摘要:
It is intended to provide a drug which is efficacious against pathological conditions relating to arginine-vasopressin V1b receptor. More particularly speaking, it is intended to provide a drug which has a therapeutic or preventive effect on depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorders, hypertension, digestive diseases, drug addiction, epilepsy, brain infarction, brain ischemia, brain edema, head injury, inflammation, immune diseases, alopecia and so on. As the results of intensive studies, a novel 1,3-dihydro-2H-indol-2-one compound and a pyrrolidin-2-one compound fused with a heteroaromatic ring, which are highly selective antagonists of arginine-vasopressin V1b receptor, have high metabolic stabilities and show favorable brain penetration and high plasma concentrations, are found, thereby achieving the above objective.
摘要:
The present invention provides a 4-mercaptophenyl ester of acetic acid, which is useful as a raw material for synthesizing a developer, etc., and a process for producing the same. The present invention provides a 4-mercaptophenyl ester of acetic acid represented by Formula (1); wherein Ac is an acetyl group, and R is a C1-4 alkyl group, and a process for producing the 4-mercaptophenyl ester of acetic acid having a step of reducing a 4-halosulfonylphenyl ester of acetic acid represented by Formula (2); wherein Ac is an acetyl group, R is a C1-4 alkyl group, and X is a halogen atom.
摘要:
The invention provides para substituted dialkylphenol derivatives of propofol. The invention further provides pharmaceutical compositions comprising such analogs, methods for preparing such analogs, and methods of using such analogs to induce general anesthesia, sedation, and/or hypnotic or sleep effects in a patient.
摘要:
The invention relates to novel sulphonylamino(thio) carbonyl compounds of the formula (I), in which A represents a single bond, oxygen, sulphur or the group N—R, in which R represents hydrogen, alkyl, alkenyl, alkinyl or cycloalkyl, Q represents oxygen or sulphur, R1 represents hydrogen or formyl or represents in each case optionally substituted alkyl, alkenyl, alkinyl, alkylcarbonyl, alkoxycarbonyl, alkylsulphonyl, cycloalkyl, cycloalkylcarbonyl or cycloalkylsulphonyl, R2 represents cyano or halogen or represents in each case optionally substituted alkyl, alkenyl, alkinyl, alkoxy, alkenyloxy or alkinyloxy, and R3 represents in each case optionally substituted heterocyclyl having 5 ring members of which at least one is oxygen, sulphur or nitrogen and from one to three further ring members can be nitrogen, and salts of compounds of the formula (I), the previously known compounds 4,5-dimethoxy-2-(2,5-dimethoxy-phenylsulphonylaminocarbonyl)-2,4-dihydro-3H-1,2,4-triazol-3-one, 4,5-diethoxy-2-(2,5-dimethoxy-phenylsulphonylaminocarbonyl)-2,4-dihydro-3H-1,2,4-triazol-3-one and N-(2,5-dimethoxy-phenylsulphonyl)-1,5-dimethyl-1H-pyrazole-3-carboxamide being excluded by disclaimer; and also to processes and novel intermediates for the preparation of the novel substances and to their use as herbicides.
摘要:
The present invention provides a monomer having the formula A-B, wherein A is represented by Formula I: 1 wherein B is selected from nullOCFnullCF2 and nullA; wherein, when B isnullOCFnullCF2, the orientation of B is meta or para to the trifluorovinyloxy group of A; wherein, when B is A, the bond joining the A groups is para to the trifluorovinyloxy group of each A; and wherein each Z is independently selected from nullSO2F, nullSO2Cl, nullSO3H, nullSO2nullN(M)nullSO2CF3, and nullSO2nullN(M)nullSO2Rf; wherein M is any suitable cation and Rf is a Cl to CIO fluorocarbon or fluorinated ether group. The present invention also provides a monomer according to Formula II: 2 wherein X is F, Cl, or N(M)SO2Rf, wherein M is any suitable cation and Rf is a C1 to C10 fluorocarbon or fluorinated ether group.
摘要:
The present invention relates to a linker shown by the following formula (I): X—SO2—R1—(A)m—R2 (I) wherein R1 is a group of the formula (A): [wherein R3, R4 and R5 are the same or different hydrogen, etc], etc, R2 is a group which can form a chemical bond to a resin which may be protected by a conventional protective group, A is lower alkylene, etc, X is a leaving group, and m is an integer of 0 or 1, with proviso that A is (C2-C6)alkylene, and m is an integer of 1, when R1 is a group of the formula (A).
摘要:
The present invention provides the new bis-stilbene compounds, which are useful as optical brighteners and correspond to the formulaR.sub.1 -- CH = CH -- X -- CH = CH -- R.sub.2in which X represents a diphenyl residue bound in positions 4 and 4' to the =CH-- groups; R.sub.1 and R.sub.2 independently of each other, each represents a monocyclic benzene residue, a diphenyl, naphthyl or pyridyl residue, and in which at least one of the cyclic systems R.sub.1, R.sub.2, X contains a possibly functionally modified sulphonic acid group, a sulphone group, a possibly functionally modified carboxylic acid group, a nitrile, hydroxyl, mercapto or methyl group.
摘要:
The present disclosure relates to the methods for the preparation of reactive [F-18]fluoride in a form of [F-18]sulfonyl fluoride suitable for efficient radiolabeling without an azeotropic evaporation step by the use of anion exchange resin and sulfonyl chloride, and its applications in the manufacturing of PET radiopharmaceuticals.
摘要:
The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role.