Polycyclo Ring System Having The Thiazole Ring As One Of The Cyclos Patents (Class 514/366)
  • Patent number: 6489354
    Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.
    Type: Grant
    Filed: March 1, 2000
    Date of Patent: December 3, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Jianming Bao, Robert K. Baker, William H. Parsons, Kathleen Rupprecht
  • Patent number: 6476059
    Abstract: The invention relates to the use of polycyclic 2-aminothiazole systems and their physiologically tolerated salts and physiologically functional derivatives for the treatment of obesity. The treatment involves administration of a compound of formula I, in which the radicals have the stated meanings, and of their physiologically tolerated salts and physiologically functional derivatives.
    Type: Grant
    Filed: February 10, 2000
    Date of Patent: November 5, 2002
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Gerhard Jähne, Karl Geisen, Hans-Jochen Lang, Martin Bickel
  • Patent number: 6444669
    Abstract: 8,8a-Dihydroindeno[1,2-d]thiazole derivatives which carry in the 2-position a substituent having a sulfonamide structure or sulfone structure; processes for their preparation and their use as medicaments The invention relates to polycyclic dihydrothiazoles and to their physiologically acceptable salts and physiologically functional derivatives. Compounds of formula I, in which the radicals are as defined above, and their physiologically acceptable salts and processes for their preparation are described. The compounds are suitable, for example, as anorectics.
    Type: Grant
    Filed: January 17, 2002
    Date of Patent: September 3, 2002
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Gerhard Jaehne, Hans Jochen Lang, Matthias Gossel, Martin Bickel
  • Publication number: 20020103231
    Abstract: 8,8a-Dihydroindeno[1,2-d]thiazole derivatives which carry in the 2-position a substituent having a sulfonamide structure or sulfone structure; processes for their preparation and their use as medicaments
    Type: Application
    Filed: January 17, 2002
    Publication date: August 1, 2002
    Inventors: Gerhard Jaehne, Hans Jochen Lang, Matthias Gossel, Martin Bickel
  • Patent number: 6426341
    Abstract: This invention is directed to methods, pharmaceutical compositions and kits comprising an aldose reductase inhibitor (ARI), a prodrug thereof or a pharmaceutically acceptable salt of said ARI or said prodrug and a selective COX-2 inhibitor, a prodrug thereof or a pharmaceutically acceptable salt of said selective COX-2 inhibitor or said prodrug. This invention further relates to methods of using those pharmaceutical compositions for the treatment of diabetic complications such as diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, myocardial infarction, cataracts and diabetic cardiomyopathy.
    Type: Grant
    Filed: June 23, 2000
    Date of Patent: July 30, 2002
    Assignee: Pfizer Inc.
    Inventor: Banavara L. Mylari
  • Publication number: 20020099074
    Abstract: The invention relates to a novel anilide compound and a pharmaceutical composition comprising the same.
    Type: Application
    Filed: December 19, 2001
    Publication date: July 25, 2002
    Applicant: Kowa Company, Ltd.,Japan
    Inventors: Kimiyuki Shibuya, Katsumi Kawamine, Yukihiro Sato, Toshiyuki Edano, Mitsuteru Hirata, Chiyoka Ozaki
  • Patent number: 6413965
    Abstract: This invention is directed to methods, pharmaceutical compositions and kits comprising an aldose reductase inhibitor (ARI), a prodrug thereof or a pharmaceutically acceptable salt of said ARI or said prodrug and a selective COX-2 inhibitor, a prodrug thereof or a pharmaceutically acceptable salt of said selective COX-2 inhibitor or said prodrug. This invention further relates to methods of using those pharmaceutical compositions for the treatment of diabetic complications such as diabetic neuropathy, diabetic nephropathy, diabetic retinopathy and diabetic cardiomyopathy.
    Type: Grant
    Filed: June 23, 2000
    Date of Patent: July 2, 2002
    Assignee: Pfizer Inc.
    Inventor: Banavara L. Mylari
  • Patent number: 6410577
    Abstract: The invention relates to substituted 8,8a-dihydro-3aH-indeno[1,2-d]thiazoles and to their physiologically acceptable salts and physiologically functional derivatives. Compounds of formula I, in which the radicals are as defined above, and their physiologically acceptable salts and processes for their preparation are described. The compounds are suitable, for example, as anorectics.
