JP2017514853A5 - - Google Patents

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Publication number: JP2017514853A5
Authority: JP; Japan
Prior art keywords: item; agent; composition according; cancer; composition
Prior art date: 2015-04-30
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.): Granted

Application number

JP2016566286A

Other languages

English (en)

Japanese (ja)

Other versions

JP6594339B2 (ja

JP2017514853A (ja

Filing date

2015-04-30

Publication date

2018-06-14

2014-05-08 Priority claimed from CN201410192569.2A external-priority patent/CN104208069A/zh

2015-04-30 Application filed filed Critical

2017-06-08 Publication of JP2017514853A publication Critical patent/JP2017514853A/ja

2018-06-14 Publication of JP2017514853A5 publication Critical patent/JP2017514853A5/ja

2019-10-23 Application granted granted Critical

2019-10-23 Publication of JP6594339B2 publication Critical patent/JP6594339B2/ja

Status Active legal-status Critical Current

2035-04-30 Anticipated expiration legal-status Critical

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239000003795 chemical substances by application Substances 0.000 claims description 28
NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 claims description 24
229960004622 raloxifene Drugs 0.000 claims description 20
GZUITABIAKMVPG-UHFFFAOYSA-N raloxifene Chemical compound C1=CC(O)=CC=C1C1=C(C(=O)C=2C=CC(OCCN3CCCCC3)=CC=2)C2=CC=C(O)C=C2S1 GZUITABIAKMVPG-UHFFFAOYSA-N 0.000 claims description 20
239000008194 pharmaceutical composition Substances 0.000 claims description 19
239000003886 aromatase inhibitor Substances 0.000 claims description 18
229940122815 Aromatase inhibitor Drugs 0.000 claims description 16
239000000203 mixture Substances 0.000 claims description 16
229940079593 drug Drugs 0.000 claims description 15
239000003814 drug Substances 0.000 claims description 15
229960001603 tamoxifen Drugs 0.000 claims description 12
206010028980 Neoplasm Diseases 0.000 claims description 7
229960002932 anastrozole Drugs 0.000 claims description 7
YBBLVLTVTVSKRW-UHFFFAOYSA-N anastrozole Chemical compound N#CC(C)(C)C1=CC(C(C)(C#N)C)=CC(CN2N=CN=C2)=C1 YBBLVLTVTVSKRW-UHFFFAOYSA-N 0.000 claims description 7
201000011510 cancer Diseases 0.000 claims description 7
239000002552 dosage form Substances 0.000 claims description 6
206010027304 Menopausal symptoms Diseases 0.000 claims description 3
206010006187 Breast cancer Diseases 0.000 claims description 2
208000026310 Breast neoplasm Diseases 0.000 claims description 2
206010009944 Colon cancer Diseases 0.000 claims description 2
206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
208000005718 Stomach Neoplasms Diseases 0.000 claims description 2
108091008605 VEGF receptors Proteins 0.000 claims description 2
102100033177 Vascular endothelial growth factor receptor 2 Human genes 0.000 claims description 2
229940046844 aromatase inhibitors Drugs 0.000 claims description 2
208000032852 chronic lymphocytic leukemia Diseases 0.000 claims description 2
208000029742 colonic neoplasm Diseases 0.000 claims description 2
102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims description 2
108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims description 2
102000015694 estrogen receptors Human genes 0.000 claims description 2
108010038795 estrogen receptors Proteins 0.000 claims description 2
206010017758 gastric cancer Diseases 0.000 claims description 2
201000007270 liver cancer Diseases 0.000 claims description 2
208000014018 liver neoplasm Diseases 0.000 claims description 2
201000005202 lung cancer Diseases 0.000 claims description 2
208000020816 lung neoplasm Diseases 0.000 claims description 2
208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
239000012528 membrane Substances 0.000 claims description 2
YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims description 2
201000002528 pancreatic cancer Diseases 0.000 claims description 2
208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
