Plural Piperidine Rings Patents (Class 546/186)
  • Publication number: 20040006085
    Abstract: This invention is directed to a class of compounds (Formula I) including hydroxyalkanoyl amino pyrazoles, hydroxyalkanoyl amino thiadiazoles, hydroxyalkanoyl amino acid esters, hydroxyalkanoyl amino acid amides, hydroxyalkanoyl amino alcohols, hydroxyalkanoyl amino ketoes, hydroxyalkanoyl amino hydantoins, hydroxyalkanoyl anilines, and hydroxyalkanoyl derivatives of privileged structures. The invention is also directed to a pharmaceutical formation comprising such compound in a pharmaceutically acceptable salt form or prodrug thereof. The invention is further directed to a method for inhibiting &bgr;-amyloid peptide release and/or synthesis, a method for inhibiting &ggr;-secretase activity and a method for treating neurological disorders associated with &bgr;-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.
    Type: Application
    Filed: January 31, 2003
    Publication date: January 8, 2004
    Inventors: Jay S. Tung, Ashley C. Guinn, Gene Thorsett, Mike A. Pleiss
  • Publication number: 20040006081
    Abstract: Compounds of formula (I), compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).
    Type: Application
    Filed: December 10, 2002
    Publication date: January 8, 2004
    Inventors: Jeremy Burrows, Anne Cooper, John Cumming, Thomas McInally, Howard Tucker
  • Publication number: 20040006106
    Abstract: Peptide mimetic small molecule inhibitors of Sur-2 are provided having the general formula: 1
    Type: Application
    Filed: April 2, 2003
    Publication date: January 8, 2004
    Applicant: Baylor College of Medicine
    Inventors: Motonari Uesugi, Shinichi Asada
  • Publication number: 20040006089
    Abstract: A subject of the present application is new derivatives of 4-aminopiperidines of formula 1
    Type: Application
    Filed: May 23, 2002
    Publication date: January 8, 2004
    Inventors: Christophe Thurieau, Jerome Gonzalez, Christhope Moinet
  • Publication number: 20030236283
    Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
    Type: Application
    Filed: December 11, 2002
    Publication date: December 25, 2003
    Inventors: Heike Radeke, Liming Shao
  • Patent number: 6656954
    Abstract: A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
    Type: Grant
    Filed: November 29, 2001
    Date of Patent: December 2, 2003
    Assignee: Pharmacia Corporation
    Inventors: Louis J. Bedell, Joseph J. McDonald, Thomas E. Barta, Daniel P. Becker, Shashidhar N. Rao, John N. Freskos, Brent V. Mischke, Daniel P. Getman, Gary A. DeCrescenzo
  • Publication number: 20030220423
    Abstract: The present invention relates to 1-alkoxy-polyalkyl-piperidine derivatives containing a structural element of formula (I) 1
    Type: Application
    Filed: April 24, 2003
    Publication date: November 27, 2003
    Inventors: Andreas Kramer, Peter Nesvadba
  • Publication number: 20030216383
    Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.
    Type: Application
    Filed: October 1, 2002
    Publication date: November 20, 2003
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Weimin Liu, Denice M. Spero, David S. Thomson, Yancey D. Ward, Erick R.R. Young
  • Publication number: 20030207872
    Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.
    Type: Application
    Filed: January 11, 2002
    Publication date: November 6, 2003
    Applicant: BAYER CORPORATION
    Inventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, Mary-Katherine Monahan, Reina Natero, Joel Renick, Robert N. Sibley
  • Publication number: 20030207917
    Abstract: The present invention discloses compounds, which are novel muscarinic receptor antagonists, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such muscarinic receptor antagonists as well as methods for using them to treat cognitive disorders such as Alzheimer's disease.
    Type: Application
    Filed: October 8, 2002
    Publication date: November 6, 2003
    Applicant: Schering Corporation
    Inventors: Yuguang Wang, Samuel Chackalamannil
  • Patent number: 6642233
    Abstract: The invention relates to the compounds of formula: as well as to the salts thereof with inorganic or organic acids, to solvates thereof and/or to hydrates thereof, which have strong affinity and high selectivity for the human NK1 receptors of substance P. The invention also relates to the process for preparing them, to the intermediate compounds of formula (VII) which are useful for the preparation, to pharmaceutical compositions containing them and to their fuse for the manufacture of medicinal products intended for treating any pathology in which substance P and the human NK1 receptors are involved.
