497 results about "Imidazopyridine" patented technology

The present invention relates to 8-amino-aryl-substituted imidazopyrazines which modulate the activity of protein kinases ("PKs"). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.

A method of treating dermal lesions caused by envenomation comprising applying a therapeutically effective amount of an immune response modifier compound selected from the group consisting of imidazoquinoline amines, imidazopyridine amines, 6,7-fused cycloalkylimidazopyridine amines, imidazonaphthyridine amines, tetrahydroimidazonaphthyridine amines, oxazolopyridine amines, oxazoloquinoline amines, thiazolopyridine amines, thiazoloquinoline amines and 1,2-bridged imidazoquinoline amines to the site of the lesion is disclosed.

The present invention relates to imidazopyridine and triazolopyridine derivatives, pharmaceutical compositions and methods of use thereof.

Aqueous gel formulations, including an immune response modifier (IRM), such as those chosen from imidazoquinoline amines, tetrahydroimidazoquinoline amines, imidazopyridine amines, 6,7-fused cycloalkylimidazopyridine amines, 1,2-bridged imidazoquinoline amines, imidazonaphthyridine amines, imidazotetrahydronaphthyridine amines, oxazoloquinoline amines, thiazoloquinoline amines, oxazolopyridine amines, thiazolopyridine amines, oxazolonaphthyridine amines, thiazolonaphthyridine amines, pyrazolopyridine amines, pyrazoloquinoline amines, tetrahydropyrazoloquinoline amines, pyrazolonaphthyridine amines, tetrahydropyrazolonaphthyridine amines, and 1H-imidazo dimers fused to pyridine amines, quinoline amines, tetrahydroquinoline amines, naphthyridine amines, or tetrahydronaphthyridine amines, are provided. Methods of use and kits are also provided.

Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: wherein j is 0 or 1, k is 0 or 1, m is 0, 1, or 2; n is 1 or 2; A is selected from the partial Formulas: where q is 1, 2, or 3, W3 is -O-; -N(R9)-; or -OC(=O)-; R7 is selected from -H; -(C1-C6) alkyl, -(C2-C6) alkenyl, or -(C2-C6) alkynyl substituted by 0 to 3 substituents R10; -(CH2)u-(C3-C7) cycloalkyl where u is 0, 1 or 2, substituted by 0 to 3 R10; and phenyl or benzyl substituted by 0 to 3 R14; R8 is tetrazol-5-yl; 1,2,4-triazol-3-yl; 1,2,4-triazol-3-on-5-yl; 1,2,3-triazol-5-yl; imidazol-2-yl; imidazol-4-yl; imidazolidin-2-on-4-yl; 1,3,4-oxadiazolyl; 1,3,4-oxadiazol-2-on-5-yl; 1,2,4-oxadiazol-3-yl; 1,2,4-oxadiazol-5-on-3-yl; 1,2,4-oxadiazol-5-yl; 1,2,4-oxadiazol-3-on-5-yl; 1,2,5-thiadiazolyl; 1,3,4-thiadiazolyl; morpholinyl; parathiazinyl; oxazolyl; isoxazolyl; thiazolyl; isothiazolyl; pyrrolyl; pyrazolyl; succinimidyl; glutarimidyl; pyrrolidonyl; 2-piperidonyl; 2-pyridonyl; 4-pyridonyl; pyridazin-3-onyl; pyridyl; pyrimidinyl; pyrazinyl; pyridazinyl; indolyl; indolinyl; isoindolinyl; benzo[b]furanyl; 2,3-dihydrobenzofuranyl; 1,3-dihydroisobenzofuranyl; 2H-1-benzopyranyl; 2-H-chromenyl; chromanyl; benzothienyl; 1H-indazolyl; benzimidazolyl; benzoxazolyl; benzisoxazolyl; benzothiazolyl; benzotriazolyl; benzotriazinyl; phthalazinyl; 1,8-naphthyridinyl; quinolinyl; isoquinolinyl; quinazolinyl; quinoxalinyl; pyrazolo[3,4-d]pyrimidinyl; pyrimido[4,5-d]pyrimidinyl; imidazo[1,2-a]pyridinyl; pyridopyridinyl; pteridinyl; or 1H-purinyl; or A is selected from phosphorous and sulfur acid groups; W is -O-; -S(=O)t-, where t is 0, 1, or 2; or -N(R3)-; Y is =C(R1a)-, or -[N<custom-character file="US20020111495A1-20020815-P00900.TIF" wi="20" he="20" id="custom-character-00001" / >(O)k] where k is 0 or 1; R4, R5 and R6 are (1) -H; provided that R5 and R6 are not both -H at the same time, -F; -Cl; -(C2-C4) alkynyl; -R16; -OR16; -S(=O)pR16; -C(=O)R16, -C(=O)OR16, -C(=O)OR<highlight><sup

