Abstract: The invention relates to a novel anilide compound and a pharmaceutical composition comprising the same. The invention relates to a compound represented by the following general formula:
represents a divalent residue of benzene with a substituent(s), heterocycle-condensed benzene which may or may not have a substituent, pyridine which may or may not have a substituent, cyclohexane or naphthalene or
Ar represents an aryl group which may or may not have a substituent;
X represents —NH—, oxygen atom or sulfur atom;
Y represents —NR4—, oxygen atom, sulfur atom, sulfoxide or sulfone;
Z represents single bond or —NR5—;
R4 represents hydrogen atom, a lower alkyl group, an aryl group or a silylated lower alkyl group which may or may not have a substituent;
R5 represents hydrogen atom, a lower alkyl group, an aryl group or a silylated lower alkyl group which may or may not have a substituent; and
n represents an integer of 0 to 15.
Abstract: Disclosed are novel compounds of formula (I): 1
Type:
Application
Filed:
August 2, 2001
Publication date:
February 7, 2002
Inventors:
Roger John Snow, Mario Cardozo, Daniel Goldberg, Abdelhakim Hammach, Tina Morwick, Neil Moss, Usha R. Patel, Anthony S. Prokopowicz, Hidenori Takahashi, Matt Aaron Tschantz, Xiao-Jun Wang
Abstract: A compound selected from the group consisting of a compound of the formula
wherein the substituents are defined as set forth in the specification and its salts with non-toxic pharmaceutically acceptable acids and bases useful for treating loss of bone matrix.
Type:
Grant
Filed:
June 29, 2000
Date of Patent:
January 15, 2002
Assignees:
Aventis Pharma S.A., Genetech, Inc.
Inventors:
Denis Carniato, Thomas R. Gadek, Jean-Francois Gourvest, Jochen Knolle, Robert S. McDowell, Anurschirwan Peyman
Abstract: Benzimidazoles, substituted in the 2-position by substituted benzyl groups or heteroaryl groups are effective as NMDA NR2B antagonists and are useful for relieving pain.
Type:
Grant
Filed:
October 25, 2000
Date of Patent:
November 13, 2001
Assignee:
Merck & Co., Inc.
Inventors:
John A. McCauley, Cory R. Theberge, Nigel J. Liverton, David A. Claremon, Christopher F. Claiborne
Abstract: Novel 4-substituted cyclohexanes substituted in the 1-position with 2-benzimidazoles, 2-imidazopyridines, or 4-imidazoles either directly or through a C1-C4alkyl, cycloalkyl, hydroxyalkyl, alkoxy or aminoalkyl chain are effective as NMDA NR2B antagonists useful for relieving pain.
Type:
Grant
Filed:
October 25, 2000
Date of Patent:
September 18, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Wayne Thompson, David A. Claremon, Peter M. Munson, John A. McCauley
Abstract: Compounds of the formula
wherein the substituents are as defined in the application and their pharmaceutically acceptable acid and base salts thereof which are useful for preventing loss of bone matrix.
Type:
Grant
Filed:
July 7, 2000
Date of Patent:
August 21, 2001
Assignee:
Aventis Pharma S.A.
Inventors:
Denis Carniato, Thomas R. Gadek, Francois Goubet, Jean-Francois Gourvest, Jochen Knolle, Robert S. McDowell, Karl-Heinz Scheunemann
Abstract: The dihalopropene compounds of the general formula [I] have excellent insecticidal/acaricidal activity, so that they are satisfactorily effective for the control of noxious insects, mites and ticks.
Abstract: The present invention provides an efficient and versatile method for the synthesis and screening of combinatorial libraries of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof. In order to expedite the synthesis of large arrays of compounds possessing these core structures, a general methodology for solid phase synthesis of these derivatives is provided. Arrays of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antiviral, antimicrobial, anticoagulant, and antiulcer activity, or use in the treatment of inflammation, hypertension, cancer, and other conditions can be prepared by this method.
Abstract:
A novel benzimidazole derivative [specifically, for example, 2-ethoxy-1-[{4′-(2″-N,N-dimethylaminoethoxycarbonyl)phenyl}methyl]-1H-benzimidazole-6-carboxylic acid morpholide] represented by formula (I) and a salt thereof. The compound exhibits satisfactory curative effects for cardiac and nephric diseases, although having little action on blood-pressure.
Abstract: A benzimidazole derivative or a salt thereof expressed by the following Formula (I):
wherein one of A and B is a hydrocarbon group of C10-30 expressed by R1 and the other is —(CH2)n—NR2R3; R2 and R3 individually represent H, lower alkyl, phenyl or benzyl, or —NR2R3 may be a heterocycle having 3-7 members, or —CONR5—(CH2)n—NR2R3 may be the following Group (W):
wherein R2 is H, lower alkyl, phenyl or benzyl and ring E is a heterocycle of 6 or 7 members; R4 is selected from the group consisting of H, halogen, cyano, trifluoromethyl, lower alkyl and etc.; R5 is H, lower alkyl, lower acyl or lower alkylcarbamoyl; m is 0 or 1; and n is an integer of 0-5. The benzimidazole derivative or the salt thereof has excellent hair growth and regrowth promoting effects, which are useful for care, improvement or prevention of hair loss in mammals and, in particular, in human.
Type:
Grant
Filed:
September 17, 1999
Date of Patent:
March 20, 2001
Assignee:
Shiseido Co., Ltd.
Inventors:
Koji Kobayashi, Hirotada Fukunishi, Kenichi Umishio, Masahiro Tajima
Abstract: This invention relates to a heterocyclic compound of the formula
wherein
a group of the formula:
is a group of the formula
X is O, S or N-R5,
R1 is lower alkyl, etc.,
R5 is hydrogen, lower alkyl, etc.,
R2 is hydrogen, halogen, lower alkyl, etc.,
R3 is halogen, lower alkyl, etc.,
R4 is amino optionally having suitable substituent(s),
and
A is lower alkylene,
and a salt thereof, to processes for preparation thereof, and to a pharmaceutical composition comprising the same for the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.
Abstract: The hetero-linked phenylglycinolamides are prepared by reaction of the corresponding hetero-linked phenylacetic acids with appropriate phenylglycinols. The hetero-linked phenylglycinolamides are suitable as active compounds in medicaments.
Type:
Grant
Filed:
December 4, 1998
Date of Patent:
February 20, 2001
Assignee:
Bayer Aktiengesellschaft
Inventors:
Siegfried Goldmann, Ulrich Müller, Richard Connell, Hilmar Bischoff, Dirk Denzer, Rudi Grützmann, Martin Beuck