AR072235A1 - Proceso enzimatico para obtener 17-alfa monoesteres de cortexolona y/o sus 9,11-dehidro derivados - Google Patents

Proceso enzimatico para obtener 17-alfa monoesteres de cortexolona y/o sus 9,11-dehidro derivados

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Publication number
AR072235A1
AR072235A1 ARP080103135A ARP080103135A AR072235A1 AR 072235 A1 AR072235 A1 AR 072235A1 AR P080103135 A ARP080103135 A AR P080103135A AR P080103135 A ARP080103135 A AR P080103135A AR 072235 A1 AR072235 A1 AR 072235A1
Authority
AR
Argentina
Prior art keywords
alpha
derivatives
cortexolona
monosteres
dehydra
Prior art date
Application number
ARP080103135A
Other languages
English (en)
Inventor
Luigi Moro
Mauro Ajani
Original Assignee
Cosmo Spa
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=40278805&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR072235(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Cosmo Spa filed Critical Cosmo Spa
Publication of AR072235A1 publication Critical patent/AR072235A1/es

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    • 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
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16—Masculine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/08—Antiseborrheics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28—Antiandrogens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
    • C07J5/0046—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa
    • C07J5/0053—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa not substituted in position 16
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/008—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P33/00—Preparation of steroids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P33/00—Preparation of steroids
    • C12P33/005—Degradation of the lateral chains at position 17

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Biochemistry (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • General Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Medicinal Preparation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Crystals, And After-Treatments Of Crystals (AREA)

Abstract

La presente solicitud se refiere a un nuevo proceso enzimático para obtener 17-alfa-monoésteres de cortexolona y/o sus 9,11-dehidro-derivados a partir de los correspondientes 17-alfa,21-diésteres que comprende una reaccion de alcoholisis enzimática. La presente se refiere además a nuevas formas cristalinas del 17-alfa-propionato de cortexolona y del 17-alfa butanoato de 9,11-dehidro cortexolona.
ARP080103135A 2007-08-03 2008-07-18 Proceso enzimatico para obtener 17-alfa monoesteres de cortexolona y/o sus 9,11-dehidro derivados AR072235A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
IT001616A ITMI20071616A1 (it) 2007-08-03 2007-08-03 Processo enzimatico per l'ottenimento di 17-alfa monoesteri del cortexolone e/o suoi 9,11-deidroderivati.

Publications (1)

Publication Number Publication Date
AR072235A1 true AR072235A1 (es) 2010-08-18

Family

ID=40278805

Family Applications (3)

Application Number Title Priority Date Filing Date
ARP080103135A AR072235A1 (es) 2007-08-03 2008-07-18 Proceso enzimatico para obtener 17-alfa monoesteres de cortexolona y/o sus 9,11-dehidro derivados
ARP180100810A AR111351A2 (es) 2007-08-03 2018-04-03 FORMA CRISTALINA I DEL 17-a-PROPIONATO DE CORTEXOLONA, COMPOSICIÓN FARMACÉUTICA QUE LA CONTIENE Y SU EMPLEO EN EL TRATAMIENTO DE UNA PATOLOGÍA RELACIONADA CON EL APARATO UROGENITAL, ENDÓCRINO O DE LA PIEL Y/O ANEXOS DE ÉSTA
ARP180100811A AR111202A2 (es) 2007-08-03 2018-04-03 Formas cristalinas de cortexolona

Family Applications After (2)

Application Number Title Priority Date Filing Date
ARP180100810A AR111351A2 (es) 2007-08-03 2018-04-03 FORMA CRISTALINA I DEL 17-a-PROPIONATO DE CORTEXOLONA, COMPOSICIÓN FARMACÉUTICA QUE LA CONTIENE Y SU EMPLEO EN EL TRATAMIENTO DE UNA PATOLOGÍA RELACIONADA CON EL APARATO UROGENITAL, ENDÓCRINO O DE LA PIEL Y/O ANEXOS DE ÉSTA
ARP180100811A AR111202A2 (es) 2007-08-03 2018-04-03 Formas cristalinas de cortexolona

