CN108290853B - 烟曲霉醇衍生物及其多晶型物 - Google Patents

烟曲霉醇衍生物及其多晶型物 Download PDF

Info

Publication number
CN108290853B
CN108290853B CN201680072272.XA CN201680072272A CN108290853B CN 108290853 B CN108290853 B CN 108290853B CN 201680072272 A CN201680072272 A CN 201680072272A CN 108290853 B CN108290853 B CN 108290853B
Authority
CN
China
Prior art keywords
trans
formula
aminocyclohexyl
aspergillus fumigatus
polymorph
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
CN201680072272.XA
Other languages
English (en)
Chinese (zh)
Other versions
CN108290853A (zh
Inventor
J.S.彼得森
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
SynDevRX Inc
Original Assignee
SynDevRX Inc
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 SynDevRX Inc filed Critical SynDevRX Inc
Publication of CN108290853A publication Critical patent/CN108290853A/zh
Application granted granted Critical
Publication of CN108290853B publication Critical patent/CN108290853B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic 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
    • C07D407/02—Heterocyclic 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
    • C07D407/08—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
    • C07D303/02—Compounds containing oxirane rings
    • C07D303/12—Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms
    • C07D303/18—Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by etherified hydroxyl radicals
    • C07D303/31—Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by etherified hydroxyl radicals in which the oxirane rings are condensed with a carbocyclic ring system having three or more relevant rings
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/336—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
    • 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
    • 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
    • C07C309/28—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
    • C07D303/02—Compounds containing oxirane rings
    • C07D303/38—Compounds containing oxirane rings with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D303/46—Compounds containing oxirane rings with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals by amide or nitrile radicals
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Epoxy Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
CN201680072272.XA 2015-12-10 2016-12-09 烟曲霉醇衍生物及其多晶型物 Active CN108290853B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562265675P 2015-12-10 2015-12-10
US62/265675 2015-12-10
PCT/US2016/065799 WO2017100553A1 (en) 2015-12-10 2016-12-09 Fumagillol derivatives and polymorphs thereof

Publications (2)

Publication Number Publication Date
CN108290853A CN108290853A (zh) 2018-07-17
CN108290853B true CN108290853B (zh) 2022-05-31

Family

ID=57589276

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201680072272.XA Active CN108290853B (zh) 2015-12-10 2016-12-09 烟曲霉醇衍生物及其多晶型物

Country Status (11)

Country Link
US (2) US9969722B2 (enExample)
EP (1) EP3386956B1 (enExample)
JP (2) JP7553224B2 (enExample)
KR (2) KR102849342B1 (enExample)
CN (1) CN108290853B (enExample)
AU (1) AU2016366306B2 (enExample)
CA (1) CA3005450A1 (enExample)
DK (1) DK3386956T3 (enExample)
ES (1) ES2893749T3 (enExample)
MX (2) MX2018006904A (enExample)
WO (1) WO2017100553A1 (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3858385B1 (en) 2010-05-25 2024-09-11 Syndevrx, Inc. Polymer-conjugated metap2 inhibitors, and therapeutic methods of use thereof
MX371095B (es) 2013-04-10 2020-01-16 Syndevrx Inc Inhibidores de metionina aminopeptidasa-2 y metodos de tratamiento de la obesidad.
CN108290853B (zh) * 2015-12-10 2022-05-31 辛德弗雷克斯公司 烟曲霉醇衍生物及其多晶型物
CA3008960C (en) 2016-01-11 2024-07-02 Syndevrx, Inc. TREATMENT OF TUMORS INDUCED BY METABOLIC DYSFUNCTION
EP3870231A1 (en) 2018-10-26 2021-09-01 Syndevrx, Inc. Biomarkers of metap2 inhibitors and applications thereof
WO2024040009A2 (en) * 2022-08-17 2024-02-22 Primetime Life Sciences, Llc Inhibitors of methionine aminopeptidase-2 and methods of preparation and uses thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103140512A (zh) * 2010-05-25 2013-06-05 辛德弗雷克斯公司 聚合物缀合的MetAP2抑制剂及其应用的治疗方法
WO2014169026A1 (en) * 2013-04-10 2014-10-16 Syndevrx, Inc. Metap2 inhibitors and methods of treating obesity
CN104364251A (zh) * 2012-05-09 2015-02-18 扎夫根股份有限公司 烟曲霉醇型化合物及其制备和使用方法

