Abstract: Novel tubulin binding compounds having potent tubulin depolymerization activity and inhibitory activity against tubulin polymerization. The compounds are effective agents for inhibiting cellular proliferation, for example, in cancer cells. The compounds are adapted to interact favorably with a novel tubulin binding pocket, which pocket is useful for screening of anti-tubulin, anti-proliferation, and anti-cancer drugs.
Abstract: The present invention provides an efficient stereoselective method for manufacturing (2S,4S)-2-[[(R)-hydroxy-(3R)-cyclic amine-3-yl]methyl]pyrrolidine-4-thiol or a salt thereof which is useful as an intermediate for the manufacture of carbapenem and also provides the intermediate.
A method for manufacturing which comprises the step of reacting a compound of the formula (I):
(wherein, R1 is a lower alkylsulfonyl group, an optionally substituted arylsulfonyl group or an alkylsilyl group; and R2 is a protecting group for an amino group) with a compound of the formula (II):
(wherein, R3 is a substituted or unsubstituted lower alkyl group or aryl group; X is an oxygen atom or a sulfur atom; Y is an azide group or a nitro group; and m is an integer of 2 to 5).
Abstract: A compound, having utility as an immunomodulating agent, which is a prodigiosine of formula (I):
wherein
R1 is hydrogen or C1-C5 alkyl; and
R2 is a C1-C5 alkyl;
or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
October 7, 1999
Date of Patent:
April 9, 2002
Assignee:
Pharmacia & Upjohn S.p.A.
Inventors:
Roberto D'Alessio, Ermes Vanotti, Alberto Bargiotti, Marcellino Tibolla, Mario Ferrari, Anna Maria Isetta, Francesco Colotta
Abstract: The present invention is directed to 1-pyrrolidin-1-ylmethyl-3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
Type:
Application
Filed:
May 24, 2001
Publication date:
March 21, 2002
Inventors:
Malcolm Wilson Moon, Walter Morozowich, Ping Gao
Abstract: Compounds of the formula:
useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.
Type:
Grant
Filed:
January 27, 2000
Date of Patent:
March 19, 2002
Assignee:
American Cyanamid Company
Inventors:
Jeremy I. Levin, Aranapakam M. Venkatesan, James M. Chen, Arie Zask, Vincent P. Sandanayaka, Mila T. Du, Jannie L. Baker
Abstract: Ethers of polyalkyl or polyalkenyl N-hydroxyalkyl succinimides having the formula:
or a fuel soluble salt thereof; wherein
R is a polyalkyl or polyalkenyl group having an average molecular weight in the range of about 450 to about 5,000;
n is an integer from 2 to 5; and Z is a moiety selected from the group consisting of
wherein R1 is a hydroxy, nitro, cyano or —(CH2)x—NR3R4, wherein R3 and R4 are independently hydrogen or lower alkyl of 1 to 6 carbon atoms and x is 0 or 1; and R2 is hydrogen, hydroxy, nitro, cyano or —(CH2)y—NR5R6, wherein R5 and R6 are independently hydrogen or lower alkyl of 1 to 6 carbon atoms and y is 0 or 1. The compounds of formula I are useful as fuel additives for the prevention and control of engine deposits.
Abstract: This application relates to novel compounds of formula (I) (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula (I), and the use of the compounds of formula (I) as thrombin inhibitors.
Type:
Grant
Filed:
January 24, 2000
Date of Patent:
February 26, 2002
Assignee:
Eli Lilly And Company
Inventors:
Nicholas J Bach, Jolie A. Bastian, Nickolay Y Chirgadze, Michael L Denney, Robert J. Foglesong, Richard W Harper, Mary G Johnson, Ho-Shen Lin, Michael P Lynch, Jefferson R McCowan, Alan D Palkowitz, Daniel J Sall, Gerald F Smith, Kumiko Takeuchi, Minsheng Zhang
Abstract: The invention relates to a method of simultaneous high-throughput preformulation quantification of potential drug candidates, where an aliquot of a mixture of solutions containing different compounds is injected into a high pressure liquid chromatograph. The concentration of each compound can be determined by high pressure liquid chromatographic analysis, and correlated to a physico-chemical property of the compound.
