The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/510)
  • Patent number: 6939889
    Abstract: Novel compounds and pharmaceutical compositions containing such compounds and possessing anti-tussive activity, and a method of administering the same to warm-blooded animals, including humans.
    Type: Grant
    Filed: December 23, 2003
    Date of Patent: September 6, 2005
    Assignee: UCB Farchim SA
    Inventors: Gregory N. Beatch, Lewis S. L. Choi, Clive P. Page, Bertrand M. C. Plouvier, Yuzhong Liu
  • Publication number: 20040229931
    Abstract: 1-Aryl-3-(indol-5-yl)prop-2-en-1-ones, compositions containing them and use thereof are disclosed and claimed. The present invention relates specifically to novel substituted 1-aryl-3-(indol-5-yl)prop-2-en-1-ones of formula (I) having a therapeutic activity, particularly, in oncology.
    Type: Application
    Filed: April 30, 2004
    Publication date: November 18, 2004
    Applicant: Aventis Pharma S. A.
    Inventors: Patrick Mailliet, Fabienne Thompson, Luc Bertin, Gerard Leclere, Gilles Tiraboschi
  • Patent number: 6794406
    Abstract: The invention relates to new indole derivatives, processes for their preparation, and their use in medicaments.
    Type: Grant
    Filed: December 21, 2001
    Date of Patent: September 21, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Helmut Haning, Michael Woltering, Gunter Schmidt, Hilmar Bischoff, Axel Kretschmer, Verena Vöhringer, Christiane Faeste
  • Publication number: 20040176614
    Abstract: A process for the preparation of compounds of formula 1
    Type: Application
    Filed: March 18, 2004
    Publication date: September 9, 2004
    Inventors: Annemarie Wolleb, Heinz Wolleb
  • Patent number: 6759427
    Abstract: A tetrahydroindolone derivative or analogue comprises a 9-atom bicyclic moiety, moiety A, linked through a linker L to a moiety B, where B is a carboxylic acid, a carboxylic acid ester, or a moiety of the structure N(Y1)-D, where Y1 can be one of a variety of substituents, including hydrogen or alkyl, and D is a moiety that enhances the pharmacological effects, promotes absorption or blood-brain barrier penetration of the derivative or analogue. The moiety A has a six-membered ring fused to a five-membered ring. The moiety A can have one, two, or three nitrogen atoms in the five membered ring. The moiety A can be a tetrahydroindolone moiety. The moiety B can be one of a variety of moieties, including moieties having nootropic activity or other biological or physiological activity.
    Type: Grant
    Filed: April 20, 2001
    Date of Patent: July 6, 2004
    Assignee: Spectrum Pharmaceuticals, Inc.
    Inventors: David B. Fick, Mark M. Foreman, Alvin J. Glasky
  • Publication number: 20040092750
    Abstract: 2-Methylindole-4-acetic acid, which is represented by the formula (I) and is an intermediate for an important indole derivative as medicines; and a process for producing the compound and the synthetic intermediates.
    Type: Application
    Filed: August 29, 2003
    Publication date: May 13, 2004
    Inventors: Tomoyuki Hasegawa, Yasufumi Kawanaka
  • Publication number: 20040024190
    Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: 1
    Type: Application
    Filed: July 18, 2002
    Publication date: February 5, 2004
    Applicant: Boehringer Ingelheim (Canada) Ltd.
    Inventors: Pierre Louis Beaulieu, Gulrez Fazal, Sylvie Goulet, George Kukolj, Martin Poirier, Youla S. Tsantrizos, Eric Jolicoeur, James Gillard, Marc-Andre Poupart, Jean Rancourt
  • Patent number: 6656961
    Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.
    Type: Grant
    Filed: March 14, 2001
    Date of Patent: December 2, 2003
    Assignee: Sloan-Kettering Institute for Cancer Research
    Inventors: Samuel J. Danishefsky, Peter Bertinato, Dai-Shi Su, Dang Fang Meng, Ting-Chao Chou, Ted Kamenecka, Erik J. Sorensen, Aaron Balog, Kenneth A. Savin
  • Patent number: 6656711
    Abstract: The invention relates to a new process for concentrating epothilones in culture media, a new process for the production of epothilones, a new process for separating epothilones A and B and a new strain obtained by mutagenesis for the production of epothilones, as well as aspects related thereto. New crystal forms of epothilone B are also described.
