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179results about How to "Promote apoptosis" patented technology

Carbamic acid compounds comprising a piperazine linkage as hdac inhibitors

InactiveUS20050143385A1Promote apoptosisInhibiting cell cycle progressionOrganic active ingredientsNervous disorderAcetylase activityProdrug
This invention pertains to certain carbamic acid compounds which inhibit HDAC (histone deacetylase) activity of the following formula:
wherein: Cy is independently a cyclyl group; Q1 is independently a covalent bond or cyclyl leader group; the piperazin-1,4-diyl group is optionally substituted; J1 is independently a covalent bond or —C(═;O)—; J2 is independently —C(═O)— or —S(═O)2—; Q2 is independently an acid leader group; wherein: Cy is independently: C3-20carbocyclyl, C3-20heterocyclyl, or C5-20aryl; and is optionally substituted; Q1 is independently: a covalent bond; C1-7alkylene; or C1-7alkylene-X—C1-7alkylene, —X—C1-7alkylene, or C1-7alkylene-X—, wherein X is —O— or —S—; and is optionally substituted; Q2 is independently: C4-8alkylene; and is optionally substituted; and has a backbone length of at least 4 atoms; or: Q2 is independently: C5-20arylene; C5-20arylene-C1-7alkylene; C1-7alkylene-C5-20arylene; or, C1-7alkylene-C5-20arylene-C1-7alkylene; and is optionally substituted; and has a backbone length of at least 4 atoms; or a pharmaceutically acceptable salt, solvate, amide, ester, ether, chemically protected form, or prodrug 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 HDAC, and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.
Owner:TOPOTARGET UK LTD

Imidazo[4,5-B]Pyridin-2-One and Oxazolo[4,5-B]Pyridin-2-One Compounds and Analogs Thereof as Therapeutic Compounds

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 formula (I): 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, RP3, and RP4 is independently —H or a substituent; and additionally RP1 and RP2 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—; exactly one linker moiety is —NRN—, or: exactly two linker moieties are —NRN—; 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.
Owner:THE INST OF CANCER RES ROYAL CANCER HOSPITAL +2

Tetrastigma hemsleyanum Duels et Gilg tea with high contents of Tetrastigma hemsleyanum Duels et Gilg flavone, polysaccharide and kaempferol and manufacturing method of same

The invention belongs to the technical field of tea production, and particularly relates to a Tetrastigma hemsleyanum Duels et Gilg tea with high contents of Tetrastigma hemsleyanum Duels et Gilg flavone, polysaccharide and kaempferol, and a manufacturing method of the Tetrastigma hemsleyanum Duels et Gilg tea. The method comprises the following steps: (1), spreading fresh Tetrastigma hemsleyanumDuels et Gilg leaves for 10-20 minutes; (2), fixation: deactivating enzymes of the Tetrastigma hemsleyanum Duels et Gilg leaves by adopting a microwave tea fixation drier; (3), flat pressing for shaping: uniformly spreading the Tetrastigma hemsleyanum Duels et Gilg leaves subjected to fixation on a bamboo skin board, and pressing another bamboo skin board on the leaves to enable the cooled Tetrastigma hemsleyanum Duels et Gilg leaves to be shaped; and (4), drying: drying the semi-finished products processed in the step (2) by a microwave tea machine. The Tetrastigma hemsleyanum Duels et Gilg tea is natural green, is bright green in color and light green in grounds, does not contain caffeine, is rich in Tetrastigma hemsleyanum Duels et Gilg flavone, polysaccharide, kaempferol and other ingratiates, can effectively inhibit cancer cell proliferation, promotes cancer cell poptosis, has no toxic or side effects and is easy to absorb and beneficial to health. The Tetrastigma hemsleyanum Duels et Gilg leaves are tender, have less fibers, and can be eaten after being brewed.
Owner:丽水市莲都区绿谷三叶青珍稀植物研究所

