Sulfur Containing Hetero Ring Patents (Class 548/527)
  • Patent number: 6320059
    Abstract: There is provided a process for the preparation of 2-aryl-5-(perfluoroalkyl)pyrrole compounds from N-[1-chloro-1-(perfluoroalkyl)methyl]arylimidoyl chloride compounds. The 2-aryl-5-(perfluoroalkyl)pyrrole compounds are useful for the control of insect and acrid pests, and may also be used to prepare other pesticidal arylpyrrole compounds. In addition, the present invention provides compounds which are useful as intermediates in the preparation of arylpyrrole compounds.
    Type: Grant
    Filed: March 7, 2000
    Date of Patent: November 20, 2001
    Assignee: American Cyanamid Company
    Inventor: Venkataraman Kameswaran
  • Publication number: 20010041705
    Abstract: A compound of the formula 1
    Type: Application
    Filed: May 22, 2001
    Publication date: November 15, 2001
    Inventor: Harry R. Howard
  • Patent number: 6312811
    Abstract: The photochromic compounds of the invention correspond to the formula: in which Th2 represents a bithienyl group in one of the positions 5 to 10 of the naphthenic ring system system, R1 denotes a bithienyl or trithienyl group and R2 denotes a bithienyl, trithienyl, aryl, naphthyl, thienyl, furyl, pyrrolyl or N-alkylpyrrolyl group.
    Type: Grant
    Filed: July 8, 1999
    Date of Patent: November 6, 2001
    Assignee: Essilor International Compagnie Generale d'Optique
    Inventors: Michel Frigoli, Nicole Rebiere-Galy, Corinne Moustrou, Andre Samat, Robert Guglielmetti
  • Patent number: 6313164
    Abstract: Compounds of the formula (I): wherein one of m and n is 0, and the other is 0, 1 or 2; k is 0 or 1 to 12; R1 is hydrogen, a substituent which is an aryl or a heterocyclic, or an optionally substituted alkyl group; A is a single bond, an oxygen atom, a carbonyl group or a group of the formula —N(R2)CO—, —N(R2)CS—, —N(R2)SO2—, —CON(R2)N(R3)CO—, —CON(R2)CO—, —CON(R2)CS—, —CON(R2)SO2—, —O—CO—, —ON(R2)CO—, —ON(R2)SO2—, —O—CON(R2)N(R3)CO—, —O—CON(R2)CO—, —O—CON(R2)SO2—, —CO—O—, —CO—CO—, —CO—CON(R2)N(R3)CO—, —CO—CON(R2)CO—, —CO—CON(R2)SO2—, —N(R2)O—, —N(R2)COCO—, —N(R2)N(R3)CO—, —N(R2)N(R3)SO2—, —N(R2)CON(R3)N(R4)CO—, —N(R2)CON(R3)CO—, —N(R2)CON(R3)SO2&mdas
    Type: Grant
    Filed: July 15, 1999
    Date of Patent: November 6, 2001
    Assignee: Sankyo Company, Limited
    Inventors: Takashi Fujita, Tomihisa Yokoyama
  • Publication number: 20010027254
    Abstract: A 1-substituted 2,5-dithienylpyrrole derivative having the following 1
    Type: Application
    Filed: March 12, 2001
    Publication date: October 4, 2001
    Inventor: Katsuyuki Ogura
  • Patent number: 6294680
    Abstract: A process has been provided to produce semi synthetic statins, as for instance simvastatin with a high yield, for another statin, preferably a naturally occurring statin, as for instance lovastatin. Also a number of novel intermediate compounds, prepared during said process, has been provided.
    Type: Grant
    Filed: January 5, 2000
    Date of Patent: September 25, 2001
    Assignee: Plus Chemicals, B.V.
    Inventors: Ton Rene Vries, Hans Wijnberg, Wijnand Sjourd Faber, Venetka Ivanova Kalkman-Agayn, Mieke Ivanova Sibeyn
  • Patent number: 6284785
    Abstract: 1-Arenesulfonyl-2-Aryl-pyrrolidine and pyridine derivatives having activity as ligands of metabotropic glutamate receptors of the formula are disclosed.
    Type: Grant
    Filed: March 24, 2000
    Date of Patent: September 4, 2001
    Assignee: Hoffmann- La Roche Inc.
