Tricyclo Ring System Having The Thiazole Ring As One Of The Cyclos Patents (Class 548/150)
  • Patent number: 7485655
    Abstract: The present invention relates generally to a class of 2-aminothiazole derivatives which have recently been identified as allosteric enhancers of the A1? adenosine receptor. These compounds, and therapeutic compositions containing them, are useful for treating conditions in which activation of the A1? adenosine receptor would be beneficial, for example, those conditions in which stimulation of angiogenesis would improve blood flow to ischemic tissues.
    Type: Grant
    Filed: January 16, 2003
    Date of Patent: February 3, 2009
    Assignee: University of Virginia Patent Foundation
    Inventors: Joel Linden, Timothy L. MacDonald, Lauren Murphree, Mahendra D. Chordia
  • Patent number: 7407977
    Abstract: There are presented compounds of the formula or a pharmaceutically acceptable salt thereof, which are useful in the treatment of diabetes, diabetic retinopathy, asthma and diarrhea.
    Type: Grant
    Filed: July 29, 2005
    Date of Patent: August 5, 2008
    Assignee: Hoffman-La Roche Inc.
    Inventors: Jianping Cai, Adrian Wai-Hing, Fariborz Firooznia, Kevin Richard Guertin, Lida Qi
  • Patent number: 7338720
    Abstract: An organic electroluminescent (EL) device which uses, as a luminescence-assisting agent, a novel coumarin derivative with a specific structure. The coumarin derivative effectively accelerates in such an organic EL device the transfer of excited energy in a host compound to a guest compound. Thus, the coumarin derivative affords the organic EL device which is superior in a color purity, luminescent efficiency and life expectancy when used in combination with appropriate host and guest compounds.
    Type: Grant
    Filed: April 23, 2002
    Date of Patent: March 4, 2008
    Assignee: Kabushiki Kaisha Toyota Jidoshokki
    Inventors: Makoto Satsuki, Natsuko Ishida, Sadaharu Suga, Hisayoshi Fujikawa, Yasunori Taga, Satoshi Nakagawa, Takanori Murasaki, Yoshifumi Kato
  • Publication number: 20080045578
    Abstract: Compounds of the following structure are described: wherein R1-R6, R16, m, V, W, X, Y, and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.
    Type: Application
    Filed: August 13, 2007
    Publication date: February 21, 2008
    Applicant: Wyeth
    Inventors: Thomas Joseph Commons, Andrew Fensome, Gavin David Heffernan, Casey Cameron McComas, Richard Page Woodworth, Michael Byron Webb, Michael Anthony Marella, Edward George Melenski, Ronald Charles Bernotas
  • Patent number: 7326258
    Abstract: The present invention relates to a cosmetic composition for dyeing keratin fibres, in particular human keratin fibres such as the hair, comprising, in a suitable dyeing medium, at least one hydroxyalkyl compound of general formula (I) below: and at least one cosmetic adjuvant according to the invention. The present invention also relates to a process for dyeing keratin fibres using these compositions based on hydroxyalkyl compounds, to a device with compartments and to the use of these compounds in hair dyeing.
    Type: Grant
    Filed: June 20, 2005
    Date of Patent: February 5, 2008
    Assignee: L'Oreal S.A.
    Inventor: Alain Lagrange
  • Patent number: 7252892
    Abstract: An organic electroluminescent (EL) device which contains a novel coumarin derivative composed of a coumarin ring, a naphthalene ring with one or more hydrocarbon groups, and a five-membered hetero ring condensed with the naphthalene ring so as to give an electronic resonance through the coumarin and naphthalene rings. The coumarin derivative emits a visible luminescence with a satisfactory color purity, which consistently continues over a long period of time even at an elevated temperature when used in such an organic device.
    Type: Grant
    Filed: April 23, 2002
    Date of Patent: August 7, 2007
    Assignees: Kabushiki Kaisha Hayashibara Seibutsu Kagaku Kenkyujo, Kabushiki Kaisha Toyota Jidoshokki
    Inventors: Makoto Satsuki, Natsuko Ishida, Sadaharu Suga, Hisayoshi Fujikawa, Yasunori Taga
  • Patent number: 7132436
    Abstract: The present invention relates to compounds with the formula (I) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.
