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7612207 |
Method for preparing clopidogrel 1,5-naphthalenedisulfonate or hydrate thereof
The present invention relates to a method for preparing clopidogrel 1,5-naphthalenedisulfonate or a hydrate thereof, which comprises reacting a clopidogrel-acid addition salt with disodium...
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7612089 |
Tetrahydroisoquinolines as 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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7598265 |
Compositions and methods for treating CNS disorders
The invention generally relates to thienopyridinone 5-HT 4 receptor modulators, and in particular the use of these compounds and their pharmaceutical compositions, e.g., in the treatment,...
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7598236 |
Diazabicyclic central nervous system active agents
Compounds of formula I
pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.
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7592455 |
Bicyclic heteroaromatic compounds as kinase inhibitors
A series of 5-6 fused ring bicyclic heteroaromatic derivatives, based in particular on the 6-oxo-6,7-dihydrothieno[2,3-b]pyridine ring system, being inhibitors of p38 kinase, are accordingly of use...
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7592353 |
Substituted 3-amino-thieno[2,3-b]pyridine-2-carboxylic acid amide compounds and processes for preparing and their uses
Disclosed are compounds of formula (I):
wherein R 1 and R 4 are defined herein, which are useful as inhibitors of the kinase activity of the IκB kinase (IKK) complex. The compounds are...
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7592352 |
Substituted thieno and furo-pyridines
This invention relates to newly identified compounds for treating and preventing tumors and cancers, and methods for treating proliferative diseases associated with the imbalance or inappropriate...
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7576212 |
Thieno[2,3-B] pyridines as potassium channel inhibitors
The invention provides compounds of the formula:
wherein
R1 is aryl, heteroaryl, cycloalkyl or alkyl; R2 is H, alkyl, nitro, CO 2 R7, CONR5R6 or halo; R3 and R4 are H, NR5R6, NC(O)R7,...
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7576211 |
Synthesis of thienopyridinone compounds and related intermediates
The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated...
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7576072 |
Heterocyclic inhibitors of MEK and methods of use thereof
Disclosed are compounds of the Formula I
and pharmaceutically acceptable salts and prodrugs thereof, wherein R 1 , R 2 , R 7 , R 8 and R 9 , W, X, Y and Z are as defined in the specification....
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7557101 |
4,5,6,7-tetrahydro-thieno[3,2-c] pyridine derivatives
The present invention relates to compounds of formula I
wherein R 1 and R 2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are...
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7553849 |
Compounds
A compound of formula (I)
wherein
R is methyl, ethyl, n-propyl, iso-propyl, n-butyl or allyl; R′ is hydrogen, C 1 -C 4 alkyl, C 1 -C 3 alkoxy; halogen, trifluoromethyl or OCH x F y , R″...
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7553848 |
Vanilloid receptor ligands and their use in treatments
bis-Bicyclic amides and derivatives thereof and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster...
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7547786 |
Process for producing thiazole derivative
The present invention provides processes for producing a compound (5) based on the following reaction scheme.
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7531659 |
***WITHDRAWN PATENT AS PER THE LATEST USPTO WITHDRAWN LIST***
Tetrahydropyridothiophenes
Compounds of a certain formula (I)
in which Ra and Rb have the meanings indicated in the description, are novel, effective compounds with anti-proliferative and/or apoptosis inducing activity.
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7521460 |
Thienopyridone derivatives as kinase inhibitors
A series of thieno[2,3-b]pyridin-6(7H)-one derivatives, substituted in the 2-position by a carbonyl- or sulfonyl-linked pyrrolidin-1-yl or related moiety, being inhibitors of p38 MAP kinase, are...
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7517986 |
Tetrahydropyridothiophenes for use in the treatment of cancer
Compounds of the formula (I)
in which Ra and Rb have the meanings indicated in the description, are novel effective compounds with anti-proliferative and/or apoptosis inducing activity.
