Nitrogen Or A -c(=x)- Group, Wherein X Is Chalcogen, Attached Directly To The Bicyclo Ring System By Nonionic Bonding Patents (Class 549/57)
  • Patent number: 7019027
    Abstract: The present invention relates to a compound of formula (I): wherein: R3 is selected from the group consisting of 1-napthyl, 2-napthyl and cycloalkylphenyl; and R4 and R5 taken together form a ring having from 5 to 10 carbon atoms. Additionally, the invention provides a therapeutic method for preventing or treating a pathological condition or symptom in a mammal subject, such as a human, wherein increased angiogenesis is desired, comprising administering to a mammal in need of such therapy an effective amount of the aforementioned thiophene selective adenosine A1 allosteric enhancer.
    Type: Grant
    Filed: March 23, 2004
    Date of Patent: March 28, 2006
    Inventors: Joel M. Linden, Ray A. Ollson, Peter J. Scammells
  • Patent number: 7019024
    Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 9, 2001
    Date of Patent: March 28, 2006
    Assignee: Allelix Neuroscience Inc.
    Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
  • Patent number: 6998407
    Abstract: Chemical compounds which are antagonists of Monocyte Chemoattractant Protein-1 (MCP-1) function, pharmaceutical compositions comprising these compounds, methods of treatment employing these compounds and compositions, and processes for preparing these compounds. The compounds are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection.
    Type: Grant
    Filed: November 18, 2003
    Date of Patent: February 14, 2006
    Assignees: Telik, Inc., Sanwa Kagaku Kenkyusho Co. Ltd.
    Inventors: Edgardo Laborde, Louise Robinson, Fanying Meng, Brian T. Peterson, Hugo O. Villar, Steven E. Anuskiewicz, Yoshiro Ishiwata, Shoji Yokochi, Yukiharu Matsumoto, Takuji Kakigami, Hideaki Inagaki, Takahito Jomori, Kouji Matsushima
  • Patent number: 6982348
    Abstract: The present invention provides a pharmaceutical agent having cholesteryl ester transfer protein inhibitory action and useful as a blood lipid lowering agent and the like. The present invention relates to a compound represented by the formula wherein Ar1 is an aromatic ring group optionally having substituents, Ar2 is an aromatic ring group having substituents, OR? is an optionally protected hydroxyl group, R is an acyl group, R? is a hydrogen atom or a hydrocarbon group optionally having substituents, or a salt thereof, and a pharmaceutical composition containing a compound of the formula (I) or a salt thereof or a prodrug thereof.
    Type: Grant
    Filed: January 25, 2002
    Date of Patent: January 3, 2006
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Masakuni Kori, Kazumasa Hamamura, Hiromitsu Fuse, Toshihiro Yamamoto
  • Patent number: 6962929
    Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, vascular restenosis, microbial infections, and psoriasis, or as lead compounds for the development of such agents.
    Type: Grant
    Filed: October 11, 2002
    Date of Patent: November 8, 2005
    Assignee: Tularik Inc.
    Inventors: John A. Flygare, Julio Cesar Medina, Bei Shan, David Louis Clark, Terry J. Rosen
  • Patent number: 6960669
    Abstract: A method is disclosed for the preparation of benzo[b]thiophenecarbodithioic esters of the formula: wherein R is alkyl, R1 is hydrogen, halogen, or alkyl, R2, R3, R4, and R5 are independently selected from the group consisting of hydrogen, halogen, alkyl, alkoxy, alkylthio, trifluoromethyl, cyano, and aryl, wherein said method comprises reacting an equivalent of an S-thiol ester of the formula: with one-third of an equivalent of P2S5, 2 equivalents of at least one alkali metal carbonate, about 2.5 mole percent of a phase transfer catalyst, and a catalytic amount of water in hot toluene.
