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7384939 |
Process for preparation of pyridine derivatives of NK-1 receptor antagonist
The present invention provides a process for preparing a pyridine compound of the formula:
wherein R 1 , R 2 , R 3 and a are those defined herein.
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7335653 |
Bis-aryl sulfonamides
Compounds are provided that act as potent antagonists of chemokine receptors. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the...
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7320977 |
Substituted 2-phenyl-3(2h)-pyridazinones
The invention relates to substituted 2-Phenyl-3(2H)-Pyridazinones, to a method for the production thereof, and to their use as medicaments for the prophylaxis and/or treatment of diseases in humans...
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7312211 |
Pryanone compounds useful as reversible inhibitors of cysteine proteases
Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R 2 , R 3 , R 4 , R 6 , R 8 and Y are defined herein. The compounds are useful for...
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7304057 |
Substituted 6-membered N-heterocyclic compounds and method for their use as neurological regulator
This invention relates to substituted 6-membered N-Herterocyclic neurotrophic compounds of formula (I) or pharmaceutically acceptable salts or hydrates thereof, wherein R 1 , R 2 , X, Y, and Z are...
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7279470 |
Compounds and uses thereof for decreasing activity of hormone-sensitive lipase
Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The...
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7259158 |
Naphthaline derivatives as H3 inverse agonists
The present invention relates to compounds of formula I:
and pharmaceutically acceptable salts thereof, to the preparation of such compounds and pharmaceutical compositions containing them. The...
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7253205 |
Gem-disubstituted cyclohexane derivatives and their use as therapeutic agents
The present invention relates compounds of the formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and R 10 represent a variety of substituents, ring A is a phenyl or pyridyl...
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7241758 |
Compounds useful as anti-inflammatory agents
Disclosed are novel aromatic compounds of the formula (I) wherein G, X, Ar, L and Q are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological...
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7238689 |
Isoxazoline derivative and herbicide comprising the same as active ingredient
An isoxazoline derivative represented by the following general formula [I]:
wherein R 1 and R 2 may be the same or different and are each an alkyl group;
R 3 , R 4 , R 5 and R 6 are...
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7229987 |
Multicyclic compounds for use as melanin concentrating hormone antagonists in the treatment of obesity and diabetes
The present invention relates to a melanin concentrating hormone antagonist compound of formula I: (I); or a pharmaceutically acceptable salt, solvate, enantiomer or prodrug thereof useful in the...
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7217707 |
Amide of R-2-(aminoaryl)-propionic acid for use in the prevention of leucocyte activation
N-(2-aminoaryl-propionyl)-amides of formula (1) are described.
The process for their preparation and pharmaceutical preparations thereof are also described. The amides of the invention are...
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7214694 |
3-ox(adi)azolylpropanohydroxamic acids useful as procollagen C-proteinase inhibitors
Compounds of formula (I):
wherein the substituents are as defined herein, and their salt, solvates, and prodrugs are procollagen C-proteinase (PCP) inhibitors useful in treating conditions...
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7211575 |
Methods of treating cytokine mediated diseases
Disclosed are methods of treating acute and chronic inflammation in the lung caused by inhalation of smoke, endometriosis, Behcet's disease, uveitis, ankylosing spondylitis, pancreatitis, cancer,...
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7202254 |
Antibacterial compounds: process for their preparation and pharmaceutical compositions containing them
The present invention relates to novel triazole compounds of formula (I), their derivatives, their analogs, their tautomeric forms, their regioisomers, their rotamers, their stereoisomers, their...
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7189712 |
1,3-Oxazole compounds for the treatment of cancer
Oxazole derivatives, which are useful as VEGFR2, CDK2, and CDK4 inhibitors are described herein. The described invention also includes methods of making such oxazole derivatives as well as methods...
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7179804 |
Tachykinin receptor antagonists
The present invention relates to selective NK-1 receptor antagonists of Formula (I); or a pharmaceutically acceptable salt thereof, for the treatment of disorders associated with an excess 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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7141560 |
Alanine 2,6-dialkoxyphenyl ester derivatives as hypnotics
The present invention relates to alanine 2,6-dialkoxyphenyl ester derivatives having the general formula I
The invention also relates to pharmaceutical compositions comprising said derivatives,...
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7115600 |
Histamine-3 receptor modulators
This invention is directed to a compound of the formula I
as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a...
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7115597 |
Tyrosine kinase inhibitors
The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to...
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7109186 |
HIV integrase inhibitors
The present invention describes novel compounds of Formula I which inhibit HIV integrase. The invention also describes compositions and treatments of AIDS or ARC by using these compounds
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7101874 |
Antimicrobial dihydrothiazine and dihydrothiopyran oxazolidinones
The present invention provides a compound of formula I
or a pharmaceutically acceptable salt thereof wherein Y is —S(═O) n —, —S(═NR 8 )—, or —S(═NR 8 )(═O)—; Z is...
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7101873 |
Pyrimidinedione derivatives
Pyrimidinedione derivatives of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and...
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7074784 |
Medicaments against viral diseases
Novel dihydropyrimidines and combinations thereof with other antiviral agents, suitable for combating HBV infections.