    Inventors: Vincent Mutel, Eric Vieira, Jürgen Wichmann
  • Patent number: 6245804
    Abstract: This invention describes the new, nonsteroidal gestagens of general formula I in which A, B, Ar, R1, R2 and R3 have the meanings that are indicated in more detail in the description. The new compounds show a very great affinity to the gestagen receptor. They can be used alone or in combination with estrogens in contraceptive preparations. In addition, they can be used for treating endometriosis. Together with estrogens, they can also be used in preparations for treating gynecological disorders, for treating premenstrual symptoms and for substitution therapy. Based on the androgenic action, they can also be used for male birth control, male HRT and hormone therapy and for treating andrological disease agents.
    Type: Grant
    Filed: May 29, 1998
    Date of Patent: June 12, 2001
    Assignee: Schering Aktiengesellschaft
    Inventors: Manfred Lehmann, Klaus Schoellkopf, Peter Strehlke, Nikolaus Heinrich, Karl-Heinrich Fritzemeier, Rolf Krattenmacher, Hans-Peter Muhn
  • Patent number: 6197750
    Abstract: This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.
    Type: Grant
    Filed: October 22, 1998
    Date of Patent: March 6, 2001
    Assignee: Idun Pharmaceuticals, Inc.
    Inventors: Donald S. Karanewsky, Robert J. Ternansky
  • Patent number: 6174879
    Abstract: Aminocyclohexylester compounds, including thioesters, are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the blockade of ion channels and the treatment of arrhythmias.
    Type: Grant
    Filed: March 17, 1999
    Date of Patent: January 16, 2001
    Assignee: University of British Columbia
    Inventors: Bernard A. MacLeod, Michael J. A. Walker, Richard A. Wall
  • Patent number: 6172240
    Abstract: The present invention relates to pyrrole derivatives, particularly 2-(2-thienyl)-5-(5-tricyanoethenyl-2-thienyl)pyrrole derivatives, which has metallic luster, good stability in air, and a high solubility in an organic solvent, and which is suitable for a film-forming material.
    Type: Grant
    Filed: December 29, 1999
    Date of Patent: January 9, 2001
    Assignee: Chiba University
    Inventor: Katsuyuki Ogura
  • Patent number: 6166082
    Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula(T).sub.x A--B--D--E--Gwherein A and B are aryl or heteroaryl rings; each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR1## the group E represents a three carbon chain bearing one to three substituent groups which are independent or are involved in ring formation, possible structures being shown in the text and claims; and the group G represents --M, ##STR2## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12 ; andR.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids, and include pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: April 9, 1998
    Date of Patent: December 26, 2000
    Assignee: Bayer Corporation
    Inventors: Harold Clinton Eugene Kluender, Guenter Hans Heinz Herbert Benz, David Ross Brittelli, William Harrison Bullock, Kerry Jeanne Combs, Brian Richard Dixon, Stephan Schneider, Jill Elizabeth Wood, Michael Christopher VanZandt, Donald John Wolanin, Scott M. Wilhelm
  • Patent number: 6159995
    Abstract: Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.
    Type: Grant
    Filed: May 8, 1998
    Date of Patent: December 12, 2000
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Bernhard Neises, Gunter Billen
  • Patent number: 6133288
    Abstract: The present invention provides compounds of formula I and II: ##STR1## wherein X is --O--, --S--, or --NR.sup.5 --;Y is --O--, --S--, --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, or --NR.sup.5 --;B is --CH.sup.2 -- or --CO--;R.sup.1, R.sup.2, and R.sup.3 are each independently --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl), --OSO.sub.2 CF.sub.3, Cl, or F;n is 1 or 2;W is CH.sub.2 or C.dbd.O;R.sup.4 is 1-piperidinyl, 2-oxo-1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 2-oxo-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino;R.sup.5 is C.sub.1 -C.sub.3 alkyl, --COC.sub.6 H.sub.5, --CO(C.sub.1 -C.sub.6 alkyl), --C(O)OC.sub.6 H.sub.5, --C(O)O(C.sub.1 -C.sub.6 alkyl), --SO.sub.2 (C.sub.1 -C.sub.6 alkyl), --SO.sub.2 C.sub.6 H.sub.5, or --SO.sub.2 CF.sub.3 ;or a pharmaceutically acceptable salt or solvate thereof.
