Nitrogen Attached Indirectly To The Piperidine Ring By Nonionic Bonding Patents (Class 546/229)
  • Patent number: 6525069
    Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
    Type: Grant
    Filed: June 21, 2000
    Date of Patent: February 25, 2003
    Assignee: Bristol-Myers Squibb Pharma Co.
    Inventors: Soo S. Ko, George V. Delucca, John V. Duncia, Ui Tae Kim, Dean A. Wacker, Changsheng Zheng
  • 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
  • Patent number: 6509356
    Abstract: A class of substituted benzylnaphthylene compounds of the structure where R1 and R2 are independently hydrogen, alkyl of one to six carbon atoms, acyl of two to six carbon atoms, or phenacyl; X is —(CH2)1-6; Y is absent or is selected from 1,4-piperazinylene; ureido; N-(lower alkyl)ureido; N′-(lower alkyl)ureido; or N, N′-(di-lower alkyl ureido; and Z is 1-, 2- or 3-pyrrolidinyl; 1-, 2-, or 3-[1-(lower alkyl) pyrrolidinyl]; 1- 2-, 3- or 4-piperidinyl; 1-, 2-, 3- or 4-[1-lower alkyl)piperidinyl]; N,N-dialkyl; 1-azepinyl; 1- or 2-naphthylamino, 4-morpholinyl, dimethyl-4-morpholinyl, 3-azaspiro[5.
    Type: Grant
    Filed: August 4, 1998
    Date of Patent: January 21, 2003
    Assignee: Eli Lilly and Company
    Inventors: Jeffrey Alan Dodge, Andrew Lawrence Glasebrook, Charles Willis Lugar, III
  • Publication number: 20030013720
    Abstract: In one embodiment, this invention provides a novel class of compounds as antagonists of the MCH receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more of the compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention or amelioration or one or more of diseases associated with the MCH receptor.
    Type: Application
    Filed: April 10, 2002
    Publication date: January 16, 2003
    Applicant: PHARMACOPEIA, INC.
    Inventors: Douglas W. Hobbs, Tao Guo, Rachael C. Hunter, Huizhong Gu, Suresh D. Babu, Yuefei Shao
  • 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: 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
  • Patent number: 6498169
    Abstract: A cyclic amine compound represented by the following general formula (1): wherein, R1, R2 and R3 each independently represent a hydrogen atom or an alkoxy group; W1 an W2 each independently represent N or CH; X represents O, NR4, CONR4 or NR4CO; R4 each independently represents a hydrogen atom, or an alkyl, aryl, heteroaryl, aralkyl, or heteroalkyl group; and l, m and n each represents a number of 0 to 1, a salt thereof and a hydrate thereof are provided. These compounds have inhibitory effects on both cell adhesion and cell infiltration and are useful as anti-asthmatic agents, anti-allergic agents, anti-rheumatic agents, anti-arteriosclerotic agents, anti-inflammatory agents, anti-Sjogren's syndrome agents or the like.
    Type: Grant
    Filed: October 26, 2001
    Date of Patent: December 24, 2002
    Assignee: Kowa Co., Ltd.
    Inventors: Tatsuhiko Kodama, Masahiro Tamura, Toshiaki Oda, Yukiyoshi Yamazaki, Masahiro Nishikawa, Shunji Takemura, Takeshi Doi, Yoshinori Kyotani, Masao Ohkuchi
  • Publication number: 20020188130
    Abstract: This disclosure relates to the use of &agr;,&agr;-dibromo-&agr;-chloroacetophenone compounds as intermediates for the preparation of aromatic carbonyl compounds, especially aromatic amides. The compound 2,5-bis(2,2,2-trifluoroethoxy)-&agr;,&agr;-dibromo-&agr;-chloro-acetophenone is especially useful as an intermediate for the preparation of flecainide, a known pharmaceutical.
