KR101732084B1 - 9-아미노메틸 치환된 테트라사이클린 화합물 - Google Patents

9-아미노메틸 치환된 테트라사이클린 화합물 Download PDF

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KR101732084B1
KR101732084B1 KR1020147005035A KR20147005035A KR101732084B1 KR 101732084 B1 KR101732084 B1 KR 101732084B1 KR 1020147005035 A KR1020147005035 A KR 1020147005035A KR 20147005035 A KR20147005035 A KR 20147005035A KR 101732084 B1 KR101732084 B1 KR 101732084B1
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KR20140050694A (ko
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후이 장
얀얀 동
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케이비피 바이오사이언시즈 씨오., 엘티디.
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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
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    • 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
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    • 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
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    • C07D205/00Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
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    • 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
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    • 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
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    • 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D305/00Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms
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    • 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
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    • 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
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00Systems containing two condensed rings
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00Systems containing at least three condensed rings
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    • 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
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    • C07C2603/93Spiro compounds
    • C07C2603/94Spiro compounds containing "free" spiro atoms

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  • 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)
KR1020147005035A 2011-07-26 2012-07-26 9-아미노메틸 치환된 테트라사이클린 화합물 Active KR101732084B1 (ko)

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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KR20140050694A KR20140050694A (ko) 2014-04-29
KR101732084B1 true KR101732084B1 (ko) 2017-05-02

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KR (1) KR101732084B1 (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
KR101660050B1 (ko) 2008-01-04 2016-09-26 인텔리카인, 엘엘씨 특정 화학 물질, 조성물 및 방법
NZ612909A (en) 2011-01-10 2015-09-25 Infinity Pharmaceuticals Inc Processes for preparing isoquinolinones and solid forms of isoquinolinones
CN103717571B8 (zh) 2011-07-26 2017-05-17 山东亨利医药科技有限责任公司 9‑氨基甲基取代的四环素类化合物
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
PL2914296T5 (pl) 2012-11-01 2022-01-17 Infinity Pharmaceuticals, Inc. Leczenie nowotworu z zastosowaniem modulatorów izoform kinazy PI3
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
MX381701B (es) * 2016-06-22 2025-03-13 Kbp Biosciences Co Ltd Formas cristalinas de un compuesto de tetraciclina sustituido con 9-aminometilo y un metodo para la preparacion de las mismas
IL263680B1 (en) 2016-06-24 2025-06-01 Infinity Pharmaceuticals Inc Pi3k inhibitors for use in combination with a second therapeutic agent in treating, managing, or preventing cancer
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
AU2019335203B2 (en) 2018-09-04 2025-06-19 Paratek Pharmaceuticals, Inc. Methods of treating mycobacterial infections using tetracycline compounds
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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DK1679305T3 (da) 2000-07-07 2012-05-29 Tufts College 9-substituerede minocyclinforbindelser
WO2003007587A2 (en) * 2001-07-13 2003-01-23 Centillium Communications, Inc. Application of metering tones to a dsl and voice communications system
CN101307017A (zh) 2002-03-08 2008-11-19 帕拉特克药品公司 氨基-甲基取代的四环素类化合物
CA2502464A1 (en) * 2002-10-24 2004-05-06 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds for the treatment of malaria
WO2004064728A2 (en) 2003-01-16 2004-08-05 Paratek Pharmaceuticals, Inc. Use of specific tetracycline compounds in therapy
EP2298322A3 (en) * 2003-07-09 2011-05-11 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds
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
CN103717571B8 (zh) 2011-07-26 2017-05-17 山东亨利医药科技有限责任公司 9‑氨基甲基取代的四环素类化合物

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CN103717571B8 (zh) 2017-05-17
WO2013013505A1 (zh) 2013-01-31
PT2738156T (pt) 2018-03-28
HK1191931A1 (zh) 2014-08-08
CA2842838C (en) 2017-04-25
JP2014529342A (ja) 2014-11-06
NO2738156T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 2018-06-02
CA2842838A1 (en) 2013-01-31
ES2664516T3 (es) 2018-04-19
CN103717571B (zh) 2016-01-13
HUE036696T2 (hu) 2018-07-30
LT2738156T (lt) 2018-05-25
SI2738156T1 (en) 2018-05-31
DK2738156T3 (en) 2018-03-26
JP5792902B2 (ja) 2015-10-14
EP2738156B1 (en) 2018-01-03
US20140179638A1 (en) 2014-06-26
PL2738156T3 (pl) 2018-06-29
KR20140050694A (ko) 2014-04-29
HRP20180444T1 (hr) 2018-05-04
BR112014001798B1 (pt) 2021-07-27
BR112014001798A2 (pt) 2017-02-21
CN103717571A (zh) 2014-04-09
EP2738156A1 (en) 2014-06-04
EP2738156A4 (en) 2015-01-07
US9365499B2 (en) 2016-06-14

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