Abstract: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to &agr;4 integrin. They are used as therapeutic agents for various diseases concerning &agr;4 integrin.
Abstract: This invention describes novel pyrazole compounds of formula IIa:
wherein R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-7 membered ring having 0-3 heteroatoms; and R2 and R2 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
Type:
Grant
Filed:
December 19, 2001
Date of Patent:
November 25, 2003
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
David Bebbington, Jean-Damien Charrier, Robert Davies, Julian M. C. Golec, David Kay, Ronald Knegtel, Sanjay Patel
Abstract: The present invention provides novel nucleoside and nucleotide derivatives that are useful agonists or antagonists of P1 or P2 receptors. For example, the present invention provides a compound of formula A-M, wherein A is modified adenine or uracil and M is a constrained cycloalkyl group. The adenine or uracil is bonded to the constrained cycloakyl group. The compounds of the present invention are useful in the treatment or prevention of various diseases including airway diseases (through A2B, A3, P2Y2 receptors), cancer (through A3, P2 receptors), cardiac arrhythmias (through A1 receptors), cardiac ischemia (through A1, A3 receptors), epilepsy (through A1, P2X receptors), and Huntington's Disease (through A2A receptors).
Abstract: This invention relates to urea compounds containing a pyridine, quinoline, or isoquinoline functionality which is oxidized at the nitrogen heteroatom and which are useful in the treatment of (i) raf mediated diseases, for example, cancer, (ii) p38 mediated diseases such as inflammation and osteoporosis, and (iii) VEGF mediated diseases such as angiogenesis disorders.
Type:
Application
Filed:
February 11, 2003
Publication date:
November 20, 2003
Applicant:
BAYER CORPORATION
Inventors:
Jacques Dumas, William J. Scott, Bernd Riedl
Abstract: A method and composition for the treatment, prevention and/or prophylaxis of a host, and in particular, a human, infected with Epstein-Barr virus (EBV), is provided that includes administering an effective amount of a 5-substituted uracil nucleoside or its pharmaceutically acceptable salt or prodrug, optionally in a pharmaceutically acceptable diluent or excipient.
Type:
Application
Filed:
December 19, 2002
Publication date:
September 18, 2003
Inventors:
Raymond F. Schinazi, Junxing Shi, Joyce D. Fingeroth, Erik Gustafson
Abstract: Substituted aryl ether derived compounds represented by the general structure (I) are described. X and Y are independent of each other and are represented by hydrogen, halogen, cyano, nitro, (C1-4)alkyl, (C1-4)haloalkyl, or (C1-4)haloalkoxy; Z is oxygen or sulfur; Q is selected form Q1 to Q6;
A is oxygen, sulfur, or imino; R1 is hydrogen, (C1-4)alkyl, (C1-4)haloalkyl, or amino and can be independent of each other in a single molecule; R2 and R3 are independent of each other and may be selected from the group consisting of hydrogen, halogen, cyano, nitro, (C1-4)alkyl, (C1-4)haloalkyl, (C2-6)alkenyl, (C2-6)haloalkenyl and amino which may be optionally substituted with (C1-4)alkyl or (C1-4)haloalkyl; Ar is substituted or unsubstituted carbocyclic or heterocyclic aromatic ring being at least a five or six membered ring. This ring can be fused with another substituted or unsubstituted five or six membered carbocyclic or heterocyclic ring.
Type:
Grant
Filed:
December 5, 2001
Date of Patent:
September 2, 2003
Assignee:
Ishihara Sangyo Kaisha, Ltd.
Inventors:
Sandeep Gupta, Masamitsu Tsukamoto, Mark Read
Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure:
wherein A, Q, R1, R2, R3a, R3b, R4, R5, R6 and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
Type:
Grant
Filed:
January 25, 2001
Date of Patent:
August 19, 2003
Assignee:
Neurocrine Biosciences, Inc.
Inventors:
Yun-Fei Zhu, Chen Chen, Fabio C. Tucci, Zhiqiang Guo, Timothy D. Gross, Martin Rowbottom, R. Scott Struthers
Abstract: Methods and compounds useful for the inhibition of convulsive disorders, including epilepsy, are disclosed. The methods and compounds of the invention inhibit or prevent ictogenesis and/or epileptogenesis. Methods for preparing the compounds of the invention are also described.
Type:
Application
Filed:
April 11, 2002
Publication date:
August 14, 2003
Applicant:
Queen's University
Inventors:
Donald F. Weaver, Buhendwa Musole Guillain, John R. Carran, Kathryn Jones
Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
Type:
Application
Filed:
December 20, 2002
Publication date:
August 7, 2003
Inventors:
Francesco Salituro, Guy Bemis, John Cochran
Abstract: This invention relates to certain novel 2′-halomethylidene, 2′-ethenylidene and 2′-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.