    Type: Grant
    Filed: September 10, 2003
    Date of Patent: November 1, 2005
    Assignee: Crompton Co./Cie
    Inventors: Ewa M. Osika, Walter G. Brouwer
  • Patent number: 6933317
    Abstract: Compounds of the general formula (I) which are metabolically stable and have an antagonistic activity against PGD2 receptor: ? wherein Y is bicyclic ring; R1 is optionally substituted heteroaryl; R2 is hydrogen, etc.; R3 is —CH2—CH2—CH2—CH2—CH?CH—COOR4, —CH2—CH2—CH2—CH2—X1—CH2—COOR4, —CH2—CH?CH—CH2—X1—CH2—COOR4 or —CH2—CH2—CH2—COOR4; R4 is hydrogen, etc.; X1 is —O—, etc.
    Type: Grant
    Filed: October 26, 2001
    Date of Patent: August 23, 2005
    Assignee: Shionogi & Co. Ltd.
    Inventors: Norihiko Tanimoto, Yoshiharu Hiramatsu, Tsunetoshi Honma, Masanao Inagaki
  • Patent number: 6887869
    Abstract: The invention concerns novel mikanolide derivatives, their preparation method and their therapeutic uses, in particular as anti-cancer and anti-viral agents.
    Type: Grant
    Filed: January 11, 2002
    Date of Patent: May 3, 2005
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Olivier Lavergne, Christophe Lanco, Grégoire Prevost, Beng Poon Teng
  • Patent number: 6878706
    Abstract: Compounds according to the following formula (I): wherein the variables Q and R1 to R6 are as described herein, which reversibly inhibit the cysteine proteases, such as cathepsins K, S, F, L and B; pharmaceutical compositions containing such compounds, and method of treating diseases and pathological conditions exacerbated by these cysteine proteases such as, but not limited to rheumatoid arthritis, multiple sclerosis and other autoimmune diseases, osteoporosis, asthma, Alzheimer's disease, atherosclerosis and endometriosis.
    Type: Grant
    Filed: March 27, 2003
    Date of Patent: April 12, 2005
    Assignee: Boehringer Ingelheim Pharmaceuticals Inc.
    Inventors: Thomas A. Gilmore, Eugene Richard Hickey, Weimin Liu, Peter Allen Nemoto, Denice M. Spero
  • Patent number: 6872730
    Abstract: The present invention relates to novel substituted benzofurans and benzothiophenes compounds that are antagonists of alpha V (?v) integrins, for example ?v?3 and ?v?5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by ?v?3 and ?v?5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula I: where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, m, n, i, j and k are defined herein.
    Type: Grant
    Filed: April 26, 2002
    Date of Patent: March 29, 2005
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Beth M. Anaclerio, Juan J. Marugan Sanchez, Victor J. Marder, David C. U'Prichard, Bruce E. Tomczuk
  • Patent number: 6869913
    Abstract: Novel pyridazin-3-one derivatives of formula [1] are provided, which are useful as active ingredients of herbicides, wherein R1 is haloalkyl; R2 and R3 are hydrogen, alkyl, haloalkyl, or alkoxyalkyl; and Q is [Q-1], [Q-2], [Q-3], [Q-4] or [Q-5]. Also provided are their use and intermediates for their production.
    Type: Grant
    Filed: February 9, 2004
    Date of Patent: March 22, 2005
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Tadashi Katayama, Shinichi Kawamura, Yuzuru Sanemitsu, Yoko Mine
  • Patent number: 6869972
    Abstract: The subject invention pertains to novel compounds (and salts thereof), and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns methods of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. This results in an improved safety profile. The new compounds have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The compounds also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.
    Type: Grant
    Filed: March 11, 2004
    Date of Patent: March 22, 2005
    Assignee: ARYx Therapeutics
    Inventor: Pascal Druzgala
  • Patent number: 6812243
    Abstract: The invention relates to tyrosine kinase inhibitors of the bis-indolyl compound type of the general formula I: pharmaceuticals containing them and their use for the treatment of malignant and other diseases based on pathological cell proliferation.
