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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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7361654 |
Substituted heteroaryl amide modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
The present invention relates to new class of non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity...
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7300939 |
Substituted 1-propiolylpiperazine compounds, their preparation and use
Substituted 1-propiolylpiperazine compounds corresponding to formula I
in which X denotes N or C—R 2 , and n is an integer from 0 to 8, a method for producing such substituted...
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7297693 |
Nitrogen-containing heterocyclic compounds and their use as Raf inhibitors
Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac...
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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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7238688 |
Piperidine compounds
Disclosed are novel compounds of the formula
Also disclosed are pharmaceutical compositions comprising the compounds of Formula I. Also disclosed are methods of treating various diseases or...
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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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7101886 |
Phenylalkyl and pyridylalkyl piperazine derivatives
This invention relates to compounds of the formula 1
wherein R 1 , R 3 , R 4 , X 1 , and X 2 are defined as in the specification, pharmaceutical compositions containing them and their use in...
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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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RE39265 |
Heteroarylpiperidines, and their use as antipsychotics and analgetics
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a...
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7094778 |
Heterocyclylalkylamines as muscarinic receptor antagonists
This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I:
wherein X, Y, and Z are O, S or NR 5 , and the other...
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7087610 |
Benzothiazole antiviral agents
The invention encompasses a series of benzothiazole compounds which inhibit HIV entry and are useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions...
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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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6979690 |
Oxo or oxy-pyridine compounds as 5-HT4 receptor modulators
This invention provides compounds of the formula (I) and (II):
or the pharmaceutically acceptable esters thereof, and the pharmaceutically acceptable salts thereof: wherein R 1 is hydrogen or...
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6875767 |
(5-cyano-2-thiazolyl)amino-4-pyridine tyrosine kinase inhibitors
The present invention relates to compounds having the formula I:
which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and...
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6872724 |
Polymorphs with tyrosine kinase activity
The present invention relates to active polymorphs of 4-[2-(5-cyano-thiazol-2-ylamino)-pyridin-4-ylmethyl]-piperaz
ine-1-carboxylic acid methylamide which inhibit, regulate and/or modulate tyrosine...
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6833369 |
Angiogenesis inhibiting 5-substituted-1,2,4,-thiadiazolyl derivatives
This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; R 1 is...
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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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6821972 |
3-heterocyclylpropanohydroxamic acid PCP inhibitors
Compounds of formula (I): and their salts, solvates, hydrates and prodrugs are useful PCP inhibitors, processes for making the same, compositions comprising the same, and methods of treating a...
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6784173 |
Aromatic dicarboxylic acid derivatives
Compounds of formula I wherein A, R 1 and R 2 are defined in the specification. These compounds are useful as HDAC inhibitors. Also disclosed are methods of making and using said compounds.
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6756374 |
Diaminothiazoles having antiproliferative activity
Disclosed are novel diaminothiazoles of formula wherein R 1 , R 2 , R 3 , R 4 and R 5 are as herein disclosed. These compounds and their pharmaceutically acceptable salts and esters are...
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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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6617339 |
Oxazolidinone derivatives, process for their preparation and pharmaceutical compositions containing them
Compounds of formula (I) as defined herein, or a pharmaceutically acceptable salt, or an in-vivo-hydrolysable ester thereof, are useful as antibacterial agents. Processes for their manufacture and...
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6610707 |
Heterocyclic compounds as inhibitors of rotomase enzymes
Compounds of the formula: wherein R 1 , Y, W, A and R 2 are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore moderate neuronal...
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6596745 |
Method for treating fibrotic diseases with azolium chroman compounds
Provided is a method of treating or ameliorating hypertension in an animal comprising administering an effective amount of a compound of formula I:
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6596724 |
Oxadiazole and thiadiazole derivatives of dihydropyridine NPY antagonists
A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of oxadiazole, thiadiazole and thiadiazole oxide derivatives of dihydropyridines of Formula I. wherein B is...
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6579880 |
Isoxazoles and oxadiazoles as anti-inflammatory inhibitors of IL-8
The invention relates to isoxazole and oxadiazole compounds of Formulae I and II, pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds...
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6576630 |
Compounds and compositions as protease inhibitors
The present invention relates to novel alkanoyl-substituted heterocyclic derivatives which are cysteine protease inhibitors; the pharmaceutically acceptable salts and N-oxides thereof; their uses...
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6573262 |
Composition and antiviral activity of substituted indoleoxoacetic piperazine derivatives
The invention comprises substituted indoleoxoacetic piperazine derivatives of general Formula I, compositions thereof and their use as antiviral agents, and particularly for treating HIV infection.
