TWI797249B - 新生黴素（ｎｏｖｏｂｉｏｃｉｎ）類似物及脯胺酸之共晶型、其製造方法及用途 - Google Patents

新生黴素（ｎｏｖｏｂｉｏｃｉｎ）類似物及脯胺酸之共晶型、其製造方法及用途 Download PDF

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TWI797249B
TWI797249B TW108104336A TW108104336A TWI797249B TW I797249 B TWI797249 B TW I797249B TW 108104336 A TW108104336 A TW 108104336A TW 108104336 A TW108104336 A TW 108104336A TW I797249 B TWI797249 B TW I797249B
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proline
crystal
powder diffraction
ray powder
diffraction pattern
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TW108104336A
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TW201945381A (zh
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江昕
約翰 艾倫 威林
梅蘭妮 Ｊ 畢菲
克里斯多夫 Ｓ 希迪克
傑瑞德 Ｐ 斯密特
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美商瑞塔醫藥有限責任公司
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20—Carbocyclic rings
    • C07H15/207—Cyclohexane rings not substituted by nitrogen atoms, e.g. kasugamycins
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/401—Proline; Derivatives thereof, e.g. captopril
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives
    • C07H1/06—Separation; Purification
    • 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
    • C07B2200/07—Optical isomers
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyrane Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
TW108104336A 2018-02-07 2019-02-01 新生黴素（ｎｏｖｏｂｉｏｃｉｎ）類似物及脯胺酸之共晶型、其製造方法及用途 TWI797249B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862627570P 2018-02-07 2018-02-07
US62/627,570 2018-02-07

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TW201945381A TW201945381A (zh) 2019-12-01
TWI797249B true TWI797249B (zh) 2023-04-01

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TW108104336A TWI797249B (zh) 2018-02-07 2019-02-01 新生黴素（ｎｏｖｏｂｉｏｃｉｎ）類似物及脯胺酸之共晶型、其製造方法及用途
TW112106332A TWI868593B (zh) 2018-02-07 2019-02-01 新生黴素（novobiocin）類似物及脯胺酸之共晶型及其用途

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TW112106332A TWI868593B (zh) 2018-02-07 2019-02-01 新生黴素（novobiocin）類似物及脯胺酸之共晶型及其用途

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US (3) US10717755B2 (https=)
EP (1) EP3749675B1 (https=)
JP (3) JP2021512910A (https=)
KR (2) KR20240155354A (https=)
CN (2) CN112020506B (https=)
AR (1) AR114245A1 (https=)
AU (3) AU2019217821B2 (https=)
BR (1) BR112020016205A2 (https=)
CA (2) CA3226385A1 (https=)
CL (2) CL2020002051A1 (https=)
CO (1) CO2020009761A2 (https=)
EA (1) EA202091885A1 (https=)
IL (2) IL276583B2 (https=)
MX (2) MX2020008326A (https=)
MY (1) MY209803A (https=)
PE (1) PE20211446A1 (https=)
SG (1) SG11202007530XA (https=)
TW (2) TWI797249B (https=)
WO (1) WO2019156907A1 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3749675B1 (en) 2018-02-07 2025-12-31 Reata Pharmaceuticals, Inc. CO-CRISTALLIN FORMS OF A NOVOBIOCIN AND PROLINE ANALOGUE
MY204234A (en) 2018-08-27 2024-08-16 Regeneron Pharma Use of raman spectroscopy in downstream purification
CN115181146B (zh) * 2021-04-02 2024-06-04 浙江普洛家园药业有限公司 一种新生霉素的提取工艺

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013537901A (ja) * 2010-09-23 2013-10-07 ナフォーミックス リミテッド アプレピタントｌ−プロリン組成物および共結晶
TW201414745A (zh) * 2012-08-31 2014-04-16 Novartis Ag 用於治療病毒感染的２’－支鏈核苷
US9422320B2 (en) * 2012-02-09 2016-08-23 University Of Kansas C-terminal HSP90 inhibitors
CN106536498A (zh) * 2014-06-24 2017-03-22 堪萨斯大学 作为hsp90抑制剂和hsp70诱导剂的具有经修饰醚基的联苯酰胺

