PT1963354E - 17alfa-cianometil-17beta-hidroxi-estra-4,9-dieno-3-ona de alta pureza e processo para a síntese da mesma - Google Patents

17alfa-cianometil-17beta-hidroxi-estra-4,9-dieno-3-ona de alta pureza e processo para a síntese da mesma Download PDF

Info

Publication number: PT1963354E
Authority: PT; Portugal
Prior art keywords: formula; estra; diene; hydroxy; cyanomethyl
Prior art date: 2005-12-05

Application number

PT06808800T

Other languages

English (en)

Inventor

Lajosne Dancsi

Sandor Maho

Antal Aranyi

Janos Horvath

Original Assignee

Richter Gedeon Nyrt

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.)

2005-12-05

Filing date

2006-10-11

Publication date

2010-01-06

2006-10-11 Application filed by Richter Gedeon Nyrt filed Critical Richter Gedeon Nyrt

2010-01-06 Publication of PT1963354E publication Critical patent/PT1963354E/pt

Links

230000015572 biosynthetic process Effects 0.000 title abstract 2
238000000034 method Methods 0.000 title abstract 2
238000003786 synthesis reaction Methods 0.000 title abstract 2
229960003309 dienogest Drugs 0.000 abstract 5
AZFLJNIPTRTECV-FUMNGEBKSA-N dienogest Chemical compound C1CC(=O)C=C2CC[C@@H]([C@H]3[C@@](C)([C@](CC3)(O)CC#N)CC3)C3=C21 AZFLJNIPTRTECV-FUMNGEBKSA-N 0.000 abstract 4
239000004480 active ingredient Substances 0.000 abstract 3
XFFZLECPCHQJIR-BBCBXFPWSA-N (8r,9s,13s,14s)-3-methoxy-13-methyl-1,4,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-17-ol Chemical compound C1C[C@@H]2C(CC=C(C3)OC)=C3CC[C@H]2[C@@H]2CCC(O)[C@]21C XFFZLECPCHQJIR-BBCBXFPWSA-N 0.000 abstract 2
JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 abstract 2
WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 abstract 2
JHIVVAPYMSGYDF-UHFFFAOYSA-N cyclohexanone Chemical compound O=C1CCCCC1 JHIVVAPYMSGYDF-UHFFFAOYSA-N 0.000 abstract 2
239000008194 pharmaceutical composition Substances 0.000 abstract 2
NSUVCVKCWGOYPV-VXNCWWDNSA-N (8r,9s,13s,14s)-3-methoxy-13-methyl-4,6,7,8,9,11,12,14,15,16-decahydro-1h-cyclopenta[a]phenanthren-17-one Chemical compound C1C[C@@H]2C(CC=C(C3)OC)=C3CC[C@H]2[C@@H]2CCC(=O)[C@]21C NSUVCVKCWGOYPV-VXNCWWDNSA-N 0.000 abstract 1
OFIPMSSTKFSADG-UHFFFAOYSA-N [Li]CC#N Chemical compound [Li]CC#N OFIPMSSTKFSADG-UHFFFAOYSA-N 0.000 abstract 1
SMZOGRDCAXLAAR-UHFFFAOYSA-N aluminium isopropoxide Chemical compound [Al+3].CC(C)[O-].CC(C)[O-].CC(C)[O-] SMZOGRDCAXLAAR-UHFFFAOYSA-N 0.000 abstract 1
239000000969 carrier Substances 0.000 abstract 1
238000001514 detection method Methods 0.000 abstract 1
239000003085 diluting agent Substances 0.000 abstract 1
238000010438 heat treatment Methods 0.000 abstract 1
239000012535 impurity Substances 0.000 abstract 1
239000000463 material Substances 0.000 abstract 1
150000007524 organic acids Chemical class 0.000 abstract 1
239000003960 organic solvent Substances 0.000 abstract 1
239000000546 pharmaceutical excipient Substances 0.000 abstract 1
238000002953 preparative HPLC Methods 0.000 abstract 1
UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 abstract 1
JQRYUMGHOUYJFW-UHFFFAOYSA-N pyridine;trihydrobromide Chemical compound [Br-].[Br-].[Br-].C1=CC=[NH+]C=C1.C1=CC=[NH+]C=C1.C1=CC=[NH+]C=C1 JQRYUMGHOUYJFW-UHFFFAOYSA-N 0.000 abstract 1
238000001953 recrystallisation Methods 0.000 abstract 1
YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 abstract 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0094—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
- 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
- A61P15/18—Feminine contraceptives
- 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
- A61P5/34—Gestagens

