CN103347870A - Metap-2抑制剂的结晶固体及其制备和使用方法 - Google Patents

Metap-2抑制剂的结晶固体及其制备和使用方法 Download PDF

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Publication number
CN103347870A
CN103347870A CN2011800600503A CN201180060050A CN103347870A CN 103347870 A CN103347870 A CN 103347870A CN 2011800600503 A CN2011800600503 A CN 2011800600503A CN 201180060050 A CN201180060050 A CN 201180060050A CN 103347870 A CN103347870 A CN 103347870A
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crystallized form
solution
ray diffraction
powder
crystalline
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CN2011800600503A
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Chinese (zh)
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T·克劳福德
H·A·瑞斯
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Larimar Therapeutics Inc
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Zafgen Inc
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/336Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D301/00Preparation of oxiranes
    • C07D301/32Separation; Purification
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D303/00Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
    • C07D303/02Compounds containing oxirane rings
    • C07D303/12Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms
    • C07D303/16Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by esterified hydroxyl radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D303/00Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
    • C07D303/02Compounds containing oxirane rings
    • C07D303/12Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms
    • C07D303/18Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by etherified hydroxyl radicals
    • C07D303/20Ethers with hydroxy compounds containing no oxirane rings
    • C07D303/24Ethers with hydroxy compounds containing no oxirane rings with polyhydroxy compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/04Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/08Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a carbon chain containing alicyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Epoxy Compounds (AREA)
  • Medicinal Preparation (AREA)
CN2011800600503A 2010-11-09 2011-11-09 Metap-2抑制剂的结晶固体及其制备和使用方法 Pending CN103347870A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201710158431.4A CN106905267A (zh) 2010-11-09 2011-11-09 Metap‑2抑制剂的结晶固体及其制备和使用方法

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US41165510P 2010-11-09 2010-11-09
US61/411,655 2010-11-09
PCT/US2011/059966 WO2012064838A1 (en) 2010-11-09 2011-11-09 Crystalline solids of a metap-2 inhibitor and methods of making and using same

Related Child Applications (1)

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CN201710158431.4A Division CN106905267A (zh) 2010-11-09 2011-11-09 Metap‑2抑制剂的结晶固体及其制备和使用方法

Publications (1)

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CN103347870A true CN103347870A (zh) 2013-10-09

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CN2011800600503A Pending CN103347870A (zh) 2010-11-09 2011-11-09 Metap-2抑制剂的结晶固体及其制备和使用方法
CN201710158431.4A Pending CN106905267A (zh) 2010-11-09 2011-11-09 Metap‑2抑制剂的结晶固体及其制备和使用方法

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US (4) US8349891B2 (enExample)
EP (1) EP2638023B1 (enExample)
JP (1) JP6239977B2 (enExample)
KR (1) KR101892768B1 (enExample)
CN (2) CN103347870A (enExample)
AU (1) AU2011326566B2 (enExample)
BR (1) BR112013011550A2 (enExample)
CA (1) CA2817199C (enExample)
EA (1) EA029941B1 (enExample)
ES (1) ES2610216T3 (enExample)
IL (1) IL226238B (enExample)
MX (1) MX2013005208A (enExample)
MY (1) MY177039A (enExample)
NZ (1) NZ610569A (enExample)
PH (1) PH12013500934A1 (enExample)
SG (1) SG190688A1 (enExample)
UA (1) UA111479C2 (enExample)
WO (1) WO2012064838A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108697807A (zh) * 2016-01-11 2018-10-23 辛德弗雷克斯公司 代谢功能障碍引起的肿瘤的治疗