Abstract: There is provided amino acid derivatives of formula I,
wherein p, q, R1, R2, R3, R4, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
Abstract: The invention provides compounds which are potent inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to compounds having a structure according to the following Formula (I):
wherein R1, R2, X, Z, m, and n are defined below.
to This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. The compounds of the present invention are useful for the treatment of diseases and conditions which are characterized by unwanted metalloprotease activity. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for metalloprotease-related maladies using these compounds or the pharmaceutical compositions containing them.
Type:
Grant
Filed:
March 23, 1999
Date of Patent:
December 11, 2001
Assignee:
The Procter & Gamble Company
Inventors:
Menyan Cheng, Michael George Natchus, Biswanath De, Neil Gregory Almstead, Yetunde Olabisi Taiwo, Stanislaw Pikul
Abstract: The present invention provides compounds of the formula
where R1-R5 are each, independently, a hydrogen atom or a normal or branched C1-C6-alkyl group; A is a methionyl, phenylalanyl or phenylglycyl residue; n is 0 or 1; R6 is a hydrogen atom; and R7 is a carbocylic group, an aromatic group, a C1-C4-alkyl group, a pyridylalkyl group or a heterocyclic group. In another embodiment, R6 is benzyl or —C(O)OR8, where R8 is a C1-C6-alkyl group, and R7 is a heteroaromatic group, such as a 2-thiazolyl group.
Type:
Grant
Filed:
March 31, 2000
Date of Patent:
November 27, 2001
Assignees:
BASF Aktiengesellschaft, Arizona Board of Regents
Inventors:
George R. Pettit, Jayaram K. Srirangam, Michael D. Williams, Kieran P. M. Durkin, Teresa Barlozzari, Andreas Kling, Bernd Janssen, Andreas Haupt
Abstract: The present invention relates to new compounds of the formula (I)
in which
X represents halogen,
Y represents halogen or alkyl and
Z represents halogen or alkyl,
with the proviso that always one of the radicals Y and Z represents halogen while the other represents alkyl, and
Het represents one of the groups
in which
A, B, D and G have the meanings given in the description,
to a plurality of processes for their preparation and to their use as pesticides and herbicides.
Type:
Grant
Filed:
October 31, 1997
Date of Patent:
November 13, 2001
Assignee:
Bayer Aktiengesellschaft
Inventors:
Folker Lieb, Hermann Hagemann, Arno Widdig, Michael Ruther, Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Peter Dahmen, Markus Dollinger, Hans-Joachim Santel, Alan Graff, Wolfram Andersch, Norbert Mencke, Andreas Turberg
Abstract: A process for preparing a compound of the formula I:
or pharmaceutical acceptable salts thereof wherein X is —NR1—, —S(O)g—, or —O—; R1 is —H, C1-6 alkyl optionally substituted with one or more —OH, —CN, or halo, or R1 is —(CH2)h-aryl, —COR1-1, —COOR1-2, —CO—(CH2)h—COR1-1, C1-6 alkyl sulfonyl, —SO2—(CH2)h-aryl, or —(CO)i-Het; R2 is —H, C1-6 alkyl, —(CH2)h-aryl, or halo; R3 and R4 are the same or different and are —H or halo; R6 is —H, C1-12 alkyl optionally substituted with one or more halo, C3-12 cycloalkyl, C1-6 alkoxy. The compounds are useful antimicrobial agents.
Type:
Grant
Filed:
March 3, 2000
Date of Patent:
November 6, 2001
Assignee:
Pharmacia & Upjohn Company
Inventors:
Michael Dalton Ennis, Robert Louis Hoffman, Douglas K. Hutchinson, David John Anderson, Toni-Jo Poel, Richard Charles Thomas
Abstract: A compound of the following formula:
and the salts thereof, wherein A is hydrogen, halo, or hydroxy; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, or pyridyl, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, or C1-C4 alkyl; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.
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 inhibiting retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
Type:
Grant
Filed:
December 1, 1999
Date of Patent:
October 30, 2001
Assignee:
G. D. Searle & Co.
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
Abstract: Disclosed are “acid-amide” calixarenes of formula (I) wherein: L is [—CH2—] or [—O—CH2—O—] and may be the same or different between each aryl group; R5 is H, halogen, or C1-C10 aliphatic hydrocarbyl group, C6-C20 aryl group, C6-C10 hydrocarbyaryl group, any of which may optionally be substituted by one or more halo or oxo groups or interrupted by one or more oxo groups, and R5 may be the same or different on each aryl group; R1 comprises an optionally protected carboxy group; two groups out of R2, R3, and R4 are H; the one group out of R2, R3, and R4 not being H comprises an amide group. The amide group may be linked to a second calixarene to form a dimer. Also disclosed are methods of use of such calixarenes for the purposes of metal sequestration, especially of lanthanides and actinides. Also disclosed are calixarene dimer derivatives of the calixarenes of the invention. Also disclosed are processes for preparing the calixarenes and dimers.