Family Cites Families (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8500209D0 (en) 1985-01-04 1985-02-13 Ceskoslovenska Akademie Ved Synthetic polymeric drugs
SE8702550D0 (sv) 1987-06-18 1987-06-18 Anders Grubb Cysteinproteashemmare
US5166172A (en) 1988-09-01 1992-11-24 Takeda Chemical Industries, Ltd. Fumagillol derivatives and pharmaceutical compositions thereof
US4997878A (en) 1988-12-29 1991-03-05 Exxon Research And Engineering Company Hydrophobically associating polymers containing dimethyl acrylamide functionality
US5258453A (en) 1992-01-21 1993-11-02 University Of Utah Drug delivery system for the simultaneous delivery of drugs activatable by enzymes and light
GB9320781D0 (en) 1993-10-08 1993-12-01 Erba Carlo Spa Polymer-bound camptothecin derivatives
US20030220233A1 (en) 1994-01-24 2003-11-27 Neorx Corporation Radiolabeled annexins
TW527183B (en) 1996-06-06 2003-04-11 Daiichi Seiyaku Co Drug complex
TW409058B (en) 1996-06-06 2000-10-21 Daiichi Seiyaku Co Method for preparation of a drug complex
US6759509B1 (en) 1996-11-05 2004-07-06 Bristol-Myers Squibb Company Branched peptide linkers
AU9376998A (en) 1997-09-02 1999-03-22 Johns Hopkins University School Of Medicine, The Vitamin d3 analog loaded polymer formulations for cancer and neurodegenerative disorders
AU3352799A (en) 1997-10-31 1999-08-23 Children's Medical Center Corporation Method for regulating size and growth of vascularized normal tissue
KR100357542B1 (ko) 1998-05-15 2002-10-18 주식회사종근당 푸마질롤 유도체 및 그 제조방법
EA003398B1 (ru) 1998-05-22 2003-04-24 Дайити Фармасьютикал Ко., Лтд. Лекарственный комплекс c полимерным носителем
US6464850B1 (en) 1998-07-31 2002-10-15 Biowhittaker Molecular Applications, Inc. Method for producing hydrophilic monomers and uses thereof
EP1155702A4 (en) 1998-10-30 2004-12-15 Daiichi Seiyaku Co DDS CONNECTIONS AND TEST METHODS
WO2001018080A1 (en) 1999-09-08 2001-03-15 School Of Pharmacy, University Of London Uniform molecular weight polymers
US6811788B2 (en) 2000-01-19 2004-11-02 Baofa Yu Combinations and methods for treating neoplasms
US6548477B1 (en) 2000-11-01 2003-04-15 Praecis Pharmaceuticals Inc. Therapeutic agents and methods of use thereof for the modulation of angiogenesis
US20070161570A1 (en) 2000-11-01 2007-07-12 Praecis Pharmaceuticals, Inc. Methionine aminopeptidase-2 inhibitors and methods of use thereof
EP1243276A1 (en) 2001-03-23 2002-09-25 Franciscus Marinus Hendrikus De Groot Elongated and multiple spacers containing activatible prodrugs
US7091186B2 (en) 2001-09-24 2006-08-15 Seattle Genetics, Inc. p-Amidobenzylethers in drug delivery agents
US7087768B2 (en) 2001-09-27 2006-08-08 Equispharm Co., Ltd. Fumagillol derivatives and preparing method thereof
WO2003070173A2 (en) 2002-02-15 2003-08-28 Sympore Gmbh Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof
AU2003230852B2 (en) 2002-04-11 2008-07-10 Children's Medical Center Corporation TNP-470 polymer conjugates and use thereof
US20040001801A1 (en) 2002-05-23 2004-01-01 Corvas International, Inc. Conjugates activated by cell surface proteases and therapeutic uses thereof
US20040116348A1 (en) 2002-09-23 2004-06-17 Ying Chau Polymer-linker-drug conjugates for targeted drug delivery
