摘要:
The invention concerns a saturated or unsaturated abietane derivative of general formula (I) wherein: Z is selected among -COOR?5, -CONR1R2¿, -COONR?3R4, -COR6¿, -CON, -COOR5, -CHOHR?7, -SR8, -OR8¿, -CN, -CNO, -CNS, -NCO, -NCS, -R1R2CR9; wherein R?1, R2, R3 and R4¿ represent a hydrogen atom, a C¿1?-C10 alkyl, a C6-C20 aryl optionally substituted; a C7-C10 alkene; a C1-C10 alkyne; an aminoacyl or peptidyl optionally substituted; or R?1 and R2 or R3 and R4¿ together can form a cycle or a heterocycle; R5 represents a hydrogen, a C¿1?-C10 alkyl, a C1-C10 alkene, a C1-C10 alkyne; an aryl, optionally substituted into C6-C20; R?6¿ represents a hydrogen, a halogen, a C¿1?-C10 alkyl, a C1-C10 alkene, a C1-C10 alkyne, an aryl optionally substituted into C6-C20; R?7¿ represents a hydrogen, a C¿1?-C10 alkyl, a C1-C10 alkene, a C1-C10 alkyne; R?8¿ represents a hydrogen, a C¿1?-C10 alkyl, a C1-C10 alkene, a C1-C10 alkyne; and R?9¿ is selected among -CN, -CNO, -CNS, -NCO, and -NCS. The invention also concerns a derived conjugate and the use of said derivative and said conjugate in a diagnostic composition, a reagent and a device.
摘要:
Provided herein are compounds of the formula (I), as well as pharmaceutically acceptable salts thereof, wherein R1, R2, R2´, R3, R4, R5 and X are as defined in the specification and claims. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.
摘要:
Phenylalanine derivatives of the following formula and analogues thereof have an antagonistic activity to α 4 β 7 integrin and a selectivity toward α 4 β 1 integrin. They are used as therapeutic agents for various diseases to which α 4 β 7 integrin relates.
摘要:
A fused benzeneoxyacetic acid derivative of the formula (I):
(wherein
or
A is -COW, -NR 4 -Y or -Z-NR 4 CONR2R3; W is -NR 2 R 3 , -NR 4 -OR 5 , -NR 4 -NR 2 R 3 or -NR 4 -N=CR 2 R 3 ; Y is -CO-R 5 , -CO-U-NR 2 R 3 or -CS-U-NR 2 R 3 ; Z is -CH=N- or -CH 2 -NR 6 -; R 1 is H or alkyl; R 2 or R 3 is H, (benzoyl)phenyl or R 5 ; R 5 is phenyl, hetero ring containing N atom or alkyl substituted by hetero ring containing one N atom or phenyl; R 4 or R 6 is H, alkyl or (substituent)phenyl; U is bond or alkylene; e is 3-5; f is 1-3; p or r is 0-4; q is 0-2; s is 0-3) and salts thereof possess an agonistic on PGl 2 receptor, so it is useful for prevention and/or treatment of thrombosis, arteriosclerosis, ischemic heart diseases, gastric ulcer and hypertention.
摘要翻译:式(I)的稠合苯氧基乙酸衍生物:(其中CHEM> A是-COW,-NR 4 -Y或-Z-NR 4 -CONR 2 R 3; W是-NR 2 R 3,-NR 4 -OR 5,-NR 4 -NR 2 R 3或-NR 4 -N = CR 2 R 3,Y是-CO-R 5,-CO-U-NR 2 R 3或-CS-U-NR 2 R 3; Z是-CH = N- 或-CH 2 -NR 6 - ; R 1是H或烷基; R 2或R 3是H,(苯甲酰基)苯基或R 5; R 5是苯基,杂环 含有N原子或被含有一个N原子或苯基的杂环取代的烷基; R 4或R 6是H,烷基或(取代)苯基; U是键或亚烷基; e是3-5; f是1 -3; p或r为0-4; q为0-2; s为0-3>,其盐对PG1受体具有激动作用,因此可用于预防和/或治疗血栓形成,动脉硬化,缺血性心脏 疾病,胃溃疡和高血压。
摘要:
A phenylalanine derivative of formula (1-1) or analogues thereof exhibit an α4β7 integrin inhibiting activity and selectivity for α4β1 integrin, thus being useful as remedies for various diseases related to α4β7 integrin.
摘要:
A coupling agent useful in conducting immunoassays, particularly assays for B12, is disclosed. The coupling agent has formula (I) where Z and Z' can be the same or different, and each is H2NHN, ICH2, (a) or (b); k, m and n are integers from 1 to 10, X is an alkylene group, a cycloalkylene group, an alkylcycloalkylene group, a bivalent aromatic group, or an aminoalkylene group, R and R' can be the same or different, and each is a substituted or unsubstituted aminoalkylene group having from 1 to 10 carbon atoms or a cycloalkylene or alkylcycloalkylene group having from 5 to 20 carbon atoms. Z and Z' are the same except that they can be the same or different when both are (c). A method for purifying an aqueous intrinsic factor solution which contains R-protein is disclosed. The method involves adding to the intrinsic factor solution an amount of cobinamide sufficient to bind substantially all of the R-protein in the solution and an amount of an intrinsic factor affinity resin sufficient to bind the intrinsic factor in the solution, washing the bound cobinamide and the R-protein from the resin, eluting the intrinsic factor from the resin, and dialyzing the eluted intrinsic factor. The purified intrinsic factor can contain less than 0.004 percent cross reactivity with cobinamides, and at least 95 percent of the proteins in the purified material can bind cobalamins. A conjugate where microparticles and the purified intrinsic factor are conjugated by a moiety from one of the foregoing coupling agents is also disclosed, as is a kit for conducting an assay for cobalamins which includes the conjugate of microparticles and purified intrinsic factor. A method for conducting an assay for cobalamins, which method involves the use of the conjugate of microparticles and purified intrinsic factor is also disclosed.