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US20090291948 |
SULFONAMIDE PERI-SUBSTITUTED BICYCLICS FOR OCCLUSIVE ARTERY DISEASE
Acyl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed. The compounds are of the...
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US20090286814 |
HCV PROTEASE INHIBITORS
This invention relates to macrocyclic compounds of formula (I) or (II) shown in the specification. These compounds can be used to treat hepatitis C virus infection.
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US20090281141 |
MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS
Inhibitors of HCV replication of formula (I)
and the N-oxides, salts, and stereoisomers thereof, wherein X is N, CH and where X bears a double bond it is C; R 1 is —OR 1 , —NH—SO 2 R 6 ;...
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US20090281140 |
Macrocyclic inhibitors of hepatitis c virus
Inhibitors of HCV replication of formula (I)
and the N-oxides, salts, and stereoisomers, wherein
each dashed line represents an optional double bond;
X is N, CH and where X bears a double...
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US20090281100 |
Benzimidazole quinolinones and uses thereof
Methods of inhibiting various enzymes and treating various conditions are provided that include administering to a subject a compound of Structure I or IB, a pharmaceutically acceptable salt...
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US20090280068 |
POLYMORPH OF 8-HYDROXY-5-[(1R)-1-HYDROXY-2-[[(1R)-2-(4-METHOXYPHENYL)-1-METHYLETHYL]AMINO]ETHYL]-2(1H)-QUINOLINONE MONOHYDROCHLORIDE
Crystal form D of 8-hydroxy-5-[(1R)-1-hydroxy-2-[[(1R)-2-(4-methoxyphenyl)-1-m
ethylethyl]-amino]ethyl]-2(1H)-quinolinone monohydrochloride is highly crystalline, easy to prepare, and stable.
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US20090280067 |
CRYSTAL FORM OF 8-HYDROXY-5-[(1R)-1-HYDROXY-2-[[(1R)-2-(4-METHOXYPHENYL)-1-METHYLETHYL]AMINO]ETHYL]-2(1H)-QUINOLINONE MONOHYDROCHLORIDE
Crystal form E of 8-hydroxy-5-[(1R)-1-hydroxy-2-[[(1R)-2-(4-methoxyphenyl)-1-m
ethylethyl]-amino]ethyl]-2(1H)-quinolinone monohydrochloride is highly crystalline, easy to prepare, and stable.
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US20090274693 |
Method of Treating Cancer using a cMet and AXL Inhibitor and an ErbB Inhibitor
The present invention relates to a method of treating cancer in a patient comprising administering to the patient therapeutically effective amounts of: a) a compound of formula A:
or a...
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US20090274652 |
Hepatitis C Virus Inhibitors
Hepatitis C virus inhibitors having the general formula
are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
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US20090270391 |
THIENOPYRIDINE DERIVATIVE, OR QUINOLINE DERIVATIVE, OR QUINAZOLINE DERIVATIVE, HAVING c-MET AUTOPHOSPHORYLATION INHIBITING POTENCY
An objective of the present invention is to provide compounds having antitumor activity. According to the present invention, there is provided compounds represented by formula (I) and...
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US20090270371 |
QUINOLINE DERIVATIVES USEFUL IN THE TREATMENT OF MGLUR5 RECEPTOR-MEDIATED DISORDERS
Compounds of formula (I): and/or enantiomers and/or racemates and/or diastereomers and/or pharmaceutically acceptable salts thereof formed with acids or bases, to the process for their preparation,...
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US20090269352 |
ANTITUMOR AGENT COMPRISING SULFONAMIDE-CONTAINING HETEROCYCLIC COMPOUND COMBINED WITH AN ANGIOGENESIS INHIBITOR
The present invention provides a composition and a kit for treating tumors, which permits a sulfonamide-containing heterocyclic compound to exhibit its angiogenesis inhibitory activity and...
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US20090269305 |
NOVEL MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS REPLICATION
The embodiments provide compounds of the general Formulae I, II, III, IV, V, VI, VII, and X, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The...
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US20090264464 |
ANTITUMOR AGENT FOR UNDIFFERENTIATED GASTRIC CANCER
The present invention relates to a therapeutic agent represented by the General formula (I), or a pharmacologically acceptable salt thereof, or a solvate of the compound or the salt thereof:
The...
