JP2015501847A5 - - Google Patents
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- JP2015501847A5 JP2015501847A5 JP2014547528A JP2014547528A JP2015501847A5 JP 2015501847 A5 JP2015501847 A5 JP 2015501847A5 JP 2014547528 A JP2014547528 A JP 2014547528A JP 2014547528 A JP2014547528 A JP 2014547528A JP 2015501847 A5 JP2015501847 A5 JP 2015501847A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- fluoroalkyl
- alkyl
- solvate
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 26
- 125000002733 (C1-C6) fluoroalkyl group Chemical group 0.000 claims 23
- 150000003839 salts Chemical class 0.000 claims 20
- 239000012453 solvate Substances 0.000 claims 20
- 125000002947 alkylene group Chemical group 0.000 claims 13
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 12
- 229910052736 halogen Inorganic materials 0.000 claims 12
- 150000002367 halogens Chemical class 0.000 claims 12
- 125000006747 (C2-C10) heterocycloalkyl group Chemical group 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims 8
- 125000001072 heteroaryl group Chemical group 0.000 claims 8
- 230000007812 deficiency Effects 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 102000015694 estrogen receptors Human genes 0.000 claims 4
- 108010038795 estrogen receptors Proteins 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 102000007399 Nuclear hormone receptor Human genes 0.000 claims 2
- 108020005497 Nuclear hormone receptor Proteins 0.000 claims 2
- 125000003725 azepanyl group Chemical group 0.000 claims 2
- 125000002393 azetidinyl group Chemical group 0.000 claims 2
- 210000003169 central nervous system Anatomy 0.000 claims 2
- 230000001419 dependent effect Effects 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 201000010260 leiomyoma Diseases 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 239000000243 solution Substances 0.000 claims 2
- KJAAPZIFCQQQKX-UHFFFAOYSA-N 2-[4-[2-[3-(fluoromethyl)azetidin-1-yl]ethoxy]phenyl]-3-(3-hydroxyphenyl)-4-methyl-2h-chromen-6-ol Chemical compound O1C2=CC=C(O)C=C2C(C)=C(C=2C=C(O)C=CC=2)C1C(C=C1)=CC=C1OCCN1CC(CF)C1 KJAAPZIFCQQQKX-UHFFFAOYSA-N 0.000 claims 1
- NAHHIXKSGGSPOL-UHFFFAOYSA-N 2h-chromen-6-ol Chemical compound O1CC=CC2=CC(O)=CC=C21 NAHHIXKSGGSPOL-UHFFFAOYSA-N 0.000 claims 1
- 125000004208 3-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C([H])C(*)=C1[H] 0.000 claims 1
- -1 4-((S) -2-((R) -3-fluoropyrrolidin-1-yl) propoxy) phenyl Chemical group 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000023328 Basedow disease Diseases 0.000 claims 1
- 206010005949 Bone cancer Diseases 0.000 claims 1
- 208000018084 Bone neoplasm Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010008635 Cholestasis Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000035473 Communicable disease Diseases 0.000 claims 1
- 208000027219 Deficiency disease Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 201000009273 Endometriosis Diseases 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 208000015023 Graves' disease Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000029725 Metabolic bone disease Diseases 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010049088 Osteopenia Diseases 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000028017 Psychotic disease Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 208000016599 Uterine disease Diseases 0.000 claims 1
- 206010046798 Uterine leiomyoma Diseases 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 230000037182 bone density Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 231100000359 cholestasis Toxicity 0.000 claims 1
- 230000007870 cholestasis Effects 0.000 claims 1
- 230000007882 cirrhosis Effects 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 239000006185 dispersion Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000002526 effect on cardiovascular system Effects 0.000 claims 1
- 239000000839 emulsion Substances 0.000 claims 1
- 201000006828 endometrial hyperplasia Diseases 0.000 claims 1
- 239000000499 gel Substances 0.000 claims 1
