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7615560 |
Thienopyrimidines as cooling agents
Use of a compound of formula (I) where R 1 is a C 4-6 alkylene linkage optionally substituted by a C 1-4 alkyl group; R 2 is ═NH, —NH 2 or —OH; R 3 is C 1-5 alkyl optionally terminated...
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7598259 |
mGluR1 antagonists as therapeutic agents
In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J 1 -J 4 , X, and R 1 -R 5 are as defined herein) useful as metabotropic glutamate receptor...
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7579356 |
Thia-tetraazaacenaphthylene kinase inhibitors
The present invention is directed to novel thia-tetraazaacenaphthylene compounds of Formula (I):
and pharmaceutically acceptable forms thereof and their synthesis and use as inhibitors of...
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7576092 |
Benzofuro- and benzothienopyrimidine modulators of the histamine H4 receptor
Benzofuro- and benzothienopyrimidine compounds are described, which are useful as H 4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment...
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7576091 |
Thiazolo-, oxazalo and imidazolo-quinazoline compounds capable of inhibiting protein kinases
A compound of formula 1, or a pharmaceutically acceptable salt thereof, wherein:
X is S, O, or NH; “a” is a single bond; or “a” is a double bond and one of R 3 and R 4 , and one of R 5...
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7572802 |
7-[2-[4-(6-fluoro-3-methyl-1,2-benzisoxazol-5-yl)-1-piperazinyl]ethyl]-2-(1-propynyl)-7H-pyrazolo-[4,3-e]-[1,2,4]-triazolo-[1,5-C]-pyrimidin-5-amine
The compound having the structural formula I
or a pharmaceutically acceptable salt thereof, is disclosed, as well as its use in the treatment of central nervous system diseases, in particular...
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7557116 |
Substance which exhibits antiviral and antibacterial activity and is based on derivatives of 2,8-dithioxo-1H-pyrano[2,3d 6,5-d′]dipyrimidyne and 10-aza-analogue thereof
The present invention relates generally to synthetic pyrimidine derivatives and, more particularly, to the methods of deriving the compounds that are the derivatives of...
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7547706 |
1H-pyrimido[4,5-b]indole derivatives, their preparation and therapeutic use
The invention concerns compounds of general formula (I):
Wherein n, X, Y, R 1 and R 2 are as defined herein. The invention also concerns a method for preparing the compounds and their...
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7547705 |
Substituted 8′-pyri(MI)dinyl-dihydrospiro-[cycloalkylamine]-pyrimido[1,2-a]pyrimidin-6-one derivatives
The invention relates to a dihydrospiro-[cycloalkylamine]-pyrimidone derivative represented by formula (I) or a salt thereof:
wherein: X, Y, R1, R2, R3, R4, o, m, n, p and q are as defined...
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7528141 |
Use of cyclopenta[g]quinazoline derivatives for treating cancer
Method for aiding regression and palliation of a solid tumor in a patient in need of such treatment, comprising administering to the patient an effective amount of a cyclopenta[g]quinazoline of the...
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7511125 |
Pyrimidine derivatives for labeled binding partners
Compounds having structure (1)
wherein R 1 is —H a protecting group, a linker or a binding partner; and R 2 and R 34 are as defined in the specification. The invention also provides...
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7511050 |
Purinone derivatives as HM74A agonists
The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their...
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7507743 |
Substituted 8′-pyridinyl-dihydrospiro-[cycloalkyl]-pyrimido[1,2-a] pyrimidin-6-one and 8′-pyrimidinyl-dihydrospiro-[cycloalkyl]-pyrimido[1,2-a] pyrimidin-6-one derivatives
The invention relates to therapeutic uses of a dihydrospiro-[cycloalkyl]-pyrimidone derivative represented by formula (I) or a salt thereof:
wherein X, Y, R1, R2, R3, m, n, p and q are as...
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7501418 |
Fused heterocyclic isoxazoline derivatives and their use as anti-depressants
The invention concerns fused heterocyclic isoxazoline derivatives of Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof...
