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Class 544/325 - Substituent on 5-position contains carbocyclic ring


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein a substituent which contains a carbocyclic
No. of patents: 142
Last issue date: 09/23/2008


1        
NumberTitleIssue Date
7427628Heterocyclic compounds which inhibit leukocyte adhesion mediated by αintegrins
Disclosed are compounds which bind α4 integrins, preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by α4 integrins, preferably VLA-4. Such compounds are useful in the ...
09/23/2008
7371758Antimalarial pyrimidine derivatives and methods of making and using them
Compounds of the formula (I) wherein R1 represents a hydrogen atom or a 3-halogen atom, and R2 represents a straight-chain alkyl group containing up to 6 carbon atoms, a straight-chain alkyl group containing up to 3 carbon atoms with unsubstitu...
05/13/2008
7319100Substituted pyrazinones, pyridines and pyrimidines as corticotropin releasing factor ligands
Compounds provided herein are novel substituted pyrazinones, pyridines and pyrimidines of Formula (I) and (II): Such compounds are particularly useful as CRF receptor ligands, and hence, in the treatment of vario...
01/15/2008
7317014Bio-active pyrimidine molecules
The present invention relates to novel derivatives of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmaceutical...
01/08/2008
73170152-Substituted pyrimidines
The invention relates to 2-substituted pyrimidines of the formula I in which the index n and these substituents R1, R2 and R3 are as defined in the description and R4 i...
01/08/2008
7288547CDK-inhibitory 2-heteroaryl-pyrimidines, their production and use as pharmaceutical agents
This invention relates to 2-heteroaryl-pyrimidine derivatives of general formula I or If as inhibitors of the cyclin-dependent kinases, their production as well as their use as medications for treating various diseases. ...
10/30/2007
7205297Substituted 5-alkynyl pyrimidines having neurotrophic activity
The present invention relates to a series of novel substituted 5-alkynyl pyrimidines, pharmaceutical compositions which contain them, methods for their preparation, and their use in therapy, particularly in the treatment of neurodegenerative or other neurological di...
04/17/2007
7205310Pyrimidine hydantoin analogues which inhibit leukocyte adhesion mediated by VLA-4
Disclosed are compounds which bind VLA-4 and/or LPAM-1. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4 and/or LPAM-1. Such compounds are useful in the treatment of inflammatory diseases in a mammal...
04/17/2007
71574554-Aminopyrimidine-5-one derivatives
Novel 4-aminopyrimidine-5-one derivatives are disclosed. These compounds inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are ...
01/02/2007
71538605-Phenylpyrimidines, methods and intermediate products for the production thereof and use of the same for controlling pathogenic fungi
The invention relates to 5-phenylpyrimidine of formula (I) wherein the substituents have the following designations: R1 represents a five to ten-membered saturated, partially unsaturated or aromatic monocyclic or bicyclic heterocycle which contains betwee...
12/26/2006
7153964Pyrimidine compounds
Pyrimidine derivatives of formula (I) wherein: Qh1 and Q2 are independently selected from aryl or carbon linked heteroaryl optionally substituted as defined within; and one of Q1 and Q2 or both Q1 and Q2
12/26/2006
7148198Antibacterial agents
A compound of formula (I) or a pharmaceutically or veterinarily acceptable salt thereof for the inhibition of activity of bacterial PDF enzyme: wherein A represents a group of formula (IA) or (IB)
12/12/2006
70675222,4,DI (hetero-) arylamino (-oxy)-5-substituted pyrimidines as antineoplastic agents
Pyrimidine derivatives of formula (I) wherein Q1, Q2, G and R1 are as defined within; and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described. Processes for their manufacture, pharmaceutical compos...
06/27/2006
7026328Heterocyclic compounds which inhibit leukocyte adhesion mediated by αintegrins
Disclosed are compounds which bind α4 integrins, preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by α4 integrins, preferably VLA-4. Such compounds are useful in the ...
04/11/2006
7008949Heterocyclic compounds which inhibit leukocyte adhesion mediated by αintegrins
Disclosed are compounds which bind α4 integrins, where the α4 integrin is preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by α4 integrins, where the α
03/07/2006
6953802Beta-amino acid derivatives-inhibitors of leukocyte adhesion mediated by VLA-4
Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, su...
10/11/2005
6951866Bicyclic pyrimidine compounds and therapeutic use thereof
1. A pyrimidine derivative of the formula (1) or a salt thereof; has an inhibitory activity of production of Th2 type cytokines such as IL-4, IL-5, etc., and is useful as an therapeutic agent for allergic diseases, aut...
10/04/2005
6943172Rho-kinase inhibitors
Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary hea...
09/13/2005
6943252Fungicidal 5-phenyl substituted 2-(cyanoamino) pyrimidines
Pyrimidines of formula I in which R1 represents hydrogen or alkyl, haloalkyl, alkenyl, alkynyl, alkadienyl, alkoxy, cycloalkyl, phenyl, or 5- or 6-membered heteroaryl or 5-...
