摘要:
The invention relates to compounds of formula: and to solvates and/or hydrates thereof, with affinity for and selectivity towards the V1b receptors or both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to a process for preparing them, to the intermediate compounds of formula (II) which are useful for preparing them, to pharmaceutical compositions containing them and to their use for preparing medicinal products.
摘要翻译:本发明涉及以下化合物:并且对V 1 B 1 N 2受体具有亲和力和选择性,并且对V 1b和V N 2 >精氨酸 - 加压素受体1a> 1a。 本发明还涉及制备它们的方法,可用于制备它们的式(II)中间体化合物,含有它们的药物组合物及其用于制备药用产品的用途。
摘要:
A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a mammal in need thereof of an effective amount of a compound of the formula (I) and/or a physiologically acceptable derivative thereof, wherein the substituents have the meaning given in the description. Disclosed are also novel compounds of formula (I) and processes for their preparation.
摘要:
This invention relates to novel diazabicyclic biaryl derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
摘要:
The present invention relates to a compound formula [I] wherein R1 and R5 are each independently hydrogen, halogen, lower alkyl, etc., R2 is hydrogen or an amino protective group, x is bond, -o-o, —O—CH2—, etc., y is in which Z is bond, —O—(CH2)m— (in which m is 1 to 4), etc., R3 is lower alkanoyl, carboxy, lower alkoxycarbonyl, etc., and R4 is hydrogen, halogen, hydroxy, phenoxy, lower alkyl, lower alkoxy, etc., and n is 0, 1 or 2, or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.
摘要:
Compounds of formula in free or salt or solvate form, where Ar is a group of formula Y is carbon or nitrogen and R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n, p, q and r are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of obstructive or inflammatory airways diseases.
摘要:
Compositions and methods for inhibiting and controlling the growth of microbes are disclosed. The composition comprises at least one chemically-modified peptide with antimicrobial activity and at least one carrier. The method comprises of administering an amount, effective for the prevention, inhibition and termination of microbial growth for industrial, pharmaceutical, household and personal care use.
摘要:
A hydroxyeicosenoic acid analog represented by the following Formula (I), the bond ≡ represents a cis-vinylene group or an ethynylene group; Y represents CH2, O or S(O)p wherein p is 0, 1 or 2; m represents an integer of 1 to 4 inclusive; n represents an integer of 0 to 3 inclusive; the sum of m and n is an integer of 3 to 7 inclusive; R1 represents a C1-4 alkyl group or a C3-8 cycloalkyl group; R2 represents a hydrogen atom or a methyl group; R3 represents COR4, a nitrile group, a halogen atom, a tetrazole group or a thiazolidinedione group; R4 represents OR6, NHR6, N(OH)R6, NHSO2R5, glycerol or functionalized glycerols; R5 represents a C1-15 alkyl group, a C6-10 aryl group or a C7-14 aryl group substituted with alkyl groups, halogens or amino groups; R6 represents a hydrogen, a C1-10 alkyl group or a C1-10 alkyl group substituted with a hydroxyl group, or a pharmaceutically acceptable salt or hydrate thereof. The compounds of the present invention are useful as an elastase release inhibitor.
摘要翻译:由下式(I)表示的羟基二十碳烯酸类似物,键=表示顺式亚乙烯基或亚乙炔基; Y表示CH 2,O或S(O)p,其中p为0,1或2; m表示1〜4的整数, n表示0〜3的整数, m和n的和为3〜7的整数, R 1表示C 1-4烷基或C 3-8环烷基; R 2表示氢原子或甲基; R 3表示COR 4,腈基,卤素原子,四唑基或噻唑烷二酮基; R 4表示OR 6,NHR 6,N(OH)R 6,NHSO 2 R 5,甘油或官能化甘油; R 5代表C1-15烷基,C6-10芳基或被烷基,卤素或氨基取代的C7-14芳基; R 6表示氢,C 1-10烷基或被羟基取代的C 1-10烷基,或其药学上可接受的盐或水合物。 本发明的化合物可用作弹性蛋白酶释放抑制剂。
摘要:
This invention relates to compounds which are generally CRF-1 receptor antagonists and which are represented by Formula I or Formula II: wherein Ar is optionally substituted aryl or heteroaryl, R1-R4 are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts thereof. The invention further relates to processes for preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods for their use as therapeutic agents.
摘要:
Novel phenethyl-5-bromopyridylthiourea (PBT) and dihydroalkoxybenzyloxopyrimidine (DABO) derivatives exhibiting spermicidal activity as well as anti-viral activity. These novel compounds can be incorporated within contraceptive compositions to provide for spermicidal or sperm-immobilizing activity.
摘要:
The present invention teaches a composition comprising a .beta.-adrenergic agonist in a bioadhesive carrier. Preferably, the composition comprises terbutaline in polycarbophil. The present invention additionally teaches the local administration of a .beta.-adrenergic agonist for the purpose of treating or preventing dysmenorrhea or premature labor. Using this composition and the method of treatment provides sufficient local levels of the drug to provide therapeutic efficacy, but avoids many untoward adverse events.