Type:
Grant
Filed:
December 13, 1999
Date of Patent:
October 2, 2001
Assignee:
The Secretary of State for Defence in Her Brittanic Majesty's
Government of the United Kingdom of Great Britain and Northern
Ireland
Inventors:
Graeme P. Nicholson, Mark J. Kan, Gareth Williams, Michael G. Drew, Paul D. Beer
Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-linked sulfonamides of heterocyclic thioesters having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.
Type:
Grant
Filed:
March 1, 2000
Date of Patent:
September 25, 2001
Assignee:
GPI Nil Holdings, Inc.
Inventors:
Gregory S. Hamilton, Jai-He Li, Wei Huang
Abstract: A compound of the following formula:
and the salts thereof, wherein A is hydrogen, halo, hydroxy, or the like; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl or the like; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, pyridyl, and the like, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, C1-C4 alkyl, or the like; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, and the like or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.
Abstract: 1-Arenesulfonyl-2-Aryl-pyrrolidine and pyridine derivatives having activity as ligands of metabotropic glutamate receptors of the formula
are disclosed.
Type:
Grant
Filed:
March 24, 2000
Date of Patent:
September 4, 2001
Assignee:
Hoffmann- La Roche Inc.
Inventors:
Vincent Mutel, Eric Vieira, Jürgen Wichmann
Abstract: This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of the compounds of formula I as thrombin inhibitors.
Type:
Grant
Filed:
January 21, 2000
Date of Patent:
September 4, 2001
Assignee:
Eli Lilly and Company
Inventors:
Nickolay Y Chirgadze, Richard W Harper, Todd J Kohn, Ho-Shen Lin, Jefferson R McCowan, Alan D Palkowitz, Daniel J Sall, Gerald F Smith, Kumiko Takeuchi, Michael R Wiley, Minsheng Zhang
Abstract: The present invention relates to a process for the preparation of &ggr;-lactams of the general formula I
The invention relates also to novel advantageous intermediates of the general formulae V, IV and II and their salts
and their use.
The compounds of the general formula I are obtained by cyclising compounds of the general formula II
which can be prepared from the intermediate compounds V.
Type:
Grant
Filed:
May 21, 1999
Date of Patent:
August 28, 2001
Assignee:
Degussa-Huls AG
Inventors:
Karlheinz Drauz, Günter Knaup, Michael Schwarm
Abstract: The present invention provides compounds having the structure:
and pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB4 production, such as psoriasis, ulcerative colitis, IBD, and asthma.
Type:
Grant
Filed:
May 14, 1999
Date of Patent:
July 24, 2001
Assignee:
G. D. Searle & Company
Inventors:
Barbara Baosheng Chen, Helen Chen, Mark Andrew Russell, Julie Marion Miyashiro, James Malecha, Thomas Dale Penning
Abstract: This application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula I as defined herein. It also provides novel compounds of formula I, processes and intermediates for their preparation, and pharmaceutical formulations comprising the novel compounds of formula I.
Type:
Grant
Filed:
August 5, 1999
Date of Patent:
July 24, 2001
Assignee:
Eli Lilly and Company
Inventors:
Kenneth Jeff Thrasher, Kenneth Lee Hauser, Alan David Palkowitz
Abstract: Methods, compositions, and compounds for modulating the activity of an endothelin peptide are provided. The methods use compositions that contain compounds of formula (1):
where X and Y are selected from groups that include O, S, and NH; and Ar1, Ar2 and Ar3 are independently selected from substituted or unsubstituted groups that include 5 to 6 membered aryl groups and heteroaryl groups that contain one or two heteroatom(s). The methods are effected by contacting endothelin receptors with one or more of the compounds or with compositions containing one or more of the compounds prior to, simultaneously with, or subsequent to contacting the receptors with an endothelin peptide.
Type:
Grant
Filed:
June 8, 1999
Date of Patent:
July 24, 2001
Assignee:
Texas Biotechnology Corporation
Inventors:
Ming Fai Chan, Vitukudi Narayanaiyengar Balaji, Rosario Silvestre Castillo, Adam Kois, Bore Gowda Raju, Chengde Wu
Abstract: There is provided compounds of formula I,
wherein R1, R2, R3, Rx, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required as in thrombosis or as anticoagulants.