    Type: Grant
    Filed: February 23, 2001
    Date of Patent: June 25, 2002
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Gerhard Jaehne, Hans-Jochen Lang, Matthias Gossel, Martin Bickel
  • Patent number: 6410578
    Abstract: The present invention discloses a method for repelling insects, mites and ticks from warm-blooded animals with a benzazole compound.
    Type: Grant
    Filed: October 27, 2000
    Date of Patent: June 25, 2002
    Assignee: Novartis Animal Health US, Inc.
    Inventors: Jacques Bouvier, Catherine Christinaz, Olivier Froelich
  • Patent number: 6403624
    Abstract: The invention relates to polycyclic dihydrothiazoles and to their physiologically acceptable salts and physiologically functional derivatives. Compounds of formula I, in which the radicals are as defined above, and their physiologically acceptable salts and processes for their preparation are described. The compounds are suitable, for example, as anorectics.
    Type: Grant
    Filed: February 23, 2001
    Date of Patent: June 11, 2002
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Gerhard Jaehne, Matthias Gossel, Martin Bickel
  • Patent number: 6399638
    Abstract: The present invention relates to 12,13-position modified epothilone derivatives, methods of preparation of the derivatives and intermediates therefor.
    Type: Grant
    Filed: March 29, 1999
    Date of Patent: June 4, 2002
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gregory D. Vite, Soong-Hoon Kim, Gerhard Höfle
  • Publication number: 20020061913
    Abstract: The present invention provides compounds of formula (I): 1
    Type: Application
    Filed: June 22, 2001
    Publication date: May 23, 2002
    Inventors: Christopher John Urch, Terence Lewis, Raymond Leo Sunley, Roger Salmon, Christopher Richard Ayles Godfrey, Christopher Ian Brightwell, Matthew Brian Hotson
  • Publication number: 20020058658
    Abstract: The invention relates to polycyclic dihydrothiazoles and to their physiologically acceptable salts and physiologically functional derivatives.
    Type: Application
    Filed: February 23, 2001
    Publication date: May 16, 2002
    Inventors: Gerhard Jaehne, Matthias Gossel, Martin Bickel
  • Publication number: 20020058659
    Abstract: A novel class of imidazo heterocyclic compounds, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.
    Type: Application
    Filed: March 16, 2001
    Publication date: May 16, 2002
    Inventors: Knud Erik Andersen, Florencio Zaragiza Dorwald, Bernd Peschke, Ulla Grove Sidelmann, Klaus Rudolf, Dirk Stenkamp, Rudolf Hurnaus, Stephan Georg Muller, Bernd Krist, Birgitte Eriksen
  • Patent number: 6387919
    Abstract: Compounds of formula (I): wherein X is N, CH, CCF3, or C(C1-12 aliphatic); R4 is sulfonic acid, C1-12 aliphatic-sulfonyl, sulfonyl-C1-12 aliphatic, C1-12 aliphatic-sulfonyl-C1-6 aliphatic, C1-6 aliphatic-amino, R7-sulfonyl, R7 sulfonyl-C1-12 aliphatic, R7-aminosulfonyl, R7-aminosulfonyl-C1-12 aliphatic, R7-sulfonylamino, R7-sulfonylamino-C1-12 aliphatic, aminosulfonylamino, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl-C1-12 aliphatic, (R8)1-3-Arylamino, (R8)1-3-Arylsulfonyl, (R8)1-3-Aryl-aminosulfonyl, (R8)1-3-Aryl-sulfonylamino, Het-amino, Het-sulfonyl, Het-aminosulfonyl, aminoiminoamino, or aminoiminoaminosulfonyl, R5 is hydrogen; and further wherein R4 and R5 are optionally joined to form a fused ring, pharmaceutical formulations comprising them and their use in therapy, especially in the treatment of diseases mediated by CDK2 activity, such as alopecia induced by ca
    Type: Grant
    Filed: June 6, 2000
    Date of Patent: May 14, 2002
    Assignee: Glaxo Wellcome Inc.