    Type: Grant
    Filed: November 9, 1999
    Date of Patent: October 17, 2000
    Assignee: Eli Lilly and Company
    Inventor: Timothy Alan Grese
  • Patent number: 6133455
    Abstract: There is provided a process for the preparation of 2-aryl-5-(perfluoroalkyl)pyrrole compounds from N-(arylmethylene)-1-chloro-1-(perfluoroalkyl)methylamine compounds. The 2-aryl-5-(perfluoroalkyl)pyrrole compounds are useful for the control of insect and acarid pests, and may also be used to prepare other pesticidal arylpyrrole compounds.In addition, the present invention provides N-(arylmethylene)-1-chloro-1-(perfluoroalkyl)methylamine compounds which are useful as intermediates in the preparation of arylpyrrole compounds.
    Type: Grant
    Filed: February 9, 1999
    Date of Patent: October 17, 2000
    Assignee: American Cyanamid Company
    Inventor: Venkataraman Kameswaran
  • Patent number: 6133252
    Abstract: A method of controlling Take-all disease of plants by applying, preferably to the seed prior to planting, a fungicide of the formula ##STR1## wherein Z.sub.1 and Z.sub.2 are C or N and are part of an aromatic ring selected from benzene, pyridine, thiophene, furan, pyrrole, pyrazole, thiazole, and isothiazole;A is selected from --C(X)-amine, --C(O)--SR.sub.3, --NH--C(X)R.sub.4, and --C(.dbd.NR.sub.3)--XR.sub.7 ;B is --W.sub.m --Q(R.sub.2).sub.3 or selected from o-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R.sub.4 ;Q is C, Si, Ge, or Sn;W is --C(R.sub.3).sub.p H.sub.(2-p) --; or when Q is C, W is selected from --C(R.sub.3).sub.p H.sub.(2-p) --, --N(R.sub.3).sub.m H.sub.(1-m) --, --S(O).sub.p --, and --O--;X is O or S;n is 0, 1, 2, or 3;m is 0 or 1;p is 0, 1, or 2;each R is independently selected from functional groups disclosed the specification.
    Type: Grant
    Filed: November 4, 1998
    Date of Patent: October 17, 2000
    Assignee: Monsanto Company
    Inventors: Dennis Paul Phillion, Diane Susan Braccolino, Matthew James Graneto, Wendell Gary Phillips, Karey Alan Van Sant, Daniel Mark Walker, Sai Chi Wong
  • Patent number: 6127391
    Abstract: Compounds of peptide mimetic nature having the general formula I ##STR1## wherein a and b are independently 1 or 2, R.sup.1 and R.sup.2 are independently H or C.sub.1-6 alkyl, G and J are independently, inter alia, aromats, and D and E are independently several different groups are growth hormone secretagogous with improved bioavailability.
    Type: Grant
    Filed: December 21, 1998
    Date of Patent: October 3, 2000
    Assignee: Novo Nordisk A/S
    Inventors: Thomas Kruse Hansen, Bernd Peschke, Jesper Lau, Behrend Friedrich Lundt, Michael Ankersen, Brett Watson, Kjeld Madsen
  • Patent number: 6121293
    Abstract: The invention provides benzothiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia, and estrogen-dependent cancer.
    Type: Grant
    Filed: June 29, 1998
    Date of Patent: September 19, 2000
    Assignee: Eli Lilly and Company
    Inventors: George Joseph Cullinan, Brian Stephen Muehl
  • Patent number: 6114358
    Abstract: Compounds of the formula ##STR1## where A, B, E and D have the meanings indicated in the description, and their preparation are described. The substances are suitable for controlling diseases.
    Type: Grant
    Filed: February 10, 1999
    Date of Patent: September 5, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Dorit Baucke, Udo Lange, Helmut Mack, Werner Seitz, Thomas Zierke, Hans Wolfgang Hoffken, Wilfried Hornberger
  • Patent number: 6103910
    Abstract: New compounds have the formula: ##STR1## wherein R, R.sup.1, X and Y have the meanings described herein. Methods are set forth for synthesizing these compounds and using these compounds to treat diseases associated with amyloidosis, such as Alzheimer's disease, maturity onset diabetes mellitus, familial amyloid polyneuropathy, scrapie, and Kreuzfeld-Jacob disease.