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
General Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Veterinary Medicine (AREA)
Pharmacology & Pharmacy (AREA)
Bioinformatics & Cheminformatics (AREA)
Endocrinology (AREA)
Engineering & Computer Science (AREA)
Public Health (AREA)
Reproductive Health (AREA)
Toxicology (AREA)
Diabetes (AREA)
Gynecology & Obstetrics (AREA)
Steroid Compounds (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Lubricants (AREA)

PT06808800T 2005-12-05 2006-10-11 17alfa-cianometil-17beta-hidroxi-estra-4,9-dieno-3-ona de alta pureza e processo para a síntese da mesma PT1963354E (pt)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
HU0501132A HUP0501132A2 (en)	2005-12-05	2005-12-05	17-alpha-cyanomethyl-17betha-hydroxyestra-4,9-diene-3-one of high purity and process for its production

Publications (1)

Publication Number	Publication Date
PT1963354E true PT1963354E (pt)	2010-01-06

Family

ID=89986433

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
PT06808800T PT1963354E (pt)	2005-12-05	2006-10-11	17alfa-cianometil-17beta-hidroxi-estra-4,9-dieno-3-ona de alta pureza e processo para a síntese da mesma

Country Status (22)

Country	Link
US (1)	US8314145B2 (pt)
EP (1)	EP1963354B1 (pt)
JP (1)	JP5399711B2 (pt)
CN (1)	CN101360757B (pt)
AT (1)	ATE451383T1 (pt)
AU (1)	AU2006323005B2 (pt)
BR (1)	BRPI0619428B8 (pt)
CA (1)	CA2631748C (pt)
CY (1)	CY1110063T1 (pt)
DE (1)	DE602006011052D1 (pt)
DK (1)	DK1963354T3 (pt)
EA (1)	EA014558B1 (pt)
ES (1)	ES2338047T3 (pt)
HR (1)	HRP20100102T1 (pt)
HU (1)	HUP0501132A2 (pt)
IL (1)	IL191915A (pt)
MX (1)	MX2008007243A (pt)
PL (1)	PL1963354T3 (pt)
PT (1)	PT1963354E (pt)
SI (1)	SI1963354T1 (pt)
UA (1)	UA91390C2 (pt)
WO (1)	WO2007066158A2 (pt)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
EP2256128B1 (en) *	2009-05-22	2011-12-07	HEYL Chemisch-Pharmazeutische Fabrik GmbH und Co. KG	Method for synthesis of dienogest from estrone-3-methylether
WO2011132045A2 (en)	2010-04-20	2011-10-27	Lupin Limited	Process for the preparation of dienogest substantially free of impurities
CN101863947A (zh) *	2010-06-29	2010-10-20	沈阳药科大学	一种地诺孕素的合成方法
CN103304619B (zh) *	2013-06-08	2015-12-02	西藏海思科药业集团股份有限公司	一种地诺孕素化合物
HU230788B1 (en) *	2013-12-16	2018-05-02	Richter Gedeon Nyrt	Norsteroid intermediates and process for their preparation
JP6002869B1 (ja) *	2015-10-16	2016-10-05	持田製薬株式会社	ジエノゲスト含有錠剤
JP6002870B1 (ja) *	2015-10-16	2016-10-05	持田製薬株式会社	低用量薬物を含有する口腔内崩壊錠
CN110357937A (zh) *	2018-03-26	2019-10-22	华润紫竹药业有限公司	一种地诺孕素化合物
CN110655551A (zh) *	2019-09-23	2020-01-07	华润紫竹药业有限公司	一种地诺孕素药物单一新晶型及其制备方法
CN114736261A (zh) *	2022-05-17	2022-07-12	梯尔希（南京）药物研发有限公司	8,11-二烯地塞米松的合成方法