    Inventors: Stephen Thomas Davis, Scott Howard Dickerson, Philip Anthony Harris, Robert Neil Hunter, III, Lee Frederick Kuyper, Michael Joseph Luzzio, James Marvin Veal, Duncan Herrick Walker
  • Patent number: 6387935
    Abstract: The invention relates to polycyclic dihydrothiazoles, and to their physiologically acceptable salts and physiologically functional derivatives. The compounds are according to formula I: in which the radicals have the meanings indicated, and their physiologically acceptable salts and process for their preparation are described. The compounds are suitable, for example, for use as anorectics.
    Type: Grant
    Filed: November 6, 2000
    Date of Patent: May 14, 2002
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Gerhard Jaehne, Matthias Gossel, Hans-Jochen Lang, Martin Bickel
  • Patent number: 6380200
    Abstract: This invention is directed to methods, pharmaceutical compositions and kits comprising an aldose reductase inhibitor (ARI), a prodrug thereof or a pharmaceutically acceptable salt of said ARI or said prodrug and selective serotonin reuptake inhibitor (SSRI), a prodrug thereof or a pharmaceutically acceptable salt of said SSRI or said prodrug. This invention further relates to methods of using those pharmaceutical compositions for the treatment of diabetic complications such as diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, myocardial infarction, cataracts and diabetic cardiomyopathy.
    Type: Grant
    Filed: December 1, 2000
    Date of Patent: April 30, 2002
    Assignee: Pfizer, Inc.
    Inventor: Banavara L. Mylari
  • Patent number: 6380258
    Abstract: A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
    Type: Grant
    Filed: June 24, 1999
    Date of Patent: April 30, 2002
    Assignee: G. D. Searle, L.L.C.
    Inventors: Louis J. Bedell, Joseph J. McDonald, Thomas E. Barta, Daniel P. Becker, Shashidhar N. Rao, John N. Freskos, Brent V. Mischke, Daniel P. Getman, Gary A. DeCrescenzo
  • Publication number: 20020049242
    Abstract: A compound represented by the formula: 1
    Type: Application
    Filed: May 3, 2001
    Publication date: April 25, 2002
    Inventors: Tsuneo Yasuma, Tsuneo Oda, Masatoshi Hazama, Shigehisa Taketomi
  • Patent number: 6369086
    Abstract: The present invention relates generally to novel substituted oxindole compounds and compositions. Such compounds and compositions have utility as pharmacological agents in treating diseases or conditions alleviated by the inhibition or antagonism of protein kinase activated signalling pathways. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit protein tyrosine kinase and protein serine/threonine kinase inhibition, and which are useful in inhibiting tumor growth via inhibition of such kinases as well as protecting a patient undergoing chemotherapy from chemotherapy induced alopecia.
    Type: Grant
    Filed: March 4, 1999
    Date of Patent: April 9, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: Stephen Thomas Davis, Scott Howard Dickerson, Philip Anthony Harris, Robert Neil Hunter, III, Lee Frederick Kuyper, Karen Elizabeth Lackey, Michael Joseph Luzzio, James Marvin Veal, Duncan Herrick Walker
  • Patent number: 6352987
    Abstract: 8,8a-Dihydroindeno[1,2-d]thiazole derivatives which carry in the 2-position a substituent having a sulfonamide structure or sulfone structure; processes for their preparation and their use as medicaments The invention relates to polycyclic dihydrothiazoles and to their physiologically acceptable salts and physiologically functional derivatives. Compounds of formula I, in which the radicals are as defined above, and their physiologically acceptable salts and processes for their preparation are described. The compounds are suitable, for example, as anorectics.
    Type: Grant
    Filed: February 26, 2001
    Date of Patent: March 5, 2002
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Gerhard Jaehne, Hans Jochen Lang, Matthias Gossel, Martin Bickel
  • Patent number: 6350747
    Abstract: The present invention relates generally to novel amine substituted oxindole compounds and compositions. Such compounds and compositions have utility as pharmacological agents in treating diseases or conditions alleviated by the inhibition or antagonism of protein kinase activated signalling pathways in general, and in particular in the pathological processes which involve aberrant cellular proliferation, such as tumor growth. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit protein tyrosine kinase and protein serine/threonine kinase inhibition, and which are useful in inhibiting tumor growth via inhibition of tumor-related angiogenesis.