201000011549 stomach cancer Diseases 0.000 claims description 2
UCJGJABZCDBEDK-UHFFFAOYSA-N bazedoxifene Chemical compound C=1C=C(OCCN2CCCCCC2)C=CC=1CN1C2=CC=C(O)C=C2C(C)=C1C1=CC=C(O)C=C1 UCJGJABZCDBEDK-UHFFFAOYSA-N 0.000 description 4
229960000817 bazedoxifene Drugs 0.000 description 4
-1 borozole Chemical compound 0.000 description 4
230000000694 effects Effects 0.000 description 4
229960002367 lasofoxifene Drugs 0.000 description 4
GXESHMAMLJKROZ-IAPPQJPRSA-N lasofoxifene Chemical compound C1([C@@H]2[C@@H](C3=CC=C(C=C3CC2)O)C=2C=CC(OCCN3CCCC3)=CC=2)=CC=CC=C1 GXESHMAMLJKROZ-IAPPQJPRSA-N 0.000 description 4
NOECSYBNZHIVHW-LKADTRSGSA-N [(2r,3as,3bs,5as,6r,8as,8br,10as)-2,6-diethynyl-3a,5a-dimethyl-2-propanoyloxy-1,3,3b,4,5,7,8,8a,8b,9,10,10a-dodecahydroindeno[5,4-e]inden-6-yl] propanoate Chemical compound C([C@]1(C)[C@](OC(=O)CC)(C#C)CC[C@H]1[C@@H]1CC2)C[C@@H]1[C@]1(C)[C@@H]2C[C@@](C#C)(OC(=O)CC)C1 NOECSYBNZHIVHW-LKADTRSGSA-N 0.000 description 3
MCGDSOGUHLTADD-UHFFFAOYSA-N arzoxifene Chemical compound C1=CC(OC)=CC=C1C1=C(OC=2C=CC(OCCN3CCCCC3)=CC=2)C2=CC=C(O)C=C2S1 MCGDSOGUHLTADD-UHFFFAOYSA-N 0.000 description 3
229950005529 arzoxifene Drugs 0.000 description 3
XZEUAXYWNKYKPL-WDYNHAJCSA-N levormeloxifene Chemical compound C1([C@H]2[C@@H](C3=CC=C(C=C3OC2(C)C)OC)C=2C=CC(OCCN3CCCC3)=CC=2)=CC=CC=C1 XZEUAXYWNKYKPL-WDYNHAJCSA-N 0.000 description 3
229950002728 levormeloxifene Drugs 0.000 description 3
CLPFFLWZZBQMAO-UHFFFAOYSA-N 4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile Chemical compound C1=CC(C#N)=CC=C1C1N2C=NC=C2CCC1 CLPFFLWZZBQMAO-UHFFFAOYSA-N 0.000 description 2
BFYIZQONLCFLEV-DAELLWKTSA-N Aromasine Chemical compound O=C1C=C[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CC(=C)C2=C1 BFYIZQONLCFLEV-DAELLWKTSA-N 0.000 description 2
229960000255 exemestane Drugs 0.000 description 2
229950011548 fadrozole Drugs 0.000 description 2
229960004421 formestane Drugs 0.000 description 2
OSVMTWJCGUFAOD-KZQROQTASA-N formestane Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1O OSVMTWJCGUFAOD-KZQROQTASA-N 0.000 description 2
229960003881 letrozole Drugs 0.000 description 2
HPJKCIUCZWXJDR-UHFFFAOYSA-N letrozole Chemical compound C1=CC(C#N)=CC=C1C(N1N=CN=C1)C1=CC=C(C#N)C=C1 HPJKCIUCZWXJDR-UHFFFAOYSA-N 0.000 description 2
229960003969 ospemifene Drugs 0.000 description 2
LUMKNAVTFCDUIE-VHXPQNKSSA-N ospemifene Chemical compound C1=CC(OCCO)=CC=C1C(\C=1C=CC=CC=1)=C(\CCCl)C1=CC=CC=C1 LUMKNAVTFCDUIE-VHXPQNKSSA-N 0.000 description 2
206010003694 Atrophy Diseases 0.000 description 1
208000004930 Fatty Liver Diseases 0.000 description 1
206010019708 Hepatic steatosis Diseases 0.000 description 1
206010022489 Insulin Resistance Diseases 0.000 description 1
208000001132 Osteoporosis Diseases 0.000 description 1
230000037444 atrophy Effects 0.000 description 1
239000008280 blood Substances 0.000 description 1
210000004369 blood Anatomy 0.000 description 1
239000005018 casein Substances 0.000 description 1
BECPQYXYKAMYBN-UHFFFAOYSA-N casein, tech. Chemical compound NCCCCC(C(O)=O)N=C(O)C(CC(O)=O)N=C(O)C(CCC(O)=N)N=C(O)C(CC(C)C)N=C(O)C(CCC(O)=O)N=C(O)C(CC(O)=O)N=C(O)C(CCC(O)=O)N=C(O)C(C(C)O)N=C(O)C(CCC(O)=N)N=C(O)C(CCC(O)=N)N=C(O)C(CCC(O)=N)N=C(O)C(CCC(O)=O)N=C(O)C(CCC(O)=O)N=C(O)C(COP(O)(O)=O)N=C(O)C(CCC(O)=N)N=C(O)C(N)CC1=CC=CC=C1 BECPQYXYKAMYBN-UHFFFAOYSA-N 0.000 description 1
235000021240 caseins Nutrition 0.000 description 1
230000001413 cellular effect Effects 0.000 description 1
230000003247 decreasing effect Effects 0.000 description 1
208000010706 fatty liver disease Diseases 0.000 description 1
150000002632 lipids Chemical class 0.000 description 1
210000000056 organ Anatomy 0.000 description 1
231100000240 steatosis hepatitis Toxicity 0.000 description 1
UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 description 1
208000001072 type 2 diabetes mellitus Diseases 0.000 description 1
230000004584 weight gain Effects 0.000 description 1
235000019786 weight gain Nutrition 0.000 description 1

