Plural Ring Hetero Atoms In The Tricyclo Ring System Patents (Class 546/80)
  • Publication number: 20030186970
    Abstract: Compounds, pharmaceutical compositions, and methods for modulating processes mediated by steroid receptors. In particular, preparation and methods of use of non-steroidal compounds and compositions that are agonists, partial agonists, and antagonists for the androgen receptor (AR) are described. Further, described are the methods of making and use of critical intermediates including a stereoselective synthetic route to intermediates for the AR modulators.
    Type: Application
    Filed: September 9, 2002
    Publication date: October 2, 2003
    Inventors: Robert Higuchi, Kristen L. Arienti, Mani Neelakandha, Barbara Pio, Lin Zhi, Penghui Chen, Thomas R. Caferro
  • Patent number: 6627636
    Abstract: Compounds of the following structure are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids such as lowering LDL cholesterol and/or increasing HDl cholesterol, and treating hyperlipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis and pharmaceutically acceptable salts thereof, wherein X is O, S, SO, SO2 or NR7; Z is n is 0 or 1; R1 and R2 are the same or different and are independently selected from alkyl, arylalkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, heteroaryl or cycloheteroalkyl; and R3 to R10 are as defined herein.
    Type: Grant
    Filed: December 4, 2001
    Date of Patent: September 30, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventor: Jeffrey A. Robl
  • Publication number: 20030149069
    Abstract: The present invention provides methods for synthesizing novel tetrahydroquinoline derivatives that are useful for cancer chemotherapy and anti-viral applications. The present invention provides compounds useful for cancer chemotherapy and methods for the preparation of these compounds. The present invention also includes cancer chemotherapy methods.
    Type: Application
    Filed: September 24, 2002
    Publication date: August 7, 2003
    Inventors: Chao-Jun Li, Jianheng Zhang
  • Patent number: 6593335
    Abstract: Compounds having the formula I: are useful in treating diseases prevented by or ameliorated with potassium channel openers. Also disclosed are potassium channel opening compositions and a method of opening potassium channels in a mammal.
    Type: Grant
    Filed: June 23, 1999
    Date of Patent: July 15, 2003
    Assignee: Abbott Laboratories
    Inventors: William A. Carroll, Yiyuan Chen, Mark W. Holladay, Michael E. Kort, Philip R. Kym, James P. Sullivan, Rui Tang, Lin Yi, Henry Q. Zhang, Irene Drizin
  • Publication number: 20030130517
    Abstract: The present invention provides thienopyridine derivatives, which are useful as anti-inflammatory drugs, particularly as remedies for arthritis; processes for producing them, and pharmaceutical compositions containing them.
    Type: Application
    Filed: August 22, 2002
    Publication date: July 10, 2003
    Inventors: Tsuneo Yasuma, Atsuo Baba, Haruhiko Makino, Isao Aoki, Toshiaki Nagata
  • Patent number: 6579883
    Abstract: The invention relates to compounds of formula (I), to a method for producing them and to their use in medicaments as NOS inhibitors.
    Type: Grant
    Filed: May 10, 2001
    Date of Patent: June 17, 2003
    Assignee: Schering Aktiengesellschaft
    Inventors: Stefan Jaroch, Hartmut Rehwinkel, Peter Hölscher, Detlev Sülzle, Margrit Hillmann, Gerardine Anne Burton, Fiona Macdougall McDonald
  • Patent number: 6576640
    Abstract: The present invention concerns compounds of formula (I) the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C5-12alkanediyl; n is 1 or 2; p is 1 and q is 2; or p is 2 and q is 1; X is —O—, —S—, —S(═O)—, —S(═O)2— or NR2; each R1 is independently hydrogen, halogen, C1-6alkyl, nitro, hydroxy or C1-4alkyloxy; R2 is hydrogen, C1-6alkyl, aryl or C1-6alkyl substituted with aryl; aryl is phenyl or phenyl substituted with a halogen or C1-6alkyl; D is an optionally substituted benzophenone or 3-benzisoxazolyl; having central &agr;2-adrenoceptor antagonist activity. It further relates to their preparation, pharmaceutical use and compositions.
