Sulfur In Substituent Q Patents (Class 564/85)
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Patent number: 7026477Abstract: The invention relates to a preparation process for a compound (I) or a salt thereof, in which Q, X*, Y, Z, R, R1, R2 and R3 are as defined in claim 1, which comprises a) ammonolyzing a comp. (II) in which Hal=halogen atom to give (III), pref. (a1) carrying out the reaction in an organic solvent mixture (org. solv. mixture) comprising (1) opt. halogenated aromatic hydrocarbons and (2) polar aprotic solvents, in a weight ratio of solv. (1): solv. (2) of 20:1 to 1:1, (b) phosgenating the comp. (III) with phenylsulfonyl isocyanate of the formula (IV), pref. (b1) in the case X*=halogen, carrying out the reaction with phosgene in an org. solv. in the presence of isocyanates R?-NCO as catalyst, where R?=(subst.) hydrocarbon, with or without addition of an amine base, (c) reacting the resulting compound (IV) in org. solv. with the aminoheterocycle H2N-Het (Het=heterocycle as in (I)) to give the comp. (I) or a salt thereof, pref. (c1) carrying out the reaction in a solv. mixture of opt. halogenated arom.Type: GrantFiled: September 28, 2000Date of Patent: April 11, 2006Assignee: Aventis CropScience GmbHInventors: Jan Vermehren, Ernst Schmidt, Mark James Ford, Richard W. G. Foster, Ian A. Bourne
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Patent number: 6919375Abstract: Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof.Type: GrantFiled: July 22, 1998Date of Patent: July 19, 2005Assignee: Shionogi & Co., Ltd.Inventors: Fumihiko Wantanabe, Hiroshige Tsuzuki, Mitsuaki Ohtani
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Patent number: 6908947Abstract: The present invention relates to compounds of formula I, in which X1, X2, X3, X4, Y1, Y2, Y3, Y4, R(3), R(4) and R(5) have the meanings mentioned in the specification, their preparation and their use, in particular in pharmaceuticals. The compounds effect the potassium channel or the IKs channel opened by cyclic adenosine monophosphate (cAMP) and are outstandingly suitable as pharmaceutical active compounds, for example for the prophylaxis and therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal disorders.Type: GrantFiled: October 25, 2001Date of Patent: June 21, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Joachim Brendel, Hans Jochen Lang, Uwe Gerlach
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Patent number: 6890956Abstract: Compounds of formula I: inhibit the processing of APP by gamma-secretase, and hence are useful in treating or preventing Alzheimer's disease.Type: GrantFiled: October 6, 2003Date of Patent: May 10, 2005Assignee: Merck Sharp & Dohme LimitedInventors: Ian Churcher, Timothy Harrison, Sonia Kerrad, Alan John Nadin, Andrew Pate Owens, Duncan Edward Shaw, Joanne Thomson, Susannah Williams
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Patent number: 6838483Abstract: Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof.Type: GrantFiled: November 8, 2002Date of Patent: January 4, 2005Assignee: Shionogi & Co., Ltd.Inventors: Fumihiko Wantanabe, Hiroshige Tsuzuki, Mitsuaki Ohtani
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Patent number: 6734182Abstract: This invention is directed to novel aryl sulfonamide and sulfamide compounds which bind selectively to and inhibit the activity of the human Y5 receptor. This invention is also related to uses of these compounds for the treatment of feeding disorders such as obesity, anorexia nervosa, bulimia nervosa, and abnormal conditions such as sexual/reproductive disorders, depression, epileptic seizure, hypertension, cerebral hemorrhage, congestive heart failure or sleep disturbances and for the treatment of any disease in which antagonism of a Y5 receptor may be useful.Type: GrantFiled: April 2, 2002Date of Patent: May 11, 2004Assignee: Synaptic Pharmaceutical CorporationInventors: Imadul Islam, Daljit S. Dhanoa, John M. Finn, Ping Du, Charles Gluchowski, Yoon T. Jeon