JP2016566286A 2014-05-08 2015-04-30 アノルドリン組成物および疾患を処置するための方法 Active JP6594339B2 (ja)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
CN201410192569.2A CN104208069A (zh)	2014-05-08	2014-05-08	双炔失碳酯组合物和疾病治疗方法
CN201410192569.2		2014-05-08
PCT/CN2015/077942 WO2015169173A1 (en)	2014-05-08	2015-04-30	Anordrin compositions and methods for treating diseases

Related Child Applications (1)

Application Number	Title	Priority Date	Filing Date
JP2019089931A Division JP2019142969A (ja)	2014-05-08	2019-05-10	アノルドリン組成物および疾患を処置するための方法

Publications (3)

Publication Number	Publication Date
JP2017514853A JP2017514853A (ja)	2017-06-08
JP2017514853A5 true JP2017514853A5 (2)	2018-06-14
JP6594339B2 JP6594339B2 (ja)	2019-10-23

Family

ID=52090245

Family Applications (4)

Application Number	Title	Priority Date	Filing Date
JP2016566286A Active JP6594339B2 (ja)	2014-05-08	2015-04-30	アノルドリン組成物および疾患を処置するための方法
JP2019089931A Withdrawn JP2019142969A (ja)	2014-05-08	2019-05-10	アノルドリン組成物および疾患を処置するための方法
JP2020219768A Active JP7084467B2 (ja)	2014-05-08	2020-12-29	アノルドリン組成物および疾患を処置するための方法
JP2022042432A Withdrawn JP2022078330A (ja)	2014-05-08	2022-03-17	アノルドリン組成物および疾患を処置するための方法

Family Applications After (3)

Application Number	Title	Priority Date	Filing Date
JP2019089931A Withdrawn JP2019142969A (ja)	2014-05-08	2019-05-10	アノルドリン組成物および疾患を処置するための方法
JP2020219768A Active JP7084467B2 (ja)	2014-05-08	2020-12-29	アノルドリン組成物および疾患を処置するための方法
JP2022042432A Withdrawn JP2022078330A (ja)	2014-05-08	2022-03-17	アノルドリン組成物および疾患を処置するための方法

Country Status (5)

Country	Link
US (3)	US10231978B2 (2)
EP (1)	EP3139928B1 (2)
JP (4)	JP6594339B2 (2)
CN (3)	CN113101292B (2)
WO (1)	WO2015169173A1 (2)

