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7384944 |
Piperazine derivatives useful as CCR5 antagonists
The use of CCR5 antagonists of the formula
or a pharmaceutically acceptable salt thereof, wherein
R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R 1 is hydrogen or...
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7345042 |
MCH antagonists for the treatment of obesity
The present invention discloses methods of using antagonists for melanin-concentrating hormone (MCH), to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes, as...
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7307081 |
Piperidine derivatives useful as CCR5 antagonists
The present invention provides a compound of the formula
or a pharmaceutically acceptable salt or solvate thereof, wherein the various moieties are as defined in the specification. The present...
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7288545 |
Piperazinedione compounds
This invention relates to a method for treating an angiogenesis-related disease. The method includes administering to a subject in need thereof an effective amount of a piperazinedione compound...
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7247631 |
Pegylated interferon alfa-CCR5 antagonist combination HIV therapy
Methods for treating treatment-naive as well as treatment-experienced adult and pediatric patients having HIV-1 infections as well as patients co-infected with HIV-1 and HCV involving administering...
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7229997 |
Compounds and their use
Compounds of the general formula (I):
wherein R 1 , R 2 , R 3 and R 4 are as described in the specification.
Further included are pharmaceutical compositions comprising the...
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7214679 |
Piperidine/piperazine-type inhibitors of p38 kinase
Compounds of the formula:
wherein the substituents are as defined herein are useful for treating conditions mediated by p38 kinase.
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7196106 |
Cyanothiophene derivatives, compositions containing such compounds and methods of use
The present invention addresses substituted cyanothiophene derivatives of the formula I:
as well as compositions containing such compounds and methods of treatment. The compounds in the present...
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7196080 |
Phenylpyridinecarbonylpiperazinederivative
The present invention relates to a compound which is represented by the following general formula and has type 4 phosphodiesterase inhibitory action, and uses and an intermediate compound thereof. ...
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7101885 |
Piperazinyl-aryloxy and piperazinyl-heteroaryloxy-n-aryl lactams
The present invention relates to compounds of formula I
wherein Ar, Y and G are as defined in the specification, a is 1 to 4, Z and W are carbon or nitrogen and n is 1, 2 or 3; and to...
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7098213 |
CCR5 antagonists useful for treating AIDS
Compounds of the formula
or a pharmaceutically acceptable salt or isomer thereof, wherein:
Q, X and Z are CH or N; R, R 4 –R 7 and R 13 are H or alkyl; R 1 is H, alkyl, fluoroalkyl,...
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7091219 |
Bis-sulfonamide hydroxyethyl-amino retroviral protease inhibitors
Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease...
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7067518 |
Pyridinyl-methyl-ethyl cyclohexanecarboxamides as serotonergic agents
A compound having 5-HT 1A receptor activity, represented by the chemical formula
wherein:
Ar is 2-methoxyphenyl, 1H-indol-4-yl or 2,3-dihydro-1,4-benzodioxin-5-yl; R 1 is 2-, 3- or...
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7067517 |
Use of compounds 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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7026320 |
Serotonergic agents
Novel piperazine derivatives are provided having the formula
wherein R 1 is cyano, nitro, trifluoromethyl or halogen, or pharmaceutically acceptable acid addition salts thereof, which are...
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7026314 |
Therapeutic chromone compounds
Provided herein is a compound of the formula (I) wherein said compound is useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating,...
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7019008 |
Pyrrolidine sulfonamides
A compound of Formula (I):
wherein:
R 1 is C 1-6 alkyl, benzyl, or (CH 2 ) n —C(O)NH 2 ; wherein the benzyl may be unsubstituted or substituted by one or two C 1-6 alkyl, halogen, C 1-6 ...
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7008946 |
CCR5 antagonists useful for treating AIDS
Compounds of the formula
or a pharmaceutically acceptable salt or isomer thereof, wherein:
Q, X and Z are CH or N; R, R 4 –R 7 and R 13 are H or alkyl; R 1 is H, alkyl, fluoroalkyl,...
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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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6916817 |
Inhibitors of metalloproteinases
Arylpiperazines of Formula I useful as metalloproteinase inhibitors, especially as MMP13 inhibitors.
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6900222 |
Pyrrolidinyl, piperdinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
The present invention concerns compounds of formula (I)
a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein...
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6867230 |
Hygromycin A derivatives
This invention relates to compounds of the formula
and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R 1 , R 2 , R 3 and R 10 are as defined herein. The...
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6825200 |
Substituted dipeptides having nos inhibiting activity
The present invention a compound represented by the formula (I): where the structural variables R 1 -R 6 are defined herein.
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6767907 |
4-aryl-1-(indanmethyl dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl) piperidines tetrahydropyridines or piperazines
4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl)piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I), wherein one of X and Y is CH 2 and...
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6753331 |
Heterocyclic derivatives which inhibit factor Xa
The invention relates to heterocyclic derivatives of formula (I), or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful...
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6723722 |
Acylhydrazine derivatives, their production and use
Novel acylhydrazine derivatives exhibiting an inhibitory activity against activated blood coagulation factor X, which are compounds of general formula (I) or salts thereof, wherein R is an...
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6706716 |
Compounds specific for the human α1d adrenergic receptor and uses thereof
This invention is directed towards a method of inhibiting activation of a human α 1d adrenergic receptor which comprises contacting the receptor with a compound so as to inhibit activation of the...
