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7381738 |
Substituted bicycloalkylamine derivatives as modulators of chemokine receptor activity
The present application describes modulators of MCP-1 of formula (I):
or stereoisomers or pharmaceutically acceptable salts thereof, wherein X, Z, a, b, c, d, n, R 1 , R 2 , R 3 , R 4 , R 5 , R...
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7371751 |
Thiazole derivatives
The present invention relates to compounds of formula (I)
wherein R 1 , R 2 , R 3 and R 4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof, for use...
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7361682 |
Indole derivatives as H3 inverse agonists
The present invention relates to compounds of formula I:
wherein X, R 1 , R 2 , R 3 , R 4 and R 5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof,...
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7358245 |
Treatment of gastroesophageal reflux disease
The administration of cannabinoid receptor agonists for inhibition of transient lower esophageal sphincter relaxations, gastroesophageal reflux disease and regurgitation is disclosed.
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7323462 |
Morpholine dopamine agonists
Compounds of formula (I), (Ia) and (Ib)
useful as a medicament.
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7319098 |
1,3-dioxoisoindole derivatives having selective antagonism of T-type calcium channel
The present invention relates to 1,3-dioxoisoindole derivatives of Formula (1) or pharmaceutically acceptable salts thereof, a preparation method thereof and use thereof as a T-type calcium channel...
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7256189 |
3-(4-amidopyrrol-2-ylmethylidene)-2-indolinone der 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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7256188 |
3-aminoalkyl-2-aryl-indole derivatives and their use as GnRH antagonists
The present invention relates to compounds of formula I which are antagonists of gonadotropin releasing hormone (GnRH) activity. The invention also relates to pharmaceutical formulations, the use...
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7250413 |
C-25 carbamate rifamycin derivatives with activity against drug-resistant microbes
Compounds of the current invention relate to rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms. More specifically, compounds of the...
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7247627 |
Salts and polymorphs of a pyrrole-substituted indolinone compound
The invention relates to non-hygroscopic salts of 5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl
]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-
pyrrole-3-carboxamide,...
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7244730 |
2-iminopyrrolidine derivatives
A 2-iminopyrrolidine derivative represented by the formula:
{wherein ring B represents a benzene ring, pyridine ring, etc.; R 101 –R 103 represent hydrogen, halogen, C 1-6 alkyl, etc.; R 5 ...
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7241789 |
Substituted indoles and their use as integrin antagonists
The present invention relates to novel substituted indole compounds that are antagonists of alpha V (αv) integrins, for example α v β 3 and α v β 5 integrins, their pharmaceutically...
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7241754 |
2-Desmethyl ansamycin compounds
2-Desmethyl ansamycins having a structure according to formula I, where R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined herein, and other 2-desmethyl ansamycins are useful as antiproliferative...
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7189727 |
Guanidino compounds
Compounds having the general structure III are provided:
where D is N or C; W is selected from
Z 1 , Z 2 , and Z 3 are independently selected from CR 8 and N; and the other variables have...
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7173027 |
Receptor selective cannabimimetic aminoalkylindoles
Disclosed are cannabimimetic aminoalkylindole compounds and methos for their manufacture. The disclosed compounds are surprisingly potent and selective cannabinoinds. Also disclosed are methods of...
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7169775 |
Amino methyl imidazoles as C5a receptor modulators
Amino methyl imidazoles of Formula I are provided:
wherein R, R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are defined herein.
Such compounds are ligands of C5a receptors. Preferred compounds of...
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7163949 |
4-phenyl substituted tetrahydroisoquinolines and use thereof
Provided herein are compounds of the formulae IA–IF. These compounds are tetrahydroisoquinolines of the following structure:
wherein R 1 –R 8 for compounds of each of the formulae IA, IB,...
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7148249 |
Indolinones substituted by heterocycles, the preparation thereof and their use as medicaments
The present invention relates to heterocyclically substituted indolinones of general formula
wherein
R 1 to R 5 and X are defined as in claim 1, the tautomers, the diastereomers, the...
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7141595 |
Amino benzothiazole compounds with NOS inhibitory activity
The present invention provides novel amino benzothiazole compounds, compositions comprising these compounds and methods of using these compounds as neuroprotectants. In particular, the compounds...
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7138410 |
Aza-bicyclic N-biarylamides with affinity for the α7 nicotinic acetylcholine receptor
The invention relates to novel 1-aza-bicyclic N-biarylamides, methods for production and use thereof for the production of medicaments for the treatment and/or prophylaxis of diseases and for...
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7135466 |
Quinoline and quinazoline derivatives and drugs containing the same
There are provided compounds which can be used in the treatment of diseases mediated by the autophosphorylation of a PDGF receptor, specifically, compounds which can inhibit neointima formation...
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7129240 |
1,3-dihydro-2H-indol-2one derivatives, process for preparing them and pharmaceutical compositions containing them
The invention relates to compounds of formula:
as well as the possible salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, which have affinity for and...
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7125870 |
Isoxazoline derivatives as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme
The present application describes novel isoxazoline of formula I or II:
or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, R 1 , R 2 , R 3 , R 4 , Z, U, X, Y, Z a , and n...
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7109231 |
Cyclohept[b]indole derivatives
A novel class of tricyclic compounds of the following formula (I): (formula I); is disclosed together with the use of such compounds for inhibiting sPLA 2 mediated release of fatty acids for...
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7109212 |
Quinoline and isoquinoline derivatives, a process for their production and their use as inflammation inhibitors
The invention relates to quinoline and isoquinoline derivatives of general formula I
and a process for their production, and their use as inflammation inhibitors.
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7109196 |
1,8 Naphthyridine derivatives and their use to treat diabetes and related disorders
The invention relates generally to naphthyridine derivatives of the formula
wherein one of U, X, Y and Z is nitrogen and the others are C—R, where R is hydrogen or a substituent. More...