    Type: Grant
    Filed: August 9, 2001
    Date of Patent: November 4, 2003
    Assignee: Sanofi-Synthelabo
    Inventors: Jean-Philippe Ducoux, Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto
  • Publication number: 20030191117
    Abstract: The present invention relates to acyclic piperazine and piperidine derivatives, which are especially useful for treating or preventing neuronal damage, particularly damage associated with neurological diseases. These compounds are also useful for stimulating nerve growth. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage or for stimulating nerve growth.
    Type: Application
    Filed: June 13, 2002
    Publication date: October 9, 2003
    Inventors: David Lauffer, Ronald Tomlinson, Eckhard Ottow, Martyn Botfield
  • Publication number: 20030186963
    Abstract: A novel class of substituted piperidines, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.
    Type: Application
    Filed: September 12, 2002
    Publication date: October 2, 2003
    Inventor: Florencio Zaragoza Dorwald
  • Publication number: 20030181484
    Abstract: The invention relates to a compound of formula (I): 1
    Type: Application
    Filed: March 3, 2003
    Publication date: September 25, 2003
    Inventors: Otto Meth-Cohn, Chu-Yi Yu, Pierre Lestage, Marie-Cecile Lebrun, Daniel-Henri Caignard, Pierre Renard
  • Publication number: 20030175848
    Abstract: The invention concerns substituted dithio-bis-nitrobenzenes (dithio-bis-nitrobenzylamines, dithio-bis-nitrobenzamides or dithio-bis-nitrophenacyls) and their uses as alternative substrates for NAD(P)H-dependent disulphide-reductase enzymes, such as trypanothion reductase and thioredoxine reductase and as a means for screening inhibitors of said enzymes. The invention also concerns an enzymatic test using said substrates and assay kits containing them. Said dithio-bis-nitrobenzenes correspond to general formula (I).
    Type: Application
    Filed: January 22, 2003
    Publication date: September 18, 2003
    Applicant: Institut Pasteur De Lille
    Inventors: Elisabeth Davioud-Charvet, Christian Sergheraert, Katja Becker-Brandenburg, Heiner Schirmer
  • Publication number: 20030176460
    Abstract: Compounds of formula (I) in free or salt form, where Ar1 is phenyl substituted by one or more halogen atoms, Ar2 is phenyl or naphthyl which is unsubstituted or substituted by one or more substituents selected from halogen, cyano, hydroxy, nitro, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy or C1-C8-alkoxycarbonyl, R1 is hydrogen or C1-C8-alkyl optionally substituted by hydroxy, C1-C8-alkoxy, acyloxy, N(R2)R3, halogen, carboxy, C1-C8-alkoxycarbonyl, —CON(R4)R5 or by a monovalent cyclic organic group, R2 and R3 are each independently hydrogen or C1-C8-alkyl, or R2 is hydrogen and R3 is acyl or —SO2R4 and R5 are each independently with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclic group, R4 and R5 are each independently hydrogen or C1-C8-alkyl, or R4 and R5 together with the nitrogen atom to which they are attached denote a 5-6-membered heterocyclic group, R6 is C1-C8-alkyl, C1-C8-haloalkyl, or phenyl optionally substituted by C1-C8-alkyl, and n is 1, 2, 3, or 4,
    Type: Application
    Filed: April 17, 2003
    Publication date: September 18, 2003
    Inventors: Trevor John Howe, Gurdip Bhalay, Darren Mark Le Grand, Thomas Storz
  • Publication number: 20030171588
    Abstract: The invention relates to combinatorial libraries containing two or more novel piperidine-3-carboxamide derivative compounds, methods of preparing the piperidine-3-carboxamide derivative compounds and piperidine-3-carboxamide derivative compounds bound to a resin
    Type: Application
    Filed: March 7, 2002
    Publication date: September 11, 2003
    Inventors: Jeffrey D. Kahl, Normand Hebert
  • Patent number: 6613769
    Abstract: The invention relates to bifunctional tryptase inhibitors of formula (I) wherein H1 and H2 comprise a Q group and L is a linker of formula and the conformation of the H1, H2 and L groups is such that the groups are separated by a distance of from 20 to 45 Å. Pharmaceutical compositions and crystal forms of the compounds are described in addition to methods for producing and identifying such compounds, as well as the use of such compounds in methods of treating allergic and inflammatory diseases.