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6569878 |
Substituted 4-amino-thiazol-2-yl compounds as cyclin-dependent kinase inhibitors
Pharmaceutical compositions containing effective amounts of CDK-inhibiting diaminothiazole compounds of the following formula (where R 1 and R 2 are as defined in the specification) or their...
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6465456 |
Isoxazolinone antibacterial agents
This invention describes isoxazolinone derivatives which possess antibacterial activity and are useful in the treatment of bacterial diseases. More particularly, new isoxazolinones are provided...
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RE37886 |
1-(1,2-Disubstituted piperidinyl)-4-substituted piperazine derivatives
This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, as substance-P antagonists; their...
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6458790 |
Substituted piperidines as melanocortin receptor agonists
Certain novel substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are...
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6444677 |
5-membered heteroaryl substituted 1,4-dihydropyridine compounds as bradykinin antagonists
This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof wherein A is independently halo; Y 1 is —(CH 2 ) m —, C(O) or S(O); Y 2 is N or CH;...
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6432958 |
2-piperazinoalkylaminobenzoazole derivatives: dopamine receptor subtype specific ligands
Disclosed are compounds of the formula: or pharmaceutically acceptable salts thereof, wherein: A is (un)substituted alkylene; R 1 and R 2 are the same or different and represent hydrogen,...
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6369063 |
Selective factor Xa inhibitors
Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating...
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6355643 |
Inhibitors of prenyl-protein transferase
The present invention comprises unsubstituted and substituted piperazine-containing compounds having alkanoyl, alkylsulfonyl, alkylamido or alkoxycarbonyl substituents, and having the formula A, ...
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6284775 |
3-[4-(1-substituted-4-piperazinyl)butyl]-4-thiazolidinone and related compounds
There are disclosed compounds of the formula, ##STR1## where n is 0, 1 or 2; A is ##STR2## where X in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy,...
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6284759 |
2-piperazinoalkylaminobenzo-azole derivatives: dopamine receptor subtype specific ligands
Disclosed are compounds of the formula: ##STR1## or pharmaceutically acceptable salts thereof, wherein: A is (un)substituted alkylene; R 1 and R 2 are the same or different and represent...
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6277872 |
Oxadiazoles, processes for their preparation and their use as medicaments
The invention relates to oxadiazole derivatives of general formula (I) ##STR1## wherein X, Y, Z and R 1 are defined as described in the specification and claims, processes for preparing them...
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6239134 |
Diazole derivatives as serotonergic agents
The present invention provides compounds of the general formula (1): ##STR1## wherein: two atoms of X, Y, or Z are nitrogen and the third atom is sulfur or oxygen; R is H, halogen, OH, SH, 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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6211183 |
Selective factor Xa inhibitors
Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating...
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6166033 |
2-carbonylthiazole derivatives and use of the same
This invention provides a 2-carbonylthiazole derivative represented by formula (I): ##STR1## wherein each of Ar 1 and Ar 2 represents a phenyl group or a substituted phenyl group; R 1 represents...
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6130217 |
Compounds enhancing antitumor activity of other cytotoxic agents
This invention relates to certain heterocyclic compounds and their pharmaceutically acceptable salts, which are useful for sensitizing multidrug-resistant tumor cells to anticancer agents and...
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6114328 |
Isoxazoline and isoxazole fibrogen receptor antagonists
This invention relates to novel isoxazolines and isoxazoles which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex or the vitronectin receptor, to...
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6090813 |
Use of oxido-squalene cyclase inhibitors to lower blood cholesterol
A compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein G, T 1 , T 2 and T 3 are selected from CH and N; provided that T 2 and T 3 are not both CH; A is selected from...
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6090807 |
Use of heterocyclic compounds
The present invention relate to the use of heterocyclic compounds of the following formula: Het--A--B--Ar where Het, A, B and Ar have the meanings stated in the description. The compounds...
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6066631 |
Chroman derivatives
The present invention relates to chroman derivatives of the formula (I): ##STR1## [wherin R 1 represents a hydrogen atom, a halogen atom, a C 1 -6 alkyl group, a C 1 -6 alkoxy group, a C 3 -6...
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6060472 |
Thiadiazole compounds useful as inhibitors of H.sup.+ /K.sup.+ atpase
Novel 3,5-disubstituted 1,2,4-thiadiazole compounds are provided, which are effective in treating peptic ulcers by the inhibition of H + /K + -ATPase. The compounds of the present invention are...
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