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7498336 |
Deazaflavin compounds and methods of use thereof
The present invention features 5-deazaflavin compounds, pharmaceutical compositions of 5-deazaflavin compounds and methods of treating a patient suffering from cancer, the method comprising...
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7491729 |
3-Substituted 3,4-dihydro-thieno[2,3-d]pyrimidin-4-one derivatives, production and use thereof
3-Substituted 3,4-dihydrothieno[2,3-d]pyrimidin-4-one derivatives, production and use thereof. The invention relates to 3,4-dihydrothieno[2,3-d]pyrimidin-4-one derivatives which are substituted in...
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7485648 |
mGluR1 antagonists as therapeutic agents
In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J 1 -J 4 , X, and R 1 —R 5 are as defined herein) useful as metabotropic glutamate receptor...
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7482354 |
Pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors
Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical...
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7473694 |
Pyrazolopyrimidine derivatives or pharmaceutically acceptable salts thereof
A pyrazolopyrimidine derivative represented by formula (1) and pharmaceutically acceptable salt thereof exhibit excellent inhibitory activity against MAPKAP-K2. Accordingly, medicines containing...
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7470698 |
Adenosine A3 receptor modulators
The compounds of the following formula:
wherein R, R 2 , R 3 and A have the meanings given in the specification, are endowed with selective A 3 adenosine receptor antagonist activity. These...
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7470690 |
4-(2-Fluorophenyl)-6-methyl-2-(1-piperazinyl)thieno[2,3-D)pyrimidine in the treatment of functional bowel disorder
Use of 4-(2-Fluorophenyl)-6-Methyl-2-(1-Piperazinyl)Thieno[2,3-D]Py
rimidine or a salt thereof for the manufacture of a medicament for the treatment of functional bowel disorder.
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7468373 |
Arylindenopyridines and arylindenopyrimidines and related therapeutic and prophylactic methods
This invention provides novel arylindenopyridines and arylindenopyrimidines of the formula:
wherein R 1 , R 2 , R 3 , R 4 , and X are as defined above, and pharmaceutical compositions...
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7465740 |
2-heteroaryl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
Compounds having the structural formula I
or a pharmaceutically acceptable salt thereof, wherein
R is R 1 -isoxazolyl, R 1 -oxadiazolyl, R 1 -dihydrofuranyl, R 1 -pyrazolyl, R 1...
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7465739 |
Compounds and their use in therapy
Thiophenepyrimidinone compounds and their use in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent diseases or disorders, such as steroid hormone...
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7462624 |
Purinone derivatives as HM74a agonists
The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their...
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7459459 |
Tri-heterocyclic compounds and a pharmaceutical comprising them as an active ingredient
Tri-heterocyclic compound of formula (I)
wherein each of W, X and Y is carbon or nitrogen; each of U and Z is CR 2 , NR 13 , nitrogen, oxygen, sulfur etc.; A ring is carbocyclic ring,...
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7446108 |
Tri-and tetraaza-acenaphthylen derivatives as CRF receptor antagonists
CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded...
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7439249 |
Inhibitors of phosphatases
The present invention relates to compounds that inhibit phosphatases, compositions thereof, and methods of using those compounds and compositions for treating diseases.
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7435740 |
Adenosine A3 receptor modulators
A class of novel antagonists for the adenosine A 3 receptor are disclosed. These compounds are useful as therapeutic agents for a number of diseases and medical conditions that are mediated by the...
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7429598 |
Spirocondensed quinazolinones and their use as phosphodiesterase inhibitors
The invention relates to compounds of formula (I)
wherein R 1 , R 2 and m are as defined in the description, their use as medicament, pharmaceutical compositions containing them and a process...
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7427625 |
Substituted thiatriazaacenaphthylene-6-carbonitrile kinase inhibitors
The present invention is directed to substituted thiatriazaacenaphthylene-6-carbonitrile compounds of formula (I):
and forms thereof, their synthesis and use for treating, preventing or...
