CN103635484B - 大环化合物及其制备方法 - Google Patents

大环化合物及其制备方法 Download PDF

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Publication number
CN103635484B
CN103635484B CN201280026793.3A CN201280026793A CN103635484B CN 103635484 B CN103635484 B CN 103635484B CN 201280026793 A CN201280026793 A CN 201280026793A CN 103635484 B CN103635484 B CN 103635484B
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compound
alkyl
added
sanglifehrin
cells
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Chinese (zh)
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CN103635484A (zh
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S·J·摩斯
M·A·格雷戈里
B·威尔金森
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Biotica Technology Ltd
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Biotica Technology Ltd
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Priority claimed from GBGB1105293.3A external-priority patent/GB201105293D0/en
Priority claimed from GBGB1113629.8A external-priority patent/GB201113629D0/en
Priority claimed from GBGB1202060.8A external-priority patent/GB201202060D0/en
Application filed by Biotica Technology Ltd filed Critical Biotica Technology Ltd
Priority to CN201611126823.4A priority Critical patent/CN107417766A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/06—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06—Tripeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/06—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Virology (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Transplantation (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Peptides Or Proteins (AREA)
  • Saccharide Compounds (AREA)
CN201280026793.3A 2011-03-29 2012-03-29 大环化合物及其制备方法 Active CN103635484B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201611126823.4A CN107417766A (zh) 2011-03-29 2012-03-29 大环化合物及其制备方法

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
GB1105293.3 2011-03-29
GBGB1105293.3A GB201105293D0 (en) 2011-03-29 2011-03-29 Novel compounds and methods for their production
GBGB1113629.8A GB201113629D0 (en) 2011-08-08 2011-08-08 Novel compounds and methods for their production
GB1113629.8 2011-08-08
GBGB1202060.8A GB201202060D0 (en) 2012-02-07 2012-02-07 Novel compounds and methods for their production
GB1202060.8 2012-02-07
PCT/GB2012/050707 WO2012131377A1 (en) 2011-03-29 2012-03-29 Macrocyclic compounds and methods for their production

Related Child Applications (1)

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CN103635484B true CN103635484B (zh) 2017-05-10

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BR112012019866A8 (pt) 2010-02-09 2017-12-26 Biotica Tech Limited Composto, uso do mesmo, composição farmacêutica, e, processo para preparar um composto
JO3063B1 (ar) * 2011-03-29 2017-03-15 Neurovive Pharmaceutical Ab مركب مبتكر وطرق لانتاجه
CN103130734A (zh) * 2011-12-01 2013-06-05 上海药明康德新药开发有限公司 一种合成1,2-吗啉盐酸盐的方法
CN105695541B (zh) * 2016-03-10 2019-03-15 苏州华赛生物工程技术有限公司 一种抗生素nvp018中间体的分离纯化方法
KR20180036522A (ko) 2016-09-30 2018-04-09 (주)나노믹스 스틸벤 유도체 및 그 제조 방법
BR112019009903A2 (pt) * 2016-11-18 2019-08-13 Neurovive Pharmaceutical Ab análogo de sangliferina, combinação, composição farmacêutica, e, método para tratamento de um sujeito sofrendo de câncer ou de malignidade de célula-b
CN112410353B (zh) * 2019-08-23 2023-01-24 上海医药工业研究院 一种fkbS基因、含其的基因工程菌及其制备方法和用途
CA3159561A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
IL301298A (en) 2020-09-15 2023-05-01 Revolution Medicines Inc Indole derivatives as RAS inhibitors in cancer therapy
WO2022235870A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Ras inhibitors for the treatment of cancer
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
CN115028681B (zh) * 2022-08-11 2022-11-15 中国科学院微生物研究所 一种降解亲环素a的嵌合体化合物及其制备方法与应用

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US6124453A (en) 1995-07-04 2000-09-26 Novartis Ag Macrolides
EP2124992A2 (en) 2007-01-04 2009-12-02 Debiopharm S.A. Non-immunosuppressive cyclosporin for treatment of ullrich congenital muscular dystrophy
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US8962329B2 (en) 2008-09-24 2015-02-24 Shanghai Institute Of Organic Chemistry, Chinese Academy Of Sciences Gene cluster
BR112012019866A8 (pt) * 2010-02-09 2017-12-26 Biotica Tech Limited Composto, uso do mesmo, composição farmacêutica, e, processo para preparar um composto
WO2011098805A1 (en) * 2010-02-09 2011-08-18 Biotica Technology Limited Sanglifehrin based compounds
WO2011098808A1 (en) * 2010-02-09 2011-08-18 Biotica Technology Limited Sanglifehrin based compounds
EP2654753B1 (en) * 2010-12-20 2018-10-31 Neurovive Pharmaceutical AB Sanglifehrin derivatives and methods for their production
JO3063B1 (ar) * 2011-03-29 2017-03-15 Neurovive Pharmaceutical Ab مركب مبتكر وطرق لانتاجه

