3590 results about "Pyridyne" patented technology

The present invention relates to novel compounds, in particular novel thieno-pyridine and thieno-pyrimidine derivatives according to Formula (I), wherein all radicals are defined in the application. The compounds according to the invention are positive allosteric modulators of metabotropic receptors-subtype 2 ("mGluR2") which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

The present invention relates to urotensin II receptor antagonists, pharmaceutical compositions containing them and their use.

The invention relates to the field of pharmaceutical chemistry and specifically discloses an aryl ruthenium-beta-carboline complex and its preparation method and application. The aryl ruthenium-beta-carboline complex is [Ru(Eta6-arene)(N-N)Cl](PF6), wherein Eta6-arene is aryl ligand p-cymene(p-cymene, CYM) or benzene(benzene, Ben), N-N is beta-carboline alkaloid derivative1-(2-pyridine)-9H-pyridine[3,4-b]indole(L1), 1-(2-quinoline)-9H-pyridine[3,4-b]indole(L2) or 1-(2-imidazole)-9H-pyridine[3,4-b]indole(L3). The complex provided by the invention has very outstanding activity in in-vitro antitumor screening. In addition, in comparison with cancer cell lines, toxicity of the complex to normal cells is greatly reduced, and the complex has a good potential for development of antitumor drugs.

The invention relates to certain pyrrolobenzodiazepines (PBDs), and in particular pyrrolobenzodiazepine dimers bearing C2 substitutions, including compounds of formula (T): wherein: R² is CHR^2A, and R^2A is independently selected from H, R, CO₂R, COR, CHO, CO₂H, and halo; R⁶ and R⁹ are independently selected from H, R, OH, OR, SH, SR, NH₂, NHR, NRR′, NO₂, Me₃Sn and halo; R⁷ is independently selected from H, R, OH, OR, SH, SR, NH₂, NHR, NRR′, NO₂, Me₃Sn and halo; R⁸ is independently selected from H, R, OH, OR, SH, SR, NH₂, NHR, NRR′, NO₂, Me₃Sn and halo; R is independently selected from optionally substituted C_1-12 alkyl, C_3-20 heterocyclyl and C_5-20 aryl groups; or the compound is a dimer with each monomer being of formula (M), where the R⁷ groups or R⁸ groups of each monomer form together a dimer bridge having the formula —X—R″—X— linking the monomers; wherein R″ is a C_3-12 alkylene group, which chain may be interrupted by one or more heteroatoms, e.g. O, S, N(H), and/or aromatic rings, e.g. benzene or pyridine; and each X is independently selected from O, S, or N(H); or any pair of adjacent groups from R⁶ to R⁹ together form a group —O—(CH₂)_p—O—, where p is 1 or 2, and salts and solvates thereof, and their use as intermediates for the preparation of other PBD compounds.

The invention provides methods for treating and/or preventing and/or slowing the onset and/or development of ALS using hydrogenated pyrido(4,3-b)indoles, such as dimebon.

The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate receptors subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and such compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

The invention discloses a preparation method for an iron-nitrogen co-doped porous carbon sphere material. The preparation method comprises the following steps: by taking 2-aminopyridine as a monomer and taking ammonium persulfate and ferric chloride as oxidants, performing in-situ polymerization reaction in a duct of a porous silicon dioxide template to obtain a precursor; performing high-temperature carbonization treatment on the precursor in a tubular furnace and an inert gas nitrogen-gas environment; and removing the silicon dioxide template by hydrofluoric acid to obtain the iron-nitrogen co-doped porous carbon sphere material which is taken as an electric catalyst to achieve good catalytic effect in oxygen gas reduction reaction. The preparation method has the advantages that the process is simple and easy to perform and the raw materials are cheap. The prepared carbon material contains a three-dimensional communicated pore structure, has a high specific surface area and a large pore volume, can effectively improve the electric catalytic activity through the heteroatom nitrogen-iron doping, has relatively high electric catalytic efficiency while being applied as a low-price electric catalyst, and has an important value and significance in the fields of doped type porous carbon material preparation and proton membrane fuel battery electric catalysis.

Compositions based on hydrogenated pyrido[4,3-b]indoles (variants) of formula (1) or formula (2): are provided, as are methods and kits using those compositions for the treatment of anxiety or mood disorders characterized by stresses, anxiety, neuroses, obsessive fears and their consequences.