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TWI542596B (zh) * 2011-05-09 2016-07-21 健生藥品公司 （２ｓ,３ｒ,４ｒ,５ｓ,６ｒ）－２－（３－（（５－（４－氟苯基）噻吩－２－基）甲基）－４－甲基苯基）－６－（羥甲基）四氫－２ｈ－哌喃－３,４,５－三醇之ｌ－脯胺酸及檸檬酸共晶體
CA2892832C (en) * 2011-11-25 2020-04-14 Nuformix Technologies Limited Aprepitant l-proline solvates - compositions and cocrystals
EP2602249B1 (en) * 2011-12-06 2015-08-12 F.I.S. Fabbrica Italiana Sintetici S.p.A. Synthesis of rosuvastatin by means of co-crystals
TW201512201A (zh) * 2013-03-14 2015-04-01 Forum Pharmaceuticals Inc 化合物的多晶型及鹽類
KR20170060035A (ko) * 2014-09-30 2017-05-31 지앙수 헨그루이 메디슨 컴퍼니 리미티드 나트륨 글루코스 공동운반체 2 억제제의 ｌ- 프롤린 화합물, 및 ｌ- 프롤린 화합물의 모노하이드레이트 및 결정
EP3749675B1 (en) 2018-02-07 2025-12-31 Reata Pharmaceuticals, Inc. CO-CRISTALLIN FORMS OF A NOVOBIOCIN AND PROLINE ANALOGUE

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013537901A (ja) * 2010-09-23 2013-10-07 ナフォーミックス リミテッド アプレピタントｌ−プロリン組成物および共結晶
US9422320B2 (en) * 2012-02-09 2016-08-23 University Of Kansas C-terminal HSP90 inhibitors
TW201414745A (zh) * 2012-08-31 2014-04-16 Novartis Ag 用於治療病毒感染的２’－支鏈核苷
CN106536498A (zh) * 2014-06-24 2017-03-22 堪萨斯大学 作为hsp90抑制剂和hsp70诱导剂的具有经修饰醚基的联苯酰胺

Non-Patent Citations (1)

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Title
期刊 Bhaskar Reddy Kusuma, Liang Zhang, Teather Sundstrom, Laura B. Peterson, Rick T. Dobrowsky, and Brian S. J. Blagg Synthesis and Evaluation of Novologues as C-Terminal Hsp90 Inhibitors with Cytoprotective Activity against Sensory Neuron Glucotoxicity J. Med. Chem 2012, 55, 12 Publication Date:June 15, 2012 P5797–5812 *

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TWI868593B (zh) 2025-01-01
IL276583A (en) 2020-09-30
JP2026012851A (ja) 2026-01-27
US11401294B2 (en) 2022-08-02
EA202091885A1 (ru) 2021-01-15
AU2022283638B2 (en) 2024-07-25
CA3226385A1 (en) 2019-08-15
CN112020506A (zh) 2020-12-01
IL315865A (en) 2024-11-01
US20190241599A1 (en) 2019-08-08
MY209803A (en) 2025-08-05
MX2022012856A (es) 2022-11-30
SG11202007530XA (en) 2020-09-29
CN112020506B (zh) 2024-10-11
AU2022283638A1 (en) 2023-02-02
PE20211446A1 (es) 2021-08-05
MX2020008326A (es) 2020-09-28
CL2022003784A1 (es) 2023-06-09
CL2020002051A1 (es) 2021-02-19
NZ767558A (en) 2024-11-29
AR114245A1 (es) 2020-08-12
IL276583B1 (en) 2024-11-01
JP2021512910A (ja) 2021-05-20
EP3749675B1 (en) 2025-12-31
US20240043465A1 (en) 2024-02-08
KR102718111B1 (ko) 2024-10-17
US10717755B2 (en) 2020-07-21
WO2019156907A1 (en) 2019-08-15
BR112020016205A2 (pt) 2020-12-15
CA3090646C (en) 2024-02-27
TW201945381A (zh) 2019-12-01
JP2024001167A (ja) 2024-01-09
AU2019217821B2 (en) 2022-09-08
AU2024227646A1 (en) 2024-11-14
CO2020009761A2 (es) 2020-10-30
CN118894894A (zh) 2024-11-05
KR20200141985A (ko) 2020-12-21
TW202323267A (zh) 2023-06-16
AU2019217821A1 (en) 2020-09-24
EP3749675A1 (en) 2020-12-16
KR20240155354A (ko) 2024-10-28
CA3090646A1 (en) 2019-08-15
US20200347088A1 (en) 2020-11-05
IL276583B2 (en) 2025-03-01
TW202510893A (zh) 2025-03-16

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