Structure of radioactive micro balls and preparation method

The invention relates to the structure of radioactive micro balls and a preparation method. At least one micro ball having isotopes which can radiate beta or gamma-ray is added in a biocompatible substance; and the biocompatible substance represents biological materials and chemical materials which can be used for the clinical cure: biologic glass, biologic ceramics, biologic resin and liposome, etc. The preparation method comprises the steps: 1. activation method: putting phosphorus or yttrium-containing into an irradiation container of an atom reacting device, and irradiating the micro balls with neutron, so that the phosphorus or the yttrium is activated to be radioactive phosphorus (32P) or radioactive yttrium (90Y); and 2. mixing method: mixing isotope (such as 125I and 103Pd) which has radiate beta or gamma- ray with entitative or hollow micro balls, carrying the isotopes into human bodies by taking the micro balls as the carrier of the isotope for the radiotherapy of tumor. The radioactive micro balls have the volume which is in the range of nanometer and micrometer, and can release beta or gamma ray; and the isotope is one or several, has short radiation range, reduces the side effects of the radiotherapy of the tumor, and can be induced into the human bodies by means of local intervention or surgery through blood vessels.
Owner:李树义

Chinese medicinal composition for treating malignant tumor diseases and preparation method thereof

The invention discloses a Chinese medicinal composition and a preparation method and application thereof. The Chinese medicinal composition is prepared from 20 to 40 percent of astragalus extract, 20 to 40 percent of asparagus root extract, 5 to 25 percent of finger citron extract and 15 to 35 percent of American ginseng in percentage by weight. Pharmacological experiments and clinical experiments show that the Chinese medicinal composition provided by the invention has the functions of strengthening body resistance and eliminating evil, nourishing yin and tonifying qi, clearing heat and releasing toxin, eliminating tuberculosis and dissipating stagnation, and mainly treats the symptoms of qi and yin deficiency, qi stagnation, blood stasis, phlegm coagulation, toxin aggregation and the like caused by malignant tumors; when the Chinese medicinal composition is used with radiation therapy and chemical therapy, the Chinese medicinal composition has the effects of increasing efficacy, reducing toxicity and inhibiting growth and transfer of the tumors, can reverse the medicament resistance of tumor cells and promote apoptosis of the tumor cells, and has not obvious toxic or side effect; and meanwhile, the preparation method for the Chinese medicinal composition has the advantages of quality stability and controllability, extraction of high active ingredient content and strong operability, and is suitable for industrialized mass production.
Owner:常熟雷允上制药有限公司

Carbamic acid compounds comprising an ester or ketone linkage as hdac inhibitors

InactiveUS20060058282A1Promote apoptosisInhibiting cell cycle progressionBiocideOrganic chemistryKetoneOxygen
This invention pertains to certain carbamic acid compounds of the formula (I), which inhibit HDAC (histone deacetylase) activity: wherein: J is a linking functional group and is independently: —O—C(═O)— or —C(═O)—O— or —C(═O)—; Cy is a cyclyl group and is independently: C3-20carbocyclyl, C3-20heterocyclyl, or C5-20aryl; and is optionally substituted; Q1 is a cyclyl leader group, and is independently a divalent bidentate group obtained by removing two hydrogen atoms from a ring carbon atom of a saturated monocyclic hydrocarbon having from 4 to 7 ring atoms, or by removing two hydrogen atoms from a ring carbon atom of saturated monocyclic heterocyclic compound having from 4 to 7 ring atoms including 1 nitrogen ring atom or 1 oxygen ring atom; and is optionally substituted; Q2 is an acid leader group, and is independently: C1-8alkylene; and is optionally substituted; or: Q2 is an acid leader group, and is independently: C5-20arylene; C5-20arylene-C1-7alkylene; C1-7alkylene-C5-20arylene; or C1-7alkylene-C5-20arylene-C1-7alkylene; and is optionally substituted; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, 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 HDAC, and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.
Owner:TOPOTARGET UK LTD
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