The present invention provides a compound which has an effect of inhibiting amyloid-β production and is useful as a therapeutic agent for diseases induced by production, secretion and/or deposition of amyloid-β proteins. The present invention relates to a compound represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof:

wherein A is optionally substituted carbocyclic diyl or optionally substituted heterocyclic diyl; B is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R¹ is a group such as optionally substituted lower alkyl; R² is a group such as hydrogen; and R^3a and R^3b are each independently a group such as hydrogen, provided that the following compound is excluded.

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 —NR^N1−; R^N1, if present, is independently —H or a substituent; R^N2 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 R^P1, R^P2, R^P5, and R^P4 is independently —H or a substituent; and additionally R^P1 and R^P2 taken together may be CH═CH—CH═CH—; and additionally R^P1 and R^P5 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—, —NR^N—, —C(═X)—, or —S(═O)₂—; either: exactly one linker moiety is —NR^N—, or: exactly two linker moieties are —NR^N—; 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 —NR^N—; X is independently ═O or ═S; each R^N is independently —H or a substituent; A is independently: C_6-14carboaryl, C_5-14heteroaryl, C_3-12carbocyclic, C_3-12heterocyclic; 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 present disclosure provides substituted 9H-pyrimido[4,5-b]indoles and 5H-pyrido[4,3-b]indoles and related analogs represented by Formula I:

and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R^1a, A, B¹, B², G, X¹, Y¹, Y², and Y³ are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains. Compounds of the present disclosure are especially useful for treating cancer.

To provide a diagnostic drug which binds specifically to an amyloid aggregate and/or an amyloid deposit, to thereby realize imaging and quantification of a disease caused by amyloid aggregation and/or deposition.

The invention provides a compound represented by formula (1):

(wherein X¹ represents an optionally substituted bicyclic heterocyclic group;

• • X² represents a hydrogen atom, a halogen atom, or a chelate-forming group;
  • ring A represents a benzene ring or a pyridine ring; and
  • ring B represents an optionally substituted 5-membered aromatic heterocyclic group which is bonded to the benzene ring or the pyridine ring via a carbon atom of ring B), a salt thereof, a solvate of any of these, or a transition metal coordination compound of any of these, and a diagnostic, preventive, or therapeutic drug containing the same.

Derivatives of pyrrolo[2,3-b]pyridine which are useful as SGK-1 kinase inhibitors are described herein. The invention described herein also describes pharmaceutical compositions containing derivatives of pyrrolo[2,3-b]pyridine and methods of using pyrrolo[2,3-b]pyridine derivatives and pharmaceutical compositions thereof in the treatment of diseases mediated by SGK-1.

A 2-phenyl-6-azolylpyridine-based ligand is represented by the following formula (I):

wherein, X represents nitrogen or C—R¹⁰; R¹, R², R³, R⁴, R⁵, R⁶, R⁷, R⁸ and R¹⁰ independently represent hydrogen, halogen, a cyano group, an amino group, an optionally substituted aryl group, an optionally substituted heteroaryl group, sulfate, —COOH, an alkoxy group, a carbonyl group, a C₁-C₁₀ haloalkyl group, a C₁-C₁₂ alkyl group, a C₂-C₁₀ alkenyl group, a C₂-C₁₀ alkynyl group, a C₃-C₂₀ cycloalkyl group, a C₃-C₂₀ cycloalkenyl group, a C₁-C₂₀ heterocycloalkyl group, or a C₁-C₂₀ heterocycloalkenyl group; and R⁹ represents hydrogen or alkali metal.

Certain quinolizidine and octahydropyridopyrazine compounds, pharmaceutical compositions, and methods of their use, inter alia, as opioid receptor antagonists are disclosed.

The invention relates to a method for preparing (S)-(4-chlorphenyl)-(pyridine-2-yl)-methanol by utilizing microbial catalysis, and belongs to the technical field of biological catalysis. According to the method, 4-chlorphenyl-(pyridine-2-yl)-ketone is subjected to asymmetrical reduction by utilizing kluyveromycessp (CCTCCM 2011385) whole cells to synthesize the (S)-(4-chlorphenyl)-(pyridine-2-yl)-methanol. The method comprises the following steps of: sieving a microbe which has high-stereoselectivity carbonyl reductase activity on a prochiral ketone substrate, determining a series of conditions of asymmetrical reduction reaction, such as reaction temperature, pH, the concentration of cells, the concentration of the substrate and reaction time and additives (including various secondary solvents, polyethyleneglycol (PEG), phosphates and the like), wherein the enantiomer excess value and yield of the (S)-(4-chlorphenyl)-(pyridine-2-yl)-methanol serving as a product can reach 86.7 percent e.e and 92.1. The product is separated and extracted initially by silicagel column chromatography, so that the purity of the separated product is 99.2 percent, and the extraction yield is 56.7 percent.