The disclosure provides methods for the treatment and prevention of periodontal disease. In preferred embodiments, the invention provides for local treatment of periodontal tissues with a pharmaceutical composition including an immune response modifier (IRM) selected from the group of immune response modifiers comprising imidazoquinoline amines, imidazopyridine amines, 6,7-fused cycloalkylimidazopyridine amines, imidazonaphtyridine amines, oxazoloquinoline amines, thiazoloquinoline amines and 1,2-bridged imidazopyridine amines.

Dye labeled imidazonaphthyridine, imidazopyridine and imidazoquinoline compounds having immune response modulating activity are disclosed. The compounds arc useful, inter alia, for determining the binding and / or receptor sites of the molecules.

The present invention provides a compound represented by the formula (I):whereinring A is a ring which is optionally further substituted;R1 is a hydrogen atom or a substituent;R2 is a hydrogen atom or a substituent;R3 is a hydrogen atom or a substituent;R4 is a hydrogen atom or a substituent;R5 is a hydrogen atom or a substituent;R6 is a hydrogen atom or a substituent;X is ═N— or ═C(Z)- (Z is a hydrogen atom or a substituent);when X is ═C(Z)-, Z and R6 are optionally bonded to each other to form, together with the carbon atom bonded thereto, an optionally substituted ring,provided that when X is ═CH—, then R6 is not optionally substituted 2-piperidinyl, excluding N-imidazo[1,2-a]pyridin-2-yl-4-methyl-benzamide, N-imidazo[1,2-a]pyridin-2-yl-benzamide and N-(7-methylimidazo[1,2-a]pyridin-2-yl)-benzamide, or a salt thereof, and a pharmaceutical agent containing same.The compound of the present invention has an ASK1 inhibitory action, and is useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, inflammatory diseases and the like, and the like.

The invention belongs to the field of medicinal chemical engineering, and relates to application of 2-arylimidazo[1,2-alpha]pyridine-3-acetamide derivatives to prepare medicines for controlling PTSD (posttraumatic stress disorder). Specifically, the invention relates to application of a compound shown as a formula I and pharmaceutically salts thereof to prepare medicines for controlling and / or treating and / or auxiliarily treating PTSD, wherein the compound and the pharmaceutically salts thereof are used as TSPO (translocator protein) ligands. The TSPO ligands such as the compounds shown as the formula I and the pharmaceutically salts are capable of effectively preventing and / or treating and / or auxiliarily treating PTSD, and can be used to prevent medicines for controlling and / or treating and / or auxiliarily treating PTSD.

The present invention provides novel purine and imidazopyridine derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formulas:

The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt, amide or ester thereof, wherein R<1 >represents a hydrogen atom or a halogen atom; R<2 >represents a hydrogen atom, etc.; R<3 >represents an alkyl group having from 1 to 10 carbon atoms; said alkyl group of R<3 >is substituted by at least one substituent selected from the group consisting of substituents alpha; said substituents alpha is aryl, hydroxy, oxo, etc.; said aryl having 6 to 10 carbon atoms; said aryl is unsubstituted or substituted by at least one alkyl group having from 1 to 6 carbon atoms; said heterocyclic and the heterocyclic moiety of said heterocycliccarbonyl, both of substituents alpha, are 5- to 10-membered cyclic groups containing from 1 to 4 heteroatoms selected from the group consisting of nitrogen atoms, oxygen atoms and sulfur atoms These compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt thereof, wherein R<1 >represents a hydrogen atom or a halogen atom; R<2 >represents a methyl group or an ethyl group; R<3 >represents a branched alkyl group having from 3 to 6 carbon atoms or an alkyl group having from 3 to 6 carbon atoms substituted by an alkoxy group having from 1 to 6 carbon atoms; with the proviso that when the terminal carbon atom of said alkyl group of R<3 >is substituted by said alkoxy group, said alkyl group is a branched alkyl group. These compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

The present invention provides novel purine and imidazopyridine derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formulas:

The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5 b]pyridin-2-one compounds and analogs thereof, which, inter alia, inhibit RAF (e.g., B RAF) activity, inhibit cell proliferation, treat cancer, etc., and more particularly to compounds of the formulae: wherein: J is independently —O— or —NRN1−; RN1, if present, is independently —H or a substituent; RN2 is independently —H or a substituent; Y is independently —CH═ or —N═; Q is independently —(CH2)j-M-(CH2)k— wherein: j is independently 0, 1 or 2; k is independently 0, 1, or 2; j+k is 0, 1, or 2; M is independently O—, —S—, —NH—, —NMe-, or —CH2—; each of RP1, RP2, RP5, and RP4 is independently —H or a substituent; and additionally RP1 and RP2 taken together may be CH═CH—CH═CH—; and additionally RP1 and RP5 taken together may be CH═CH—CH═CH—; L is independently: a linker group formed by a chain of 2, 3, or 4 linker moieties; each linker moiety is independently CH2—, —NRN—, —C(═X)—, or —S(═O)2—; either: exactly one linker moiety is —NRN—, or: exactly two linker moieties are —NRN—; either: exactly one linker moiety is —C(═X)—, and no linker moiety is —S(═O)2—, or: exactly one linker moiety is —S(═O)2—, and no linker moiety is —C(═X)—; no two adjacent linker moieties are —NRN—; X is independently ═O or ═S; each RN is independently —H or a substituent; A is independently: C6-14carboaryl, C5-14heteroaryl, C3-12carbocyclic, C3-12heterocyclic; and is independently unsubstituted or substituted; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, N-oxides, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., B-RAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and conditions that are ameliorated by the inhibition of RAF, RTK, etc., proliferative conditions such as cancer (e.g., colorectal cancer, melanoma), etc.

The invention relates to imidazopyridines of formula I with anti-cancer and / or anti-inflammatory activity and more specifically to imidazopyridines which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt, amide or ester thereof, wherein R1 represents a hydrogen atom or a halogen atom; R2 represents a hydrogen atom, etc.; R3 represents an alkyl group having from 1 to 10 carbon atoms; said alkyl group of R3 is substituted by at least one substituent selected from the group consisting of substituents α; said substituents α is aryl, hydroxy, oxo, etc.; said aryl having 6 to 10 carbon atoms; said aryl is unsubstituted or substituted by at least one alkyl group having from 1 to 6 carbon atoms; said heterocyclic and the heterocyclic moiety of said heterocycliccarbonyl, both of substituents α, are 5- to 10-membered cyclic groups containing from 1 to 4 heteroatoms selected from the group consisting of nitrogen atoms, oxygen atoms and sulfur atomsThese compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