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Patent number: 6720424Abstract: Aminobenzoic acid derivatives represented by Formula (1) as follows: (wherein, R1 represents a hydrogen atom, a C1-6alkyl group, or the like; R2 represents a hydrogen atom, a C1-6alkyl group, or the like; R3 represents a C8-25alkyl group, or the like; R4 represents a hydrogen atom or a group represented by OR9 or CO2R10 (wherein R9 and R10 represent a hydrogen atom or a C1-6 alkyl group); A represents a group represented by S(O)qR15 (wherein q is 0, 1, or 2, R15 represents a C1-6alkyl group, a phenyl C1-3alkyl group, or a group represented by (CH2)mOR16 (wherein m is 2 or 3, and R16 represents a hydrogen atom or a methoxymethyl group), or the like; X represents O, a single bond, CH═CH, or a group represented by NR27 (wherein R27 represents a hydrogen atom or a t-butoxycarbonyl group); Y represents O, CONH, NHCO, or a group represented by NR28 (wherein R28 represents a hydrogen atom or a t-butoxycarbonyl group); and n is an integer of 0 to 15) or pharmaceutically acceptable salts of theType: GrantFiled: January 2, 2002Date of Patent: April 13, 2004Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Hisaya Wada, Hajime Asanuma, Tetsuo Takayama, Masakazu Sato, Takehiro Yamagishi, Masabumi Shibuya
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Patent number: 6699884Abstract: Methods of treating cyclooxygenase-2 mediated disorders comprising administering to a subject a therapeutically effective amount of one or more fluoro-substituted benzenesulfonyl compounds corresponding to Formula I: wherein A, X, n, R1, R2, and R3 are as described in the specification, and novel fluoro-substituted benzenesulfonyl compounds within Formula I.Type: GrantFiled: December 13, 2002Date of Patent: March 2, 2004Assignee: Pharmacia CorporationInventors: David L. Brown, Matthew J. Graneto, Cindy L. Ludwig, John M. Molyneaux, John J. Talley
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Publication number: 20030208006Abstract: A method is provided for making aromatic-imide and aromatic-methylidynetrissulfonyl species by reaction of aromatic species with a reactant according to formula (I):Type: ApplicationFiled: May 12, 2003Publication date: November 6, 2003Applicant: 3M Innovative Properties CompanyInventor: Steven Joseph Hamrock
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Publication number: 20030204097Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: ApplicationFiled: March 15, 2002Publication date: October 30, 2003Applicant: G.D. Searle & Co.Inventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, David L. Brown, Joseph J. McDonald
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Publication number: 20030158252Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: 1Type: ApplicationFiled: February 6, 2003Publication date: August 21, 2003Applicant: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan, Thomas P. Stagnaro
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Publication number: 20030135063Abstract: Compounds of formula I are useful for treating conditions associated with hyperglycemia, especially Type II diabetes. These compounds are useful in stimulating the kinase activity of the insulin receptor, activating the insulin receptor, and stimulating the uptake of glucose. Pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.Type: ApplicationFiled: September 6, 2002Publication date: July 17, 2003Inventors: Wayne R. Spevak, Songyuan Shi, Prasad V.V.S.V. Manchem, Michael R. Kozlowski, Steven R. Schow, Robert T. Lum
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Patent number: 6583318Abstract: A method of synthesizing &agr;-sulfonamido amide, carboxylic acid or hydroxamic acid derivatives comprising providing a set of polymer-bound reactant(s) (sulfonamide, aldehyde or ketone, isocyanide or acid) to react with three sets of the other three reactants to form an array of polymer-bound &agr;-sulfonamido amide-type intermediates and use of such intermediates for the preparation of combinatorial libraries.Type: GrantFiled: May 15, 2002Date of Patent: June 24, 2003Assignee: Advanced Syntech, LLCInventors: Eugene Campian, Boliang Lou, Adnan M. M. Mjalli
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Patent number: 6583161Abstract: The invention provides compounds, compositions and methods relating to novel aromatic derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: December 12, 2000Date of Patent: June 24, 2003Assignee: Tularik Inc.Inventor: Julio C. Medina
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Patent number: 6552086Abstract: The present invention provides certain sulfonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.Type: GrantFiled: January 23, 2001Date of Patent: April 22, 2003Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, Paul Leslie Ornstein, Edward C. R. Smith, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Patent number: 6541422Abstract: A method of selectively controlling undesirable vegetation in crops by using a postemergent application of an herbicidally effective amount of a metal chelate of a 2-(substituted benzoyl)-1,3-cyclohexanedione compound to the locus of such undesirable vegetation.Type: GrantFiled: May 28, 1999Date of Patent: April 1, 2003Assignee: Syngenta LimitedInventors: Herbert B. Scher, Jinling Chen
