3 is hydrogen or a hydroxyl protecting group; and X is halogen or a leaving group. The preparation method therefor has the advantages of mild reaction conditions, high selectivity, easy purification, low synthesis cost and the like, being suitable for large scale production.
C07D 307/30 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07D 407/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 307/28 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 407/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
The present invention relates to an amphiphilic block copolymer represented by formula I, a preparation method thereof, and a nanomicelle drug delivery system formed from the copolymer and a poorly soluble drug. The amphiphilic block copolymer includes a hydrophilic chain segment, a hydrophobic chain segment, and a linker for linking the hydrophilic chain segment to the hydrophobic chain segment. The linker contains an unsaturated structure, which can enhance the interaction between the poorly soluble drug and the copolymer to improve the drug loading ability and stability of the nanomicelle. The invention also relates to a nanomicelle drug-loading system, a preparation method thereof, and the use of the nanomicelle drug-loading system for preparing medicines for treating tumors, inflammation, diabetes, central nervous system diseases, cardiovascular diseases, and psychological disorders.
Disclosed in the present invention are an imidazolone androgen receptor antagonist, a preparation method therefor and use thereof. The imidazolone androgen receptor antagonist of the present invention has a structure represented by formula I, and can be used for treating and preventing diseases associated with androgen receptors, such as prostate cancer.
C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 411/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
The present invention provides a 1-methyl-tryptophan compound and a preparation method and use thereof. The 1-methyl-tryptophan compound of the present invention has a structure shown in formula I. Compared to a corresponding non-deuterated compound, the deuterated 1-methyl-tryptophan compound of the present invention has more excellent pharmacokinetic properties. (I)
C07D 209/20 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals substituted additionally by nitrogen atoms, e.g. tryptophane
A61K 31/405 - Indole-alkanecarboxylic acidsDerivatives thereof, e.g. tryptophan, indomethacin
A deuterated 3-quinuclidone compound, a preparation method, and a use. In particular, the present invention provides a compound shown in general formula I or a pharmaceutically acceptable salt, isomer or a mixture thereof, solvate, polymorph, stable isotopic derivative, or prodrug thereof and a preparation method and pharmaceutical application of the same. The deuterated 3-quinuclidone compound has excellent pharmacokinetic properties and antitumor activity. (I)
C07D 453/02 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
C07B 59/00 - Introduction of isotopes of elements into organic compounds
Provided are a chiral 3-quinuclidone compound, a preparation method, and a use. In particular, the present invention provides a compound shown in general formula I-A or I-B or a pharmaceutically acceptable salt, isomer or a mixture thereof, solvate, polymorph, stable isotopic derivative, or prodrug thereof and a preparation method and application of the same. The compound has good cell proliferation inhibitory activity and pharmacokinetic properties and can be used to treat cancer, autoimmune diseases, etc. (IA) (IB)
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
Disclosed in the present invention are an indoleamine-2,3-dioxygenase inhibitor compound, a preparation method therefor, and an application thereof. The indoleamine-2,3-dioxygenase inhibitor compound provided by the present invention is as represented by formula I. Compared with a corresponding non-deuterated compound, the deuterated compound in the present invention has obviously more excellent pharmacodynamic properties and pharmacokinetic properties, and Cmax is increased by 50% or more, and AUC is increased by 10% or more. Thus, the exposure of the deuterated compound in animal bodies is significantly increased. Therefore, the deuterated compound is more suitable as an indoleamine-2,3-dioxygenase inhibitor, and is accordingly more suitable for preparation of drugs for treatment of diseases associated with indoleamine-2,3-dioxygenase inhibitors.
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
8.
POLY(ADP-RIBOSE) POLYMERASE INHIBITOR, PREPARATION METHOD AND USE
Disclosed are a compound as shown in general formula I, a pharmaceutically acceptable salt, an isomer or a mixture thereof, and a solvate, a polymorph, a stable isotope derivative or a prodrug thereof. The compound of the present invention has comparatively strong PARP inhibitory activity and can be used for treating diseases associated with PARP, such as cancers and inflammatory diseases.
C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
Disclosed are an intermediate of Eribulin and a preparation method therefor. In particular, disclosed are compounds as represented by formula II, formula III and formula V and a preparation method therefor. Ar is C1-10 alkyl substituted, alkyloxy substituted or unsubstituted aryl; R1 and R2 is an acetal protecting group or a thioacetal protecting group; R3 is hydrogen or a hydroxyl protecting group; and X is halogen or a leaving group. The preparation method therefor has the advantages of mild reaction conditions, high selectivity, easy purification, low synthesis cost and the like, being suitable for large scale production.
C07F 7/18 - Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
C07D 407/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 307/28 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 493/22 - Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains four or more hetero rings
10.
COMPOUND WITH KINASE INHIBITORY ACTIVITY AND PREPARATION METHOD AND USE THEREOF
The present invention provides a compound as shown in general formulas (I) or (II) and a pharmaceutically acceptable salt, an isomer or a mixture form thereof, a solvate, a polymorph, a stable isotope derivative, or a prodrug of the same. The compound of the present invention has CDK kinase inhibitory activity and can be used in treating a disease related to CDK kinase, such as a cancer.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
Disclosed are a boric acid and borate ester compound, and a preparation method and use therefor. Specifically disclosed are a borate ester compound of formula I, a crystal form, and pharmaceutically acceptable salts, hydrates or solvates thereof, and a borate ester compound of formula II, a crystal form, and pharmaceutically acceptable salts, hydrates or solvates thereof. The boric acid and borate ester compound of the present invention have the function of inhibiting proteasome and can be used for treating multiple myeloma.
C07C 233/81 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
C07C 47/02 - Saturated compounds having —CHO groups bound to acyclic carbon atoms or to hydrogen
C07C 321/12 - Sulfides, hydropolysulfides, or polysulfides having thio groups bound to acyclic carbon atoms
patents
