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1. (WO2019030641) FLUOROPIPERIDINE COMPOUNDS AS PURE 5-HT6 RECEPTOR ANTAGONISTS
Latest bibliographic data on file with the International BureauSubmit observation

Pub. No.: WO/2019/030641 International Application No.: PCT/IB2018/055894
Publication Date: 14.02.2019 International Filing Date: 06.08.2018
IPC:
C07D 413/04 (2006.01) ,A61K 31/4545 (2006.01) ,A61P 25/28 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
445
Non-condensed piperidines, e.g. piperocaine
4523
containing further heterocyclic ring systems
4545
containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25
Drugs for disorders of the nervous system
28
for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
Applicants:
SUVEN LIFE SCIENCES LIMITED [IN/IN]; Serene Chambers, Road-5, Avenue – 7, Banjara Hills Hyderabad Telangana 500034, IN
Inventors:
NIROGI, Ramakrishna; IN
SHINDE, Anil Karbhari; IN
MOHAMMED, Abdul Rasheed; IN
BADANGE, Rajesh Kumar; IN
BOJJA, Kumar; IN
GOYAL, Vinod Kumar; IN
PANDEY, Santosh Kumar; IN
THENTU, Jagadeesh Babu; IN
JASTI, Venkateswarlu; IN
Agent:
KULSHRESHTHA, Garima; IN
SUBRAMANIAM, Hariharan; IN
GANDHI, Ritu; IN
BHASIN, Gayatri; IN
MAHLA, Aaysu; IN
KAPOOR, Divya; IN
VENKITACHALAM, Manoj; IN
ELANGBAM, Nanda; IN
Priority Data:
20174102802407.08.2017IN
Title (EN) FLUOROPIPERIDINE COMPOUNDS AS PURE 5-HT6 RECEPTOR ANTAGONISTS
(FR) COMPOSÉS DE FLUOROPIPÉRIDINE UTILISÉS EN TANT QU'ANTAGONISTES PURS DU RÉCEPTEUR 5-HT 6
Abstract:
(EN) The present invention relates to fluoropiperidine compounds of formula (I), their stereoisomers, isotopic forms or pharmaceutically acceptable salts thereof as 5-HT6 receptor antagonists. In particular the present invention discloses the methods of preparation, pharmaceutical composition, combinations and use of fluoropiperidine compounds, their stereoisomers, isotopic forms or pharmaceutically acceptable salts thereof. In formula (I), R1 represents phenyl or pyridyl; wherein the phenyl or pyridyl is optionally substituted with one or more groups selected from halogen, (C1-6)-alkyl or halo(C1-6 )-alkyl; R2 represents hydrogen or (C1-6)-alkyl; R3 represents hydrogen or (C1-6)-alkyl; or R2 and R3 can combine together to form (C3-6)- cycloalkyl; R4 represents hydrogen, (C1-6)-alkyl or halo(C1-6)-alkyl; R5 represents hydrogen, (C1-6)-alkyl, halo(C1-6)-alkyl or -(CH2)0-3- (C3-6)-cycloalkyl. The compounds can be used in the treatment of cognitive disorder mediated by the 5-Hydroxytryptamine 6 receptor, wherein said cognitive disorder is selected from the group consisting of dementia in Alzheimer's disease, dementia in Parkinson's disease, dementia in Huntington's disease, dementia associated with Down syndrome, dementia associated with Tourette's syndrome, dementia associated with post menopause, frontotemporal dementia, Lewy body dementia, Vascular dementia, dementia in HIV, dementia in Creutzfeldt-Jakob disease, substance-induced persisting dementia, dementia in Pick's disease, dementia in schizophrenia, dementia in general medical conditions and senile dementia.
(FR) La présente invention concerne des composés de fluoropipéridine de formule (I), leurs stéréoisomères, leurs formes isotopiques ou leurs sels pharmaceutiquement acceptables en tant qu'antagonistes du récepteur 5-HT6. La présente invention concerne particulièrement les procédés de préparation, la composition pharmaceutique, les combinaisons et l'utilisation des composés de fluoropipéridine, leurs stéréoisomères, leurs formes isotopiques ou leurs sels pharmaceutiquement acceptables. Dans la formule (I), R1 représente phényle ou pyridyle; le phényle ou le pyridyle étant éventuellement substitué par un ou plusieurs groupes choisis parmi halogène, alkyle en (C1-6) ou alkyle halo (C1-6 ); R2 représente hydrogène ou alkyle en (C1-6); R3 représente hydrogène ou alkyle en (C1-6); ou R2 et R3 peuvent se combiner ensemble pour former un cycloalkyle en (C3-6); R4 représente hydrogène, alkyle en (C1-6) ou alkyle halo (C1-6); R5 représente hydrogène, alkyle en (C1-6), alkyle halo (C1-6) ou cycloalkyle -(CH2)0 -3- (C3-6). Les composés peuvent être utilisés dans le traitement d'un trouble cognitif induit par le récepteur 5-Hydroxytryptamine 6, ledit trouble cognitif étant choisi dans le groupe constitué par la démence dans la maladie d'Alzheimer, la démence dans la maladie de Parkinson, la démence dans la maladie de Huntington, la démence associée au syndrome de Down, la démence associée au syndrome de Tourette, la démence associée à la ménopause, la démence frontotemporale, la démence à corps de Lewy, la démence vasculaire, la démence en VIH, la démence dans la maladie de Creutzfeldt-Jakob, la démence persistante induite par une substance, la démence dans la maladie de Pick, la démence dans la schizophrénie, la démence dans des conditions médicales générales et la démence sénile.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)