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US20090263488 |
PRESSURISED METERED DOSE INHALERS CONTAINING SOLUTIONS OF BETA-2 AGONISTS
The present invention relates to a pharmaceutical formulation for use in the administration of 2(1H)-quinolinone derivatives long-acting β 2 -agonists by inhalation. In particular this invention...
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US20090258853 |
Somatostatin Agonists
This invention relates to compounds which are agonists of somatostatin and selective toward somatostatin receptor subtype SSTR2. The compounds are useful in the treatment and prevention of...
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US20090253739 |
Amine Derivatives
The invention relates to compounds of formula (1)
and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives....
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US20090253727 |
NOCICEPTIN ANALOGS
A compound of the having the general formula (I) or general formula (II):
wherein
Z, A, B, C, R 1 , R 2 , Q, W, and n are as described herein.
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US20090253726 |
TRI-, TETRA-SUBSTITUTED-3-AMINOPYRROLIDINE DERIVATIVE
A quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria,...
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US20090253655 |
QUINOLINONE FARNESYL TRANSFERASE INHIBITORS FOR THE TREATMENT OF SYNUCLEINOPATHIES AND OTHER INDICATIONS
Novel quinolinone farnesyl transferase inhibitors are provided. These new compounds are useful in the treatment or prevention of synucleinopathies, such as Parkinson's Disease, Diffuse Lewy Body...
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US20090247578 |
5-HYDROXYMETHYL-OXAZOLIDIN-2-ONE-DERIVATIVES AND THEIR USES AS ANTIBACTERIALS
The invention relates to novel chimeric antibiotics of formula I
wherein
R 1 represents OH, OPO 3 H 2 or OCOR 5 ; R 2 represents H, OH or OPO 3 H 2 ; A represents N or CR 6 ; R 3 represents...
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US20090247577 |
PYRROLIDINE DERIVATIVES USEFUL AS BACE INHIBITORS
Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment...
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US20090247576 |
ANTI-TUMOR AGENT FOR MULTIPLE MYELOMA
The object of the invention is to provide a pharmaceutical composition and a therapeutic method which can exert their effects with higher efficiency on a living organism having at least one cell...
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US20090246277 |
Controlled release system
The invention relates to a system for controlled release of medicinally active substances, which comprises sucrose acetate isobutyrate (SAIB) and a further solvent.
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US20090239904 |
COMPOUNDS HAVING BETA2 ADRENERGIC RECEPTOR AGONIST AND MUSCARINIC RECEPTOR ANTAGONIST ACTIVITY
This invention provides compounds of formula I:
wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8a , R 8b , W, a, b, c and m are as defined in the specification, or a pharmaceutically...
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US20090239903 |
TETRAHYDROQUINOLINE ANALOGUES AS MUSCARINIC AGONISTS
The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with...
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US20090238770 |
Organic compounds
A medicament comprising, separately or together, (A) a compound of formula I
in free or salt or solvate form, where W, R x , R y , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 have the meanings...
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US20090233964 |
METHODS FOR IMPROVING THE PHARMACOKINETICS OF HIV INTEGRASE INHIBITORS
The invention provides methods for improving the pharmacokinetics of an HIV integrase inhibiting compound by administering food and/or ritonavir or a pharmaceutically acceptable salt thereof with...
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US20090232889 |
CRYSTALLINE SALTS OF QUINOLINE COMPOUNDS AND METHODS FOR PREPARING THEM
A stable solid pharmaceutical composition consisting essentially of an effective amount of a crystalline salt of formula (II)
together with an alkaline-reacting component maintaining the pH...
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US20090227625 |
CXCR2 INHIBITORS
The invention relates to compounds of the formula I
in which R1, R2, X, A, B, Z and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug...
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US20090227610 |
NOVEL TRIGLYCERIDE REDUCING AGENT
The present invention relates to hypotriglyceridemic agent containing HMG-CoA reductase inhibitor and cAMP protease inhibitor.
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US20090227571 |
Androgen Receptor Modulator Compounds and Methods
Provided herein are compounds that bind to androgen receptors and modulate the activity and/or the amount of androgen receptors and to methods for making and using such compounds. Also provided are...
