DK1963354T3 - 17alfa-cyanomethyl-17beta-hydroxy-estra-4,9-dien-3-on med høj renhed og fremgangsmåde til syntese deraf - Google Patents

17alfa-cyanomethyl-17beta-hydroxy-estra-4,9-dien-3-on med høj renhed og fremgangsmåde til syntese deraf

Info

Publication number: DK1963354T3
Authority: DK; Denmark
Prior art keywords: formula; estra; hydroxy; cyanomethyl; diene
Prior art date: 2005-12-05

Application number

DK06808800.4T

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

2010-04-12

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

2010-04-12 Application granted granted Critical

2010-04-12 Publication of DK1963354T3 publication Critical patent/DK1963354T3/da

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)

DK06808800.4T 2005-12-05 2006-10-11 17alfa-cyanomethyl-17beta-hydroxy-estra-4,9-dien-3-on med høj renhed og fremgangsmåde til syntese deraf DK1963354T3 (da)

Applications Claiming Priority (2)

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
PCT/HU2006/000091 WO2007066158A2 (en)	2005-12-05	2006-10-11	HIGH PURITY 17α-CYANOMETHYL-17β-HYDROXY-ESTRA-4,9-DIENE-3-ONE AND PROCESS FOR THE SYNTHESIS THEREOF

Publications (1)

Publication Number	Publication Date
DK1963354T3 true DK1963354T3 (da)	2010-04-12

Family

ID=89986433

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
DK06808800.4T DK1963354T3 (da)	2005-12-05	2006-10-11	17alfa-cyanomethyl-17beta-hydroxy-estra-4,9-dien-3-on med høj renhed og fremgangsmåde til syntese deraf

Country Status (22)

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

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
ATE536362T1 (de)	2009-05-22	2011-12-15	Heyl Chem Pharm	Verfahren zur synthese von dienogest aus estron-3-methylether
US20130041166A1 (en)	2010-04-20	2013-02-14	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
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
WO2017064814A1 (ja) *	2015-10-16	2017-04-20	持田製薬株式会社	ジエノゲスト含有錠剤
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
DE59108246D1 (de) *	1990-07-09	1996-11-07	Jenapharm Gmbh	UNGESÄTTIGTE 15-DEHYDRO-17alpha-CYANOMETHYL-17beta- HYDROXYSTEROIDE
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.
CA2642566C (en) *	2006-02-17	2014-04-15	Janssen Pharmaceutica N.V.	17-phosphorous steroid derivatives useful as progesterone receptor modulators

2005
- 2005-12-05 HU HU0501132A patent/HUP0501132A2/hu unknown
2006
- 2006-10-11 DE DE602006011052T patent/DE602006011052D1/de active Active
- 2006-10-11 UA UAA200808851A patent/UA91390C2/ru unknown
- 2006-10-11 MX MX2008007243A patent/MX2008007243A/es active IP Right Grant
- 2006-10-11 US US12/096,209 patent/US8314145B2/en active Active
- 2006-10-11 ES ES06808800T patent/ES2338047T3/es active Active
- 2006-10-11 AT AT06808800T patent/ATE451383T1/de active
- 2006-10-11 CA CA2631748A patent/CA2631748C/en active Active
- 2006-10-11 JP JP2008543921A patent/JP5399711B2/ja active Active
- 2006-10-11 DK DK06808800.4T patent/DK1963354T3/da active
- 2006-10-11 WO PCT/HU2006/000091 patent/WO2007066158A2/en not_active Ceased
- 2006-10-11 BR BRPI0619428A patent/BRPI0619428B8/pt active IP Right Grant
- 2006-10-11 PL PL06808800T patent/PL1963354T3/pl unknown
- 2006-10-11 AU AU2006323005A patent/AU2006323005B2/en active Active
- 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 SI SI200630561T patent/SI1963354T1/sl unknown
- 2006-10-11 PT PT06808800T patent/PT1963354E/pt unknown
- 2006-10-11 EA EA200801508A patent/EA014558B1/ru unknown
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
HUP0501132A2 (en)	2007-06-28
AU2006323005A1 (en)	2007-06-14
WO2007066158A2 (en)	2007-06-14
JP5399711B2 (ja)	2014-01-29
CN101360757B (zh)	2011-07-20
WO2007066158A3 (en)	2007-08-09
CN101360757A (zh)	2009-02-04
EP1963354B1 (en)	2009-12-09
EA014558B1 (ru)	2010-12-30
AU2006323005B2 (en)	2013-05-30
EP1963354A2 (en)	2008-09-03
CY1110063T1 (el)	2015-01-14
IL191915A (en)	2016-04-21
US20080287404A1 (en)	2008-11-20
BRPI0619428B8 (pt)	2021-05-25
BRPI0619428A2 (pt)	2011-10-04
CA2631748A1 (en)	2007-06-14
HU0501132D0 (en)	2006-01-30
JP2009518377A (ja)	2009-05-07
UA91390C2 (en)	2010-07-26
MX2008007243A (es)	2008-10-22
PT1963354E (pt)	2010-01-06
DE602006011052D1 (de)	2010-01-21
EA200801508A1 (ru)	2008-10-30
IL191915A0 (en)	2008-12-29
PL1963354T3 (pl)	2010-05-31
HRP20100102T1 (hr)	2010-04-30
BRPI0619428B1 (pt)	2021-02-17
ATE451383T1 (de)	2009-12-15
CA2631748C (en)	2013-12-03
SI1963354T1 (sl)	2010-03-31
ES2338047T3 (es)	2010-05-03
US8314145B2 (en)	2012-11-20