    Type: Grant
    Filed: May 22, 2001
    Date of Patent: November 7, 2006
    Assignee: Biovitrum AB
    Inventors: Guido Kurz, Marianne Nilsson
  • Patent number: 7101533
    Abstract: Disclosed is an agent for inducing receptor potential, which comprises an organic dye compound capable of inducing/evoking receptor potential in response to photostimulation in the optic nerve, wherein the organic dye compound is a polymethine organic dye compound. Also disclosed is a substituent material for the retina comprising the agent.
    Type: Grant
    Filed: September 30, 2003
    Date of Patent: September 5, 2006
    Assignee: Kabushiki Kaisha Hayashibara Seibutsu Kagaku Kenkyujo
    Inventors: Toshihiko Matsuo, Yasufumi Dan-Oh, Sadaharu Suga
  • Patent number: 7022721
    Abstract: In one embodiment, the present invention relates to compounds and compositions including pharmaceutical compositions containing the compounds and associated methods that uncouple sugar-mediated coupling of proteins, lipids, nucleic acids, and other biomaterials, and any combination thereof. In another embodiment, the compositions and associated methods have utility in vivo to reduce the deleterious effects of sugar-mediated coupling processes in an organism, when the organism is exposed to the compound or composition internally, by ingestion, transdermal application, or other means. In yet another embodiment, the compositions and associated methods are useful for the ex-vivo treatment of organs, cells and tissues and external treatment of hair, nails and skin to rejuvenate them by changing deformability and increase the tissue diffusion coefficient. In a further embodiment, the present invention relates to novel compounds and pharmaceutical compositions.
    Type: Grant
    Filed: March 8, 2004
    Date of Patent: April 4, 2006
    Inventors: Peter C Ulrich, Sheng Ding Fang, Michael L Brines, Qiao-Wen Xie, Anthony Cerami
  • Patent number: 7008798
    Abstract: The present invention pertains to luminescent dyes and methods for covalently attaching the dyes to a component or mixture of components so that the components may be detected and/or quantified by luminescence detection methods. The dyes are cyanine and cyanine-type dyes that contain or are derivatized to contain a reactive group. The reactive group is covalently reactive with amine, hydroxy and/or sulfhydryl groups on the component so that the dye can be covalently bound to the component. In addition, the dyes are preferably soluble in aqueous or other medium in which the component is contained. The components to be labeled can be either biological materials, such as antibodies, antigens, peptides, nucleotides, hormones, drugs, or non-biological materials, such as polymers, glass, or other surfaces. Any luminescent or light absorbing detecting step can be employed in the method of the invention.
    Type: Grant
    Filed: March 22, 2002
    Date of Patent: March 7, 2006
    Assignee: Carnegie Mellon University
    Inventor: Alan S. Waggoner
  • Patent number: 6995262
    Abstract: The invention relates to a novel polymethine dyes containing at least one acylsulfonamido group of the formula (I) in which n, Y, A and R have the meaning given in the claims, and at least one compound of the formulae (a) to (n) given in the claims. The polymethine dyes according to the invention are suitable for use as dyes and/or labels, in particular for staining or labeling biomolecules.
    Type: Grant
    Filed: July 24, 2000
    Date of Patent: February 7, 2006
    Assignee: Bayer CropScience AG
    Inventors: Geert Deroover, Michael Missfeldt, Lydia Simon
  • Patent number: 6989275
    Abstract: The present invention pertains to luminescent dyes and methods for covalently attaching the dyes to a component or mixture of components so that the components may be detected and/or quantified by luminescence detection methods. The dyes are cyanine and cyanine-type dyes that contain or are derivatized to contain a reactive group. The reactive group is covalently reactive with amine, hydroxy and/or sulfhydryl groups on the component so that the dye can be covalently bound to the component. In addition, the dyes are preferably soluble in aqueous or other medium in which the component is contained. The components to be labeled can be either biological materials, such as antibodies, antigens, peptides, nucleotides, hormones, drugs, or non-biological materials, such as polymers, glass, or other surfaces. Any luminescent or light absorbing detecting step can be employed in the method of the invention.
