AR067440A1 - ÁCIDO BILIAR SINTETICO, UNA COMPOSICION QUE LO COMPRENDE, UN METODO PARA SU PREPARACION, COMPUESTOS INTERMEDIARIOS DE SíNTESIS Y SU EMPLEO EN LA ELIMINACION DE LOS DEPoSITOS DE GRASA CORPORAL - Google Patents

ÁCIDO BILIAR SINTETICO, UNA COMPOSICION QUE LO COMPRENDE, UN METODO PARA SU PREPARACION, COMPUESTOS INTERMEDIARIOS DE SíNTESIS Y SU EMPLEO EN LA ELIMINACION DE LOS DEPoSITOS DE GRASA CORPORAL

Info

Publication number
AR067440A1
AR067440A1 ARP080102625A ARP080102625A AR067440A1 AR 067440 A1 AR067440 A1 AR 067440A1 AR P080102625 A ARP080102625 A AR P080102625A AR P080102625 A ARP080102625 A AR P080102625A AR 067440 A1 AR067440 A1 AR 067440A1
Authority
AR
Argentina
Prior art keywords
formula
compound
reaction
alkyl
protective group
Prior art date
Application number
ARP080102625A
Other languages
English (en)
Inventor
John Gregory Reid
Jr Roy A Swaringen
Robert M Moriarty
Nadir Ahmeduddin Mahmood
Nathaniel E David
Achampeta Rathan Prasad
Original Assignee
Kythera Biopharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41226994&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR067440(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from US12/035,339 external-priority patent/US20080318870A1/en
Priority claimed from GB0807615A external-priority patent/GB2452358C/en
Application filed by Kythera Biopharmaceuticals Inc filed Critical Kythera Biopharmaceuticals Inc
Publication of AR067440A1 publication Critical patent/AR067440A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/63—Steroids; Derivatives thereof
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/06—Preparations for care of the skin for countering cellulitis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0003—Androstane derivatives
    • C07J1/0011—Androstane derivatives substituted in position 17 by a keto group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0003—Androstane derivatives
    • C07J1/0018—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa
    • C07J1/0022—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
    • C07J13/007—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 17 (20)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • C07J9/005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to the cyclopenta[a]hydrophenanthrene skeleton
    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Dermatology (AREA)
  • Birds (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Obesity (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Child & Adolescent Psychology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Acidos biliares y composiciones relacionadas y métodos de síntesis y uso. Más específicamente el ácido desoxicolico y las composiciones relacionadas, dichas composiciones están libres de todas las porciones de origen animal y libres de porciones pirogénicas. Intermediarios para síntesis. Reivindicacion 1: Un compuesto que es el ácido desoxicolico (DCA) o una prodroga del mismo o una sal aceptable para uso farmacéutico del compuesto o la prodroga de formula (1) donde dicho compuesto no se aísla a partir de un organismo mamífero o microbiano que produce DCA naturalmente. Reivindicacion 10: Un método para la preparacion del ácido desoxicolico (DCA) o de un éster del mismo o de una sal aceptable para uso farmacéutico de los mismos de formula (1a) dicho método comprende (a) la reaccion de 9a-hidroxiandrost-4-en-3,17-diona de formula (2) con H2 bajo condiciones de hidrogenacion para formar el compuesto de formula (3); (b) la reaccion del compuesto de formula (3) con ácido para formar el compuesto de formula (4); (c) la reaccion del compuesto de formula (4) con un agente reductor para formar el compuesto de formula (5) como una mezcla del compuesto de formula (5) y el de formula (6); (d) la reaccion del compuesto de formula (5) con un reactivo de olefinacion de dos carbonos bajo condiciones de formacion de olefinas para formar el compuesto de formula (7); (e) la conversion del compuesto de formula (7) en un compuesto de formula (8) caracterizado porque P es un grupo protector; (f) la reaccion de un compuesto de formula (8) con un propiolato de alquilo-CH2CH2C(O)OR o un acrilato de alquilo-CH2=CHC(O)OR caracterizado porque R es un alquilo en la presencia de un ácido de Lewis para formar un compuesto de formula (9) caracterizado porque P es un grupo protector, R es un alquilo, y la línea punteada es un enlace simple o doble; (g) la reaccion de un compuesto de formula (9) con H2 bajo condiciones de hidrogenacion para formar un compuesto de formula (10) caracterizado porque P es un grupo protector y R es un alquilo; (h) la reaccion de un compuesto de formula (10) con un agente oxidante para formar un compuesto de formula (11) caracterizado porque P es un grupo protector y R es un alquilo; (i) la reaccion de un compuesto de formula (11) con H2 bajo condiciones de hidrogenacion para formar un compuesto de formula (12) caracterizado porque P es un grupo protector y R es un alquilo; (j) la reaccion de un compuesto de formula (12) con un agente reductor para formar un compuesto de formula (13) caracterizado porque P es un grupo protector y R es un alquilo; y (k) la exposicion de un compuesto de formula (13) a condiciones de desproteccion para formar un éster del mismo y de forma opcional a condiciones apropiadas de hidrolisis para formar el ácido desoxicolico o la sal aceptable para uso farmacéutico del mismo.
ARP080102625A 2007-06-19 2008-06-19 ÁCIDO BILIAR SINTETICO, UNA COMPOSICION QUE LO COMPRENDE, UN METODO PARA SU PREPARACION, COMPUESTOS INTERMEDIARIOS DE SíNTESIS Y SU EMPLEO EN LA ELIMINACION DE LOS DEPoSITOS DE GRASA CORPORAL AR067440A1 (es)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US94503507P 2007-06-19 2007-06-19
US95687507P 2007-08-20 2007-08-20
US12/035,339 US20080318870A1 (en) 2007-06-19 2008-02-21 Synthetic bile acid compositions and methods
GB0807615A GB2452358C (en) 2008-04-25 2008-04-25 Preparation of bile acids.
US12/153,446 US7902387B2 (en) 2008-04-25 2008-05-16 Preparation of bile acids and intermediates thereof

Publications (1)

Publication Number Publication Date
AR067440A1 true AR067440A1 (es) 2009-10-14

Family

ID=41226994

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP080102625A AR067440A1 (es) 2007-06-19 2008-06-19 ÁCIDO BILIAR SINTETICO, UNA COMPOSICION QUE LO COMPRENDE, UN METODO PARA SU PREPARACION, COMPUESTOS INTERMEDIARIOS DE SíNTESIS Y SU EMPLEO EN LA ELIMINACION DE LOS DEPoSITOS DE GRASA CORPORAL

Country Status (28)

Country Link
EP (3) EP3002290B1 (es)
JP (2) JP2010530876A (es)
KR (7) KR101598402B1 (es)
CN (4) CN108191940B (es)
AR (1) AR067440A1 (es)
AU (1) AU2008265721B2 (es)
BR (1) BRPI0813140C1 (es)
CA (2) CA2789109C (es)
CR (2) CR20170070A (es)
CY (1) CY1116700T1 (es)
DK (1) DK2407475T3 (es)
EA (1) EA020806B1 (es)
ES (2) ES2826429T3 (es)
HK (2) HK1165807A1 (es)
HR (1) HRP20150879T1 (es)
HU (1) HUE025909T2 (es)
IL (1) IL202203B (es)
JO (1) JO3172B1 (es)
MX (2) MX2009013664A (es)
MY (1) MY160040A (es)
NZ (1) NZ581081A (es)
PL (1) PL2407475T3 (es)
PT (1) PT2407475E (es)
SI (1) SI2407475T1 (es)
SM (1) SMP201000003B (es)
TW (2) TWI503396B (es)
WO (1) WO2008157635A2 (es)
ZA (1) ZA200907928B (es)

Families Citing this family (24)

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US8242294B2 (en) 2007-06-19 2012-08-14 Kythera Biopharmaceuticals, Inc. Synthetic bile acid compositions and methods
WO2008157635A2 (en) * 2007-06-19 2008-12-24 Kythera Biopharmaceuticals, Inc. Synthetic bile acid composition, method, and preparation
US20080318870A1 (en) 2007-06-19 2008-12-25 Kythera Biopharmaceuticals, Inc. Synthetic bile acid compositions and methods
JOP20180077A1 (ar) 2007-06-19 2019-01-30 Kythera Biopharmaceuticals Inc تركيبات وطرق لحمض صفراوي تخليقي
GB2480632A (en) 2010-05-25 2011-11-30 Kythera Biopharmaceuticals Inc Preparation of 12-keto and 12-alpha-hydroxy steroids
CA2783017C (en) * 2010-08-12 2018-05-15 Kythera Biopharmaceuticals, Inc. Synthetic bile acid compositions and methods
TWI572616B (zh) * 2011-06-16 2017-03-01 凱瑟拉生物製藥有限公司 去氧膽酸之組成物及用途及其相關方法
US20130102580A1 (en) * 2011-09-22 2013-04-25 Kythera Biopharmaceuticals, Inc. Compositions and methods related to deoxycholic acid and its polymorphs
WO2013142873A2 (en) 2012-03-23 2013-09-26 The Board Of Trustees Of The University Of Illinois Complex and structurally diverse compounds
CN103059087B (zh) * 2012-12-30 2015-10-14 中山百灵生物技术有限公司 一种脱氧胆酸的合成方法
KR101447901B1 (ko) * 2013-04-16 2014-10-16 한양대학교 산학협력단 지방세포 표적 비바이러스성 유전자 전달체
BR112018001869A2 (pt) 2015-07-30 2018-09-18 Intercept Pharmaceuticals Inc método para preparação de ácidos biliares e derivados dos mesmos
KR20180100309A (ko) * 2015-11-04 2018-09-10 키쎄라 바이오파마슈티컬즈 인코포레이티드 데옥시콜산 및 이의 염을 사용한 축적된 지방의 치료 방법
US11117925B2 (en) 2016-06-06 2021-09-14 Bionice, S.L.U. Methods for the preparation of deoxycholic acid, and intermediates useful in the preparation of deoxycholic acid
JP6937893B2 (ja) * 2017-08-03 2021-09-22 メディトックス インク． 胆汁酸類を製造するための方法
CN111511755A (zh) * 2017-10-24 2020-08-07 比奥尼斯有限责任公司 脱氧胆酸的制备
RU2705314C1 (ru) * 2019-03-18 2019-11-06 Федеральное бюджетное учреждение науки "Государственный научный центр прикладной микробиологии и биотехнологии" Федеральной службы по надзору в сфере защиты прав потребителей и благополучия человека (ФБУН ГНЦ ПМБ) Способ производства сухих очищенных солей желчных кислот для бактериологии
KR102456989B1 (ko) 2020-06-12 2022-10-21 (주)케어젠 항비만 활성을 가지는 디옥시콜산-펩타이드 결합체 및 이의 용도
WO2022059948A1 (ko) * 2020-09-18 2022-03-24 서울대학교 산학협력단 소디움 타우로디옥시콜레이트의 대량 생산 방법
WO2023287260A1 (ko) 2021-07-16 2023-01-19 주식회사 스카이테라퓨틱스 담즙산 또는 담즙산 염의 분자 회합체 및 이를 포함하는 국소지방제거용 의약 조성물
EP4371551A1 (en) 2021-07-16 2024-05-22 Scai Therapeutics Co., Ltd. Molecular assembly of bile acid or bile salt and pharmaceutical composition comprising same for removing local fat
CN114478676B (zh) * 2022-02-18 2024-05-10 国药集团化学试剂有限公司 一种脱氧胆酸钠的制备方法
CN115974949B (zh) * 2022-10-26 2023-12-22 湖南科瑞生物制药股份有限公司 一种植物源脱氧胆酸中间体的制备方法
CN118344420A (zh) * 2023-01-16 2024-07-16 北京诺博特生物科技有限公司 一种脱氧胆酸的制备方法