Type:
Application
Filed:
June 6, 2002
Publication date:
June 12, 2003
Inventors:
James R. McCarthy, Michael L. Edwards, Donald P. Matthews
Abstract: The present invention relates to inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
Type:
Application
Filed:
December 3, 2001
Publication date:
May 29, 2003
Inventors:
Francesco Salituro, Guy Bemis, Jeremy Green, Jasna Fejzo, Xiaoling Xie
Abstract: The invention relates to novel substituted phenyluracils of the general formula (I)
in which
A represents alkanediyl or alkenediyl, each of which has 2 to 5 carbon atoms and each of which is optionally substituted by cyano, halogen or by in each case optionally halogen- or C1-C4-alkoxy-substituted C1-C4-alkyl, C1-C4-alk-oxy-carbonyl or C2-C4-alkenyl or interrupted by O (oxygen), or represents cyclohexane-1,2-diyl or 1,2-phenylene,
Q1 represents O (oxygen) or S (sulphur),
Q2 represents O (oxygen) or S (sulphur),
R1 represents hydrogen, amino or optionally cyano-, halogen- or C1-C4-alkoxy-substituted alkyl having 1 to 4 carbon atoms,
R2 represents optionally halogen-substituted alkyl having 1 to 4 carbon atoms,
R3 represents hydrogen, halogen or optionally halogen-substituted alkyl having 1 to 4 carbon atoms,
R4 represents hydrogen, cyano, carbamoyl, thiocarbamoyl or halogen,
R5 represents cyano, carbamoyl, thiocarbamoyl or in each case optionally halogen-substituted alkyl or alkoxy ha
Type:
Grant
Filed:
January 10, 2002
Date of Patent:
May 13, 2003
Assignee:
Bayer Aktiengesellschaft
Inventors:
Roland Andree, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
Abstract: The invention relates to novel substituted phenyluraciles of the general formula (I)
in which
m, n, Q and R1-7 are each as defined in the description,
and to processes for their preparation and to their use as herbicides.
Type:
Grant
Filed:
September 5, 2000
Date of Patent:
April 15, 2003
Assignee:
Bayer Aktiengesellschaft
Inventors:
Roland Andree, Markus Dollinger, Mark Wilhelm Drewes, Ingo Wetcholowsky, Randy Allen Myers
Abstract: The invention relates to a process for the preparation of 4,6-dihydroxypyrimidine by reaction of malonic ester with formamide and alkali metal alkoxide. The malonic ester is added alone or simultaneously with the total quantity or a portion of the formamide, in portions or continuously with monitoring of the temperature, to the alkali metal alkoxide prepared as a solution or suspension in an alcohol, alone or together with the total quantity or remaining quantity of the formamide. A temperature of from 102 to <120° C. is then set for from 10 to <60 minutes. The work-up after the holding time in said temperature range is then carried out by methods known per se.
Abstract: Novel uracil substituted phenyl sulfamoyl carboxamides I
and salts thereof, where
A=oxygen or sulfur;
X1=H, halogen, C1-C4-alkyl;
X2=H, CN, CS—NH2, halogen, C1-C4-alkyl, C1-C4-haloalkyl;
X3=H, CN, C1-C6-alkyl, C1-C6-alkoxyalkyl, C3-C7-cycloalkyl, C3-C6-alkenyl, C3-C6-alkynyl, optionally substituted benzyl;
R1, R2=H, halogen, optionally substituted hydroxy, C1-C10-alkyl, C2-C10-alkenyl, C3-C10-alkynyl, C3-C7-cycloalkyl, phenyl, benzyl or C5-C7-cycloalkenyl,
or R1+R2 together with the atom to which they are attached form 3- to 7-membered heterocyclic ring;
Q is selected from Q1 to Q40 as defined in the description.
Use: As herbicides; for the desiccation/defoliation of plants.
Type:
Grant
Filed:
May 4, 2001
Date of Patent:
March 18, 2003
Assignee:
BASF Aktiengesellschaft
Inventors:
Marianne Carlsen, Michael Anthony Guaciaro, James Jan Takasugi
Abstract: Compounds and compositions are provided which are useful for the treatment of viral infections, particularly human Cytomegalovirus infection. The compounds include novel pyrimidine-based derivatives.