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7507827 |
Stereoselective method for the production of Clopidogrel
The present invention relates to processes for preparing a compound of the general formula (Ia)
wherein X is a halogen atom, or a pharmaceutically acceptable salt thereof, wherein a compound of...
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7491733 |
Bicyclic guanidine derivatives and therapeutic uses thereof
The invention relates to compounds of general formula (I), in which A, X, Y and R1 are defined in Claim 1 . These compounds may be used in the treatment of pathologies associated with insulin...
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7482452 |
Process for preparing 3-aminothienopyridone derivatives
This invention provides a class of 3-amino-7H-thieno[2,3-b]pyridin-6-one derivatives, substituted in the 7-position by an aryl, heteroaryl, cycloalkyl or heterocycloalkyl moiety, and in the...
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7470707 |
Crystalline monohydrate clopidogrel naphthalenedisulfonate and process of preparation
A crystalline clopidogrel naphthalenesulfonate or a hydrate thereof, a method for preparing same, and a pharmaceutical composition containing same are provided.
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7470693 |
Oxalamide derivatives as kinase inhibitors
The invention is directed to compounds having the following Formula I:
and methods of using them for the treatment of proliferative diseases.
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7456192 |
3β-amino azabicyclooctane heteroaromatic amid derivatives preparation method and therapeutic uses thereof
The invention concerns compounds of general formula 1, wherein: A, B, D and E represent one or two nitrogen atoms, the others being carbon atoms; X represents a S or, a O, thereby forming a...
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7449580 |
Method of preparing thieno[3,2-c]pyridine derivatives and intermediates used therein
Ticlopidine and clopidogrel having high blood platelet aggregation inhibitory and anti-thrombotic activities are simply prepared by reacting a substituted thiophene derivative with a...
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7449472 |
Methods of inhibiting p38 with substituted bicyclic pyrimidines
The present invention discloses compounds corresponding to the formula
wherein A, X, Y, R, R 1 and R 2 are as defined within, pharmaceutical formulations, methods of making and uses thereof.
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7446200 |
Rapid resolution process of clopidogrel base and a process for preparation of clopidogrel bisulfate polymorph-form I
The present invention discloses a rapid resolution process of racemic clopidogrel base followed by conversion of the resolved (S) isomer to crystalline Clopidogrel bisulfate Form I. The invention...
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7439247 |
Bicyclic pyridine and pyrimidine P38 kinase inhibitors
The present invention discloses compounds corresponding to formula
wherein A, R, X, Y, R, R 1 and R 2 are as defined above, pharmaceutical formulations, methods of making and uses thereof.
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7439246 |
Fused heterocyclic kinase inhibitors
In general, the instant invention comprises compounds of Formulas I and II
including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase...
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7435819 |
4,5,6,7-tetrahydro-[1,2]dithiolo[4,3-C] pyridine-3-thione compounds
The present invention relates to new compounds directly increasing kinase activity of p90 ribosomal S6 kinase 1 (RSK1), a pharmaceutical composition comprising them as active ingredient, a use...
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7425562 |
Inhibitors of cruzipain and other cysteine proteases
Compounds of general formula (I) or general formula (II)
wherein R 1 , P 1 , P 2 , Q, Y, (X) o , (W) n , (V) m , Z and U are as defined in the specification, are inhibitors of cruzipain and...
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7423047 |
Arylamine substituted bicyclic heteroaromatic compounds as p38 kinase inhibitors
Bicyclic heteroaromatic derivatives of formula (1) are described: F (1) where: the dashed line joining A and C(R a ) is present and represents a bond and A is a —N═ atom or a —C(R b )═...
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7411066 |
Amino methylated 2-pyridinones
Novel amino methylated 2-pyridinones, precursors, intermediates, and derivatives; the methods for the preparation of the same; uses of the same for inhibiting pili formation in bacteria; and...
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7407972 |
Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
The present invention provides compounds of Formula (I):
wherein A, B, C, G, and W 1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are...