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Also Published As

Publication number Publication date
TWI503396B (zh) 2015-10-11
EP2407475B1 (en) 2015-08-12
HK1165807A1 (en) 2012-10-12
WO2008157635A3 (en) 2009-06-04
KR20150013305A (ko) 2015-02-04
HRP20150879T1 (hr) 2015-09-25
EP3002290A2 (en) 2016-04-06
EP3002290A3 (en) 2016-06-29
JP2013075918A (ja) 2013-04-25
DK2407475T3 (en) 2015-10-26
CR20170070A (es) 2017-04-27
HUE025909T2 (en) 2016-04-28
ES2550504T3 (es) 2015-11-10
CY1116700T1 (el) 2017-03-15
IL202203B (en) 2018-04-30
CA2690841C (en) 2012-11-27
JP2010530876A (ja) 2010-09-16
CR11174A (es) 2010-03-23
KR101916024B1 (ko) 2018-11-08
TW201534684A (zh) 2015-09-16
WO2008157635A2 (en) 2008-12-24
EP2069383A2 (en) 2009-06-17
KR20160150646A (ko) 2016-12-30
KR20130133881A (ko) 2013-12-09
KR20180061401A (ko) 2018-06-07
NZ581081A (en) 2012-12-21
CN101711254A (zh) 2010-05-19
CN106146594A (zh) 2016-11-23
CN108191940A (zh) 2018-06-22
CA2789109A1 (en) 2008-12-24
BRPI0813140B1 (pt) 2019-02-05
TW200918550A (en) 2009-05-01
BRPI0813140A2 (pt) 2014-12-23
AU2008265721B2 (en) 2014-03-20
EP2407475A3 (en) 2012-06-13
KR102061001B1 (ko) 2020-01-03
IL202203A0 (en) 2010-06-16
CN106083969B (zh) 2018-02-27
AU2008265721A1 (en) 2008-12-24
EP3002290B1 (en) 2020-09-09
JO3172B1 (ar) 2018-03-08
HK1223372A1 (zh) 2017-07-28
KR20100031512A (ko) 2010-03-22
CA2789109C (en) 2015-10-06
KR101863131B1 (ko) 2018-06-01
SMAP201000003A (it) 2010-03-01
CN106083969A (zh) 2016-11-09
MX2009013664A (es) 2010-04-07
KR20180122483A (ko) 2018-11-12
KR101598402B1 (ko) 2016-03-03
CA2690841A1 (en) 2008-12-24
TWI503327B (zh) 2015-10-11
SMP201000003B (it) 2010-11-12
EA201000032A1 (ru) 2010-04-30
ES2826429T3 (es) 2021-05-18
JP5589102B2 (ja) 2014-09-10
MY160040A (en) 2017-02-15
CN108191940B (zh) 2021-02-09
PL2407475T3 (pl) 2015-12-31
EP2407475A2 (en) 2012-01-18
EA020806B1 (ru) 2015-01-30
MX360094B (es) 2018-10-19
KR20160025044A (ko) 2016-03-07
BRPI0813140C1 (pt) 2021-05-25
PT2407475E (pt) 2015-11-20
SI2407475T1 (sl) 2016-03-31
ZA200907928B (en) 2011-05-28

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