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7419969 |
HIV integrase inhibitors: cyclic pyrimidinone compounds
The invention encompasses a series of pyrimidinone compounds which inhibit HIV integrase and thereby prevent viral integration into human DNA. This action makes the compounds useful for treating...
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7414058 |
Adenosine A2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders
There is disclosed a method for the treatment of Extra Pyramidal syndrome (EPS) comprising the administration of an adenosine A2a receptor antagonist, alone or in combination with other agents...
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7407964 |
Caspase inhibitors and uses thereof
This invention provides novel caspase inhibitors of formula I:
wherein R 1 is hydrogen, CHN 2 , R, or —CH 2 Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group,...
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7388014 |
Quinazoline derivatives and therapeutic use thereof
Quinazoline derivatives represented by the general formula
pharmacologically acceptable salts thereof, and compositions containing such compounds are described. Methods for using the compounds...
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7378424 |
Derivatives of pyrimido[6, 1-A]isoquinolin-4-one
The invention provides compounds or salts thereof of the general formula (I):
wherein each of R 1 and R 2 independently represents a C 1-6 alkyl or C 2-7 acyl group; X represents OCH 2 or...
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7371765 |
Quinoline derivatives having VEGF inhibiting activity
The invention relates to compounds of formula (I) wherein: either any one of G 1 , G 2 , G 3 , G 4 and G 5 is nitrogen and the other four are —CH—, or G 1 , G 2 , G 3 , G 4 and G 5 are all...
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7371757 |
Fused heterocycles as inhibitors of glutamate racemase(MURI)
This invention relates to novel compounds having formula: (I) or (II) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis...
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7368449 |
2-alkynyl- and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
Compounds having the structural formula I
or a pharmaceutically acceptable salt thereof, wherein
R is
R 1 , R 2 , R 3 , R 4 and R 5 are H, alkyl or alkoxyalkyl; R 6 is...
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7365078 |
Triaza-cyclopenta[cd]indene derivatives
An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be...
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7361664 |
Vitamin D receptor antagonists and related compositions and methods of use
A compound of formula:
wherein X is a C 2-10 spacer, and R is a substituted or unsubstituted C 6-30 aryl, a substituted or unsubstituted C 5-30 heteroaryl, or
Where R′...
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7358255 |
Therapeutic agent for keratoconjunctival disorder
Object of the present invention is to search a novel pharmaceutical use of 5-[4-(6-methoxy-1-methyl-1H-benzimidazol-2-ylmethoxy)benzyl]
thiazolidine-2,4-dione being a condensed heterocyclic...
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7345049 |
Phenylalanine derivatives
Specific phenylalanine derivatives and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin.
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7329668 |
Pyrazolopurine-based tricyclic compounds and pharmaceutical compositions comprising same
The present invention provides for pyrazolopurine-based tricyclic compounds having the formula (I),
wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as described herein. The present invention...
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7329667 |
CRF receptor antagonists
The present invention relates to tricyclic pyrimidines compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof,
to processes for...
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7329666 |
Derivatives of variolin B
The invention provides antitumour compounds of formula (I), wherein R 1 is an aromatic substituent; R 2 is hydrogen or a substituent when the dotted line is absent, or R 2 is absent when the...
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7326713 |
Substituted tricyclic compound as protein kinase inhibitors
Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following...
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7326712 |
Substituted tricyclic compounds as protein kinase inhibitors
Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following...
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7320981 |
Variolin derivatives as anti-cancer agents
The invention provides variolin derivatives of formula (I), wherein: R 1 and R 2 are each independently selected from the group consisting of H, OH, OR, SH, SR, SOR, SO 2 R, NO 2 , NH 2 , NHR,...
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7319103 |
Non-imidazole tertiary amines as histamine 3 receptor inhibitors for the treatment of cognitive and sleep disorders, obesity and other CNS disorders
This invention relates to compounds having pharmacological activity, to compositions containing these compounds, and to a method of treatment employing the compounds and compositions. More...
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