    Type: Grant
    Filed: February 28, 2000
    Date of Patent: February 26, 2002
    Assignee: Glaxo Wellcome Inc.
    Inventors: Kimberley Caroline Glennon, Lee Frederick Kuyper, Karen Elizabeth Lackey, Robert Walton Mcnutt, Jr.
  • Publication number: 20020019425
    Abstract: The therapeutic use of temporary p53 inhibitors in the treatment of p53-mediated diseases, conditions, and injuries is disclosed.
    Type: Application
    Filed: September 6, 2001
    Publication date: February 14, 2002
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Andrei V. Gudkov, Pavel G. Komarov, Elena A. Komarova
  • Publication number: 20020006941
    Abstract: The therapeutic use of temporary p53 inhibitors in the treatment of p53-mediated diseases, conditions, and injuries is disclosed.
    Type: Application
    Filed: June 13, 2001
    Publication date: January 17, 2002
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Andrei V. Gudkov, Pavel G. Komarov, Elena A. Komarova
  • Patent number: 6329373
    Abstract: A compound of formula (I) wherein X is a —CONHOH group and the R groups are defined in the claims. The compounds are inhibitors of matrix metalloproteinases involved in tissue degradation and inhibitors of the release of tumour necrosis factor from cells.
    Type: Grant
    Filed: January 7, 2000
    Date of Patent: December 11, 2001
    Assignee: British Biotech Pharmaceuticals, Ltd.
    Inventors: Fionna Mitchell Martin, Christopher Norman Lewis, Mark Whittaker
  • Patent number: 6329407
    Abstract: The invention relates to the use of polycyclic thiazole systems and their physiologically tolerated salts and physiologically functional derivatives for the treatment of obesity. The treatment involves administration of a compound of formula I, in which the radicals have the stated meanings, and of their physiologically tolerated salts and physiologically functional derivatives.
    Type: Grant
    Filed: February 9, 2000
    Date of Patent: December 11, 2001
    Assignee: AventisPharma Deutschland GmbH
    Inventors: Gerhard Jähne, Karl Geisen, Hans-Jochen Lang, Martin Bickel
  • Publication number: 20010044437
    Abstract: Disclosed are methods of reducing serum uric acid levels, the methods comprising administration of substituted indolealkanoic acids to patients in need of such treatment. Also disclosed are such compounds useful in the treatment of gout and related diseases. Also disclosed are pharmaceutical compositions containing the compounds.
    Type: Application
    Filed: January 11, 2001
    Publication date: November 22, 2001
    Inventors: Dale Robinson, Marcele Boyd
  • Publication number: 20010041715
    Abstract: This invention provides substituted compounds of the general formulae: 1
    Type: Application
    Filed: March 2, 2001
    Publication date: November 15, 2001
    Inventors: Michael S. Malamas, Richard E. McDevitt, Folake O. Adebayo
  • Publication number: 20010039278
    Abstract: 8,8a-Dihydroindeno[1,2-d]thiazole derivatives which carry in the 2-position a substituent having a sulfonamide structure or sulfone structure; processes for their preparation and their use as medicaments
    Type: Application
    Filed: February 26, 2001
    Publication date: November 8, 2001
    Inventors: Gerhard Jaehne, Hans Jochen Lang, Matthias Gossel, Martin Bickel
  • Publication number: 20010031752
    Abstract: The invention relates to substituted 8,8a-dihydro-3aH-indeno[1,2-d]thiazoles and to their physiologically acceptable salts and physiologically functional derivatives.
    Type: Application
    Filed: February 23, 2001
    Publication date: October 18, 2001
    Inventors: Gerhard Jaehne, Hans-Jochen Lang, Matthias Gossel, Martin Bickel
  • Patent number: 6303643
    Abstract: This invention is directed to indole and benzothiazole compounds which are selective for cloned human alpha 2 receptors. This invention is also related to uses of these compounds for any indication where use of an alpha 2 agonist may be appropriate. Specifically, this includes use as analgesic, sedative and anaesthetic agents. In addition, this invention includes using such compounds for lowering intraocular pressure, presbyopia, treating migraine, hypertension, alcohol withdrawal, drug addiction, rheumatoid arthritis, ischemic pain, spasticity, diarrhea, nasal decongestion, urinary incontinence as well as for use as cognition enhancers and ocular vasoconstriction agents. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: October 17, 2000
    Date of Patent: October 16, 2001
    Assignee: Synaptic Pharmaceutical Corporation
    Inventors: Yoon T. Jeon, Charles Gluchowski
  • Patent number: 6291486
    Abstract: Polycyclic dihydrothiazoles, processes for their preparation, and their pharmaceutical uses are provided. Preferred compounds are represented by the formula I wherein the radicals may have various meanings. The compounds are particularly useful as anorectics.