    Type: Grant
    Filed: October 27, 1998
    Date of Patent: August 15, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Cornelia Hertel, Torsten Hoffmann, Roland Jakob-Roetne, Roger David Norcross
  • Patent number: 6063928
    Abstract: Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having the following formula I: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Ar.sup.1 is a heterocyclic moiety which is selected from imidazolyl, pyrrolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, indolyl, indazolyl and benzimidazolyl, which is bonded to X.sup.1 through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C.sub.1-4 alkyl and the like; X.sup.1 is a direct bond or C.sub.1-4 alkylene; Ar.sup.2 is phenylene optionally substituted with halo, hydroxy, cyano, amino and the like; X.sup.2 is --A--X-- or --X--A-- wherein A is a direct bond or C.sub.1-4 alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar.sup.3 is phenylene, pyridylene, thienylene, furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C.sub.1-4 alkyl and the like; R.sup.1 and R.
    Type: Grant
    Filed: December 8, 1998
    Date of Patent: May 16, 2000
    Assignee: Pfizer Inc
    Inventors: Rodney W. Stevens, Takashi Mano, Kazunari Nakao, Yoshiyuki Okumura
  • Patent number: 6060468
    Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.1a, R.sup.2, R.sup.2a, p, r and s are as defined in the detailed part of the present description or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to secretion and circulation of insulin antagonising peptides.
    Type: Grant
    Filed: October 3, 1997
    Date of Patent: May 9, 2000
    Assignee: Novo Nordisk A/S
    Inventors: Tine Krogh J.o slashed.rgensen, Erik Fischer, Rolf Hohlweg, Knud Erik Andersen, Uffe Bang Olsen, Zdenek Polivka, Vladimir Valenta, Karel Sindelar
  • Patent number: 6060488
    Abstract: This invention is related to novel benzothiophene compounds of formula I: ##STR1## where R, R.sup.1, R.sup.2, X and m are as defined in the specification, which are useful for the inhibition of the various medical conditions associated with postmenopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus, and cervix. The present invention further relates to pharmaceutical formulations of compounds of formula I.
    Type: Grant
    Filed: September 22, 1998
    Date of Patent: May 9, 2000
    Assignee: Eli Lilly and Company
    Inventors: Jeffrey Alan Dodge, Mark Gregory Stocksdale
  • Patent number: 6057441
    Abstract: This invention concerns the compounds of formula (I), ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R.sup.1 and R.sup.2 each independently are hydrogen; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; halomethylcarbonyl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R.sup.3 and R.sup.4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkyloxycarbonyl; each R.sup.5 independently is C.sub.1-6 alkyl, cyano or halomethyl; X is CR.sup.6 R.sup.7, NR.sup.8, O, S, S(.dbd.O) or S(.dbd.O).sub.
    Type: Grant
    Filed: October 6, 1998
    Date of Patent: May 2, 2000
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Pilar Gil-Lopetegui, Francisco Javier Fernandez-Gadea, Theo Frans Meert
  • Patent number: 6037340
    Abstract: Methods for preparing thiophene and pyrrole-based heterocyclic compounds are disclosed. Also disclosed are libraries of thiophene and pyrrole-based heterocyclic compounds, methods for preparing the libraries of thiophene and pyrrole-based heterocyclic compounds, and methods for using the thiophene and pyrrole-based heterocyclic compounds and compound libraries of the invention. The compounds of the invention have biological activity including anti-cancer activity.
    Type: Grant
    Filed: May 28, 1997
    Date of Patent: March 14, 2000
    Assignee: Cadus Pharmaceutical Corporation
    Inventors: Arlindo L. Castelhano, Bryan McKibben
  • Patent number: 6030952
    Abstract: The present invention provides novel heteroaryl compounds having the general formula (I): ##STR1## their pharmaceutical compositions to be used as human and veterinary medicine, particularly in the treatment of dermatological, rheumatic, respiratory, cardiovascular and ophthalmologic conditions, and their use in cosmetic compositions.
