JP2010529152A5 - - Google Patents
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- Publication number
- JP2010529152A5 JP2010529152A5 JP2010511525A JP2010511525A JP2010529152A5 JP 2010529152 A5 JP2010529152 A5 JP 2010529152A5 JP 2010511525 A JP2010511525 A JP 2010511525A JP 2010511525 A JP2010511525 A JP 2010511525A JP 2010529152 A5 JP2010529152 A5 JP 2010529152A5
- Authority
- JP
- Japan
- Prior art keywords
- homo
- cyano
- androst
- methylene
- ene
- Prior art date
- Legal status (The legal status 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 status listed.)
- Pending
Links
- 229910052739 hydrogen Inorganic materials 0.000 claims 14
- 239000001257 hydrogen Substances 0.000 claims 14
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 229940011871 estrogen Drugs 0.000 claims 8
- 239000000262 estrogen Substances 0.000 claims 8
- 239000003814 drug Substances 0.000 claims 7
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000000816 ethylene group Chemical group [H]C([H])([*:1])C([H])([H])[*:2] 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- BFPYWIDHMRZLRN-UHFFFAOYSA-N 17alpha-ethynyl estradiol Natural products OC1=CC=C2C3CCC(C)(C(CC4)(O)C#C)C4C3CCC2=C1 BFPYWIDHMRZLRN-UHFFFAOYSA-N 0.000 claims 1
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 claims 1
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- RSEPBGGWRJCQGY-RBRWEJTLSA-N Estradiol valerate Chemical compound C1CC2=CC(O)=CC=C2[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CCCC)[C@@]1(C)CC2 RSEPBGGWRJCQGY-RBRWEJTLSA-N 0.000 claims 1
- BFPYWIDHMRZLRN-SLHNCBLASA-N Ethinyl estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 BFPYWIDHMRZLRN-SLHNCBLASA-N 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 238000006664 bond formation reaction Methods 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 229960005309 estradiol Drugs 0.000 claims 1
- 229930182833 estradiol Natural products 0.000 claims 1
- 229960004766 estradiol valerate Drugs 0.000 claims 1
- 229960002568 ethinylestradiol Drugs 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- -1 hydroxymethylene Chemical group 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102007027636A DE102007027636A1 (de) | 2007-06-12 | 2007-06-12 | 17ß-Cyano-18a-homo-19-nor-androst-4-en-Derivat, dessen Verwendung und das Derivat enthaltende Arzneimittel |
| PCT/EP2008/004428 WO2008151745A1 (de) | 2007-06-12 | 2008-06-04 | 17beta-cyano-18a-homo-19-nor-androst-4-en-derivat, dessen verwendung und das derivat enthaltende arzneimittel |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010529152A JP2010529152A (ja) | 2010-08-26 |
| JP2010529152A5 true JP2010529152A5 (https=) | 2011-07-21 |
Family
ID=38858372
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010511525A Pending JP2010529152A (ja) | 2007-06-12 | 2008-06-04 | １７β−シアノ−１８ａ−ホモ−１９−ノル−アンドロスト−４−エン誘導体、その使用及び該誘導体を含む医薬 |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US20090048218A1 (https=) |
| EP (1) | EP2178899B1 (https=) |
| JP (1) | JP2010529152A (https=) |
| KR (1) | KR20100017780A (https=) |
| CN (1) | CN101679477A (https=) |
| AR (1) | AR066970A1 (https=) |
| AU (1) | AU2008261277A1 (https=) |
| BR (1) | BRPI0813455A2 (https=) |
| CA (1) | CA2689563A1 (https=) |
| CL (1) | CL2008001721A1 (https=) |
| DE (1) | DE102007027636A1 (https=) |
| ES (1) | ES2397879T3 (https=) |
| IL (1) | IL202300A0 (https=) |
| MX (1) | MX2009013626A (https=) |
| PA (1) | PA8784201A1 (https=) |
| PE (1) | PE20090312A1 (https=) |
| RU (1) | RU2010100334A (https=) |
| TW (1) | TW200906846A (https=) |
| UY (1) | UY31145A1 (https=) |
| WO (1) | WO2008151745A1 (https=) |
