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: January 31, 1995
    Date of Patent: February 11, 1997
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Patent number: 5583132
    Abstract: Sulfonylalkanoylamino hydroxyethylamino sulfamic acid compounds which are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: February 2, 1995
    Date of Patent: December 10, 1996
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Patent number: 5578594
    Abstract: Sulfonamidocarboxamides of the formula ##STR1## wherein A, M, Q, X and Y have the significance given in the description, as well as hydrates, solvates and salts thereof, which inhibit thrombin-induced blood platelet aggregation and clotting of fibrinogen in plasma, as described. The compounds of formula I can be prepared by amidination of a cyclic amino group standing for grouping X or by C(O)N(Q) amide formation.
    Type: Grant
    Filed: December 21, 1994
    Date of Patent: November 26, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, David Banner, Klaus Gubernator, Kurt Hilpert, G erard Schmid
  • Patent number: 5559153
    Abstract: Urea-substituted benzoylguanidines, process for their preparation, their use as pharmaceutical or diagnostic, and pharmaceutical containing themThere are described benzoylguanidines of the formula I ##STR1## where R(1), R(3) or R(4) is --NR(6) C.dbd.X NR(7)R(8); X is oxygen, sulfur, R(6), R(7) and R(8) are H, (perfluoro)alk(en)yl, where R(7) and R(8) can also together be 4 or 5 methylene groups,the substituents R(1) to R(5) remaining in each case are H, Hal, (fluoro) alk(en)yl, CN, NO.sub.2, NR(16)R(17).
    Type: Grant
    Filed: August 11, 1994
    Date of Patent: September 24, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Jan-Robert Schwark, Hans-Jochen Lang, Heinz-Werner Kleemann, Andreas Weichert, Wolfgang Scholz, Udo Albus
  • Patent number: 5530128
    Abstract: Compounds of formula (1) are described wherein R represents a --CONHOH, carboxyl, carboxyl ester, or --P(O)(X.sup.1 R.sup.8)X.sup.2 R.sup.9, where X.sup.1 and X.sup.2 are the same or different and each is oxygen or sulphur, R.sup.8 and R.sup.9 are the same or different and each represents hydrogen or an optionally substituted alkyl, aryl or aralkylthioalkyl group; R.sup.2 represents an optionally substituted alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aralkoxy, or aralkylthio group, or an amino, substituted amino, carboxyl, or carboxyl ester group; R.sup.3 represents hydrogen or alkyl; R.sup.4 represents hydrogen or alkyl; R.sup.5 represents an optionally substituted alkyl or alkenyl group optionally interrupted by one or more --O-- or --S-- atoms or --N(R.sup.7)-- groups, where R.sup.7 is a hydrogen atom or a C.sub.1-6 alkyl group, or --(Alk).sub.n R.sup.6 where Alk is an alkyl or alkenyl group optionally interrupted by one or more --O-- or --S-- atoms or --N(R.sup.
    Type: Grant
    Filed: February 2, 1994
    Date of Patent: June 25, 1996
    Assignee: Celltech Therapeutics Limited
    Inventors: John R. Porter, John R. Morphy, Thomas A. Millican, Nigel R. A. Beeley
  • Patent number: 5521219
    Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: August 24, 1993
    Date of Patent: May 28, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5510388
    Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: April 23, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5508294
    Abstract: Sulfonamide-containing hydroxethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: April 16, 1996
    Assignee: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5481005
    Abstract: The invention relates to N-sulfonyl derivatives of formulae (I) and (I)' ##STR1## to their preparation, and to pharmaceutical compositions in which they are present. The compounds of formulae (I) and (I)' have an affinity for the vasopressin and ocytocin receptors.