    Type: Grant
    Filed: October 13, 1998
    Date of Patent: February 29, 2000
    Assignee: Centre International de Recherches Dermatologioues galderma
    Inventors: Philippe Diaz, Bruno Charpentier
  • Patent number: 6025371
    Abstract: The invention provides chemistry libraries containing fused 2,4-pyrimidinediones. The invention also provides methods for the construction of fused 2,4-pyrimidinedione containing libraries. The invention further provides methods for the identification of bioactive, fused 2,4-pyrimidinediones from those libraries.
    Type: Grant
    Filed: October 28, 1996
    Date of Patent: February 15, 2000
    Assignee: Versicor, Inc.
    Inventors: Mikhail F. Gordeev, Dinesh V. Patel
  • Patent number: 6025383
    Abstract: The invention relates to novel thiophene derivatives of the formula (I) ##STR1## in which X represents halogen, alkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, nitro or cyano, or two substituents X, together with the carbon atoms to which they are attached, form a saturated or unsaturated, optionally substituted ring,n represents a number from 1 to 3, andZ represents one of the groups ##STR2## in which A, B, D, G, Q.sup.1, Q.sup.2 and Q.sup.3 have the meaning given in the description, to processes for their preparation and to their use as pesticides and herbicides.
    Type: Grant
    Filed: June 3, 1998
    Date of Patent: February 15, 2000
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reiner Fischer, Jacques Dumas, Thomas Bretschneider, Bernd Gallenkamp, Folker Lieb, Konrad Wernthaler, Christoph Erdelen, Ulrike Wachendorff-Neumann, Norbert Mencke, Andreas Turberg
  • Patent number: 6013663
    Abstract: A compound of formula (I): ##STR1## wherein one of m and n represents 0, and the other represents 0, 1 or 2; k represents 0 or 1 to 12; R.sup.1 is hydrogen, an aryl, a heterocyclic, an alkyl, a hydroxy or --OR.sup.7, wherein R.sup.7 is an alkyl, an alkenyl or an aralkyl; A is --CON(R.sup.2)SO.sub.2--, wherein R.sup.2 is hydrogen, an alkyl or an aralkyl; B is a single bond; and pharmaceutically acceptable salts thereof. The compounds have the ability to enhance the activity of glutathione reductase and can therefore be used for the treatment and prevention of a variety of diseases including cataracts.
    Type: Grant
    Filed: March 31, 1998
    Date of Patent: January 11, 2000
    Assignee: Sankyo Company, Limited
    Inventors: Takashi Fujita, Tomihisa Yokoyama
  • Patent number: 6011161
    Abstract: There is provided a process for the preparation of 2-aryl-5-(perfluoroalkyl)pyrrole compounds from N-(perfluoroalkylmethyl)arylimidoyl chloride compounds. The 2-aryl-5-(perfluoroalkyl)pyrrole compounds are useful for the control of insect and acarid pests, and may also be used to prepare other pesticidal arylpyrrole compounds. In addition, the present invention provides N-(perfluoroalkylmethyl)arylimidoyl chloride compounds which are useful as intermediates in the preparation of arylpyrrole compounds.
    Type: Grant
    Filed: February 9, 1999
    Date of Patent: January 4, 2000
    Assignee: American Cyanamid Company
    Inventor: Venkataraman Kameswaran
  • Patent number: 6005113
    Abstract: The invention relates to fluorescent dyes that are substituted or unsubstituted derivatives of 1-(isoindolyl)methylene-isoindole that are bound through both isoindole nitrogens to a boron difluoride moiety, forming a fluorescent dibenzopyrrometheneboron difluoride compound ##STR1## that is further substituted by bathochromic substituents that are aryl or heteroaryl moieties further substituted by an additional aryl or heteroaryl, that is itself optionally further substituted by an additional aryl or heteroaryl. These aryl and heteroaryl groups are separated by a covalent bond, or by an ethenyl, butadienyl or hexatrienyl linkage. The dyes of the invention are particularly useful as labels for carriers, particularly polymeric microparticles. The resulting microparticles have a long-wavelength fluorescence emission, and possess utility for tracing flow in biological systems, particularly in tracing blood flow.
    Type: Grant
    Filed: May 14, 1997
    Date of Patent: December 21, 1999
    Assignee: Molecular Probes, Inc.
    Inventors: Yexin Wu, Dieter H. Klaubert, Hee Chol Kang, Yu-Zhong Zhang
  • Patent number: 6004964
    Abstract: Anti-pruritic pharmaceutical formulations containing kappa agonist compounds and methods of prevention or treatment of pruritus in a mammal with the anti-pruritic formulations.
