TW201613897A - Acid addition salt of Trk inhibitor compound - Google Patents

Acid addition salt of Trk inhibitor compound

Info

Publication number
TW201613897A
TW201613897A TW104126689A TW104126689A TW201613897A TW 201613897 A TW201613897 A TW 201613897A TW 104126689 A TW104126689 A TW 104126689A TW 104126689 A TW104126689 A TW 104126689A TW 201613897 A TW201613897 A TW 201613897A
Authority
TW
Taiwan
Prior art keywords
trk
compound
acid addition
addition salt
inhibitor compound
Prior art date
Application number
TW104126689A
Other languages
English (en)
Other versions
TWI560185B (en
Inventor
Jun Takeuchi
Satoshi Itadani
Masahiro Ikura
Masato Higashino
Hideomi Kijima
Shizuka Ono
Tetsuya Yasuhiro
Takeshi Nagaura
Original Assignee
Ono Pharmaceutical Co
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 Ono Pharmaceutical Co filed Critical Ono Pharmaceutical Co
Publication of TW201613897A publication Critical patent/TW201613897A/zh
Application granted granted Critical
Publication of TWI560185B publication Critical patent/TWI560185B/zh

Links

Classifications

    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P17/04—Antipruritics
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • 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
    • 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
    • A61P37/08—Antiallergic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
TW104126689A 2014-08-18 2015-08-17 Acid addition salt of trk inhibitor compound TWI560185B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP2014165622 2014-08-18

Publications (2)

Publication Number Publication Date
TW201613897A true TW201613897A (en) 2016-04-16
TWI560185B TWI560185B (en) 2016-12-01

Family

ID=55350699

Family Applications (2)

Application Number Title Priority Date Filing Date
TW105109673A TWI573794B (zh) 2014-08-18 2015-08-17 ＴｒＫ阻礙化合物之酸附加鹽
TW104126689A TWI560185B (en) 2014-08-18 2015-08-17 Acid addition salt of trk inhibitor compound

Family Applications Before (1)

Application Number Title Priority Date Filing Date
TW105109673A TWI573794B (zh) 2014-08-18 2015-08-17 ＴｒＫ阻礙化合物之酸附加鹽

Country Status (22)

Country Link
US (1) US10399959B2 (zh)
EP (1) EP3184519B1 (zh)
JP (2) JP5979335B2 (zh)
KR (1) KR20170042591A (zh)
CN (2) CN106573913B (zh)
AU (1) AU2015304438B2 (zh)
BR (2) BR112017003302A2 (zh)
CA (1) CA2958423A1 (zh)
DK (1) DK3184519T3 (zh)
ES (1) ES2732026T3 (zh)
HU (1) HUE045237T2 (zh)
IL (2) IL250603A0 (zh)
MX (1) MX2017002199A (zh)
PH (2) PH12017500287A1 (zh)
PL (1) PL3184519T3 (zh)
PT (1) PT3184519T (zh)
RU (1) RU2708236C2 (zh)
SG (1) SG11201701208WA (zh)
TR (1) TR201908736T4 (zh)
TW (2) TWI573794B (zh)
WO (1) WO2016027754A1 (zh)
ZA (1) ZA201701174B (zh)