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EP2576638B1 (en) 2010-05-25 2020-12-23 Syndevrx, Inc. Polymer-conjugated metap2 inhibitors, and therapeutic methods of use thereof
US9895449B2 (en) 2010-05-25 2018-02-20 Syndevrx, Inc. Polymer-conjugated MetAP2 inhibitors, and therapeutic methods of use thereof
WO2012012642A1 (en) 2010-07-22 2012-01-26 Zafgen Corporation Tricyclic compounds and methds of making and using same
PH12013500934A1 (en) 2010-11-09 2022-10-24 Zafgen Inc Crystalline solids of a metap-2 inhibitor and methods of making and using same
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CN103402989B (zh) 2011-01-26 2016-04-06 扎夫根股份有限公司 四唑化合物及其制备和使用方法
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WO2012154676A1 (en) 2011-05-06 2012-11-15 Zafgen Corporation Partially saturated tricyclic compounds and methods of making and using same
KR20140040739A (ko) 2011-05-06 2014-04-03 자프겐 인크. 삼환식 피라졸 설폰아마이드 화합물 그리고 그의 제조방법 및 그를 이용하는 방법
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MX2014008706A (es) 2012-01-18 2015-03-05 Zafgen Inc Compuestos tricíclicos de sulfonamida y métodos para elaborarlos y usarlos.
BR112014017780A8 (pt) 2012-01-18 2017-07-11 Zafgen Inc Compostos de sulfona tricíclicos e métodos para fazer e usar os mesmos
KR20150016303A (ko) 2012-05-07 2015-02-11 자프겐 인크. 6-o-(4-디메틸아미노에톡시) 신나모일 푸마지롤의 옥살레이트 염의 다형체 염 및 이의 제조 및 사용 방법
EP2846792B1 (en) 2012-05-08 2018-08-15 Zafgen, Inc. Treating hypothalamic obesity with metap2 inhibitors
JP6177888B2 (ja) 2012-05-09 2017-08-09 ザフゲン,インコーポレイテッド フマギロール型化合物ならびにその製造および使用方法
WO2014071363A1 (en) 2012-11-05 2014-05-08 Zafgen, Inc. Tricyclic compounds and methods of making and using same
US9868717B2 (en) 2012-11-05 2018-01-16 Zafgen, Inc. Tricyclic sulphonamide compounds and methods of making and using same
JP6169716B2 (ja) 2012-11-05 2017-07-26 ザフゲン,インコーポレイテッド 肝疾患を治療する方法
US20150361139A1 (en) * 2013-01-30 2015-12-17 Sandoz Ag Crystalline form of linaclotide
EP3431475B1 (en) * 2013-02-21 2021-04-07 Pfizer Inc Solid forms of a selective cdk4/6 inhibitor
US9597309B2 (en) 2013-03-14 2017-03-21 Zafgen, Inc. Methods of treating renal disease and other disorders
BR112015025892A2 (pt) 2013-04-10 2017-07-25 Syndevrx Inc inibidores de metap2 e métodos para tratar obesidade
AR101608A1 (es) * 2014-08-22 2016-12-28 Zafgen Inc Formulaciones que contienen un inhibidor de metap-2
CN106432255A (zh) 2015-08-11 2017-02-22 扎夫根公司 烟曲霉素醇螺环化合物和制备和使用其的方法
AR105671A1 (es) 2015-08-11 2017-10-25 Zafgen Inc Compuestos heterocíclicos de fumagillol y sus métodos de elaboración y uso
DK3386956T3 (da) 2015-12-10 2021-10-11 Syndevrx Inc Fumagillolderivater og polymorfer deraf
CA3117666A1 (en) 2018-10-26 2020-04-30 Syndevrx, Inc. Biomarkers of metap2 inhibitors and applications thereof

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Publication number Priority date Publication date Assignee Title
CN108697807A (zh) * 2016-01-11 2018-10-23 辛德弗雷克斯公司 代谢功能障碍引起的肿瘤的治疗
CN108697807B (zh) * 2016-01-11 2021-11-26 辛德弗雷克斯公司 代谢功能障碍引起的肿瘤的治疗

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EP2638023A1 (en) 2013-09-18
JP6239977B2 (ja) 2017-11-29
US8735447B2 (en) 2014-05-27
JP2013543867A (ja) 2013-12-09
US20150018413A1 (en) 2015-01-15
AU2011326566A1 (en) 2013-05-30
MX2013005208A (es) 2013-08-01
US9371312B2 (en) 2016-06-21
NZ610569A (en) 2015-06-26
BR112013011550A2 (pt) 2017-10-24
EA201390675A1 (ru) 2013-08-30
SG190688A1 (en) 2013-07-31
EP2638023B1 (en) 2016-09-07
KR20140009994A (ko) 2014-01-23
CA2817199A1 (en) 2012-05-18
ES2610216T3 (es) 2017-04-26
KR101892768B1 (ko) 2018-08-28
MY177039A (en) 2020-09-03
WO2012064838A1 (en) 2012-05-18
EA029941B1 (ru) 2018-06-29
IL226238B (en) 2019-02-28
CN106905267A (zh) 2017-06-30
US8349891B2 (en) 2013-01-08
AU2011326566B2 (en) 2016-12-01
IL226238A0 (en) 2013-07-31
CA2817199C (en) 2019-01-15
PH12013500934A1 (en) 2022-10-24
US9827221B2 (en) 2017-11-28
US20170087119A1 (en) 2017-03-30
UA111479C2 (uk) 2016-05-10
US20120316233A1 (en) 2012-12-13
US20130197078A1 (en) 2013-08-01

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