    Type: Grant
    Filed: May 3, 2002
    Date of Patent: November 2, 2004
    Assignee: Zentaris AG
    Inventors: Siavosh Mahboobi, Sabine Kuhr, Herwig Pongratz, Alfred Popp, Harald Hufsky, Frank-D Bohmer, Steffen Teller, Andrea Uecker, Thomas Beckers
  • Publication number: 20040176437
    Abstract: The subject invention pertains to novel compounds (and salts thereof), and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns methods of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. This results in an improved safety profile. The new compounds have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The compounds also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.
    Type: Application
    Filed: March 11, 2004
    Publication date: September 9, 2004
    Inventor: Pascal Druzgala
  • Publication number: 20040157841
    Abstract: Mono-acylated o-phenylendiamines derivatives of formula I 1
    Type: Application
    Filed: February 3, 2004
    Publication date: August 12, 2004
    Inventors: Georg Fertig, Frank Herting, Manfred Kubbies, Anja Limberg, Ulrike Reiff, Michael Weidner
  • Publication number: 20040110692
    Abstract: This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of magnesium to the plasma membranes of their cells. These methods consist of administering to a mammal in need of such treatment a compound selected from a series of disubstituted trans, trans 1,3-butadienes, 1,3-disubstituted perhydrobutadienes, 1,2-disubstituted trans ethylenes and 1,2 disubstituted ethanes and disubstituted propanes, each of which embodies, in common, the unique structural feature essential for the biological activity of these compounds. This invention also provides for pharmaceutical formulations that employ these novel compounds.
    Type: Application
    Filed: October 28, 2003
    Publication date: June 10, 2004
    Applicant: Magnesium Diagnostics, Inc.
    Inventor: Ibert Clifton Wells
  • Patent number: 6723848
    Abstract: Process for the preparation of benzo-fused heterocycles of general formula I: in which X, R1, R2, R3, R4, R5 and n are as defined in claim 1, by reacting tetrahydrobenzo-fused heterocycles of formula II: in which X, R1, R2, R3, R4, R5, n and Ac are as defined in claim 1, with a catalytic amount of a noble metal catalyst in the presence of a hydrogen acceptor and then deacylating the acylated amino group by the addition of an amine.
    Type: Grant
    Filed: October 9, 2002
    Date of Patent: April 20, 2004
    Assignee: Merck Patent Gesellschaft mit Beschränkter Haftung
    Inventors: Frank-Hardi Wartenberg, Thomas Koppe, Walter Wetzel, Markus Wydra, Achim Benz
  • Patent number: 6720423
    Abstract: Compounds of the formula where the variables have the meaning defined in the specification, are specific or selective agonists of RXR retinoid receptors.
    Type: Grant
    Filed: April 30, 2002
    Date of Patent: April 13, 2004
    Assignee: Allergan, Inc.
    Inventors: Jayasree Vasudevan, Dehua Huang, Vidyasagar Vuligonda, Roshanta S. Chandraratna
  • Patent number: 6713638
    Abstract: The present invention relates to a compound of formula (I): wherein: R3 is selected from the group consisting of 1-napthyl, 2-napthyl and cycloalkylphenyl; and R4 and R5 taken together form a ring having from 5 to 10 carbon atoms. Additionally, the invention provides a therapeutic method for preventing or treating a pathological condition or symptom in a mammal subject, such as a human, wherein increased angiogenesis is desired, comprising administering to a mammal in need of such therapy an effective amount of the aforementioned thiophene selective adenosine A1 allosteric enhancer.
    Type: Grant
    Filed: May 20, 2002
    Date of Patent: March 30, 2004
    Inventors: Joel M. Linden, Ray A. Ollson, Peter J. Scammells
  • Patent number: 6710070
    Abstract: The subject invention pertains to novel compounds (and salts thereof), and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns methods of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. This results in an improved safety profile. The new compounds have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The compounds also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.