    Type: Application
    Filed: May 8, 2002
    Publication date: December 12, 2002
    Inventors: Anup K. Ray, Hiren Patel, Shilpa V. Merai, Mahendra R. Patel
  • Patent number: 6492394
    Abstract: A compound of the Formula (I): wherein Z, R1, R, and Ar2 are as defined in the specification. This invention also relates to sulfonamide compounds of the Formula (I) that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use, and methods for preparing the compounds.
    Type: Grant
    Filed: December 22, 1999
    Date of Patent: December 10, 2002
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Roland Joseph Billledeau, Chris Allen Broka, Jeffrey Allen Campbell, Jian Jeffrey Chen, Sharon Marie Dankwardt, Nancy Delaet, Leslie Ann Robinson, Keith Adrian Murray Walker
  • Patent number: 6492400
    Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
    Type: Grant
    Filed: December 17, 1999
    Date of Patent: December 10, 2002
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Soo S. Ko, George V. DeLucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker, Ui Tae Kim
  • 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: 20020177721
    Abstract: One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invention relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in the synthesis of compounds useful for treatment of numerous ailments, conditions and diseases that afflict mammals, including but not limited to addiction and pain. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the substituted piperidines using the methods of the present invention. An additional aspect of the present invention relates to enantiomerically substituted pyrrolidines, piperidines, and azepines.
    Type: Application
    Filed: December 4, 2001
    Publication date: November 28, 2002
    Inventors: Brian M. Aquila, Thomas D. Bannister, Gregory C. Cuny, James R. Hauske, Michele L.R. Heffernan, Michael Z. Hoemann, Donald W. Kessler, Liming Shao, Xinhe Wu, Roger L. Xie
  • 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
  • Patent number: 6479514
    Abstract: Compounds of formula (I) in which the substituents and symbols have the meanings indicated in the description, are suitable for the control of Helicobacter bacteria.
    Type: Grant
    Filed: November 17, 2000
    Date of Patent: November 12, 2002
    Assignee: Altana Pharma AG
    Inventors: Peter Zimmerman, Gerhard Grundler
  • Patent number: 6476226
    Abstract: This invention relates to novel isoxazolines and isoxazoles of formula (I): or a pharmaceutically acceptable salt or prodrug form thereof. The invention relates to novel isoxazolines which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.
    Type: Grant
    Filed: July 13, 2001
    Date of Patent: November 5, 2002
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Joanne M. Smallheer, Shuaige Wang, Prabhakar Kondaji Jadhav
  • Patent number: 6476054
    Abstract: The present invention is directed to cyclic amines of the formula I: (wherein R1, R2, R3, m and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.
    Type: Grant
    Filed: October 17, 2000
    Date of Patent: November 5, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Charles G. Caldwell, Paul E. Finke, Malcolm Maccoss, Sander G. Mills, Bryan Oates, Dooseop Kim, Shankaran Kothandaraman, Liping Wang
  • Patent number: 6472397
    Abstract: The compounds represented by the formula (I), and pharmacologically acceptable salts and solvates thereof are disclosed. The compound is hydrolyzed in organisms into a compound represented by the formula in which W represents a hydrogen atom, and D represents the group —V—(CH2)p—COOR, wherein R represents a hydrogen atom. The compound inhibits the aggregation of platelets via the inhibition of the linkage of the platelet membrane protein GPIIb/IIIa to fibrinogen. wherein A represents CH2 or CO, B represents the group —(CH2)k— or —(CH2)m—CO—, X and Y are different from each other and represent N or CH, W represents an ester moiety which can be removed under the physiological condition, and Z represents the groups (II) or (III): wherein D represents the group —V—(CH2)p—COOR.
