Benzothiazoles (including Hydrogenated) Patents (Class 544/135)
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Publication number: 20040235842Abstract: The present invention relates to a compound of formula I 1Type: ApplicationFiled: May 18, 2004Publication date: November 25, 2004Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
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Publication number: 20040204584Abstract: The present invention relates to compounds of the general formula I 1Type: ApplicationFiled: March 30, 2004Publication date: October 14, 2004Inventors: Alexander Flohr, Roger David Norcross
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Patent number: 6743788Abstract: Disclosed are novel aromatic compounds of the formula(I) described herein, wherein G, E, W, Ar, X, Y and Z are disclosed herein. The compounds are useful for treating cytokine mediated diseases or conditions such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.Type: GrantFiled: May 17, 2002Date of Patent: June 1, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Victor Kamhi, John Robinson Regan, Michele Tsang
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Patent number: 6734179Abstract: The present invention relates to compounds of the formula wherein R1 and R2 are as described within. The compounds of formula I have been found to be adenosine receptor ligands. Specifically, the compounds of the present invention have a good affinity to the A2A-receptor and they may be used in the treatment of diseases, related to this receptor.Type: GrantFiled: December 2, 2002Date of Patent: May 11, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
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Patent number: 6730671Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes, for making such novel compounds.Type: GrantFiled: February 13, 2003Date of Patent: May 4, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Charles L. Cywin, Michel J. Emmanuel, Tina Morwick, Denice M. Spero, David S. Thomson, Yancey D. Ward
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Publication number: 20040030131Abstract: A compound of the formula in which R1 and R2 are each hydrogen or C1-4 alkyl, or R1 and R2 together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl or morpholino group, said group being optionally substituted with 1 to 3 substituents selected from C1-4 alkyl, hydroxymethyl, C1-4 alkoxymethyl and amido, R3 is a naphthyl, indolyl, benzothienyl, benzofuranyl, benzothiazolyl, quinolinyl or isoquinolinyl group, said group being optionally substituted, and n is 1 or 2; and m is 0 or 1, provided that when m is 1 then n is 1; or a salt or ester thereof.Type: ApplicationFiled: September 3, 2003Publication date: February 12, 2004Inventors: Martine Keenan, Vincent Patrick Rocco, Kumiko Takeuchi, David Edward Tupper, Vincent Vivien
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Patent number: 6667307Abstract: Selected sulfonylalkanoylamino hydroxyethylamine 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: GrantFiled: February 26, 2002Date of Patent: December 23, 2003Assignee: G.D. Searle & Co.Inventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, Joseph J. McDonald
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Publication number: 20030199501Abstract: The present invention relates to using a compound having the formula (I) wherein T is I) thienyl, which optionally is substituted with halogen, or II) phenyl optionally substituted with halogen and/or C1-6-alkyl; E is a bond, —CH2— or —CO—; L is a bond, —CH2—, —CHR4— or —NR3—; R3 is H, C1-6-alkyl, C1-6-acyl or —COR4; R4 is morpholino or C1-6-amido; R6 and R7 are independently hydrogen or C1-6-alkyl; and R8 and R9 are independently hydrogen or C1-6-alkyl, as well as pharmaceutically acceptable salts, hydrates and solvates thereof, in the manufacture of a medicament for the treatment or prevention of diabetes, syndrome X, obesity, glaucoma, hyperlipidemia, hyperglycemia, hyperinsulinemia, osteoporosis, tuberculosis, dementia, depression, virus diseases and inflammatory disorders.Type: ApplicationFiled: March 18, 2003Publication date: October 23, 2003Inventors: Marianne Nilsson, Jerk Vallgarda, Tjeerd Barf
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Patent number: 6624163Abstract: The present invention relates to compounds of the formula wherein R1 and R2 are as defined herewithin. The compounds of formula I have been found to be adenosine receptor ligands. Specifically, the compounds of the present invention have a good affinity to the A2A-receptor and they are therefore useful in the treatment of diseases, related to this receptor.Type: GrantFiled: November 15, 2002Date of Patent: September 23, 2003Assignee: Hoffman-La Roche Inc.Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
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Publication number: 20030176695Abstract: The present invention relates to substituted benzothiazole derivitives and to their pharmaceutically acceptable salts useful for the treatment of diseases related to the adenosine receptor.Type: ApplicationFiled: December 18, 2002Publication date: September 18, 2003Inventors: Alexander Alanine, Alexander Flohr, Aubry Kern Miller, Roger David Norcross, Claus Riemer