    Type: Grant
    Filed: December 10, 2002
    Date of Patent: March 23, 2004
    Assignee: ARYx Therapeutics
    Inventor: Pascal Druzgala
  • Patent number: 6677369
    Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
    Type: Grant
    Filed: April 25, 2002
    Date of Patent: January 13, 2004
    Assignee: Eli Lilly and Company
    Inventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
  • Publication number: 20030232988
    Abstract: Methods for making bis-heterocyclic compounds, especially bis-heterocyclic compounds having five and six-membered heterocyclic linkers are described. Also described are methods for making an alpha amino ketone synthon that enables facile syntheses of bisindole compounds, including topsentins and dragmacidins.
    Type: Application
    Filed: December 5, 2002
    Publication date: December 18, 2003
    Inventors: David A. Horne, Kenichi Yakushijin
  • Publication number: 20030195226
    Abstract: The present invention relates to novel oxime carbamyl derivatives and pharmaceutical compositions comprising said derivatives which inhibit fatty acid amide hydrolase. These pharmaceutical compositions are useful for the treatment of conditions which can be effected by inhibiting fatty acid amide hydrolase including, but not limited to, neuropathic pain, emesis, anxiety, altering feeding behaviors, movement disorders, glaucoma, brain injury, and cardiovascular disease.
    Type: Application
    Filed: February 4, 2003
    Publication date: October 16, 2003
    Inventors: Sing-Yuen Sit, Kai Xie, Hongfeng Deng
  • Publication number: 20030187053
    Abstract: The invention relates to triamide MTP/ApoB inhibitors of the formula 1 1
    Type: Application
    Filed: June 20, 2002
    Publication date: October 2, 2003
    Applicant: Pfizer Inc.
    Inventors: Peter Bertinato, Alan E. Blize, Brian S. Bronk, Hengmiao Cheng, Jin Li, Hiep Huatan, Clive Mason
  • Publication number: 20030134880
    Abstract: Compounds of formula (I) wherein R is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl or heterocyclyl; R1 is bicyclyl or heterobicyclyl; R2 is aryl, heteroaryl, heterocyclyl, alkoxy, alkyl, hydroxy or optionally substituted amino and n is from 0 to 3; with the provisos than when n is 0 R2 is alkyl or when n is from 1 to 3 R2 is not alkyl, are useful in the treatment and prophylaxis of conditions mediated by CD23 or TNF.
    Type: Application
    Filed: October 25, 2002
    Publication date: July 17, 2003
    Inventors: Gordon Bruton, Barry Sidney Orlek, Kishore Kalidas Rana
  • Patent number: 6555697
    Abstract: The invention concerns a novel method for preparing a benzofuran or benzothiophene compound by cyclizing an aromatic compound bearing a side-chain comprising at least two carbon atoms, one of the carbon atoms being bound to the benzene cycle by an oxygen or sulphur atom, the other carbon atom is in carboxylic form and a formyl radical in ortho position relative to said chain. The inventive method is characterised in that it consists in cyclizing the latter in the presence of an efficient amount of a carbonate base in a medium comprising a carboxylic acid anhydride and optionally an organic solvent.
    Type: Grant
    Filed: April 11, 2002
    Date of Patent: April 29, 2003
    Assignee: Rhodia Chimie
    Inventor: Thierry Schlama
  • Patent number: 6518291
    Abstract: The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.
    Type: Grant
    Filed: September 14, 1999
    Date of Patent: February 11, 2003
    Assignee: Vertex Pharmaceuticals, Incorporated
    Inventors: Jeffrey O. Saunders, David M. Armistead, Michael C. Badia, Randy S. Bethiel, Catherine A. Frank, Doug Naegele, Perry M. Novak, David A. Pearlman, Steven M. Ronkin
  • Patent number: 6509369
    Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:
    Type: Grant
    Filed: January 8, 2002
    Date of Patent: January 21, 2003
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, III, Richard Cordova, Kevin Pan, Joseph Meschino
  • Patent number: 6506780
    Abstract: This invention relates to a series of substituted benzophenone and sulfone compounds of the formula I wherein ring A, Z, Y, R and X are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.
    Type: Grant
    Filed: July 2, 2001
    Date of Patent: January 14, 2003
    Assignee: Pfizer Inc.
