Sulfur Containing Hetero Ring Patents (Class 548/527)
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Patent number: 6320059Abstract: 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: GrantFiled: March 7, 2000Date of Patent: November 20, 2001Assignee: American Cyanamid CompanyInventor: Venkataraman Kameswaran
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Publication number: 20010041705Abstract: A compound of the formula 1Type: ApplicationFiled: May 22, 2001Publication date: November 15, 2001Inventor: Harry R. Howard
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Patent number: 6312811Abstract: 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: GrantFiled: July 8, 1999Date of Patent: November 6, 2001Assignee: Essilor International Compagnie Generale d'OptiqueInventors: Michel Frigoli, Nicole Rebiere-Galy, Corinne Moustrou, Andre Samat, Robert Guglielmetti
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Patent number: 6313164Abstract: 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&mdasType: GrantFiled: July 15, 1999Date of Patent: November 6, 2001Assignee: Sankyo Company, LimitedInventors: Takashi Fujita, Tomihisa Yokoyama
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Publication number: 20010027254Abstract: A 1-substituted 2,5-dithienylpyrrole derivative having the following 1Type: ApplicationFiled: March 12, 2001Publication date: October 4, 2001Inventor: Katsuyuki Ogura
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Patent number: 6294680Abstract: 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: GrantFiled: January 5, 2000Date of Patent: September 25, 2001Assignee: Plus Chemicals, B.V.Inventors: Ton Rene Vries, Hans Wijnberg, Wijnand Sjourd Faber, Venetka Ivanova Kalkman-Agayn, Mieke Ivanova Sibeyn
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Patent number: 6284785Abstract: 1-Arenesulfonyl-2-Aryl-pyrrolidine and pyridine derivatives having activity as ligands of metabotropic glutamate receptors of the formula are disclosed.Type: GrantFiled: March 24, 2000Date of Patent: September 4, 2001Assignee: Hoffmann- La Roche Inc.Inventors: Vincent Mutel, Eric Vieira, Jürgen Wichmann
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Patent number: 6245804Abstract: 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: GrantFiled: May 29, 1998Date of Patent: June 12, 2001Assignee: Schering AktiengesellschaftInventors: Manfred Lehmann, Klaus Schoellkopf, Peter Strehlke, Nikolaus Heinrich, Karl-Heinrich Fritzemeier, Rolf Krattenmacher, Hans-Peter Muhn
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Patent number: 6197750Abstract: 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: GrantFiled: October 22, 1998Date of Patent: March 6, 2001Assignee: Idun Pharmaceuticals, Inc.Inventors: Donald S. Karanewsky, Robert J. Ternansky
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Patent number: 6174879Abstract: 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: GrantFiled: March 17, 1999Date of Patent: January 16, 2001Assignee: University of British ColumbiaInventors: Bernard A. MacLeod, Michael J. A. Walker, Richard A. Wall
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Patent number: 6172240Abstract: 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: GrantFiled: December 29, 1999Date of Patent: January 9, 2001Assignee: Chiba UniversityInventor: Katsuyuki Ogura
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Patent number: 6166082Abstract: 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: GrantFiled: April 9, 1998Date of Patent: December 26, 2000Assignee: Bayer CorporationInventors: 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
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Patent number: 6159995Abstract: 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: GrantFiled: May 8, 1998Date of Patent: December 12, 2000Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Bernhard Neises, Gunter Billen
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Patent number: 6133288Abstract: 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: GrantFiled: November 9, 1999Date of Patent: October 17, 2000Assignee: Eli Lilly and CompanyInventor: Timothy Alan Grese
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Patent number: 6133455Abstract: 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: GrantFiled: February 9, 1999Date of Patent: October 17, 2000Assignee: American Cyanamid CompanyInventor: Venkataraman Kameswaran
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Patent number: 6133252Abstract: 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: GrantFiled: November 4, 1998Date of Patent: October 17, 2000Assignee: Monsanto CompanyInventors: Dennis Paul Phillion, Diane Susan Braccolino, Matthew James Graneto, Wendell Gary Phillips, Karey Alan Van Sant, Daniel Mark Walker, Sai Chi Wong
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Patent number: 6127391Abstract: 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: GrantFiled: December 21, 1998Date of Patent: October 3, 2000Assignee: Novo Nordisk A/SInventors: Thomas Kruse Hansen, Bernd Peschke, Jesper Lau, Behrend Friedrich Lundt, Michael Ankersen, Brett Watson, Kjeld Madsen