    Type: Grant
    Filed: March 22, 2002
    Date of Patent: January 24, 2006
    Assignee: Carnegie Mellon University
    Inventor: Alan S. Waggoner
  • Patent number: 6956032
    Abstract: The present invention pertains to luminescent dyes and methods for covalently attaching the dyes to a component or mixture of components so that the components may be detected and/or quantified by luminescence detection methods. The dyes are cyanine and cyanine-type dyes that contain or are derivatized to contain a reactive group. The reactive group is covalently reactive with amine, hydroxy and/or sulfhydryl groups on the component so that the dye can be covalently bound to the component. In addition, the dyes are preferably soluble in aqueous or other medium in which the component is contained. The components to be labeled can be either biological materials, such as antibodies, antigens, peptides, nucleotides, hormones, drugs, or non-biological materials, such as polymers, glass, or other surfaces. Any luminescent or light absorbing detecting step can be employed in the method of the invention.
    Type: Grant
    Filed: December 19, 2000
    Date of Patent: October 18, 2005
    Assignee: Carnegie Mellon University
    Inventor: Alan S. Waggoner
  • Patent number: 6887868
    Abstract: The present invention provides compounds of Formula (I): wherein: R1, R2, R3, R4, R5, R6 R7, R8, n, m, and X have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula (I). The compounds are 5-HT ligands and are useful for treating diseases wherein modulation of 5-HT activity is desired.
    Type: Grant
    Filed: September 19, 2002
    Date of Patent: May 3, 2005
    Assignee: Pharmacia & Upjohn Company
    Inventor: Jian-Min Fu
  • Publication number: 20040180934
    Abstract: Dihydropyrroloindoles and tetrahydropyridoindoles are prostaglandin receptor antagonists useful for the treatment of prostaglandin-mediated diseases such as allergic rhinitis, nasal congestion and asthma.
    Type: Application
    Filed: October 15, 2003
    Publication date: September 16, 2004
    Inventors: Zhaoyin Wang, Christian Beaulieu, Claude Dufresne, Daniel Guay, Yves LeBlanc
  • Patent number: 6777557
    Abstract: In one embodiment, the present invention relates to compounds and compositions including pharmaceutical compositions containing the compounds and associated methods that uncouple sugar-mediated coupling of proteins, lipids, nucleic acids, and other biomaterials, and any combination thereof. In another embodiment, the compositions and associated methods have utility in vivo to reduce the deleterious effects of sugar-mediated coupling processes in an organism, when the organism is exposed to the compound or composition internally, by ingestion, transdermal application, or other means. In yet another embodiment, the compositions and associated methods are useful for the ex-vivo treatment of organs, cells and tissues and external treatment of hair, nails and skin to rejuvenate them by changing deformability and increase the tissue diffusion coefficient. In a further embodiment, the present invention relates to novel compounds and pharmaceutical compositions.
    Type: Grant
    Filed: February 7, 2002
    Date of Patent: August 17, 2004
    Inventors: Peter C Ulrich, Sheng Ding Fang, Michael L Brines, Qiao-Wen Xie, Anthony Cerami
  • Publication number: 20040141920
    Abstract: Cyanine dye bioconjugates useful for diagnostic imaging and therapy are disclosed. The conjugates include several cyanine dyes with a variety of bis- and tetrakis (carboxylic acid) homologs. The compounds may be conjugated to bioactive peptides, carbohydrates, hormones, drugs, or other bioactive agents. The small size of the compounds allows more favorable delivery to tumor cells as compared to larger molecular weight imaging agents. The various dyes are useful over the range of 350 to 1300 nm, the exact range being dependent upon the particular dye. The use of dimethylsulfoxide helps to maintain the fluorescence of the compounds. The inventive compounds are useful for diagnostic imaging and therapy, in endoscopic applications for the detection of tumors and other abnormalities, for localized therapy, for photoacoustic tumor imaging, detection and therapy, and for sonofluoresence tumor imaging, detection and therapy.
    Type: Application
    Filed: September 3, 2003
    Publication date: July 22, 2004
    Applicant: MALLINCKRODT INC.
    Inventors: Samuel I. Achilefu, Raghavan Rajagopalan, Richard B. Dorshow, Joseph E. Bugaj, Muthunadar P. Periasamy
  • Patent number: 6759428
    Abstract: Compounds of the formula (I) wherein m, n, R1, R2, R3, R4, R5 and R6 are as described herein, together with methods for making the compounds and using the compounds for treatment of diseases or conditions mediated by Cathepsin K.
    Type: Grant
    Filed: June 2, 2003
    Date of Patent: July 6, 2004
    Assignee: Roche Palo Alto LLC
    Inventors: Joe Timothy Bamberg, Tobias Gabriel, Nancy Elisabeth Krauss, Taraneh Mirzadegan, Wylie Solang Palmer, David Bernard Smith
  • Publication number: 20040127526
    Abstract: Antiatherosclerotic agents are provided which are represented by Formulas I or II: 1
    Type: Application
    Filed: December 10, 2003
    Publication date: July 1, 2004
    Applicant: Wyeth
    Inventors: Robert J. Steffan, Amedeo A. Failli
  • Patent number: 6743785
    Abstract: The present invention provides selective kinase inhibitors of formula (I).
    Type: Grant
    Filed: May 21, 2002
    Date of Patent: June 1, 2004
    Assignee: Eli Lilly and Company
    Inventors: Rima Salim Al-Awar, Kyle Andrew Hecker, Jianping Huang, Sajan Joseph, James Edward Ray, Philip Parker Waid
  • Patent number: 6730793
    Abstract: Provided are chromophores of the formula Q—(—L—Z)x, wherein x is 2 or 3, wherein Q is selected from the group consisting of wherein L is wherein R is an alkyl group having 1 to 20 carbon atoms, and wherein Z is selected from the group consisting of
    Type: Grant
    Filed: June 13, 2002
    Date of Patent: May 4, 2004
    Assignee: The United States of America as represented by the Secretary of the Air Force
    Inventors: Ramamurthi Kannan, Loon-Seng Tan, Bruce A. Reinhardt, Richard A. Vaia
  • Publication number: 20040053923
    Abstract: This invention relates to compounds represented by the general formula [I] 1
    Type: Application
    Filed: April 8, 2003
    Publication date: March 18, 2004
    Applicant: Banyu Pharmaceutical Co., Ltd.
    Inventors: Toshio Nagase, Tomoharu Iino, Yoshiyuki Sato, Teruyuki Nishimura, Jun-Ichi Eiki
  • Publication number: 20040039197
    Abstract: The invention relates to novel, substituted, fused indole and heteroindole derivatives of the general formula I 1
    Type: Application
    Filed: August 30, 2002
    Publication date: February 26, 2004
    Inventors: Heinz Weinberger, Thomas Beckers, Mathias Schmidt, Silke Baasner, Bernd Nickel
  • Patent number: 6689777
    Abstract: The present invention is directed to substituted naphthothiazolium, aromatic guanylhydrazones, and other compounds and compositions with anti-malarial activity useful for the treatment and prophylaxis of malaria. The compounds are provided for the treatment of malaria or the sequelae of malarial infection, for depolymerizing malaria pigment (hemozoin), and for ameliorating the adverse effects of hemozoin on host cells.
    Type: Grant
    Filed: October 23, 2002
    Date of Patent: February 10, 2004
    Assignee: Kenneth S. Warren Institute
    Inventors: Peter C. Ulrich, Anthony Cerami
  • Patent number: 6664283
    Abstract: This invention relates to pharmaceuticals for neuropathic pains comprising an mGluR1 receptor antagonist for systemic administration. Drugs efficacious in treating various neuropathic pain can be provided by the invention.
    Type: Grant
    Filed: May 15, 2002
    Date of Patent: December 16, 2003
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Masamichi Okada, Yukinori Nagakura, Tetsuo Kiso, Takashi Toya, Satoshi Hayashibe
  • Publication number: 20030191164
    Abstract: Provided is a pharmaceutical composition containing a propane-1,3-dione derivative as the active ingredient, particularly a GnRH receptor antagonist. Also, provided is a propane-1,3-dione derivative having a GnRH antagonistic effect.
    Type: Application
    Filed: December 19, 2002
    Publication date: October 9, 2003
    Inventors: Masaaki Hirano, Eiji Kawaminami, Akira Toyoshima, Hiroyuki Moritomo, Norio Seki, Ryutaro Wakayama, Minoru Okada, Toshiyuki Kusayama
  • Patent number: 6624186
    Abstract: The present invention relates to ion channel modulating agents. More particularly, the present invention relates to a particular class of chemical compounds that has proven useful as modulators of SKCa, IKCa and BKCa channels. In further aspects, the present invention relates to the use of these SK/IK/BK channel modulating agents for the manufacture of medicaments, and pharmaceutical compositions comprising the SK/IK/BK channel modulating agents. The SK/IK/BK channel modulating agents of the invention are useful for the treatment or alleviation of diseases and conditions associated with the SK/IK/BK channels.
