JP6951451B2 - エストロゲン受容体モジュレーター - Google Patents
エストロゲン受容体モジュレーター Download PDFInfo
- Publication number
- JP6951451B2 JP6951451B2 JP2019538615A JP2019538615A JP6951451B2 JP 6951451 B2 JP6951451 B2 JP 6951451B2 JP 2019538615 A JP2019538615 A JP 2019538615A JP 2019538615 A JP2019538615 A JP 2019538615A JP 6951451 B2 JP6951451 B2 JP 6951451B2
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- compound
- tetrahydro
- pyrido
- indole
- 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.)
- Active
Links
- 0 CCC(C)C1=CC(C2(CC)C(C)C2)=C(*)C2C1C2 Chemical compound CCC(C)C1=CC(C2(CC)C(C)C2)=C(*)C2C1C2 0.000 description 6
- ALHOKFPHBWNKDF-MPBGBICISA-N C[C@H](Cc1c2[nH]c3ccccc13)N(CC(F)(F)F)[C@@H]2c(cc(cc1)Br)c1OC Chemical compound C[C@H](Cc1c2[nH]c3ccccc13)N(CC(F)(F)F)[C@@H]2c(cc(cc1)Br)c1OC ALHOKFPHBWNKDF-MPBGBICISA-N 0.000 description 2
- SXOWHFQHUQKEAK-QIKQAKPGSA-N CC(CN([C@H](C)Cc(c1c2)c3[nH]c1ccc2F)[C@@H]3C(C(F)=CC1)=C(C)C1Br)C(OC)=O Chemical compound CC(CN([C@H](C)Cc(c1c2)c3[nH]c1ccc2F)[C@@H]3C(C(F)=CC1)=C(C)C1Br)C(OC)=O SXOWHFQHUQKEAK-QIKQAKPGSA-N 0.000 description 1
- BUVXXDQCPBBBSZ-UHFFFAOYSA-N CCC(C)(CC)CC(CO)(F)F Chemical compound CCC(C)(CC)CC(CO)(F)F BUVXXDQCPBBBSZ-UHFFFAOYSA-N 0.000 description 1
- OQTBSRIIHCNDGF-UHFFFAOYSA-N CCC(CC(C(F)F)F)C(C)C Chemical compound CCC(CC(C(F)F)F)C(C)C OQTBSRIIHCNDGF-UHFFFAOYSA-N 0.000 description 1
- VUZWAQHSVLWNSK-UHFFFAOYSA-N CCC(CC)C(C1OC)C=CC=C1C(C)(C)CC Chemical compound CCC(CC)C(C1OC)C=CC=C1C(C)(C)CC VUZWAQHSVLWNSK-UHFFFAOYSA-N 0.000 description 1
- WYEZTLYMQFJJRH-UHFFFAOYSA-N CCOCC1(COC1)N Chemical compound CCOCC1(COC1)N WYEZTLYMQFJJRH-UHFFFAOYSA-N 0.000 description 1
- XNAYPGSXPCMEGR-KVUUWBKYSA-N C[C@H](CN([C@H](C)Cc(c1c2)c3[nH]c1ccc2F)[C@@H]3c(c(C)c(cc1)OCCOS(C)(=O)=O)c1F)C(OC)=O Chemical compound C[C@H](CN([C@H](C)Cc(c1c2)c3[nH]c1ccc2F)[C@@H]3c(c(C)c(cc1)OCCOS(C)(=O)=O)c1F)C(OC)=O XNAYPGSXPCMEGR-KVUUWBKYSA-N 0.000 description 1
- IURRISDHEMQJRJ-OYLFLEFRSA-N C[C@H](Cc1c2[nH]c3c1cccc3)N(CC(F)(F)F)[C@@H]2c(c(F)c(cc1)OCCNCCCF)c1F Chemical compound C[C@H](Cc1c2[nH]c3c1cccc3)N(CC(F)(F)F)[C@@H]2c(c(F)c(cc1)OCCNCCCF)c1F IURRISDHEMQJRJ-OYLFLEFRSA-N 0.000 description 1
- OGXNITFFRCUOPE-XHCCPWGMSA-N C[C@H](Cc1c2[nH]c3c1cccc3)N(CC1(COC1)F)[C@@H]2c(cc(cc1)OCCNCCCF)c1OC Chemical compound C[C@H](Cc1c2[nH]c3c1cccc3)N(CC1(COC1)F)[C@@H]2c(cc(cc1)OCCNCCCF)c1OC OGXNITFFRCUOPE-XHCCPWGMSA-N 0.000 description 1
- GYILNKRTBRMCHH-DNOBIOAJSA-N C[C@H](Cc1c2[nH]c3ccccc13)N(CC(F)(F)F)[C@@H]2c(c(F)ccc1OCCN(CCCF)C(OC(C)(C)C)=O)c1F Chemical compound C[C@H](Cc1c2[nH]c3ccccc13)N(CC(F)(F)F)[C@@H]2c(c(F)ccc1OCCN(CCCF)C(OC(C)(C)C)=O)c1F GYILNKRTBRMCHH-DNOBIOAJSA-N 0.000 description 1
- SLTNEYDLIVCLGL-VOIUYBSRSA-N C[C@H](Cc1c2[nH]c3ccccc13)N(CC(F)(F)F)[C@@H]2c(cc(cc1)OCCNCCCF)c1F Chemical compound C[C@H](Cc1c2[nH]c3ccccc13)N(CC(F)(F)F)[C@@H]2c(cc(cc1)OCCNCCCF)c1F SLTNEYDLIVCLGL-VOIUYBSRSA-N 0.000 description 1
