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7601840 |
Carboline derivatives useful in the inhibition of angiogenesis
In accordance with the present invention, compounds that inhibit the expression of VEGF post-transcriptionally have been identified, and methods for their use provided. In one aspect of the...
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7576072 |
Heterocyclic inhibitors of MEK and methods of use thereof
Disclosed are compounds of the Formula I
and pharmaceutically acceptable salts and prodrugs thereof, wherein R 1 , R 2 , R 7 , R 8 and R 9 , W, X, Y and Z are as defined in the specification....
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7482336 |
Aminocyclohexanes as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
The present invention is directed to novel substituted aminocyclohexanes which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment...
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7465726 |
Substituted pyrrolo[2.3-B]pyridines
Compounds represented by Formula (I):
or stereoisomers or pharmaceutically acceptable salts thereof, are inhibitors of least two of the Abl, Aurora-A, Blk, c-Raf, cSRC, Src, PRK2, FGFR3,...
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7417041 |
Imidazopyrimidines as transforming growth factor (TGF) inhibitors
Novel fused heteroaromatic compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described....
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7265128 |
3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and...
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7230100 |
Stereoselective method for the preparation of nucleosides
A process for producing predominantly cis nucleosides or nucleoside analogues and derivatives of formula (A):
wherein R1 is a pyrimidine base or a pharmaceutically acceptable derivative thereof...
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7179910 |
3-(4-amidopyrrol-2-ylmethlidene)-2-indolinone derivatives as protein kinase inhibitors
The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to...
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7074929 |
Certain alkylene diamine-substituted heterocycles
This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The novel compounds encompassed by the...
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7038053 |
Process for imidazo[4,5-c]pyridin-4-amines
A process and intermediates for preparing 1H-imidazo[4,5-c]pyridin-4-amines are disclosed. The process includes providing a 7H-imidazo[4,5-c]tetrazolo[1,5-a]pyridine and converting a...
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6992188 |
Substituted heterocyclic derivatives
Corticotropin-releasing factor (CRF) antagonists having the formula
wherein the dashed lines, A, B, D E, F, Z, G, R 3 , and R 5 having the definitions set forth in the specification...
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6984646 |
Imidazopyridinones as p38 map kinase inhibitors
The invention relates to imidazopyridinones of the formula
wherein the groups R 1 , R 2 , R 3 , and R 4 are as defined in claim 1, to the process for their preparation, to pharmaceutical...
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6875772 |
[1,2,4]-Triazole bicyclic adeonsine A2a receptor antagonists
Compounds having the structural formula I
wherein:
n is 0, 1, 2 or 3; A is C(R 1 ) or N; R 1 and R 1a are H, (C 1 -C 6 )-alkyl, halo, CN or —CF 3 ; X is —C(O)—, —O—, —SO...
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6867217 |
Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade
The invention relates to substituted polycyclic aryl and heteroaryl pyridone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods...
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6673810 |
Imidazo-heterobicycles as factor Xa inhibitors
The present application describes imidazo-heterobicycles of formulas I and III: or pharmaceutically acceptable salt or prodrug forms thereof. Compounds of the present invention are useful as...
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6610692 |
Thrombin inhibitors
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein b is NY...
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6569869 |
Annulated azole derivatives useful as microbicidal agents
Novel fused azole derivatives of the formula in which R 1 , R 2 , A and G are as defined in the description, and also their acid addition salts and metal salt complexes, a plurality of processes...
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6525056 |
Heterocyclyl-substituted ring-fused pyridines and pyrimidines as corticotropin releasing hormone (CRH) antagonists, useful for treating cns and stress-related disorders
Corticotropin releasing factor (CRF) antagonists of Formula (I): and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress...
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6479506 |
Triazolo-pyridine derivatives as ligands for GABA receptors
Substituted or 6,7-ring fused 1,2,3-triazolo[4,5-b]pyridine derivatives are selective ligands for GABA A receptors useful in the treatment of disorders of the central nervous system.
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6458950 |
Compounds and pharmaceutical compositions containing the same
A compound shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the...
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6159975 |
Antagonists of gonadotropin releasing hormone
There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety...
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6156766 |
Benzamide compounds and pharmaceutical use thereof
Benzamide compounds of the formula ##STR1## wherein each symbol is defined in the specification, isomers thereof and pharmaceutically acceptable acid addition salts thereof. Pharmaceutical...
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6046136 |
Herbicidal heterocyclic N-oxides compounds
This invention relates to novel optionally substituted heterocyclic N-oxide compounds of formula (I): ##STR1## wherein: R, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , A, X, Z and m are defined...
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5912348 |
Method of making arylamino triazolopyridines
Method for making 4-arylamino-1-alkyl- 1,2,3!triazolo 4,5-c!pyridines by base-promoted isomerization of 7-alkylamino-3-aryl- 1,2,3!triazolo 4,5-b!pyridines.
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5874382 |
Cyclic sulfonamide herbicides
Compounds of Formula I and II, and their agriculturally-suitable salts, are disclosed which are useful for controlling undesired vegetation ##STR1## wherein X is a direct bond; O; S; NH; N(C 1 -C...
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5846990 |
Substituted biphenyl isoxazole sulfonamides
Compounds of the formula ##STR1## inhibit the activity of endothelin. The symbols are defined as follows: R 1 , R 2 , R 3 and R 4 are each directly bonded to a ring carbon and are each...
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5840894 |
Preparation of 1,2,4-triazolium salts and 1,2,4-triazolines
A process for the preparation of 1,2,4-triazolium salts Ia ##STR1## where R 1 , and R 2 and R 3 are C-organic radicals, it being possible for R 2 and R 3 to be connected to give a 5- to...