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SI2350071T1 (sl) 2008-10-22 2014-05-30 Array Biopharma, Inc. Substituirane pirazolo(1,5-a)pirimidinske spojine kot Trk kinazni inhibitorji
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
ES2628418T3 (es) 2010-05-20 2017-08-02 Array Biopharma, Inc. Compuestos macrocíclicos como inhibidores de la TRK cinasa
HUE042591T2 (hu) 2013-02-19 2019-07-29 Ono Pharmaceutical Co TRK-gátló vegyület
CN113354649A (zh) 2014-11-16 2021-09-07 阵列生物制药公司 一种新的晶型
TN2017000502A1 (en) 2015-06-01 2019-04-12 Loxo Oncology Inc Methods of diagnosing and treating cancer
SI3322706T1 (sl) 2015-07-16 2021-04-30 Array Biopharma, Inc. Substituirane pirazolo(1,5-A)piridinske spojine kot zaviralci ret-kinaze
US10724102B2 (en) 2015-10-26 2020-07-28 Loxo Oncology, Inc. Point mutations in TRK inhibitor-resistant cancer and methods relating to the same
WO2017155018A1 (ja) * 2016-03-11 2017-09-14 小野薬品工業株式会社 Ｔｒｋ阻害剤抵抗性の癌治療剤
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
BR112018070017A2 (pt) 2016-04-04 2019-02-05 Loxo Oncology Inc métodos de tratamento de cânceres pediátricos
CU20180125A7 (es) 2016-04-04 2019-05-03 Loxo Oncology Inc Formulaciones líquidas de (s)-n-(5-((r)-2-(2,5-difluorofenil) -pirrolidin-1-il)-pirazolo[1,5-alpirimidin-3-il)-3 hidroxipirrolidina-1-carboxamida
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療
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TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
US11168090B2 (en) 2017-01-18 2021-11-09 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyrazines as RET kinase inhibitors
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
US10180422B1 (en) * 2017-08-22 2019-01-15 Scripps Health Methods of treating a neuroendocrine tumor
WO2019049891A1 (ja) 2017-09-06 2019-03-14 小野薬品工業株式会社 Ｔｒｋ阻害剤とキナーゼ阻害剤の併用による癌治療方法
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
TWI812649B (zh) 2017-10-10 2023-08-21 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
CA3080157A1 (en) 2017-10-26 2019-05-02 Array Biopharma Inc. Formulations of a macrocyclic trk kinase inhibitor
CN111971286B (zh) 2018-01-18 2023-04-14 阿雷生物药品公司 作为RET激酶抑制剂的取代的吡咯并[2,3-d]嘧啶化合物
WO2019143994A1 (en) 2018-01-18 2019-07-25 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors
CA3087578C (en) 2018-01-18 2023-08-08 Array Biopharma Inc. Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors
CA3095366A1 (en) 2018-03-29 2019-10-03 Loxo Oncology, Inc. Treatment of trk-associated cancers
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JP2022500383A (ja) 2018-09-10 2022-01-04 アレイ バイオファーマ インコーポレイテッド Ｒｅｔキナーゼ阻害剤としての縮合複素環式化合物
WO2020131674A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
CN113884584B (zh) * 2020-08-07 2023-07-28 北京泰德制药股份有限公司 一种氟比洛芬和/或氟比洛芬酯含量的检测方法

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EP2324825A1 (en) * 2002-02-11 2011-05-25 Bayer Healthcare LLC Aryl ureas with angiogenesis inhibiting activity
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
JP6160613B2 (ja) * 2012-04-26 2017-07-12 小野薬品工業株式会社 Ｔｒｋ阻害化合物
HUE042591T2 (hu) 2013-02-19 2019-07-29 Ono Pharmaceutical Co TRK-gátló vegyület

Also Published As

Publication number Publication date
IL250603A0 (en) 2017-04-30
US10399959B2 (en) 2019-09-03
TWI560185B (en) 2016-12-01
EP3184519A1 (en) 2017-06-28
TWI573794B (zh) 2017-03-11
SG11201701208WA (en) 2017-03-30
AU2015304438A1 (en) 2017-03-09
CA2958423A1 (en) 2016-02-25
EP3184519A4 (en) 2018-03-07
JPWO2016027754A1 (ja) 2017-04-27
MX2017002199A (es) 2017-08-18
CN110655502A (zh) 2020-01-07
PH12017500287A1 (en) 2017-06-28
TR201908736T4 (tr) 2019-07-22
RU2708236C2 (ru) 2019-12-05
AU2015304438B2 (en) 2019-06-20
PH12017501720A1 (en) 2019-09-30
BR112017003302A2 (pt) 2017-11-28
JP5979335B2 (ja) 2016-08-24
WO2016027754A1 (ja) 2016-02-25
PT3184519T (pt) 2019-07-01
DK3184519T3 (da) 2019-07-08
RU2017104918A3 (zh) 2019-03-06
JP5979329B1 (ja) 2016-08-24
PL3184519T3 (pl) 2019-09-30
US20170240527A1 (en) 2017-08-24
TW201623284A (zh) 2016-07-01
ZA201701174B (en) 2019-06-26
KR20170042591A (ko) 2017-04-19
ES2732026T3 (es) 2019-11-20
CN106573913B (zh) 2019-11-19
IL254351A0 (en) 2017-11-30
CN106573913A (zh) 2017-04-19
EP3184519B1 (en) 2019-04-24
RU2017104918A (ru) 2018-09-23
JP2016155828A (ja) 2016-09-01
BR122017020365A2 (pt) 2019-09-10
HUE045237T2 (hu) 2019-12-30

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