| ZA (1) | ZA201000185B (https=) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010066354A1 (de) * | 2008-12-12 | 2010-06-17 | Bayer Schering Pharma Aktiengesellschaft | VERWENDUNG VON 17β-CYANO-18A-HOMO-19-NOR-ANDROST-4-EN-DERIVATEN ZUR HERSTELLUNG EINES ARZNEIMITTELS IN DEPOT-FORM ZUR PARENTERALEN ANWENDUNG SOWIE DEPOT-ARZNEIMITTEL ENTHALTEND 17β-CYANO-18A-HOMO-19-NOR-ANDROST-4-EN-DERIVATE ZUR PARENTERALEN ANWENDUNG |
| WO2012059594A1 (en) | 2010-11-04 | 2012-05-10 | Bayer Pharma Aktiengesellschaft | Mineralcorticoid receptor antagonists for the treatment of corticoid-induced obesity |
| WO2012116290A2 (en) * | 2011-02-25 | 2012-08-30 | Washington University | Neuroactive 17(20)-z-vinylcyano-substituted steroids, prodrugs thereof, and methods of treatment using same |
| CN119192266A (zh) | 2011-10-14 | 2024-12-27 | 萨奇治疗股份有限公司 | 3,3-二取代的19-去甲孕甾烷化合物、组合物、及其用途 |
| MX365644B (es) | 2012-12-18 | 2019-06-10 | Univ Washington | Esteroides neuroactivos sustituidos con 19-alcoxi-17, profarmacos de los mismos, y metodos de tratamiento usando los mismos. |
| US9512170B2 (en) | 2013-03-01 | 2016-12-06 | Washington University | Neuroactive 13, 17-substituted steroids as modulators for GABA type-A receptors |
| US9365502B2 (en) | 2013-03-11 | 2016-06-14 | Washington University | Neuroactive substituted cyclopenta[b]phenanthrenes as modulators for GABA type-A receptors |
| US9562026B2 (en) | 2013-03-14 | 2017-02-07 | Washington University | Neuroactive substituted cyclopent[a]anthracenes as modulators for GABA type-A receptors |
| WO2014169831A1 (en) | 2013-04-17 | 2014-10-23 | Sage Therapeutics, Inc. | 19-nor c3,3-disubstituted c21-c-bound heteroaryl steroids and methods of use thereof |
| JP6470258B2 (ja) | 2013-04-17 | 2019-02-13 | セージ セラピューティクス， インコーポレイテッド | １９−ノルｃ３，３−ジ置換ｃ２１−ｎ−ピラゾリルステロイドおよびその使用方法 |
| ES2807264T3 (es) | 2013-04-17 | 2021-02-22 | Sage Therapeutics Inc | Esteroides neuroactivos 19-nor para métodos de tratamiento |
| WO2014169836A1 (en) | 2013-04-17 | 2014-10-23 | Sage Therapeutics, Inc. | 19-nor neuroactive steroids and methods of use thereof |
| WO2015010054A2 (en) | 2013-07-19 | 2015-01-22 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| ES2848823T3 (es) | 2013-08-23 | 2021-08-12 | Sage Therapeutics Inc | Esteroides neuroactivos, composiciones y usos de los mismos |
| WO2015195962A1 (en) | 2014-06-18 | 2015-12-23 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| US10577390B2 (en) | 2014-10-16 | 2020-03-03 | Sage Therapeutics, Inc. | Compositions and methods for treating CNS disorders |
| ME03809B (me) | 2014-10-16 | 2021-04-20 | Sage Therapeutics Inc | KOMPOZICIJE I POSTUPCI ZA LEČENJE POREMEĆAJA CNS-a |
| WO2016082789A1 (en) | 2014-11-27 | 2016-06-02 | Sage Therapeutics, Inc. | Compositions and methods for treating cns disorders |
| WO2016123056A1 (en) | 2015-01-26 | 2016-08-04 | Sage Therapeutics, Inc. | Compositions and methods for treating cns disorders |
| EP4155314A1 (en) | 2015-02-20 | 2023-03-29 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| MA45599A (fr) | 2016-07-11 | 2019-05-15 | Sage Therapeutics Inc | Stéroïdes neuroactifs substitués en c17, c20 et c21 et leurs procédés d'utilisation |
| US20190233465A1 (en) | 2016-07-11 | 2019-08-01 | Sage Therapeutics, Inc. | C7, c12, and c16 substituted neuroactive steroids and their methods of use |
| CR20240234A (es) | 2019-05-31 | 2024-07-09 | Sage Therapeutics Inc | ESTEROIDES NEUROACTIVOS Y COMPOSICIONES DE ESTOS (Divisional 2021-629) |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3043833A (en) * | 1961-07-14 | 1962-07-10 | Ormonoterapia Richter Spa | 17-cyanohydrin of 19-nor androstenedione and 3-derivatives thereof |
| DE1183500B (de) | 1962-10-12 | 1964-12-17 | Schering Ag | Verfahren zur Herstellung von alpha, beta-Methylenketonen der Steroidreihe |
| US3579509A (en) * | 1965-06-21 | 1971-05-18 | Smith Kline French Lab | Process and 6-beta-substituted ethyl intermediates for preparing 6,6-ethylene-3-keto-delta**4 steroids |
