- NEW HETEROCYCLIC COMPOUNDS
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The invention provides new heterocyclic compounds having the general formula (IA) wherein A, L, X, Y, m, n, R1 and R2 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.
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Page/Page column 67; 72-73
(2019/06/17)
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- Substituted heterocyclic compounds and application of same to medicines
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The invention relates to substituted heterocyclic compounds and application of the same to medicines and specifically provides the novel substituted heterocyclic compounds or stereoisomers, tautomers, nitrogen oxides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof, and preparation methods thereof. The invention also relates to pharmaceutical compositions containing the compounds and application of the compounds or pharmaceutical compositions to treatment of diseases related to 5-HT6 receptors, especially Alzheimer's disease.
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Paragraph 0201; 0211; 0212; 0213; 0214; 0339; 0340-0342
(2017/04/29)
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- Substituted heterocyclic compounds and its application on the medicament (by machine translation)
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The invention relates to substituted heterocyclic compounds and its application on the medicament, in particular to a novel class of substituted heterocyclic compounds or its isomer, tautomer, nitrogen oxide, hydrate, solvate, metabolite, pharmaceutically acceptable salt or prodrug, and their method of preparation. The invention also relates to the compounds of the invention pharmaceutical composition, and said compound or pharmaceutical compositions for the treatment5-HT6receptor-related diseases, in particular Alzheimer's disease in the use thereof. (by machine translation)
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Paragraph 0200; 0201; 0202; 0203; 0292; 0293; 0294; 0295
(2017/06/02)
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- 3-PIPERIDIN-4-YL-INDOLE ORL-1 RECEPTOR MODULATORS
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The present invention is directed to novel 3-piperidin-4-yl-indole derivatives of formula (I) and forms thereof, wherein X, R1, R2, R3, R4 and R5 are as herein defined, pharmaceutical compositions thereof and use as ORL-1 receptor modulators for treating, preventing or ameliorating ORL-1 receptor mediated disorders and conditions.
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Page/Page column 49
(2008/06/13)
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- INDOLYLPIPERIDINE DERIVATIVES AS ANTIHISTAMINIC AND ANTIALLERGIC AGENTS
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The invention relates to indolyl piperidinyl derivatives of formula (I) wherein: A1 represents an alkylene, alkyleneoxy, alkylenethio, alkanoylene or hydroxyalkylene group; A2 represents an alkylene, alkyleneoxy, alkylenethio, alkanoylene or an alkyleneoxyalkylene group; W1 represents a phenylene, furanylene or pyridinylene group which is unsubstituted or substituted by one or more halogen atoms, alkoxy groups and/or alkyl groups; W2 represents a 3-10 membered monocyclic or bicyclic group containing from 1 to 3 heteroatoms said group being unsubstituted or substituted by one or more halogen atoms, alkyl groups, alkoxy groups and/or oxo groups; R1 represents a hydrogen or halogen atom or an alkyl, alkoxy or methylamino group; and R2 represents a carboxyl group; and pharmaceutically acceptable salts thereof; to processes for their preparation; to pharmaceutical compositions containing them; and to their medical use as antihistaminic and antiallergic agents.
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- Synthesis and structure-activity relationships of novel histamine H 1 antagonists: Indolylpiperidinyl benzoic acid derivatives
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A series of indolylpiperidinyl derivatives were prepared and evaluated for their activity as histamine H1 antagonists. Structure-activity relationship studies were directed toward improving in vivo activity and pharmacokinetic profile of our first lead (1). Substitution of fluorine in position 6 on the indolyl ring led to higher in vivo activity in the inhibition of histamine-induced cutaneous vascular permeability assay but lower selectivity toward 5HT2 receptor. Extensive optimization was carried out within this series and a number of histamine H1 antagonists showing potency and long duration of action in vivo and low brain penetration or cardiotoxic potential were identified. Within this novel series, indolylpiperidines 15, 20, 48, 51 and 52 exhibited a long half-life in rat and have been selected for further preclinical evaluation.
- Fonquerna, Silvia,Miralpeix, Montse,Pagès, Lluís,Puig, Carles,Cardús, Arantxa,Antón, Francisca,Cárdenas, álvaro,Vilella, Dolors,Aparici, Mónica,Calaf, Elena,Prieto, José,Gras, Jordi,Huerta, Josep M.,Warrellow, Graham,Beleta, Jorge,Ryder, Hamish
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p. 6326 - 6337
(2007/10/03)
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- α1b-adrenergic receptor antagonists
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There are provided compounds represented by the general formula (I): [wherein Ar is indole etc., R1is hydrogen etc., B is bond, or B—N—R1forms a ring structure and is piperidine etc., n is 0, 1, etc., A is trimethylene, butylene, etc., Q is piperidine, isoindoline, etc.], or pharmacologically acceptable acid addition salts thereof, and α1B adrenoceptor antagonists composed of these substances. The invented compounds are antagonists having high affinity for α1B adrenoceptor and are useful as pharmaceutical agents for use in prophylaxis/therapy of diseases (e.g., hypertension) in which α1B adrenoceptor is involved or as pharmacological tools for elucidation of physiological activities mediated by α1B adrenoceptor.
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Page/Page column 74
(2010/11/30)
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- NEW INDOLYLPIPERIDINE DERIVATIVES AS POTENT ANTIHISTAMINIC AND ANTIALLERGIC AGENTS
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This invention is directed to new potent and selective antagonists of H1 histamine receptors having the general formula (I) to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy as antiallergic agents.
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- Studies toward the discovery of the next generation of antidepressants. Part 2: Incorporating a 5-HT1A antagonist component into a class of serotonin reuptake inhibitors
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The design and synthesis of a novel series of indole derivatives (9) having dual 5-HT transporter reuptake and 5-HT1A antagonist activity are described.
- Mewshaw, Richard E.,Meagher, Kristin L.,Zhou, Ping,Zhou, Dahui,Shi, Xiaojie,Scerni, Rosemary,Smith, Deborah,Schechter, Lee E.,Andree, Terrance H.
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p. 307 - 310
(2007/10/03)
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- Novel chemoselective reduction of the tetrahydro-4-pyridyl versus indole moiety governed by electron donation: First X-ray evidence for indolopiperidyl-borane complexation
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A series of amino-borane complexes of structure type 2 are the key intermediates in the preparation of 3-(piperidyl) indole derivatives. The selective reduction of the tetrahydro-4-pyridyl double bond via 2 under strongly acidic conditions is feasible only when the pyridyl double bond is conjugated with electron rich substituents, such as indoles. This reduction methodology allows the presence of reducible and hydrogenolizable functional groups. An improved process to prepare 2 by treatment of the 3-(tetrahydro-4-pyridyl) indole derivatives with NaBH4 in THF under acidic conditions (AcOH or CF3COOH) is also described.
- Borghese, Alfio,Antoine, Luc,Stephenson, Gregory
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p. 8087 - 8090
(2007/10/03)
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- COMPOUNDS HAVING EFFECTS ON SEROTONIN-RELATED SYSTEMS
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A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1 A receptor. The compounds are particularly useful for alleviating the symptoms of n
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- Compounds having effects on serotonin-related systems
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A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1A receptor. The compounds are particularly useful for alleviating the sym
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- COMPOUNDS HAVING EFFECTS ON SEROTONIN-RELATED SYSTEMS
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A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1 A receptor. The compounds are particularly useful for alleviating the symptoms of n
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- 1H-indole and benzo(b)thiophene derivatives with 4-(1,2,3,6-tetra:hydro:pyridinyl)- and 4-piperidinyl-groups bound to the heterocyclic ring as inhibitors of serotonin reuptake
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The pharmaceutical use of novel compounds of formula I: where Z is a structure of formula A-B is -C=CH- or -C(R5)-CH2-; X is S or NR4; R1is H, halo, formyl, C1-C4alkyl, C1-C4alkoxy, thienylmethyloxy, 4,5-dihydrothiazol-2-yl, cyano, nitro, carboxamido, trifluoromethyl or hydroxy; R2is H or halo; R3is H, C1-C4alkyl, (C1-C4alkylene)-aryl, or -CH2-Y-NR7R8; R4is H, C1-C4alkyl, C1-C5acyl, or phenylsulfonyl; R5is H or OH; R6is H or methyl; Y is -CH2- or -C(O)-; R7is pyridinyl; and R8is H or -C(O)-(C3-C6cycloalkyl); and pharmaceutically acceptable salts thereof.
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- COMPOUNDS HAVING EFFECTS ON SEROTONIN-RELATED SYSTEMS
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A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1 A receptor. The compounds are particularly useful for alleviating the symptoms of n
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- Piperidinylalkyl quinazoline compounds, composition and method of use
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Novel quinazoline derivatives, comprising in the heterocyclic part of their quinazoline nucleus at least one carbonyl or thiocarbonyl group and a particularly substituted piperidinyl-alkyl side chain, said compounds being potent serotonin-antagonists.
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