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7384952 |
Pyrazolopyrimidine compound and a process for preparing the same
The present invention provides a novel pyrazolopyrimidine compound of the formula [I]: wherein R′ is (A) a substituted aryl group, (B) an optionally substituted nitrogen-containing aliphatic...
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7378409 |
Substituted cycloalkylamine derivatives as modulators of chemokine receptor activity
The present application describes modulators of MCP-1 of formula (I):
or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis,...
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7371750 |
Compounds and compositions as protein kinase inhibitors
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated...
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7345048 |
Heterocyclic compounds and uses thereof as D-alanyl-D-alanine ligase inhibitors
The invention relates to D-Ala-D-Ala ligase inhibitors having the formula:
wherein R 1 is NH 2 ; R 2 is NH 2 ; R 3 is selected from hydrogen, alkyl, amino, hydroxy, alkoxy, and alkylamino;...
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7332498 |
Modulation of KSP kinesin activity with heterocyclic-fused pyrimidinone derivatives
A method of modulating KSP kinesin activity in vitro comprising contacting KSP kinesin with at least one chemical entity chosen from compounds represented by Formula I:
and pharmaceutically...
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7332497 |
Pyrazolopyrimidines as therapeutic agents
The present invention provides compounds of Formula I,
including pharmaceutically acceptable salts and/or prodrugs thereof, where G, R a , R 2 , and R 3 are defined as described herein.
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7323471 |
Topical azathioprine for the treatment of oral autoimmune diseases
A method for treating or preventing symptoms associated with oral autoimmune diseases comprises treating a patient with an oral topical formulation of azathioprine or a pharmaceutically acceptable...
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7285558 |
Pyrazolo[3,4-d]pyrimidines inhibiting H. pylori infections
Compounds having the general formula
and pharmaceutical compositions containing them, and their use in the treatment or prophylaxis of H. pylori infection.
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7276491 |
Anticoagulant and fibrinolytic therapy using p38 MAP kinase inhibitors
Disclosed are methods for a treating a disease or condition relating to blood coagulation and fibrinolysis using p38 MAP kinase inhibitors.
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7268133 |
Cannabinoid receptor ligands and uses thereof
Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein
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7268128 |
1,3,5-trisubstituted-5-phenyl and 5-pyridyl pyrazolopyrimidinone derivatives having PDE7 inhibiting action
Pyrazolopyrimidinone derivatives expressed by the following general formula (IA) or (IB):
where the symbols are as disclosed in the specification, are provided as desired compounds. These...
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7262200 |
Indazolinone compositions useful as kinase inhibitors
The present invention provides compounds of formula I:
These compounds, and pharmaceutically acceptable compositions thereof, are useful generally as kinase inhibitors, particularly as...
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7262192 |
Substituted pyrazolo[4,3-d]pyrimidines and their use as PDE-5 inhibitors
The present invention comprises a class of 5,7-diaminopyrazolo[4,3-d]pyrimidine compounds. These compounds are useful as phosphodiesterase type 5 inhibitors. The present invention further comprises...
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7259157 |
N-substituted nonaryl-heterocyclo amidyl NMDA/NR2B Antagonists
Compounds represented by Formula (I):
or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.
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7235551 |
1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
Novel substituted pyrimidol[4,5-d]pyrimidin-2-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.
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7223387 |
Antiviral formulations comprising propylene glycol and an isopropyl alkanoic acid ester
A topical composition comprising an antiinflammatory glucocorticoid and a nucleoside analogue antiviral agent in a pharmaceutical carrier characterized in that the carrier comprises about 15 to...
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7173039 |
Protein kinase inhibitors
Disclosed are compounds which inhibit or modulate the activity of protein kinases and pharmaceutical compositions containing such compounds. The disclosed compound contain two or more ligand...
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7157449 |
Medicament for the treatment of diseases caused by parasitic protozoa
The present invention relates to the use of an inhibitor of CTP synthetase, such as a glutamine analogue, and a substance capable of suppressing toxic effects thereof in vivo, in the manufacture of...
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7148228 |
Pyrazolopyrimidines and related analogs as HSP90-inhibitors
A compound represented by Formula I, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:
wherein: R 1 is halogen, —OR 1 , —SR 11 or...
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7135493 |
HDAC inhibitor
A compound having the following formula (I):
wherein
R 1 is N-containing heterocyclic ring optionally substituted with one or more suitable substituent(s), R 2 is hydroxyamino, R 3 is...
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7132426 |
Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
The present invention relates to certain fused aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism.
Accordingly, compounds of the present invention are useful in the...
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7115658 |
Inhibitors of hepatitis C virus RNA-dependent RNA polymerase
Compounds of formula I are hepatitis C virus (HCV) RNA-dependent RNA polymerase (RdRp) inhibitors, and are useful in therapeutic and prophylactic treatment of persons infected with hepatitis C virus
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7091209 |
Dihydroxypyridmidine carboxylic acids as viral polymerase inhibitors
A class of 2-aryl-4,5-dihydroxy-6-carboxypyrimidines of formula (I): wherein Ar is an optionally substituted aryl or heterocyclicgroup; as well as compounds of formula (I) which are derivatized at...
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7078408 |
[1,2,4]-Triazole bicyclic adenosine 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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7074797 |
Pyrazolopyrimidines as CRF receptor antagonists
This invention concerns compounds of formula
including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R 1 is NR 4 R 5 or OR 5 ; R 2 is C 1-6...
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7064119 |
Fused bicyclic pyrimidine derivatives
A novel fused bicyclic pyrimidine derivative or a salt thereof that acts as a tachykinin receptor antagonist and, in particular, as an NK1 receptor antagonist is represented by the following...
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7053073 |
Treatment for reactive arthritis or bursitis
A treatment for conditions in human beings associated with either or both reactive arthritis or bursitis comprising a combination of valacyclovir hydrochloride, minocycline hydrochloride, and...
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7041666 |
Adenosine A2a receptor antagonists
Disclosed are compounds having the structural formula
or pharmaceutically acceptable salts or solvates thereof, wherein
R is optionally substituted heteroaryl, optionally substituted...
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7030129 |
Method of reducing and treating UVB-induced immunosuppression
Methods of preventing and/or treating UV-induced immunosuppression by administration of immune response modifier compounds are disclosed herein. Suitable immune response modifier compounds include...
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7022709 |
Selective PDE 2 inhibitors as pharmaceuticals for improving perception
The invention relates to the use of selective phosphodiesterase 2 (PDE 2) inhibitors for producing pharmaceuticals for improving perception, concentration, learning and/or memory.
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RE39056 |
4-Azasteroids for treatment of hyperandrogenic conditions
Compounds of structural Formula (I)
and pharmacologically acceptable salts and esters thereof possess 5α-reductase inhibitory activity. These compounds inhibit 5α-reductase type 1 and type...
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6989386 |
Pharmaceutically active ornithine derivatives, ammonium salts thereof and methods of making same
In one embodiment, the present invention relates to a new class of ammonium salts of N δ -acyl derivatives of N α -(4-amino-4-deoxypteroyl)-L-ornithine compounds having a structure according to...
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6967204 |
Treatment of insulin resistance syndrome and type 2 diabetes with PDE9 inhibitors
This invention is directed to a method of treating insulin resistance syndrome (IRS), hypertension and/or type 2 diabetes in a mammal comprising administering to said mammal a cGMP PDE9 inhibitor...
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6964957 |
Fused pyrazole compounds, pharmaceutical compositions, and methods for modulating or inhibiting ERAB or HADH2 activity
Pyrazole compounds represented by the formula:
are described. The pyrazole compounds and pharmaceutical compositions containing them may be used in inhibiting ERAB or HADH2 activity and in...
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6962915 |
Pyrazolo-pyrimidine aniline compounds useful as kinase inhibitors
Compounds having the formula (I),
and pharmaceutically acceptable salts or prodrugs thereof, are useful as kinase inhibitors, wherein Y is —C(═O)NR 1 —, —NR 1 C(═O)—, —NR 1...
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6960592 |
1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one compound for the treatment of impotence
The present invention relates to new 1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one compounds of formula (I), or a pharmaceutically acceptable salt or a stereoisomer thereof, useful for treatment of...
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6939884 |
Pharmaceutical agents containing acyclovir, fusaric acid and derivatives thereof
Compositions are provided, which comprise at least one nucleoside analogue inhibitor, pharmaceutically acceptable salts, solvates, or prodrugs thereof and fusaric acid, derivatives, or...
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6930113 |
Nitrosated and nitrosylated phosphodiesterase inhibitors, compositions and methods of use
The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase...
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6903096 |
Quinazoline derivatives as medicaments
The invention is directed to methods to inhibit TGF-β and/or p38-α kinase using compounds of the formula
or the pharmaceutically acceptable salts thereof
wherein R 3 is a...
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6894054 |
Heterocyclic inhibitors of glycine transporter 2
Compounds, compositions, and methods for inhibiting the glycine transporter 2 and for inhibiting glycine transporter mediated neuronal activity. These compounds are particularly useful for...
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6894041 |
Oxazolyl-acid amide derivatives useful as inhibitors of PDE4 isozymes
This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic...
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6894021 |
Method for identifying and using A2B adenosine receptor antagonists to mediate mammalian cell proliferation
This invention concerns methods for identifying A 2B adenosine receptor agonists and antagonists as well as methods for using A 2B adenosine receptor antagonists to treat cell proliferation...
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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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6875745 |
Method and composition for the treatment of cancer
We have discovered that the administration of a G1 and/or S phase drug such as β-lapachone in combination with a G2/M drug such as a taxane derivative such as paclitaxel resulted in a greater than...
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6869945 |
Pyrrolyl-and imidazolyl-acid amide derivatives useful as inhibitors of PDE4 isozymes
This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic...
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6867208 |
Vitronectin receptor antagonists, their preparation and their use
The present invention relates to compounds of the formula I
A—B—D—E—F—G (I)
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6864254 |
Inhibitor for 20-hete-yielding enzyme
An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is...
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6858616 |
Nitrogen containing heterobicycles as factor Xa inhibitors
The present application describes nitrogen containing heterobicyclics and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
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6815434 |
Methods for treating hearing loss
In one aspect, the present invention provides otoprotectant compositions useful for ameliorating hearing loss. In some embodiments, the otoprotective compositions comprise at least one glutathione...
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6784174 |
Pyridine and pyrimidine derivatives and their use as inhibitors of cytokine mediated disease
This invention concerns a bicyclic compound of Formula (I), wherein: G is N, CH or C(CN); ring X is a 5- or 6-membered fused heteroaryl ring which contains 1, 2, or 3 heteroatoms selected from...
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