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5767141 |
Substituted propane derivatives, a process for their preparation and the use of the compounds for treating diseases
Substituted propane derivatives, a process for their preparation and the use of the compounds for treating diseases Propane derivatives of the formula I ##STR1## in which the radicals have the...
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5719170 |
Substituted cyclohexanol esters, their use for treating diseases, and pharmaceutical preparations
Cyclohexanol esters of the formula I ##STR1## are described in which the radicals have the given meaning. The compounds are pharmacologically active and may therefore be used as pharmaceuticals, in...
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5679700 |
Substituted phosphinic acid-containing peptidyl derivatives as antidegenerative agents
Novel phosphinic acid-containing peptidyl compounds of formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis,...
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5599773 |
(2-imidazolin-2-yl) fused heteropyridine compounds and use of said compounds as herbicidal agents
There are provided novel (2-imidazolin-2-yl) fused heteropyridine compounds, and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and...
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5593943 |
Heteroaromatically condensed hydroxypyridonecarboxamides, their preparation and use as herbicides
Heteroaromatically condensed hydroxypyridonecarboxamides of the structure I ##STR1## where the substituents and the ring Q have the following meanings: R 1 hydrogen, hydroxyl, substituted or...
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5536839 |
(2-Imidazolin-2-yl) fused heteropyridine compounds
There are provided novel (2-imidazolin-2-yl) fused heteropyridine compounds, and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and...
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5514688 |
Carbocyclic adenosine analogs useful as immunosuppressants
This invention relates to carbocyclic adenosine compounds of the formula (1) ##STR1## wherein the hydroxy substituent on the cyclopentanyl ring is in the CIS configuration relative to the bicyclic...
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5459129 |
Condensed heterocyclic compounds, their production and use
A novel compound of the formula: ##STR1## wherein a ring A stands for an optionally substituted 5-membered ring; B stands for an optionally substituted divalent cyclic or chain group; either one of...
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5302596 |
Tricyclic compounds as TXA.sub.2 antagonists
Novel tricyclic compound represented by formula ##STR1## possess a TXA 2 biosynthesis inhibiting activity and/or a TXA 2 receptor antagonizing activity, and are expected to have preventive and...
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5290936 |
Nitro substituted chemiluminescent labels and their conjugates, and assays therefrom
A novel chemiluminescent labeling compositions comprising an ester, thiolester or amide covalently and jointly bonded to (1) a carbon of a heterocyclic ring or ring system that is susceptible to...
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5256661 |
Substituted 2-aminotetralins and pharmaceutical use
Certain novel compounds having the structural formula ##STR1## where R 2 , R 3 and R 4 are each selected from the group consisting of H and OA; A is H or is selected from the group consisting of...
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5248681 |
Dihydropyridine antiallergy agents
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5240937 |
Pharmaceutically active triazolopyridine compounds
This invention describes the preparation and use of anticonvulsant agents. In particular, triazolopyridine compounds are described which have utility in the treatment of epilepsy in mammals.
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5232930 |
2-heteroaryl-substituted benzodioxoic having 5-lipoxygenase inhibitory activity
The invention concerns a benzodioxole derivative of the formula I ##STR1## wherein Ar 1 is an optionally substituted 9- or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen...
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5214044 |
1,4-dihydropyridines useful as pharmaceuticals
The invention provides compounds of the formula: ##STR1## The variables are defined in the specification. The compounds are useful e.g. for the curative or prophylactic treatment of allergic...
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5166209 |
Pharmacologically active compounds
This invention describes the preparation and use of anticonvulsant agents. In particular, triazolopyridine compounds are described which have utility in the treatment of epilepsy in mammals.
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5133798 |
Certain herbicidal 1,2,4-triazolo[4,5-b]pyridines
A compound of formula (I): ##STR1## in which the dotted lines indicate the presence of two double bonds arranged so as to form a fused hetero-aromatic ring system; Ar is an optionally...
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5077407 |
Substituted 2-[monoannelated (3,4-,4,5-, and 5,6-) pyridylalkylenesulfinyl]benzimidazoles
The present invention provides novel substituted 2-[monoannelated(3,4- 4,5-, and 5,6-)pyridylalkylenesulfinyl]-benzimidazoles with gastric acid inhibiting effects.
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5039689 |
Antiparasitic 3(4-amino benzotriazo-1-yl-)1,2-cyclopentanediols
The present invention relates to the use of a compound of formula (I) ##STR1## wherein R represents a hydrogen atom; a C 1 -4 alkyl group; a group COR 1 wherein R 1 represents amino or C 1...
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5010198 |
Intermediates for the synthesis of benzoxazol- and benzothiazolamine derivatives, useful as anti-anoxic agents
Benzoxazol- and benzothiazolamine derivatives having anti-anoxic properties which compounds are useful in the treatment of anoxia. These compounds are produced from certain benzoxazol- and...
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4908056 |
Heterocyclic acyl sulfonamides
This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.
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4861785 |
Benzoxazol-and benzothiazolamine derivatives, useful as anti-anoxic agents
Benzoxazol-and benzothiazolamine derivatives having anti-anoxic properties which compounds are useful in the treatment of anoxia.
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4816457 |
Aralkylaminoethanol heterocyclic compounds
Heterocyclic aminoethanols of the formula: Het--CHOH--CH 2 --NH-aralkyl where Het is a 6-10 membered N-heterocycle are disclosed. The compounds are useful as pharmaceuticals.
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