US20040228831A1 (en) 2003-05-15 2004-11-18 Belinka Benjamin A. Polymeric conjugates for tissue activated drug delivery
JP4682152B2 (ja) 2003-12-31 2011-05-11 ザ・ペン・ステート・リサーチ・ファンデーション 卵巣がんの化学療法に対する抵抗性を予測および克服するための方法ならびに結腸がんの発生を予測するための方法
US20070287680A1 (en) 2004-05-10 2007-12-13 University Of Utah Research Foundation Combined Active and Passive Targeting of Biologically Active Agents
US7214664B2 (en) 2004-12-03 2007-05-08 The Curators Of The University Of Missouri Peptidyl prodrugs that resist P-glycoprotein mediated drug efflux
WO2006084054A2 (en) 2005-02-02 2006-08-10 Children's Medical Center Corporation Method of treating angiogenic diseases
US7629315B2 (en) 2005-03-09 2009-12-08 University Of Pittsburgh Of The Commonwealth System Of Higher Education Compositions for blocking the inhibitory effect of human CRP on human leptin
WO2006124711A1 (en) 2005-05-16 2006-11-23 The Board Of Trustees Of The University Of Illinois Composition and method for providing localized delivery of a therapeutic agent
WO2009003110A2 (en) 2007-06-26 2008-12-31 Children's Medical Center Corporation Metap-2 inhibitor polymersomes for therapeutic administration
WO2009036108A1 (en) 2007-09-13 2009-03-19 Children's Medical Center Corporation Methods and compositions for inhibiting vascular leakage
US20090104210A1 (en) 2007-10-17 2009-04-23 Tota Michael R Peptide compounds for treating obesity and insulin resistance
NZ585547A (en) 2007-11-28 2012-12-21 Mersana Therapeutics Inc Biocompatible biodegradable fumagillin analog conjugates
US20100298371A1 (en) 2007-12-04 2010-11-25 Mayank Ghanshyambhai Dave Process for preparing chemically and chirally pure solifenacin base and its salts
EP2244712B1 (en) 2008-01-22 2015-08-05 Thar Pharmaceuticals Inc. In vivo studies of crystalline forms of meloxicam
CN102105156B (zh) 2008-05-22 2016-05-25 特拉维夫大学拉莫特有限公司 连接有治疗活性剂和血管生成靶向部分的聚合物的新型缀合物及其在治疗血管生成相关疾病中的用途
DE102008027574A1 (de) 2008-06-10 2009-12-17 Merck Patent Gmbh Neue Pyrrolidinderivate als MetAP-2 Inhibitoren
WO2010065877A2 (en) 2008-12-04 2010-06-10 Zafgen Corporation Methods of treating an overweight or obese subject
US8642650B2 (en) 2008-12-04 2014-02-04 Zafgen, Inc. Methods of treating an overweight or obese subject
TWI373345B (en) 2009-02-19 2012-10-01 Academia Sinica Breast cancer-targeting peptides and use thereof
EP2493497A4 (en) 2009-11-01 2013-07-24 Brigham & Womens Hospital NOTCH INHIBITION IN THE TREATMENT AND PROPHYLAXIS OF ADIPOSITAS AND METABOLISM SYNDROME
WO2011127304A2 (en) 2010-04-07 2011-10-13 Zafgen Corporation Methods of treating an overweight subject
US9895449B2 (en) 2010-05-25 2018-02-20 Syndevrx, Inc. Polymer-conjugated MetAP2 inhibitors, and therapeutic methods of use thereof
EP2575887A4 (en) 2010-05-25 2015-01-14 SynDevRX CONJUGATES OF OPTIMIZED MEDICINES
PH12013500934A1 (en) 2010-11-09 2022-10-24 Zafgen Inc Crystalline solids of a metap-2 inhibitor and methods of making and using same
JP5876513B2 (ja) 2011-03-08 2016-03-02 ザフゲン，インコーポレイテッド オキサスピロ［２．５］オクタン誘導体および類似体
CN108290853B (zh) * 2015-12-10 2022-05-31 辛德弗雷克斯公司 烟曲霉醇衍生物及其多晶型物
CA3008960C (en) 2016-01-11 2024-07-02 Syndevrx, Inc. TREATMENT OF TUMORS INDUCED BY METABOLIC DYSFUNCTION

