Nitrogen Attached Directed Or Indirectly To Morpholine Ring By Nonionic Bonding Patents (Class 544/162)
  • Patent number: 6608196
    Abstract: Provided are processes for synthesizing structurally diverse pyruvate-derived compounds using a parallel approach on a solid phase support. Examples of such a solid phase support include resins which have also been used in solid phase peptide synthesis.
    Type: Grant
    Filed: May 3, 2002
    Date of Patent: August 19, 2003
    Assignee: Galileo Pharmaceuticals, Inc.
    Inventors: Bing Wang, Satyanarayana Janagani, Wyeth B. Callaway, Jonathan L. Sessler
  • Publication number: 20030149020
    Abstract: The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system.
    Type: Application
    Filed: May 13, 2002
    Publication date: August 7, 2003
    Inventors: Ulf Bremberg, Patrizia Caldirola, Annika J. Jensen, Gary Johansson, Andrew Mott, Lori Sutin, Jan Tejbrant
  • Publication number: 20030144277
    Abstract: The present application describes modulators of CCR3 of formula (I): 1
    Type: Application
    Filed: September 18, 2002
    Publication date: July 31, 2003
    Inventor: George V. DeLucca
  • Publication number: 20030140431
    Abstract: The present patent application relates to 3-(2,5-diaminophenyl)acrylamide derivatives of general formula (I) or to physiologically tolerated, water-soluble-salts thereof 1
    Type: Application
    Filed: October 21, 2002
    Publication date: July 31, 2003
    Inventors: Laurent Chassot, Hans-Juergen Braun
  • Publication number: 20030144276
    Abstract: Described is a heterocycle-containing carboxylic acid derivative represented by the following formula (I): 1
    Type: Application
    Filed: January 6, 2003
    Publication date: July 31, 2003
    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
  • Publication number: 20030138374
    Abstract: A compound represented by the formula (I):
    Type: Application
    Filed: September 20, 2002
    Publication date: July 24, 2003
    Inventors: Yukitsuda Kudo, Masako Suzuki, Takahiro Suemoto, Hiroshi Shimazu
  • Patent number: 6596772
    Abstract: The invention relates to trifluoromethyl sulfonyl and trifluoromethyl sulfonamido compounds and the physiologically acceptable salts and the prodrugs thereof. These compounds are expected to modulate the activity of protein tyrosine enzymes which are related to cellular signal transduction, in particular, protein tyrosine phosphatase, and therefore are expected to be useful in the prevention and treatment of disorders associated with abnormal protein tyrosine enzyme related cellular signal transduction such as cancer, diabetes, immuno-modulation, neurologic degenerative diseases, osteoporosis and infectious diseases. The invention also relates to the use of compounds containing fluoromethyl sulfonyl groups as phosphate mimics. These mimics may be used to inhibit, regulate or modulate the activity of a phosphate binding protein in a cell.
    Type: Grant
    Filed: August 25, 2000
    Date of Patent: July 22, 2003
    Assignee: Sugen, Inc.
    Inventors: Ping Huang, Chung Chen Wei, Peng Cho Tang, Chris Liang, John Ramphal, Bahija Jallal, John Biltz, Sharon Li, Matt Mattson, Gerald McMahon, Marcel Koenig
  • Publication number: 20030130256
    Abstract: The present invention relates to cyclized amide derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.
    Type: Application
    Filed: February 5, 2003
    Publication date: July 10, 2003
    Inventors: David Lauffer, Michael Mullican, Brian Ledford
  • Publication number: 20030130509
    Abstract: The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA)
    Type: Application
    Filed: January 28, 2003
    Publication date: July 10, 2003
    Applicant: Pharmacia & Upjohn Company
    Inventor: Bruce Allen Pearlman
  • Patent number: 6586432
    Abstract: Compounds having the general formula R1R2N—CH2CH2—CHAr1—CH2—NR3—CO—R4   (I) wherein R1, R2, R3, R4 and Ar are as defined in the specification, methods of making such compounds, methods of using such compounds for the treatment of diseases and pharmaceutical compositions comprising such compounds.
    Type: Grant
    Filed: November 1, 2002
    Date of Patent: July 1, 2003
    Assignee: Astrazenela AB
    Inventor: Peter Robert Bernstein
  • Publication number: 20030109523
    Abstract: This invention provides novel bicyclic compounds of Formula (I): 1
    Type: Application
    Filed: June 6, 2002
    Publication date: June 12, 2003
    Applicant: Wyeth
    Inventors: Arie Zask, Diane B. Hauze, Kenneth L. Kees, Richard D. Coghlan, John Yardley
  • Publication number: 20030109700
    Abstract: 1 Compounds of formula (1) wherein R2—C, R3—C, R4—C or R5—C may be replaced by N; and wherein n is 1, 2 or 3; R1 is aryl, heteroaryl or (aryl or heteroaryl)-lower alkoxy; R2, R3, R4 and R5 are independently hydrogen, lower alkyl, lower alkoxy, halo, trifluoromethyl or cyano; R6 is (i) or (ii) m is 1, 2 or 3; R7 is hydrogen, lower alkyl (aryl or heteroaryl)-lower alkyl, lower alkoxy, (aryl or heteroaryl)-lower alkoxy, hydroxy, oxo, lower alkylenedioxy or lower alkanoyloxy; W is O, S or NR8; R8 is —CORa, (iii), —COORd, —SO2Re, hydrogen, optionally substituted lower alkyl, aryl, heteroaryl or (aryl or heteroaryl)-lower alkyl; Ra, Rd and Re, are independently optionally substituted lower alkyl, cycloalkyl, adamantyl, aryl, heteroaryl or (aryl or heteroaryl)-lower alkyl; Rb and Rc are independently hydrogen, cycloalkyl, optionally substituted lower alkyl, aryl, heteroaryl or (aryl or heteroaryl) lower alkyl; or Rb and Rc together represent lower alkylene; and pharmac
    Type: Application
    Filed: July 11, 2002
    Publication date: June 12, 2003
    Inventor: Gary Michael Ksander
  • Publication number: 20030105132
    Abstract: The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2 R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.
    Type: Application
    Filed: March 12, 2002
    Publication date: June 5, 2003
    Inventors: Stephen Challenger, Andrew Simon Cook, Adam Thomas Gillmore, Donald Stuart Middleton, David Cameron Pryde, Alan Stobie
  • Publication number: 20030105099
    Abstract: The present invention relates to novel cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
    Type: Application
    Filed: June 26, 2002
    Publication date: June 5, 2003
    Inventors: Michael Graupe, James T. Palmer, John W. Patterson, Stephen D. Pickett, David J. Aldous, Sukanthini Thurairatnam, Andreas P. Timm, Frank Halley, Justine Lai, John Link, Jiayao Li
  • Publication number: 20030105079
    Abstract: The present invention relates to novel 1,2- or 1,3-diamine and amide compounds and pharmaceutically useful salts thereof and methods for treating central nervous system diseases. The present 1,2- or 1,3-diamine and amide compounds have high binding affinity to the sigma receptor.
    Type: Application
    Filed: June 12, 2002
    Publication date: June 5, 2003
    Inventors: Yong-Moon Choi, Yong-Kil Kim, Chun-Eung Park, Eun-Ho Lee
  • Publication number: 20030105096
    Abstract: The present invention relates to the therapeutic use of non-amine tropane analogues that bind to the SERT to treat neuropsychiatric disorders.
    Type: Application
    Filed: February 28, 2002
    Publication date: June 5, 2003
    Inventors: Bertha K. Madras, Peter C. Meltzer
  • Publication number: 20030105097
    Abstract: The invention provides compounds of formula (I) 1
    Type: Application
    Filed: May 6, 2002
    Publication date: June 5, 2003
    Applicant: Pfizer Inc.
    Inventors: Andrew Simon, Alan Stobie
  • Publication number: 20030105161
    Abstract: There are provided novel compounds of formula (I), 1
    Type: Application
    Filed: August 22, 2002
    Publication date: June 5, 2003
    Inventors: Tim Birkinshaw, David Cheshire, Antonio Mete
  • Publication number: 20030096737
    Abstract: The present invention relates to novel classes of compounds of formula I which are caspase and TNF-alpha 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 caspase and TNF-alpha activity and consequently, can be advantageously used as agents against caspase-, interleukin-1-(“IL-1”), apoptosis-, interferon-&ggr; inducing factor- (IGIF), interferon-&ggr;- (“IFN-&ggr;”), or TNF-alpha mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to processes for preparing the compounds of this invention.
    Type: Application
    Filed: April 19, 2002
    Publication date: May 22, 2003
    Inventors: Anita Diu-Hercend, Julian Golec, Thierry Hercend, Ronald Knegtel, Paul Lang, Andrew Miller, Karen Miller, Michael Mortimore, Peter Weber
  • Publication number: 20030092713
    Abstract: Compounds having the general formula
    Type: Application
    Filed: November 1, 2002
    Publication date: May 15, 2003
    Inventor: Peter Robert Bernstein
  • Publication number: 20030087890
    Abstract: The present application describes novel 1,2-disubsituted cyclic derivatives of formula I: 1
    Type: Application
    Filed: January 9, 2002
    Publication date: May 8, 2003
    Inventors: Chu-Biao Xue, Carl Decicco, Xiaohua He
  • Publication number: 20030078428
    Abstract: Phenylamino benzhydroxamic acid derivatives of formula (I) where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as psoriasis and restenosis.
    Type: Application
    Filed: June 4, 2002
    Publication date: April 24, 2003
    Inventors: Stephen Douglas Barrett, Alexander James Bridges, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Haile Tecle
  • Patent number: 6552025
    Abstract: Compositions, methods of use, isolation and biosynthesis of diimino-piperazine derivatives useful for the modification of sphingolipid metabolism and other biological functions are described. The preferred derivative is 2,6-bis-(&ohgr;-aminobutyl)-3,5-diimino-piperazine. This is a naturally occurring biochemical compound isolated from cells. The diimino-piperazine derivatives are useful as therapeutic agents when administered to patients to treat diseases and disorders involving cell regulation.
    Type: Grant
    Filed: November 17, 2000
    Date of Patent: April 22, 2003
    Assignee: Emory University
    Inventors: Alfred H. Merrill, Jr., Lisa Warden, Dennis C. Liotta
  • Patent number: 6545152
    Abstract: Novel chiral derivitaves of non-nucleoside inhibitors (NNI), particularly R-isomers of halopyridyl and thiazoyl thiourea compounds are provided as potent inhibitors of reverse transcriptase (RT), and particularly of retroviral RT, most particularly HIV RT. The stereospecific compounds and compositions of the invention inhibit replication of retrovirus, particularly human immunodeficiency virus-1 (HIV-1) and drug resistant strains.
    Type: Grant
    Filed: July 18, 2000
    Date of Patent: April 8, 2003
    Assignee: Parker Hughes Institute
    Inventors: Fatih M. Uckun, Taracad K. Venkatachalam
  • Publication number: 20030065170
    Abstract: This invention relates to novel compounds of Formula (I) to (VII), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
    Type: Application
    Filed: September 5, 2002
    Publication date: April 3, 2003
    Inventors: Katherine Louisa Widdowson, Qi Jin
  • Patent number: 6541505
    Abstract: This invention is directed to an (aminoiminomethyl or aminomethyl)benzoheteroaryl compound of formula I which is useful for inhibiting the activity of Factor Xa by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.
    Type: Grant
    Filed: June 30, 2000
    Date of Patent: April 1, 2003
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: William P. Dankulich, Daniel G. McGarry, Christopher Burns, Timothy F. Gallagher, Francis A. Volz
  • Publication number: 20030050298
    Abstract: This invention relates to novel compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
    Type: Application
    Filed: September 5, 2002
    Publication date: March 13, 2003
    Inventors: Michael R Palovich, Katherine L Widdowson, Hong Nie
  • Patent number: 6531471
    Abstract: This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: December 14, 2001
    Date of Patent: March 11, 2003
    Assignee: Synaptic Pharmaceutical Corporation
    Inventors: Bharat Lagu, Dhanapalan Nagarathnam, Dake Tian, Charles Gluchowski
  • Publication number: 20030045478
    Abstract: This invention encompasses the novel compounds of Formula I, which are useful in the treatment of caspase-3 mediated diseases.
    Type: Application
    Filed: December 14, 2001
    Publication date: March 6, 2003
    Inventors: Yongxin Han, Renee Aspiotis, Andre Giroux, Erich L. Grimm, Christophe Mellon, Robert Zamboni, Christopher I. Bayly
  • Publication number: 20030032802
    Abstract: This invention relates to the novel use of dianilino squarates in the treatment of disease states mediated by the chemokine, Interteukin-8 (IL-8).
    Type: Application
    Filed: August 30, 2002
    Publication date: February 13, 2003
    Inventors: Michael R. Palovich, Joseph Weinstock, Katherine L. Widdowson
  • Publication number: 20030032803
    Abstract: The present application describes novel amides and derivatives thereof of formula 1
    Type: Application
    Filed: February 12, 2002
    Publication date: February 13, 2003
    Inventors: Jingwu Duan, Carl P. Decicco, David J. Nelson, Chu-Biao Xue
  • Patent number: 6514996
    Abstract: An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)—C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z represents C
    Type: Grant
    Filed: November 19, 1997
    Date of Patent: February 4, 2003
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Ohshima, Takashi Kawakita, Koji Yanagawa, Kyoichiro Iida, Rie Koike, Yoshisuke Nakasato, Tohru Matsuzaki, Kenji Ohmori, Soichiro Sato, Hidee Ishii, Haruhiko Manabe, Michio Ichimura, Fumio Suzuki
  • Publication number: 20030013846
    Abstract: Certain known and novel pyruvate derivatives are particularly active in restoring or preserving metabolic integrity in oxidatively competent cells that have been subjected to oxygen deprivation. These pyruvate-derived compounds include, but are not limited to oximes, amides, pyruvate analogues, modified pyruvate analogues, esters of pyruvate (e.g., polyol-pyruvate esters, pyruvate thioesters, glycerol-pyruvate esters and dihydroxyacetone-pyruvate esters). Such pyruvate derivatives (including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof) are useful in the manufacture of pharmaceutical compositions for treating a number of conditions characterized by oxidative stress.
    Type: Application
    Filed: May 3, 2002
    Publication date: January 16, 2003
    Inventors: Bing Wang, Guy Miller, Satyanarayana Janagani, Wei Zhang
  • Publication number: 20030013847
    Abstract: Certain known and novel pyruvate derivatives are particularly active in restoring or preserving metabolic integrity in oxidatively competent cells that have been subjected to oxygen deprivation. These pyruvate-derived compounds include, but are not limited to oximes, amides, pyruvate analogues, modified pyruvate analogues, esters of pyruvate (e.g., polyol-pyruvate esters, pyruvate thioesters, glycerol-pyruvate esters and dihydroxyacetone-pyruvate esters). Such pyruvate derivatives (including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof) are useful in the manufacture of pharmaceutical compositions for treating a number of conditions characterized by oxidative stress.
    Type: Application
    Filed: May 3, 2002
    Publication date: January 16, 2003
    Inventors: Bing Wang, Guy Miller, Wei Zhang, Satyanarayana Janagani, Jiangao Song
  • Publication number: 20030009029
    Abstract: The present invention relates to a process preparing compounds of the general formula (I) 1
    Type: Application
    Filed: June 5, 2002
    Publication date: January 9, 2003
    Applicant: Merck Patent GmbH
    Inventors: Herwig Buchholz, Urs Welz-Biermann
  • Publication number: 20030004151
    Abstract: The present application describes modulators of MCP-1 of formula (I): 1
    Type: Application
    Filed: December 20, 2001
    Publication date: January 2, 2003
    Inventor: Robert Cherney
  • Patent number: 6500823
    Abstract: The object of the invention consists of novel unsaturated hydroximic acid derivatives, the process for their preparation and as active substance such as compounds containing pharmaceutical compositions. The novel compounds possess valuable pharmaceutical effects, so they can be used in the treatment of states connected with energy deficiency of the cell caused by PARP inhibition, in diabetes complications, in oxygen deficient status of the heart and brain, in neurodegenerative diseases, in the treatment of autoimmune and/or viral diseases. In formula (I).
    Type: Grant
    Filed: March 2, 2001
    Date of Patent: December 31, 2002
    Assignee: N-Gene Research Laboratories, Inc.
    Inventors: Péter Literáti Nagy, Kálmán Takács, Balázs Sümegi
  • Publication number: 20020198200
    Abstract: Substituted benzene acetamide compounds and pharmaceutically acceptable salts thereof are useful as glucokinase activators.
    Type: Application
    Filed: June 25, 2002
    Publication date: December 26, 2002
    Inventors: Robert F. Kester, Ramakanth Sarabu
  • Publication number: 20020198378
    Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Application
    Filed: December 11, 2001
    Publication date: December 26, 2002
    Applicant: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • 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
  • Publication number: 20020183260
    Abstract: Compounds of the formula 1
    Type: Application
    Filed: May 9, 2002
    Publication date: December 5, 2002
    Inventor: Cynthia Anne Fink
  • Publication number: 20020173507
    Abstract: Selected novel urea compounds are effective for prophylaxis and treatment of diseases, such as cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving stoke, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Application
    Filed: August 14, 2001
    Publication date: November 21, 2002
    Inventors: Vincent Santora, Benny Askew, Arup Ghose, Andrew Hague, Tae Seong Kim, Ellen Laber, Aiwen Li, Brian Lian, Gang Liu, Mark Norman, Leon Smith, Andrew Tasker, Christopher Tegley, Kevin Yang
  • Publication number: 20020169159
    Abstract: Compounds, compositions and methods that are useful in the treatment of inflammatory and immune conditions and diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of a chemokine receptor. The subject methods are useful for the treatment of inflammatory and immunoregulatory disorders and diseases, such as multiple sclerosis, rheumatoid arthritis and type I diabetes.
    Type: Application
    Filed: December 11, 2001
    Publication date: November 14, 2002
    Applicant: Tularik Inc.
    Inventors: Julio C. Medina, Michael G. Johnson, An-Rong Li, Jiwen Liu, Alan Xi Huang, Liusheng Zhu, Andrew P. Marcus
  • Patent number: 6479491
    Abstract: The present invention relates to compounds of formula (I), any of it enantiomers, or any mixture thereof, or a pharmaceutically acceptable acid addition salt thereof, wherein R1, R2, R3, R4, R11, R12, R13, R14 and R15 each independently are hydrogen, alkyl, alkoxy, halogen, trifluoromethyl, nitro, cyano, amino, acyl, alkylamino, dialkylamino, aminocarbonyl, or acylamino; R5 is hydrogen, alkyl, alkoxyalkyl, or phenylalkyl; X is —CH2—Z—, Z—CH2—, NH—CO—, —CO—NH—, or —CH═CH—; wherein Z is O, S, CH2, or NH; Y is O, —CH2—W—, —W—CH2—; wherein W is O, or S; and n is 0, 1 or 2. The compounds are useful in the treatment of psychotic disorders.
    Type: Grant
    Filed: November 13, 2000
    Date of Patent: November 12, 2002
    Assignee: Neurosearch A/S
    Inventors: Oskar Axelsson, Dan Peters, Jorgen Scheel-Kruger, Elsebet Ostergaard Nielsen
  • Publication number: 20020165222
    Abstract: The present invention provides 7-14 membered ring ether protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.
    Type: Application
    Filed: July 2, 2002
    Publication date: November 7, 2002
    Applicant: SmithKline Beecham Corporation
    Inventors: Robert Wells Marquis, Daniel Frank Veber
  • Publication number: 20020160961
    Abstract: Compositions comprising TRH and a compound of the general formula A—B—C—D(—E)p are used for treating the catabolic state of prolonged critical illness.
    Type: Application
    Filed: December 4, 2001
    Publication date: October 31, 2002
    Inventor: Michael Ankersen
  • Publication number: 20020144361
    Abstract: Couplers for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): 1
    Type: Application
    Filed: January 18, 2002
    Publication date: October 10, 2002
    Inventors: Mu-lll Lim, Yuh-Guo Pan, Gottfried Wenke
  • Publication number: 20020143011
    Abstract: Compounds of general formula (1) are described: 1
    Type: Application
    Filed: March 14, 2001
    Publication date: October 3, 2002
    Applicant: Celltech Therapeutics, Limited
    Inventors: Graham John Warrellow, Ewan Campbell Boyd, Rikki Peter Alexander
  • Publication number: 20020143176
    Abstract: Compounds having the formula (I), 1
    Type: Application
    Filed: November 29, 2001
    Publication date: October 3, 2002
    Inventors: Chunjian Liu, T.G. Murali Dhar, Henry H. Gu, Edwin J. Iwanowicz, Katerina Leftheris, William J. Pitts, Timothy F. Herpin, Zulan Pi, Gregory S. Bisacchi
  • Publication number: 20020137736
    Abstract: There are provided novel compounds of formula (I) 1
    Type: Application
    Filed: February 27, 2001
    Publication date: September 26, 2002
    Inventors: Kenneth Mattes, Robert Murray, Eifion D Phillips, Hans Schmitthenner