ME02458B - Postupci i intermedijeri za spravljanje jak inhibitora - Google Patents

Postupci i intermedijeri za spravljanje jak inhibitora

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Publication number
ME02458B
ME02458B MEP-2016-43A MEP201643A ME02458B ME 02458 B ME02458 B ME 02458B ME P201643 A MEP201643 A ME P201643A ME 02458 B ME02458 B ME 02458B
Authority
ME
Montenegro
Prior art keywords
formula
compound
salt
mixture
process according
Prior art date
Application number
MEP-2016-43A
Other languages
German (de)
English (en)
French (fr)
Inventor
Jiacheng Zhou
Pingli Liu
Ganfeng Cao
Yongzhong Wu
Original Assignee
Incyte Holdings Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Incyte Holdings Corp filed Critical Incyte Holdings Corp
Publication of ME02458B publication Critical patent/ME02458B/me

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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 containing two hetero rings
    • C07D401/06—Heterocyclic 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 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/113—Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Transplantation (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Claims (23)

1.Postupak, koji obuhvata reakciju jedinjenja Formule III:ili njegove soli, sa jedinjenjem Formule IV:u prisustvu redukcionog agensa da se formira jedinjenje Formule II:ili njegove soli, obezbedjujući da redukcioni agens nije natrijum cijanoborodeuterid; gde je P1 zaštitna grupa.
2.Postupak prema patentnom zahtevu 1, gde je spomenuta zaštitna grupa –CH2OCH2CH2Si(CH3)3.
3.Postupak prema bilo kojem od patentnih zahteva od 1 do 2, gde je spomenuti redukcioni agens izabran od cijanoborohidrid natrijuma i natrijum triacetoksiborohidrida.
4.Postupak prema bilo kojem od patentnih zahteva od 1 do 2, gde je spomenuti redukcioni agens natrijum triacetoksiborohidrid.
5.Postupak prema bilo kojem od patentnih zahteva od 1 do 4, u kome su svako od jedinjenja Formula II, III i IV slobodna baza.
6.Postupak prema bilo kojem od patentnih zahteva od 1 do 5, dalje obuhvatajući uklanjanje zaštite Formule II, ili njegove soli, za formiranje jedinjenja Formule I: ili njegove soli.
7.Postupak prema patentnom zahtevu 6, gde spomenuto uklanjanje zaštite obuhvata tretman sa bor trifluorid eteratom, praćeno tretiranjem sa vodenim rastvorom amonijum hidroksida.
8.Postupak prema bilo kojem od patentnih zahteva od 6 do 8, gde spomenuti postupak dalje uključuje reakcije jedinjenja Formule I sa adipinskom kiselinom da se formira adipinska so.
9.Postupak prema bilo kojem od patentnih zahteva od 6 do 8, gde su svako od jedinjenja formula I, II, III i IV slobodna baza.
10.Postupak prema bilo kojem od patentnih zahteva od 6 do 7, gde spomenuti postupak dalje obuhvata: (a) grejanje jedinjenja Formule I u metanolu na refluksu da se formira smešu; (b) nakon (a), dodavanje metil izobutil ketona smeši; (c) nakon (b), uklanjanje dela rastvora destilacijom na unutrašnjoj temperaturi od 40°C do 50°C da se formira koncentrovanu smešu; (d) nakon (c), dodavanje metanola koncentrovanoj smeši za formiranje rastvora smeše; (e) nakon (d), grejanje razblažene smeše na refluksu da se formira smeša; (f) nakon (e), dodavanje metil izobutil ketona smeši; (g) nakon (f), uklanjanje dela rastvarača destilacijom na unutrašnjoj temperaturi od 40°C do 50°C da se formira koncentrat smeše; (h) nakon (g), dodavanje adipinske kiseline i metanola koncentrovanoj smeši; (i) posle (h), grejanje smeše na refluksu; i (j) nakon (i), uklanjanja dela rastvarača destilacijom na unutrašnjoj temperaturi od 40°C do 50°C da se formira koncentrat smeše; (k) nakon (j), dodavanje heptana smeši; i (l) nakon (k) mešanjem smeše na sobnoj temperaturi za dobijanje soli adipinske kiseline za jedinjenje Formule I.
11.Postupak prema bilo kojem od patentnih zahteva od 6 do 10, gde su jedinjenje Formule IV ili njegova so dobijeni postupkom koji obuhvata uklanjanje zaštite jedinjenja Formule V: ili soli od njega.
12.Postupak prema patentnom zahtevu 11, gde spomenuto uklanjanje zaštite obuhvata reakciju sa tečnom kiselinom.
13.Postupak prema patentnom zahtevu 12, gde je spomenuta kiselina hlorovodonična kiselina.
14.Postupak prema bilo kojem od patentnih zahteva od 11 do 13, gde je svako od jedinjenja formula I, II, III, IV i V slobodna baza.
15.Postupak prema bilo kojem od patentnih zahteva od 11 do 14, gde je jedinjenje formule V ili njegove soli proizvod postupka koji obuhvata reakciju jedinjenja Formule VI: sa jedinjenjem Formule VII: u prisustvu agensa za spajanje.
16.Postupak prema patentnom zahtevu 15, gde je agens spajanje benzotriazol-1-iloksi-tris (dimetilamino)-fosfonijum heksafluorofosfat (BOP).
17.Postupak dobijanja jedinjenja Formule IV: ili njegove soli, obuhvatajući uklanjanje zaštite jedinjenja Formule V: ili njegove soli, za formiranje jedinjenja Formule IV, ili njegove spomenute soli.
18.Postupak prema patentnom zahtevu 17, gde se spomenuto uklanjanje zaštite obuhvata reakciju sa tečnom kiselinom.
19.Postupak prema patentnom zahtevu 18, gde je spomenuta kiselina hlorovodonična kiselina.
20.Postupak prema bilo kojem od patentnih zahteva od 17 do 19, gde su svako od jedinjenja Formule IV i V slobodna baza.
21.Postupak spravljanja jedinjenja Formule V: ili njegove soli, obuhvatajući reakciju jedinjenja Formule VI: ili njegove soli, sa jedinjenjem Formule VII: ili njegove soli, u prisustvu agensa za spajanje da se formira jedinjenje Formule V, ili spomenute soli od njega.
22.Postupak prema patentnom zahtevu 21, gde je je agens spajanja benzotriazol-1-iloksi-tris (dimetilamino)-fosfonijum heksafluorofosfat (BOP).
23.Jedinjenje Formule V: ili soli od njega. 7
MEP-2016-43A 2011-09-07 2012-09-06 Postupci i intermedijeri za spravljanje jak inhibitora ME02458B (me)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161531896P 2011-09-07 2011-09-07
PCT/US2012/053921 WO2013036611A1 (en) 2011-09-07 2012-09-06 Processes and intermediates for making a jak inhibitor
EP12770334.6A EP2753621B1 (en) 2011-09-07 2012-09-06 Processes and intermediates for making a jak inhibitor

Publications (1)

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ME02458B true ME02458B (me) 2017-02-20

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US (2) US9487521B2 (me)
EP (1) EP2753621B1 (me)
JP (2) JP5977354B2 (me)
KR (1) KR102002277B1 (me)
CN (1) CN104024256B (me)
AR (2) AR087794A1 (me)
AU (1) AU2012304650B2 (me)
BR (1) BR112014005174B1 (me)
CA (1) CA2847728C (me)
CL (1) CL2014000534A1 (me)
CO (1) CO6910194A2 (me)
CR (1) CR20140120A (me)
CY (1) CY1117276T1 (me)
DK (1) DK2753621T3 (me)
EA (1) EA026122B1 (me)
ES (1) ES2564133T3 (me)
HR (1) HRP20160241T1 (me)
HU (1) HUE026497T2 (me)
IL (1) IL231389A (me)
IN (1) IN2014DN02177A (me)
ME (1) ME02458B (me)
MX (1) MX339715B (me)
MY (1) MY169617A (me)
PE (1) PE20142360A1 (me)
PH (1) PH12014500521A1 (me)
PL (1) PL2753621T3 (me)
PT (1) PT2753621E (me)
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SG (1) SG11201400414XA (me)
SI (1) SI2753621T1 (me)
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KR20140072878A (ko) 2014-06-13
UA111854C2 (uk) 2016-06-24
AU2012304650A1 (en) 2014-03-27
CY1117276T1 (el) 2017-04-26
TWI577690B (zh) 2017-04-11
ES2564133T3 (es) 2016-03-18
HRP20160241T1 (hr) 2016-04-08
SI2753621T1 (sl) 2016-05-31
EA026122B1 (ru) 2017-03-31
PT2753621E (pt) 2016-03-31
AR116431A2 (es) 2021-05-05
CN104024256B (zh) 2016-02-10
CN104024256A (zh) 2014-09-03
HK1199445A1 (zh) 2015-07-03
BR112014005174A2 (pt) 2017-04-18
TW201317246A (zh) 2013-05-01
EP2753621A1 (en) 2014-07-16
MX339715B (es) 2016-06-07
IN2014DN02177A (me) 2015-05-15
IL231389A (en) 2016-11-30
US9718834B2 (en) 2017-08-01
MY169617A (en) 2019-04-23
NZ622295A (en) 2015-07-31
IL231389A0 (en) 2014-04-30
SG11201400414XA (en) 2014-04-28
PL2753621T3 (pl) 2016-07-29
JP2014526466A (ja) 2014-10-06
RS54615B1 (sr) 2016-08-31

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