    Type: Grant
    Filed: July 26, 2001
    Date of Patent: June 10, 2003
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Ludo Edmond Josephine Kennis, Josephus Carolus Mertens, Serge Maria Aloysius Pieters
  • Publication number: 20030087926
    Abstract: A substituted 1,2,3,4-tetrahydroquinoline-2-carboxylic acid derivative of formula I 1
    Type: Application
    Filed: August 7, 2002
    Publication date: May 8, 2003
    Applicant: GRUENENTHAL GmbH
    Inventors: Matthias Gerlach, Michael Przewosny, Werner Englberger, Elke Reissmueller, Petra Bloms-Funke, Corinna Maul, Utz-Peter Jagusch
  • 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: 20030078268
    Abstract: Compounds of the formula 1
    Type: Application
    Filed: July 24, 2002
    Publication date: April 24, 2003
    Applicant: Wyeth
    Inventors: Rulin Zhao, Megan Tran, Richard E. Mewshaw, Gary P. Stack
  • Patent number: 6548515
    Abstract: The invention relates to compound of formula (I): wherein: represents a single or double bond, R0 represents hydrogen or hydroxy or alkoxy, R1 and R2, which are identical or different, each represents hydrogen or halogen or alkyl, alkoxy, hydroxy, polyhaloalkyl, nitro or optionally substituted amino or  wherein m represents an integer such that 1≦m≦4, or form together with the carbon atoms carrying them an aromatic or non-aromatic, mono- or bi-cyclic group having from 5 to 12 ring members and optionally containing 1 or 2 hetero atoms selected from O, S and N, R3 represents hydrogen or aryl, heteroaryl, cycloalkyl, optionally substituted alkyl or a group of formula COR7 wherein R7 represents aryl, optionally substituted alkyl, optionally substituted amino or OR10 wherein R10 represents aryl or optionally substituted alkyl, X represents oxygen or sulphur or —CH2— or —CH2—CH2—, Ar represents aryl, heteroaryl or arylalkyl, its op
    Type: Grant
    Filed: November 22, 2000
    Date of Patent: April 15, 2003
    Assignee: Les Laboratories Servier
    Inventors: Henri-Philippe Husson, Sylviane Giorgi-Renault, Christophe Tratrat, Ghanem Atassi, Alain Pierre, Pierre Renard, Bruno Pfeiffer
  • Publication number: 20030065182
    Abstract: The present invention relates to novel radioligands and test methods using those radioligands in screening compounds.
    Type: Application
    Filed: July 30, 2002
    Publication date: April 3, 2003
    Inventors: Robert J. Altenbach, Gary A. Rotert, William A. Carroll, Murali Gopalakrishnan, Eduardo Jose Vicente Molinari, Rachel A. Davis-Taber, Victoria Eleanor Sarah Scott
  • Publication number: 20030050304
    Abstract: The present invention provides compounds of formula (I): 1
    Type: Application
    Filed: June 25, 2002
    Publication date: March 13, 2003
    Inventors: William W. McWhorter, Valentina Badescu
  • Publication number: 20030045542
    Abstract: Compounds of the formula: 1
    Type: Application
    Filed: August 27, 2002
    Publication date: March 6, 2003
    Applicant: Wyeth
    Inventors: Megan Tran, Gary P. Stack
  • Publication number: 20030032652
    Abstract: The invention relates to hydroxamic and carboxylic acid derivatives.
    Type: Application
    Filed: September 6, 2002
    Publication date: February 13, 2003
    Inventors: Duncan Batty, Verity Margaret Sabin, Robert John Watson, Hazel Joan Dyke, Andrew Sharpe, Richard John Davenport, David Alan Owen, Andrew Douglas Baxter
  • Patent number: 6514981
    Abstract: The invention relates to certain indolinone compounds, their method of synthesis, and a combinatorial library consisting of the indolinone compounds. The invention also relates to methods of modulating the function of protein tyrosine kinases using indolinone compounds and methods of treating diseases by modulating the function of protein tyrosine kinases and related signal transduction pathways.