    Type: Grant
    Filed: June 27, 2000
    Date of Patent: September 18, 2001
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Gerhard Jaehne, Heiner Glombik, Karl Geisen, Martin Bickel
  • Patent number: 6291494
    Abstract: The invention relates to 2-aminothiazol-fused 2-aminoindans and 2-aminotetralins having general formula (1): wherein R1 and R2, which may be identical or different, are selected from the group consisting of a hydrogen atom, alkyl or haloalkyl groups of 1 to 7 carbon atoms, (alkyl)cycloalkyl groups of 3 to 7 carbon atoms, alkenyl or alkynyl groups of 3 to 6 carbon atoms, arylalkyl having 1 to 3 carbon atoms in the alkyl moiety, while the aryl nucleus may be substituted; and n and m are 1 or 2; and the enantiomers and the acid addition salts thereof, pharmaceutical compositions containing them and their use in the preparation of medicaments having an effect on the dopaminergic system of the central nervous system and/or the circulation.
    Type: Grant
    Filed: February 9, 2001
    Date of Patent: September 18, 2001
    Inventors: Håkan Vilhelm Wikström, Per Erik Andrén, Per Arvid Emil Carlsson, Durk Dijkstra, Lars Gunne, Leonard Alexander Van Vliet
  • Patent number: 6288094
    Abstract: The invention relates to polycyclic thiazolidin-2-ylidene amines and their physiologically tolerated salts and physiologically functional derivatives. Polycyclic thiazolidin-2-ylidene amines of the formula I, in which the radicals have the stated meanings, and their physiologically tolerated salts and processes for their preparation are described. The compounds are suitable, for example as anorectics and in the treatment or prophylaxis of type II diabetes.
    Type: Grant
    Filed: January 31, 2001
    Date of Patent: September 11, 2001
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Gerhard Jähne, Karl Geisen, Hans-Jochen Lang, Martin Bickel
  • Patent number: 6288093
    Abstract: The invention relates to polycyclic thiazolidin-2-ylidene amines and their physiologically tolerated salts and physiologically functional derivatives. Polycyclic thiazolidin-2-ylidene amines of the formula I, in which the radicals have the stated meanings, and their physiologically tolerated salts and processes for their preparation are described. The compounds are suitable, for example as anorectics and in the treatment or prophylaxis of type II diabetes.
    Type: Grant
    Filed: October 27, 2000
    Date of Patent: September 11, 2001
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Gerhard Jähne, Karl Geisen, Hans-Jochen Lang, Martin Bickel
  • Publication number: 20010011096
    Abstract: The invention relates to polycyclic thiazolidin-2-ylidene amines and their physiologically tolerated salts and physiologically functional derivatives.
    Type: Application
    Filed: January 31, 2001
    Publication date: August 2, 2001
    Inventors: Gerhard Jahne, Karl Geisen, Hans-Jochen Lang, Martin Bickel
  • Patent number: 6268391
    Abstract: Compounds of general formula (I) wherein: R1 is H or optionally joined with R2 to form a fused ring selected from the group consisting of five to ten membered aryl, heteroaryl or heterocyclyl rings, R2 and R3 are independently H, HET, aryl, C1-12 aliphatic, CN, NO2, halogen, R10, —OR10, —SR10, —S(O)R10, —SO2R10, —NR10R11, —NR11R12, —NR12COR11, —NR12CO2R11, —NR12CONR11R12, —NO12SO2R11, —NR12C(NR 12)NHR11, —COR11, —CO2R11, —CONR12R11, —SO2NR12R11, —OCONR12R11, C(NR12)NR12R11, R6 and R7 are independently halogen, CN, NO2, —CONR10R11, —SO2NR10R11, —NR10R11, or —OR11, where R10 and R11 are as defined below; R8 is OH, NHSO2R12 or NHCOCF3; and their use in therapy, especially in the treatment of disorders mediated by cRaf1 kinase.
