Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R1, R2, R3, R4, R5, R6, R8, R9 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:
September 27, 2002
Publication date:
April 1, 2004
Applicant:
Boehringer Ingelheim Pharmaceuticals Inc.
Inventors:
Younes Bekkali, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey D. Ward, Erick R.R. Young, Eugene R. Hickey, Weimin Liu, Usha R. Patel
Abstract: The invention concerns the use of amide derivatives of formula (I) wherein: R1 and R2 are substituents such as hydroxy, C1-6alkoxy, mercapto, C1-6alkylthio, amino, C1-6alkylamino and di-(C1-6alkyl)amino; m and p are independently 0-3; R3 is C1-4alkyl; q is 0-4; and R4 is aryl or cycloalkyl; or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in the treatment of diseases or medical conditions mediated by cytokines
Type:
Grant
Filed:
October 8, 2002
Date of Patent:
February 3, 2004
Assignee:
Zeneca Limited
Inventors:
Dearg S Brown, George R Brown, Philip Cohen
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
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),
wherein X is —C(O)—, —C(S)—, or —S(O)2—; A is an optionally-substituted saturated or unsaturated monocyclic or bicyclic ring; B is a saturated or unsaturated monocyclic or bicyclic ring system having at least one substituent Q which is selected from R7 and R8; R7 is selected from (C0-C6)alkyl, (C2-C6)alkenyl and (C2-C6)alkynyl and R7 is substituted with
R8 is selected from (C0-C6)alkyl, (C2-C6)alkenyl and (C2-C6)alkynyl and R8 is substituted with
and Z1 through Z5 are as defined in the specification.
Type:
Grant
Filed:
May 23, 2002
Date of Patent:
September 9, 2003
Assignee:
Bristol-Myers Squibb Co.
Inventors:
Edwin J. Iwanowicz, Katerina Leftheris, Chunjian Liu, Toomas Mitt, Scott H. Watterson
Abstract: N-(3,5-bis-disubstituted aminomethyl-4-hydroxy)benzyl aromatic sulfonamides and N-(3,5-bis-disubstituted aminomethyl-4-hydroxy)phenyl aromatic sulfonamides compounds in accordance with the animal test, are active in the prevention and the treatment of cardiac arrhythmia. These compounds are prepared as corresponding diamines by the condensation of optionally substituted aromatic sulfochlorides with p-hydroxybenzylamine, p-aminophenol, or the like, which followed by the Mannich reaction of the resulted corresponding aromatic sulfamides with formaldehyde and secondary amines; or directly obtained by the reaction of the aromatic sulfamides with 4-amino-2,6-bis-disubstituted aminomethylphenol. Subsequently, the diamines are reacted with various acids to provide their salts.
Type:
Grant
Filed:
June 7, 2002
Date of Patent:
August 12, 2003
Assignee:
Shanghai Institute of Materia Medica Chinese Academy of
Science
Inventors:
Donglu Bai, Weizhou Chen, Yunxin Bu, Yiping Wang, Yueli Dong, Aili Kang
Abstract: The invention concerns the use of amide derivatives of formula (I) wherein: R1 and R2 are substituents such as hydroxy, C1-6alkoxy, mercapto, C1-6alkylthio, amino, C1-6alkylamino and di-(C1-6alkyl)amino; m and p are independently 0-3R3 is C1-4alkyl; q is 0-4; and R4 is aryl or cycloalkyl; or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in the treatment of diseases or medical conditions mediated by cytokines
Type:
Grant
Filed:
March 7, 2000
Date of Patent:
December 24, 2002
Assignee:
Zeneca Limited
Inventors:
Dearg S Brown, George R Brown, Philip Cohen
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
Abstract: The invention concerns amide derivatives of formula (I)
wherein R3 is (1-6C)alkyl or halogeno; m is 0-3, p is 0-2 and q is 0-4; each of R1 and R2 is a group such as hydroxy, halogeno, trifluoromethyl and cyano; R4 is a basic group such as amino, (1-6C)alkylamino, di-[(1-6C)alkyl]amino, di-[(1-6C)alkyl]amino-(1-6C)alkyl, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, heteroaryl, heteroaryloxy, heteroaryl-(1-6C)alkoxy, heterocyclyl, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy; and Q2 is a group such as heteroaryl, heteroaryloxy or heteroaryl-(1-6C)alkoxy which is optionally substituted; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
Abstract: An amidoaromatic ring sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as are a treatment process that comprises administering a contemplated amidoaromatic ring sulfonamide 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:
June 4, 1999
Date of Patent:
September 17, 2002
Assignee:
Monsanto Company
Inventors:
Robert M. Heintz, Daniel P. Getman, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard, S. Zaheer Abbas
Abstract: This invention relates to a novel class of partial or full muscarinic receptor agonists intermediates for their preparation, and pharmaceutical compositions and methods of use for the treatment or prevention of diseases the treatment or prevention of which is mediated by muscarinic receptor agonism
Type:
Application
Filed:
February 15, 2000
Publication date:
August 1, 2002
Inventors:
Anabella Villalobos, Daniel Yohannes, Jolanta Nowakowski, Dane Liston
Abstract: Sulfonylcarboxamide derivatives of formula I, their physiologically acceptable salts and/or physiologically functional derivatives, methods of making these compounds, their use for preparing medicines for the prevention and treatment of hyperlipidemia and arteriosclerotic disorders.
Type:
Application
Filed:
September 27, 2001
Publication date:
June 13, 2002
Inventors:
Reinhard Kirsch, Hans-Ludwig Schaefer, Eugen Falk, Horst Hemmerle
Abstract: Ultraviolet absorbents and photostabilizers have an excellent absorption ability in a wide range of ultraviolet rays, and also have high stability and high safety.
Abstract: 1-phenyl-3 -dimethylaminopropane compounds corresponding to the formula I
a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
June 19, 2001
Assignee:
Gruenenthal GmbH
Inventors:
Helmut Buschmann, Wolfgang Strassburger, Elmar Friderichs
Abstract: Tachykinin receptor antagonists that are useful for treating or preventing attention deficit disorder, optionally associated with hyperactivity in a patient, are desclosed.
Type:
Grant
Filed:
May 31, 2000
Date of Patent:
June 5, 2001
Assignee:
Merck & Co., Inc.
Inventors:
David L. Glatt, Mark S. Kramer, Nadia Rupniak
Abstract: This invention relates to cardiac diseases improving agents substantially free from antagonistic action to type 1 receptor of angiotensin II which participates to hypotensive action. Particularly, this invention relates to cardiac diseases improving agents composed of effective ingredients of aromatic compounds or pharmacologically acceptable salts thereof shown by below mentioned general formula.
Chemical formula 1
[General formula (I)]
(wherein, substituents thereof typically include, R1, R4, R13 representing hydrogen atom, an alkyl group, a haloalkyl group and so forth, R8 representing —CO—, —SO2— or single bond, R2 representing a 3-7 membered aliphatic cyclic amino group having at least one nitrogen atom, R7 representing —CO—or —SO2—, and R12 representing N-substituted valeramido group.