    Type: Grant
    Filed: January 22, 2001
    Date of Patent: September 2, 2003
    Assignees: Max-Planck-Gesellschaft zur Föderung der Wissenschaften. e.V., Altana Pharma AG
    Inventors: Wolfram Bode, Luis Moroder, Pedro Jose Barbosa Pereira, Andreas Bergner, Robert Huber, Christian Sommerhoff, Norbert Schaschke, Thomas Bär, Thomas Martin, Josef Stadlwieser, Wolf-Rüdiger Ulrich, Andreas Dominik, Ulrich Thibaut, Daniela Bundschuh, Rolf Beume, Karl-Josef Goebel
  • Publication number: 20030158415
    Abstract: The present invention relates to a class of nitrogen-containing heterocyclic compounds which bind to opioid receptors. The inventive compounds can be used to treat a variety of disease states which involve the opioid receptors.
    Type: Application
    Filed: October 9, 2002
    Publication date: August 21, 2003
    Applicant: Research Triangle Institute
    Inventors: Frank I. Carroll, James B. Thomas, S. Wayne Mascarella
  • Publication number: 20030149023
    Abstract: Compounds of general formula (I) 1
    Type: Application
    Filed: August 19, 2002
    Publication date: August 7, 2003
    Applicant: AstraZeneca Canada Inc.
    Inventors: Daniel Delorme, Edward Roberts, Zhongyong Wei
  • Patent number: 6602885
    Abstract: The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is H, alkyl or alkenyl; R2 is optionally substituted phenyl, phenylalkyl, heteroaryl or heteroarylalkyl, naphthyl, fluorenyl or diphenylmethyl; R3 is optionally substituted phenyl, heteroaryl or naphthyl; R4 is H, alkyl, fluoro-alkyl, cyclopropylmethyl, —CH2CH2OH, —CH2CH2—O-alkyl, —CH2C(O)—O-alkyl, —CH2C(O)NH2, —CH2C(O)—NHalkyl or —CH2C(O)—N(alkyl)2; R19 is optionally substituted phenyl, heteroaryl or naphthyl, cycloalkyl, cycloalkylalkyl or alkoxyalkyl; and R5, R13, R14, R15 and R16 are hydrogen or alkyl for the treatment of HIV, solid organ transplant rejection, graft v.
    Type: Grant
    Filed: November 8, 2001
    Date of Patent: August 5, 2003
    Assignee: Schering Corporation
    Inventors: Bahige M. Baroudy, John W. Clader, Hubert B. Josien, Stuart W. McCombie, Brian A. McKittrick, Michael W. Miller, Bernard R. Neustadt, Anandan Palani, Ruo Steensma, Jayaram R. Tagat, Susan F. Vice, Mark A. Laughlin
  • Publication number: 20030144289
    Abstract: The invention provides compounds of formula (I):
    Type: Application
    Filed: July 30, 2002
    Publication date: July 31, 2003
    Inventors: Alan P. Kozikowski, Gian Luca Araldi, Amir P. Tamiz
  • Publication number: 20030139597
    Abstract: The present application describes novel cyclic hydroxamic acids of formula I: 1
    Type: Application
    Filed: June 20, 2002
    Publication date: July 24, 2003
    Inventors: Chu-Biao Xue, Carl P. Decicco, Xiaohua He
  • Publication number: 20030139405
    Abstract: The present invention relates to compounds, and prodrugs thereof, compositions and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and prodrugs thereof, selectively inhibit certain proteases of the coagulation cascade.
    Type: Application
    Filed: October 3, 2002
    Publication date: July 24, 2003
    Applicant: Pharmacia Corporation
    Inventors: Michael S. South, Ronald K. Webber, Horng-Chih Huang, Mihaly V. Toth, Alan E. Moormann, Jeffery S. Snyder, Jeffrey A. Scholten, Danny J. Garland, Melvin L. Rueppel, William L. Neumann, Scott Long, Wei Huang, John Trujillo, John J. Parlow, Darin E. Jones, Brenda Case, Michael J. Hayes
  • Publication number: 20030130253
    Abstract: Novel aminoazetidine, -pyrrolidine, and -piperidine derivatives, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.
    Type: Application
    Filed: September 12, 2002
    Publication date: July 10, 2003
    Inventors: Florencio Zaragoza Dorwald, Rolf Hohlweg
  • Publication number: 20030121110
    Abstract: 1,4-Diamino-2-alkenylbenzene derivatives of general formula (I) or physiologically tolerated water-soluble salts thereof 1
    Type: Application
    Filed: July 10, 2002
    Publication date: July 3, 2003
    Inventors: Laurent Chassot, Hans-Juergen Braun
  • Patent number: 6583179
    Abstract: The present invention is directed to a series of novel substituted aminoalkylamide derivatives, pharmaceutical compositions containing them and their use in the treatment of reproductive disorders and affective conditions. Further, the compounds of the invention are antagonists of follicle stimulating hormone, a hormone associated with the human reproductive system.
    Type: Grant
    Filed: December 21, 2000
    Date of Patent: June 24, 2003
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Steven J. Coats, Louis J. Fitzpatrick, Dennis J. Hlasta, Carolina L. Lanter, Mark J. Macielag, Ke Pan, Ralph A. Rivero, Stephen S. Palmer
  • Patent number: 6583245
    Abstract: The present invention relates to a polymerizable composition, comprising a) at least one compound of formula (I) (RG)—A—(Stab)  (I), wherein (Stab) is a light stabilizer radical selected from the group consisting of sterically hindered amines, hydroxyphenyl-s-triazines, hydroxyphenyl-benzotriazols and o-hydroxy-benzophenones; A is a spacer group or a direct bond; and (RG) is a group containing at least one ethylenically unsaturated functional group; and either b1) a compound of formula (II) Y—X  (II),  wherein X represents a group having at least one carbon atom and is such that the free radical derived from X is capable of initiating polymerization and Y represents a group being such that the free radical Y· derived from it forms a stable free radical; or b2) a stable free radical Y· and a free radical source from which a radical is formed capable of initiating polymerization, or b3) a compound of formula (III)  and a cat
    Type: Grant
    Filed: June 21, 2001
    Date of Patent: June 24, 2003
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Alfred Steinmann, Michael Roth, Werner Stauffer, Peter Nesvadba, Andreas Mühlebach
  • Publication number: 20030109517
    Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases.
    Type: Application
    Filed: September 16, 2002
    Publication date: June 12, 2003
    Applicant: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Scott C. Miller, Juan Jose Marugan Sanchez, Kristin D. Haslow, Jonathan Hall
  • Patent number: 6570038
    Abstract: Hexasubstituted guanidinium chlorides are prepared by a method which affords them in high yield as aqueous solutions, optionally also containing alkali metal chlorides. The solutions may be employed as sources of hexasubstituted guanidinium salts useful as phase transfer catalysts for the reaction of alkali metal salts of dihydroxyaromatic compounds with substituted imides to form polyetherimides or their intermediates.
    Type: Grant
    Filed: June 9, 2000
    Date of Patent: May 27, 2003
    Inventors: Joseph John Caringi, Peter David Phelps, Thomas Link Guggenheim, Daniel Joseph Brunelle
  • Publication number: 20030096828
    Abstract: The invention relates to compounds represented by the following general formula (1): 1
    Type: Application
    Filed: June 19, 2002
    Publication date: May 22, 2003
    Applicant: KOWA CO., LTD.