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7067514 |
Pyrimidine compounds
This invention features pyrimidine compounds of formula (I):
R 1 is
aryl, or heteroaryl; each of R 2 and R 4 , independently, is R c , halogen, nitro, cyano, isothionitro, SR c ,...
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7060705 |
Mitotic kinesin inhibitors
The present invention relates to quinazolinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for...
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7053085 |
EP4 receptor agonist, compositions and methods thereof
This invention relates to potent selective agonists of the EP 4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which...
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RE39112 |
Purine derivatives and adenosine A2 receptor antagonists serving as preventives/remedies for diabetes
The present invention provides a preventive or therapeutic agent of a new type for diabetes mellitus and diabetic complications on the basis of an adenosine A2 receptor antagonist action. A purine...
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7045517 |
Triazine compounds
This invention relates to triazine compounds of formula (I):
R 1 is , aryl,
or heteroaryl; each of R 2 , R 4 , and R 5 , independently, is R c , halogen, nitro, nitroso, cyano, azide,...
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7022705 |
Isoxazoline derivatives useful as antimicrobials
Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof,
wherein, for example,
HET is an N-linked 5-membered, fully or partially...
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7022695 |
Thioether-substituted benzamides as inhibitors of Factor Xa
Thioether-substituted benzamide compounds having the formula:
are provided that exhibit exceptionally strong inhibition of Factor Xa in combination with weak hERG binding.
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7022678 |
Pregabalin lactose conjugates
In accordance with the present invention, there is provided pregabalin lactose conjugate compounds. Also provided as part of the present invention is a novel method of central nervous system...
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7019000 |
Method of treating a disease condition caused or exacerbated by an HPV
The invention provides agents and compounds (see (I) and (II)) for use in the treatment or prophylaxis of disease conditions caused or exacerbated by mammalian papillomaviruses, such as human...
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7015218 |
Amide compounds and medicinal use thereof
The present invention relates to a compound of the formula
wherein R 1 is substituted aryl, heteroaryl and the like, R 2 and R 3 are hydrogen, alkyl, halogen, hydroxyl group and the like, Q...
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7015217 |
Cyclic sulfone derivatives as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE)
The present application describes novel cyclic sulfone derivatives of formula I:
or pharmaceutically acceptable salt or prodrug forms thereof, which are useful as inhibitors of matrix...
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6960575 |
Thiazine derivatives
A compound having 3-oxo-3, 4-dihydro-2H-1, 4-thiazine 4-tetrahydropyrazine as a main skeleton. The compound is a chymase inhibitor and is represented by the following formula [I] and salts thereof:...
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6958331 |
Bradykinin receptor antagonists
The invention relates to sulfonyl amine derivatives of formula IA
wherein R 5A , X 1 , X 2 , R 9 and R 10 are as defined herein, which derivatives are useful as bradykinin B 1 receptor...
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6936616 |
Pyrimidine matrix metalloproteinase inhibitors
Selective MMP-13 inhibitors are pyrimidine derivatives of the formula
or a pharmaceutically acceptable salt thereof,
wherein: R 2 is hydrogen, halo, hydroxy, C 1 -C 6 alkyl, C 1 -C 6 ...
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6927238 |
Regulation of phospholipase D activity
Novel inhibitors of polyisoprenyl phosphate signaling regulates phopholipase D activity.
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6927217 |
HIV protease inhibitors
The present invention relates to novel dihydropyrones of Formula I
wherein X is NH or NR 8 , which inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in...
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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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6924278 |
Aroyl-piperazine derivatives, their preparation and their use as tachykinin antagonists
This invention relates to piperazine derivatives of the formula:
wherein each symbol is as defined in the description, and its pharmaceutically acceptable salt, to processes for preparation...
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6916807 |
Triaryl-oxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors
The present invention relates to triaryl-oxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula
wherein said ring X is a 5-7 membered heterocyclic ring, and wherein...
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6916800 |
Combination therapy including a matrix metalloproteinase inhibitor and an antineoplastic agent
The present invention provides methods to treat or prevent neoplasia disorders in a mammal using a combination of a matrix metalloproteinase inhibitor and an antineoplastic agent.
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6916797 |
α-arylethylpiperazine derivatives as neurokinin antagonists
The invention relates to new α-arylethylpiperazine of the formula
wherein
Z represents 0 or S; n′ represents 1 or 2; R 2 represents a hydrogen atom or a methyl group; W, Ar 1 and...
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6900201 |
N-substituted-heteroaryloxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors
The present invention relates to N-substituted-heteroaryloxy-aryl-spiro-pyrimidine-2,4,6-trio
ne metalloproteinase inhibitors of the formula
wherein ring X is a 5-7 membered heterocyclic ring,...
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6894046 |
IL-5 inhibiting 6-azauracil derivatives
The present invention is concerned with the compounds of formula
the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p is 0 to...
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6884804 |
Inhibitors of Src and other protein kinases
The present invention provides compounds of formula I:
wherein A is N or CR, and G, R 1 , R 2 and R 3 are as described in the specification. These compounds are inhibitors of protein kinase,...
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6867207 |
IL-5 inhibiting 6-azauracil derivatives
The present invention is concerned with the compounds of formula
the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, p and q are 0, 1,...
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