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7619110 |
Amino acid derived prodrugs of propofol, compositions, uses and crystalline forms thereof
The present invention provides a prodrug of propofol and crystalline forms thereof, methods of making the propofol prodrug and crystalline forms thereof, pharmaceutical compositions of the propofol...
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7612099 |
Vinylogous acid derivatives
The invention is concerned with vinylogous acids derivatives of formula (I)
wherein A and R 1 to R 6 are as defined in the description and in the claims, as well as physiologically acceptable...
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7612064 |
Sulfopyrroles
The invention relates to compounds of formula (I) wherein R 1 represents aryl, aralkyl or heteroaryl, R 2 is aryl or heteroaryl and R 3 is aryl, heteroaryl or optionally substituted aminomethyl,...
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7598280 |
Heterocyclic compounds, compositions comprising them and methods of their use
Heterocyclic compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of inflammatory and autoimmune diseases and disorders are disclosed....
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7582668 |
Imidazoyl-benzamide anti-cancer agents
Provided are compounds of Formula I and pharmaceutically acceptable salts thereof which may be useful for the treatment of cancer or other proliferative disorders.
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7579320 |
IAP BIR domain binding compounds
Disclosed is an isomer, enantiomer, diastereoisomer or tautomer of a compound represented by Formula I or II
or a salt thereof, in which R 1 , R 2 , R 3 , R 100 , R 200 , R 300 , A, A 1 , BG, Q...
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7576098 |
Heterocyclic compounds as inhibitors of factor VIIa
The present invention relates generally to compounds that inhibit serine proteases. In particular it is directed to novel heterocyclic compounds, or a stereoisomer or pharmaceutically acceptable...
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7560483 |
Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require...
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7557102 |
Pyrazolidine-1,2-dicarboxyldiphenylamide derivatives as coagulation factor Xa inhibitors for the treatment of thromboses
Novel compounds of the formula (I), in which R, R 1 , R 2 and R 3 have the meanings indicated in Patent Claim 1 , are inhibitors of coagulation factor Xa and can be employed for the prophylaxis...
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7553862 |
4-amino-1,5-substituted-1,5-dihydro-imidazol-2-ones
The present invention relates to compounds of formula I
wherein
R 1 , R 2 , R 3 , and R 4 are as defined herein
and to pharmaceutically acceptable acid addition salts thereof. Compounds of...
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7550496 |
Compositions and methods for treating cancer
Hypoxia-activated prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.
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7547703 |
Indoline derivatives substituted in the 6-position, their preparation and their use as medicaments
The present invention relates to indolinone derivatives, substituted in the 6-position, of the formula
in which
R 1 to R 6 and X are as defined in claim 1 , to their tautomers,...
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7538128 |
Dipeptidyl peptidase IV inhibitors, process for their preparation and compositions containing them
The present invention relates to novel compounds useful as dipeptidyl peptidase IV (DPP-IV) inhibitors of the formula:
wherein X, Y, a, R 1 , and R 2 are as defined herein.
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7528156 |
Compounds
The invention provides compounds of general formula (D wherein m, n, Q, Z1, Z2, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification, processes for their preparation,...
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7524867 |
Tetrasubstituted imidazole derivatives as cannabinoid CB1 receptor modulators with a high CB1/CB2 receptor subtype selectivity
The present invention relates to 1,2,4,5-tetrasubstituted imidazole derivatives as selective cannabinoid CB 1 receptor modulators, in particular CB 1 receptor antagonists or inverse agonists...
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7521470 |
Factor Xa inhibitors
The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The...
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7521461 |
Benzoic acid derivatives as modulators of PPAR alpha and gamma
A compound of formula (I) wherein R 1 represents aryl optionally substituted by a heterocyclic group or a heterocyclic group optionally substituted by aryl wherein each aryl or heterocyclic group...
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7498348 |
1 H-imidazole derivatives as cannabinoid receptor modulators
The invention relates to a group of 1H-imidazole derivatives which are modulators of cannabinoid receptors, to methods for the preparation of these compounds, to novel intermediates useful for the...
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7491743 |
Inhibitors of cellular necrosis
The present invention relates to compounds and pharmaceutical preparations and their use in therapy for preventing or treating trauma, ischemia, stroke and degenerative diseases associated with...
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7491742 |
Imidazole derivatives as phosphodiesterase VII inhibitors
Imidazole derivatives of the formula I
in which
R 1 is H, A, benzyl, indan-5-yl, 1,2,3,4-tetrahydronaphthalen-5-yl, dibenzothien-2-yl, or phenyl which is unsubstituted or mono-, di- or...
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7482374 |
Pyrrolidine-2-ones as Factor Xa inhibitors
The invention relates to compounds of formula (I):
wherein substituents are as defined.
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7482349 |
Amino-5,5-diphenylimidazolone derivatives for the inhibition of β-secretase
The present invention provides a compound of formula I and the use thereof for the therapeutic treatment, prevention or amelioration of a disease or disorder characterized by elevated β-amyloid...
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7462635 |
Thiazole and oxazole VDAC regulator
The present invention provides a VDAC regulator comprising a compound represented by the formula (I):
wherein R 1 is a halogen atom, an optionally substituted heterocyclic group, an optionally...
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7456210 |
Benzyloxy derivatives
The present invention relates to compounds of formula I
wherein R 1 and R 2 are as defined in the specification and to pharmaceutically acceptable salts thereof for the treatment of diseases,...