Type:
Grant
Filed:
December 15, 2000
Date of Patent:
March 4, 2003
Assignee:
Tularik INC
Inventors:
Timothy D. Cushing, Heather L. Mellon, Juan C. Jaen, John A. Flygare, Shi-Chang Miao, Xiaoqi Chen, Jay P. Powers
Abstract: Phenoxy- and thiophenoxyacrylic acid compounds of the formula I
in which Het, R1, R2, R3, V, W and Z are as defined in claim 1 and processes for their preparation, intermediates for their preparation, herbicidally active compositions comprising the compounds of the formula I and a method for controlling harmful fungi are described.
Type:
Grant
Filed:
June 5, 2002
Date of Patent:
March 4, 2003
Assignee:
BASF Aktiengesellschaft
Inventors:
Gerhard Hamprecht, Michael Puhl, Robert Reinhard, Ingo Sagasser, Cyrill Zagar, Karl-Otto Westphalen, Matthias Witschel, Helmut Walter
Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.
Type:
Grant
Filed:
May 15, 2000
Date of Patent:
February 11, 2003
Assignees:
Emory University, Triangle Pharmaceuticals, Inc.
Inventors:
George R. Painter, Dennis C. Liotta, Merrick R. Almond, Darryl G. Cleary, Josè D. Soria, Marcos Sznaidman
Abstract: Novel 2-alkoxy-5-methoxypyrimidines and tautomeric forms thereof and also processes for preparing them are described. The 2-alkoxy-5-methoxypyrimidines according to the invention can be synthesized in few reaction steps and in high yields from simple precursors.
Abstract: The invention relates to inhibitors of kinases, compositions comprising the inhibitors, and methods of using the inhibitors and inhibitor compositions. The inhibitors and compositions comprising them are useful for treating disease or disease symptoms. The invention also provides for methods of making kinase inhibitor compounds, methods of inhibiting kinase activity, and methods for treating disease or disease symptoms.
Type:
Application
Filed:
February 16, 2001
Publication date:
January 2, 2003
Inventors:
David M. Armistead, Jean E. Bemis, Lucian V. DiPietro, Stephanie D. Geuns-Meyer, Gregory J. Habgood, Joseph L. Kim, Joseph J. Nunes, Vinod F. Patel, Leticia M. Toledo-Sherman
Abstract: The invention relates to a process for preparing ar(alk)yluracils of the general formula (I)
in which
A represents a single bond or represents alkanedlyl,
Ar represents optionally substituted aryl,
R1 represents optionally substituted alkyl and
R2 represents hydrogen, halogen or alkyl,
and to novel intermediates for this purpose and to processes for their preparation.
Abstract: Disclosed are compositions inducing cleavage of an RNA substrate, as well as their use for inducing cleavage of RNA substrates in vitro and in vivo. The compositions contain part of an active center, with the other part of the active center provided by the RNA substrate. The subunits of the active center region of the compositions are nucleotides and/or nucleotide analogues. The disclosed compositions also have flanking regions contributing to the formation of a specific hybridization with an RNA substrate. Preferred compositions form, in combination with an RNA substrate, a structure resembling a hammerhead structure. The active center of the disclosed compositions is characterized by the presence of I15.1 which allows cleavage of RNA substrates having C16.1.
Abstract: The invention relates to novel substituted phenyluracils of the general formula (I)
in which
R1, R2, R3, R4, R5 and R6 are each as defined in the description,
to processes for their preparation, to novel intermediates and to their use as herbicides.
Type:
Grant
Filed:
January 16, 2001
Date of Patent:
September 24, 2002
Assignee:
Bayer Aktiengesellschaft
Inventors:
Roland Andree, Mark Wilhelm Drewes, Markus Dollinger, Hans-Joachim Santel
Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women.
Type:
Application
Filed:
January 25, 2001
Publication date:
September 19, 2002
Applicant:
Neurocrine Biosciences, Inc.
Inventors:
Yun-Fei Zhu, Chen Chen, Fabio C. Tucci, Zhiqiang Guo, Timothy D. Gross, Martin Rowbottom, R. Scott Struthers
Abstract: There are provided compositions and methods comprising compounds of formula I:
wherein R1, A, B, X, Y and Z have the meaning given in claim 1, for the control of insect and acarid pests.
Type:
Grant
Filed:
November 29, 2000
Date of Patent:
August 27, 2002
Assignee:
BASF Aktiengesellschaft
Inventors:
William Wakefield Wood, Linda Fleming, Salvatore John Cuccia
Abstract: The invention is directed to a process for the preparation of a substituted phenyluracil of the formula:
The process broadly comprises reacting a carbonylphenyluracil of the formula:
with an amino compound, an alcohol or a mercaptan. The resultant products are useful as herbicides.