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Patent number: 6121293Abstract: 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: GrantFiled: June 29, 1998Date of Patent: September 19, 2000Assignee: Eli Lilly and CompanyInventors: George Joseph Cullinan, Brian Stephen Muehl
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Patent number: 6114358Abstract: 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: GrantFiled: February 10, 1999Date of Patent: September 5, 2000Assignee: BASF AktiengesellschaftInventors: Dorit Baucke, Udo Lange, Helmut Mack, Werner Seitz, Thomas Zierke, Hans Wolfgang Hoffken, Wilfried Hornberger
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Patent number: 6103910Abstract: 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: GrantFiled: October 27, 1998Date of Patent: August 15, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Cornelia Hertel, Torsten Hoffmann, Roland Jakob-Roetne, Roger David Norcross
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Patent number: 6063928Abstract: 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: GrantFiled: December 8, 1998Date of Patent: May 16, 2000Assignee: Pfizer IncInventors: Rodney W. Stevens, Takashi Mano, Kazunari Nakao, Yoshiyuki Okumura
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Patent number: 6060468Abstract: 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: GrantFiled: October 3, 1997Date of Patent: May 9, 2000Assignee: Novo Nordisk A/SInventors: Tine Krogh J.o slashed.rgensen, Erik Fischer, Rolf Hohlweg, Knud Erik Andersen, Uffe Bang Olsen, Zdenek Polivka, Vladimir Valenta, Karel Sindelar
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Patent number: 6060488Abstract: 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: GrantFiled: September 22, 1998Date of Patent: May 9, 2000Assignee: Eli Lilly and CompanyInventors: Jeffrey Alan Dodge, Mark Gregory Stocksdale
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Patent number: 6057441Abstract: 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: GrantFiled: October 6, 1998Date of Patent: May 2, 2000Assignee: Janssen Pharmaceutica, N.V.Inventors: Pilar Gil-Lopetegui, Francisco Javier Fernandez-Gadea, Theo Frans Meert
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Patent number: 6037340Abstract: 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: GrantFiled: May 28, 1997Date of Patent: March 14, 2000Assignee: Cadus Pharmaceutical CorporationInventors: Arlindo L. Castelhano, Bryan McKibben
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Patent number: 6030952Abstract: 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: GrantFiled: October 13, 1998Date of Patent: February 29, 2000Assignee: Centre International de Recherches Dermatologioues galdermaInventors: Philippe Diaz, Bruno Charpentier
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Patent number: 6025371Abstract: 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: GrantFiled: October 28, 1996Date of Patent: February 15, 2000Assignee: Versicor, Inc.Inventors: Mikhail F. Gordeev, Dinesh V. Patel
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Patent number: 6025383Abstract: 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: GrantFiled: June 3, 1998Date of Patent: February 15, 2000Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Jacques Dumas, Thomas Bretschneider, Bernd Gallenkamp, Folker Lieb, Konrad Wernthaler, Christoph Erdelen, Ulrike Wachendorff-Neumann, Norbert Mencke, Andreas Turberg
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Patent number: 6013663Abstract: 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: GrantFiled: March 31, 1998Date of Patent: January 11, 2000Assignee: Sankyo Company, LimitedInventors: Takashi Fujita, Tomihisa Yokoyama
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Patent number: 6011161Abstract: 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: GrantFiled: February 9, 1999Date of Patent: January 4, 2000Assignee: American Cyanamid CompanyInventor: Venkataraman Kameswaran
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Patent number: 6005113Abstract: 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: GrantFiled: May 14, 1997Date of Patent: December 21, 1999Assignee: Molecular Probes, Inc.Inventors: Yexin Wu, Dieter H. Klaubert, Hee Chol Kang, Yu-Zhong Zhang
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Patent number: 6004964Abstract: 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: GrantFiled: November 2, 1998Date of Patent: December 21, 1999Assignee: Adolor CorporationInventors: John J. Farrar, An-Chih Chang, Virendra Kumar, Wei Yuan Zhang, Alan Cowan
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Patent number: 5977111Abstract: 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: GrantFiled: June 21, 1996Date of Patent: November 2, 1999Assignee: Suntory LimitedInventors: Akira Mizuno, Makoto Shibata, Tomoe Iwamori, Norio Inomata