- CGWBNWSADUPPAJ-VOIUYBSRSA-N C[C@H](Cc1c2[nH]c3ccccc13)N(CC(F)(F)F)[C@@H]2c(cc(nc1)OCCNCCCF)c1OC Chemical compound C[C@H](Cc1c2[nH]c3ccccc13)N(CC(F)(F)F)[C@@H]2c(cc(nc1)OCCNCCCF)c1OC CGWBNWSADUPPAJ-VOIUYBSRSA-N 0.000 description 1
- WQRGBGPICCTFCJ-UHFFFAOYSA-N NCCN(CCCF)C(OCc1ccccc1)=O Chemical compound NCCN(CCCF)C(OCc1ccccc1)=O WQRGBGPICCTFCJ-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Steroid Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762451971P | 2017-01-30 | 2017-01-30 | |
| US62/451,971 | 2017-01-30 | ||
| US201762523695P | 2017-06-22 | 2017-06-22 | |
| US62/523,695 | 2017-06-22 | ||
| US201762560304P | 2017-09-19 | 2017-09-19 | |
| US62/560,304 | 2017-09-19 | ||
| US201762592485P | 2017-11-30 | 2017-11-30 | |
| US62/592,485 | 2017-11-30 | ||
| PCT/EP2018/052040 WO2018138303A1 (en) | 2017-01-30 | 2018-01-29 | Estrogen receptor modulators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020505354A JP2020505354A (ja) | 2020-02-20 |
| JP2020505354A5 JP2020505354A5 (https=) | 2020-11-12 |
| JP6951451B2 true JP6951451B2 (ja) | 2021-10-20 |
Family
ID=61223883
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019538615A Active JP6951451B2 (ja) | 2017-01-30 | 2018-01-29 | エストロゲン受容体モジュレーター |
Country Status (35)
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109362222B (zh) | 2016-02-05 | 2021-03-19 | 益方生物科技(上海)股份有限公司 | 选择性雌激素受体降解物及其用途 |
| LT3555097T (lt) | 2016-12-16 | 2022-08-25 | Janssen Pharmaceutica Nv | Imidazo[4,5-d]pirolo[2,3-b]piridino junginiai kaip janus kinazės inhibitoriai |
| JOP20190144A1 (ar) | 2016-12-16 | 2019-06-16 | Janssen Pharmaceutica Nv | إيميدازو بيرولو بيريدين كمثبطات لعائلة jak الخاصة بإنزيمات الكيناز |
| TW202016110A (zh) | 2018-06-15 | 2020-05-01 | 比利時商健生藥品公司 | Ｊａｋ激酶家族之小分子抑制劑 |
| LT3810283T (lt) * | 2018-06-21 | 2023-08-25 | F. Hoffmann-La Roche Ag | 3-((1r,3r)-1-(2,6-difluor-4-((1-(3-fluorpropil)azetidin-3- il)amino) fenil)-3-metil-1,3,4,9-tetrahidro-2h-pirido[3,4-b]indol-2-il)- 2,2- difluorpropan-1-olio tartrato druskos kietosios formos, jų paruošimo procesas ir jų naudojimo būdai vėžiui gydyti |
| US20220370625A1 (en) * | 2019-09-19 | 2022-11-24 | Totus Medicines Inc. | Therapeutic conjugates |
| BR112023018286A2 (pt) | 2021-03-11 | 2023-10-31 | Janssen Pharmaceutica Nv | Lorpucitinib para uso no tratamento de distúrbios mediados por jak |
| CN115557920B (zh) * | 2022-09-22 | 2024-02-20 | 吉林奥来德光电材料股份有限公司 | 一种发光辅助材料、其制备方法及有机电致发光器件 |
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| ES2349762T3 (es) | 2000-08-10 | 2011-01-11 | Pfizer Italia S.R.L. | Biciclo-pirazoles activos como inhibidores de quinasas, procedimientos para su preparación y composiciones farmacéuticas que los comprenden. |
| US8008076B2 (en) * | 2004-04-27 | 2011-08-30 | Chugai Seiyaku Kabushiki Kaisha | Method of producing a nucleic acid encoding an antibody |
| TW200716628A (en) | 2005-03-22 | 2007-05-01 | Astrazeneca Ab | Novel compounds |
