30 results about "Chemoprotective" patented technology

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.

Compounds and a method of synthesis of compounds of formula (Ia) or (Ib): and salts, solvates, and chemically protected forms thereof, wherein the dotted lines indicate the optional presence of a double bond between C1 and C2 or C2 and C3; R² and R³ are independently selected from —H, ═O, ═CH₂, —CN, —R, OR, halo, ═CH—R, O—SO₂—R, CO₂R and COR; R¹⁰ is a carbamate-based nitrogen protecting group; and R¹¹ is an oxygen protecting group.

The present invention pertains to certain alkane diol derivatives (including, e.g., mono- and di-esters) of the formula R¹—O-A-O—R², wherein: A is a C_2-10 alkylene group; R¹ is independently a first hydroxy protecting group (e.g., an ester group); and, R² is independently —H or a second hydroxy protecting group (e.g., an ester group); and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrug thereof, which, inter alia, inhibit osteoclast survival, formation, and/or activity; and/or inhibit bone resorption. 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 osteoclast survival, formation, and/or activity, and to inhibit conditions mediated by osteoclasts and/or characterised by bone resorption, such as osteoporosis, rheumatoid arthritis, cancer associated bone disease, Paget's disease, and the like; and/or conditions associated with inflammation or activation of the immune system.

The present invention pertains to certain pyrazines and pyridines, and derivatives 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: (I) wherein: Q is independently —N═ or —CH═; one of R^P2 and R^P3 is independently a group of the formula -J¹-L¹-Z; wherein: if Q is —N═, then -J¹-L¹-Z is independently: —NH-Z; —O-Z; or S-Z; if Q is —CH═, then -J¹-L¹-Z is independently: —NH—(CH₂)_n-Z, wherein n is independently 0 or 1; —O-Z; or —S-Z; Z is independently: C_6-14 carboaryl, C_5-14 heteroaryl, C_3-12carbocyclic, C_3-12 heterocyclic; and is independently unsubstituted or substituted; the other of R^P2 and R^P3 is independently —H, —NHR^N1, or —NHC(═O)R^N2; wherein: R^N1, if present, is independently —H or aliphatic saturated C_1-4alkyl; R^N2, if present, is independently —H or aliphatic saturated C_1-4alkyl; one of R^P5 and R^P6 is independently a group of the formula —W—Y; wherein: W is independently: a covalent bond; —NR^N4—, —O—, —S—, —C(═O)—, —CH₂—; —NR^N4—CH₂—, —O—CH₂—, —S—CH₂—, —C(═O)—CH₂—, —(CH₂)₂—; —CH₂—NR^N4—, —CH₂—O—, —CH₂—S—, or —CH₂—C(═O)—; wherein R^N4, if present, is independently —H or aliphatic saturated C_1-4alkyl; Y is independently: C_6-14carboaryl, C_5-14heteroaryl, C_3-12carbocyclic, C_3-12heterocyclic; and is independently unsubstituted or substituted; the other of R^P5 and R^P6 is independently —H; 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, e.g., 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.

Compounds of formula (I): A-B-C and isomers, salts, solvates, chemically protected forms, and prodrugs thereof wherein: B is selected from the group consisting of formula (i) where RN is H or Me; or B is a divalent C5 heterocyclic residue containing one or two ring heteroatoms; A is formula (ii) RA3 and RA5 are independently selected from halo, ORO and RAC, where RO is H or Me, and RAC is H or C1-4 alkyl; XA is selected from N and CRA4, where RA4 is selected from H, ORO, CH2OH, CO2H, NHSO2Me and NHCOMe; RA2 and RA6 are independently selected from H, halo and ORO; or RA3 and RA4 together with the carbon atoms to which they are attached, or RA2 and RA3 together with the carbon atoms to which they are attached, may form a C5-6 heterocylic or heteroaromatic ring, containing at least one nitrogen ring atom; where if X is not N, 1 , 2, or 3 of RA2 to RA6 are not H; C is formula (iii) where X is selected from N and CH, Y is selected from N and CH, and Z is selected from N and CRC6; RC3 is selected from H, halo and an optionally substituted N-containing C5-7 heterocyclic group; RC5 is a group selected from formula (iv) which group may be selected by one or two C1-4 alkyl groups or a carboxy group; RC6 is H; or, when X and Y are N, RC5 and RC6 (when Z is CRC6) together with the carbon atoms to which they are attached may form a fused C6 aromatic ring selected from the group consisting of formula (v).

An antioxidizing health-care nutritive liquid is prepared from haw and red sage root and features use of saccharomyces cerevisiae (CGMCC No.0775) for high-purity fermentation. Its advantage is its high health-care actions of removing free radicals of oxygen, regulating internal secretion, lowering blood sugar, blood fat and blood pressure, preventing and treating cardiovascular and cerebrovascular diseases and cancers, delaying senility and beautifying skin.

Compounds of formula (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof one of X1, X2 and X3 is N, and the others are CH; RN1 and RN2 together with the nitrogen atom to which they are attached form a nitrogen-containing heterocyclic ring having from 4 to 8 ring atoms; RN3 and RN4 together with the nitrogen atom to which they are attached form a nitrogen-containing heterocyclic ring having from 4 to 8 ring atoms and their use in treating diseases ameliorated by the inhibition of mTOR.

The present invention is a method for obtaining a formulation of resveratrol and rice bran oil. The resulting product in the form of an oil or solid proves to increase the therapeutic potential of resveratrol by the synergistic action of the components of the rice oil.

The product obtained through the method of the invention is an active principle which, when incorporated in nutraceutical and/or pharmaceutical compositions, provides antioxidant, anti-inflammatory, antiviral, cardioprotective, neuroprotective and/or cancer chemoprotective action, besides protecting against infections and ischemia, reducing obesity, and preventing illnesses of old age.

The present invention relates to a series of phosphoryl-containing steroidal compounds, a preparation method and an application thereof, in particular to the compounds as a formula I, an isomer, pharmaceutically acceptable salts or chemically protected forms thereof, the preparation method thereof, and the application of the compounds in preparation of a medicine for treating cancer-related diseases. The compounds of the present invention have the good activity for inhibiting malignant tumors such as melanoma and prostate cancer.

The present invention describes new biological activities of immunomodulating 6-substituted purinyl compounds which make them particularly useful during the treatment of cancer. Collectively, these new biological activities make these purinyl compounds useful chemoprotective agents for the treatment of myelosuppression which is associated with cancer chemotherapy and/or radiotherapy. This chemoprotective activity is in addition to the immunomodulating and subsequent anticancer activity displayed by these compounds. The chemoprotective usefulness of these compounds is further enhanced by the use of medium-chain fatty acids or salts or triglycerides or mono- or diglycerides in combination with the 6-substituted purinyl compounds of this invention.

The invention provides a structure of a 3beta-hydroxy-ergosta-5-ene steroid compound, and applications of the compound and the pharmaceutically acceptable form of chemical protection or a prodrug in the preparation of drugs capable of preventing or treating LXRbeta related metabolic syndromes. The LXRbeta related metabolic syndromes include hyperlipidemia, atherosclerosis or hypertension. Throughthe discovery of the evaluation of lipid-lowering activity in animal bodies, the compound has obvious effects on lipid lowering, so that the compound has potentials of further developing into a novellipid-lowering drug.

A chemoprotective method for treating, inhibiting or preventing loss of barrier function in skin caused by ultraviolet (UV) light by using an effective amount of pterostilbene is provided. Pharmaceutical and nutraceutical compositions containing pterostilbene suitable for administration to an individual in order to prevent subsequent UV-mediated loss of barrier function in skin are provided.

The present disclosure relates to prodrugs, double prodrugs, derivatives and analogues of 3-(methylamino)-2-((methylamino)methyl)propane-1-thiol. Their use as radio- and chemo-protectors is also described.

Compositions and methods for converting at least one glucosinolate to an isothiocyanate using Bacillus subtilis 839, Bacillus subtilis CO4_4, Pediococcus pentosaceus M3_H01, and/or Pediococcus pentosaceus M2_H12, or active variants thereof, are provided. Conversion of glucosinolates, such as glucoraphanin, to isothiocyanates, such as sulforaphane, leads to the stimulation of the Nrf2/Keap pathway and phase II enzymes, providing chemoprotective and anti-inflammatory effects. Accordingly, provided herein are compositions comprising Bacillus subtilis 839, Bacillus subtilis CO4_4, Pediococcus pentosaceus M3_H01, and/or Pediococcus pentosaceus M2_H12, or active variants thereof, for administration to subjects for increasing isothiocyanate (e.g., sulforaphane) production, increasing the expression of genes regulated by the Nrf2 transcription factor, including phase II enzymes, decreasing inflammation, and treating or preventing an inflammatory disorder or a cancer. The composition can comprise at least one glucosinolate or a plant, plant part or an extract thereof comprising glucosinolate(s).

The present invention relates to a class of xanthine derivatives, pharmaceutically acceptable salts thereof, solvates of said derivatives, solvates of pharmaceutically acceptable salts, chemically protected forms or prodrugs thereof, and preparation methods thereof and Use; also relates to the intermediate compound used to prepare the xanthine derivative and the preparation method of the intermediate compound. The xanthine derivatives and pharmaceutical compositions thereof can effectively inhibit the activity of DPP-IV, and can be used to prepare medicines for diseases related to dipeptidyl peptidase (DPP-IV).