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Patent number: 6538159Abstract: The invention relates to &agr;-sulfin- and &agr;-sulfonamino acid amides of the general formula I including the optical isomers thereof and mixtures of such isomers, wherein n is a number zero or one; R1 is C1-C12alkyl, C1-C12alkyl substituted with C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or C3-C6alkenyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl; or a group NR12R13 wherein R12 and R13 are each independently of the other hydrogen or C1-C6-alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently hydrogen; C1-C8alkyl; C1-C8alkyl substituted with hydroxy, mercapto, C1-C4alkoxy or C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered hydrocarbon ring; R4, R5, R6 and R7 are each independently hydrogen or C1-C4alkType: GrantFiled: June 1, 2001Date of Patent: March 25, 2003Assignee: Syngenta Participations AGInventors: Martin Zeller, André Jeanguenat, Clemens Lamberth
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Patent number: 6538016Abstract: The invention relates to &agr;-sulfin- and &agr;-sulfonamino acid amides of the general formula I including the optical isomers thereof and mixtures of such isomers, wherein n is a number zero or one; R1 is C1-C12alkyl, C1-C12alkyl substituted with C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl; or a group NR12R13 wherein R12 and R13 are each independently of the other hydrogen or C1-C6-alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently hydrogen; C1-C8alkyl; C1-C8alkyl substituted with hydroxy, mercapto, C1-C4alkoxy or C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered hydrocarbon ring; R4, R5, R6 and R7 are each independently hydrogen or C1-C4alType: GrantFiled: June 1, 2001Date of Patent: March 25, 2003Assignee: Syngenta Participations AGInventors: Martin Zeller, André Jeanguenat, Clemens Lamberth
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Patent number: 6521667Abstract: The present invention features calcilytic compounds. “Calcilytic compounds” refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.Type: GrantFiled: August 11, 1998Date of Patent: February 18, 2003Assignees: NPS Pharmaceuticals, Inc., SmithKline Beecham, PLC, SmithKline Beecham, Corp.Inventors: Eric G. Del Mar, Robert M. Barmore, Derek Sheehan, Bradford C. Van Wagenen, James F. Callahan, Richard M. Keenan, Nikesh R. Kotecha, Maria Amparo Lago, Linda Sue Southall, Mervyn Thompson
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Publication number: 20030032657Abstract: Methods of treating cyclooxygenase-2 mediated disorders comprising administering to a subject a therapeutically effective amount of one or more fluoro-substituted benzenesulfonyl compounds corresponding to Formula I: 1Type: ApplicationFiled: April 16, 2002Publication date: February 13, 2003Applicant: Pharmacia CorporationInventors: David L. Brown, Matthew J. Graneto, Cindy L. Ludwig, John M. Molyneaux, John J. Talley
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Publication number: 20030023016Abstract: The present invention is concerned with novel ion-exchange membranes, their method of preparation and their uses. The membranes are made of a polymer obtained from a monomer or a mixture of bifunctional monomers of general formula [T-SO2—Y—SO2T′]−M+. The polymers are useful in an alkali-chloride electrolysis process, as a separator in an electrochemical preparation of inorganic and organic compounds, as a separator between an aqueous and an organic phase, or as a catalyst for Diels-Alder additions, Friedel-Craft reactions, aldol condensations, cationic polymerizations, esterifications, and acetal formations.Type: ApplicationFiled: July 23, 2002Publication date: January 30, 2003Inventors: Christophe Michot, Michel Armand
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Publication number: 20030013125Abstract: The present invention provides compounds and libraries of compounds having formula (I): 1Type: ApplicationFiled: May 10, 2002Publication date: January 16, 2003Inventors: Andrew C. Braisted, Daniel A. Erlanson, Jeffrey W. Jacobs