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7407966 |
Thienopyridinone compounds and methods of treatment
The invention relates to 5-HT 4 receptor agonists and partial agonists. Thienopyridinone compounds and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT 4 ...
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7405226 |
Cycloalkyl-hydroxyl compounds and compositions for cholesterol management and related uses
The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions...
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7405225 |
Substituted 3-amino-thieno[2,3-b]pyridine-2-carboxylic acid amide compounds and processes for preparing and their uses
Disclosed are compounds of formula (I):
wherein R 1 and R 2 are defined herein, which are useful as inhibitors of the kinase activity of the IκB kinase (IKK) complex. The compounds are...
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7399770 |
Thieno-imino acid derivatives for use as matrix metalloproteinase inhibitors
The invention is directed to a compound of the formula I
wherein the variables are as defined herein, or
a stereoisomeric form thereof, mixture of stereoisomeric forms, in any ratio, or a...
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7396931 |
Process for the preparation of amorphous form of a platelet aggregation inhibitor drug
The present invention relates to a new method of preparation of the polymorph form 1 of methyl (S)-(+)-(2-chlorophenyl)-2-(6,7-dihydro-4H-thieno[3,2-c]pyri
dine-5-yl-acetate hydrogensulfate of the...
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7390903 |
Thieno-pyridine derivatives as allosteric enhancers of the GABAB receptors
The present invention relates to compounds of formula I
wherein R 1 , R 2 , R 3 , R 4 , and R 5 are as defined in the specification. Compounds of the invention are active on the GABAB receptor...
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7371752 |
Aryl fused substituted 4-oxy-pyridines
Disclosed are compounds of the formula:
wherein X, Q, W and
are as defined herein. These compounds are agonists, antagonists or inverse agonists for GABA A brain receptors or prodrugs of...
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7365080 |
Pharmaceutical compositions comprising thieno[2,3-c]pyridine derivatives and use thereof
The present invention provides thieno[2,3-C]pyridine derivatives, pharmaceutical compositions comprising the thieno[2,3-C]pyridine derivatives, and methods of use thereof. The compounds capable of...
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7342014 |
Diamine derivatives
A compound represented by the general formula (1):
Q 1 -Q 2 -T 0 -N(R 1 )-Q 3 -N(R 2 )-T 1 -Q 4 (1)
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7332504 |
Heterocyclic substituted aminoazacycles useful as central nervous system agents
Heterocyclic substituted aminoazacyclic compounds of formula I
Z-R 3 I,
...
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7332487 |
Nitrogen-containing 5-membered ring compound
The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]:
wherein symbols in the formula have the following meanings;
...
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7329751 |
Process for the preparation of clopidogrel
A process for the preparation of clopidogrel (1)
by reaction of the N,N′-bis-4,5,6,7-tetrahydro-[3,2-c]-thienopyridyl methane (12)
with (R)-2-chlorophenylacetic acid...
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7323494 |
Compounds and methods
Disclosed is a compound of having the formula:
pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables...
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7312218 |
Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors
The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula Ia-If:
or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic...
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7291735 |
Process for the manufacture of (+)-(s)-clopidogrel bisulfate form-1
The present invention relates to a novel process for the manufacture of blood-platelet aggregation inhibiting agent. In particular, the present invention is directed to a process for the...
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7291734 |
N-sulfonylaminothiazole
N-(4,5,6,7-tetrahydro-thiazolo-[5,4-c]pyridin-2-yl)-(C 6-18 )arylsulfonamides, wherein the nitrogen atom of the pyridine is substituted, and wherein the pyridine ring is optionally bridged, useful...
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7276519 |
Thieno[3,2-b]pyridine-6-carbonitriles and thieno[2,3-b]pyridine-5-carbonitriles as protein kinase inhibitors
This invention provides compounds of Formula (1 a )–(1 f ), II
wherein:
X, m, n, q, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , Y, Q, Z, Z′, Z′″, Z″ and J are defined...
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