    Type: Grant
    Filed: April 7, 2000
    Date of Patent: July 31, 2001
    Assignee: Glaxo Wellcome Inc.
    Inventors: Scott Howard Dickerson, Philip Anthony Harris, Robert Neil Hunter, III, David Kendall Jung, Karen Elizabeth Lackey, Robert Walton McNutt, Jr., Michael Robert Peel, James Marvin Veal
  • Publication number: 20010008903
    Abstract: Compounds of formula I 1
    Type: Application
    Filed: December 27, 2000
    Publication date: July 19, 2001
    Inventors: Alan Martin Birch, Paul Anthony Bradley
  • Patent number: 6262095
    Abstract: The invention concerns the therapeutic use of tricyclic salts and their pharmaceutically acceptable salts having the general formula: in which: A is either a sulfur atom, an oxygen atom, or an R3N radical where R3 is a hydrogen atom, a C1-C5 alkyl radical, or a substituted or unsubstituted aromatic ring, or a substituted or unsubstituted heteroaromatic ring. R1 is either a C1-C5 alkyl radical, or an R4NH radical where R4 is a hydrogen atom, a C1-C5 alkyl radical, or a substituted or unsubstituted aromatic ring, or a substituted or unsubstituted heteroaromatic ring, or an aromatic ring that may or may not be substituted by one or more acceptor or donor groups, or a heteroaromatic ring having one or more heteroatoms, which may or may not be substituted by acceptor or donor groups.
    Type: Grant
    Filed: October 14, 1998
    Date of Patent: July 17, 2001
    Assignee: Laboratoire Innothera
    Inventors: Odile Boutherin-Falson, Stéphanie Desquand-Billiald, Anita Favrou, Michel Finet, Olivier Tembo, Jean-Luc Torregrosa, Sylvie Yannic-Arnoult, Florence Domagala-Le Marquer
  • Patent number: 6251922
    Abstract: The invention relates to polycyclic 2-aminothiazole systems and their physiologically tolerated salts and physiologically functional derivatives. The polycyclic 2-aminothiazole systems are according to formula I, in which the radicals have the stated meanings, and their physiologically tolerated salts and processes for their preparation are described. The compounds are suitable, for example, as anorectics.
    Type: Grant
    Filed: February 10, 2000
    Date of Patent: June 26, 2001
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Gerhard Jähne, Karl Geisen, Hans-Jochen Lang, Martin Bickel
  • Patent number: 6248755
    Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6, R14 and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
    Type: Grant
    Filed: April 4, 2000
    Date of Patent: June 19, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Kevin Chapman, Jeffrey Hale, Dooseop Kim, Christopher Lynch, Shrenik Shah, Kothandaraman Shankaran, Dong-Ming Shen, Christopher Willoughby, Malcolm MacCoss, Sander G. Mills, Jennifer L. Loebach, Ravindra N. Guthikonda
  • Patent number: 6248766
    Abstract: A compound of the formula: wherein R1 is H or a substituent; m is 1-3; Ar is an aromatic group which may be substituted; X is a bond or a divalent straight-chain group having 1-6 atoms which may be substituted; Y is —S—, —O—, or —N(R2— (R2 is H or a substituent group), Z is —N═ or —C(R3)═ (R3 is H or a hydrocarbon group), ring A is a benzene ring; ring B is a 5- to 7-membered ring which may be substituted, or a salt thereof is useful for eliciting a prostaglandin I2 receptor agonistic effect.
    Type: Grant
    Filed: March 9, 1999
    Date of Patent: June 19, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shigenori Ohkawa, Masaki Setoh, Zen-ichi Terashita
  • Patent number: 6235763
    Abstract: The invention relates to polycyclc 2-aminodihydrothiazole systems and their physiologically tolerated salts and physiologically functional derivatives. Compounds of the formula I, in which the radicals have the stated meanings, and their physiologically tolerated salts and processes for their preparation are described. The compounds are suitable, for example, as anorectics.