Type:
Grant
Filed:
April 24, 2001
Date of Patent:
August 20, 2002
Assignee:
Bayer Aktiengesellschaft
Inventors:
Mark Wilhelm Drewes, Roland Andree, Markus Dollinger
Abstract: Heterocyclically substituted benzamides of the formula I
are described, where R1, R2, R3, R4, R5, X, m and n have the meanings given in the description. The novel compounds are useful for controlling diseases.
Abstract: A compound having the formula:
wherein X′ is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; X is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value greater than 0, less than 0, but not equal to 0; A, A′ and A″ are individually substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; Z′ is a substituent other than hydrogen; j is an integer from 0 to 5; and the wavy line in the structure indicates that the compound can exist in the form of an enantiomer or a diasteromer; Z″ is hydrogen or a substituent other than hydrogen; Y is C═O, C(OH)R′ or C—A, where R′ is hydrogen or lower alkyl.
Type:
Grant
Filed:
April 27, 2000
Date of Patent:
July 9, 2002
Assignee:
Targacept, Inc.
Inventors:
Peter Anthony Crooks, Haeil Park, Balwinder Singh Bhatti, William Scott Caldwell, Gary Maurice Dull
Abstract: The invention relates to novel aminouracils of the general formula (I)
in which,
Q, R1, R2, R3, R4, R5, R6 and R7 are each as defined in the description, to their use as herbicides and to novel intermediates.
Type:
Grant
Filed:
January 21, 1998
Date of Patent:
July 9, 2002
Assignee:
Bayer Aktiengesellschaft
Inventors:
Roland Andree, Mark Wilhelm Drewes, Otto Schallner, Markus Dollinger, Hans-Joachim Santel
Abstract: A 5,6-dihydrouracil compound given by the formula [I]:
wherein, R1 represents C1-C2 haloalkyl group and Q represents Q1 of the formula below, etc.:
wherein, R3 is hydrogen atom or halogen atom, R15 is C3-C6 alkynyl group, etc., Z is oxygen atom, sulfur atom or NH group, and T is direct bond or methylene group, has an excellent herbicidal efficacy.
Abstract: The present invention relates to methods and compositions for preparing biologically important nucleoside analogues containing 1,3-dioxolane sugar rings. In particular, this invention relates to the stereoselective synthesis of the beta (cis) isomer by glycosylating the base with an intermediate of formula (II) below a temperature of about −10° C.
Type:
Application
Filed:
November 16, 2001
Publication date:
May 16, 2002
Applicant:
BIOCHEM PHARMA INC.
Inventors:
Tarek Mansour, Alex Cimpoia, Krzysztof Bednarski
Abstract: The invention relates to inhibitors of kinases, compositions comprising the inhibitors, and methods of using the inhibitors and inhibitor compositions. The inhibitors and compositions comprising them are useful for treating disease or disease symptoms. The invention also provides for methods of making kinase inhibitor compounds, methods of inhibiting kinase activity, and methods for treating disease or disease symptoms.
Type:
Application
Filed:
February 16, 2001
Publication date:
May 2, 2002
Inventors:
David M. Armistead, Jean E. Bemis, Lucian V. DiPietro, Stephanie D. Geuns-Meyer, Gregory J. Habgood, Joseph L. Kim, Joseph J. Nunes, Vinod F. Patel, Leticia M. Toledo-Sherman
Abstract: Compounds incorporating aryl substituted olefinic amine are provided. Representative compounds are (4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-pyrimidinyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-methoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(6-amino-5-methyl-3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-bromo-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-ethoxy-3-pyridyl)-4-penten-2-amine, (2S)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine and (2S)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine.
Type:
Application
Filed:
October 9, 2001
Publication date:
May 2, 2002
Applicant:
Targacept, Inc.
Inventors:
William Scott Caldwell, Gary Maurice Dull, Balwinder Singh Bhatti, Srishailkumar B. Hadimani, Haeil Park, Jared Miller Wagner, Peter Anthony Crooks
Abstract: The disclosure concerns pyrimidine derivatives represented by the following general formulas [I] and [I′] and having antiviral activity, particularly antiretroviral activity such as anti-HIV activity:
and pharmaceutical compositions having antiviral activity and comprising the above-described derivative(s) as an active ingredient.
Type:
Grant
Filed:
October 23, 1997
Date of Patent:
February 4, 2003
Assignee:
Mitsubishi Chemical Corporation
Inventors:
Tadashi Miyasaka, Hiromichi Tanaka, Erik Desiré DeClercq, Masanori Baba, Richard Thomas Walker, Masaru Ubasawa