    Type: Grant
    Filed: May 15, 2001
    Date of Patent: September 23, 2003
    Assignee: Neurosearch A/S
    Inventors: Lene Teuber, Palle Christophersen, Dorte Strobaek, Bo Skaaning Jensen
  • Patent number: 6608098
    Abstract: This invention relates to compounds represented by the general formula [I]   wherein, R represents an azido group, etc., R1 and R2 are the same or different and represent hydrogen atoms, etc., R3 and R4 are the same or different and represent hydrogen atoms, etc., X1 represents an oxygen atom, etc., X2 represents an oxygen atom, etc., Y represents an oxygen atom, etc., and Z represents a condensed aryl group, etc., or a pharmaceutically acceptable salt thereof, preparation processes thereof, and an agent for treating diabetes, a prophylactic agent for chronic complications of diabetes or a drug against obesity, containing, as an effective ingredient, the compound or the pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 25, 2002
    Date of Patent: August 19, 2003
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Toshio Nagase, Tomoharu Iino, Yoshiyuki Sato, Teruyuki Nishimura, Jun-ichi Eiki
  • Publication number: 20030125361
    Abstract: The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.
    Type: Application
    Filed: September 19, 2002
    Publication date: July 3, 2003
    Inventors: Michael Clare, Lifeng Geng, Gunnar J. Hanson, He Huang, Donna M. Iula, Shuyuan Liao, Michael A. Stealy, Richard M. Weier, Suzanne Metz, Michael L. Vazquez
  • Publication number: 20030091931
    Abstract: An optical recording medium having an organic dye layer as a recording layer on a substrate, wherein at least one benzobisazole-based compound represented by a general formula (1) is contained in the recording layer: 1
    Type: Application
    Filed: June 28, 2002
    Publication date: May 15, 2003
    Inventors: Akira Ogiso, Shinobu Inoue, Hisashi Tsukahara, Taizo Nishimoto, Tsutami Misawa
  • Publication number: 20030087909
    Abstract: This invention relates generally to a novel class of fused heterocyclic compounds of the Formula (I) or Formula (II): 1
    Type: Application
    Filed: April 8, 2002
    Publication date: May 8, 2003
    Inventors: Irina C. Jacobson, Mimi L. Quan, Ruth R. Wexler
  • Publication number: 20030013747
    Abstract: Antiatherosclerotic agents are provided which are represented by Formulas I or II: 1
    Type: Application
    Filed: August 6, 2002
    Publication date: January 16, 2003
    Applicant: Wyeth
    Inventors: Robert J. Steffan, Amedeo A. Failli
  • Publication number: 20020156288
    Abstract: A symmetric cyanine of the formula: 1
    Type: Application
    Filed: January 2, 2002
    Publication date: October 24, 2002
    Inventors: Giuseppe Caputo, Leopoldo Della Ciana
  • Publication number: 20020156287
    Abstract: The present invention relates to new bromo- and chlorothiazolium salts of the formula (I) 1
    Type: Application
    Filed: December 18, 2001
    Publication date: October 24, 2002
    Inventors: Joachim Rudolph, Ralf Wischnat
  • Patent number: 6458908
    Abstract: A sulfur-containing unsaturated carboxylate compound comprising a sulfur-containing substituent and at least two &agr;,&bgr;-unsaturated carboxylic acid residues, which are each attached to a secondary or tertiary carbon atom via an oxygen atom; a polymerizable composition comprising the sulfur-containing unsaturated carboxylate compound; a cured product prepared by polymerizing the polymerizable composition; an optical component consisting of the cured product; and novel intermediate compounds for preparation of the above carboxylate.
    Type: Grant
    Filed: May 31, 2000
    Date of Patent: October 1, 2002
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Masao Imai, Kenichi Sugimoto, Kenichi Fujii, Atsuo Otsuji, Tadashi Ohkuma, Masatoshi Takagi, Rihoko Suzuki, Keisuke Takuma
  • 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: 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: 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
  • 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
  • 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: 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: 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
  • Publication number: 20020006944
    Abstract: A compound of the formula: 1
    Type: Application
    Filed: March 7, 2001
    Publication date: January 17, 2002
    Inventors: Shigenori Ohkawa, Masaki Setoh, Zen-ichi Terashita
  • 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: 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
  • 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: 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: 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