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CN113101292B (zh)	2014-05-08	2023-07-11	上海市生物医药技术研究院	双炔失碳酯组合物和疾病治疗方法
CN105279394B (zh) *	2015-10-13	2017-12-26	山西农业大学	用于神经肽受体筛选的方法
JP6788255B2 (ja) *	2015-11-19	2020-11-25	国立大学法人信州大学	新規ベクター及びこれを用いた可溶化タンパク質の製造方法
ES2909576T3 (es)	2016-10-11	2022-05-09	Univ Duke	Tratamiento con lasofoxifeno del cáncer de mama ER+
WO2018090049A1 (en) *	2016-11-14	2018-05-17	The Brigham And Women's Hospital, Inc.	Estrogen sensing through gper1 regulates normal and malignant liver growth
CN115737637A (zh)	2017-01-10	2023-03-07	王巍	拉索昔芬调节膜结合雌激素信号的应用及治疗癌症的方法
WO2019041078A1 (en) *	2017-08-28	2019-03-07	Zhejiang Jiachi Pharmaceutical Development Ltd.	ASYMMETRIC SYNTHESIS AND USES OF COMPOUNDS IN TREATMENT OF DISEASES
CN109662968B (zh) *	2017-10-13	2021-05-18	上海奥奇医药科技有限公司	含A-失碳-5α雄甾烷化合物的升白制剂及其应用
US11497730B2 (en)	2018-04-10	2022-11-15	Duke University	Lasofoxifene treatment of breast cancer
CN111773388B (zh) *	2019-04-04	2023-07-18	上海奥奇医药科技有限公司	A-失碳-5α雄甾烷化合物类药物与抗癌药物的联合应用
US20210299098A1 (en) *	2020-03-31	2021-09-30	Cipla Limited	Selective estrogen receptor modulator for treatment of pancreatic cancer
WO2022246634A1 (en) *	2021-05-25	2022-12-01	Zhejiang Jiachi Development Pharmaceuticals Ltd.	Compositions for treating insomnia and uses thereof
GB202116903D0 (en)	2021-11-18	2022-01-05	Sermonix Pharmaceuticals Inc	Lasofoxifene treatment of aromatase-resistant er+ cancer

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US5001120A (en) *	1989-05-10	1991-03-19	Natural Pharmacia International, Inc.	Use of A-Nor-steroids as malignant cells growth inhibitors
US7985422B2 (en) *	2002-08-05	2011-07-26	Torrent Pharmaceuticals Limited	Dosage form
WO2004026823A1 (en) *	2002-09-20	2004-04-01	Pfizer Products Inc.	Amide and sulfonamide ligands for the estrogen receptor
WO2005048942A2 (en) *	2003-11-13	2005-06-02	Pharmacia Corporation	Combination therapy comprising a cox-2 inhibitor and an antineoplastic agent
CN1976944A (zh) *	2004-06-30	2007-06-06	默克公司	雌激素受体调节剂
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2014
- 2014-05-08 CN CN202110246492.2A patent/CN113101292B/zh active Active
- 2014-05-08 CN CN202010899146.XA patent/CN111956653B/zh active Active
- 2014-05-08 CN CN201410192569.2A patent/CN104208069A/zh active Pending
2015
- 2015-04-30 EP EP15788674.8A patent/EP3139928B1/en active Active
- 2015-04-30 JP JP2016566286A patent/JP6594339B2/ja active Active
- 2015-04-30 WO PCT/CN2015/077942 patent/WO2015169173A1/en not_active Ceased
- 2015-04-30 US US15/309,426 patent/US10231978B2/en active Active
2019
- 2019-01-30 US US16/262,617 patent/US10857158B2/en active Active
- 2019-05-10 JP JP2019089931A patent/JP2019142969A/ja not_active Withdrawn
2020
- 2020-11-19 US US16/953,168 patent/US11911397B2/en active Active
- 2020-12-29 JP JP2020219768A patent/JP7084467B2/ja active Active
2022
- 2022-03-17 JP JP2022042432A patent/JP2022078330A/ja not_active Withdrawn

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