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US20090227547 |
Novel salt form of a Beta2-adrenergic agonist quinolin-2-one derivative
A 2,5-dichlorobenzenesulfonate salt of compound (I):
is disclosed along with formulations thereof, processes for making the same, and methods of treatment or prophylaxis administering the same.
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US20090221635 |
QUINOLINYL AND BENZOTHIAZOLYL MODULATORS
Compounds, compositions and methods are provided that are useful in the treatment or prevention of a condition or disorder mediated by PPARγ. In particular, the compounds of the invention modulate...
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US20090220554 |
Transglutaminase Inhibitors and Methods of Use Thereof
Transglutaminase inhibitors and methods of use thereof are provided.
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US20090215800 |
Enzyme and Receptor Modulation
Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or...
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US20090209580 |
ANTITUMOR AGENT FOR THYROID CANCER
The objective of the present invention is to provide a pharmaceutical composition and a therapeutic method that are specifically effective against at least one disease selected from multiple...
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US20090209502 |
COMPOSITIONS OF GLYCOPYRRONIUM SALT FOR INHALATION
A process for preparing dry powder formulations of a glycopyrronium salt for inhalation that have good stability. The process involves (a) micronising a glycopyrronium salt together with an...
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US20090203693 |
THERAPEUTIC AGENT FOR LIVER FIBROSIS
The present invention provides a therapeutic agent for hepatic fibrosis and a method for treatment of hepatic fibrosis....
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US20090203685 |
ANTI-PROLIFERATIVE COMPOUNDS FROM A 3-ARYL-COUMARINE OR 3-ARYL-QUINOLIN-2-ONE AND USES THEREOF
The present invention is directed to molecules deriving from a 3-aryl-coumarine or 3-aryl-quinolin-2-one and having potent anti-proliferative and/or cytotoxic activity, especially against tumoral...
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US20090197913 |
SYNERGISTIC MODULATION OF FLT3 KINASE USING A FLT3 INHIBITOR AND A FARNESYL TRANSFERASE INHIBITOR
The invention is directed to a method of inhibiting FLT3 tyrosine kinase activity or expression or reducing FLT3 kinase activity or expression in a cell or a subject comprising the administration...
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US20090197888 |
FLUORINATED TRIPEPTIDE HCV SERINE PROTEASE INHIBITORS
The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof:
which inhibit serine protease activity, particularly the activity of...
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US20090197878 |
SUBSTITUTED BENZO[d][1,3]OXAZIN-2(4H)-ONES AND RELATED DERIVATIVES AND THEIR USES FOR MODULATING THE PROGESTERONE RECEPTOR
Compounds of formula (I), or pharmaceutically acceptable salts thereof, are provided, wherein R 1 -R 6 and X are defined herein. Also provided are methods of preparing the compounds of formula...
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US20090197834 |
QUINOLONE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
[Problem] To provide a compound having excellent platelet aggregation inhibitory activity. [Means for Resolution] It was found that quinolone derivatives characterized in that these have lower...
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US20090192148 |
Organic Compounds
The invention relates to 3,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a...
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US20090181996 |
SUBSTITUTED QUINOLONES III
The invention relates to substituted quinolones and to methods for their preparation as well as to their use for the production of medicaments for the treatment and/or prophylaxis of diseases,...
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US20090180983 |
BICYCLIC, C5-SUBSTITUTED PROLINE DERIVATIVES AS INHIBITORS OF THE HEPATITIS C VIRUS NS3 PROTEASE
The present invention relates to compounds of Formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof:
which inhibit serine protease activity, particularly the activity of...
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US20090176826 |
COMBINATION DRUG CONTAINING PROBUCOL AND A TETRAZOLYLALKOXY-DIHYDROCARBOSTYRIL DERIVATIVE WITH SUPEROXIDE SUPRESSANT EFFECTS
This invention relates to a combination drug comprising a combination of a tetrazolylalkoxy-dihydrocarbostyril derivative of the formula:
wherein R is cycloalkyl, A is lower alkylene, and the...
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US20090170896 |
c-Met modulators and methods of use
The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration...
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US20090165723 |
METHODS OF PRODUCING AVIAN EGGS AND BIRDS OF SPECIFIED GERM-FREE STATUS
The invention provides an improved method of rearing a bird of specified germ-free status. Specifically, the present invention is directed to a method for increasing the hatchability and viability...
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