| FR2884252B1 (fr) | 2005-04-08 | 2007-05-18 | Aventis Pharma Sa | Nouveaux derives d'isoindoles, compositions les contenant, leur preparation et leurs utilisations pharmaceutiques notamment en tant qu'inhibiteurs d'activites de la proteine chaperone hsp90 |
| AR058223A1 (es) | 2005-11-25 | 2008-01-23 | Palau Pharma Sa | Un comuesto de derivados de pirazoloisoquinolina, un procedimiento para l a preparacion de dicho compuesto y una composicion farmaceutica que comprende dicho compuesto |
| EP2223925A1 (en) | 2006-10-09 | 2010-09-01 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| US20120157402A1 (en) * | 2009-05-27 | 2012-06-21 | Liangxian Cao | Methods for treating brain tumors |
| MX373926B (es) | 2009-05-27 | 2020-07-10 | Ptc Therapeutics Inc | Metodos para tratar cancer y estados no neoplasicos. |
| US20120157401A1 (en) | 2009-05-27 | 2012-06-21 | Ptc Therapeutics, Inc. | Methods for treating neurofibromatosis |
| HUE033581T2 (hu) | 2010-06-10 | 2017-12-28 | Seragon Pharmaceuticals Inc | Ösztrogén receptor modulátorok és alkalmazásaik |
| US8853423B2 (en) | 2010-06-17 | 2014-10-07 | Seragon Pharmaceuticals, Inc. | Indane estrogen receptor modulators and uses thereof |
| JP6112625B2 (ja) | 2011-12-14 | 2017-04-12 | セラゴン ファーマシューティカルズ，インク． | フッ素化したエストロゲン受容体モジュレーターおよびその使用 |
| TWI653235B (zh) * | 2013-05-28 | 2019-03-11 | 阿斯特捷利康公司 | 作為抗癌劑之吲哚衍生物 |
| EA031077B1 (ru) | 2013-06-19 | 2018-11-30 | Серагон Фармасьютикалз, Инк. | Модулятор рецептора эстрогена и его применения |
| BR112015030595A2 (pt) | 2013-06-19 | 2017-07-25 | Seragon Pharmaceuticals Inc | moduladores de receptor de estrogênio de azetidina e usos dos mesmos |
| WO2015092634A1 (en) | 2013-12-16 | 2015-06-25 | Novartis Ag | 1,2,3,4-tetrahydroisoquinoline compounds and compositions as selective estrogen receptor antagonists and degraders |
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| CN107406424B (zh) | 2014-12-18 | 2020-08-25 | 豪夫迈·罗氏有限公司 | 雌激素受体调节剂及其用途 |
| KR102785474B1 (ko) | 2014-12-18 | 2025-03-26 | 에프. 호프만-라 로슈 아게 | 테트라하이드로-피리도[3,4-b]인돌 에스트로겐 수용체 조절제 및 이의 용도 |
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| EP3303326B1 (en) | 2015-05-26 | 2020-12-16 | H. Hoffnabb-La Roche Ag | Heterocyclic estrogen receptor modulators and uses thereof |
| KR20180012853A (ko) | 2015-06-16 | 2018-02-06 | 지앙수 헨그루이 메디슨 컴퍼니 리미티드 | 피페리딘 유도체 및 이의 제조 방법 및 약학적 용도 |
| CN106518768B (zh) | 2015-09-15 | 2021-07-02 | 江苏恒瑞医药股份有限公司 | 丙烯酸类衍生物、其制备方法及其在医药上的应用 |
| KR102710603B1 (ko) | 2015-10-01 | 2024-09-27 | 올레마 파마슈티컬스 인코포레이티드 | 테트라히드로-1H-피리도[3,4-b]인돌 항에스트로겐 약물 |
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| WO2017192991A1 (en) | 2016-05-06 | 2017-11-09 | Xavier University Of Louisiana | Selective estrogen receptor down-regulators (serds) |
| WO2018001232A1 (zh) | 2016-06-29 | 2018-01-04 | 浙江海正药业股份有限公司 | 丙烯酸类衍生物及其制备方法和其在医药上的用途 |
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| KR102276022B1 (ko) | 2016-12-16 | 2021-07-13 | 일라이 릴리 앤드 캄파니 | 돌연변이체 idh1 및 idh2 억제제로서의 7-페닐에틸아미노-4h-피리미도[4,5-d][1,3]옥사진-2-온 화합물 |