    Inventors: Hiroyuki Ishiwata, Seiichi Sato, Mototsugu Kabeya, Soichi Oda, Yukio Hattori, Makoto Suda, Manabu Shibasaki, Hiroshi Nakao, Takao Nagoya
  • Publication number: 20030092694
    Abstract: The invention relates to compounds of the general formula (I): 1
    Type: Application
    Filed: October 11, 2002
    Publication date: May 15, 2003
    Applicant: Biovitrum, AB, a Stockholm, Sweden corporation
    Inventors: Bjorn Nilsson, Jan Tejbrant, Benjamin Pelcman, Erik Ringberg, Markus Thor, Jonas Nilsson, Mattias Jonsson
  • Publication number: 20030083344
    Abstract: Compounds of the formula (I), in which M, A1, A2, K1 and K2 have the meanings indicated in the description are novel active tryptase inhibitors.
    Type: Application
    Filed: September 20, 2002
    Publication date: May 1, 2003
    Inventor: Thomas Martin
  • Publication number: 20030060460
    Abstract: The sulfonamide or carboamide derivatives of the formula (I) and a pharmaceutical composition which comprise them as an active ingredient: 1
    Type: Application
    Filed: July 30, 2002
    Publication date: March 27, 2003
    Inventors: Shuichi Ohuchida, Yuuki Nagao
  • Patent number: 6538141
    Abstract: The invention concerns a method for preparing nitroxides, which consists in oxidising, in a two-phase medium, using an aliphatic peroxide, secondary amines with steric hindrance or having a —CH in the nitrogen atom &agr;.
    Type: Grant
    Filed: September 24, 2001
    Date of Patent: March 25, 2003
    Assignee: Atofina
    Inventors: Jean-Philippe Gillet, Olivier Guerret, Jean-Pierre Lascombe
  • Publication number: 20030055054
    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: August 29, 2002
    Publication date: March 20, 2003
    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: 6518267
    Abstract: The present invention provides bis-aminomethyl carbonyl protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions 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: Grant
    Filed: November 21, 2000
    Date of Patent: February 11, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: William Edward Bondinell, Renee Louise DesJarlais, Daniel Frank Veber, Dennis Shinji Yamashita
  • Patent number: 6511993
    Abstract: Compounds of formula (I) and pharmaceutically-acceptable derivatives thereof, are matrix metalloprotease inhibitors, useful in treatment of conditions mediated by matrix metalloproteases, such as chronic dermal ulcers.
    Type: Grant
    Filed: June 2, 2000
    Date of Patent: January 28, 2003
    Inventors: Kevin Neil Dack, Michael Jonathan Fray, Gavin Alistair Whitlock, Mark Llewellyn Lewis, Nicholas Murray Thomson
  • Publication number: 20030004340
    Abstract: There is provided a compound of formula I, 1
    Type: Application
    Filed: March 19, 2002
    Publication date: January 2, 2003
    Inventors: Stephen Paul Gibson, Ivan Tommasini, Kimberley Verrier, Christopher James Dutton, David Morris Gethin, Douglas James Critcher, Richard Edward Armer
  • Publication number: 20030004185
    Abstract: The use of CCR5 antagonists of the formula 1
    Type: Application
    Filed: November 8, 2001
    Publication date: January 2, 2003
    Inventors: Bahige M. Baroudy, John W. Clader, Hubert B. Josien, Stuart W. McCombie, Brian A. McKittrick, Michael W. Miller, Bernard R. Neustadt, Anandan Palani, Ruo Steensma, Jayaram R. Tagat, Susan F. Vice, Mark A. Laughlin
  • Patent number: 6498168
    Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) wherein R, R1, R2, R3, R4, R21, R27, R28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula or other compounds capable of enhancing acetylcholine release with acetylcholinesterase inhibitors.
    Type: Grant
    Filed: July 11, 2001
    Date of Patent: December 24, 2002
    Assignee: Schering Corporation
    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: 20020183315
    Abstract: The present invention discloses compounds useful in treating or preventing IMPDH-associated disorders, such as transplant rejection and autoimmune diseases, having the formula (I), 1
    Type: Application
    Filed: May 23, 2002
    Publication date: December 5, 2002
    Inventors: Edwin J. Iwanowicz, Katerina Leftheris, Chunjian Liu, Toomas Mitt, Scott H. Watterson
  • Patent number: 6489327
    Abstract: The invention relates to novel inhibitors of human tryptase which are used in the pharmaceutical industry for the production of medicaments.