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Patent number: 6498253Abstract: Compounds of the formula (I) and salts thereof in which W1, W2, R, n, R1, R2, R4, X, Y and Z are as defined in claim 1 and R3 is an acyl radical, are suitable as herbicides and plant growth regulators. The herbicides can be prepared by the process variants from claim 5, the novel intermediate products (II), (IV), (VI) and (VIII)* of claims 9 and 10 being employed.Type: GrantFiled: February 25, 1999Date of Patent: December 24, 2002Assignee: Hoechst Schering AgrEvo GmbHInventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer
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Publication number: 20020183393Abstract: Compounds of formula 1: 1Type: ApplicationFiled: September 14, 2001Publication date: December 5, 2002Inventors: David J. Morgans, Teri Melese, Stuart Tugendreich
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Patent number: 6489365Abstract: Compounds of the formula which is explained more fully in the specification, may be prepared by conventional methods and used therapeutically in conventional galenic preparations.Type: GrantFiled: January 18, 2000Date of Patent: December 3, 2002Assignee: Boehringer Ingelheim KGInventors: Ralf Anderskewitz, Kurt Schromm, Ernst-Otto Renth, Frank Himmelsbach, Franz Birke, Armin Fugner
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Patent number: 6455502Abstract: The present invention relates to novel N-cyanomethyl amides which are cysteine protease inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.Type: GrantFiled: March 15, 2000Date of Patent: September 24, 2002Assignee: AXYS Pharmaceuticals, Inc.Inventors: Clifford M. Bryant, Barry A. Bunin, Erica A. Kraynack, John W. Patterson
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Patent number: 6448293Abstract: A compound of general formula (I), or pharmaceutically acceptable salts, solvates or polymorphs thereof; wherein; R1 and R2, which may be the same or different, are hydrogen, C1-C6alkyl, (CH2)m (C3-C6cycloalkyl) wherein m =0, 1, 2 or 3, or R1 and R2 together with the nitrogen to which they are attached form an azetidine ring; each R3 is independently CF3, OCF3, C1-4alkylthio or C1-C4alkoxy; n is 1, 2 or 3; and R4 and R5, which may be the same or different, are: A—X, wherein A =—CH=CH— or —(CH2)p— where p is 0, 1 or 2; X is hydrogen, F, Cl, Br, I, CONR6R7, SO2NR6R7, SO2NHC(=O)R6, OH, C1-4alkoxy, NR8SO2R9, NO2, NR6R11, CN, CO2R10, CHO, SR10, S(O)R9 or SO2R10; R6, R7, R8 and R10 which may be the same or different, are hydrogen or C1-6alkyl optionally substituted independently by one or more R12; R9 is C1-6 alkyl optionally substituted independently by one or more R12; R11 is hydrogen, C1-6 alkyl optionally substituted independently by one or more R12, C(OType: GrantFiled: March 16, 2001Date of Patent: September 10, 2002Assignee: Pfizer Inc.Inventors: Mark David Andrews, David Hepworth, Donald Stuart Middleton, Alan Stobie
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Patent number: 6414020Abstract: Amidino and benzamidino compounds, including compounds of the formula: wherein R1-R4, R6-R9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.Type: GrantFiled: May 9, 2001Date of Patent: July 2, 2002Assignee: 3- Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Carl R. Illig, Richard M. Soll
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Publication number: 20020052349Abstract: This invention relates to anti-inflammatory and analgesic compounds, especially to certain p-(sulfonyl)phenyl amino derivatives, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.Type: ApplicationFiled: April 26, 2001Publication date: May 2, 2002Inventors: Nancy Elisabeth Krauss, Taraneh Mirzadegan, David Bernard Smith, Keith Adrian Walker
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Patent number: 6362230Abstract: The present invention provides novel sulphonamide derivatives which are useful for potentiating glutamate receptor function in a mammal requiring treatment, processes for their preparation, and pharmaceutical compositions containing them.Type: GrantFiled: November 21, 2000Date of Patent: March 26, 2002Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, Paul Leslie Ornstein, Dennis Michael Zimmerman, Ana Maria Escribano
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Patent number: 6342512Abstract: Sulfonylcarboxamide derivatives of formula I, their physiologically acceptable salts and/or physiologically functional derivatives, methods of making these compounds, their use for preparing medicines for the prevention and treatment of hyperlipidemia and arteriosclerotic disorders. The compounds of formula I have the following structure: in which the radicals are as defined and their physiologically acceptable salts and physiologically functional derivatives are described.Type: GrantFiled: September 1, 2000Date of Patent: January 29, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Reinhard Kirsch, Hans-Ludwig Schaefer, Eugen Falk, Horst Hemmerle