    Type: Grant
    Filed: November 28, 1994
    Date of Patent: January 2, 1996
    Assignee: Sanofi
    Inventors: Jean Wagnon, Paul de Cointet, Dino Nisato, Claude Plouzane, Claudine Serradeil-Legal, Bernard Tonnerre
  • Patent number: 5476850
    Abstract: There are described amino-substituted benzenesulfonylureas and -thioureas of the formula I ##STR1## The compounds I are used for the treatment of cardiac arrhythmias and for the prevention of sudden heart death caused by arrhythmias and can therefore be used as antiarrhythmics. They are particularly suitable for those cases in which arrhythmias are a result of constriction of a coronary vessel, such as in angina pectoris or in acute cardiac infarct.
    Type: Grant
    Filed: December 5, 1994
    Date of Patent: December 19, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinrich Englert, Dieter Mania, Jens Hartung, Heinz Gogelein, Joachim Kaiser
  • Patent number: 5473066
    Abstract: Process for stereoselectivity preparing a cis-form of 5-(aminoalkylamino)-1,5-benzothiazepine derivative represented by formula (VI): ##STR1## is provided, said process comprising carrying out a stereoselective addition reaction of an o-(aminoalkylamino) thiophenyl derivative with a trans-substituted glycidic ester at an elevated temperature in a nonpolar solvent in the presence of a divalent or trivalent iron ion to prepare a threo-form intermediate, hydrolyzing the ester group of said intermediate, acetylating the hydroxyl group of said hydrolyzed compound, and subjecting said acetylated compound to a ring closure reaction to obtain the objective compound (VI).
    Type: Grant
    Filed: January 19, 1994
    Date of Patent: December 5, 1995
    Assignee: Shionogi & Co., Ltd.
    Inventors: Teruo Yamamori, Hiroshi Harada, Eiichi Oosugi, Katsunori Sakai
  • Patent number: 5424309
    Abstract: The present invention provides an N-substituted acylamino acid compound of the formula: ##STR1## a process for their production and pharmaceutical uses, and intermediates useful for their production.
    Type: Grant
    Filed: February 22, 1994
    Date of Patent: June 13, 1995
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Hajime Morishima, Yutaka Kokie, Masato Nakano, Shugo Atsuumi, Seiichi Tanaka, Kenji Matsuyama
  • Patent number: 5294708
    Abstract: This invention relates to new heterocyclic derivatives of guanidine and more particularly to such derivatives which have hypoglycemic activity, their methods of use for treating hyperglycemia and novel intermediate compounds for their preparation.
    Type: Grant
    Filed: July 20, 1993
    Date of Patent: March 15, 1994
    Assignee: McNeilab, Inc.
    Inventors: Henry J. Breslin, Michael J. Kukla, Chris R. Rasmussen, Robert W. Tuman
  • Patent number: 5256657
    Abstract: Compounds having the structural formula ##STR1## wherein X is HONH or HO and especially wherein the carbon atom bearing CH.sub.2 R.sup.1 has the R-configuration, the carbon atom bearing CH.sub.2 R.sup.2 has the S-configuration, R.sup.1 is isopropyl, R.sup.2 is 3-indolyl, m is 2, n is 0, p is 2 and R.sup.3 and R.sup.4 taken alone are each methyl or R.sup.3 and R.sup.4 taken together with N are morpholino and pharmaceutically acceptable acid addition salts or solvates or acid addition salts-solvates thereof, which are matrix-metalloprotease inhibitors useful in treatment of disease in which matrix-metalloprotease promoted connective tissue remodelling is a causative factor, for example, rheumatoid arthritis and cancer, and a method of preparation and method of use thereof and methods of preparation of intermediates therefor are disclosed.
    Type: Grant
    Filed: August 19, 1991
    Date of Patent: October 26, 1993
    Assignee: Sterling Winthrop, Inc.
    Inventors: Jasbir Singh, Barry A. Morgan, James A. Gainor, Thomas D. Gordon, Robert C. Wahl
  • Patent number: 5220022
    Abstract: Disclosed are novel compounds of the formula ##STR1## wherein: R is ##STR2## where Ph is phenyl, or ##STR3## X is --NR.sub.5 R.sub.6 or --OR.sub.7 ; R.sub.1 and R.sub.2 are independently hydrogen, methyl, ethyl, cyclohexyl, ##STR4## butyl, or heptyl; R.sub.4 is o-phenylene or p-phenylene and R.sub.4 can be alkyl- halo- or alkoxy- substituted;R.sub.3 is hydrogen;R.sub.5, R.sub.6, and R.sub.7 are independently hydrogen, methyl, ethyl, tert-butyl, isobutyl, butyl, alkoxy, acyl, acylamino, aryl, amino, cyclohexyl, aminoalkyl and substituted or unsubstituted phenylamino;Y is sulfur and oxygen atom; and n is zero or 1; provided n=1 when Y is sulfur.
    Type: Grant
    Filed: January 28, 1991
    Date of Patent: June 15, 1993
    Assignee: International Paper Co.
    Inventors: Bruce M. Resnick, Allan J. Wexler
  • Patent number: 5185334
    Abstract: Novel 2,2-disubstituted glycerol-like compounds are disclosed for use as anti-allergic and anti-inflammatory compounds. The compounds are antagonists of platelet activating factor ("PAF"). Also disclosed are methods of synthesizing and using the compounds of the invention as well as pharmaceutical compositions thereof. The compounds have the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are as defined in the specification.
    Type: Grant
    Filed: September 6, 1991
    Date of Patent: February 9, 1993
    Assignee: Schering Corporation
    Inventors: Daniel Solomon, James J. Kaminski, Steven K. White, Laura S. Lehman de Gaeta, Ashit K. Ganguly
  • Patent number: 5147857
    Abstract: New glycolic acid derivatives of the formula IX--O--CR.sup.1 R.sup.2 --CO--Y--NR.sup.3 --CHR.sup.4 --CR.sup.5 --CH.sub.2 --CR.sup.6 R.sup.7 --Z Iin which R.sup.1 to R.sup.7, X, Y and Z have the meanings indicated herein, and salts thereof, inhibit the activity of human plasma renin.
    Type: Grant
    Filed: March 18, 1991
    Date of Patent: September 15, 1992
    Assignee: Merck Patent Gesellschaft mit beschraenkter Haftung
    Inventors: Peter Raddatz, Claus J. Schmitges, Klaus-Otto Minck
  • Patent number: 5116861
    Abstract: Novel nitrosothiol derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.3 is a hydrogen atom, an acyl group or a hydrocarbon residue which may be substituted; X.sup.1 is a hydrogen atom, an acyl group, a lower alkoxy group or a hydrocarbon residue which may be substituted; X.sup.2 is an acyl group or a carboxyl group which may be esterified or which may form an amide; with proviso that when X.sup.2 is a carboxyl group X.sup.1 is not a hydrogen atom or acetyl group and that when both R.sup.1 and R.sup.2 are hydrogen atoms X.sup.1 is not acetyl group or .gamma.-glutamyl group, and salts thereof, show excellent hypotensive action, antiarrhythmic action, anti-anginal action, cardiotonic action or coronary vasodilation, thus being useful as therapeutic or prophylactic agents for the cardiovascular diseases such as hypertension and angina pectoris.
    Type: Grant
    Filed: August 3, 1990
    Date of Patent: May 26, 1992
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Giichi Goto, Shigenori Ohkawa, Shoji Fukumoto
  • Patent number: 5114937
    Abstract: The invention concerns novel renin-inhibitory compounds which are useful for treating renin-associated hypertension, congestive heart failure, hyperaldosteronism, glaucoma, and diseases caused by retroviruses including HTLV-I, -II, and -III. Processes for preparing the compounds, novel intermediates useful in the preparation thereof, compositions containing them, and methods of using them are included. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertension, congestive heart failure, or hyperaldosteronism.
    Type: Grant
    Filed: November 28, 1989
    Date of Patent: May 19, 1992
    Assignee: Warner-Lambert Company
    Inventors: James M. Hamby, James S. Kaltenbronn, Joseph T. Repine
  • Patent number: 5096918
    Abstract: The invention concerns pharmaceutially useful heterocyclic nitromethane compounds of the formula I: ##STR1## in which ring Q is a heterocycle of 4 to 7 ring atoms, the fragment completing the ring Q having 2 to 5 atoms, one of which is carbon, oxygen, sulphur or a group of the formula --NRa--, and the remainder are carbon; Ra is hydrogen, (1-6C)alkyl, (2-6C)alkanoyl, trifluoroacetyl, phenyl, benzoyl, or phenyl(1-4C)alkyl, the latter three optionally substituted; and R.sup.1 R.sup.2 and R.sup.3 are independently hydrogen, hydroxy, (1-6C)alkyl, (1-6C)alkoxy, phenyl, phenoxy or phenyl(1-4C)alkyl, the last three optionally substituted, or two of R.sup.1, R.sup.2 and R.sup.3 situated on adjacent ring carbon atoms and together with said carbon atoms form a benzene ring fused to ring Q, the benzene ring itself optionally substituted, provided that when the fragment completion ring Q is of 3 atoms then at least one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen; and salts thereof.
    Type: Grant
    Filed: February 5, 1990
    Date of Patent: March 17, 1992
    Assignee: Imperial Chemical Industries PLC
    Inventor: Keith B. Mallion
  • Patent number: 5086054
    Abstract: Novel arylcycloalkanepolyalkylamines useful as anti-psychotic, anti-ischemia, anti-stroke, anti-dementia and anti-convulsant agents. These arylcycloalkanepolyalkylamines are selective high-affinity ligands to the sigma binding-sites containing three basic units: arylcycloalkyl group, an amine group and an intermediate chain. Their preparation and use for treatment of psychoses, ischemia, stroke, dementia and convulsions are also disclosed.
    Type: Grant
    Filed: July 31, 1990
    Date of Patent: February 4, 1992
    Assignee: SRI International
    Inventor: Daniel W. Parish
  • Patent number: 5053504
    Abstract: A process is disclosed for providing benzazepine intermediates of the formulae ##STR1## wherein R.sub.3, R.sub.4 and Y are as defined herein, which intermediates are useful in a process for the preparation of pharmaceutically useful benzazepine derivatives.
    Type: Grant
    Filed: November 29, 1989
    Date of Patent: October 1, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Wen-Sen Li, John K. Thottathil, Michael Murphy
  • Patent number: 5025005
    Abstract: Novel lipid derivatives of the formula ##STR1## [wherein R.sup.1 is alkyl or alkylcarbamoyl; R.sup.2 is hydrogen, hydroxy which may be substituted, amino which may be substituted or cyclic amino; R.sup.3 is a chemical binding or alkylene which may be substituted; R.sup.4 is hydrogen, alkyl or aralkyl; X and Y are independently O, S or an imino group which may be substituted, and when Y is an imino group, Y, together with the imino group represented by X or R.sup.4, may form a ring; and Z is imino or a nitrogen-containing heterocyclic ring which may be substituted] and salts thereof have inhibiting activity on platelet activating factor and are useful as a preventive or therapeutic agent for a variety of circulatory diseases and allergic disorders and also as an antineoplastic agent.
    Type: Grant
    Filed: July 23, 1990
    Date of Patent: June 18, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hiroaki Nomura, Kohei Nishikawa, Susumu Tsushima
  • Patent number: 5001148
    Abstract: Antihypercholesterolemic activity, due to competitive inhibition of HMG CoA reductase, has been found in compounds of the formula ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 are independently selected from:(1) alkyl,(2) substituted alkyl in which one or more substituents are selected from(a) halogen,(b) hydroxyl,(c) alkoxy,(d) alkoxycarbonyl,(e) acyloxy,(f) cycloalkyl,(g) phenyl,(h) substituted phenyl in which one or more substituents are X or Y,(i) alkyl-S(O).sub.n,(j) cycloalkyl-S(O).sub.n,(k) phenyl-S(O).sub.n,(l) substituted phenyl-S(O).sub.n in which one or more substituents are X or Y, and(m) oxo,(3) alkoxy,(4) alkenyl,(5) cycloalkyl,(6) substituted cycloalkyl in which one or more substituents are selected from(a) alkyl,(b) substituted alkyl in which one or more substituents are selected from(i) halogen,(ii) hydroxy,(iii) alkoxy,(iv) alkoxycarbonyl(v) acyloxy(vi) phenyl(vii) substituted phenyl in which one or more substituents are X and Y,(viii) alkyl-S(O).sub.n,(ix) cycloalkyl-S(O).sub.
    Type: Grant
    Filed: June 7, 1989
    Date of Patent: March 19, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jeffrey O. Saunders, Eric M. Gordon
  • Patent number: 5001156
    Abstract: Lipophilic quaternary ammonium salicylate, characterized in that it corresponds to the formula: ##STR1## in which: (i) R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be identical or different, denote an alkyl or alkylcycloalkyl radical, optionally substituted or interrupted;(ii) R.sub.3 and/or R.sub.4 denote(s) a group:R.sub.8 [OC.sub.2 H.sub.3 R.sub.7 ].sub.n [OCH.sub.2 CHOH--CH.sub.2 ].sub.pin which 0.ltoreq.n.ltoreq.4 and p denotes 0 or 1; R.sub.8 denotes H or an alkyl, alkenyl, alkylcycloalkyl or alkylaryl radical;(iii) R.sub.4 denotes an alkylphenyl radical;(iv), (v) R.sub.1 and R.sub.2 can form a saturated or unsaturated aromatic or non-aromatic heterocycle;(vi) R.sub.1, R.sub.2 and R.sub.3 form polycyclic derivatives with the nitrogen atoms; R.sub.5 denotes a group corresponding to the formula: ##STR2## in which n is an integer varying between 0 and 10.
    Type: Grant
    Filed: December 1, 1987
    Date of Patent: March 19, 1991
    Assignee: L'Oreal
    Inventors: Michel Philippe, Henri Sebag, Michel Hocquaux, Bernard Jacquet, Jean P. Laugier
  • Patent number: 4997980
    Abstract: Disclosed are novel compounds of the formula: ##STR1## wherein: X=--NR.sub.5 R.sub.6, or --OR.sub.7 ;R.sub.1 and R.sub.2 are independently hydrogen, substituted or unsubstituted alkyl, haloalkyl, hydroxyalkyl alkoxyalkyl, alkylaminoalkyl or arylalkyl having up to 18 carbons, cycloalkyl; phenyl or naphthyl; alkylphenyl, cyanophenyl, halophenyl or alkoxyphenyl substituents;R.sub.3 is hydrogen, benzyl, alkoxybenzyl, halobenzyl or alkylbenzyl, provided that if neither R.sub.1 nor R.sub.2 is hydrogen, then R.sub.3 is hydrogen;R.sub.4 is a divalent aromatic group which is substituted or unsubstituted;R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen, alkyl, hydroxyalkyl, haloalkyl, alkoxyalkyl, alkylaminoalkyl, acylaminoalkyl, aminoalkyl or phenylalkyl having up to 12 carbons; a cycloalkyl substitutent; phenyl or naphthyl; an alkylphenyl, cyanophenyl, halophenyl or alkoxyphenyl substituent;Furthermore, either R.sub.1 and R.sub.3 or R.sub.1 and R.sub.
    Type: Grant
    Filed: April 17, 1989
    Date of Patent: March 5, 1991
    Assignee: Anitec Image Corporation
    Inventors: Bruce M. Resnick, Allan J. Wexler
  • Patent number: 4987130
    Abstract: Substituted amino derivatives represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 each stand for an acyclic hydrocarbon residue or an alicyclic hydrocarbon residue; R.sup.3 and R.sup.4 each stand for hydrogen or a hydrocarbon residue optionally containing hetero-atom(s); A stands for a carbon chain having two or more carbon atoms optionally containing ether linkage or sulfide linkage, which may be substituted and which may per se form a ring; X.sup.1 and X.sup.2 each stand for oxygen atom or sulfur atom; and Y stands for amino group or an organic residue bonded through nitrogen atom, which may form a ring by combining with a carbon atom constituting A; and their salts have anti-arrhythmic activity and are useful for prevention and treatment of a variety of arrhythmias.
    Type: Grant
    Filed: December 22, 1989
    Date of Patent: January 22, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Susumu Tsushima, Muneo Takatani, Minoru Hirata
  • 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: 4906634
    Abstract: Novel N-[4-(aminosubstituted)phenyl]methanesulfonamides and their use as cardiovascular agents, especially as antiarrhythmic agents are described. Pharmaceutical formulations containing such compounds are also discussed.
    Type: Grant
    Filed: March 8, 1988
    Date of Patent: March 6, 1990
    Assignee: Schering A.G.
    Inventors: Stanley S. Greenberg, William C. Lumma, Jr., Klaus Nickisch, Ronald A. Wohl
  • Patent number: 4895840
    Abstract: Novel N-(Aryl-,aryloxy-,arylthio-,arylsulfinyl-and arylsulfonyl-)alkyl-N,N'-(or N',N')alkylaminoalkyl ureas, thioureas and cyanoguanidines represented by the following formula: ##STR1## wherein Ar is aryl selected from the group consisting of 1- and 2-naphthyl, 2,3-dihydro-1H-inden-4(or 5)-yl,2-furanylmethyl,2-pyridinyl, phenyl and phenyl substituted by 1-3 radicals commonly used in the pharmaceutical art; (X).sub.d is oxygen, thio, sulfinyl, sulfonyl or d is zero; Z and W are each R or-(CH.sub.2).sub.m -NR.sup.1 R.sup.2 wtih the proviso that when Z is R, W is-(CH.sub.2).sub.m -NR.sup.1 R.sup.2 and when Z is-(CH.sub.2).sub.m -NR.sup.1 R.sup.2, W is R; B is carbonyl, thioxomethyl, or cyanoiminomethyl; R, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are selected from the group consisting of hydrogen, loweralkyl, cycloalkyl, phenyl or phenyl-loweralkyl wherein phenyl may be substituted by 1-3 radicals commonly used in the pharmaceutical art; R.sup.1 and R.sup.2, and R.sup.3 and R.sup.
    Type: Grant
    Filed: June 10, 1987
    Date of Patent: January 23, 1990
    Assignee: A. H. Robins Company, Incorporated
    Inventor: James R. Shanklin, Jr.
  • Patent number: 4889953
    Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is a higher alkyl group which may be substituted; R.sup.2 is a hydrogen, a lower alkyl group which may be substituted, a lower alkanoyl group which may be substituted or a lower alkylthiocarbamoyl group; R.sup.3 is a primary to tertiary amino group or a quaternary ammonium group; and n is 2 or 3, and salts thereof, have antitumor activity and platelet activating factor inhibitory activity.
    Type: Grant
    Filed: July 22, 1987
    Date of Patent: December 26, 1989
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Keizo Inoue, Hiroaki Nomura, Tetsuya Okutani
  • Patent number: 4873327
    Abstract: Compounds of the general formula ##STR1## in which each of A and B independently represents a halogen atom or an alkyl group; m is 0 or 1; Q represents a group of general formula ##STR2## in which R is as defined, or Q represents a group of general formula --CR.sup.2 R.sup.3 R.sup.4 in which R.sup.2, R.sup.3 and R.sup.4 are as defined; together with processes for the preparation of such compounds, pesticidal compositions containing them and their pesticidal use, and certain novel intermediates.
    Type: Grant
    Filed: March 8, 1988
    Date of Patent: October 10, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Martin Anderson, Anthony G. Brinnand