摘要:
Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and anti-pruritic agents are provided.The compound of formula I, having the structure: ##STR1## wherein R.sub.1, R.sub.2 ;X; and ArY, Z and n are as described in the specification.
摘要翻译:提供了具有κ阿片样物质激动剂活性的化合物,含有它们的组合物和使用它们作为止痛剂和抗瘙痒剂的方法。 具有以下结构的式I化合物:其中R1,R2; X; Ar Y,Z和n如说明书中所述。
摘要:
Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and anti-pruritic agents are provided. The compound of formulae IIA, having the structure: ##STR1## wherein R.sub.1, R.sub.2 ;X.sub.4, X.sub.5 ; andAr and n are as described in the specification.
摘要:
Anti-pruritic pharmaceutical formulations containing kappa agonist compounds and methods of prevention or treatment of pruritus in a mammal with the anti-pruritic formulations.
摘要:
Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided. The compound of formula II has the structure: ##STR1## wherein X.sub.4, X.sub.5 ; R.sub.1, R.sub.2 ; and Ar and n are as described in the specification.
摘要:
4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl heterocyclic carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with either a heterocyclic carboxylic acid in the presence of an acid-acceptor or the alkali metal salt of a heterocyclic carboxylic acid.
摘要:
Substituted N-cycloalkylmethyl-1H-pyrazolo[3,4-b]quinolin-4-amines, pharmaceutical compositions containing them and methods for a) effecting c-GMP-phosphodiesterase inhibition, b) treating heart failure and/or hypertension, c) reversing or reducing nitrate-induced tolerance and d) treating angina pectoris, congestive heart disease and myocardial infarction utilizing them.
摘要:
A garbled circuit is generated for a client in a leakage-resilient manner with a reduced memory requirement. The garbled circuit is used for secure function evaluation between the client and a server. The garbled circuit is generated with a reduced storage requirement by obtaining a token from the server; querying the token gate-by-gate, wherein for each gate of the garbled circuit, the token generates new wire garblings and stores them with the client using a Stream Cipher and interacts with the leakage-protected area to generate a garbled table for the gate; and receiving the garbled circuit from the token. The token comprises a leakage-protected area. The Stream Cipher is leakage-resilient and can be a symmetric-key cryptographic primitive that has a secret key as an input and generates an unbounded stream of pseudorandom bits as an output. The number of evaluations of the Stream Cipher is kept to a substantial minimum. For example, the Stream Cipher can execute with a same key only twice, such as only once for an encryption and only once for a decryption.
摘要:
A garbled circuit is generated for a client in a leakage-resilient manner with a reduced memory requirement. The garbled circuit is used for secure function evaluation between the client and a server. The garbled circuit is generated with a reduced storage requirement by obtaining a token from the server; querying the token gate-by-gate, wherein for each gate of the garbled circuit, the token generates new wire garblings and stores them with the client using a Stream Cipher and interacts with the leakage-protected area to generate a garbled table for the gate; and receiving the garbled circuit from the token. The token comprises a leakage-protected area. The Stream Cipher is leakage-resilient and can be a symmetric-key cryptographic primitive that has a secret key as an input and generates an unbounded stream of pseudorandom bits as an output. The number of evaluations of the Stream Cipher is kept to a substantial minimum.
摘要:
Solid dispersions of stable, amorphous opioid antagonists, particularly [[2(S)-[[4(R)-(3-hydroxyphenyl)-3(R),4-dimethyl-piperidinyl]methyl]-1-oxo-3-phenylpropyl]amino]acetic acid, with improved water solubility and bioavailability are disclosed. Also disclosed are methods of preventing or treating a side effect associated with an opioid. In addition, methods of treating or preventing pain, ileus, and opioid bowel dysfunction are disclosed.
摘要:
Methods for prevention or treatment of pruritus are provided. The methods comprise administering to a patient an effective amount of a kappa opioid receptor agonist compound. The involved kappa opioid receptor agonist compounds are of the type represented by the following formula III wherein R1, R2, Ar, X7, and n are as defied in the specification.