    Type: Grant
    Filed: November 3, 2000
    Date of Patent: October 29, 2002
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Kazumi Ota, Kazuko Kobayashi, Tomoaki Miura, Takahiro Imai, Kazumasa Aizawa, Hisashi Suzuki, Shokichi Ohuchi, Kiyoaki Katano, Takashi Ando
  • Publication number: 20020156113
    Abstract: Compound of formula (I): 1
    Type: Application
    Filed: January 16, 2002
    Publication date: October 24, 2002
    Inventors: Patrick Casara, Thierry Le Diguarher, Gilbert Dorey, John Hickman, Alain Pierre, Gordon Tucker, Nicolas Guilbaud
  • Publication number: 20020151712
    Abstract: A series of 3-pyrrolidinyloxy-3′-pyridyl ether compounds, a method for selectively controlling neurotransmitter release in mammals using these compounds, and pharmaceutical compositions including these compounds. Preferred compounds are 3-pyrrolidinylmethoxy-3′-(5′-and/or 6′-substituted) pyridyl ethers.
    Type: Application
    Filed: March 19, 2002
    Publication date: October 17, 2002
    Inventors: Nan-Horng Lin, Yihong Li, Irene Drizin, John F. Kincaid, Anwer Basha, Liming Dong, Ahmed A. Hakeem
  • Publication number: 20020151545
    Abstract: Compounds of formula I and II, 1
    Type: Application
    Filed: November 7, 2001
    Publication date: October 17, 2002
    Inventors: Gregory S. Bisacchi, James C. Sutton, Shung C. Wu
  • Publication number: 20020151566
    Abstract: PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs.
    Type: Application
    Filed: January 22, 2002
    Publication date: October 17, 2002
    Applicant: MEMORY PHARMACEUTICALS CORP.
    Inventors: Richard A. Schumacher, William F. Brubaker, Michael De Vivo, Hans-Jurgen Ernst Hess, Allen Hopper, Ashok Tehim, Ruiping Liu, Axel Unterbeck
  • 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: 20020147345
    Abstract: The present invention provides non-peptidic amino derivatives, their therapeutic use as well as pharmaceutical compositions that possess activity as Follicle Stimulating Hormone (FSH) agonists and are useful in the for treatment of infertility. In particular, the invention provides cyclic and acyclic alpha- and beta-aminocarboxamides, more particularly tetrahydroisoquinolinecarboxamides, piperidinecarboxamides, pyrrolidinecarboxamides, and 2-amino-3-carboxamidopyridine derivatives.
    Type: Application
    Filed: May 28, 2002
    Publication date: October 10, 2002
    Inventors: Nabil El Tayer, Adulla Reddy, David Buckler, Sharad Magar
  • Publication number: 20020137934
    Abstract: A new ligands that include a benzene ring in the backbone can be combined with a metal or metal precursor compound or formed into a metal-ligand complex catalyze a number of different chemical transformations, including olefin polymerization reactions. The ligands, complexes formed with the ligands and compositions including the ligands are useful catalysts, depending on the reaction.
    Type: Application
    Filed: September 18, 2001
    Publication date: September 26, 2002
    Applicant: Symyx Technologies
    Inventors: Anil Guram, Cheryl Lund, Howard W. Turner, Tetsuo Uno
  • Patent number: 6455545
    Abstract: Compounds of general formula (I) are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.
    Type: Grant
    Filed: January 18, 2001
    Date of Patent: September 24, 2002
    Assignee: AstraZeneca Canada Inc.
    Inventors: Daniel Delorme, Edward Roberts, Zhongyong Wei
  • Patent number: 6455560
    Abstract: This invention relates to novel isoxazolines of formula (I): or a pharmaceutically acceptable salt form thereof. This invention also relates to novel isoxazolines of formula (I) which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.