09/13/2005
6924290Rho-kinase inhibitors
Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary hea...
08/02/2005
68384642,4-Di(hetero-)arylamino(-oxy)-5-substituted pyrimidines as antineaoplastic agents
Pyrimidine derivatives of formula (I) wherein Q1, Q2, G and R1 are as defined within; and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described. Processes for their manufacture, pharmaceutical compos...
01/04/2005
6818649Chromenylmethyl pyrimidinediamines as antibacterial agents
This invention is concerned with substituted chromene derivatives of the general formula (I) in which R1-R4 are as defined in the specification and claims. The invention further relates to the pha...
11/16/2004
67875392,4,5,-trisubstituted pyrimidine derivatives
The invention relates to compounds of the formula wherein R1 is lower alkyl, lower alkoxy, pyridinyl, pyrimidinyl, phenyl, —S-lower alkyl, —S(O)2-lower alkyl, —N(R)—(CH2)
09/07/2004
6656935Aromatic nitrogen-containing 6-membered cyclic compounds
An aromatic nitrogen-containing 6-membered cyclic compound of the formula (I): ##STR1## wherein Ring A is a substituted or unsubstituted nitrogen-containing heterocyclic group; R1 is a substituted or unsubstituted lower alkyl group, --NH--...
12/02/2003
6586459Antithrombotic agents
This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well a...
07/01/2003
6583173Antithrombotic agents
This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well a...
06/24/2003
6583148Neurotrophic substituted pyrimidines
The present invention relates to novel derivatives of a series of substituted pyrimidines, to pharmaceutical compositions which contain them, to methods for their preparation and to their use in therapy, particularly in the treatment of neurodegenerative ...
06/24/2003
6518425Method of manufacture of 1,3-oxathiolane nucleosides
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 process...
02/11/2003
6479498Sodium channel drugs and uses
The compounds of this invention comprise 2-10 ligands covalently connected, each of the ligands being capable of binding to a ligand binding site in a Na+ channel, thereby modulating the biological activities thereof....
11/12/2002
6410729Substituted pyrimidine compounds and methods of use
Selected novel substituted pyrimidine compounds are effective for prophylaxis and treatment of diseases, such as TNF-଱, IL-1ଲ, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel c...
06/25/2002
6313151Antithrombotic agents
This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its...
11/06/2001
6254669Bleed reduction agents for ink printing inks
A compound of the Formula (1) and salts thereof: ##STR1## wherein: Ar, Ar1, J, J1, X, X1 W, W1, L and m are as defined in the description. The compounds of Formula (1) are useful as additives in inks, especially...
07/03/2001
6251900Heterocyclic compounds and antitumor agent containing the same as active ingredient
Heterocyclic compounds in which s-triazine or pyrimidine is substituted with benzimidazole and morpholine and which are represented by the Formula I or phermaceutically acceptable acid addition salts thereof: ##STR1## wherein X and Y respectively represen...
06/26/2001
6235746Substituted 2-anilinopyrimidines useful as protein kinase inhibitors
Compounds of general formula (1) are described: ##STR1## wherein R1 is a hydrogen or halogen atom or an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group or a group selected from hydroxyl (--OH), substituted hydr...
05/22/2001
6229011N-aroylphenylalanine derivative VCAM-1 inhibitors
Compounds of the formula: ##STR1## are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 ...
05/08/2001
6172066Dihydropyrimidines and uses thereof
This invention is directed to dihydropyrimidine compounds which are selective antagonists for human 򳄚 receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthes...
01/09/2001
6136971Preparation of sulfonamides
The present invention provides a process for preparing 1,2-diheteroethylene sulfonamide of the formula: ##STR1## by reacting a pyrimidine monohalide of the formula: ##STR2## with a mono-protected 1,2-diheteroethylene anion of the formula M1...
10/24/2000
6124308Optically active phenyl pyrimidine derivatives as analgesic agent
A pyrimidine of formula (I) ##STR1## and its pharmaceutically acceptable acid addition salts are useful as analgesics, as anticonvulsants or in the treatment of irritable bowel syndrome or bipolar disorder....
09/26/2000
5958935Substituted 2-anilinopyrimidines useful as protein kinase inhibitors
2-Anilinopyrimidines, processes for their preparation, pharmaceutical compositions containing them, their use in medicine. In a preferred embodiment, the compounds have the general formula (1): ##STR1## wherein R1 is preferably methoxy; R
09/28/1999
5939424Compounds for treating disorders of lipid metabolism and their preparation
The invention relates to 4-Amino-2-ureidopyrimidine-5-carboxamides of the formula I ##STR1## in which R1 is H or (C1 -C8)-alkyl, where one or more H can be replaced by F; R2 is selected from the group consi...
08/17/1999
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