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Patent number: 6608057Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases.Type: GrantFiled: October 24, 2001Date of Patent: August 19, 2003Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Charles L. Cywin, Michel J. Emmanuel, Tina Morwick, Denice M. Spero, David S. Thomson, Yancey D. Ward
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Publication number: 20030153566Abstract: The present invention relates to compounds of the formula 1Type: ApplicationFiled: December 2, 2002Publication date: August 14, 2003Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
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Publication number: 20030144288Abstract: The present invention relates to compounds of the formula 1Type: ApplicationFiled: December 2, 2002Publication date: July 31, 2003Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
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Patent number: 6596718Abstract: A compound of the formula A compound of formula I has a good affinity to the A2A receptor and is useful for the treatment of diseases mediated by this receptor.Type: GrantFiled: November 18, 2002Date of Patent: July 22, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Flohr, Roland Jakob-Roetne, Norcross David Roger, Claus Riemer
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Publication number: 20030134855Abstract: The present invention relates to compounds of the formula 1Type: ApplicationFiled: November 15, 2002Publication date: July 17, 2003Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
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Publication number: 20030114448Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: ApplicationFiled: May 28, 2002Publication date: June 19, 2003Applicant: Millennium Pharmaceuticals, Inc.Inventors: Penglie Zhang, Bing-Yan Zhu, Wenrong Huang, Robert M. Scarborough
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Patent number: 6562817Abstract: The present invention provides a compound of the formula (I): wherein A ring, B ring and C ring are each independently optionally substituted aromatic carbocycle or optionally substituted 5- or 6-membered heterocycle which may fuse with benzene ring, W1, W2 and/or W3 represents a bond when A ring, B ring and/or C ring is optionally substituted 5-membered heterocycle, X is —O—, —NR1— wherein R1 is hydrogen, lower alkyl etc. or the like, Y is hydrogen, lower alkyl, lower alkenyl or the like, one of V1 and V2 is a bond, and the other is a bond, —O— or the like, and a pharmaceutical composition comprising the same.Type: GrantFiled: July 21, 2000Date of Patent: May 13, 2003Assignee: Shionogi & Co., Ltd.Inventors: Norihiko Tanimoto, Yasushi Hasegawa, Nobuhiro Haga
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Patent number: 6552199Abstract: The subject matter of the invention are new xanthene derivatives of the formula I, wherein R1,R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and X, Y, are as defined herein. The compounds according to the invention provide molecules that are—due to their spectral properties (absorption maxima in the range of approx. 650 nm and above as well as emission maxima above 670 nm)—very suitable for the use as dyes and in particular as fluorescence dyes. The compounds of the formula I according to the invention are used for the production of fluorescence conjugates, for their application in immunoassays, for DNA analytics, for in-vivo diagnostics or as a laser dye.Type: GrantFiled: May 11, 2000Date of Patent: April 22, 2003Assignee: Roche Diagnostics GmbHInventors: Ewald Daltrozzo, Alexander Reiss
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Patent number: 6548667Abstract: The present invention provides a novel sulfonamide derivative of general formula (I) useful as an inhibitor of matrix metalloproteinase (MMP), its isomers, pharmaceutically acceptable salts thereof and a process for preparing the same. Since the sulfonamide derivatives of the present invention selectively inhibit MMP activity in vitro, the MMP inhibitors comprising the sulfonamide derivatives as an effective ingredient can be practically applied for the prevention and treatment of all sorts of diseases caused by overexpression and overactivation of MMP.Type: GrantFiled: December 6, 2001Date of Patent: April 15, 2003Assignee: Samsung Electronics Co. Ltd.Inventors: Young-Jun Park, Hae-Young Bae, Ji-Uk Yoo, Myeong-Yun Chae, Sang-Hyun Paek, Hye-Kyung Min, Hyun-Gyu Park, Choon-Ho Ryu, Kyung-Chul Kim, Jeoung-Wook Lee
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Publication number: 20020169314Abstract: The present invention provides a novel sulfonamide derivative of general formula (I) useful as an inhibitor of matrix metalloproteinase (MMP), its isomers, pharmaceutically acceptable salts thereof and a process for preparing the same. Since the sulfonamide derivatives of the present invention selectively inhibit MMP activity in vitro, the MMP inhibitors comprising the sulfonamide derivatives as an effective ingredient can be practically applied for the prevention and treatment of all sorts of diseases caused by overexpression and overactivation of MMP.Type: ApplicationFiled: December 6, 2001Publication date: November 14, 2002Inventors: Young-Jun Park, Hae-Young Bae, Ji-Uk Yoo, Myeong-Yun Chae, Sang-Hyun Paek, Hye-Kyung Min, Hyun-Gyu Park, Choon-Ho Ryu, Kyung-Chul Kim, Jeoung-Wook Lee