    Type: Grant
    Filed: July 13, 2001
    Date of Patent: September 24, 2002
    Inventors: John Wityak, Prabhakar K. Jadhav
  • Patent number: 6452013
    Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R1 is C1-6alkyloxy, C2-6alkenyloxy or C2-6alkynyl-oxy; R2 is hydrogen, C1-6alkyl C1-6alkyloxy; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl, or L is a radical of formula —Alk—R6—, Alk—X—R7, -Alk-Y—C(═O)—R9, or -Alk-Y—C(═O)—NR11R12 wherein each Alk is C1-12alkanediyl; and R6 is hydrogen, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, or a heterocyclic ringsystem; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, or a heterocyclic ringsystem; X is O, S, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy or hydroxy; Y is NR10 or a direct bond; said R10 being hydrogen, or C1-6alkyl; R11 an
    Type: Grant
    Filed: January 5, 2000
    Date of Patent: September 17, 2002
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jean-Paul René Marie André Bosmans, Michel Anna Jozef De Cleyn, Michel Surkyn
  • Publication number: 20020123494
    Abstract: One embodiment of the present invention relates to acylaminoalkyl-substituted benzenesulfonamide derivatives of the formula (I), 1
    Type: Application
    Filed: November 2, 2001
    Publication date: September 5, 2002
    Inventors: Holger Heitsch, Heinrich Christian Englert
  • Patent number: 6444686
    Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
    Type: Grant
    Filed: December 17, 1999
    Date of Patent: September 3, 2002
    Assignee: Brsitol-Myers Squibb Pharma Company
    Inventors: Soo S. Ko, George V. DeLucca, John V. Duncia, Ui Tae Kim, Joseph B. Santella, III, Dean A. Wacker
  • Publication number: 20020120146
    Abstract: The present invention is directed to compounds of the formula I: 1
    Type: Application
    Filed: February 14, 2002
    Publication date: August 29, 2002
    Inventors: Paul E. Finke, Kerry A. Hilfiker, Malcolm MacCoss, Kevin T. Chapman, Jennifer L. Loebach, Sander G. Mills, Ravi N. Guthikonda, Shrenik K. Shah, Dooseop Kim, Dong-Ming Shen, Bryan Oates
  • Publication number: 20020119960
    Abstract: Compounds, compositions, and methods for treating multidrug resistance are disclosed. Suitable compounds are 2-substituted heterocyclic compounds.
    Type: Application
    Filed: December 19, 2000
    Publication date: August 29, 2002
    Inventors: Charles Raymond Degenhardt, David Joseph Eickhoff
  • Patent number: 6440440
    Abstract: This invention concerns compounds of formula. stereochemically isomeric forms thereof, acid or base addition salts thereof, N-oxides thereof, or quaternary ammonium derivatives thereof, wherein the dotted line is an optional bond; X is a direct bond when the dotted line represents a bond, or X is hydrogen or hydroxy, when the dotted line does not represent a bond; R1, R2, R5 and R6 are each independently selected from hydrogen, halo, hydroxy, C1-4alkyl, C1-4alkyloxy, —SO3H, and the like; R3 and R4 are each independently selected from hydrogen, halo, hydroxy, C1-4alkyl, C1-4alkyloxy, nitro, amino, cyano, trifluoromethyl, or trifluoromethoxy; L is a radical of formula wherein A1 is a direct bond or C1-6alkanediyl; A2 is C2-6alkanediyl; and R7 to R11 are hydrogen, C1-6alkyl, aminoC1-6alkyl and the like; having biocidal properties; their preparation, compositions containing them and their use as a biocide.
    Type: Grant
    Filed: September 22, 2000
    Date of Patent: August 27, 2002
    Inventors: Lieven Meerpoel, Mark Arthur Josepha Van der Flaas, Louis Jozef Elisabeth Van Der Veken, Jan Heeres
  • Patent number: 6441177
    Abstract: Tertiary amines of the formula wherein A1, A2, A3, A4, M, p, T and Q are as defined herein, and acid addition salts thereof, have antimycotic and cholesterol-lowering activity.