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7453002 |
Five-membered heterocycles useful as serine protease inhibitors
The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound...
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7446118 |
3-amino-1-arylpropyl indoles and aza-substituted indoles and uses thereof
The present invention provides compounds of the formula:
or pharmaceutically acceptable salts, solvates or prodrugs thereof,
wherein p, Ar, R 1 , R 2 , R 3 , R a , R b , R c , R d and R e ...
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7439374 |
Azabenzofuran substituted thioureas; inhibitors of viral replication
The present invention provides compounds of Formula 1,
wherein the variables Ar, A 1 , A 2 , A 3 , A 4 , R 5 , R 6 , R 7 , V, W, X, and Y are defined herein.
Certain compounds of Formula 1...
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7435750 |
Method of using substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs as activators of caspases and inducers of apoptosis and the use thereof
The present invention is directed to substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I:
wherein Ar 1 , Ar 3 , A, B and D are defined herein. The...
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7425638 |
Cis-imidazolines
The present invention provides compounds according to formula I
having the designations provided herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit the...
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7423015 |
Antihelminthic drugs as a treatment for hyperproliferative diseases
The present invention is directed to the use of benzimidazole derivatives for the treatment of tumors and in combination with tumor suppressor gene therapy. In a particular embodiment, treatment of...
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7417158 |
Cationic substituted benzofurans as antimicrobial agents
A method of treating a Mycobacterium tuberculosis infection in a subject in need thereof by administering to the subject an effective amount of a cationic substituted benzofuran compound. Methods...
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7402683 |
Cinnamic acid amides
The present invention relates to compounds, to processes for preparing them, to pharmaceutical compositions comprising them, and to their use in the therapy and/or prophylaxis in illnesses in...
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7402597 |
Activator of peroxisome proliferator-activated receptor δ
A compound represented by the formula (I) or a salt of the compound, and a PPAR-δ activator which contains the compound or salt as the active ingredient:
(wherein A represents O or S; B 1 ...
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7402579 |
Quinobenzoxazine analogs and compositions
The present invention relates to quinobenzoxazines analogs having the general formula:
and pharmaceutically acceptable salts, esters and prodrugs thereof; wherein A, U, W, X, Z, B, L, R 1...
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7393857 |
Use of 5-HT3 receptor antagonists for treating musculoskeletal diseases
The present invention relates to a new use for compounds having 5-HT 3 (serotonin M) receptor antagonist activity, especially tropisetron, for the manufacture of a pharmaceutical composition for...
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7378421 |
Chromenone derivatives
Novel compounds of the formula I
in which
R 1 , R 2 , R 3 and Het are as defined herein, which
are inhibitors of tyrosine kinases and/or Raf kinases and can be employed for the treatment of...
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7371772 |
Bicyclic compound, production and use thereof
The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is...
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7368467 |
Ion channel modulators
The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein...
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7361678 |
Azole derivatives and fused bicyclic azole derivatives as therapeutic agents
This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of...
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7342028 |
Medical use for tachykinin antagonists
The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel...
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7329679 |
1,2 Diarylbenzimidazoles and their pharmaceutical use
Benzimidazoles of general formula I
and the use of benzimidazole derivatives for the production of pharmaceutical agents for treatment and prophylaxis of diseases that are associated with a...
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7323433 |
R-(-)-1-[2-(7-chlorobenzo[b]thiopen-3-yl-methoxy)-2-(2,4-dichlorophenyl)-ethyl]-1H-imidazole
The invention relates to R-(−)-1-[2-(7-Chloro-benzo[b]thiophen-3-yl-methoxy)-2-(2,4
-dichloro-phenyl)-ethyl]-1H-imidazole and the salts thereof. The invention also relates to compositions thereof...
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7314885 |
Pyrrole compounds useful as kinase inhibitors
The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds, processes for...
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7304072 |
Spiro compounds
Compounds represented by the general formula (I)
wherein Ar 1 represents an aryl or heteroaryl which may be substituted; n represents 0 or 1; T, U, V and W each independently represent a...
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7297708 |
Heteroaromatic substituted cyclopropane as corticotropin releasing hormone ligands
Provided herein are novel heteroaromatic substituted cyclopropanes of the Formula (I):
as well as compositions, including pharmaceutical compositions, containing the same, and the use thereof...
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7294641 |
Heterocyclic compound for stimulating or inducing the growth of the hair or eyelashes and/or slowing down their loss, composition comprising it and its uses
Heterocyclic compounds useful for stimulating/inducing the growth of keratinous fibers, notably human hair/eyelashes, and/or slowing the loss of same, have the following structural formula (I) or...
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7285554 |
Pyrazole derivative
Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in...
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7282503 |
Fungicidal mixtures based on imidazole derivatives
Disclosed are fungicidal mixtures containing a synergistically effective amount of A) a triazolopyrimidine of formula I, and B) imidazole derivatives of formula II, wherein X 1 and X 2 represent...
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7279497 |
Benzopyran derivatives substituted with secondary amines including imidazole, their preparation and pharmaceutical compositions containing them
The present invention relates to benzopyran derivatives substituted with secondary amines including imidazole, their preparation, and pharmaceutical compositions containing them. The present...
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7279496 |
Dihydroimidazo[4,5-e]indole and 7h-pyrrolo[3,2-f]quinoxaline derivatives as nicotinic acetylcholine receptor ligands and/or serotonergic ligands
Compounds of the formula (I) in which R 1 , R 2 , R 3 and R 4 are as defined in Claim 1 , are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the...
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