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Patent number: 6333349Abstract: The present invention relates to compounds of formula I, in which X1, X2, X3, X4, Y1, Y2, Y3, Y4, R(3), R(4) and R(5) have the meanings mentioned in the specification, their preparation and their use, in particular in pharmaceuticals. The compounds effect the potassium channel or the IKs channel opened by cyclic adenosine monophosphate (cAMP) and are outstandingly suitable as pharmaceutical active compounds, for example for the prophylaxis and therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal disorders.Type: GrantFiled: June 29, 1999Date of Patent: December 25, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Joachim Brendel, Hans Jochen Lang, Uwe Gerlach
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Patent number: 6333337Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.Type: GrantFiled: January 13, 1999Date of Patent: December 25, 2001Assignee: ICAgen, Inc.Inventors: Michael F. Gross, Neil A. Castle
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Patent number: 6221914Abstract: The present invention is directed to compounds which are capable of inhibiting the activity of tryptase. Such compounds are useful in the treatment or prevention of inflammatory disease, particularly those disease states which are mediated by mast cell activation. Also encompassed by the invention are formulations comprising the noted compounds, processes for preparing such compounds and methods for treating or preventing an inflammatory disease.Type: GrantFiled: October 27, 1998Date of Patent: April 24, 2001Assignee: Array Biopharma Inc.Inventors: Laurence E. Burgess, James P. Rizzi
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Patent number: 6221866Abstract: in which R(1) to R(8) have the meanings stated in the claims, act on the Kv1.5 potassium channel, and inhibit a potassium current, referred to as “ultra-rapidly activating delayed rectifier,” in the human atrium. They are therefore very particularly suitable as novel antiarrhythmic active substances, in particular for the treatment and prophylaxis of atrial arrhythmias, e.g., atrial fibrillation or atrial flutter.Type: GrantFiled: June 23, 2000Date of Patent: April 24, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Joachim Brendel, Uwe Gerlach, Hans Ulrich Stilz, Hans-Jochen Lang
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Patent number: 6214882Abstract: Benzenesulphonamide compounds of general formula (I), wherein R1 is a hydrogen or halogen atom such as chlorine or fluorine, or a straight or branched C1-4 alkyl or C1-4 alkoxy group, each of R2, R3 and R4, which are the same or different, is a hydrogen atom or a straight, branched or cyclic C1-4 alkyl group, and R1 is a hydrogen atom or a C1-2 alkyl, C1-2 fluoroalkyl or C1-2 perfluoroalkyl group, in the form of enantiomers, diastereoisomers or mixtures thereof, including racemic mixtures, as well as pharmaceutically acceptable acid addition salts thereof, are provided for therapeutical use.Type: GrantFiled: January 16, 1998Date of Patent: April 10, 2001Assignee: SynthelaboInventors: Thomas Purcell, Christophe Philippo
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Patent number: 6211241Abstract: This invention is directed to novel aryl sulfonamide and sulfamide compounds which bind selectively to and inhibit the activity of the human Y5 receptor. This invention is also related to uses of these compounds for the treatment of feeding disorders such as obesity, anorexia nervosa, bulimia nervosa, and abnormal conditions such as sexual/reproductive disorders, depression, epileptic seizure, hypertension, cerebral hemorrhage, congestive heart failure or sleep disturbances and for the treatment of any disease in which antagonism of a Y5 receptor may be useful.Type: GrantFiled: June 1, 1998Date of Patent: April 3, 2001Assignee: Synaptic Pharmaceutical CorporationInventors: Imadul Islam, Daljit S. Dhanoa, John M. Finn, Ping Du, Charles Gluchowski, Yoon T. Jeon
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Patent number: 6211176Abstract: &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: GrantFiled: July 1, 1999Date of Patent: April 3, 2001Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 6191170Abstract: The invention provides compounds, compositions and methods relating to novel aromatic derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: January 7, 1999Date of Patent: February 20, 2001Assignee: Tularik Inc.Inventor: Julio C. Medina