    Inventor: John A. Lowe, III
  • Patent number: 6492390
    Abstract: A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I′ wherein X, A1, A2, A3, A4, R, R″, R1 and R2 are as described in the specification.
    Type: Grant
    Filed: May 24, 2001
    Date of Patent: December 10, 2002
    Assignee: G.D. Searle & Co.
    Inventors: Jeffery S Carter, Mark G Obukowicz, Balekudru Devadas, John J Talley, David L Brown, Matthew J Graneto, Stephen R Bertenshaw, Donald J Rogier, Jr., Srinivasan Raj Nagarajan, Cathleen E Hanau, Susan J Hartmann, Cindy L Ludwig, Suzanne Metz, Donald E Korte
  • Publication number: 20020173645
    Abstract: The present invention is directed to chemical processes for preparing 2-aryl-6-hydroxy-3-[4-(2-aminoethoxy)benzoyl]benzo[b]-thiophenes. The present invention is also directed to crystalline solvates and a non-solvated crystalline form of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]-benzo[b]thiophene hydrochloride, as well as processes for their preparation.
    Type: Application
    Filed: February 26, 2002
    Publication date: November 21, 2002
    Inventor: Wayne Douglas Luke
  • Patent number: 6479604
    Abstract: A diarylethene compound of the following formula (1) wherein R1 is a hydrogen or a substituted or unsubstituted C1-22 alkyl group, a fluoro group, a substituted or unsubstituted phenyl group, a substituted or unsubstituted phenylalkyl group, R2 is a C1-22 alkylene group which may be unsubstituted or substituted with fluorine, R3 is a chemical bond, O, S, NR1, N(R2R1), or a C1-3 alkylene group which may be unsubstituted or substituted with one or more oxygen atoms or fluorine atoms, X and Y independently of one another O, S, nitrogen, NR1, or N(R2R1), and Z is a carbonyl group or a methylene group which may be unsubstituted or substituted with fluorine.
    Type: Grant
    Filed: January 27, 2000
    Date of Patent: November 12, 2002
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Eun-Kyoung Kim, Yun-Ki Choi
  • Publication number: 20020161242
    Abstract: A process for preparing a compound having PGD2 antagonism represented by the formula (I), or a pharmaceutically acceptable salt or hydrate thereof, which process comprises reacting an amino alcohol of the formula (II) or its salt with a compound of the formula (III) or its reactive derivative, oxidizing the product with halo oxoacid in the presence of 2,2,6,6-tetramethylpiperidine-1-oxyls, reacting the product with an ylide under the conditions for Wittig reaction, and optionally deprotecting the product.
    Type: Application
    Filed: April 29, 2002
    Publication date: October 31, 2002
    Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu
  • Publication number: 20020156297
    Abstract: A process for preparing a compound having PGD2 antagonism represented by the formula (I), or a pharmaceutically acceptable salt or hydrate thereof, which process comprises reacting an amino alcohol of the formula (II) or its salt with a compound of the formula (III) or its reactive derivative, oxidizing the product with halo oxoacid in the presence of 2,2,6,6-tetramethylpiperidine-1-oxyls, reacting the product with an ylide under the conditions for Wittig reaction, and optionally deprotecting the product.
    Type: Application
    Filed: April 29, 2002
    Publication date: October 24, 2002
    Inventors: Tetsuo Okada, Makoto Kakinuma
  • Patent number: 6465508
    Abstract: Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs.
    Type: Grant
    Filed: February 23, 2001
    Date of Patent: October 15, 2002
    Assignee: Wyeth
    Inventors: Frances Christy Nelson, Arie Zask, James Ming Chen, Dominick Mobilio, Ramaswamy Nilakantan
  • Patent number: 6465662
    Abstract: A process for preparing a compound having PGD2 antagonism represented by the formula (I), or a pharmaceutically acceptable salt or hydrate thereof, which process comprises reacting an amino alcohol of the formula (II) or its salt with a compound of the formula (III) or its reactive derivative, oxidizing the product with halo oxoacid in the presence of 2,2,6,6-tetramethylpiperidine-1-oxyls, reacting the product with an ylide under the conditions for Wittig reaction, and optionally deprotecting the product.