Abstract: This application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula I as defined herein. It also provides novel compounds of formula I, processes and intermediates for their preparation, and pharmaceutical formulations comprising the novel compounds of formula I.
Type:
Grant
Filed:
May 14, 1999
Date of Patent:
June 26, 2001
Assignee:
Eli Lilly and Company
Inventors:
Jolie Anne Bastian, Nickolay Yuri Chirgadze, Michael Lyle Denney, Matthew Joseph Fisher, Robert James Foglesong, Richard Waltz Harper, Mary George Johnson, Valentine Joseph Klimkowski, Todd Jonathan Kohn, Ho-Shen Lin, Michael Patrick Lynch, Jefferson Ray McCowan, Alan David Palkowitz, Michael Enrico Richett, Daniel Jon Sall, Gerald Floyd Smith, Kumiko Takeuchi, Jennifer Marie Tinsley, Minsheng Zhang
Abstract: The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof. Such compounds and salts are tachykinin antagonists.
Type:
Grant
Filed:
June 1, 1998
Date of Patent:
June 5, 2001
Assignee:
Pfizer Inc.
Inventors:
Alexander Roderick MacKenzie, Allan Patrick Marchington, Donald Stuart Middleton, Sandra Dora Meadows
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:
Grant
Filed:
August 5, 1999
Date of Patent:
May 22, 2001
Assignee:
Applied Research Systems ARS Holding N.A.
Inventors:
Nabil El Tayer, Adulla Reddy, David Buckler, Sharad Magar
Abstract: Pharmaceutical compositions comprising an inhibitor of ras farnesylation of formula (I) wherein, R1 is for example H and further values as defined in the specification; R2 is for example H and further values as defined in the specification; R3 is for example H or a substituent having values as defined in the specification; p is 0-3 in which R3 values can be the same or different; L is a linking moiety for example —CO—NH2— and further values as defined in the specification; A is selected from phenyl; naphthyl; a 5-10 membered monocyclic or bicyclic heteroaryl ring containing up to 5 heteroatoms where the heteroatoms are independently selected from O, N and S; or a —S—S— dimer thereof when R2=H; or an enantiomer, diastereoisomer, pharmaceutically acceptable salt, prodrug or solvate thereof together with a pharmaceutically acceptable diluent or carrier. A particular use is cancer therapy.
Type:
Grant
Filed:
February 3, 1998
Date of Patent:
May 15, 2001
Assignee:
Zeneca Limited
Inventors:
David Huw Davies, Francis Thomas Boyle, James Michael Wardleworth, Peter Wedderburn Kenny, Peter Beverley Scholes, Zbigniew Stanely Matusiak
Abstract: Compounds of formula I are useful antidepressant agents
demonstrating potent inhibition of 5-HT reuptake. Z is selected from among various phenyl and hetaryl moieties while Y is benzyl or indolyl.
Type:
Grant
Filed:
December 21, 1999
Date of Patent:
May 1, 2001
Assignee:
Bristol-Myers Squibb Company
Inventors:
Michael A. Poss, David R. Tortolani, Ronald J. Mattson, Joseph P. Yevich
Abstract: The present invention provides synthetic methodology to produce novel dipeptide compounds and pharmaceutically acceptable salts thereof which exhibit excellent HIV protease inhibitory activity and excellent bioavailability from digestive tracts. Methods of using the dipeptide compounds and pharmaceutically acceptable salts thereof also are provided.
Abstract: The present invention provides an efficient stereoselective method for manufacturing (2S,4S)-2-[[(R)-hydroxy-(3R)-cyclic amine-3-yl]methyl]pyrrolidine-4-thiol or a salt thereof which is useful as an intermediate for the manufacture of carbapenem and also provides the intermediate.
A method for manufacturing which comprises the step of reacting a compound of the formula (I):
(wherein, R1 is a lower alkylsulfonyl group, an optionally substituted arylsulfonyl group or an alkylsilyl group; and R2 is a protecting group for an amino group) with a compound of the formula (II):
(wherein, R3 is a substituted or unsubstituted lower alkyl group or aryl group; X is an oxygen atom or a sulfur atom; Y is an azide group or a nitro group; and m is an integer of 2 to 5).