Country Status (25)

Country Link
US (9) US8785427B2 (es)
EP (5) EP2503004B1 (es)
JP (3) JP5646992B2 (es)
KR (1) KR101495192B1 (es)
CN (3) CN104861023B (es)
AR (3) AR072235A1 (es)
AU (1) AU2008285784B2 (es)
BR (1) BRPI0814163A2 (es)
CA (3) CA2871025C (es)
DK (4) DK2173891T3 (es)
ES (4) ES2732326T3 (es)
HR (4) HRP20140421T1 (es)
HU (3) HUE026507T2 (es)
IT (1) ITMI20071616A1 (es)
LT (1) LT2966175T (es)
MX (4) MX363701B (es)
NZ (3) NZ615953A (es)
PL (4) PL2173891T3 (es)
PT (4) PT2503004E (es)
RS (4) RS53310B (es)
RU (2) RU2482190C2 (es)
SI (4) SI2503005T1 (es)
TR (1) TR201909129T4 (es)
WO (1) WO2009019138A2 (es)
ZA (2) ZA201000587B (es)

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ITMI20071616A1 (it) 2007-08-03 2009-02-04 Cosmo Spa Processo enzimatico per l'ottenimento di 17-alfa monoesteri del cortexolone e/o suoi 9,11-deidroderivati.
ITMI20132157A1 (it) 2013-12-20 2015-06-21 Cosmo Dermatos Srl Cortexolone 17alfa-propionate for use in the treatment of skin wounds and/or atrophic skin disorders . cortexolone 17alfa-propionato per uso nel trattamento delle ferite della pelle e/o disordini atrofici della pelle.
EP3006453A1 (en) * 2014-10-08 2016-04-13 Cosmo Technologies Ltd. 17alpha-monoesters and 17alpha,21-diesters of cortexolone for use in the treatment of tumors
EP3108879A1 (en) * 2015-06-25 2016-12-28 Cassiopea S.p.A. High concentration formulation
CN112028956A (zh) * 2020-09-10 2020-12-04 那路新 合成21-羟基-17-(1-氧代丙氧基)孕甾-4-烯-3,20-二酮的方法
CH719319B1 (it) * 2020-10-19 2024-08-15 Ind Chimica Srl Processo per la preparazione di 21-(acetilossi)-17-(1-ossopropossi)-pregn-4-ene-3,20-dione
IT202100008429A1 (it) 2021-04-06 2022-10-06 Farmabios Spa Processo per la preparazione di cortexolone 17α-propionato e sua nuova forma cristallina idrata
CN114410727B (zh) * 2022-01-25 2023-09-19 山东诺明康药物研究院有限公司 一种克拉考特酮的制备方法
CN115073546A (zh) * 2022-06-01 2022-09-20 浙江神洲药业有限公司 一种新型雄激素受体抑制剂的制备方法
CN115466301A (zh) * 2022-08-29 2022-12-13 扬州奥锐特药业有限公司 一种甾体化合物，其晶型a及它们的制备方法和用途
WO2024165502A1 (en) 2023-02-07 2024-08-15 Farmabios S.P.A. Cocrystals of cortexolone 17-propionate and methods for their preparation
WO2024208997A1 (en) 2023-04-07 2024-10-10 Cassiopea S.P.A. Clascoterone and minoxidil combination therapy for use in treating hair loss

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EP3108879A1 (en) 2015-06-25 2016-12-28 Cassiopea S.p.A. High concentration formulation

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ES2554934T3 (es) 2015-12-28
EP2966175B1 (en) 2019-05-08
EP2503005A3 (en) 2012-10-03
US20220280531A1 (en) 2022-09-08
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US8785427B2 (en) 2014-07-22
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RS54354B1 (en) 2016-04-28
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US10716796B2 (en) 2020-07-21
US20230104965A1 (en) 2023-04-06
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US20160326210A1 (en) 2016-11-10
ZA201000587B (en) 2011-04-28
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US11938141B2 (en) 2024-03-26
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