| JOP20190144A1 (ar) | 2016-12-16 | 2019-06-16 | Janssen Pharmaceutica Nv | إيميدازو بيرولو بيريدين كمثبطات لعائلة jak الخاصة بإنزيمات الكيناز |
| TWI831738B (zh) | 2016-12-16 | 2024-02-11 | 美商瑞塔醫藥有限責任公司 | 用於抑制ＲＯＲγ及其他用途的嘧啶三環烯酮衍生物 |
| LT3555097T (lt) | 2016-12-16 | 2022-08-25 | Janssen Pharmaceutica Nv | Imidazo[4,5-d]pirolo[2,3-b]piridino junginiai kaip janus kinazės inhibitoriai |
| CA3045224A1 (en) | 2016-12-16 | 2018-06-21 | Basf Se | Pesticidal compounds |
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-
2018
- 2018-01-29 PT PT187050976T patent/PT3494116T/pt unknown
- 2018-01-29 SI SI201830022T patent/SI3494116T1/sl unknown
- 2018-01-29 CR CR20190379A patent/CR20190379A/es unknown
- 2018-01-29 SG SG11201906767XA patent/SG11201906767XA/en unknown
- 2018-01-29 JO JOP/2019/0183A patent/JOP20190183B1/ar active
- 2018-01-29 KR KR1020197025253A patent/KR102246668B1/ko active Active
- 2018-01-29 MX MX2019008438A patent/MX2019008438A/es unknown
- 2018-01-29 AU AU2018211495A patent/AU2018211495B2/en active Active
- 2018-01-29 PL PL18705097T patent/PL3494116T3/pl unknown
- 2018-01-29 LT LTEP18705097.6T patent/LT3494116T/lt unknown
- 2018-01-29 ES ES18705097T patent/ES2766249T3/es active Active
- 2018-01-29 US US15/881,962 patent/US10221173B2/en active Active
- 2018-01-29 WO PCT/EP2018/052040 patent/WO2018138303A1/en not_active Ceased
- 2018-01-29 TN TNP/2020/000009A patent/TN2020000009A1/en unknown
- 2018-01-29 JP JP2019538615A patent/JP6951451B2/ja active Active
- 2018-01-29 HU HUE18705097A patent/HUE047761T2/hu unknown
- 2018-01-29 UA UAA201909412A patent/UA125043C2/uk unknown
- 2018-01-29 MY MYPI2019004298A patent/MY196317A/en unknown
- 2018-01-29 RS RS20200018A patent/RS59770B1/sr unknown
- 2018-01-29 MA MA052555A patent/MA52555A/fr unknown
- 2018-01-29 EP EP19203383.5A patent/EP3689873B1/en active Active
- 2018-01-29 CN CN201880008715.8A patent/CN110214140B/zh active Active
- 2018-01-29 EP EP18705097.6A patent/EP3494116B1/en active Active
- 2018-01-29 ES ES19203383T patent/ES2931320T3/es active Active
- 2018-01-29 TW TW107103088A patent/TWI794205B/zh active
- 2018-01-29 SM SM20200010T patent/SMT202000010T1/it unknown
- 2018-01-29 PE PE2019001434A patent/PE20191500A1/es unknown
- 2018-01-29 DK DK18705097.6T patent/DK3494116T3/da active
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2019
- 2019-01-31 US US16/263,683 patent/US10590132B2/en active Active
- 2019-07-15 CL CL2019001991A patent/CL2019001991A1/es unknown
- 2019-07-16 DO DO2019000183A patent/DOP2019000183A/es unknown
- 2019-07-17 ZA ZA2019/04696A patent/ZA201904696B/en unknown
- 2019-07-25 IL IL268263A patent/IL268263B/en unknown
- 2019-07-26 NI NI201900080A patent/NI201900080A/es unknown
- 2019-07-26 PH PH12019501724A patent/PH12019501724A1/en unknown
- 2019-08-16 CO CONC2019/0008941A patent/CO2019008941A2/es unknown
- 2019-08-28 EC ECSENADI201962381A patent/ECSP19062381A/es unknown
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2020
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