    Type: Grant
    Filed: April 1, 1999
    Date of Patent: February 4, 2003
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, Li Sun
  • Patent number: 6509346
    Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: and physiologically acceptable salts thereof.
    Type: Grant
    Filed: July 28, 1999
    Date of Patent: January 21, 2003
    Assignees: Millennium Pharmaceuticals, Inc., Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima, Hiroki Sone, Osamu Kotera, Geraldine C. B. Harriman
  • Publication number: 20030008891
    Abstract: 3′,4′-di-O-camphanoyl-(+)-cis-khellactone analogs according to the present invention have been found to have anti-HIV activity.
    Type: Application
    Filed: March 13, 2002
    Publication date: January 9, 2003
    Applicant: Panacos Pharmaceuticals, Inc.
    Inventors: Kuo-Hsiung Lee, Lan Xie, Graham P. Allaway, Carl T. Wild
  • Patent number: 6500839
    Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein m, R, R1, R2, A, X, Y and Z are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.
    Type: Grant
    Filed: May 18, 2001
    Date of Patent: December 31, 2002
    Assignee: Neurocrine Biosciences, Inc.
    Inventors: Mustapha Haddach, John Patrick Williams, Michael K. Schwaebe
  • Patent number: 6495555
    Abstract: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C1-6alkanediyl; n is 1 or 2; X1 is —O—, —S—, —S(═O)— or —S(═O)2—; each R1 is independently hydrogen, halogen, C1-6alkyl, nitro, hydroxy or C1-4alkyloxy; D is an optionally substituted mono, bi- or tricyclic nitrogen containing heterocycle, a 2H-benzopyranone, a benzamide, a benzophenone or a phenoxyphenyl having central &agr;2-adrenoceptor antagonist activity. It further relates to their preparation, pharmaceutical use and compositions.
    Type: Grant
    Filed: March 30, 2001
    Date of Patent: December 17, 2002
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Ludo Edmond Josephine Kennis, Frans Maria Alfons Van den Keybus, Josephus Carolus Mertens
  • Publication number: 20020169178
    Abstract: The present invention concerns the compounds of formula 1
    Type: Application
    Filed: April 16, 2002
    Publication date: November 14, 2002
    Inventors: Ludo Edmond Josephine Kennis, Serge Maria Aloysius Pieters, Francois Paul Bischoff
  • Publication number: 20020165245
    Abstract: Compounds of the formula: 1
    Type: Application
    Filed: March 12, 2002
    Publication date: November 7, 2002
    Applicant: Wyeth
    Inventors: Megan Tran, Gary P. Stack
  • Patent number: 6468996
    Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).
    Type: Grant
    Filed: October 19, 1999
    Date of Patent: October 22, 2002
    Assignees: Novo Nordisk A/S, Dr. Reddy's Research Foundation
    Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
  • Patent number: 6462038
    Abstract: Compounds, pharmaceutical compositions, and methods for modulating processes mediated by steroid receptors. In particular, preparation and methods of use of non-steroidal compounds and compositions that are agonists, partial agonists, and antagonists for the androgen receptor (AR) are described. Further, described are the methods of making and use of critical intermediates including a stereoselective synthetic route to intermediates for the AR modulators.
    Type: Grant
    Filed: August 25, 2000
    Date of Patent: October 8, 2002
    Assignee: Ligand Pharmaceuticals, Inc.
    Inventors: Robert Higuchi, Kristen L. Arienti, Mani Neelakandha, Barbara Pio, Lin Zhi, Penghui Chen, Thomas R. Caferro
  • Patent number: 6444812
    Abstract: This invention concerns intermediates in the preparation of compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; —A— is a bivalent radical of formula; R1 and R2 each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar, Ar—C1-6alkyl, Ar-oxy, Ar—C1-6alkyloxy; or when on adjacent positions R1 and R2 taken together may form a bivalent radical; R3 and R4 each independently are hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxy, Ar-oxy, C1-6alkylthio, di(C1-6alkyl)amino, trihalomethyl, trihalomethoxy, or when on adjacent positions R3 and R4 taken together may form a bivalent radical; R5 is an imidazolyl substituted with hydrogen or C1-6alky
    Type: Grant
    Filed: November 29, 2000
    Date of Patent: September 3, 2002
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Marc Gaston Venet, Patrick René Angibaud, Yannick Aimé Eddy Ligny, Virginie Sophie Poncelet, Gerard Charles Sanz
  • Publication number: 20020119992
    Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: 1
    Type: Application
    Filed: December 18, 2001
    Publication date: August 29, 2002
    Inventors: Harold G. Selnick, James C. Barrow, Philippe G. Nantermet, Peter D. Williams, Kenneth J. Stauffer, Philip E. Sanderson, Kenneth E. Rittle, Matthew M. Morrissette, Catherine M. Wiscount, Lekhanh O. Tran, Terry A. Lyle, Donnette D. Staas
  • Patent number: 6426350
    Abstract: The present invention concerns the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein each R1 is independently hydrogen, halogen, C1-6alkyl, nitro, hydroxy or C1-4alkyloxy; Alk is C1-6alkanediyl; n is 1 or 2; p is 0, 1 or 2; D is an optionally substituted mono-, bi- or tricyclic nitrogen containing heterocycle having central &agr;2-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine.
    Type: Grant
    Filed: March 30, 2001
    Date of Patent: July 30, 2002
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Ludo Edmond Josephine Kennis, Serge Maria Aloysius Pieters, François Paul Bischoff
  • Publication number: 20020094977
    Abstract: Compounds of the following structure are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids such as lowering LDL cholesterol and/or increasing HDl cholesterol, and treating hyperlipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis 1
    Type: Application
    Filed: December 4, 2001
    Publication date: July 18, 2002
    Inventors: Jeffrey A. Robl, Bang-Chi Chen, Chong-Qing Sun
  • Publication number: 20020091134
    Abstract: Compounds are provided that, by way of their selective neurotransmitter binding useful for the treatment of various neurological and psychological disorders, e.g., ADHD. Such compounds are 4-phenyl substituted tetrahydroisoquinolines having the Formula IA, IB, IIA, IIB, IIIA or IIIC as set forth herein.
    Type: Application
    Filed: July 11, 2001
    Publication date: July 11, 2002
    Inventors: James P. Beck, Anthony D. Pechulis, Arthur E. Harms
  • Patent number: 6410553
    Abstract: This invention provides novel benzosulfones of the following formulae: These compounds are useful as calcium channel antagonists with cardiovascular, antiasthmatic and antibronchoconstriction activity. Thus, this invention also provides pharmaceutical compositions, as well as methods, for preventing and treating disorders such as hypersensitivity, allergy, asthma, bronchospasm, dysmenorrhea, esophageal spasm, glaucoma, premature labor, urinary tract disorders, gastrointestinal motility disorders and cardiovascular disorders.
    Type: Grant
    Filed: December 28, 2000
    Date of Patent: June 25, 2002
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: John H. Dodd, Kenneth C. Rupert, James L. Bullington, Daniel A. Hall
  • Publication number: 20020076666
    Abstract: Disclosed is a compound represented by the following formula (I): 1
    Type: Application
    Filed: November 1, 2001
    Publication date: June 20, 2002
    Applicant: FUJI PHOTO FILM CO., LTD.
    Inventors: Katsumi Kobayashi, Takashi Katoh, Junji Nishigaki
  • Patent number: 6391887
    Abstract: The invention relates to compounds of formula (I), as defined herein. The invention also relates to the use of the inventive compounds for treatment of a disease caused by the effects of nitrogen monoxide in pathological conditions.
    Type: Grant
    Filed: August 14, 2000
    Date of Patent: May 21, 2002
    Assignee: Schering Aktiengesellschaft
    Inventors: Stefan Jaroch, Hartmut Rehwinkel, Peter Holscher, Detlev Sulzle, Margrit Hillmann, Gerardine Anne Burton, Fiona Mcdougall McDonald
  • 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
  • Publication number: 20020055499
    Abstract: Compounds of the formula (I) are disclosed which are dual fibrinogen receptor and vitronectin receptor antagonists and are useful in the treatment of atherosclerosis, in the prevention of restenosis and in the prevention of tumor metastasis and tumor growth: 1
    Type: Application
    Filed: December 12, 2001
    Publication date: May 9, 2002
    Inventors: Dirk Heerding, James Martin Samanen
  • Patent number: 6384045
    Abstract: This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone ring. The tricyclic oxypyrone synthetic method is a simple condensation reaction of pyrones with cyclohexenecarboxaldehydes, providing high yields and using few steps. The tetracyclic oxypyrone synthetic method is a simple condensation reaction of carvones with pyrones.
    Type: Grant
    Filed: June 24, 1999
    Date of Patent: May 7, 2002
    Assignee: Kansas State University Research Foundation
    Inventors: Duy H. Hua, Jean-Pierre Perchellet
  • Publication number: 20020049325
    Abstract: This invention provides novel benzoethers of the following formulae: 1
    Type: Application
    Filed: December 28, 2000
    Publication date: April 25, 2002
    Inventors: John H. Dodd, James R. Henry, Kenneth C. Rupert, James L. Bullington, Daniel A. Hall
  • Publication number: 20020049326
    Abstract: This invention provides novel benzosulfones of the following formulae: 1
    Type: Application
    Filed: December 28, 2000
    Publication date: April 25, 2002
    Inventors: John H. Dodd, Kenneth C. Rupert, James L. Bullington, Daniel A. Hall
  • Patent number: 6352999
    Abstract: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C1-6alkanediyl; n is 1 or 2; X is —O—, —S—, —S(═O)— or —S(═O)2—; each R1 is independently hydrogen, halogen, C1-6alkyl, nitro, hydroxy or C1-4alkyloxy; D is an indole, a benzisoxazole, a benzisothiazole, a 2H-benzopyranone, a phenoxyphenyl, a benzamide, a benzophenone or a benzopyrimidinone having central &agr;2-adrenoceptor antagonist activity. It further relates to their preparation, pharmaceutical use and compositions.
    Type: Grant
    Filed: March 30, 2001
    Date of Patent: March 5, 2002
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Ludo Edmond Josephine Kennis, Josephus Carolus Mertens, Mirielle Braeken
  • Publication number: 20020019410
    Abstract: Disclosed are compounds of the formula: 1
    Type: Application
    Filed: May 29, 2001
    Publication date: February 14, 2002
    Applicant: Neurogen Corporation
    Inventors: Guolin Cai, Kenneth Shaw
  • Publication number: 20020013334
    Abstract: Compounds of the following structure are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids such as lowering LDL cholesterol and/or increasing HDl cholesterol, and treating hyperlipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis 1
    Type: Application
    Filed: June 6, 2001
    Publication date: January 31, 2002
    Inventors: Jeffrey A. Robl, Bang-Chi Chen, Chong-Qing Sun
  • Publication number: 20020013333
    Abstract: A pharmacologically active compound of formula (I) 1
    Type: Application
    Filed: May 15, 2001
    Publication date: January 31, 2002
    Inventors: Duncan Batty, Verity Margaret Sabin, Robert John Watson, Hazel Joan Dyke, Andrew Sharpe, Richard John Davenport, David Alan Owen, Andrew Douglas Baxter
  • Publication number: 20010053783
    Abstract: A pharmaceutical compound of the formula 1
    Type: Application
    Filed: January 13, 1998
    Publication date: December 20, 2001
    Inventor: JOHN FAIRHURST
  • Patent number: 6329385
    Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by the following structural formula: and physiologically acceptable salts thereof.
    Type: Grant
    Filed: January 21, 1999
    Date of Patent: December 11, 2001
    Assignees: Millennium Pharmaceuticals, Inc., Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima
  • Patent number: 6323200
    Abstract: Thiazolo-, oxazolo- and selenazolo[4,5-c]quinolin-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators and induce cytokine biosynthesis, including interferon and/or tumor biosynthesis, necrosis factor, and inhibit the T-helper-type 2 immune response. The compounds are further useful in the treatment of viral and neoplastic diseases.
    Type: Grant
    Filed: June 14, 2000
    Date of Patent: November 27, 2001
    Assignee: 3M Innovative Properties Company
    Inventors: John F. Gerster, Kyle J. Lindstrom, Gregory J. Marszalek, Bryon A. Merrill, John W. Mickelson, Michael J. Rice
  • Patent number: 6316462
    Abstract: Methods are provided for treating cancer, comprising administering (1) a farnesyl protein transferase inhibitor in conjunction with (2) an additional Ras signaling pathway inhibitor to induce cancer cell death and tumor regression.
    Type: Grant
    Filed: April 9, 1999
    Date of Patent: November 13, 2001
    Assignee: Schering Corporation
    Inventors: Walter R. Bishop, Diana L. Brassard, Tattanahalli L. Nagabhushan
  • Patent number: 6313301
    Abstract: The present invention provides an intermediate for producing a thienopyridine derivative useful as a GnRH antagonist as well as an efficient and safe method for producing the same in an industrial scale at a high yield.
    Type: Grant
    Filed: December 22, 1999
    Date of Patent: November 6, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shokyo Miki, Koichiro Fukuoka, Masahiro Akita, Junichi Kawakami, Shuichi Furuya, Yoichiro Ishimaru
  • Patent number: 6306870
    Abstract: Carboline derivatives of formula (I), are potent and selective inhibitors of cyclic guanosine 3′,5′-monophoshate specific phosphodiesterase (cGMP specific PDE) and have utility in a variety of therapeutic areas where such inhibition is thought to be beneficial, including the treatment of cardivascular disorders.
    Type: Grant
    Filed: June 12, 2000
    Date of Patent: October 23, 2001
    Assignee: ICOS Corporation
    Inventor: Agnes Bombrun
  • Publication number: 20010025039
    Abstract: Novel compounds of formula (I): 1
    Type: Application
    Filed: February 27, 2001
    Publication date: September 27, 2001
    Inventors: Jonathan Mark Bentley, Paul Hebeisen, Sven Taylor
  • Patent number: 6291472
    Abstract: The present invention relates to the use of 4a, 5a, 8a, 8b-tetrahydro-6H-pyrrolo[3′,4′:4,5]furo[3,2-b]pyridine-6,8(7H)-dione derivatives of the general formula (I) and salts thereof, in which the radicals R1 to R5 have the meaning given in the description, and to novel 4a, 5a, 8a, 8b-tetrahydro-6H-pyrrolo[3′,4′:4,5]furo[3,2-b]pyridine-6,8(7H)-dione derivatives and processes for their preparation.
    Type: Grant
    Filed: May 22, 2000
    Date of Patent: September 18, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Peter Jeschke, Achim Harder, Norbert Mencke
  • Patent number: RE38257
    Abstract: A piperidine compound of the formula (I): wherein A is a fused aromatic ring; R is hydrogen, chloro or methoxy; X is (CH2)n, which may be substituted, in which n is 0 or an integer of 1 to 10, —CH≡CH—, —C≡C—, —O—, —S—, —NH—, —N(COCH3)—, —N(COOC2H5)—, —N(CHO)—, —N(CH3)—, —CO—, —SO—, or —SO2—; Y is —CH≡CH—, —CH2CH2—, —CH2CO—, —O—, —S—, —NH—, —OCH2—, —SCH2—, —NHCH2—, —CH(OH)CH2— or —CH(OH)CH(OH)—; and Q is substituted or unsubstituted n-hexyl, carboxypropyl, ethoxycarbonylpropyl, cyanopropyl, cyclohexyl, phenyl, indanyl, naphthyl, tetrahydronaphthyl, benzocycloheptyl, piperidinyl, tetrahydroisoquinolinyl, indolyl, pyrolyl, furyl, thienyl, thiazolyl, oxazolyl or N-methylpyrolyl, wherein any one or more of t
    Type: Grant
    Filed: February 10, 1999
    Date of Patent: September 23, 2003
    Assignee: Ajinomoto Co., Inc.
    Inventors: Masataka Shoji, Kozo Toyota, Chikahiko Eguchi, Ryota Yoshimoto, Yoshikatsu Koyama, Hideki Domoto, Akira Kamimura