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1. WO2016141003 - PROCESSES AND INTERMEDIATES FOR THE PREPARATION OF PIMAVANSERIN

Publication Number WO/2016/141003
Publication Date 09.09.2016
International Application No. PCT/US2016/020337
International Filing Date 02.03.2016
IPC
A61P 25/28 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for 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
C07D 233/60 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
233Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54having two double bonds between ring members or between ring members and non-ring members
56with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
60with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
C07D 211/58 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06having no double bonds between ring members or between ring members and non-ring members
36with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
56Nitrogen atoms
58attached in position 4
A61K 31/4468 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
445Non-condensed piperidines, e.g. piperocaine
4468having a nitrogen atom directly attached in position 4, e.g. clebopride, fentanyl
CPC
A61P 25/28
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for 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
C07B 2200/13
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200Indexing scheme relating to specific properties of organic compounds
13Crystalline forms, e.g. polymorphs
C07C 259/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
259Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
04without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids
06having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 269/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
269Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups , the nitrogen atom not being part of nitro or nitroso groups
04from amines with formation of carbamate groups
C07C 271/48
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
271Derivatives of carbamic acids, i.e. compounds containing any of the groups , the nitrogen atom not being part of nitro or nitroso groups
06Esters of carbamic acids
40having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings
42with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
48to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
C07D 211/58
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06having no double bonds between ring members or between ring members and non-ring members
36with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
56Nitrogen atoms
58attached in position 4
Applicants
  • TEVA PHARMACEUTICAL INDUSTRIES LTD. [IL]/[IL] (AllExceptUS)
Inventors
  • BILJAN, Tomislav
  • DOGAN, Jasna
  • METSGER, Leonid
  • PIPERCIC, Sara, Morasi
  • RATKAJ, Marina
  • SKUGOR, Maja, Matanovic
  • WANG, Yi
Agents
  • VALLA, S., Maurice
Priority Data
62/126,84002.03.2015US
62/161,42114.05.2015US
62/187,66801.07.2015US
62/188,99206.07.2015US
62/198,21829.07.2015US
62/270,31021.12.2015US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) PROCESSES AND INTERMEDIATES FOR THE PREPARATION OF PIMAVANSERIN
(FR) PROCÉDÉS ET INTERMÉDIAIRES POUR LA PRÉPARATION DE PIMAVANSÉRINE
Abstract
(EN) The present disclosure relates to novel, safe and efficient processes for the synthesis of Pimavanserin and salts thereof, as well as novel intermediates that can be used in these processes.
(FR) La présente invention concerne des procédés novateurs, sans danger et efficaces pour la synthèse de pimavansérine et de ses sels, ainsi que de nouveaux intermédiaires qui peuvent être utilisés dans ces procédés.
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