- 208000002672 hepatitis B Diseases 0.000 claims 1
- 206010021093 hypospadias Diseases 0.000 claims 1
- 208000026278 immune system disease Diseases 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 238000010253 intravenous injection Methods 0.000 claims 1
- 208000019423 liver disease Diseases 0.000 claims 1
- 239000006210 lotion Substances 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000024714 major depressive disease Diseases 0.000 claims 1
- 230000009247 menarche Effects 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 230000007971 neurological deficit Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000002674 ointment Substances 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 239000006187 pill Substances 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 230000001850 reproductive effect Effects 0.000 claims 1
- 238000010254 subcutaneous injection Methods 0.000 claims 1
- 239000007929 subcutaneous injection Substances 0.000 claims 1
- 239000000725 suspension Substances 0.000 claims 1
- 239000003826 tablet Substances 0.000 claims 1
- 238000011200 topical administration Methods 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
- 208000010579 uterine corpus leiomyoma Diseases 0.000 claims 1
- 201000007954 uterine fibroid Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161570756P | 2011-12-14 | 2011-12-14 | |
| US61/570,756 | 2011-12-14 | ||
| PCT/US2012/069933 WO2013090836A1 (en) | 2011-12-14 | 2012-12-14 | Fluorinated estrogen receptor modulators and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015501847A JP2015501847A (ja) | 2015-01-19 |
| JP2015501847A5 true JP2015501847A5 (cg-RX-API-DMAC7.html) | 2016-02-12 |
| JP6112625B2 JP6112625B2 (ja) | 2017-04-12 |
Family
ID=48613247
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014547524A Pending JP2015500346A (ja) | 2011-12-14 | 2012-12-14 | エストロゲン受容体モジュレーターおよびその使用 |
| JP2014547528A Active JP6112625B2 (ja) | 2011-12-14 | 2012-12-14 | 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 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014547524A Pending JP2015500346A (ja) | 2011-12-14 | 2012-12-14 | エストロゲン受容体モジュレーターおよびその使用 |
Country Status (15)
Families Citing this family (62)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2013528223A (ja) | 2010-06-10 | 2013-07-08 | アラゴン ファーマシューティカルズ，インク． | エストロゲン受容体モジュレーターおよびその用途 |
| US9193714B2 (en) | 2011-12-14 | 2015-11-24 | Seragon Pharmaceuticals, Inc. | Fluorinated estrogen receptor modulators and uses thereof |
| MD20140054A2 (ro) | 2011-12-16 | 2014-10-31 | Olema Pharmaceuticals, Inc. | Compuşi noi de benzopiran, compoziţii şi utilizări ale acestora |
| BR112015030595A2 (pt) | 2013-06-19 | 2017-07-25 | Seragon Pharmaceuticals Inc | moduladores de receptor de estrogênio de azetidina e usos dos mesmos |
| BR112015031903A8 (pt) | 2013-06-19 | 2019-12-31 | Seragon Pharmaceuticals Inc | composto, sal farmaceuticamente aceitável, composição farmacêutica e uso de um composto |
| KR20160132029A (ko) * | 2014-03-13 | 2016-11-16 | 에프. 호프만-라 로슈 아게 | 에스트로젠 수용체 돌연변이체의 조절을 위한 방법 및 조성물 |
| KR20160124909A (ko) * | 2014-03-13 | 2016-10-28 | 에프. 호프만-라 로슈 아게 | 에스트로겐 수용체 조절제를 함유하는 치료 조합물 |
| JP2017534627A (ja) | 2014-11-06 | 2017-11-24 | ノースウエスタン ユニバーシティＮｏｒｔｈｗｅｓｔｅｒｎ Ｕｎｉｖｅｒｓｉｔｙ | 癌細胞運動性の阻害 |
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- 2012-12-14 JP JP2014547524A patent/JP2015500346A/ja active Pending
- 2012-12-14 BR BR112014014124A patent/BR112014014124A2/pt not_active Application Discontinuation
- 2012-12-14 EP EP12857534.7A patent/EP2791133B1/en active Active
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- 2012-12-14 WO PCT/US2012/069933 patent/WO2013090836A1/en not_active Ceased
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- 2012-12-14 CA CA2857057A patent/CA2857057A1/en not_active Abandoned
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2014
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- 2014-06-13 PH PH12014501351A patent/PH12014501351A1/en unknown