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Patent number: 6174922Abstract: The present invention provides novel sulphonamide derivatives which are useful for potentiating glutamate receptor function in a mammal requiring treatment, processes for their preparation, and pharmaceutical compositions containing them.Type: GrantFiled: February 23, 1999Date of Patent: January 16, 2001Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, Paul Leslie Ornstein, Dennis Michael Zimmerman, Ana Maria Escribano
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Patent number: 6133315Abstract: Amidino and benzamidino compounds, including compounds of the formula: ##STR1## wherein R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.Type: GrantFiled: March 16, 1999Date of Patent: October 17, 2000Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Carl R. Illig, Richard M. Soll
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Patent number: 6103766Abstract: Compounds of Formula I and their pharmaceutically acceptable salts having selective dopamine D3 receptor activity suitable for treating central nervous system disorders. Formula I: ##STR1## R.sub.1 is independently H or a C.sub.1 -C.sub.8 alkyl including isomeric forms thereof;R.sub.2 is H, C.sub.1 -C.sub.3 alkyl, a halogen, OCH.sub.3 , OCF.sub.3, CF.sub.3, CN, SCH.sub.3 or NHCOCH.sub.3 ; andR.sub.3 is H, C.sub.1 -C.sub.3 alkyl, a halogen, OCH.sub.3 , OCF.sub.3, CF.sub.3, CN, SCH.sub.3 or NHCOCH.sub.3.Type: GrantFiled: May 7, 1999Date of Patent: August 15, 2000Assignee: Pharmacia & Upjohn CompanyInventors: Arthur Glenn Romero, Jeffrey A. Leiby
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Patent number: 6075166Abstract: The present invention is to novel photochemically cleavable aryl sulfonamides of the formulaP--A.sub.3 --A.sub.2 --A.sub.1 --S(O).sub.2 NR.sub.1 R.sub.2whereinR.sub.1 and R.sub.2 are independently selected from optionally substituted alkyl, arylalkyl or heteroarylalkyl;A.sub.1 is an aryl or heteroaryl moiety;A.sub.2 is a linking agent is an aryl, heteroaryl, arylalkyl, heteroaryl alkyl, or an alkyl, wherein the alkyl moiety in the arylalkyl, heteroaryl alkyl, or alkyl group is optionally interrupted one or more times independently by oxygen, NR.sub.3, sulfur or an amide group;R.sub.3 is alkyl;A.sub.3 is an electron rich aryl or heteroaryl moiety having an E.sub.1/2 potential of 0.5 to 2.0 and which moiety is capable of forming an exciplex;P is a solid support.Another aspect of the present invention is to the novel use of these photolytically cleavable aryl sulfonamides in combinatorial chemistry synthesis, for use in non-sequential encoding, as a tagging agent.Type: GrantFiled: March 31, 1995Date of Patent: June 13, 2000Assignee: SmithKline Beecham CorporationInventors: Ravi Shunker Garigipati, Jerry Leroy Adams
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Patent number: 6001881Abstract: Benzoylguanidines of the formula I ##STR1## in which: R(1) to R(4) have the meanings given in the claims, are antiarrhythmic pharmaceuticals, having a cardioprotective component, which are also valuable for the prevention of ischemically induced damage, in particular in association with the triggering of ischemically induced cardiac arrhythmias. As a consequence of inhibiting the cellular Na.sup.+ /H.sup.+ exchange mechanism, they are used for treating acute or chronic damage triggered by ischemia. In addition to this, they are notable for their strong inhibitory effect on the proliferation of cells. They are suitable for preventing the genesis of high blood pressure.Type: GrantFiled: June 4, 1997Date of Patent: December 14, 1999Assignee: Hoechst AktiengesellschaftInventors: Andreas Weichert, Joachim Brendel, Heinz-Werner Kleemann, Hans Jochen Lang, Jan-Robert Schwark, Udo Albus, Wolfgang Scholz
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Patent number: 5977384Abstract: A compound of formula I, including optical isomers thereof, ##STR1## wherein X represents --SO.sub.2 NH-- or --NHSO.sub.2 --,p, q and r independently represent 2 or 3;Y represents thienyl optionally substituted by alkyl or halogen, or phenylthio- or phenyl optionally substituted by alkyl or halogen, andeach R independently represents H or alkyl,and pharmaceutically acceptable salts, esters and amides thereof.Type: GrantFiled: September 2, 1998Date of Patent: November 2, 1999Assignee: Astra Pharmaceuticals Ltd.Inventors: Roger Victor Bonnert, Roger Charles Brown
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Patent number: 5965744Abstract: The present invention relates to ortho-substituted benzoylguanidines of the formula I, defined in the specification. The invention also embraces processes for making these compounds, as well as compositions and methods of using them. The compounds of the invention exhibit very good antiarrhythmic properties, making them useful in treating or preventing infarction, angina pectoris, and pathophysiological processes associated with ischemically induced damage.Type: GrantFiled: February 24, 1997Date of Patent: October 12, 1999Assignee: Hoeschst AktiengesellschaftInventors: Andreas Weichert, Hans-Jochen Lang, Heinz-Werner Kleemann, Jan-Robert Schwark, Wolfgang Scholz, Udo Albus
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Patent number: 5945450Abstract: Naphthalene derivatives represented by formula ?I!: ##STR1## (wherein A is a hydrogen atom, a hydroxy group, a C.sub.7 -C.sub.11 aralkyloxy group, or an alkoxy group composed of an oxy group and a C.sub.1 -C.sub.12 aliphatic or alicyclic, saturated or unsaturated hydrocarbon group where the allyl may be substituted with a C.sub.6 -C.sub.10 allyloxy group; Q represents O, S, CH.sub.2, O--CH.sub.2, S--CH.sub.2, CO, or CHOR.sup.1 ; L represents CO, CR.sup.2 R.sup.3 CO, CH.sub.2 CH.sub.2 CO, or CH.dbd.CHCO; D represents a hydrogen atom, NO.sub.2, NH.sub.2, CO.sub.2 R.sup.4, or a group having the following formula ?II!: ##STR2## (wherein G represents. a hydrogen atom, OH, SO.sub.2 NH.sub.2, CO.sub.2 R.sup.6, CN, or a tetrazol-5-yl group); E represents a hydrogen atom, OH, SO.sub.2 NH.sub.2, CO.sub.2 R.sup.5, CN, or a tetrazol-5-yl group; M represents a hydrogen atom, a C.sub.1 -C.sub.4 lower alkyl group, a nitro group, or a halogen atom; and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.Type: GrantFiled: November 22, 1996Date of Patent: August 31, 1999Assignee: Teijin LimitedInventors: Kazuya Takenouchi, Katsushi Takahashi, Masaichi Hasegawa, Takahiro Takeuchi, Keiji Komoriya
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Patent number: 5872280Abstract: The invention relates to benzoic acid derivatives being leukotriene antagonists. The compounds therefore are suitable as active ingredients in medicaments particularly in medicaments for the treatment of respiratory diseases.Type: GrantFiled: November 13, 1996Date of Patent: February 16, 1999Assignee: Bayer AktiengesellschaftInventors: Trevor Smyth Abram, Nigel James Cuthbert, Hilary Patricia Francis, Phillip John Gardiner, Peter Norman, Stephen Richard Tudhope
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Patent number: 5846926Abstract: A novel class of nonionic gemini surfactants and methods for their preparation consist of compounds with three hydrophilic heads and two lipophilic tails of the general formula: ##STR1## wherein R.sub.1 and R.sub.3 independently represents a C.sub.1 to C.sub.22 straight or branched chain alkyl, alkylene, aryl or alkylaryl, or hydrogen, with the proviso that both cannot be hydrogen; R.sub.2 represents a C.sub.1 to C.sub.5 straight or branched chain alkyl, alkylene or hydrogen, (Y) represents ##STR2## wherein R.sub.4 represents C.sub.1 to C.sub.3 alkyl or hydrogen and may be the same or different; X represents --(CH.sub.2).sub.a -- wherein a is a whole number of from 1 to 5; --S--, --S--S--, --SO.sub.2, --(CH.sub.2).sub.a SO.sub.2 (CH.sub.2).sub.a --,--O--, --C.dbd.O, or --CH.sub.2 --NR--CH.sub.2 -- wherein R is a C.sub.1 to C.sub.3 straight or branched chain alkyl, alkylene or hydrogen and x, y, and z are whole numbers of from about 6 to about 300.Type: GrantFiled: June 9, 1997Date of Patent: December 8, 1998Assignee: Rhodia Inc.Inventors: David James Tracy, Ruoxin Li, Jiang Yang
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Patent number: 5753710Abstract: Substituted benzyloxycarbonylguanidines, a process for their preparation, their use as a medicament or diagnostic, and a medicament containing them. There are described compounds of the formula I ##STR1## in which the substituents R(1) to R(7) and X have the meanings shown in the claims, and their pharmaceutically tolerable salts. These are effective inhibitors of the cellular sodium proton antiporter (Na.sup.+ /H.sup.+ exchanger). They are therefore outstandingly suitable for the treatment of all diseases which can be attributed to increased Na.sup.+ /H.sup.+ exchange.Type: GrantFiled: May 15, 1996Date of Patent: May 19, 1998Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Joachim Brendel, Jan-Robert Schwark, Andreas Weichert, Hans-Jochen Lang, Udo Albus, Wolfgang Scholz