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1. WO2019118298 - FUMARATE SALT OF (R)-3-(1-(2,3-DICHLORO-4-(PYRAZIN-2-YL)PHENYL)-2,2,2-TRIFLUOROETHYL)-1-METHYL-1-(1-METHYLPIPERIDIN-4-YL) UREA, METHODS OF PREPARATION, AND USES THEREOF

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Publication Number WO/2019/118298
Publication Date 20.06.2019
International Application No. PCT/US2018/064512
International Filing Date 07.12.2018
IPC
C07D 401/12 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
A61P 25/30 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
30for treating abuse or dependence
A61K 31/497 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
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
4965Non-condensed pyrazines
497containing further heterocyclic rings
CPC
A61K 31/497
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
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
4965Non-condensed pyrazines
497containing further heterocyclic rings
A61P 25/30
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
30for treating abuse or dependence
A61P 5/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
5Drugs for disorders of the endocrine system
06of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
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
C07D 401/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
Applicants
  • HELSINN HEALTHCARE SA [CH]/[CH]
Inventors
  • GARCIA RUBIO, Silvina
  • PERSEGHINI, Mauro
  • GUAINAZZI, Angelo
  • PIETRA, Claudio
  • GIULIANO, Claudio
Agents
  • HENNINGER, PHD, Mary
  • BAUR, PHD, Amelia F.
  • BREIER, PHD, Adam M.
  • CHO, Hojung
  • CISAR, Elizabeth
  • HERZFELD, Deborah M.
  • DOHERTY, PHD, Elizabeth A.
  • KELLEY, Lara C.
  • LEE, Victoria
  • MCNEILL, Rebecca M.
  • PRYBYLOWSKI, PHD, Kate
  • RACHINSKY, PHD, Tara
  • SCARR, PHD, Rebecca B.
  • SCHOENHARD, Amy
Priority Data
62/597,23611.12.2017US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) FUMARATE SALT OF (R)-3-(1-(2,3-DICHLORO-4-(PYRAZIN-2-YL)PHENYL)-2,2,2-TRIFLUOROETHYL)-1-METHYL-1-(1-METHYLPIPERIDIN-4-YL) UREA, METHODS OF PREPARATION, AND USES THEREOF
(FR) SEL DE FUMARATE DE L'URÉE (R)-3-(1-(2,3-DICHLORO-4-(PYRAZIN-2-YL)PHÉNYL)-2,2,2-TRIFLUOROÉTHYL)-1-MÉTHYL-1-(1-MÉTHYLPIPÉRIDIN-4-YL), PROCÉDÉS DE PRÉPARATION ET UTILISATIONS DE CELUI-CI
Abstract
(EN) Provided are various embodiments relating to fumarate salt of (R)-3-(1-(2,3-dichloro-4-(pyrazin-2-yl)phenyl)-2,2,2-trifluoroethyl)-1-methyl-1-(1-methylpiperidin-4-yl) urea, and methods of producing and using the same to treat conditions and disorders associated with an increase of ghrelin level, such as food abuse, alcohol addiction, and other disorders (e.g., Prader-Willi syndrome). Also provided are various embodiments relating to crystalline HM04 free base, different crystalline forms of HM04 fumarate salt, and methods of producing the same.
(FR) L'invention concerne divers modes de réalisation se rapportant au sel de fumarate de l'urée (R)-3-(l-(2,3-dichloro-4- (pyrazin-2-yl)phényl)-2,2,2-trifluoroéthyl)- 1 -méthyl- 1 -(1 -méthylpipéridin-4-yl), ainsi que des procédés de production et d'utilisation de celui-ci pour traiter des états pathologiques et des troubles associés à une augmentation du niveau de la ghréline, tels que l'abus d'aliments, la dépendance à l'alcool, et d'autres troubles (par exemple, le syndrome de Prader-Willi). L'invention concerne également divers modes de réalisation se rapportant à la base libre de HM04 cristallin, différentes formes cristallines du sel de fumarate de HM04, et leurs procédés de production.
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