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Patent number: 5968954Abstract: 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: GrantFiled: February 26, 1998Date of Patent: October 19, 1999Assignee: Adir et CompagnieInventors: Jean-Louis Peglion, Bertrand Goument, Mark Millan, Alain Gobert
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Patent number: 5965575Abstract: 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: GrantFiled: March 27, 1998Date of Patent: October 12, 1999Assignee: Adir Et CompagnieInventors: Jean-Louis Peglion, Bertrand Goument, Mark Millan, Alain Gobert, Valerie Audinot
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Patent number: 5958918Abstract: 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: GrantFiled: November 21, 1997Date of Patent: September 28, 1999Assignee: 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
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Patent number: 5935973Abstract: 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: GrantFiled: January 5, 1998Date of Patent: August 10, 1999Assignee: Knoll AktiengesellschaftInventors: Alan Martin Birch, David John Heal, Frank Kerrigan, Keith Frank Martin, Patricia Lesley Needham, Bruce Jeremy Sargent
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Patent number: 5925773Abstract: 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: GrantFiled: June 27, 1997Date of Patent: July 20, 1999Assignee: American Cyanamid CompanyInventor: Venkataraman Kameswaran
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Patent number: 5919923Abstract: 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: GrantFiled: May 19, 1998Date of Patent: July 6, 1999Inventors: Christian Bruckner, Ross W. Boyle, David Dolphin
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Patent number: 5886024Abstract: 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: GrantFiled: May 28, 1997Date of Patent: March 23, 1999Assignee: Bayer CorporationInventors: Harold Clinton Eugene Kluender, Guenter Hans Herbert Heinz Benz, William Harrison Bullock
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Patent number: 5859042Abstract: The instant invention is related to 5-membered heterocyclic compounds and pharmaceutical compositions which possess inhibitory activity on 5 alpha-reductase.Type: GrantFiled: March 13, 1997Date of Patent: January 12, 1999Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Sung Jai Lee, Takuya Seko, Manton Rodgers Frierson, Jagadish Chandra Sircar, Charles Xian Cao
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Patent number: 5859031Abstract: 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: GrantFiled: May 21, 1996Date of Patent: January 12, 1999Assignee: GPI NIL Holdings, Inc.Inventors: Gregory S. Hamilton, Joseph P. Steiner
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Patent number: 5856341Abstract: 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: GrantFiled: September 19, 1997Date of Patent: January 5, 1999Assignee: Eli Lilly and CompanyInventors: Michael Gregory Bell, Brian Stephen Muehl, Mark Alan Winter
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Patent number: 5854277Abstract: 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: GrantFiled: May 30, 1997Date of Patent: December 29, 1998Assignee: Bayer CorporationInventors: 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
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Patent number: 5852051Abstract: 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: GrantFiled: June 5, 1997Date of Patent: December 22, 1998Assignee: BASF AktiengesellschaftInventors: Hans-Joachim Bohm, Stefan Koser, Helmut Mack, Thomas Pfeiffer, Werner Seitz, Hans Wolfgang Hoffken, Wilfried Hornberger, Thomas Zierke
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Patent number: 5837720Abstract: 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: GrantFiled: April 17, 1997Date of Patent: November 17, 1998Assignee: Pfizer Inc.Inventor: Fumitaka Ito
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Patent number: 5834460Abstract: 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: GrantFiled: October 12, 1995Date of Patent: November 10, 1998Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Ichio Noda, Masahiro Iwata, Shuichi Sakamoto, Kazuo Koshiya, Takuma Morita, Atsuyuki Kohara
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Patent number: 5834447Abstract: 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: GrantFiled: December 8, 1995Date of Patent: November 10, 1998Assignee: Monsanto CompanyInventors: Dennis Paul Phillion, Diane Susan Braccolino, Matthew James Graneto, Wendell Gary Phillips, Karey Alan Van Sant, Daniel Mark Walker, Sai Chi Wong
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Patent number: 5817834Abstract: 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: GrantFiled: February 9, 1998Date of Patent: October 6, 1998Assignee: American Cyanamid CompanyInventor: Venkataraman Kameswaran
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Patent number: 5807889Abstract: 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: GrantFiled: June 6, 1995Date of Patent: September 15, 1998Assignee: H. Lundbeck A/SInventor: Jens K. Perregaard