A process for the preparation of imidazo[1,2-a]pyridine derivatives of the formula I: wherein R is hydrogen, halogen or a C1-C4 alkyl group; R1 and R2 are independently hydrogen, a straight or branched C1-C6 alkyl group which is unsubstituted or substituted by one or more halogen atoms, hydroxyl, N(C1-C4 alkyl)2, carbamoyl or C1-C4 alkoxy radicals, a C1-C6 alkyl hydroxy group, a C3-C6 cycloalkyl radical, a benzyl radical, a phenyl radical or R1 and R2 together with the nitrogen atom to which they are bonded are joined together to form a substituted or unsubstituted heterocyclic group optionally containing one or more additional heterocyclic atoms; and R3 and R4 are independently hydrogen, halogen or a C1-C4 alkyl group, or a pharmaceutically acceptable salt thereof, the process comprising (a) reacting an imidazo[1,2-a]pyridine carboxylic acid of the formula II wherein R, R3 and R4 have the aforestated meanings with a halogenating agent in the absence of a solvent to form an acid halide intermediate and (b) reacting the acid halide intermediate with an amine of the formula HNR1R2 wherein R1 and R2 have the aforestated meanings to form the compound of formula I.

The present invention relates to a pharmaceutical composition for the treatment or prevention of viral infections comprising as an active principle at least one imidazo[4,5-c]pyridine derivative having the general formula (Z): (formula). The invention also relates to processes for the preparation of compounds according to the invention having above mentioned general formula and their use as a medicine or to treat or prevent viral infections.

The present invention relates to pyrazolopyridines and imidazopyridines which are inhibitors of the kinase PDK1 and are thus useful for the treatment of myeloproliferative disorders or cancer. The compounds are also useful as inhibitors of other kinases such as FGFR3, NTRK3, RP-S6K and WEE1. Furthermore, the present compounds also selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease.

Imidazopyridine-based compounds and organic light emitting diodes (OLEDs) including organic layers including the imidazopyridine-based compounds are provided. The organic light emitting diodes including organic layers having the imidazopyridine-based compounds have low driving voltages, high efficiencies, high luminance, long life-times and low power consumption.

The present invention provides imidazopyridine compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.

The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5 b]pyridin-2-one compounds and analogs thereof, which, inter alia, inhibit RAF (e.g., B RAF) activity, inhibit cell proliferation, treat cancer, etc. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., B-RAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and conditions that are ameliorated by the inhibition of RAF, RTK, etc., proliferative conditions such as cancer (e.g., colorectal cancer, melanoma), etc.

The present invention provides a process of a compound of the formula (I): wherein R is heteroaryl or the like, ring A is a heteroalicyclic group or the like comprising reacting a compound of the formula (II): wherein Hal is halogen and the other symbols are the same as the above, in the presence of a sulfinic acid salt and further in the presence of an acid or a salt with an organic base, and a novel crystal form of 2-(3-isoxazolyl)-3,6,7,9-tetrahydroimidazo[4,5-d]pyrano[4,3-b]pyridine phosphate monohydrate.

This invention provides for compounds, compositions, and methods that involve anti-proliferative and anti-neoplastic activity in cancer cells. In particular, a series of benzimidazole, purine, imidazopyridine, and imidazopyrizine compounds having selected substitution patterns are disclosed, and the activity of various subject compounds is demonstrated.

The invention discloses 14 3H-imidazo[4,5-c]pyridine-6-formyl-amido acid benzyl esters shown in the general formula I. In the general formula I, AA represents L-Ser residue, L-Glu (OBzl) residue, L-Phe residue, L-Val residue, L-Arg residue, L-Tyr residue, L-Ala residue, L-Trp residue, L-Asn residue, L-Met residue, L-Ile residue, Gly residue, L-Asp (OBzl) residue or L-Leu residue. The invention discloses a preparation method of the 3H-imidazo[4,5-c]pyridine-6-formyl-amido acid benzyl esters, discloses HT-29, K562, A549 and HL60 tumor cell growth inhibition effects of the 3H-imidazo[4,5-c]pyridine-6-formyl-amido acid benzyl esters, further discloses S180-loading mice tumor growth inhibition effects of the 3H-imidazo[4,5-c]pyridine-6-formyl-amido acid benzyl esters, and also discloses use of the 3H-imidazo[4,5-c]pyridine-6-formyl-amido acid benzyl esters as antitumor drugs.

The present invention is concerned with aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine derivatives of formula I: wherein R1 to R5 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof. This class of compounds has high affinity and selectivity for GABA A α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.