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6680318 |
Piperazinomethylbenzamides as delta-opioid receptor agonists
The present application is directed to compounds having the general formula: and to the use of these compounds in therapeutic methods.
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6660739 |
Heterocyclic amides as inhibitors of factor Xa
This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor...
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6642237 |
Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamides and uses thereof
γ-Hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanam
ide compounds are inhibitors of HIV protease and inhibitors of HIV replication. These compounds are useful in the prevention or...
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6638935 |
Heteroary1 derivatives and their use as medicaments
The invention relates to novel pyridine derivatives of formula 1, to their preparation and to their use as medicaments, in particular for treating tumors
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6602874 |
Heterocyclic carboxamides
A compound of the formula wherein X, Y, Z, R 2 and R 3 are as defined above, useful in treating or preventing migraine, depression and other disorders for which a 5-HT 1 , agonist or...
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6534502 |
Substituted oximes and hydrazones as neurokinin antagonists
Compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein: a is 0-3; b, d and e are 0-2; R is H, alkyl, F or —OR 6 ; A is an optionally substituted...
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6479495 |
Aminoalkylphenol derivatives and related compounds
Novel aminoalkylphenols, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction utilizing the aminoalkylphenols or compositions thereof are disclosed.
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6316445 |
Carboxy substituted acylic carboxamide derivatives
The present invention relates to novel carboxy substituted acyclic carboxamide derivatives of formula (1)): ##STR1## and stereoisomers and pharmaceutically acceptable salts thereof and their use as...
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6277852 |
Piperazinyl 5-HT1 agonists and antagonists
A compound of the formula ##STR1## or the pharmaceutically acceptable salt thereof, wherein Z is oxygen, S(O) m wherein m is 0, 1 or 2; or NQ wherein Q is hydrogen, (C 1 -C 6 )alkyl or phenyl;...
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6258813 |
D4 receptor selectivity piperazine derivatives
Piperazine derivatives of the formula I ##STR1## in which R 1 and R 2 have the meanings given in claim 1 are dopamine ligands with a selectivity for the D4 receptor and are suitable for the...
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6255302 |
1,4-piperazine derivatives
Compounds of the formula ##STR1## are useful for the treatment of disorder of the central nervous system including anxiety, depression, panic, alcohol and drug addiction, sexual dysfunction, sleep...
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6221869 |
N-aminoalkyldibenzothiophenecarboxamides new dopamine receptor subtype specific ligands
Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R 1 , R 2 , R 3 , R 4 are the same or different and represent hydrogen, C...
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6218394 |
4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophene-methyl) piperazines
4-Aryl-1-(indanmethyl, dihydrobenzofuramethyl or dihydrobenzothiophenemethyl) piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I) ##STR1## wherein one of X and Y is CH 2...
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6187774 |
Fused heterocyclic compounds and pharmaceutical applications thereof
The present invention relates to a fused heterocyclic compound of the formula (I) ##STR1## wherein each symbol is as defined in the specification, an optical isomer thereof, a pharmaceutically...
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6172062 |
Dihydrobenzodioxine carboxamide and ketone derivatives
This invention relates to certain 5-HT 4 receptor modulators, particularly 5-HT 4 receptor antagonists, represented by Formula I: ##STR1## wherein Z is formula (A) or (B): ##STR2## wherein R 1 ,...
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6159972 |
Combination of a selective 5-HT.sub.1A antagonist and a selective ub . h5-HT.s1B antagonist or partial agonist
The invention relates to a combination of a first component (a) which is a selective 5-HT 1A receptor antagonist having the formula I wherein R 1 is n-propyl or cyclobutyl, R 2 is isopropyl,...
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6159971 |
Combination of a 5-HT reuptake inhibitor and a H5-HT1B anatagonist or partial agonist
The invention relates to a combination of a first component (a) which is a 5-HT reuptake inhibitor and a second component (b) which is selective h5-HT 1B antagonist or partial agonist having the...
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6159970 |
Combination of a monoamine oxidase inhibitor and a h5-HT.sub.1B antagonist or partial agonist
The invention relates to a combination of a first component (a) which is a monoamine oxidase inhibitor and a second component (b) which is selective h5-HT 1B antagonist or partial agonist having...
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6136808 |
Taxane derivatives
This invention relates to a taxane derivative represented by the following formula (1): ##STR1## (wherein A represents a substituted piperazino or piperidino group, X represents an alkyl, pyridyl,...
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6054437 |
Method for inducing death of neoplastic cells using piperazine derivatives
A method for inducing cell death in neoplastic cells, includes the step of administering a compound of formula I or a pharmaceutically acceptable salt thereof, as a primary chemotherapeutic agent...
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5998416 |
Piperazine, piperidine and tetrahydropyridine derivatives as 5-HT receptor agonists
A class of N-substituted piperazine, piperidine, and tetrahydropyridine derivatives, further subltitutedat the 4-position by an optionally substituted alkenyl, alkynyl, aryl-alkyl or...
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5994356 |
Carboxylic acid derivatives, medicaments comprising these compounds, their use and processes for their production
The present invention relates to carboxylic acid derivatives of the general formula ##STR1## in which R a to R c , A, B, D, E and X 1 to X 3 are as defined in claim 1, their tautomers, their...
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5981520 |
Piperazino derivatives as neurokinin antagonists
The invention relates to compounds of the formula ##STR1## These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.
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