- DI(HETERO)ARYLCYCLOHEXANE DERIVATIVES, THEIR PREPARATION, THEIR USE AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM
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The present invention relates to di(hetero)arylcyclohexane derivatives of the formula (I), in which Ar1, Ar2, R1 and R2 have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmaceutical active compounds which inhibit ATP-sensitive potassium channels in the heart muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as arrhythmias or a decreased contractility of the heart, such as can occur, for example, in coronary heart disease, cardiac insufficiency or cardiomyopathies. In particular, they are suitable for the prevention of sudden cardiac death. The invention furthermore relates to processes and intermediates for the preparation of the compounds of the formula (I), their use and pharmaceutical compositions comprising them.
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Page/Page column 96
(2009/01/24)
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- A simple and efficient synthesis of (±)-mesembrine
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A simple and efficient synthesis of (±)-mesembrine 1 is described employing double Michael addition and as the key step in 18% overall yield.
- Chavan, Subhash P.,Khobragade, Dushant A.,Pathak, Ashok B.,Kalkote
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p. 5263 - 5265
(2007/10/03)
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- Verapamil analogues with restricted molecular flexibility
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Three analogues with restricted flexibility were designed to study the active conformation of verapamil during interaction with the slow calcium channel. Thus cis- and trans-1-(3,4-dimethoxyphenyl)-4-[N-[2-(3,4-dimethoxyphenyl)ethyl]-N-me thylamino]-r-1-c
- Dei,Romanelli,Scapecchi,Teodori,Chiarini,Gualtieri
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p. 2219 - 2225
(2007/10/02)
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- Bisarylamines
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Compounds of the formula: STR1 and pharmaceutically acceptable salts thereof, wherein: Ar is phenyl, naphthyl, heteroaryl, indole, or fused arylcycloalkyl optionally substituted with hydroxy, halo, CF 3, NO 2, C 1-6 alkyl, C 1-6 alkoxy or aryloxy;A and A'
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- SYNTHESIS OF ALKALOIDS, TORTUOSAMINE, N-FORMYLTORTUOSAMINE, AND RELATED COMPOUND
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Synthesis of alkaloids, tortuosamine, N-formyltortuosamine, and related compound, was accomplished by application of a new method constructing cycloalkenopyridines by thermal rearrangement of oxime O-allyl ethers as a key step
- Koyama, Junko,Sugita, Teruyo,Suzuta, Yukio,Irie, Hiroshi
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p. 969 - 972
(2007/10/02)
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- 4-Amino-4-phenylcyclohexanone ketal compositions and process of use
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A class of new 4-amino-4-arylcyclohexanones, their ketals, and acid addition salts have been synthesized and found to be useful for relieving pain in animals. Their analgesic activity appears to be of high order, and in addition some exhibit narcotic antagonist activity that is useful in modifying the cardiovascular, respiratory, and behavioral depression caused by other analgesics. Several show mixed analgesic and narcotic antagonist activity. Preferred compounds of the class are 4-(m-hydroxyphenyl)-4-dimethylaminocyclohexanone ethylene ketal, and 4-(m-hydroxyphenyl)-4-(n-butylmethylamino)cyclohexanone ethylene ketal as free bases and as their hydrochloride salts. Processes for synthesis and intermediates are described. Unit dosage forms and therapeutic treatments are disclosed.
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- 4-Arylcyclohexylamines
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The invention relates to novel 4-hydroxymethyl(acyloxymethyl and methyl)-4-arylcyclohexylamines embraced by the formula SPC1 Wherein Ar is an aromatic ring selected from the group consisting of phenyl and naphthyl, each of which has from zero through three substituents independently selected from the group consisting of fluorine, chlorine, bromine, lower alkyl of one through three carbon atoms, lower alkoxy of one through three carbon atoms, and lower alkylthio of one through three carbon atoms; Z is selected from the group consisting of hydrogen, hydroxy and lower acyloxy of one through four carbon atoms; ? is a generic expression denoting cis and trans stereoconfiguration and mixtures thereof, with the proviso that when the stereoconfiguration of the linkage connecting the cyclohexane ring and CH2 Z is cis to the amino group, the linkage connecting the cyclohexane and Ar rings is trans, and vice versa; R1 is selected from the group consisting of hydrogen and lower alkyl of one through three carbon atoms; R2 is selected from the group consisting of hydrogen, lower alkyl of one through three carbon atoms, EQU1 WHEREIN N IS 2 THROUGH 5 AND Ar has the same meaning as above; R1 and R2 taken together with --N is a saturated heterocyclic amino radical selected from the group consisting of unsubstituted and substituted pyrrolidino, piperidino, hexamethylenimino, morpholino and piperazino; and pharmacologically acceptable acid addition salts thereof. It also relates to intermediates and processes for the preparation of the aforesaid novel compounds (I) and novel derivatives thereof. The administration to humans and animals of the novel compounds (I) depresses their central nervous systems and lowers their blood pressures.
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