    Type: Grant
    Filed: November 2, 1998
    Date of Patent: December 21, 1999
    Assignee: Adolor Corporation
    Inventors: John J. Farrar, An-Chih Chang, Virendra Kumar, Wei Yuan Zhang, Alan Cowan
  • Patent number: 5977111
    Abstract: A thiopyran derivative represented by the following formula (I) or (I'), or the salt thereof. ##STR1## wherein A is S or --CH.dbd.CH--; the dotted line indicates that the bond may be either present or absent; Z and Z' are typically ##STR2## L is an ethylene or trimethylene group; Y is CH or N; n is 2; B is a carbonyl group; m is 0 or 1; D is a phenyl group; and E.sub.1 and E.sub.2 are hydrogen atoms. These compounds exhibit a strong serotonin-2 blocking action and highly safe. Some compounds also exhibit an .alpha..sub.1 -blocking action and therefore are useful as an antihypertensive agent with less side effects. Thus, the thiopyran derivatives are useful as drugs for the treatment of circulatory diseases in general such as hypertension, ischemic heart disease, cerebrovascular disturbance, and peripheral circulatory disturbance.
    Type: Grant
    Filed: June 21, 1996
    Date of Patent: November 2, 1999
    Assignee: Suntory Limited
    Inventors: Akira Mizuno, Makoto Shibata, Tomoe Iwamori, Norio Inomata
  • Patent number: 5968954
    Abstract: New 2-aminoindan compounds of formula: ##STR1## wherein: n, Ar, R, E, X.sub.1, X.sub.2, X.sub.3, and X.sub.4 are as defined in the description, in the form of a racemic mixture and in the form of optical isomers, and physiologically-tolerable acid addition salts thereof. The products of the invention are useful as medicaments and exhibit selective binding affinity for the 5HT.sub.1B receptors.
    Type: Grant
    Filed: February 26, 1998
    Date of Patent: October 19, 1999
    Assignee: Adir et Compagnie
    Inventors: Jean-Louis Peglion, Bertrand Goument, Mark Millan, Alain Gobert
  • Patent number: 5965575
    Abstract: New N-arylpiperidine compounds of formula: ##STR1## wherein: A, m, R, E, n and Ar are as defined in the description, the isomers thereof and the addition salts thereof with a pharmaceutically acceptable acid, and medicinal products containing the same are useful in the treatment of disorders involving the serotininergic system.
    Type: Grant
    Filed: March 27, 1998
    Date of Patent: October 12, 1999
    Assignee: Adir Et Compagnie
    Inventors: Jean-Louis Peglion, Bertrand Goument, Mark Millan, Alain Gobert, Valerie Audinot
  • Patent number: 5958918
    Abstract: The compounds of formula I exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More especially, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
    Type: Grant
    Filed: November 21, 1997
    Date of Patent: September 28, 1999
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: William R. Ewing, Michael R. Becker, Henry W. Pauls, Daniel L. Cheney, Jonathan Stephen Mason, Alfred P. Spada, Yong Mi Choi-Sledeski
  • Patent number: 5935973
    Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R.sub.1 is an optional substituent; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents CO.HET, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.
    Type: Grant
    Filed: January 5, 1998
    Date of Patent: August 10, 1999
    Assignee: Knoll Aktiengesellschaft
    Inventors: Alan Martin Birch, David John Heal, Frank Kerrigan, Keith Frank Martin, Patricia Lesley Needham, Bruce Jeremy Sargent
  • Patent number: 5925773
    Abstract: There are provided ammonium oxazole intermediates of formula I and amino oxazolium intermediates of formula II, useful in the manufacture of insecticidal arylpyrrole compounds.