    Type: Grant
    Filed: October 20, 2000
    Date of Patent: December 3, 2002
    Assignees: Max-Planck-Gesellschaft zur Fordrungder Wisenschaften, e.V., Byk Gulden Lomberg Chemische Fabrik GmbH
    Inventors: Thomas Bär, Thomas Martin, Josef Stadlwieser, Wolf-Rüdiger Ulrich, Andreas Dominik, Ulrich Thibaut, Daniela Bundschuh, Rolf Beume, Karl-Josef Goebel, Wolfram Bode, Luis Moroder, Pedro Jose Barbosa Pereira, Andreas Bergner, Robert Huber, Christian Sommerhoff, Norbert Schaschke
  • Patent number: 6479485
    Abstract: This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.
    Type: Grant
    Filed: August 7, 2001
    Date of Patent: November 12, 2002
    Assignee: Berlex Laboratories, Inc.
    Inventors: Brad O. Buckman, David D. Davey, William J. Guilford, Michael M. Morrissey, Howard P. Ng, Gary B. Phillips, Shung C. Wu, Wei Xu
  • Patent number: 6465643
    Abstract: The present invention relates to compounds of the formula in which one, two or three of the radicals R1, R2, R3 and R4 are where m and n are an integer from 1 to 10, R5, R6, R7 and R8 are, independently of one another, identical or different and are a straight-chain or branched alkyl radical having 1 to 10 carbon atoms, and the remaining radical(s) R1 to R4 are or —NR9R10, where R9 and R10 are identical or different and are a straight-chain or branched alkyl radical having 1 to 10 carbon atoms, and X− is an inorganic or organic anion or an equivalent of a multiply charged inorganic or organic anion. The invention further relates to mixtures of substances comprising compounds of the formula (1), to a process for preparing the compounds of the formula (1) and to the use thereof.
    Type: Grant
    Filed: July 17, 2000
    Date of Patent: October 15, 2002
    Assignee: Clariant GmbH
    Inventors: Berthold Schiemenz, Thomas Wessel, Ralf Pfirmann
  • Publication number: 20020147342
    Abstract: Compounds of the formula 1
    Type: Application
    Filed: November 13, 2001
    Publication date: October 10, 2002
    Applicant: American Cyanamid Company
    Inventors: Jeremy I. Levin, Aranapakam M. Venkatesan, Derek C. Cole, James M. Chen, Jamie M. Davis, George T. Grosu
  • Patent number: 6458812
    Abstract: Amide derivatives of 1,4 di-substituted piperidine compounds of the formula: or a pharmaceutically acceptable salt, ester or solvate thereof, wherein R1 is optionally substituted cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or heteroaryl; R2 is H, alkyl, or optionally substituted cycloalkyl, cycloalkylalkyl, heterocycloalkyl, bridged cycloalkyl, or bridged heterocycloalkyl; R3 is alkyl or —CH2OH; and R4 is H or alkyl; are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed.
    Type: Grant
    Filed: December 17, 2001
    Date of Patent: October 1, 2002
    Assignee: Schering Corporation
    Inventors: Brian A. McKittrick, Guihua Guo, Zhaoning Zhu, Yuanzan Ye
  • Patent number: 6458806
    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 where V═O,S, NH or a bond; Ar can be unsubstituted or substituted benzimidazole, phenyl, biphenyl, pyridyl, naphthyl, quinoline or isoquinoline. The other meanings for the terms are recited in the specification below.
    Type: Grant
    Filed: August 12, 1997
    Date of Patent: October 1, 2002
    Assignee: Millennium Pharmaceuticals, Inc.
    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
  • Publication number: 20020133012
    Abstract: The invention relates to new compounds of general formula I 1
    Type: Application
    Filed: February 27, 2002
    Publication date: September 19, 2002
    Inventors: Sven Luettke, Andreas Mathes
  • Publication number: 20020119980
    Abstract: The present application describes modulators of CCR3 of formula (I): 1
    Type: Application
    Filed: October 18, 2001
    Publication date: August 29, 2002
    Inventors: Soo S. Ko, George V. Delucca, John V. Duncia, Joseph B. Santella, Dean A. Wacker