KR102141323B1 - 염화물 함량이 조절된 아나모렐린 염산염의 제조 방법 - Google Patents

염화물 함량이 조절된 아나모렐린 염산염의 제조 방법 Download PDF

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KR102141323B1
KR102141323B1 KR1020197011485A KR20197011485A KR102141323B1 KR 102141323 B1 KR102141323 B1 KR 102141323B1 KR 1020197011485 A KR1020197011485 A KR 1020197011485A KR 20197011485 A KR20197011485 A KR 20197011485A KR 102141323 B1 KR102141323 B1 KR 102141323B1
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anamorelin
composition
anamorelin monohydrochloride
monohydrochloride
item
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KR20190044697A (ko
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신 이츠 쿠와베
타케히코 야나기마치
히데유키 요시야마
씨몬 파인스
그루트 엘리노어 데
루비오 실비나 가르시아
피터 마니니
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헬신 헬스케어 에스아
오노 야꾸힝 고교 가부시키가이샤
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05Dipeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682Processes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Child & Adolescent Psychology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Polysaccharides And Polysaccharide Derivatives (AREA)
KR1020197011485A 2012-04-20 2013-04-18 염화물 함량이 조절된 아나모렐린 염산염의 제조 방법 Active KR102141323B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261636108P 2012-04-20 2012-04-20
US61/636,108 2012-04-20
PCT/US2013/037159 WO2013158874A1 (en) 2012-04-20 2013-04-18 Methods of producing anamorelin hydrochloride having controlled chloride content

Related Parent Applications (1)

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KR1020147018116A Division KR101972998B1 (ko) 2012-04-20 2013-04-18 염화물 함량이 조절된 아나모렐린 염산염의 제조 방법

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KR20190044697A KR20190044697A (ko) 2019-04-30
KR102141323B1 true KR102141323B1 (ko) 2020-08-05

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KR1020197011485A Active KR102141323B1 (ko) 2012-04-20 2013-04-18 염화물 함량이 조절된 아나모렐린 염산염의 제조 방법
KR1020147018116A Active KR101972998B1 (ko) 2012-04-20 2013-04-18 염화물 함량이 조절된 아나모렐린 염산염의 제조 방법

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US (8) US20140018391A1 (https=)
EP (3) EP2838892B1 (https=)
JP (3) JP6109925B2 (https=)
KR (2) KR102141323B1 (https=)
CN (3) CN110041304A (https=)
AP (1) AP2014008013A0 (https=)
AR (1) AR090725A1 (https=)
AU (1) AU2013249197B2 (https=)
BR (1) BR112014025972A8 (https=)
CA (2) CA2869893C (https=)
CL (1) CL2014002817A1 (https=)
CO (1) CO7131356A2 (https=)
CR (1) CR20140530A (https=)
CY (1) CY1120276T1 (https=)
DK (2) DK3517532T3 (https=)
DO (1) DOP2014000235A (https=)
EA (1) EA031581B1 (https=)
EC (1) ECSP14027739A (https=)
ES (2) ES2658862T3 (https=)
GE (2) GEP20186902B (https=)
HK (1) HK1248694A1 (https=)
HR (1) HRP20180316T1 (https=)
HU (2) HUE050865T2 (https=)
IL (1) IL235064B (https=)
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LT (1) LT2838892T (https=)
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MD (1) MD4615C1 (https=)
ME (1) ME02966B (https=)
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MY (1) MY170068A (https=)
NI (1) NI201400124A (https=)
NO (1) NO2877697T3 (https=)
NZ (1) NZ700833A (https=)
PE (1) PE20150084A1 (https=)
PH (1) PH12014502351A1 (https=)
PL (2) PL2838892T3 (https=)
PT (2) PT3517532T (https=)
PY (1) PY1316881A (https=)
RS (1) RS56869B1 (https=)
SG (2) SG10201608488RA (https=)
SI (2) SI3290410T1 (https=)
TN (1) TN2014000421A1 (https=)
TW (2) TWI677494B (https=)
UA (1) UA116207C2 (https=)
UY (1) UY34753A (https=)
WO (1) WO2013158874A1 (https=)
ZA (1) ZA201408508B (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JO3353B1 (ar) 2012-04-20 2019-03-13 Ono Pharmaceutical Co شكل صلب معزول من أحادي هيدروكلوريد أناموريلين بنسبة مولارية منخفضة من الكلوريد: أناموريلين ومحتوى منخفض من مذيب عضوي متبقي
GEP20186939B (en) * 2014-09-04 2018-12-25 Healthcare Sa Helsinn Medical treatments based on anamorelin
EP3954369B1 (en) 2015-07-24 2025-08-20 Lumos Pharma, Inc. Salts and prodrugs of 1-methyl-d-tryptophan
CN108239141A (zh) * 2016-12-23 2018-07-03 江苏先声药业有限公司 一种阿拉莫林的制备方法
BR112022002767A2 (pt) * 2019-08-30 2022-05-10 Helsinn Healthcare Sa Métodos de fabricação de um comprimido de cloridrato de anamorelina, comprimidos e método para melhorar um ou mais sintomas de caquexia de câncer

Citations (2)

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WO2001034593A1 (en) * 1999-11-10 2001-05-17 Novo Nordisk A/S Compound with growth hormone releasing properties
WO2010099522A1 (en) * 2009-02-27 2010-09-02 Helsinn Therapeutics (U.S.), Inc. Enhanced migraine treatments based on ghrelin mimetics

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1882526A (zh) * 2003-09-26 2006-12-20 兰贝克赛实验室有限公司 制备伏格列波糖的方法
CN1976921B (zh) 2004-06-29 2013-08-21 蓝宝石治疗公司 (3r)-1-(2-甲基丙氨酰-d-色氨酰)-3-(苯甲基)-3-哌啶羧酸1,2,2-三甲基酰肼的晶形
WO2008100448A2 (en) 2007-02-13 2008-08-21 Helsinn Therapeutics (U.S.), Inc. Method of treating cell proliferative disorders using growth hormone secretagogues
JO3353B1 (ar) * 2012-04-20 2019-03-13 Ono Pharmaceutical Co شكل صلب معزول من أحادي هيدروكلوريد أناموريلين بنسبة مولارية منخفضة من الكلوريد: أناموريلين ومحتوى منخفض من مذيب عضوي متبقي

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001034593A1 (en) * 1999-11-10 2001-05-17 Novo Nordisk A/S Compound with growth hormone releasing properties
WO2010099522A1 (en) * 2009-02-27 2010-09-02 Helsinn Therapeutics (U.S.), Inc. Enhanced migraine treatments based on ghrelin mimetics

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CN110041398A (zh) 2019-07-23
US20190000914A1 (en) 2019-01-03
PT3517532T (pt) 2021-11-08
CA2869893A1 (en) 2013-10-24
IL235064A0 (en) 2014-12-31
KR20190044697A (ko) 2019-04-30
BR112014025972A8 (pt) 2021-06-22
US10300105B2 (en) 2019-05-28
UY34753A (es) 2013-11-29
JP2018076375A (ja) 2018-05-17
US20150072934A1 (en) 2015-03-12
TW201722928A (zh) 2017-07-01
HUE050865T2 (hu) 2021-01-28
UA116207C2 (uk) 2018-02-26
KR20150013115A (ko) 2015-02-04
HK1202863A1 (en) 2015-10-09
PH12014502351B1 (en) 2015-01-12
CY1120276T1 (el) 2019-07-10
HK1248694A1 (en) 2018-10-19
PY1316881A (es) 2016-06-01
US20190231843A1 (en) 2019-08-01
RS56869B1 (sr) 2018-04-30
US10905737B2 (en) 2021-02-02
AU2013249197A1 (en) 2014-10-30
US9872883B2 (en) 2018-01-23
JP6109925B2 (ja) 2017-04-05
MA37524A1 (fr) 2016-06-30
CA3031652C (en) 2020-10-27
DK3517532T3 (da) 2022-01-03
CL2014002817A1 (es) 2015-08-14
US9981002B2 (en) 2018-05-29
ME02966B (me) 2018-07-20
TWI677494B (zh) 2019-11-21
EP3517532B1 (en) 2021-10-13
DOP2014000235A (es) 2015-01-31
WO2013158874A1 (en) 2013-10-24
TWI589572B (zh) 2017-07-01
EP3290410B1 (en) 2020-07-01
CN103857669A (zh) 2014-06-11
AU2013249197B2 (en) 2017-04-06
NZ700833A (en) 2016-01-29
EA031581B1 (ru) 2019-01-31
CA2869893C (en) 2019-03-05
TW201348224A (zh) 2013-12-01
EP3517532A1 (en) 2019-07-31
KR101972998B1 (ko) 2019-04-29
HRP20180316T1 (hr) 2018-04-06
SG11201406478XA (en) 2014-11-27
AR090725A1 (es) 2014-12-03
MY170068A (en) 2019-07-03
NO2877697T3 (https=) 2018-10-13
CA3031652A1 (en) 2013-10-24
US20160237115A1 (en) 2016-08-18
IL235064B (en) 2019-09-26
NI201400124A (es) 2015-09-21
JP6284665B2 (ja) 2018-02-28
PL3290410T3 (pl) 2021-01-11
PE20150084A1 (es) 2015-01-23
SI3290410T1 (sl) 2020-11-30
MD4615C1 (ro) 2019-08-31
ZA201408508B (en) 2020-01-29
CN110041304A (zh) 2019-07-23
GEP20186902B (en) 2018-10-25
CN103857669B (zh) 2019-06-28
SI2838892T1 (en) 2018-05-31
US20140018391A1 (en) 2014-01-16
AP2014008013A0 (en) 2014-10-31
JP2017101082A (ja) 2017-06-08
US20160229889A1 (en) 2016-08-11
ES2658862T3 (es) 2018-03-12
HUE035697T2 (en) 2018-05-28
DK2838892T3 (en) 2018-03-12
MD20140122A2 (ro) 2015-05-31
JP2015514779A (ja) 2015-05-21
SG10201608488RA (en) 2016-12-29
MA37524B1 (fr) 2017-04-28
MD4615B1 (ro) 2019-01-31
PL2838892T3 (pl) 2018-05-30
JP6616853B2 (ja) 2019-12-04
MX354793B (es) 2018-03-21
ES2820354T3 (es) 2021-04-20
GEAP201813634A (en) 2018-06-25
TN2014000421A1 (en) 2016-03-30
BR112014025972A2 (pt) 2017-06-27
LT2838892T (lt) 2018-03-12
PT2838892T (pt) 2018-02-28
EP2838892B1 (en) 2017-12-06
CR20140530A (es) 2015-03-25
EP3290410A1 (en) 2018-03-07
ECSP14027739A (es) 2015-12-31
US9956261B2 (en) 2018-05-01
US10576122B2 (en) 2020-03-03
EA201401151A1 (ru) 2015-06-30
JO3353B1 (ar) 2019-03-13
US9403867B2 (en) 2016-08-02
EP2838892A1 (en) 2015-02-25
US20160235804A1 (en) 2016-08-18
CO7131356A2 (es) 2014-12-01
PH12014502351A1 (en) 2015-01-12
MX2014012178A (es) 2015-08-05
US20200276259A1 (en) 2020-09-03

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