摘要:
Combinatorial libraries are disclosed which are represented by Formula I: ##STR1## wherein: ##STR2## is a solid support; T'--L-- is an identifier residue; and --L'--II' is a ligand/linker residue. These libraries contain dihydrobenzopyrans of the formula ##STR3## which interact (i.e., as agonists or antagonists) with .alpha. adrenergic receptors, dopamine receptors, .sigma.-opiate receptors, and K.sup.+ channels and are inhibitors of carbonic anhydrase isozymes. They are useful in the treatment of ocular diseases such as glaucoma.
摘要:
A special effect apparatus temporally enlarges an input video signal so as to reduce edge intrusion caused by a type of special effect processing and to eliminate color fading due to different sampling frequencies for the luminance and chrominance components of a video signal. The temporally enlarged video signal is formed by sequential selection among three signals: a reference video signal, a preceding video signal which temporally leads the reference video signal and a trailing video signal which temporally lags the reference video signal. Portions of the preceding and trailing video signals are appended to the reference video signal to produce the temporally enlarged video signal which can be processed to create a special effect devoid of edge intrusion.
摘要:
The present invention relates to a novel class of substituted spirocyclic compounds, represented by the following structural Formula: I Wherein A, B and D are independently selected from CR12, NR1a, C(O) and O; E is selected from a bond, CR12, NR1a, C(O) and O; wherein at least one of A, B, D or E is CR12; and provided that when A is O, then E is not O; G is CR12; R is selected from NH2 and OH; These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing termin differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo.
摘要:
The invention relates to compounds (I) for treating diseases of the central and peripheral nervous system, including enantiomers, racemates and acid addition and quaternary salts, ##STR1## wherein Q is selected from two H atoms, (CH.sub.2).sub.m and C(CH.sub.3).sub.2 where m is 1, 2 or 3 and n and p are; each independently 0, 1, 2 or 3, provided that n+p=1-3, and R.sup.0 is H, methyl or OH; the moiety ##STR2## R is selected from H, NH.sub.2, NH-C.sub.1-6 -alkyl, N(C.sub.1-6 -alkyl).sub.2, C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl, C.sub.2-6 -alkynyl, C.sub.3-7 - cycloalkyl, C.sub.1-6 -alkyl substituted by 1-6 halogen atoms, hydroxy- C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, C.sub.1-6 -alkylthio, C.sub.1-6 -alkoxy-C.sub.1-6 -alkyl, carboxy-C.sub.1-6 -alkyl, (C.sub.1-6 -alkoxy)carbonyl-C.sub.1-6 -alkyl, amino-C.sub.1-6 -alkyl, mono-(C.sub.1-6 -alkyl)amino-C.sub.1-6 -alkyl, di-(C.sub.1-6 -alkyl)amino-C.sub.1-6 -alkyl, 2-oxo-pyrrolidin-1-yl-methyl, aryl, diarylmethylol, and C.sub.1-6 -alkyl substituted by one or two aryl groups; R' is independently selected from the group from which R is selected and C.sub.1-6 -alkanoyl and arylcarbonyl; and aryl denotes unsubstituted phenyl or phenyl substituted by 1-3 substituents selected from halogen, C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy and CF.sub.3, subject to certain provisos.
摘要:
Heterocyclic spiro compounds represented by the following general formula and salts thereof: ##STR1## The above compounds act upon muscarinic acetylcholine receptors, thereby activating the acetylcholine nervous functions in the central nervous system.
摘要:
The present invention provides a spiro-azabicyclic compound or a salt or prodrug thereof, said compound comprising a saturated or unsaturated 5-membered heterocyclic ring containing two heteroatoms selected from oxygen, nitrogen and sulphur, no more than one of said heteroatoms being nitrogen; said heterocyclic ring having a spiro attachment to an optionally substituted azabicyclo[2.2.1]heptane or azabicyclo[3.2.1]octane ring system; which compounds are useful for the treatment of neurological and mental disorders.
摘要:
The present invention accordingly provides in one aspect, novel spiro-oxathiolane/quinuclidine compounds corresponding with the schematic structural formula (I) ##STR1## and geometrical isomers, enantiomers, diastereoisomers, racemates and acid addition salts thereof, wherein one of Y and Z is 0 and the other is S(.dbd.O).sub.n ; n is 0, 1 or 2; R' and R" are each selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, aminoalkyl, C.sub.3-7 cycloalkyl, aryl, diarylmethylol, and alkyl substituted by at least one aryl group, provided that at least R' and R" is other than hydrogen; and each X is hydrogen, or when Y is 0 and Z is S(.dbd.O).sub.n simultaneously, then each X may also be selected from the group consisting of deuterium and tritium, and provided further that when each X is hydrogen, Y is 0 and Z is S simultaneously, then at least one of R' and R" is selected from the group consisting of alkenyl, alkynyl, cyclopropyl, cyclobutyl, cycloheptyl, hydroxyalkyl and aminoalkyl.
摘要:
An industrially acceptable process for the preparation and purification of cis-2-methylspiro(1,3-oxathiolane-5,3′)quiniclidine from a cisitrans mixture of isomers. Treatment of the mixture with an organic sulfonice acid generates a less soluble acid addition salt that is enriched in the cis-isomer. Recrystallization or pulping using various organic solvents allows for enrichment of the cis-isomer by filtration. These new sulfonic acid salts of the cis-isomer of 2-methylspiro(1,3-oxathiolane-5,3′)quiniclidine prepared according to the present invention could be further converted into the hydrochloride salt by any known procedures such as treatment with a base and then hydrochloric acid salt formation or exchange of the sulfonic acid salt with hydrochloric acid.
摘要:
The present invention is directed to compounds having the formula (I): useful in treating inflammatory and immune diseases, in which K and L are independently, O or S; Q is —C(═O)— or optionally substituted C1-6alkylene; Ar is optionally-substituted aryl or heteroaryl; J1, J2, J3 and Y are selected so that ring A is a five-to-six membered optionally-substituted cycloalkenyl or heterocyclo ring having 0 to 2 nitrogen heteroatoms; R1 is N or C(R9); and R2, and R3, are as defined in the specification.
摘要:
Heterocyclic spiro compounds represented by the following general formula and salts thereof ##STR1## The above compounds act upon muscarinic acetylcholine receptors, thereby activating the acetylcholine nervous functions in the central nervous system.