| GB1089945A (en) * | 1965-09-23 | 1967-11-08 | British Drug Houses Ltd | Steroidal-6-spirocyclopropyl-4-en-3-ones |
| IL32699A (en) * | 1968-07-30 | 1973-06-29 | American Home Prod | 6-substituted-13-polycarbonalkyl-18,19 dinorpregn-4-en-3-ones,their preparation and pharmaceutical compositions containing them |
| FR2081561B1 (https=) * | 1970-03-03 | 1973-04-06 | Roussel Uclaf | |
| US3705179A (en) | 1971-03-15 | 1972-12-05 | American Home Prod | Antiandrogenic steroids |
| FR2139708B1 (https=) * | 1971-06-01 | 1974-08-23 | Roussel Uclaf | |
| US3994937A (en) * | 1972-02-11 | 1976-11-30 | Schering Aktiengesellschaft | 15α,16α-Methylene-4-estren-17β-ols |
| BE795241A (fr) | 1972-02-11 | 1973-08-09 | Schering Ag | 15alpha, 16alpha-methylene-4-oestren-17beta-ols-methylenz-4-oestren-17beta-ols et leur procede de preparation |
| NL7701384A (nl) | 1977-02-10 | 1978-08-14 | Akzo Nv | Werkwijze voor het bereiden van nieuwe steroiden van de oestraanreeks. |
| DE2922500A1 (de) | 1979-05-31 | 1980-12-04 | Schering Ag | 6 beta .7 beta |
| US4252800A (en) * | 1979-10-05 | 1981-02-24 | United States Of America | 7α-methylnorethindrone enanthate and its use in long term suppression of fertility in female mammals |
| US4544554A (en) * | 1983-09-26 | 1985-10-01 | Ortho Pharmaceutical Corporation | Triphasic oral contraceptive |
| DE3402329A1 (de) | 1984-01-20 | 1985-08-01 | Schering AG, 1000 Berlin und 4709 Bergkamen | 6,6-ethylen-15,16-methylen-3-oxo-17(alpha)-pregn-4-en-21,17-carbolactone, verfahren zu deren herstellung und diese enthaltende pharmazeutische praeparate |
| DE4344462C2 (de) * | 1993-12-22 | 1996-02-01 | Schering Ag | Zusammensetzung für die Empfängnisverhütung |
| EP0785211A1 (en) * | 1996-01-22 | 1997-07-23 | Laboratoire Theramex | New substituted 19-nor-pregnane derivatives |
| DE19651000A1 (de) * | 1996-12-01 | 1998-06-04 | Schering Ag | Oxyiminopregnancarbolactone |
| DE102004063864A1 (de) * | 2004-12-30 | 2006-07-13 | Schering Ag | 18-Methyl-19-nor-17-pregn-4-en21,17-carbolactone, sowie diese enthaltende pharmazeutische Präparate |
-
2007
- 2007-06-12 DE DE102007027636A patent/DE102007027636A1/de not_active Withdrawn
-
2008
- 2008-06-04 WO PCT/EP2008/004428 patent/WO2008151745A1/de not_active Ceased
- 2008-06-04 CN CN200880020040A patent/CN101679477A/zh active Pending
- 2008-06-04 KR KR1020097025931A patent/KR20100017780A/ko not_active Withdrawn
- 2008-06-04 CA CA002689563A patent/CA2689563A1/en not_active Abandoned
- 2008-06-04 ES ES08758989T patent/ES2397879T3/es active Active
- 2008-06-04 JP JP2010511525A patent/JP2010529152A/ja active Pending
- 2008-06-04 AU AU2008261277A patent/AU2008261277A1/en not_active Abandoned
- 2008-06-04 EP EP08758989A patent/EP2178899B1/de not_active Not-in-force
- 2008-06-04 MX MX2009013626A patent/MX2009013626A/es not_active Application Discontinuation
- 2008-06-04 BR BRPI0813455-3A2A patent/BRPI0813455A2/pt not_active Application Discontinuation
- 2008-06-04 RU RU2010100334/04A patent/RU2010100334A/ru not_active Application Discontinuation
- 2008-06-11 PE PE2008000992A patent/PE20090312A1/es not_active Application Discontinuation
- 2008-06-11 PA PA20088784201A patent/PA8784201A1/es unknown
- 2008-06-11 US US12/137,122 patent/US20090048218A1/en not_active Abandoned
- 2008-06-11 UY UY31145A patent/UY31145A1/es not_active Application Discontinuation
- 2008-06-11 CL CL2008001721A patent/CL2008001721A1/es unknown
- 2008-06-11 TW TW097121799A patent/TW200906846A/zh unknown
- 2008-06-12 AR ARP080102498A patent/AR066970A1/es unknown
-
2009
- 2009-11-24 IL IL202300A patent/IL202300A0/en unknown
-
2010
- 2010-01-11 ZA ZA2010/00185A patent/ZA201000185B/en unknown
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