Publication	Publication Date	Title
IL191915A0 (en)	2008-12-29	High purity 17??-cyanomethyl-17??-hydroxy-estra-4,9-diene-3-one and process for the synthesis thereof
CN104610250B (zh)	2017-03-22	含三个氮杂环的1,2,3‑噻二唑‑5‑甲脒类化合物及合成
Plater et al.	2004	The CA. M lattice revisited. Gel formation from a linear bis-isocyanuric acid and 2-amino-4, 6-bis-(4-tert-butylphenylamino)-1, 3, 5-triazine
KR100917698B1 (ko)	2009-09-21	레트로졸의 제조를 위한 개선된 방법
JP2022502509A (ja)	2022-01-11	サルササポゲニン構造に基づく誘導体、医薬組成物及びその使用
DE69703228T2 (de)	2001-02-22	Neue 6-Hydroxy und 6-Oxo-Androstan Verbindungen mit Kardioaktivität und pharmazeutische Präparate davon
Marvadi et al.	2019	5-Chloro-2-thiophenyl-1, 2, 3-triazolylmethyldihydroquinolines as dual inhibitors of Mycobacterium tuberculosis and influenza virus: Synthesis and evaluation
Deng et al.	2009	Synthesis of alkenyldiarylmethanes (ADAMs) containing benzo [d] isoxazole and oxazolidin-2-one rings, a new series of potent non-nucleoside HIV-1 reverse transcriptase inhibitors
Campos et al.	1997	α-Iodination of enaminones with bis (pyridine) iodonium (I) tetrafluoroborate
HU216973B (hu)	1999-10-28	Eljárás imidazolszármazékok előállítására
Demirayak et al.	2002	Synthesis and antifungal activities of some aryl (benzofuran-2-yl) ketoximes
EP3088391B1 (en)	2017-11-29	Method for producing benzyl ester 2-aminonicotinate derivative
CN114890992A (zh)	2022-08-12	一种厄贝沙坦的杂质及其制备和检测方法以及厄贝沙坦的制备方法
Xu et al.	1999	Reactions of fluoroalkanesulfonyl azides with trimethylsilyl enol ethers
Ma et al.	2011	Synthesis and biological activity of naphthyl-substituted (B-ring) benzophenone derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors
CN113698409B (zh)	2022-07-19	一种多用途的二氮杂双环类化合物、制备方法及在合成药物中的应用
CN103130782A (zh)	2013-06-05	盐酸羟胺制备拉呋替丁的方法
Zheng et al.	2012	A convenient and efficient one-pot conversion of peimisine into cyclopamine
KR20100120558A (ko)	2010-11-16	염산 사포그릴레이트의 재결정 방법
CN108658852A (zh)	2018-10-16	新化合物吗拉贝胺、其制备方法及用途
CA2478867A1 (en)	2003-09-25	Formulations of anthraquinone derivatives
Petitjean et al.	2010	Functional formamidines: pyridine substituents make an exception in the usual doubly hydrogen-bonded formamidine dimer
JP2017039659A (ja)	2017-02-23	ミルタザピンの製造方法
CN116063373B (zh)	2025-04-15	天然产物27-Deoxywithaferin A的制备方法
Su et al.	2006	A convenient synthesis of 2-methyl-3-substituted-4 (3 H)-quinazolinones using bis (trichloromethyl) carbonate as condensing agent