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7105516 |
Compounds for the treatment of premature ejaculation
The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts or solvates thereof and pharmaceutically acceptable formulations comprising said compounds
useful...
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7101881 |
Tetrahydroquinolines
The present invention relates to compounds of formula I
wherein X and Y are as defined in the specification, and to pharmaceutical compositions comprising the compound of formula I and a...
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7101877 |
Ion channel modulating compounds and uses thereof
Ion channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and...
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7084157 |
Ophthalmic pharmaceutical compositions and methods for treating ocular inflammation
The present invention relates to novel ophthalmic pharmaceutical compositions comprising an inflammation-treating amount of a 4-aminoquinoline compound, derivative, isomers, or chemical salts, and...
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7053086 |
4-heteroaryl-3-heteroarylidenyl-2-indolinones and their use as protein kinase inhibitors
The present invention relates to certain 4-heteroaryl-3-heteroarylidenyl-2-indolinones compounds and their physiologically acceptable salts which modulate the activity of protein kinases...
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7049314 |
Cyclopentyl indole derivatives
The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts or solvates thereof and pharmaceutically acceptable formulations comprising said compounds
useful...
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7049309 |
3-Thia-4-arylquinolin-2-one potassium channel modulators
This invention describes compounds of Formula (I) which are modulators of potassium channels and are useful for treating conditions affected by abnormal potassium channel activity including...
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7041668 |
Substituted benzimidazole compounds and their use for the treatment of cancer
The present invention discloses and claims benzimidazole compounds of formula (I):
in which A is aryl or heteroaryl; R 1 is selected from optionally substituted alkyl, alkoxy, aryl or...
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7041667 |
CCR5 modulators
Compounds of Formula 1
[R egion α]—[R egion β]—[R egion γ]—[R egion δ] (1)
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7019004 |
Hydantoin derivatives with affinity for somatostatin receptors
The invention provides compounds of formula (I) wherein X, Y, R 1 , R 2 , R 3 and R 4 are as defined in the description, and the preparation thereof. The compounds of the formula bind to...
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6992092 |
Anti-diabetic agents
The present invention provides compounds of formula (I)
the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs; wherein...
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6992084 |
Compounds and methods for modulating CXCR3 function
The invention provides compounds and compositions of the formula:
wherein,
the subscript n is an integer of from 0 to 4; Ar is a member selected from the group consisting of substituted...
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6982263 |
Nitriles useful as reversible inhibitors of cysteine proteases
Disclosed are novel nitrile compounds of formula (I) further defined herein, which compounds are useful as reversible inhibitors of cysteine proteases such as cathepsin K, S, F, L and B. These...
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6972288 |
4-amino-quinazoline and quinoline derivatives having an inhibitory effect on signal transduction mediated by tyrosine kinases
The present invention relates to bicyclic heterocycles of general formula
wherein
R a to R d , A to G and X are defined as in claim 1, the tautomers, the steroisomers and the salts...
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6962928 |
Tetrahydroquinoline derivatives for the inhibition of osteoporosis, estrogen dependent breast cancer, endometriosis and uterine fibrosis
The current invention provides methods for inhibiting osteoporosis, estrogen dependent breast cancer, endometriosis and uterine fibrosis comprising administering to a patient in need thereof a...
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6960597 |
Aza-bridged-bicyclic amino acid derivatives as α4 integrin antagonists
The invention is directed to aza-bridged-bicyclic compounds having Formula (I):
and pharmaceutically acceptable salts thereof. The compounds are useful (α4 integrin receptor antagonists and,...
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6943160 |
Morpholine derivatives as antagonists of orexin receptors
This invention relates to morpholine derivatives of formula (I) and their use as antagonists of orexin receptors.
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6924285 |
Bicyclic heterocyclic compounds, pharmaceutical compositions containing these compounds, their use and process for preparing them
The present invention relates to bicyclic heterocyclic groups of general formula
wherein
R a , R b , R c , R d and X are defined as in claim 1, the tautomers, the stereoisomers, the...
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6919335 |
Heterocycles that are inhibitors of IMPDH enzyme
Compounds of the formula
wherein X 1 is C(O), —S(O)—, or —S(O) 2 —;
X 2 is CR 3 or N; X 3 is —NH—, —O—, or —S—;
X 4 is CR 4 or N; X 5 is CR 5 or N; and X 6 is...
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6900206 |
Indole, azaindole and related heterocyclic sulfonylureido piperazine derivatives
This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with sulfonylureido...
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6900205 |
1,8-Naphthyridine derivatives and their use to treat diabetes and related disorders
The invention relates generally to naphthyridine derivatives of the formula
wherein one of U, X, Y and Z is nitrogen and the others are C—R, where R is hydrogen or a substituent. More...
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6855711 |
Pharmaceutical compositions comprising iron chelators for the treatment of neurodegenerative disorders and some novel iron chelators
Use of a compound of formula (I), wherein R 1 is H or hydrocarbyl; R 2 is a hydrophobic radical; R 3 is 3-(C 2 -C 6 )acyl-4-hydroxyphenyl, 3-hydroxyimino (C 2 -C 6 )-alkyl-4-hydroxyphenyl, or...
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6855710 |
Substituted indolines with an inhibitory effect on various kinases and complexes of CDKs
The present invention relates to new substituted indolinones of general formula
wherein
X and R 1 to R 5 are defined as in claim 1, the isomers and the salts thereof which have valuable...
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6846818 |
Selective inhibitors of cyclooxygenase-2
The present invention relates to cyclooxygenase-2 (COX-2) selective inhibitors of formula I:
pharmaceutical compositions containing them, to their medicinal use, and to their preparations. The...
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