    Type: Grant
    Filed: December 16, 1999
    Date of Patent: August 27, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Henrietta Dehmlow, Jacques Himber, Synèse Jolidon, Hans Lengsfeld, Olivier Morand, Gérard Schmid, Yu-Hua Ji
  • Patent number: 6436962
    Abstract: Arylhydantoin derivatives and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
    Type: Grant
    Filed: September 27, 2000
    Date of Patent: August 20, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Jacob M. Hoffman, Mark G. Bock, Robert M. DiPardo, Linda S. Payne, Michael A. Patane
  • Patent number: 6436925
    Abstract: Benzamides of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: R1—C1-C6-alkyl, branched or unbranched, where one of the C atoms in this chain may be substituted by a phenyl ring, cyclohexyl ring, indolyl ring and an SCH3 group, and the phenyl ring in turn is substituted by by [sic] a maximum of two R4 radicals, where R4 [lacuna] hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, NHCO—C1-C4-alkyl, and R2 can be NR5CO—R6 and NHR5SO2—R6, and R3 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl, CN, COOH, CONH2, COO—C1-C4-alkyl, SO2—C1-C4-alkyl, —SO2Ph, SO2NH—C1-C4-alkyl, iodine, SO2NH2 and NH2, and A can be arom
    Type: Grant
    Filed: October 3, 2000
    Date of Patent: August 20, 2002
    Assignee: Abbott Laboratories
    Inventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber, Monika Knopp
  • Publication number: 20020111368
    Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
    Type: Application
    Filed: April 18, 2001
    Publication date: August 15, 2002
    Inventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L. Brown, Joseph J. McDonald
  • Patent number: 6429213
    Abstract: The present application de gibes novel cyclic hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NRa, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as metalloprotease inhibitors.
    Type: Grant
    Filed: June 17, 1999
    Date of Patent: August 6, 2002
    Inventors: Chu-Biao Xue, Carl P. Decicco, Xiaohua He
  • Publication number: 20020103205
    Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) 1
    Type: Application
    Filed: July 11, 2001
    Publication date: August 1, 2002
    Inventors: Derek Lowe, Wei Chang, Joseph Kozlowski, Joel G. Berger, Robert McQuade, Allen Barnett, Margaret Sherlock, Wing Tom, Sundeep Dugar, Lian-Yong Chen, John W. Clader, Samuel Chackalamannil, Wang Yuguang, Stuart W. McCombie, Jayaram R. Tagat, Susan F. Vice, Wayne Vaccaro, Michael J. Green, Margaret E. Browne, Theodros Asberom
  • Publication number: 20020099214
    Abstract: There is provided a compound of formula I, 1
    Type: Application
    Filed: March 27, 2002
    Publication date: July 25, 2002
    Applicant: Pfizer Inc.
    Inventors: Stephen Paul Gibson, Ivan Tommasini, David Morris Gethin, Richard Edward Armer
  • Publication number: 20020099216
    Abstract: There is provided a compound of formula I, 1
    Type: Application
    Filed: March 27, 2002
    Publication date: July 25, 2002
    Applicant: Pfizer Inc.
    Inventors: Stephen Paul Gibson, Ivan Tommasini, David Morris Gethin, Richard Edward Armer
  • Publication number: 20020082452
    Abstract: The invention relates to &agr;-sulfin- and &agr;-sulfonamino acid amides of the general formula I 1
    Type: Application
    Filed: June 1, 2001
    Publication date: June 27, 2002
    Inventors: Martin Zeller, Andre Jeanguenat, Clemens Lamberth
  • Publication number: 20020052509
    Abstract: Calcilytic compounds and compositions and their use in treating abnormal bone or mineral homeostasis.