    Type: Grant
    Filed: April 29, 2002
    Date of Patent: October 15, 2002
    Assignee: Shionogi & Co., Ltd.
    Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu
  • Patent number: 6455684
    Abstract: A method for analyzing an objective substance, comprising reacting a labeled probe with an objective substance on a biological sample, said probe comprising a label substance of the formula (I): wherein A1 is an aromatic group, R1 is a hydrogen or —COCH2COCnF2n+1 and n is an integer of 1-6, which is bonded to a probe selected from the group consisting of nucleic acid, nucleic acid binding protein, low molecular ligand and receptor for ligand (except antibody) to give a fluorescent complex, reacting the complex with an objective substance on a biological sample and assaying fluorescence of the resultant fluorescent complex, a labeled nucleic acid probe and a labeled nucleotide. According to the method of the present invention, defects such as hindrance of fluorescence due to contaminant substance, low sensitivity and the like can be resolved, thereby enabling analysis on a tissue.
    Type: Grant
    Filed: September 28, 2001
    Date of Patent: September 24, 2002
    Assignees: Toyo Boseki Kabushiki Kaisha
    Inventors: Kazuhiro Matsui, Katsunori Ikeda, Shinichi Teshima, Yoshihisa Kawamura, Kazuko Matsumoto
  • Patent number: 6441196
    Abstract: Novel processes and intermediates useful in the preparation of 11-oxa prostaglandin analogs are disclosed.
    Type: Grant
    Filed: May 18, 2001
    Date of Patent: August 27, 2002
    Assignee: Alcon, Inc.
    Inventors: Pete Delgado, Raymond E. Conrow, William D. Dean, Michael S. Gaines
  • Publication number: 20020115871
    Abstract: A process for preparing a compound having PGD2 antagonism represented by the formula (I), or a pharmaceutically acceptable salt or hydrate thereof, which process comprises reacting an amino alcohol of the formula (II) or its salt with a compound of the formula (III) or its reactive derivative, oxidizing the product with halo oxoacid in the presence of 2,2,6,6-tetramethylpiperidine-1-oxyls, reacting the product with an ylide under the conditions for Wittig reaction, and optionally deprotecting the product.
    Type: Application
    Filed: April 29, 2002
    Publication date: August 22, 2002
    Inventors: Tetsuo Okada, Makoto Kakinuma
  • Publication number: 20020107280
    Abstract: This invention relates to compounds, which are generally anti-inflammatory and analgesic compounds, and which are represented by Formula I: 1
    Type: Application
    Filed: December 3, 2001
    Publication date: August 8, 2002
    Inventors: Kevin L. McLaren, David Bernard Smith, Jahari Laurant Tracy
  • Patent number: 6429317
    Abstract: The present invention provides novel indane-like compounds which can be useful for treating psychosis and other conditions associated with the modulation of a muscarinic receptor. The invention provides formulations and methods for using the novel compounds.
    Type: Grant
    Filed: September 5, 2000
    Date of Patent: August 6, 2002
    Assignee: Eli Lilly and Company
    Inventors: Sean P. Hollinshead, Michael A. Staszak, John S. Ward, Joseph W. Wilson, Bret E. Huff, Philip F. Hughes, Jose S. Mendoza, Charles H. Mitch
  • Patent number: 6407102
    Abstract: The invention relates to tyrosine kinase inhibitors of the bis-indolyl compound type of the general formula I: pharmaceuticals containing them and their use for the treatment of malignant and other diseases based on pathological cell proliferation.