    Type: Grant
    Filed: January 29, 2002
    Date of Patent: December 2, 2003
    Assignee: Novartis AG
    Inventors: Hans Hofmann, Marion Mahnke, Klaus Memmert, Frank Petersen, Thomas Schupp, Ernst Küsters, Michael Mutz
  • Patent number: 6635634
    Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.
    Type: Grant
    Filed: February 14, 2002
    Date of Patent: October 21, 2003
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
  • Publication number: 20030158178
    Abstract: The current invention provide novel heterocyclic retinoid compounds, methods of treating or preventing chronic obstructive pulmonary disease, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of these disorders and methods for delivering formulations of these retinoids to a mammal having these disorders.
    Type: Application
    Filed: October 30, 2002
    Publication date: August 21, 2003
    Applicant: Syntex (U.S.A.) LLC
    Inventors: Michael Klaus, Jean-Marc Lapierre
  • Publication number: 20030109568
    Abstract: The present invention relates to a novel 1H-indole derivative having a structure of formula 1 and its pharmaceutically acceptable salts as a highly selective cyclooxygenase-2 inhibitor.
    Type: Application
    Filed: October 3, 2002
    Publication date: June 12, 2003
    Applicant: CHEIL JEDANG Corporation
    Inventors: Il Hwan Cho, Jee Woong Lim, Ji Young Noh, Jong Hoon Kim, Hyung Chul Ryu, Sang Wook Park, Je Hak Kim, Hyung Ok Chun, So Young Wang, Sung Hak Lee
  • Patent number: 6566533
    Abstract: The invention relates to a method of producing heterocyclic carbamates of the general formula (I) by reacting aza-heterocyclic compounds with alkyl- or aryl-halides in the presence of carbon dioxide and alkali carbonate, and to new compounds of the general formula (I).
    Type: Grant
    Filed: July 6, 2001
    Date of Patent: May 20, 2003
    Assignee: Warner-Lambert Company LLC
    Inventors: Hubert Barth, Klaus Steiner, Simon Schneider, Ulrich Bayer, Manfred Westermayer, Ulrike Wolfsperger, Hans-Jürgen Betche
  • Patent number: 6525083
    Abstract: Certain N-substituted indoles having aryloxyacetic acid, substituents are agonists or partial agonists of PPAR gamma, and are useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR mediated diseases, disorders and conditions.
    Type: Grant
    Filed: July 25, 2001
    Date of Patent: February 25, 2003
    Assignee: Merck & Co., Inc.
    Inventors: John J. Acton, III, Regina Marie Black, Anthony Brian Jones, Harold Blair Wood
  • Patent number: 6500669
    Abstract: The compositions and methods disclosed herein provide heterobifunctional programmable genotoxic compounds that can be designed to kill selected cells present in a heterogenous cell population. The present compounds comprise a first agent that inflicts damage on cellular DNA, and a second agent that attracts a macromolecular cell component such as a protein, which in turn shields genomic lesions from repair. Unrepaired lesions therefore persist in the cellular genome and contribute to the death of selected cells. In contrast, lesions formed in nonselected cells, which lack the cell component, are unshielded and thus are repaired. As a result, compounds described herein are less toxic to nonselected cells. Compounds of this invention can be designed to cause the selective killing of transformed cells, viral-infected cells and the like.
    Type: Grant
    Filed: June 23, 1998
    Date of Patent: December 31, 2002
    Assignee: Massachusetts Institute of Technology
    Inventors: John M. Essigmann, Robert G. Croy, Kevin J. Yarema, Marshall Morningstar
  • Patent number: 6495546
    Abstract: Propanolamine derivatives represented by the following formula (I): These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.
    Type: Grant
    Filed: November 22, 2000
    Date of Patent: December 17, 2002
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
  • Patent number: 6489475
    Abstract: Heterocyclic derivatives of the formula (I) wherein each symbol is as defined in the specification, pharmaceutically acceptable salts thereof and method of producing them. Pharmaceutical compositions containing the heterocyclic derivative or a pharmaceutically acceptable salt thereof, particularly, ACAT inhibitors and lipoperoxidation inhibitors. The heterocyclic derivatives and pharmaceutically acceptable salts thereof of the present invention show superior ACAT inhibitory activity and lipoperoxidation inhibitory activity, and are useful as ACAT inhibitors and hyperlipemia inhibitors. To be specific, they are useful for the prevention and treatment of arteriosclerotic lesions of arteriosclerosis, hyperlipemia and diabetes, as well as ischemic diseases of brain, heart and the like.
    Type: Grant
    Filed: February 15, 2001
    Date of Patent: December 3, 2002
    Assignee: Sankyo Company, Limited
    Inventors: Hiroshi Matsui, Shoji Kamiya
  • Publication number: 20020173663
    Abstract: A class of aryloxyacetic acids comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.
    Type: Application
    Filed: August 17, 2001
    Publication date: November 21, 2002
    Inventors: Kun Liu, Libo Xu, A. Brian Jones
  • Patent number: 6482859
    Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and mixtures of isomers thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or by C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl: or a group NR11R12 wherein R11 and R12 are each independently of the other hydrogen or C1-C8alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are ea
    Type: Grant
    Filed: February 4, 2000
    Date of Patent: November 19, 2002
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Martin Zeller, André Jeanguenat
  • Publication number: 20020169200
    Abstract: The present invention relates to novel substituted indole compounds that are antagonists of alpha V (&agr;v) integrins, for example &agr;v&bgr;3 and &agr;v&bgr;5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by &agr;v&bgr;3 and &agr;v&bgr;5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis.
    Type: Application
    Filed: January 29, 2002
    Publication date: November 14, 2002
    Applicant: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Tianbao Lu, Louis V. LaFrance, Thomas P. Markotan, Juan Jose Marugan, Victor J. Marder, David C. U'Prichard, Beth M. Anaclerio, Zihong Guo, Wenxi Pan, Kristi A. Leonard
  • Patent number: 6414008
    Abstract: New disubstituted bicyclic heterocycles of general formula Ra—A—Het—B—Ar—E  (I) Compounds of general formula I, wherein E is an RbNH—C(═NH)— group, have valuable pharmacological properties, particularly a thrombin-inhibiting effect and the effect of prolonging thrombin time, and those wherein E is a cyano group, are valuable intermediates for preparing the other compounds of general formula I.
    Type: Grant
    Filed: October 13, 2000
    Date of Patent: July 2, 2002
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Norbert Hauel, Henning Priepke, Uwe Ries, Jean Marie Stassen, Wolfgang Wienen
  • Patent number: 6388095
    Abstract: Compounds and pharmaceutical compositions containing such compounds and possessing anti-tussive activity, and a method of administering the same to warm-blooded animals, including humans.
    Type: Grant
    Filed: June 9, 1999
    Date of Patent: May 14, 2002
    Assignee: Cardiome Pharma Corp.
    Inventors: Gregory N. Beatch, Lewis S. L. Choi, Clive P. Page, Bertrand M. C. Plouvier, Yuzhong Liu
  • Patent number: 6380227
    Abstract: The invention relates to a new process for concentrating epothilones in culture media, a new process for the production of epothilones, a new process for separating epothilones A and B and a new strain obtained by mutagenesis for the production of epothilones, as well as aspects related thereto. New crystal forms of epothilone B are also described.
    Type: Grant
    Filed: September 7, 2000
    Date of Patent: April 30, 2002
    Assignee: Novartis AG
    Inventor: Michael Mutz
  • Publication number: 20020032202
    Abstract: Described is a heterocycle-containing carboxylic acid derivative represented by the following formula (I): 1
    Type: Application
    Filed: July 23, 2001
    Publication date: March 14, 2002
    Applicant: Eisai Co. Ltd.
    Inventors: Kouichi Kikuchi, Katsuya Tagami, Hiroyuki Yoshimura, Shigeki Hibi, Mitsuo Nagai, Shinya Abe, Makoto Okita, Takayuki Hida, Seiko Higashi, Naoki Tokuhara, Seiichi Kobayashi
  • Patent number: 6323235
    Abstract: Novel compounds having strong TXA2 receptor antagonist activities and PGI2 receptor agonist activities, which are effective for therapy and prevention of diseases related to TXA2, are disclosed. The compound of the present invention is represented by the following formula (I). (wherein the meanings of the symbols in the formula are as described in the specification).
    Type: Grant
    Filed: January 13, 2000
    Date of Patent: November 27, 2001
    Inventors: Atsushi Ohtake, Kazuhiro Hoshi, Shunji Tsukamoto, Takahiro Takeda, Naohiro Yamada, Kazuhisa Matsumoto, Michihiro Ohno, Kiyotaka Ohno
  • Patent number: 6316630
    Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof, useful in the treatment of cancer and cancer which has developed a multidrug-resistant phenotype. Also provided are intermediates useful for preparing said epothilones.
    Type: Grant
    Filed: June 6, 2000
    Date of Patent: November 13, 2001
    Assignee: Sloan Kettering Institute for Cancer Research
    Inventors: Samuel J. Danishefsky, Peter Bertinato, Dai-Shi Su, DongFang Meng, Ting-Chao Chou, Ted Kamenecka, Erik J Sorensen, Aaron Balog, Kenneth A. Savin
  • Patent number: 6291508
    Abstract: Mono- or polyenic carboxylic acid derived compounds of the formula (1-I) or a physiologically acceptable salt thereof: Z—(CR3═CR2)n—COOR1  (1-I) wherein R1 is hydrogen or a carboxyl-protecting group; R2 and R3 are each independently hydrogen, halogen, linear lower alkyl, branched lower alkyl linear lower alkoxy, branched lower alkoxy or aryl, m is 1 to 3 and Z is a group or their salts have the potent ability to bind to retinoic acid receptors thus useful in treating psoriasis and rheumatoid arthritis.
    Type: Grant
    Filed: September 23, 1999
    Date of Patent: September 18, 2001
    Assignee: Eisai Co., Ltd.
    Inventors: Shigeki Hibi, Kouichi Kikuchi, Hiroyuki Yoshimura, Mitsuo Nagai, Katsuya Tagami, Shinya Abe, Ieharu Hishinuma, Junichi Nagakawa, Norimasa Miyamoto, Takayuki Hida, Aichi Ogasawara, Seiko Higashi, Kenji Tai, Takashi Yamanaka, Makoto Asada
  • Publication number: 20010021719
    Abstract: The present invention relates to new 2-Phenyl-1-[(2-Aminoethoxy)-Benzyl]-Indole compounds which are usefuil as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utiig these compounds, which have the general structures below: 1
    Type: Application
    Filed: February 8, 2001
    Publication date: September 13, 2001
    Inventors: Chris P. Miller, Michael D. Collini, Bach D. Tran, Arthur A. Santilli
  • Patent number: 6288063
    Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula (T)xA—B—D—E—G wherein A is an aryl or heteroaryl rings; B is an aryl or heteroaryl ring or a bond; each T is a substituent group; x is 0, 1, or 2; the group D represents the group E represents a two or three carbon chain bearing one to three substituent groups which are independent or are involved in ring formation, possible structures being shown in the text and claims; and the group G represents and with the proviso that when G is each of the substituents on E is an independent substituent; and include pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: May 27, 1998
    Date of Patent: September 11, 2001
    Assignee: Bayer Corporation
    Inventors: Harold Clinton Eugene Kluender, David Ross Brittelli, William Riley Schoen, Sookhee Nicole Ha
  • Publication number: 20010016661
    Abstract: Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.
    Type: Application
    Filed: March 27, 2001
    Publication date: August 23, 2001
    Applicant: The Institute for Pharmaceutical Discovery
    Inventors: Michael Jones, David Gunn, John Jones, Michael Van Zandt
  • Patent number: 6277849
    Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and isomeric mixtures thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8acycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C8alkenyloxycarbonyl, C1-C5alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl: C2-C12alknyl; C1-C12haloalkyl or a group NR11R12; wherein R11, and R12 are each independently of the other hydrogen, C1-C6alkyl or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8acycloalkyl-C1-C4alkyl or wherein the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are eac
    Type: Grant
    Filed: August 24, 1999
    Date of Patent: August 21, 2001
    Assignee: Syngenta Crop Protection, Inc.
    Inventor: Martin Zeller
  • Publication number: 20010012851
    Abstract: Nitric oxide releasing oxindole prodrugs are described which are useful in methods of treating or preventing pain, inflammation, fever, or gastrointestinal lesions in a patient in need of such treatment, or of modifying an inflammatory disease or condition by favorably affecting the outcome thereof in said patient, wherein there is administered to said patient a therapeutically effective amount of a compound of Formula (I): 1
    Type: Application
    Filed: July 29, 1999
    Publication date: August 9, 2001
    Inventors: KRISTIN M. LUNDY, MICHAEL T. CLARK
  • Patent number: 6245761
    Abstract: This invention provides a series of substituted indoles which are useful in treating or preventing a condition associated with an excess of neuropeptide Y. This invention also provides the novel substituted indoles as well as pharmaceutical formulations with comprise as an active ingredient one or more of these substituted indoles.
    Type: Grant
    Filed: August 29, 1996
    Date of Patent: June 12, 2001
    Assignee: Eli Lilly and Company
    Inventors: Thomas C. Britton, Robert F. Bruns, Jr., Donald R. Gehlert, Philip A. Hipskind, Karen L. Lobb, James A. Nixon, Paul L. Ornstein, Edward C. R. Smith, Hamideh Zarrinmayeh, Dennis M. Zimmerman
  • Patent number: 6242637
    Abstract: The invention relates to compounds of the formula in which: A is a divalent radical selected from: A1) —O—CO— A2) —CH2—O—CO— A3) —O—CH2—CO— A4) —O—CH2—CH2— A5) —N(R1)—CO— A6) —N(R1)—CO—CO— A7) —N(R1)—CH2—CH2— A8) —O—CH2— in which: R1 is a hydrogen or a (C1-C4)-alkyl; and Am is a nitrogen-containing heterocycle.
    Type: Grant
    Filed: October 20, 1998
    Date of Patent: June 5, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: Xavier Emonds-Alt, Isabelle Grossriether, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck
  • Patent number: 6242609
    Abstract: A method for manufacturing a color coupler used in a silver halide photographic light-sensitive material using an ammonium trihalide. Said method for manufacturing the color coupler comprising the following step: a step for halogenating a coupling position of a four equivalent coupler using a halogenating agent, wherein said halogenating agent is said ammonium trihalide.
    Type: Grant
    Filed: April 7, 1999
    Date of Patent: June 5, 2001
    Assignee: Konica Corporation
    Inventor: Fumio Ishii
  • Patent number: 6214790
    Abstract: The invention provides a novel amino acid, neo-tryptophan, as well as polypeptides containing this novel amino acid such as neurotensin analogs. In addition, the invention provides neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and polypeptides containing such derivatives. The invention also provides methods for making neo-tryptophan, neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and compositions containing these compounds. Further, the invention provides methods for inducing a neurotensin response in a mammal as well as methods for treating a mammal having a serotonin recognition molecule.
    Type: Grant
    Filed: April 9, 1999
    Date of Patent: April 10, 2001
    Assignee: Mayo Foundation for Medical Education And Research
    Inventors: Elliott Richelson, Bernadette Marie Cusack, Yuan-Ping Pang, Daniel J. McCormick, Abdul Fauq, Beth Marie Tyler, Mona Boules
  • Patent number: 6204388
    Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof, useful in the treatment of cancer and cancer which has developed a multidrug-resistant phenotype. Also provided are intermediates useful for preparing said epothilones.
    Type: Grant
    Filed: February 24, 1999
    Date of Patent: March 20, 2001
    Assignee: Sloan-Kettering Institute For Cancer Research
    Inventors: Samuel J. Danishefsky, Peter Bertinato, Dai-Shi Su, DongFang Meng, Ting-Chao Chou, Ted Kamenecka, Erik J Sorensen, Aaron Balog, Kenneth A. Savin, Scott Kuduk, Christina Harris, Xiu-Guo Zhang, Joseph R. Bertino
  • Patent number: 6180818
    Abstract: A silver halide photographic material is disclosed, comprising a support having thereon at least one light-sensitive silver halide emulsion layer, wherein said silver halide photographic material contains a compound by formula (IA), or which contains at least one hydroxamic acid compound having a bicyclo ring as a partial structure and represented by formula (IB).
    Type: Grant
    Filed: November 3, 1999
    Date of Patent: January 30, 2001
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Hisashi Mikoshiba, Hiroo Takizawa, Junichiro Hosokawa, Yoshio Ishii, Keiji Mihayashi, Masakazu Morigaki, Mamoru Sakurazawa
  • Patent number: 6150394
    Abstract: Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof.
    Type: Grant
    Filed: July 22, 1998
    Date of Patent: November 21, 2000
    Assignee: Shionogi & Co., Ltd.
    Inventors: Fumihiko Watanabe, Hiroshige Tsuzuki, Mitsuaki Ohtani
  • Patent number: 6114570
    Abstract: A silver halide photographic material is disclosed, comprising a support having thereon at least one light-sensitive silver halide emulsion layer, wherein said silver halide photographic material contains a compound by formula (IA), or which contains at least one hydroxamic acid compound having a bicyclo ring as a partial structure and represented by formula (IB).
    Type: Grant
    Filed: September 2, 1998
    Date of Patent: September 5, 2000
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Hisashi Mikoshiba, Hiroo Takizawa, Junichiro Hosokawa, Yoshio Ishii, Keiji Mihayashi, Masakazu Morigaki, Mamoru Sakurazawa
  • Patent number: 6110957
    Abstract: The present invention relates to novel synthetic methods for the preparation of indolylquinones. The methods of the present invention are directed to synthetic reactions involving indoles and halo-quinones in solvent and in the presence of a metal carbonate. The invention also relates to bis- and mono-indolylquinones of high purity and pharmaceutical compositions containing the same.
    Type: Grant
    Filed: May 5, 1998
    Date of Patent: August 29, 2000
    Assignee: Sugen, Inc.
    Inventors: Peng C. Tang, G. Davis Harris, Jr.
  • Patent number: 6107345
    Abstract: A compound of formula (I): ##STR1## wherein: Z.sub.1, Z.sub.2, Z.sub.3, Z.sub.4, which may be identical or different, represent a group as defined in the description,X represents oxygen, S(O).sub.p, --(CH.sub.2).sub.n -- or --CH.sub.2 --Y--CH.sub.2 -- wherein p, n and Y are as defined in the description,A represents ##STR2## wherein m, R.sub.1, R.sub.2 and G are as defined in the description, their isomers and addition salts thereof with a pharmaceutically-acceptable acid, and medicinal products containing the same are useful in the treatment of diseases like depression, panic attacks, obsessive compulsive disorders, phobias, impulsive disorders, drug abuse or anxiety.
    Type: Grant
    Filed: March 3, 1999
    Date of Patent: August 22, 2000
    Assignee: Adir et Compagnie
    Inventors: Jean-Louis Peglion, Aimee Dessinges, Jean-Christophe Harmange, Mark Millan, Adrian Newman-Tancredi, Mauricette Brocco
  • Patent number: 6090839
    Abstract: The instant invention is concerned with aryl and heteroaryl oxyacetic acid type compounds which are useful antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and related diseases and for lowering triglyceride levels are also disclosed.
    Type: Grant
    Filed: December 19, 1997
    Date of Patent: July 18, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Alan D. Adams, Derek Von Langen, Richard L. Tolman, Hiroo Koyama
  • Patent number: 6063806
    Abstract: A heterocyclic derivative of the formula (I) ##STR1## wherein each symbol is as defined in the specification, and pharmaceutically acceptable salts thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof exhibit superior ACAT inhibitory activity and lipoperoxidation inhibitory activity in mammals, and are useful as ACAT inhibitors and lipoperoxidation inhibitors. Specifically, they are useful for the prophylaxis and treatment of arteriosclerosis, hyperlipemia, arteriosclerosis in diabetes, and cerebrovascular and cardiovascular ischemic diseases.
    Type: Grant
    Filed: April 3, 1998
    Date of Patent: May 16, 2000
    Assignee: Kyoto Pharmaceutical Industries, Ltd.
    Inventors: Shoji Kamiya, Hiroaki Shirahase, Hiroshi Matsui, Shohei Nakamura, Katsuo Wada
  • Patent number: 6004536
    Abstract: The present invention relates to a family of cyanine dyes possessing lipophilic alkyl chains and either one or more reactive functional groups, bromo or chloro, or phenyl, sulfophenyl or polysulfophenyl substituents or combinations thereof. The dyes of the invention are useful for staining membranes in cells or isolated from cells, and are well-retained therein. Additionally, the reactive dyes of the invention are useful for preparing dye-conjugates, thereby conferring the membrane staining ability of the subject dye onto the resulting dye-conjugate.
    Type: Grant
    Filed: August 14, 1996
    Date of Patent: December 21, 1999
    Assignee: Molecular Probes, Inc.
    Inventors: Wai-Yee Leung, Richard P. Haugland, Fei Mao
  • Patent number: 5994379
    Abstract: The present invention relates to inhibitors of COX-2, compositions which contain such compounds and methods of use. The compounds are represented by formula I: ##STR1## and include pharmaceutically acceptable salts and esters thereof.
    Type: Grant
    Filed: February 9, 1999
    Date of Patent: November 30, 1999
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Christopher I. Bayly, Cameron Black, Nathalie Ouimet, David Percival, Serge Leger, Marc Ouellet
  • Patent number: 5981752
    Abstract: Compounds of formula (I): ##STR1## [wherein: R.sup.1 represents halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, cycloalkyl, or cycloalkyloxy; R.sup.2 represents hydrogen or halogen; R.sup.3 represents hydrogen, alkyl, or cycloalkyl; and the dotted line represents a single or double carbon--carbon bond]; and salts thereof have valuable fungicidal activities which make them of considerable value in agriculture and horticulture.
    Type: Grant
    Filed: April 9, 1998
    Date of Patent: November 9, 1999
    Assignee: Sankyo Company, Limited
    Inventors: Hideo Takeshiba, Chiaki Imai
  • Patent number: 5965745
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 AND R.sup.2 are as defined, useful in the treatment of asthma, rheumatoid arthritis, osteoarthritis, bronchitis, chronic obstructive airways diseases, psoriasis, allergic rhinitis, atopic dermatitis, shock, and other inflammatory diseases and for blocking the leucotriene D4 receptor, pharmaceutical compositions containing such compounds and methods of blocking leucotriene D4 receptors using such compositions.
    Type: Grant
    Filed: July 1, 1998
    Date of Patent: October 12, 1999
    Assignee: Pfizer Inc
    Inventors: Matthew F. Brown, Anthony Marfat
  • Patent number: 5936098
    Abstract: This invention concerns a method for the production of a 3-arylindoline compound represented by the general formula ##STR1##
    Type: Grant
    Filed: August 14, 1997
    Date of Patent: August 10, 1999
    Assignee: Tokyo Tanabe Company Limited
    Inventors: Nobuyuki Yasuda, Shin-ichi Kunii, Kouichi Kazama
  • Patent number: 5932743
    Abstract: The present invention relates to novel substituted indole compounds of formula (I) ##STR1## having pharmacological activity, to processes for their preparation, to solid phase methods for preparing libraries of the compounds, to utilizing libraries of the compounds for drug discovery, and to pharmaceutical compositions thereof.
    Type: Grant
    Filed: July 29, 1998
    Date of Patent: August 3, 1999
    Assignee: American Home Products Corporation
    Inventors: Michael D. Collini, John W. Ellingboe