    Type: Application
    Filed: December 4, 2001
    Publication date: May 2, 2002
    Applicant: SmithKline Beecham Corporation
    Inventors: Pradip Kumar Bhatnagar, James Francis Callahan, Eric G. Del Mar, Maria Amparo Lago
  • Patent number: 6376673
    Abstract: The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salt thereof; wherein R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or 2-hydroxyethyl; R3 is —CR′═NOR″ wherein R′ and R″ each independently are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, cycloalkylalkenyl, alkynyl, cycloalkylalkynyl, aryl or benzyl; R4 is phenyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, amino, nitro, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, aryl and heteroaryl; 3,4-methylenedioxyphenyl; benzyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, amino, nitro, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, aryl and heteroaryl; heteroaryl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, amino, nitro, alkox
    Type: Grant
    Filed: October 12, 1999
    Date of Patent: April 23, 2002
    Assignee: Neurosearch A/S
    Inventors: Peter Moldt, Frank Watjen, Jorgen Scheel-Kruger
  • Publication number: 20020042431
    Abstract: The present invention is directed to certain novel compounds represented by structural formula I: 1
    Type: Application
    Filed: September 21, 2001
    Publication date: April 11, 2002
    Inventors: Paul E. Finke, Laura C. Meurer, Sander G. Mills, Malcolm MacCoss, Hongbo Qi
  • Patent number: 6358979
    Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R3, R4, R5, R6, R7, R8, X, n, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
    Type: Grant
    Filed: June 8, 2000
    Date of Patent: March 19, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Paul E. Finke, Kerry A. Hilfiker, Malcolm MacCoss, Kevin T. Chapman, Jennifer L. Loebach, Sander G. Mills, Ravi N. Guthikonda, Shrenik K. Shah, Dooseop Kim, Dong-Ming Shen, Bryan Oates
  • Publication number: 20020028833
    Abstract: Aryl alkenamides derivatives of Formula I or a pharmaceutically acceptable salt thereof are novel MCP-1 antagonists and are thus useful in the treatment of inflammation, atherosclerosis, restenosis, and immune disorders such as arthritis and transplant rejection 1
    Type: Application
    Filed: August 12, 1997
    Publication date: March 7, 2002
    Inventors: RICHARD JOHN BOOTH, KENNETH GORDON CARSON, DAVID THOMAS CONNOR, ROBERTA ELLEN GLYNN, BRUCE DAVID ROTH, CHARLES F. SCHWENDER, BHARAT KALIDAS TRIVEDI, PAUL CHARLES UNANGST
  • Patent number: 6350909
    Abstract: The invention relates to new imides, to a plurality of processes for their preparation and to their use as fungicides.
    Type: Grant
    Filed: January 2, 2001
    Date of Patent: February 26, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Heinemann, Herbert Gayer, Peter Gerdes, Martin Vaupel, Astrid Mauler-Machnik, Gerd Hänssler, Klaus Stenzel, Martin Kugler, Thomas Jaetsch, Peter Wachtler
  • Publication number: 20020019374
    Abstract: Salicylohydrazide derivatives of the formula I 1
    Type: Application
    Filed: June 14, 2001
    Publication date: February 14, 2002
    Inventors: Andreas Gypser, Thomas Grote, Joachim Rheinheimer, Ingo Rose, Peter Schafer, Oliver Cullmann, Markus Gewehr, Wassilios Grammenos, Jordi Tormo i Blasco, Bernd Muller, Hubert Sauter, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
  • Publication number: 20020016337
    Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.
    Type: Application
    Filed: March 2, 2001
    Publication date: February 7, 2002
    Inventors: Gregory D. Cuny, Liming Shao, James R. Hauske, Michele L.R. Heffernan, Brian M. Aquila, Xinhe Wu, Fengjiang Wang, Thomas D. Bannister
  • Patent number: 6342607
    Abstract: This invention relates to 3-(3-phenyl-2,6-dioxopiperidin-3-yl)propionamide derivatives, and to processes for preparing the same.
    Type: Grant
    Filed: June 12, 2001
    Date of Patent: January 29, 2002
    Assignee: Sanofi-Synthelabo
    Inventors: Bertrand Castro, Hélène Mattras, Aldo Previero