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Patent number: 6403835Abstract: The invention relates to the shape selective acylation of an organic compound. In particular, the invention describes a process for such acylation wherein the process comprises reducing the number of surface acid sites without dealuminations on at least a portion of the surface of a zeolite and acylating the organic compound in the presence of the zeolite. The organic compounds used in the invention include, for example, olefins, aromatic hydrocarbons, aromatic heterocyclic compounds, and phenolic compounds wherein the organic group may be substituted or unsubstituted. The zeolite may be any natural or synthetic zeolite with a unidimensional or multidimensional network, for example a two-dimensional, or three-dimensional network, or any molecular sieve with structural features similar to these.Type: GrantFiled: November 2, 2000Date of Patent: June 11, 2002Assignee: California Institute of TechnologyInventors: Mark E. Davis, Patricia Andy, Javier Garcia Martinez, Gary Lee, Hector Gonzalez, Christopher W. Jones
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Patent number: 6380188Abstract: Selected sulfonylalkanoylamino hydroxyethylamine 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: GrantFiled: September 29, 2000Date of Patent: April 30, 2002Assignee: G. D. Searle & Co.Inventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagaraian, Joseph J. McDonald
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Publication number: 20020045620Abstract: The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, isoxazolidine compounds which have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds which have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the isoxazolidine compounds are also taught.Type: ApplicationFiled: September 21, 2001Publication date: April 18, 2002Inventors: Pascal Druzgala, Peter G. Milner
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Patent number: 6362183Abstract: An aromatic sulfonyl alpha-hydroxy hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: June 4, 1999Date of Patent: March 26, 2002Assignee: G. D. Searle & CompanyInventors: John N. Freskos, Terri L. Boehm, Brent V. Mischke, Robert M. Heintz, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard
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Patent number: 6313116Abstract: Compounds that are inhibitors of phosphodiesterase and have therapeutic utility, are of formula (i) wherein R1 is C3-6 cycoalkyl, or C1-3 alkyl optionally substituted with one or more fluorine atoms; R2 is C1-6 alkyl, C3-6 cycloalkyl, CF3, CH2CF3, C2F5 or NR4R5; R3 is a pyrazole, imidazole or isoxazole group of partial formula (A), (B) or (C) NR4R5 is a nitrogen-containing heterocyclic ring; R6 is C1-3 alkyl; and R7 and R8, which are the same or different, are each H, C1-3 alkyl, halogen, CF3 or CN, provided that both are not H; or a pharmaceutically-acceptable salt thereofType: GrantFiled: February 9, 2001Date of Patent: November 6, 2001Assignee: Darwin Discovery, Ltd.Inventors: Hazel Joan Dyke, Andrew Sharpe, Hannah Jayne Kendall, Richard John Davenport, Verity Margaret Sabin, George Martin Buckley, Marianna Dilani Richard, Alan Findlay Haughan
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Patent number: 6251913Abstract: Compounds of formula (I), wherein: n is 1 to 6; Het is a nitrogen containing ring fused to the benzene ring on two adjacent carbon atoms to form a bicyclic ring system which ring system may be optionally substituted; R1 is hydrogen, C1-8alkyl, C2-6alkenyl, C2-6alkyny, C3-8cycloalkyl, aryl, heteroaryl, heterocyclyl, arylC1-6alkyl, heteroarylC1-6alkyl, heterocyclylC1-6alkyl or C3-8cycloalkylC1-6alkyl; R2 is C1-6alkyl, C2-6alkenyl, arylC1-6alkyl, heteroarylC1-6alkyl or the side-chain of a naturally occurring amino acid; R3 is hydrogen, C1-6alkyl, C3-8cycloalkyl, C4-8cycloalkenyl, arylC1-6alkyl, heteroarylC1-6alkyl or heterocycylC1-6alkyl; R4 is hydrogen or C1-6alkyl; or R3 and R4 together with the nitrogen atom to which they are joined form a heterocyclic ring; wherein any group or ring, in R1-R4, is optionally substituted; and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof, are described as inhibitors of the production of Tumor Necrosis Factor and/or one or more matrType: GrantFiled: September 24, 1999Date of Patent: June 26, 2001Assignees: Zeneca Limited, Zeneca Pharma S.A.Inventor: Thomas Geoffrey Colerick Bird
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Patent number: 6214991Abstract: Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.Type: GrantFiled: March 31, 1999Date of Patent: April 10, 2001Assignee: The Institute for Pharmaceutical Discovery, Inc.Inventors: Michael Lee Jones, David Gunn, John Howard Jones, Michael C. Van Zandt
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Patent number: 6201126Abstract: Compounds of the formula (I) in which A represents N or a cyanomethylene radical, B represents S, O or NH and R1, R2, R3 and x have the meaning given in the description, are highly suitable for dyeing and printing high-molecular-weight materials, in particular automotive cover fabrics.Type: GrantFiled: June 2, 1997Date of Patent: March 13, 2001Assignee: Bayer AktiengesellschaftInventor: Manfred Lorenz
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Patent number: 6169085Abstract: Selected sulfonylalkanoylamino hydroxyethylamine 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: GrantFiled: October 4, 1999Date of Patent: January 2, 2001Assignee: G. D. Searle & CompanyInventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, Joseph J. McDonald
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Patent number: 6124330Abstract: The present invention is concerned with compounds of formula ##STR1## the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen, hydroxy, C.sub.1-6 alkyl or aryl; R.sup.2 is hydrogen; optionally substituted C.sub.1-12 alkyl; C.sub.3-7 cycloalkyl; C.sub.2-8 alkenyl, optionally substituted pyrrolidinyl or aryl; R.sup.3 is hydrogen, optionally substituted C.sub.1-6 alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; ##STR2## is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.Type: GrantFiled: April 29, 1999Date of Patent: September 26, 2000Assignee: Janssen-Cilag S.A.Inventors: Marc Gaston Venet, Dominique Jean-Pierre Mabire, Jean Fernand Armand Lacrampe, Gerard Charles Sanz
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Patent number: 6063795Abstract: Selected heterocyclecarbonyl 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: GrantFiled: May 10, 1999Date of Patent: May 16, 2000Assignee: G.D. Searle & CompanyInventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L Brown, Joseph J McDonald
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Patent number: 6043240Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: March 28, 2000Assignee: Hoechst Marion Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
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Patent number: 5985870Abstract: Selected sulfonylalkanoylamino hydroxyethylamine 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: GrantFiled: December 19, 1997Date of Patent: November 16, 1999Assignee: G.D. Searle & Co.Inventors: Daniel P Getman, Gary A. Decrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, Joseph J. McDonald
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Patent number: 5874432Abstract: Novel 2-substituted saccharins which inhibit the enzymatic activity of proteolytic enzymes, are useful in the treatment of degenerative diseases and have the formula ##STR1## wherein: L is --O--, --S--, --SO-- or --SO.sub.2 --;m and n are each independently 0 or 1;R.sub.1 is halo, lower-alkanoyl, 1-oxophenalenyl, phenyl or substituted phenyl, heterocyclyl or substitued heterocyclyl or, when L is --O-- and n is 1, cycloheptatrienon-2-yl or, when L is --S-- and n is 1, cyano or lower-alkoxythiocarbonyl or, when L is --SO.sub.2 -- and n is 1, lower-alkyl or trifluoromethyl;R.sub.2 is hydrogen, lower-alkoxycarbonyl, phenyl or phenylthio; andR.sub.3 and R.sub.4 are each hydrogen or various substituents and processes for preparation and pharmaceutical compositions and method of use thereof are disclosed.Type: GrantFiled: February 20, 1997Date of Patent: February 23, 1999Assignee: SanofiInventors: Richard Paul Dunlap, Neil Warren Boaz, Albert Joseph Mura, Dennis John Hlasta, Ranjit Chimanlal Desai, Chakrapani Subramanyam, Lee Hamilton Latimer, Eric Piatt Lodge
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Patent number: 5856349Abstract: 4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl heterocyclic carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with either a heterocyclic carboxylic acid in the presence of an acid-acceptor or the alkali metal salt of a heterocyclic carboxylic acid.Type: GrantFiled: June 6, 1997Date of Patent: January 5, 1999Assignee: SanofiInventors: Richard Paul Dunlap, Dennis John Hlasta, Ranjit Chimanlal Desai, Lee Hamilton Latimer, Chakrapani Subramanyam, John Joseph Court, Malcolm Rice Bell, Virendra Kumar
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Patent number: 5854263Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: December 29, 1998Assignee: Hoechst Marion Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5854243Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: December 29, 1998Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
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Patent number: 5783589Abstract: 4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl aryl and aryloxy acetates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with an aryl or aryloxyacetic acid in the presence of an acid-acceptor.Type: GrantFiled: May 24, 1995Date of Patent: July 21, 1998Assignee: SanofiInventors: Lee Hamilton Latimer, Richard Paul Dunlap
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Patent number: 5773456Abstract: Compounds having the structural formula ##STR1## wherein L is N, O or SO.sub.n wherein n is 0, 1 or 2;L--R.sup.1 is a leaving group, H--L--R.sup.1 is the conjugate acid thereof and, when L is N, H--L--R.sup.1 has a pK.sub.a value less than or equal to 6, when L is O, H--L--R.sup.1 has a pK.sub.a value less than or equal to to 8, and when L is SO.sub.n, H--L--R.sup.1 has a pK.sub.a value less than or equal to 5;R.sup.2 is primary or secondary alkyl of two to four carbon atoms, primary alkylamino of one to three carbon atoms, primary alkylmethylamino of two to four carbon atoms, diethylamino or primary alkoxy of one to three carbon atoms; andR.sup.Type: GrantFiled: September 25, 1996Date of Patent: June 30, 1998Assignee: SanofiInventors: Richard Paul Dunlap, Albert Joseph Mura, Dennis John Hlasta, Ranjit Chimanlal Desai, Lee Hamilton Latimer
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Patent number: 5705639Abstract: This invention includes compounds of Formula II and IV and a process for preparing Formula I compounds by first preparing the compounds of Formula IV and then further reacting to form the compounds of Formula II and further reacting to prepare the compounds of Formula I wherein Q, Z, R.sup.2 are as defined within.Type: GrantFiled: September 21, 1995Date of Patent: January 6, 1998Assignee: E. I. du Pont de Nemours and CompanyInventor: Rafael Shapiro
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Patent number: 5705500Abstract: Selected sulfonylalkanoylamino hydroxyethylamine 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: GrantFiled: June 7, 1995Date of Patent: January 6, 1998Assignee: G.D. Searle & Co.Inventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, Joseph J. McDonald
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Patent number: 5691356Abstract: Disubstituted heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein G is ##STR2## wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; p is 0, 1 or 2, Q is a single bond or ##STR3## and Z, A, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.6 are as defined herein.Type: GrantFiled: September 4, 1996Date of Patent: November 25, 1997Assignee: Bristol-Myers Squibb CompanyInventors: Jagabandhu Das, Spencer D. Kimball, Wan Fang Lau
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Patent number: 5663449Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: September 2, 1997Assignee: Hoechst Marion Roussel, Inc.Inventor: Joseph T. Strupczewski
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Patent number: 5658911Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: September 20, 1994Date of Patent: August 19, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau, Edward J. Glamkowski, Yulin Chiang, Grover C. Helsley
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Patent number: 5654319Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: August 5, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5652254Abstract: 4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl heterocyclic carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with either a heterocyclic carboxylic acid in the presence of an acid-acceptor or the alkali metal salt of a heterocyclic carboxylic acid.Type: GrantFiled: August 28, 1996Date of Patent: July 29, 1997Assignee: Sanofi, S.A.Inventors: Richard Paul Dunlap, Dennis John Hlasta, Ranjit Chimanlal Desai, Lee Hamilton Latimer, Chakrapani Subramanyam, John Joseph Court, Malcolm Rice Bell, Virendra Kumar
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Patent number: 5650422Abstract: Novel 2-substituted saccharins which inhibit the enzymatic activity of proteolytic enzymes, are useful in the treatment of degenerative diseases and have the formula ##STR1## wherein: L is --O--, --S--, --SO-- or --SO.sub.2 --;m and n are each independently 0 or 1;R.sub.1 is halo, lower-alkanoyl, 1-oxophenalenyl, phenyl or substituted phenyl, heterocyclyl or substitued heterocyclyl or, when L is --O-- and n is 1, cycloheptatrienon-2-yl or, whenL is --S-- and n is 1, cyano or lower-alkoxythiocarbonyl or, when L is --SO.sub.2 -- and n is 1, lower-alkyl or trifluoromethyl;R.sub.2 is hydrogen, lower-alkoxycarbonyl, phenyl or phenylthio; andR.sub.3 and R.sub.4 are each hydrogen or various substituents and processes for preparation and pharmaceutical compositions and method of use thereof are disclosed.Type: GrantFiled: July 5, 1994Date of Patent: July 22, 1997Assignee: SanofiInventors: Richard Paul Dunlap, Neil Warren Boaz, Albert Joseph Mura, Dennis John Hlasta, Ranjit Chimanlal Desai, Chakrapani Subramanyam, Lee Hamilton Latimer, Eric Piatt Lodge
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Patent number: 5639764Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: June 17, 1997Assignee: Hoechst-Marion-Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5637710Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: December 22, 1995Date of Patent: June 10, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau
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Patent number: 5633265Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: May 27, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler