DK3174881T3 - [1,2,4]triazolo[4,3-b]pyridaziner til anvendelse til behandling af proliferative sygdomme - Google Patents

[1,2,4]triazolo[4,3-b]pyridaziner til anvendelse til behandling af proliferative sygdomme Download PDF

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Publication number
DK3174881T3
DK3174881T3 DK15744308.6T DK15744308T DK3174881T3 DK 3174881 T3 DK3174881 T3 DK 3174881T3 DK 15744308 T DK15744308 T DK 15744308T DK 3174881 T3 DK3174881 T3 DK 3174881T3
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Denmark
Prior art keywords
compound
pharmaceutically acceptable
formula
piperidin
hydroxy
Prior art date
Application number
DK15744308.6T
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English (en)
Inventor
James Francis Mccabe
Zoe Ann Cotter
Robert Hugh Bradbury
Alfred Arthur Rabow
Michael James Waring
Steven Christopher Glossop
Arshed Mahmood
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Astrazeneca Ab
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Publication of DK3174881T3 publication Critical patent/DK3174881T3/da

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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C65/00—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C65/01—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups
    • C07C65/105—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups polycyclic
    • C07C65/11—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups polycyclic with carboxyl groups on a condensed ring system containing two rings
    • E—FIXED CONSTRUCTIONS
    • E21—EARTH OR ROCK DRILLING; MINING
    • E21B—EARTH OR ROCK DRILLING; OBTAINING OIL, GAS, WATER, SOLUBLE OR MELTABLE MATERIALS OR A SLURRY OF MINERALS FROM WELLS
    • E21B7/00—Special methods or apparatus for drilling
    • E21B7/04—Directional drilling
    • E21B7/06—Deflecting the direction of boreholes
    • E—FIXED CONSTRUCTIONS
    • E21—EARTH OR ROCK DRILLING; MINING
    • E21B—EARTH OR ROCK DRILLING; OBTAINING OIL, GAS, WATER, SOLUBLE OR MELTABLE MATERIALS OR A SLURRY OF MINERALS FROM WELLS
    • E21B7/00—Special methods or apparatus for drilling
    • E21B7/04—Directional drilling
    • E21B7/06—Deflecting the direction of boreholes
    • E21B7/062—Deflecting the direction of boreholes the tool shaft rotating inside a non-rotating guide travelling with the shaft
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Mining & Mineral Resources (AREA)
  • Geology (AREA)
  • Engineering & Computer Science (AREA)
  • Health & Medical Sciences (AREA)
  • Physics & Mathematics (AREA)
  • Geochemistry & Mineralogy (AREA)
  • General Life Sciences & Earth Sciences (AREA)
  • Fluid Mechanics (AREA)
  • Environmental & Geological Engineering (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (15)

1. Forbindelse med formel (I) eller et farmaceutisk acceptabelt salt deraf
hvor: R1 er gruppen
eller
qruppen og ---- angiver bindingspunktet; R2 er en Ci-C4alkyl; og n er 2 eller 3.
2. Forbindelse ifølge krav 1 eller et farmaceutisk acceptabelt salt deraf, hvor R1 er gruppen
hvor --- angiver bindingspunktet; R2 er Ci-C4alkyl; og n er 2 eller 3.
3. Forbindelse ifølge krav 1 eller et farmaceutisk acceptabelt salt deraf, hvor R1 er gruppen
hvor ---- angiver bindingspunktet; R2 er Ci-C4alkyl; og n er 2 eller 3.
4. Forbindelse ifølge krav 1 eller et farmaceutisk acceptabelt salt deraf, hvor R1 er gruppen
hvor ---- angiver bindingspunktet; R2 er Ci-C4alkyl; og n er 2 .
5. Forbindelse ifølge krav 1 eller et farmaceutisk acceptabelt salt deraf, hvilken forbindelse er valgt blandt: 4-(2-(4-(1-(3-methoxy-[l,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl)phenoxy)ethyl)-1,3-dimethylpiperazin-2-on; 1-(4-(2-(4-(1-(3-methoxy-[l,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl)phenoxy)ethyl)-3,5-dimethylpiperazin-l-yl)ethanon; 4-(3-(4-(1-(3-methoxy-[1,2,4]triazolo[4,3 —b]pyridazin-6-yl)piperidin-4-yl)phenoxy)propy1)-1,3-dimethylpiperazin-2-on; og 1-(4-(3-(4-(1-(3-methoxy-[l,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl)phenoxy)propyl)-3,5-dimethylpiperazin-l-yl)ethanon.
6. Forbindelse ifølge krav 1 eller et farmaceutisk acceptabelt salt deraf, hvilken forbindelse er valgt blandt: (R)-4-(2-(4-(1-(3-methoxy-[l,2,4]triazolo[4,3-b]pyridazin-6- yl)piperidin-4-yl)phenoxy)ethyl)-1,3-dimethylpiperazin-2-on (benævnes herefter forbindelse A); 1—((3S,5R)-4-(2-(4-(l-(3-methoxy-[l,2,4]triazolo[4,3- b]pyridazin-6-yl)piperidin-4-yl)phenoxy)ethyl)-3,5-dimethylpiperazin-l-yl)ethanon; (R)—4—(3—(4—(1—(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl)phenoxy)propyl)-i, 3-dimethylpiperazin-2-on; og 1-((3R,5S)-4-(3-(4-(1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl)phenoxy)propyl)-3,5-dimethylpiperazin-l-yl)ethanon.
7. Forbindelse ifølge krav 6 eller et farmaceutisk acceptabelt salt deraf med formel (IA):
8. Forbindelse ifølge krav 7 med formel (IA).
9. Forbindelse ifølge krav 7 og 8 i en krystalform, der har et XRPD-mønster med mindst to specifikke toppe ved 2-theta = 20,9° og 16,7° plus eller minus 0,2° 2-theta målt ved anvendelse af CuKa-stråling.
10. Cokrystal af forbindelsen med formel (IA) ifølge krav 7 og det cokrystal-dannende molekyle 6-hydroxy-2-naphthoesyre.
11. Cokrystal af forbindelsen med formel (IA) ifølge krav 7 og 6-hydroxy-2-naphthoesyre, der kan opnås ved hjælp af trinene i) blanding af en opløsning af forbindelsen med formel (IA) i et egnet opløsningsmiddel med 6-hydroxy-2-naphthoesyre-cokrystal i et egnet opløsningsmiddel; og ii) tørring af den resulterende blanding fra trin (i) til opnåelse af et faststof.
12. Forbindelse ifølge et hvilket som helst af kravene 1 til 9 eller et farmaceutisk acceptabelt salt deraf eller en cokrystal ifølge krav 10 og 11 til anvendelse som et medikament.
13. Forbindelse ifølge et hvilket som helst af kravene 1 til 9 eller et farmaceutisk acceptabelt salt deraf eller en cokrystal ifølge krav 10 og 11 til anvendelse til forebyggelse eller behandling af cancer hos et varmblodet dyr, såsom et menneske.
14. Forbindelse ifølge et hvilket som helst af kravene 1 til 9 eller et farmaceutisk acceptabelt salt deraf eller en cokrystal ifølge krav 10 og 11 til anvendelse til behandling af ovariecancer, akut myeloid og blandet cellelinje leukæmi (AML), multipelt myelom (MM), diffust storcelle B-cellelymfom (DLBCL) , kastrationsresistent prostatacancer (CRPC), ikke-småcellet lungecancer (NSCLC), småcellet lungecancer (SCLC), brystcancer, glioblastom og neuroblastom hos et varmblodet dyr, såsom et menneske.
15. Farmaceutisk sammensætning, der omfatter en forbindelse med formel (I) eller et farmaceutisk acceptabelt salt deraf ifølge et hvilket som helst af kravene 1 til 9 eller et cokrystal ifølge krav 10 og 11 og et farmaceutisk acceptabelt fortyndingsmiddel eller bæremiddel.
DK15744308.6T 2014-07-28 2015-07-24 [1,2,4]triazolo[4,3-b]pyridaziner til anvendelse til behandling af proliferative sygdomme DK3174881T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462029676P 2014-07-28 2014-07-28
PCT/GB2015/052143 WO2016016618A1 (en) 2014-07-28 2015-07-24 [1,2,4]triazolo[4,3-b]pyridazines for use in the treatment of proliferative diseases

Publications (1)

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DK3174881T3 true DK3174881T3 (da) 2018-06-06

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ID=53761420

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DK15744308.6T DK3174881T3 (da) 2014-07-28 2015-07-24 [1,2,4]triazolo[4,3-b]pyridaziner til anvendelse til behandling af proliferative sygdomme

Country Status (37)

Country Link
US (5) US9944650B2 (da)
EP (1) EP3174881B1 (da)
JP (1) JP6592503B2 (da)
KR (1) KR20170033427A (da)
CN (1) CN106536524B (da)
AP (1) AP2017009700A0 (da)
AU (1) AU2015295120B2 (da)
BR (1) BR112017001160A2 (da)
CA (2) CA3185741A1 (da)
CL (1) CL2017000223A1 (da)
CO (1) CO2017001918A2 (da)
CY (1) CY1120602T1 (da)
DK (1) DK3174881T3 (da)
DO (1) DOP2017000018A (da)
EA (1) EA032654B9 (da)
ES (1) ES2670444T3 (da)
GT (1) GT201700016A (da)
HR (1) HRP20180788T1 (da)
HU (1) HUE037571T2 (da)
IL (1) IL250104B (da)
LT (1) LT3174881T (da)
MX (1) MX374539B (da)
MY (1) MY187251A (da)
NI (1) NI201700006A (da)
NO (2) NO2719005T3 (da)
PE (1) PE20170527A1 (da)
PH (1) PH12017500159B1 (da)
PL (1) PL3174881T3 (da)
PT (1) PT3174881T (da)
RS (1) RS57242B1 (da)
SG (1) SG11201700419SA (da)
SI (1) SI3174881T1 (da)
SM (1) SMT201800260T1 (da)
SV (1) SV2017005368A (da)
TN (1) TN2017000018A1 (da)
WO (1) WO2016016618A1 (da)
ZA (1) ZA201701207B (da)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NO2719005T3 (da) * 2014-07-28 2018-01-20
CN110317216A (zh) * 2018-03-28 2019-10-11 首都医科大学 一种三唑并哒嗪类衍生物在医药领域的应用
TWI816880B (zh) * 2018-09-13 2023-10-01 大陸商恒翼生物醫藥（上海）股份有限公司 治療前列腺癌之組合療法
EP4045049A1 (en) 2019-10-14 2022-08-24 Astrazeneca AB Combination therapy for treating a hematological malignancy
KR20220124739A (ko) 2020-01-09 2022-09-14 아스트라제네카 아베 암의 치료를 위한 병용 요법
CN113143930B (zh) * 2021-04-08 2023-05-30 深圳湾实验室 化合物在制备SARS-Cov-2 E蛋白抑制剂中的用途

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Publication number Priority date Publication date Assignee Title
CA2629743A1 (en) 2005-12-08 2007-06-14 Novartis Ag Pyrazolo[1,5-a]pyridine-3-carboxylic acids as ephb and vegfr2 kinase inhibitors
GB0525065D0 (en) * 2005-12-08 2006-01-18 Novartis Ag Organic compounds
CA2709514A1 (en) 2007-12-21 2009-07-02 Astrazeneca Ab Bicyclic derivatives for use in the treatment of androgen receptor associated conditions
MX2011008452A (es) * 2009-02-10 2011-12-16 Astrazeneca Ab Derivados de triazolo [4,3-b] piridazina y sus usos para el cancer de prostata.
AU2010247190A1 (en) * 2009-05-11 2011-11-10 Astrazeneca Ab [1,2,4] triazolo [4,3-b] pyridazines as ligands of the androgen receptor
AU2010314395B2 (en) 2009-11-05 2015-04-09 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
WO2012174487A2 (en) * 2011-06-17 2012-12-20 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
US9422290B2 (en) * 2012-11-13 2016-08-23 Boehringer Ingelheim International Gmbh Triazolopyridazine
NO2719005T3 (da) * 2014-07-28 2018-01-20

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SI3174881T1 (en) 2018-06-29
PL3174881T3 (pl) 2018-08-31
CN106536524B (zh) 2019-11-15
SV2017005368A (es) 2017-05-12
US10766905B2 (en) 2020-09-08
EA032654B1 (ru) 2019-06-28
SMT201800260T1 (it) 2018-07-17
MX374539B (es) 2025-03-06
DOP2017000018A (es) 2017-03-15
CO2017001918A2 (es) 2017-05-10
BR112017001160A2 (pt) 2017-11-14
RS57242B1 (sr) 2018-07-31
NO2719005T3 (da) 2018-01-20
US20210107905A1 (en) 2021-04-15
EP3174881B1 (en) 2018-03-28
CA3185741A1 (en) 2016-02-04
EP3174881A1 (en) 2017-06-07
CL2017000223A1 (es) 2017-08-25
US20180230158A1 (en) 2018-08-16
US20230035133A1 (en) 2023-02-02
US10407432B2 (en) 2019-09-10
US11407755B2 (en) 2022-08-09
JP6592503B2 (ja) 2019-10-16
NI201700006A (es) 2017-08-25
AU2015295120A8 (en) 2017-02-09
US20200055861A1 (en) 2020-02-20
IL250104B (en) 2018-10-31
CA2956421C (en) 2023-03-14
GT201700016A (es) 2018-12-19
AU2015295120B2 (en) 2018-02-01
IL250104A0 (en) 2017-03-30
HRP20180788T1 (hr) 2018-06-29
PH12017500159A1 (en) 2017-07-10
ES2670444T3 (es) 2018-05-30
SG11201700419SA (en) 2017-02-27
KR20170033427A (ko) 2017-03-24
WO2016016618A1 (en) 2016-02-04
JP2017522338A (ja) 2017-08-10
ZA201701207B (en) 2018-12-19
MY187251A (en) 2021-09-15
CA2956421A1 (en) 2016-02-04
AU2015295120A1 (en) 2017-02-02
EA201790179A1 (ru) 2017-07-31
TN2017000018A1 (en) 2018-07-04
LT3174881T (lt) 2018-06-11
US9944650B2 (en) 2018-04-17
CY1120602T1 (el) 2019-12-11
PH12017500159B1 (en) 2020-12-09
CN106536524A (zh) 2017-03-22
EA032654B9 (ru) 2019-07-31
MX2017001218A (es) 2017-05-01
PE20170527A1 (es) 2017-05-24
US20170210747A1 (en) 2017-07-27
AP2017009700A0 (en) 2017-01-31
NO3174881T3 (da) 2018-08-25
PT3174881T (pt) 2018-05-25
HUE037571T2 (hu) 2018-09-28

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