    Type: Grant
    Filed: May 4, 1999
    Date of Patent: June 18, 2002
    Assignee: Zentaris AG
    Inventors: Siavosh Mahboobi, Sabine Kuhr, Herwig Pongratz, Alfred Popp, Harald Hufsky, Frank-D Bohmer, Steffen Teller, Andrea Uecker, Thomas Beckers
  • Patent number: 6399778
    Abstract: The present invention is directed to chemical processes for preparing 2-aryl-6-hydroxy-3-[4-(2-aminoethoxy)benzoyl]benzo[b]-thiophenes. The present invention is also directed to crystalline solvates and a non-solvated crystalline form of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]-benzo[b]thiophene hydrochloride, as well as processes for their preparation.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: June 4, 2002
    Assignee: Eli Lilly and Company
    Inventors: Elizabeth Smith LaBell, John McNeill McGill, Randal Scot Miller
  • Patent number: 6380221
    Abstract: This invention is directed to compounds of formula (III): wherein B, C, D, E, R1, R2 and R3 are disclosed herein. These components are disclosed as being useful as anti-coagulants.
    Type: Grant
    Filed: August 3, 2000
    Date of Patent: April 30, 2002
    Assignee: Berlex Laboratories, Inc.
    Inventors: Damian O. Arnaiz, Yuo-Ling Chou, Brian D. Griedel, Rushad E. Karanjawala, Monica J. Kochanny, Wheeseong Lee, Amy Mei Liang, Michael M. Morrissey, Gary B. Phillips, Karna Lyn Sacchi, Steven T. Sakata, Kenneth J. Shaw, R. Michael Snider, Shung C. Wu, Bin Ye, Zuchun Zhao
  • Patent number: 6372779
    Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:
    Type: Grant
    Filed: December 28, 1998
    Date of Patent: April 16, 2002
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, III, Richard Cordova, Kevin Pan, Joseph Meschino
  • Patent number: 6362216
    Abstract: The present invention is directed to compounds which are capable of inhibiting the activity of tryptase. Such compounds are useful in the treatment or prevention of inflammatory disease, particularly those disease states which are mediated by mast cell activation. Also encompassed by the invention are formulations comprising the noted compounds, processes for preparing such compounds and methods for treating or preventing an inflammatory disease.
    Type: Grant
    Filed: May 3, 2000
    Date of Patent: March 26, 2002
    Assignee: Array Biopharma Inc.
    Inventors: Laurence E. Burgess, James P. Rizzi
  • Patent number: 6353014
    Abstract: A method of treating glaucoma or ocular hypertension in a patient, which comprises administering to the patient a pharmaceutically effective amount of a compound of formula I:
    Type: Grant
    Filed: June 2, 1999
    Date of Patent: March 5, 2002
    Assignee: Alcon Laboratories, Inc.
    Inventors: Verney L. Sallee, Mark R. Hellberg, Peter G. Klimko
  • Publication number: 20020026061
    Abstract: Benzothiophenecarboxylic acid derivatives of the formula (I) which are useful as starting materials for producing drugs, and a process for preparing 5-hydroxybenzo[b]-thiophene-3-carboxylic acid derivatives of the formula (VI) which are specific PGD2 antagonists.
    Type: Application
    Filed: September 26, 2001
    Publication date: February 28, 2002
    Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu
  • Patent number: 6350884
    Abstract: This invention is directed to a class of acrylic and propionic acid compounds and their use in the treatment of post-menopausal symptoms and restenosis. In other embodiments, the invention is directed to intermediates and to processes for the preparation of the acrylic and propionic acid compounds.
    Type: Grant
    Filed: September 30, 1997
    Date of Patent: February 26, 2002
    Assignee: Eli Lilly and Company
    Inventors: Charles David Jones, Alan David Palkowitz, Kenneth Jeff Thrasher
  • Publication number: 20020016476
    Abstract: Benzothiophenecarboxylic acid derivatives of the formula (I) which are useful as starting materials for producing drugs, and a process for preparing 5-hydroxybenzo[b]-thiophene-3-carboxylic acid derivatives of the formula (VI) which are specific PGD2 antagonists.
    Type: Application
    Filed: September 26, 2001
    Publication date: February 7, 2002
    Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu