摘要:
The present invention relates to highly pure and crystalline compounds as starting materials and intermediates to make maralixibat and the processes of making highly pure maralixibat. The invention also relates to an amorphous form of maralixibat.
摘要:
Compounds of the formula ##STR1## in which X is --S--, --SO-- or --SO.sub.2 --; R.sup.1 is C.sub.7-10 -alkyl or C.sub.7-10 -alkoxy; R.sup.2 is a residue of the formula ##STR2## R.sup.3 is carboxy or lower-alkoxycarbonyl; and n is an integer of 1, 2 or 3; and salts of carboxylic acids of formula I can be used for the treatment of autoimmune diseases and diseases having a strong immunological component, such as psoriasis.
摘要翻译:其中X是-S-,-SO-或-SO 2 - 的式I的化合物; R1是C7-10-烷基或C7-10-烷氧基; R 2是下式的残基:R 3是羧基或低级烷氧基羰基; n为1,2或3的整数; 式I的羧酸盐可用于治疗具有强免疫组分的自身免疫性疾病和疾病,例如牛皮癣。
摘要:
A novel process for the production of compounds of the formula ##STR1## wherein A and A.sub.1, independently of one another, denote phenyl, naphthyl, diphenylyl, 2-phenyl-1,2,3-triazol-4-yl or pyridyl, it being possible for A and A.sub.1 to contain non-chromophoric substituents, and D denotes 4,4'-diphenylylene,1,5- or 2,6-naphthylene, or a 9,10-dihydrophenanthrene or dibenzofurane radical which is bonded to the vinylene groups in the 2,7-position, which comprises reacting in a first stage a compound of the formulaX-CH.sub.2 -D-CH.sub.2 -X (II)wherein X denotes halogen, especially chlorine or bromine, hydroxyl or a group ##STR2## wherein X.sub.1 represents an aliphatic cycloaliphatic or aromatic hydrocarbon radical, especially alkyl having 1 to 6 carbon atoms, or phenyl, and D has the indicated meaning, in a strongly acid medium, in a molar ratio of at least 1:2, with an organic sulphide containing 5 to 8 ring members, of the formula ##STR3## wherein B represents a polymethylene group of 4 to 7 methylene groups and wherein one of these methylene groups can be replaced by a hetero-atom and wherein these methylene groups can also contain alkyl groups with 1 to 4 carbon atoms as substituents, to give a sulphonium salt of the formula ##STR4## wherein M represents the anion of the strong acid used and n denotes the numbers 1 or 2; reacting, in a second stage, the resulting sulphonium salt with 2 mols of an aldehyde of the formula(V) A-CHOor (VI) A.sub.1 -CHOor their mixture, in the presence of strong bases, in a strongly polar, protic or aprotic, water-miscible solvent to give a diepoxide of the formula ##STR5## and subjecting in a 3rd stage, the diepoxide of the formula (VII), thus obtained, to a reduction according to processes which are in themselves known for the reduction of epoxides, with elimination of the epoxide oxygen and formation of vinylene groups.
摘要:
The application discloses a process for the preparation of 5-deoxy-L-arabinose of formula (VI); comprising the conversion of a compound of formula (XII); wherein n is 0, 1 or 2; which can be used as intermediate for the synthesis of sapropterin.
摘要:
Tri- and tetra substituted thiepane compositions having use as immunogens, therapeutics, diagnostics and for other industrial purposes are disclosed. The compositions inhibit proteolytic activity of viral enzymes and are useful for the inhibition of such enzymes as well as in assays for the detection of such enzymes. Embodiments in which antigenic polypeptides are bonded to the compositions are useful in raising antibodies against the thiepane haptens or the polypeptide. Labeled thiepanes of this invention are useful as diagnostic reagents.
摘要:
This invention relates to thioformamide derivatives of the formula: ##STR1## wherein R represents alkyl, Ar represents optionally substituted phenyl, Y represents an ethylene or methylene radical or a valency bond, and n represents 0 or 1, bioprecursors thereof and pharmaceutically acceptable salts thereof which possess useful pharmacological properties, processes for their preparation and compositions containing them.
摘要:
Pesticidally active 3-(N-alkylcarbamyloximino)-saturated heterocyclic compounds have been prepared. These compounds are useful in combating undesirable pests such as insects, acarids, nematodes, viruses, and the like.
摘要:
THIOLACTONES HAVE BEEN PREPARED BY CONTACTING LACTONES IN THE VAPOR PHASE WITH A SULFUR CONTAINING DONOR OVER A LEWIS BASE IN AN INERT ATMOSPHERE AT A TEMPERATURE OF ABOUT 150 TO 350*C.
摘要:
The present invention pertains to novel thiocycloheptyne derivatives of general formula (I): and in particular to thiacycloalkynesulfoimine derivatives and their synthesis. The invention also relates to the use of the novel thiocycloheptyne derivatives in coupling reactions with linkers and drugs. The invention further relates to the use of the novel thiocycloheptynes in bioorthogonal (copper-free) click reactions. The invention further pertains to the use of the novel thiocycloheptyne derivatives in the generation of advanced multifunctional drug delivery systems (drug-loaded) nanoparticles.