    Type: Grant
    Filed: February 8, 2000
    Date of Patent: May 22, 2001
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Gerhard Jaehne, Karl Geisen, Hans-Jochen Lang, Martin Bickel
  • Patent number: 6207689
    Abstract: The invention relates to polycyclic thiazolidin-2-ylidene amines and their physiologically tolerated salts and physiologically functional derivatives. Polycyclic thiazolidin-2-ylidene amines of the formula I, in which the radicals have the stated meanings, and their physiologically tolerated salts and processes for their preparation are described. The compounds are suitable, for example as anorectics and in the treatment or prophylaxis of type II diabetes.
    Type: Grant
    Filed: February 9, 2000
    Date of Patent: March 27, 2001
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Gerhard Jähne, Karl Geisen, Hans-Jochen Lang, Martin Bickel
  • Patent number: 6197804
    Abstract: Disclosed are novel 4,5-azolo-oxindoles having the formula These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. Thus, these compounds and their pharmaceutically acceptable salts, and *prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing these compounds, and methods for the treatment and/or prevention of cancer, particularly in the treatment or control of solid tumors using these compounds, as well as intermediates useful in the preparation of compounds of formula I.
    Type: Grant
    Filed: May 16, 2000
    Date of Patent: March 6, 2001
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kin-Chun Luk, Steven Gregory Mischke
  • Patent number: 6187801
    Abstract: The invention relates to polycyclic thiazole systems and their physiologically tolerated salts and physiologically functional derivatives. Compounds of the formula I, in which the radicals have the stated meanings, and their physiologically tolerated salts and processes for their preparation are described. The compounds are suitable, for example, as anorectics.
    Type: Grant
    Filed: February 10, 2000
    Date of Patent: February 13, 2001
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Gerhard Jähne, Karl Geisen, Hans-Jochen Lang, Martin Bickel
  • Patent number: 6187800
    Abstract: A method for treating or preventing mastitis in mammals is disclosed. The method contemplates the intramammary injection or dipping the teat with micrococcin antibiotics, preferably micrococcin P1 or P2, which do not interfere with the production of cheese and yoghurt using milk from treated animals. Hydrophobic antibiotics such as micrococcin P1 or P2 can be administered prior to infection to effectively suppress the rate, severity, and duration of subsequent bacterial infection, or can be administered subsequent to infection to effectively treat mastitis.
    Type: Grant
    Filed: December 18, 1998
    Date of Patent: February 13, 2001
    Assignee: Novartis Animal Health U.S., Inc.
    Inventors: Bruno Suri, Catherine Georges, John Edmondson Peel
  • Patent number: 6159996
    Abstract: Polycyclic thiazolidin-2-ylidene amines and their physiologically tolerable salts and physiologically functional derivatives of the formula I ##STR1## in which the radicals have the meanings indicated, and their physiologically tolerable salts and a process for their preparation are described. The compounds are suitable, for example, as anorectics.
    Type: Grant
    Filed: July 12, 1999
    Date of Patent: December 12, 2000
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Gerhard Jaehne, Karl Geisen, Hans Jochen Lang
  • Patent number: 6153634
    Abstract: Disclosed are novel 4,5-azolo-oxindoles having the formula ##STR1## These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. Thus, these compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing these compounds, and methods for the treatment and/or prevention of cancer, particularly in the treatment or control of solid tumors using these compounds, as well as intermediates useful in the preparation of compounds of formula I.
    Type: Grant
    Filed: December 15, 1999
    Date of Patent: November 28, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kin-Chun Luk, Christophe Michoud, Steven Gregory Mischke
  • Patent number: 6130236
    Abstract: The present invention relates to novel crop-protecting active ingredient mixtures having synergistically enhanced action, comprising at least two active ingredient components together with a suitable carrier, wherein component I is1-[[2-(2,4-dichorophenyl)-4-propyl-1,3-dioxolan-2-yl]methyl]-1H-1,2,4-triaz ole ("propiconazole")and component II is5-methyl-1,2,4-triazolo[3,4-b][1,3]benzothiazole ("tricyclazole");or in each case a salt or metal complex thereof.
    Type: Grant
    Filed: October 13, 1998
    Date of Patent: October 10, 2000
    Assignee: Novartis Finance Corporation
    Inventors: Gertrude Knauf-Beiter, Jurg Speich