    Type: Grant
    Filed: June 27, 1997
    Date of Patent: July 20, 1999
    Assignee: American Cyanamid Company
    Inventor: Venkataraman Kameswaran
  • Patent number: 5919923
    Abstract: The invention provides for tripyrrane compounds of the formula ##STR1## wherein: each Q represents, typically, an alkyl group, cycloalkyl group, aryl group, or a heteroaryl group; and each R represents hydrogen, an alkyl group, alcohol group, or a carbonyl-containing group. Additionally, there are described methods to prepare such compounds, for example, comprising the steps of:(a) reacting a compound of the formula:Q--CHO or Q--CH(OS)(OS')wherein S and S' are independently lower alkyl, an aryl group containing from 5 to 14 ring atoms, and --(CH.sub.2).sub.n -- where n=2-4;with a stoichiometric excess of a pyrrole having the formula: ##STR2## in the presence of a catalytic amount of an acid; (b) removing the unreacted pyrrole or any other solvents used in (a) by evaporation to form a residue; and(c) treating the residue to remove high molecular weight polymeric materials and the corresponding dipyrromethane by-product, leaving the desired compound.
    Type: Grant
    Filed: May 19, 1998
    Date of Patent: July 6, 1999
    Inventors: Christian Bruckner, Ross W. Boyle, David Dolphin
  • Patent number: 5886024
    Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR2## the group R6 represents a variety of possible substituent groups on the carbon chain between D and G, and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12; and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.
    Type: Grant
    Filed: May 28, 1997
    Date of Patent: March 23, 1999
    Assignee: Bayer Corporation
    Inventors: Harold Clinton Eugene Kluender, Guenter Hans Herbert Heinz Benz, William Harrison Bullock
  • Patent number: 5859042
    Abstract: The instant invention is related to 5-membered heterocyclic compounds and pharmaceutical compositions which possess inhibitory activity on 5 alpha-reductase.
    Type: Grant
    Filed: March 13, 1997
    Date of Patent: January 12, 1999
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Sung Jai Lee, Takuya Seko, Manton Rodgers Frierson, Jagadish Chandra Sircar, Charles Xian Cao
  • Patent number: 5859031
    Abstract: This invention relates to neurotrophic N-glyoxyl-prolyl ester compounds having an affinity for FKBP-type immunophilins, their preparation and use as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity.
    Type: Grant
    Filed: May 21, 1996
    Date of Patent: January 12, 1999
    Assignee: GPI NIL Holdings, Inc.
    Inventors: Gregory S. Hamilton, Joseph P. Steiner
  • Patent number: 5856341
    Abstract: The invention provides benzo?b!indenothiophene compounds of formula I ##STR1## wherein, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6, are as defined in the specification, intermediates, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, cardiovascular-related pathological conditions including hyperlipidemia and related cardiovascular pathologies, and estrogen-dependent cancer.
    Type: Grant
    Filed: September 19, 1997
    Date of Patent: January 5, 1999
    Assignee: Eli Lilly and Company
    Inventors: Michael Gregory Bell, Brian Stephen Muehl, Mark Alan Winter
  • Patent number: 5854277
    Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR2## the group R6 represents a variety of possible substituent groups on the carbon chain between D and G, and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12 ; and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.
    Type: Grant
    Filed: May 30, 1997
    Date of Patent: December 29, 1998
    Assignee: Bayer Corporation
    Inventors: Harold Clinton Eugene Kluender, Guenter Hans Herbert Heinz Benz, William Harrison Bullock, Brian Richard Dixon, Michael Christopher VanZandt, Scott McClelland Wilhelm, Donald John Wolanin, Jill Elizabeth Wood, David Ross Brittelli
  • Patent number: 5852051
    Abstract: Compounds of the formula I ##STR1## in which R.sup.1, A and B have the meanings stated in the description, and the preparation thereof are described. The novel compounds are suitable for controlling diseases.
    Type: Grant
    Filed: June 5, 1997
    Date of Patent: December 22, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Hans-Joachim Bohm, Stefan Koser, Helmut Mack, Thomas Pfeiffer, Werner Seitz, Hans Wolfgang Hoffken, Wilfried Hornberger, Thomas Zierke
  • Patent number: 5837720
    Abstract: A compound of formula (I): ##STR1## and its pharmaceutically acceptable salt, wherein R is hydrogen or hydroxy; Ar is unsubstituted or substituted phenyl; X is unsubstituted or substituted phenyl or heterocyclic, mono-, di- or trihalomethyl, cyano, or the like; and X.sup.2 is phenyl, naphthyl, furyl, thienyl, pyridyl, thiazolyl, benzofuryl or benzothienyl, each of which may either be unsubstituted or substituted. These compounds have agonist activity toward opioid kappa receptors and are thus useful as analgesic, anti-inflammatory, diuretic and neuroprotective agents.
    Type: Grant
    Filed: April 17, 1997
    Date of Patent: November 17, 1998
    Assignee: Pfizer Inc.
    Inventor: Fumitaka Ito
  • Patent number: 5834460
    Abstract: A serine derivative represented by the general formula (I) ##STR1## (symbols in the formula represent the following meanings; X: a sulfur atom or an oxygen atom,Y: a nitrogen atom or CH,R.sup.1 and R.sup.2 : the same or different from each other and each represents a hydrogen atom, a lower alkyl group or a protecting group for the amino group, or R.sup.1 and R.sup.2 may be combined together to form a four- to nine-membered nitrogen-containing cycloalkyl group,R.sup.3 : a hydrogen atom, a carboxyl group, a protected carboxyl group, an aralkyl group, or a lower alkyl group unsubstituted or substituted with a hydroxyl group,R.sup.4 : a hydrogen atom or a hydroxyl group,R.sup.
    Type: Grant
    Filed: October 12, 1995
    Date of Patent: November 10, 1998
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Ichio Noda, Masahiro Iwata, Shuichi Sakamoto, Kazuo Koshiya, Takuma Morita, Atsuyuki Kohara
  • Patent number: 5834447
    Abstract: A method of controlling Take-all disease of plants by applying, preferably to the seed prior to planting, a fungicide of the formula ##STR1## wherein Z.sub.1 and Z.sub.2 are C or N and are part of an aromatic ring selected from benzene, pyridine, thiophene, furan, pyrrole, pyrazole, thiazole, and isothiazole;A is selected from --C(X)--amine, --C(O)--SR.sub.3, --NH--C(X)R.sub.4, and --C(.dbd.NR.sub.3)--XR.sub.7 ;B is --W.sub.m --Q(R.sub.2).sub.3 or selected from o-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R.sub.4 ;Q is C, Si, Ge, or Sn;W is --C(R.sub.3).sub.p H.sub.(2-p) --; or when Q is C, W is selected from --C(R.sub.3).sub.p H.sub.(2-p) --, --N(R.sub.3).sub.m H.sub.(1-m) --, --S(O).sub.
    Type: Grant
    Filed: December 8, 1995
    Date of Patent: November 10, 1998
    Assignee: Monsanto Company
    Inventors: Dennis Paul Phillion, Diane Susan Braccolino, Matthew James Graneto, Wendell Gary Phillips, Karey Alan Van Sant, Daniel Mark Walker, Sai Chi Wong
  • Patent number: 5817834
    Abstract: There is provided a process for the preparation of 2-aryl-5-(perfluoroalkyl)pyrrole compounds from N-(perfluoroalkylmethyl)arylimidoyl chloride compounds. The 2-aryl-5-(perfluoroalkyl)pyrrole compounds are useful for the control of insect and acarid pests, and may also be used to prepare other pesticidal arylpyrrole compounds. In addition, the present invention provides N-(perfluoroalkylmethyl)arylimidoyl chloride compounds which are useful as intermediates in the preparation of arylpyrrole compounds.
    Type: Grant
    Filed: February 9, 1998
    Date of Patent: October 6, 1998
    Assignee: American Cyanamid Company
    Inventor: Venkataraman Kameswaran
  • Patent number: 5807889
    Abstract: Compounds of formula I ##STR1## wherein R1=(cyclo)alk(en)yl, aralkyl, alkyl(oxy)carbonyl, CONH2, etc.; R2=H, (cyclo)alk(en)yl, aralkyl, etc.; R3-R5=H, halo, alkyl, alkoxy, etc.; R6,R7=H, alkyl; R6R7=atoms to complete a ring; R8,R9=groups cited for R2, 2-oxoimidazolidinoalkyl, etc.; NR8R9=heterocyclyl; 1 of X,Y=CH2 and the other=CH2, O, S were prepd. Thus, 1-indancarboxylic acid was converted in 5 steps to 1-(N,N-dipropylaminomethyl)-6-formylaminoindane oxalate which had ED50 of 0.0055.mu.M/kg s.c. in the 8-OH DPAT cue agonism test in rats.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: September 15, 1998
    Assignee: H. Lundbeck A/S
    Inventor: Jens K. Perregaard