JP5792902B2 - 9−アミノメチルで置換されたテトラサイクリン系化合物 - Google Patents

9−アミノメチルで置換されたテトラサイクリン系化合物 Download PDF

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JP5792902B2
JP5792902B2 JP2014521914A JP2014521914A JP5792902B2 JP 5792902 B2 JP5792902 B2 JP 5792902B2 JP 2014521914 A JP2014521914 A JP 2014521914A JP 2014521914 A JP2014521914 A JP 2014521914A JP 5792902 B2 JP5792902 B2 JP 5792902B2
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alkyl
membered
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ring group
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JP2014529342A (ja
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▲けい▼ 張
▲けい▼ 張
岩岩 董
岩岩 董
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山東亨利醫藥科技有限責任公司
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/24Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
    • C07C237/26Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/65Tetracyclines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/655Azo (—N=N—), diazo (=N2), azoxy (>N—O—N< or N(=O)—N<), azido (—N3) or diazoamino (—N=N—N<) compounds
    • 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
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00Preparation of carboxylic acid amides
    • C07C231/12Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/42Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/66Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings being part of condensed ring systems and singly-bound oxygen atoms, bound to the same carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D205/00Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D205/00Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/12Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/52Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/54Spiro-condensed
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D221/00Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/20Spiro-condensed ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D221/00Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/22Bridged ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D305/00Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms
    • C07D305/02Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D305/04Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D305/06Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/04Systems containing only non-condensed rings with a four-membered ring
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00Systems containing two condensed rings
    • C07C2602/36Systems containing two condensed rings the rings having more than two atoms in common
    • C07C2602/40Systems containing two condensed rings the rings having more than two atoms in common the bicyclo ring system containing six carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00Systems containing at least three condensed rings
    • C07C2603/02Ortho- or ortho- and peri-condensed systems
    • C07C2603/40Ortho- or ortho- and peri-condensed systems containing four condensed rings
    • C07C2603/42Ortho- or ortho- and peri-condensed systems containing four condensed rings containing only six-membered rings
    • C07C2603/44Naphthacenes; Hydrogenated naphthacenes
    • C07C2603/461,4,4a,5,5a,6,11,12a- Octahydronaphthacenes, e.g. tetracyclines
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00Systems containing at least three condensed rings
    • C07C2603/93Spiro compounds
    • C07C2603/94Spiro compounds containing "free" spiro atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Indole Compounds (AREA)
JP2014521914A 2011-07-26 2012-07-26 9−アミノメチルで置換されたテトラサイクリン系化合物 Active JP5792902B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201110222016 2011-07-26
CN201110222016.3 2011-07-26
PCT/CN2012/001001 WO2013013505A1 (zh) 2011-07-26 2012-07-26 9-氨基甲基取代的四环素类化合物

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JP2014529342A JP2014529342A (ja) 2014-11-06
JP5792902B2 true JP5792902B2 (ja) 2015-10-14

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US (1) US9365499B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
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JP (1) JP5792902B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
KR (1) KR101732084B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CN (1) CN103717571B8 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
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US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
MX2010007419A (es) 2008-01-04 2010-11-12 Intellikine Inc Ciertas entidades quimicas, composiciones y metodos.
BR112013017670B1 (pt) 2011-01-10 2022-07-19 Infinity Pharmaceuticals, Inc Processos de preparação de isoquinolinonas e formas sólidas de isoquinolinonas
DK2738156T3 (en) 2011-07-26 2018-03-26 Kbp Biosciences Usa Inc 9-AMINOMETHYL SUBSTITUTED TETRACYCLINE COMPOUNDS
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
RS58023B2 (sr) 2012-11-01 2021-12-31 Infinity Pharmaceuticals Inc Lečenje kancera korišćenjem modulatora izoformi pi3 kinaza
CN103073481A (zh) * 2013-02-06 2013-05-01 上海药明康德新药开发有限公司 一种4-氮杂螺[2.4]庚烷盐酸盐的制备方法
US9580758B2 (en) 2013-11-12 2017-02-28 Luc Montagnier System and method for the detection and treatment of infection by a microbial agent associated with HIV infection
WO2015160975A2 (en) 2014-04-16 2015-10-22 Infinity Pharmaceuticals, Inc. Combination therapies
CN105384673B (zh) * 2015-11-09 2017-11-14 南京富润凯德生物医药有限公司 3‑氟代‑氮杂环丁烷衍生物的合成方法
TWI656116B (zh) * 2016-06-22 2019-04-11 山東亨利醫藥科技有限責任公司 Crystal form of 9-aminomethyl substituted tetracycline compound and preparation method thereof
MX391135B (es) 2016-06-24 2025-03-21 Infinity Pharmaceuticals Inc Terapias de combinacion.
CN106883138B (zh) * 2017-03-01 2018-07-10 郑州大学第一附属医院 老虎素的制备方法
WO2019192614A1 (en) * 2018-04-06 2019-10-10 Paratek Pharmaceuticals, Inc. Process for making sarecycline hydrochloride
KR20210090160A (ko) 2018-09-04 2021-07-19 파라테크 파마슈티컬스, 인크. 테트라시클린 화합물을 사용하여 미코박테리아 감염을 치료하는 방법
CN115057775A (zh) * 2022-07-22 2022-09-16 临海市建新化工有限公司 一种2,2-二甲基丙二酸二甲酯的制备方法

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US20030012352A1 (en) * 2001-07-13 2003-01-16 Serdar Kiykioglu Application of metering tones to a DSL and voice communications network
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ES2463457T3 (es) 2006-12-21 2014-05-28 Paratek Pharmaceuticals, Inc. Derivados de la tetraciclina para el tratamiento de infecciones bacterianas, virales y parasitarias
CN101759604A (zh) 2008-09-12 2010-06-30 山东轩竹医药科技有限公司 胍基取代的四环素衍生物
DK2738156T3 (en) 2011-07-26 2018-03-26 Kbp Biosciences Usa Inc 9-AMINOMETHYL SUBSTITUTED TETRACYCLINE COMPOUNDS

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CN103717571B (zh) 2016-01-13
BR112014001798B1 (pt) 2021-07-27
PL2738156T3 (pl) 2018-06-29
CA2842838A1 (en) 2013-01-31
CN103717571A (zh) 2014-04-09
EP2738156A4 (en) 2015-01-07
LT2738156T (lt) 2018-05-25
HRP20180444T1 (hr) 2018-05-04
HUE036696T2 (hu) 2018-07-30
PT2738156T (pt) 2018-03-28
EP2738156B1 (en) 2018-01-03
DK2738156T3 (en) 2018-03-26
WO2013013505A1 (zh) 2013-01-31
SI2738156T1 (en) 2018-05-31
US9365499B2 (en) 2016-06-14
HK1191931A1 (zh) 2014-08-08
ES2664516T3 (es) 2018-04-19
EP2738156A1 (en) 2014-06-04
US20140179638A1 (en) 2014-06-26
CN103717571B8 (zh) 2017-05-17
JP2014529342A (ja) 2014-11-06
CA2842838C (en) 2017-04-25
KR101732084B1 (ko) 2017-05-02
KR20140050694A (ko) 2014-04-29
BR112014001798A2 (pt) 2017-02-21
NO2738156T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 2018-06-02

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