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103140512A (zh) * 2010-05-25 2013-06-05 辛德弗雷克斯公司 聚合物缀合的MetAP2抑制剂及其应用的治疗方法
CN104364251A (zh) * 2012-05-09 2015-02-18 扎夫根股份有限公司 烟曲霉醇型化合物及其制备和使用方法
WO2014169026A1 (en) * 2013-04-10 2014-10-16 Syndevrx, Inc. Metap2 inhibitors and methods of treating obesity

Also Published As

Publication number Publication date
MX2018006904A (es) 2018-08-24
AU2016366306A1 (en) 2018-05-31
CN108290853A (zh) 2018-07-17
HK1258254A1 (zh) 2019-11-08
EP3386956A1 (en) 2018-10-17
JP2024103495A (ja) 2024-08-01
KR20250127347A (ko) 2025-08-26
US20180291010A1 (en) 2018-10-11
CA3005450A1 (en) 2017-06-15
JP7553224B2 (ja) 2024-09-18
US10287277B2 (en) 2019-05-14
MX2023002589A (es) 2023-03-22
KR20180093995A (ko) 2018-08-22
WO2017100553A1 (en) 2017-06-15
US9969722B2 (en) 2018-05-15
US20170166556A1 (en) 2017-06-15
AU2016366306B2 (en) 2021-02-25
DK3386956T3 (da) 2021-10-11
KR102849342B1 (ko) 2025-08-21
JP2019501898A (ja) 2019-01-24
ES2893749T3 (es) 2022-02-10
EP3386956B1 (en) 2021-07-14

Similar Documents

Publication Publication Date Title
CN108290853B (zh) 烟曲霉醇衍生物及其多晶型物
EP3710465B1 (en) Salts and crystal forms of gabaa positive allosteric modulator
EP2603503B1 (en) Dabigatran etexilate bismesylate salt, solid state forms and process for preparation thereof
KR20230021075A (ko) 베타 아드레날린성 작용제의 형태 및 조성물
HK1258254B (en) Fumagillol derivatives and polymorphs thereof
CN112739686A (zh) 用于制备(-)-西苯唑啉琥珀酸盐的新方法
CN115003657B (zh) (-)-琥珀酸西苯唑啉的多晶型
US11384073B2 (en) Maleate salt of benzothiophene compound, crystalline form thereof, and use thereof
AU2006218132B2 (en) Phosphate salts of 6-dimethylaminomethyl-l-(3-methoxyphenyl) -1,3-dihydroxycyclohexane compounds
CN112830919B (zh) 苯并哌啶衍生物可药用盐及其制备方法
US20060211887A1 (en) Phosphate salts of 6-dimethylaminomethyl-1-(3-methoxyphenyl)-1,3-dihydroxy-cyclohexane compounds
CN112300076B (zh) 一种雄性激素受体抑制剂的晶型及其制备方法
HK40037178A (en) Salts and crystal forms of gabaa positive allosteric modulator
HK40037178B (en) Salts and crystal forms of gabaa positive allosteric modulator
HK40043660A (en) Novel method for preparing (-)-cibenzoline succinate
CN113929630A (zh) 一种吉非替尼药物共晶体
AU2018264079A1 (en) New benzimidazole derivatives as dual histamine H1 and histamine H4 receptor ligands
KR20190005679A (ko) 1-[2-(2,4-디메틸페닐설파닐)페닐]피페라진의 신규염 및 이의 제조방법
WO2015067223A1 (en) L-tartrate salt of (1s,3s,5s)-2-[(2s)-2-amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl) acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile and process for preparation thereof
CZ304576B6 (cs) Oxalát TAPENTADOLU a způsob jeho přípravy

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1258254

Country of ref document: HK

GR01 Patent grant
GR01 Patent grant