Abstract: A compound represented by the following formula (12) useful as an intermediate for production of drug or agricultural chemical:
(wherein R21 to R25 are each independently a hydrogen atom, a hydroxyl group, a halogen atom, an alkyl group of 1 to 4 carbon atoms, an alkoxy group of 1 to 4 carbon atoms, a perfluoroalkyl group of 1 to 4 carbon atoms, a cyano group, a nitro group, an amino group, a carboxyl group, a thiol group, an alkylthio group of 1 to 4 carbon atoms or a carbamoyl group) can be produced by reacting a compound represented by the formula (13):
(wherein R21 to R25 have the same definitions as given above) with 1,1-cyclopropanedicarboxylic acid. The compound of the formula (12) is useful as a raw material for production of a pyrrolidinone compound useful as an active ingredient of drug.
Type:
Grant
Filed:
November 13, 1998
Date of Patent:
March 27, 2001
Assignee:
Mitsui Chemicals, Inc.
Inventors:
Hajime Iizuka, Hiroshi Nagase, Naruyoshi Mita
Abstract:
The present invention relates to a novel thrombin inhibitor which is effective even when orally administered. More specifically, the present invention relates to an aromatic amidine derivative represented by formula (I) and the salts thereof, which show potent selective inhibitory activity for thrombin in which (a), R, R1, R2, R3, A, W, Y and n are defined as described in the specification.
Type:
Grant
Filed:
November 13, 1998
Date of Patent:
March 13, 2001
Assignee:
C & C Research Laboratories
Inventors:
Bon Am Koo, Jae Ki Min, Woo Sang Hong, Eun Jung Ryu, Woong Hyun Nam, Jong Min Kim
Abstract: There are electrically conductive, electroactive functionalized conjugated polymers having formula (I):
These electrically conducive, electroactive conjugated polymers may be covalently bonded to a first biological molecule or antiligand. Polymers bonded to a first biological molecule or antiligand may be used to form an electrode and may be used to assay for, detect and/or extract a second biological molecule or ligand.
Abstract: A compound of the following formula:
and the salts thereof wherein A is hydrogen, halo, or hydroxy, broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, or pyridyl, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, or C1-C4 alkyl; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine. These compounds are useful as kappa agonists.
Abstract: This invention is directed to novel (N-substituted) indole ICE/ced-3-inhibitor compounds. The invention is also directed to pharmaceutical compositions of such indole compounds, plus the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury.
Abstract: The present invention comprises a new class of novel aryl and heteroaryl substituted fused pyrrole compounds useful for the prophylaxis and treatment of diseases or conditions, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. In particular, the compounds of the invention are useful for the prophylaxis and treatment of diseases or conditions involving inflammation. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of inflammation and other maladies, such as pain and diabetes, using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Type:
Grant
Filed:
June 8, 1999
Date of Patent:
January 30, 2001
Assignee:
Amgen Inc.
Inventors:
Jeffery A. Zablocki, Eugene Tarlton, Jr., James P. Rizzi, Nathan B. Mantlo
Abstract: A compound which is a distamycin derivative of formula (I), wherein n is 2, 3 or 4; R0is C1-C4 alkyl or C1-C3 haloalkyl; R1 and R2, which may be the same or different, are each hydrogen, C1-C4 alkyl optionally substituted by one or more fluorine atoms, or C1-C4 alkoxy; X is a halogen atom; B is selected from (A, B, C, D, E, F, G, H, I, J and K); wherein R3, R4, R5, R6, R7, R8, and R9, which may be the same or different, are each hydrogen or C1-C4 alkyl, and m is 0, 1, or 2; or a pharmaceutically acceptable salt thereof. Such compounds are useful as antineoplastic and antiviral agents.
Type:
Grant
Filed:
November 13, 1998
Date of Patent:
January 23, 2001
Assignee:
Pharmacia & Upjohn S.p.A.
Inventors:
Paolo Cozzi, Italo Beria, Marina Caldarelli, Maria Cristina Geroni, Enrico Pesenti
Abstract: Selected heterocyclecarbonyl 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:
Grant
Filed:
April 23, 1998
Date of Patent:
January 9, 2001
Assignee:
G. D. Searle & Co.
Inventors:
Daniel P. Getman, Gary A. De Crescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Deyadas, Srinivasan Nagarajan, David L. Brown, Joseph J. McDonald