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CN101242842A (zh) * 2005-06-17 2008-08-13 诺瓦提斯公司 Sanglifehrin在hcv中的用途

Non-Patent Citations (1)

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Sanglifehrin-Cyclophilin Interaction: Degradation Work, Synthetic Macrocyclic Analogues, X-ray Crystal Structure, and Binding Data;Richard Sedrani et al.;《J. AM. CHEM. SOC.》;20030603;第125卷(第13期);3849-3859 *

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US9090657B2 (en) 2015-07-28
KR101868084B1 (ko) 2018-06-18
TWI525098B (zh) 2016-03-11
CY1116318T1 (el) 2017-02-08
JP2014514290A (ja) 2014-06-19
UY33993A (es) 2012-10-31
MX2013011051A (es) 2014-03-13
EP2691413B1 (en) 2014-12-24
JP2014510746A (ja) 2014-05-01
RS53963B1 (sr) 2015-08-31
PH12013502000A1 (en) 2013-12-02
CL2013002739A1 (es) 2014-07-11
ZA201307149B (en) 2015-04-29
DK2691412T3 (en) 2015-04-07
HK1189237A1 (en) 2014-05-30
MX2013011043A (es) 2014-04-25
CN103619869B (zh) 2015-11-25
CN107417766A (zh) 2017-12-01
PL2691413T3 (pl) 2015-05-29
JP6118793B2 (ja) 2017-04-26
EP2691412A1 (en) 2014-02-05
JO3063B1 (ar) 2017-03-15
JP6118792B2 (ja) 2017-04-26
BR112013024974A2 (pt) 2016-09-06
BR112013024965A2 (pt) 2017-04-18
EA201391399A1 (ru) 2014-02-28
SI2691412T1 (sl) 2015-05-29
HRP20150184T1 (hr) 2015-05-08
CY1116186T1 (el) 2017-02-08
US20140038885A1 (en) 2014-02-06
ES2533438T3 (es) 2015-04-10
IL228508B (en) 2018-01-31
AU2012235961B2 (en) 2016-09-01
KR20140057481A (ko) 2014-05-13
MX345352B (es) 2017-01-26
TW201300398A (zh) 2013-01-01
RS53964B1 (sr) 2015-08-31
CN103619869A (zh) 2014-03-05
ES2533437T3 (es) 2015-04-10
AU2012235880A1 (en) 2013-10-17
CA2830827C (en) 2020-03-10
CN103635484A (zh) 2014-03-12
HRP20150187T1 (xx) 2015-06-05
EA023848B1 (ru) 2016-07-29
PT2691413E (pt) 2015-03-25
CL2013002740A1 (es) 2014-07-11
AU2012235961A1 (en) 2013-10-10
SG193569A1 (en) 2013-11-29
SG193568A1 (en) 2013-11-29
US9139613B2 (en) 2015-09-22
MY170637A (en) 2019-08-21
HK1189236A1 (en) 2014-05-30
IL228509A0 (en) 2013-12-31
KR101911484B1 (ko) 2018-10-24
AR085724A1 (es) 2013-10-23
CA2830827A1 (en) 2012-10-04
IL228509B (en) 2018-02-28
EP2691412B1 (en) 2014-12-24
MX345351B (es) 2017-01-26
ZA201307231B (en) 2015-05-27
AU2012235880B2 (en) 2016-11-17
EA201391396A1 (ru) 2014-02-28
WO2012131377A1 (en) 2012-10-04
KR20140071958A (ko) 2014-06-12
PT2691412E (pt) 2015-03-25
EP2691413A1 (en) 2014-02-05
SI2691413T1 (sl) 2015-05-29
PH12013502016A1 (en) 2013-12-16
DK2691413T3 (en) 2015-04-07
CA2830831A1 (en) 2012-10-04
WO2012131371A1 (en) 2012-10-04
US20120251581A1 (en) 2012-10-04
EA023907B1 (ru) 2016-07-29
MY170618A (en) 2019-08-21
IL228508A0 (en) 2013-12-31
PL2691412T3 (pl) 2015-08-31
PH12013502000B1 (en) 2018-08-10
CA2830831C (en) 2020-03-10

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