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7601728 |
Bicyclic pyrrole derivatives
Compounds represented by the general formula (I), prodrugs thereof, or pharmaceutically acceptable salts of both are provided as compounds which have high DPP-IV inhibiting activity and are...
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7601727 |
Pyrrolo[2,3-d]pyrimidine compounds
A compound of the formula
wherein R 1 , R 2 and R 3 are as defined above, which are inhibitors of the enzyme protein kinases such as Janus Kinase 3 and as such are useful therapy as...
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7601713 |
Kinase inhibitors and their uses
The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein...
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7598257 |
Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the...
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7598256 |
Pyrrolo [2,3-d] pyrimidine and their use as purinergic receptor antagonists
Use of a compound of the formula (I) wherein R 1 is selected from alkyl, alkoxy, aryloxy, alkylthio, arylthio, aryl, halogen, CN, NR 7 R 8 , NR 6 COR 7 , NR 6 CO 2 R 9 and NR 6 SO 2 R 9 ; R 2 is...
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7598255 |
Pyrimidine compounds as serotonin receptor modulators
Certain pyrimidine-containing compounds are serotonin receptor modulators useful in the treatment of serotonin-mediated diseases.
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7595325 |
Substituted pyrrolo[2,3-d]pyrimidine derivatives useful in cancer treatment
The invention relates to compounds of the formula 1
or a pharmaceutically acceptable salt, prodrug, solvate or hydrate thereof, wherein L, R 1 , R 2 , R 3 and R 4 are as defined herein. The...
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7585868 |
Substituted pyrazolo[3,4-D]pyrimidines as kinase antagonists
The present invention provides novel compounds that can be used as antagonists of a lipid kinase such as a PI3 kinase, protein tyrosine kinase, and/or protein serine-threonine kinases such as mTOR....
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7557113 |
Substituted pyrrolo[3,2-d]pyrimidine derivatives
A compound having GSK-3 inhibitory activity.
A 1 and A 3 are a single bond, an aliphatic hydrocarbon group; A 2 and A 4 are a single bond, CO, COO, CONR, O, OCO, NR, NRCO, NRCOO, etc.; G 1 ...
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7553839 |
5h-pyrrolo[3,2-D] pyrimidine inhibitors of nucleoside phosphorylases and nucleosidases
The present invention relates to compounds of the general formula (I) which are inhibitors of purine muclioside phosphorylases (PNP), purine phosphoribosyltransferases (PPRT),...
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7544672 |
Alkynyl pyrrolo[2,3-d]pyrimidines and related analogs as HSP90-inhibitors
Alkynyl pyrrolo[2,3-d]pyrimidines and related analogs are described and demonstrated to have utility as Heat Shock Protein 90 (HSP90) inhibiting agents used in the treatment and prevention of...
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7534795 |
Compounds and their use related to compositions for treating disease
Novel compounds and their uses are disclosed herein.
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7531546 |
Spiro-substituted pyrrolo[2,3-D]pyrimidines as cathepsin inhibitors
The invention provides compounds of formula (I) or a pharmaceutically acceptable salt or ester thereof formula (I) wherein the symbols have the meaning as defined in the description. Said compounds...
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7528140 |
Substituted pyrrolo[3,2-d]pyrimidines as glycogen synthase kinase (GSK) inhibitors
The invention provides pyrrolo[3,2-d]pyrimidine derivatives represented by formula (I), and their medically acceptable salts. The compounds of the invention exhibit GSK-3 inhibiting activity and...
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7507740 |
Fused heterocyclic compound
The present invention relates to a compound represented by the formula:
wherein W is C(R 1 ) or N, each A is an optionally substituted aryl group or a heteroaryl group, X 1 is —NR 3 —Y 1...
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7504407 |
Compounds specific to adenosine A1 and A3 receptors and uses thereof
This invention pertains to compounds having the structure:
wherein
m is 0, 1, 2, or 3; R 2 is a substituted or unsubstituted imidazole or pyrazole wherein the point of attachment of R 2...
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7504398 |
Substituted-4-(pyrrolo pyrimidin-6-yl)benzenesulphonamide derivatives
This invention is directed to selective antagonists of A 2A and/or A 2B adenosine receptors having the general formula (I); to processes for their preparation; to pharmaceutical compositions...
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7498334 |
Pyrrolopyrimidines as phosphodiesterase VII inhibitors
Pyrrolopyrimidine derivatives of the formula I
in which R 3 , R 4 , R 5 , R 6 and X are as defined in claim 1 , act as phosphodiesterase VII inhibitors and can be employed for the treatment...
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7470697 |
Pyrrolo[3,2-D] pyrimidines that are selective antagonists of A2B adenosine receptors
The present invention provides compounds of the following formula and pharmaceutical compositions that are selective antagonists of A 2B adenosine receptors (ARs).
These compounds and...
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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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7462622 |
Pyrrolo[2, 3-d] pyrimidine derivatives as corticotropin releasing factor antagonists
The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof
wherein
R is aryl or heteroaryl and...
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7452892 |
Triazolopyrimidine cannabinoid receptor 1 antagonists
The present application describes compounds according to both Formulas I and II, pharmaceutical compositions comprising at least one compound according to either Formula I or II and optionally one...
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7452886 |
Pyrrolo pyrimidines as agents for the inhibition of cystein proteases
The invention provides compounds of Formula I or a pharmaceutically acceptable salt or ester thereof wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use...
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7449473 |
Substituted pyrrolo[3,2-d]pyrimidin-2,4-diones as A2b adenosine receptor antagonists
Disclosed are novel compounds that are A 2B adenosine receptor antagonists having the following structure:
wherein R 1 and R 2 are independently chosen from hydrogen, optionally substituted...
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7449472 |
Methods of inhibiting p38 with substituted bicyclic pyrimidines
The present invention discloses compounds corresponding to the formula
wherein A, X, Y, R, R 1 and R 2 are as defined within, pharmaceutical formulations, methods of making and uses thereof.
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7439247 |
Bicyclic pyridine and pyrimidine P38 kinase inhibitors
The present invention discloses compounds corresponding to formula
wherein A, R, X, Y, R, R 1 and R 2 are as defined above, pharmaceutical formulations, methods of making and uses thereof.
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7439240 |
Purine-or pyrrolol[2,3-d]pyrimidine-2-carbonitiles for treating diseases associated with cysteine protease activity
The present invention therefore provides a compound of formula (I) and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of...
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7435739 |
Substituted pyrrolopyrimidines useful in the treatment of cancer
The invention relates to compounds of the formula 1
or a pharmaceutically acceptable salt, prodrug or hydrates thereof, wherein X, L, R 1 , R 2 , R 3 and R 4 are as defined herein. The...
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7429596 |
1H-pyrrolo [2,3-D] pyrimidine derivatives and methods of use thereof
This invention generally relates to pyrazolo pyrimidine derivatives useful as inhibitors of short chain dehydrogenase/reductase (SDR) family of NAD(P)(H) dependent oxido-reductases. The invention...
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7429581 |
Pyrazole-derivatives as factor Xa inhibitors
The present invention is directed to a compound of formula I,
in which R 0 ; R 1 ; R 2 ; R 3 ; R 4 ; Q; V, G and M have the meanings indicated below. The compound of formula I is a...
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7429574 |
4-heterocyclo-pyrrolo[2,3d] pyrimidine compositions and their use
Novel deazapurines are disclosed which are useful for the treatment of adenosine receptor stimulated diseases.
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7427624 |
Purine nucleoside phosphorylase inhibitory phosphonate compounds
The invention is related to phosphorus substituted purine nucleoside phosphorylase inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the...
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7427616 |
Condensed pyridines and pyrimidines with tie2 (TEK) activity
A compound of the Formula (I), wherein A together with the carbon atoms to which it is attached forms a fused 5-membered heteroaryl ring, wherein said heteroaryl ring contains 1 or 2 heteroatoms...
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7423043 |
4-Piperidin-1-yl-7H-pyrrolo[2,3-d]pyrimidine compounds
Substituted 4-piperidin-1-yl-7H-pyrrolo[2,3-D]pyrimidine compounds are disclosed, as well as compositions comprising them and methods of their use for the treatment, prevention and management of...
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7390805 |
4-amino-6-phenyl-pyrrolo[2,3-d]pyrimidine derivatives
The invention relates to 7H-pyrrolo[2,3-d]pyrimidine derivatives of formula I
wherein the symbols and substituents are as defined in the description, to processes for the preparation thereof,...
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7388005 |
Substituted 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 7-pyrimidinyl-2,3-dihydroimidazo [1,2-a]pyrimidin-5(1H)one derivatives for neurodegenerative disorders
The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein: X represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C 1-2 alkyl group and a...
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7381729 |
4-(4-trans-hydroxycyclohexyl)amino-2-phenyl-7H-pyrrolo [2,3D] pyrimidine hydrogen mesylate, its polymorphic forms, and methods for making same
The present invention relates to the novel compound 4-(4-trans-hydroxycyclohexyl)amino-2-phenyl-7H-pyrrolo[2,3d]
pyrimidine hydrogen mesylate, the polymorphic α and β forms thereof, and a method...
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7358250 |
Pyrrolo[2,3-d]pyrimidines that modulate ACK1 activity
Compounds that modulate the action of ACK1 and LCK, and related compositions methods for treating ACK1- and LCK-mediated diseases are described. In one aspect, the compounds have the general...
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7326699 |
4-Amino-5-phenyl-7-cyclobutyl-pyrrolo(2,3-d)pyrimidine derivatives
The invention relates to new 4-amino-5-phenyl-7-cyclobutyl-pyrrolo[2,3-d]pyrimidine derivatives, processes for the preparation thereof, the application thereof in a process for the treatment of the...
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7323469 |
7H-pyrrolo[2,3-d]pyrimidine derivatives
The invention relates to 7H-pyrrolo[2,3-d]pyrimidine derivatives of formula I
wherein the symbols and substituents are as defined in the description, to processes for the preparation thereof,...
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7319102 |
Pyrrolo[2,3-d]pyrimidine cytokine inhibitors
The present invention relates to 2,6,7-substituted pyrrolo[2,3-d]pyrimidines which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or...
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7307082 |
Heterocyclic derivatives as CRF antagonists
This invention relates to compounds which are generally CRF-1 receptor antagonists and which are represented by Formula I wherein X 1 is (CH 2 ) n or CO, n is 0 to 2 and R 1 , R 2 , R 3 and R 4 ...
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7301023 |
Chiral salt resolution
A method for resolving enantiomers of a compound containing the structure of the forula:
wherein R 4 or R 5 may contan one or more asymmetric centers, by mixing a racemic mixture of...
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7279474 |
Substituted pyrrolo[2,3-d]pyrimidines as antagonists of the corticotropin releasing factor (CRF)
The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof wherein the variables are as defined in the...
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7271262 |
Pyrrolopyrimidine derivatives
The invention relates to compounds of the formula 1
or a pharmaceutically acceptable salt, prodrug or hydrates thereof, wherein Q, A, L, R 1 , R 2 and R 3 are as defined herein. The invention...
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7259159 |
Guanidino derivatives as inhibitors of cell adhesion
The present invention relates to acylguanidino derivatives of formula (I), in which R 1 , R 2 , R 3 , A, B, X, Y and n have the meanings indicated in claim 1 , their physiologically tolerable...
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7259154 |
Pyrrolopyrimidines
Compounds of the formula
and N-oxides, prodrugs, acid bioisosteres, pharmaceutically acceptable salts or solvates of such compounds, or N-oxides, prodrugs, or acid bioisosteres of such salts or...
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7253166 |
6-phenyl-7H-pyrrolo[2,3-d]pyrimidine compounds that induce neuronal differentiation in embryonic stem cells
The invention provides a novel class of compounds and compositions of Formula I:
in which R 1 , R 2 and R 3 are defined herein, that are useful in the treatment or prevention of diseases...
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7250420 |
Method of treatment of transplant rejection
A method of treating or preventing chronic organ transplant rejection comprising administering a compound of the formula
wherein R 1 , R 2 and R 3 are as defined above.
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7232827 |
Heteroaryl substituted 2-pyridinyl and 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one derivatives
The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein: (I) X represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C 1-2 alkyl group...
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