摘要:
This disclosure concerns a new family of phosphorus-containing compounds of Formula (I): and pharmaceutically acceptable derivatives thereof. Compositions containing such compounds and uses thereof are also provided.
摘要:
The present invention relates to compounds which are inhibitors of the activity of Complex III of the mitochondrial electron transport chain and pharmaceutical compositions comprising said compounds alone or in combination with other active agents. The present invention further relates to use of the compounds of the invention as medicaments or as agrochemicals where their properties as inhibitors of the mitochondrial respiration is of benefit. More particularly the present invention relates to the use of the compounds of the invention in a method of treating and/or preventing cancers presenting tumor-initiating cells. (Formula I) (I)
摘要:
The present invention provides inventive conjugated polyethyleneimine (PEI) polymers and conjugated aza-macrocycles (collectively referred to herein as “conjugated lipomers” or “lipomers”) containing one or more groups of the formula (iii): wherein R3 and R4 are as defined herein. Also provided are compositions comprising the inventive conjugated lipomers, and methods of preparation and use.
摘要:
To provide a solid-liquid palladium ion adsorbent which has both extraction performance and selectivity of a liquid-liquid palladium extracting agent in a conventional solvent extraction method and which does not require use of an organic solvent, and methods for selectively separating and recovering palladium, using it.Palladium is selectively separated and recovered by using a palladium ion adsorbent comprising an amide-containing cyclic sulfide compound represented by the following formula (1) or (2), or a palladium ion adsorbent having the amide-containing cyclic sulfide compound represented by the following formula (1) or (2) fixed on a carrier: wherein R is each independently a hydrogen atom, a methyl group, an ethyl group, a C3-30 linear or branched chain hydrocarbon group, a C3-10 alicyclic hydrocarbon group or a C6-14 aromatic hydrocarbon group, m is an integer of 1 or 2, n is each independently an integer of from 1 to 12, and L is each independently a methylene group, an ethylene group, a C3-8 alkylene group or a C6-14 arylene group; wherein R is each independently a hydrogen atom, a methyl group, an ethyl group, a C3-30 linear or branched chain hydrocarbon group, a C3-10 alicyclic hydrocarbon group or a C6-14 aromatic hydrocarbon group, n is each independently an integer of from 1 to 4, and L is each independently a methylene group, an ethylene group, a C3-8 alkylene group or a C6-14 arylene group.
摘要:
Disclosed herein are macrocyclic compounds that are effective to inhibit cell migration. In one embodiment, the compounds have the structure: or any pharmaceutically acceptable salt or solvate thereof, wherein: m is 0 or 1; R1, R2 and R3 independently are H, aralkyl, acyl, lower alkyl or silyl; X is —C(O)N(R4)— or —C(S)N(R4)—; —C(O)—; —C(S)—; Y is —OC(O)—; —OC(O)N(R5)—; —N(R5)C(O)—; or —OC(O)O—; G comprises a saturated or unsaturated aliphatic chain having from 2 to about 10 atoms in the chain, the chain optionally including 1, 2, or 3 heteroatoms; the chain optionally being substituted with 1, 2 or 3 substituents independently selected from lower alkyl, —OR6, epoxy, aziridinyl, cyclopropyl, —NR7R8 and halo; R4, R5, R6, R7 and R8 independently are selected from H, lower alkyl and acyl. Also disclosed are methods for making and using compounds as well as pharmaceutical compositions including one or more of the disclosed macrocycles.
摘要:
Rapalogs of formula I, pharmaceutically acceptable salts, pharmaceutical compositions, and preparation methods and uses thereof. The rapalogs have the structure of formula I and can be used as an anti-tumor medicament. Comparing with rapamycin, the rapalogs of the present invention exhibit enhanced water solubility, and improved pharmacological and pharmacokinetic properties by introducing a hydrophilic and polar group such as a hydroxyl.
摘要:
Novel terpenes and macrocycles are activators of TGR5 and can be used for the prevention and/or treatment of Diabetes Type 2, obesity, neuropathy and/or nephropathy.
摘要:
The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要:
The present invention is directed to compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the beta-secretase enzyme in involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the beta-secretase enzyme is involved.
摘要:
New derivatives of FK 506 are disclosed. These new derivatives and other derivatives that are useful for determining the levels of FK 506 in a sample are also provided as are assay procedures and kits for use in determining the levels of FK 506 or other macrophilin binding substances in blood, particularly un-extracted blood in the presence of specific binding proteins for FK 506.