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US3391165A (en)	1966-04-07	1968-07-02	Smith	Synthesis of gon-5(10)-enes
DE2718872A1 (de) *	1976-06-14	1977-12-22	Jenapharm Veb	Verfahren zur herstellung von neuen gona-4,9(10)-dienen
DD160418A1 (de) *	1979-05-22	1983-07-27	Kurt Ponsold	Verfahren zur herstellung von 17alpha-substituierten gona-4,9-dienen
CA2086919C (en) *	1990-07-09	1998-02-24	Gerhard Teichmuller	Process for the production of unsaturated 17.alpha.-cyanomethyl -17.beta. hydroxy steroids
IL119649A (en)	1995-11-30	2002-03-10	Akzo Nobel Nv	Preparation of Cyclic Kills of History - 3 keto- (5) 10, (-9) 11 steroidadians
IT1318491B1 (it) *	2000-04-21	2003-08-25	Ind Chimica Srl	Processo per la preparazione di un precursore di tibolone e diestradiol derivati strutturalmente correlati.
SI1989218T1 (sl) *	2006-02-17	2010-04-30	Janssen Pharmaceutica Nv	17- fosforjevi steroidni derivati, koristni kot progesteronski receptorski modulatorji

2005
- 2005-12-05 HU HU0501132A patent/HUP0501132A2/hu unknown
2006
- 2006-10-11 AU AU2006323005A patent/AU2006323005B2/en active Active
- 2006-10-11 ES ES06808800T patent/ES2338047T3/es active Active
- 2006-10-11 US US12/096,209 patent/US8314145B2/en active Active
- 2006-10-11 PL PL06808800T patent/PL1963354T3/pl unknown
- 2006-10-11 BR BRPI0619428A patent/BRPI0619428B8/pt active IP Right Grant
- 2006-10-11 AT AT06808800T patent/ATE451383T1/de active
- 2006-10-11 UA UAA200808851A patent/UA91390C2/ru unknown
- 2006-10-11 SI SI200630561T patent/SI1963354T1/sl unknown
- 2006-10-11 EA EA200801508A patent/EA014558B1/ru unknown
- 2006-10-11 MX MX2008007243A patent/MX2008007243A/es active IP Right Grant
- 2006-10-11 DE DE602006011052T patent/DE602006011052D1/de active Active
- 2006-10-11 JP JP2008543921A patent/JP5399711B2/ja active Active
- 2006-10-11 CA CA2631748A patent/CA2631748C/en active Active
- 2006-10-11 PT PT06808800T patent/PT1963354E/pt unknown
- 2006-10-11 CN CN2006800515980A patent/CN101360757B/zh active Active
- 2006-10-11 HR HR20100102T patent/HRP20100102T1/hr unknown
- 2006-10-11 EP EP06808800A patent/EP1963354B1/en active Active
- 2006-10-11 WO PCT/HU2006/000091 patent/WO2007066158A2/en not_active Ceased
- 2006-10-11 DK DK06808800.4T patent/DK1963354T3/da active
2008
- 2008-06-03 IL IL191915A patent/IL191915A/en active IP Right Grant
2010
- 2010-01-29 CY CY20101100088T patent/CY1110063T1/el unknown

Also Published As

Publication number	Publication date
AU2006323005A1 (en)	2007-06-14
BRPI0619428B1 (pt)	2021-02-17
HU0501132D0 (en)	2006-01-30
UA91390C2 (en)	2010-07-26
EA200801508A1 (ru)	2008-10-30
DK1963354T3 (da)	2010-04-12
WO2007066158A2 (en)	2007-06-14
EP1963354A2 (en)	2008-09-03
US20080287404A1 (en)	2008-11-20
EP1963354B1 (en)	2009-12-09
BRPI0619428A2 (pt)	2011-10-04
PL1963354T3 (pl)	2010-05-31
CY1110063T1 (el)	2015-01-14
BRPI0619428B8 (pt)	2021-05-25
CA2631748C (en)	2013-12-03
CA2631748A1 (en)	2007-06-14
EA014558B1 (ru)	2010-12-30
CN101360757A (zh)	2009-02-04
HUP0501132A2 (en)	2007-06-28
ES2338047T3 (es)	2010-05-03
IL191915A0 (en)	2008-12-29
JP2009518377A (ja)	2009-05-07
AU2006323005B2 (en)	2013-05-30
DE602006011052D1 (de)	2010-01-21
CN101360757B (zh)	2011-07-20
IL191915A (en)	2016-04-21
SI1963354T1 (sl)	2010-03-31
HRP20100102T1 (hr)	2010-04-30
MX2008007243A (es)	2008-10-22
US8314145B2 (en)	2012-11-20
ATE451383T1 (de)	2009-12-15
JP5399711B2 (ja)	2014-01-29
WO2007066158A3 (en)	2007-08-09

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