JP2010511010A5 - - Google Patents
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- Publication number
- JP2010511010A5 JP2010511010A5 JP2009538695A JP2009538695A JP2010511010A5 JP 2010511010 A5 JP2010511010 A5 JP 2010511010A5 JP 2009538695 A JP2009538695 A JP 2009538695A JP 2009538695 A JP2009538695 A JP 2009538695A JP 2010511010 A5 JP2010511010 A5 JP 2010511010A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- optionally
- membered
- ring
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 62
- 125000001424 substituent group Chemical group 0.000 claims 47
- 229910052736 halogen Inorganic materials 0.000 claims 39
- 150000002367 halogens Chemical class 0.000 claims 39
- -1 substituted Chemical class 0.000 claims 39
- 125000003118 aryl group Chemical group 0.000 claims 38
- 125000004122 cyclic group Chemical group 0.000 claims 34
- 229910052760 oxygen Inorganic materials 0.000 claims 31
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 30
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 28
- 229910052757 nitrogen Inorganic materials 0.000 claims 28
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims 27
- 125000001072 heteroaryl group Chemical group 0.000 claims 22
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 22
- 125000005842 heteroatom Chemical group 0.000 claims 20
- 125000004043 oxo group Chemical group O=* 0.000 claims 19
- 229920006395 saturated elastomer Polymers 0.000 claims 19
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 18
- 201000010099 disease Diseases 0.000 claims 17
- 125000004430 oxygen atom Chemical group O* 0.000 claims 16
- 229910052717 sulfur Inorganic materials 0.000 claims 16
- 125000004434 sulfur atom Chemical group 0.000 claims 16
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 13
- 125000000217 alkyl group Chemical group 0.000 claims 13
- 230000001419 dependent effect Effects 0.000 claims 13
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 13
- 241000124008 Mammalia Species 0.000 claims 12
- 208000035475 disorder Diseases 0.000 claims 11
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 10
- 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 9
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 9
- 229960005309 estradiol Drugs 0.000 claims 9
- 229930182833 estradiol Natural products 0.000 claims 9
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 241000282412 Homo Species 0.000 claims 8
- 125000004432 carbon atom Chemical group C* 0.000 claims 8
- 125000005330 8 membered heterocyclic group Chemical group 0.000 claims 6
- 239000003098 androgen Substances 0.000 claims 6
- 230000003211 malignant effect Effects 0.000 claims 6
- 238000004519 manufacturing process Methods 0.000 claims 6
- 230000002265 prevention Effects 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 5
- 208000024827 Alzheimer disease Diseases 0.000 claims 4
- 206010006187 Breast cancer Diseases 0.000 claims 4
- 208000026310 Breast neoplasm Diseases 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 4
- 230000004064 dysfunction Effects 0.000 claims 4
- 239000000262 estrogen Substances 0.000 claims 4
- 229940011871 estrogen Drugs 0.000 claims 4
- 150000003951 lactams Chemical group 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 210000001519 tissue Anatomy 0.000 claims 4
- 125000001963 4 membered heterocyclic group Chemical group 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- 208000002874 Acne Vulgaris Diseases 0.000 claims 2
- 206010001233 Adenoma benign Diseases 0.000 claims 2
- 201000004384 Alopecia Diseases 0.000 claims 2
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 2
- 208000002177 Cataract Diseases 0.000 claims 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000008448 Congenital adrenal hyperplasia Diseases 0.000 claims 2
- 208000011231 Crohn disease Diseases 0.000 claims 2
- 201000004624 Dermatitis Diseases 0.000 claims 2
- 206010012442 Dermatitis contact Diseases 0.000 claims 2
- 208000005171 Dysmenorrhea Diseases 0.000 claims 2
- 206010013935 Dysmenorrhoea Diseases 0.000 claims 2
- 206010014733 Endometrial cancer Diseases 0.000 claims 2
- 206010014756 Endometrial hypertrophy Diseases 0.000 claims 2
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 2
- 201000009273 Endometriosis Diseases 0.000 claims 2
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 2
- 206010020112 Hirsutism Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000001132 Osteoporosis Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- 206010036590 Premature baby Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 206010039792 Seborrhoea Diseases 0.000 claims 2
- 206010039966 Senile dementia Diseases 0.000 claims 2
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 2
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 2
- 206010067269 Uterine fibrosis Diseases 0.000 claims 2
- 206010046788 Uterine haemorrhage Diseases 0.000 claims 2
- 206010046798 Uterine leiomyoma Diseases 0.000 claims 2
- 206010047115 Vasculitis Diseases 0.000 claims 2
- 206010052428 Wound Diseases 0.000 claims 2
- 208000027418 Wounds and injury Diseases 0.000 claims 2
- 206010000496 acne Diseases 0.000 claims 2
- 239000013543 active substance Substances 0.000 claims 2
- 125000002252 acyl group Chemical group 0.000 claims 2
- 208000002938 adenomyoma Diseases 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 231100000360 alopecia Toxicity 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 208000010668 atopic eczema Diseases 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 125000000440 benzylamino group Chemical group [H]N(*)C([H])([H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 208000010877 cognitive disease Diseases 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 208000010247 contact dermatitis Diseases 0.000 claims 2
- 125000001664 diethylamino group Chemical group [H]C([H])([H])C([H])([H])N(*)C([H])([H])C([H])([H])[H] 0.000 claims 2
- 230000006806 disease prevention Effects 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 208000024908 graft versus host disease Diseases 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 201000010260 leiomyoma Diseases 0.000 claims 2
- 239000002583 male contraceptive agent Substances 0.000 claims 2
- 208000007106 menorrhagia Diseases 0.000 claims 2
- 230000027939 micturition Effects 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 206010028417 myasthenia gravis Diseases 0.000 claims 2
- 210000000056 organ Anatomy 0.000 claims 2
- 201000010065 polycystic ovary syndrome Diseases 0.000 claims 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 210000002307 prostate Anatomy 0.000 claims 2
- 201000007094 prostatitis Diseases 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 208000008742 seborrheic dermatitis Diseases 0.000 claims 2
- 230000001568 sexual effect Effects 0.000 claims 2
- 230000021595 spermatogenesis Effects 0.000 claims 2
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 2
- 125000003375 sulfoxide group Chemical group 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 2
- 206010043778 thyroiditis Diseases 0.000 claims 2
- 238000002054 transplantation Methods 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- 230000002485 urinary effect Effects 0.000 claims 2
- 210000001635 urinary tract Anatomy 0.000 claims 2
- 206010046766 uterine cancer Diseases 0.000 claims 2
- 102100037426 17-beta-hydroxysteroid dehydrogenase type 1 Human genes 0.000 claims 1
- 108010070743 3(or 17)-beta-hydroxysteroid dehydrogenase Proteins 0.000 claims 1
- ZOXJGFHDIHLPTG-UHFFFAOYSA-N Boron Chemical group [B] ZOXJGFHDIHLPTG-UHFFFAOYSA-N 0.000 claims 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 230000000903 blocking effect Effects 0.000 claims 1
- 229910052796 boron Inorganic materials 0.000 claims 1
- 125000005620 boronic acid group Chemical group 0.000 claims 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000004404 heteroalkyl group Chemical group 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 239000002207 metabolite Substances 0.000 claims 1
- 125000002912 morpholin-4-ylsulfonyl group Chemical group O1C([H])([H])C([H])([H])N(S(=O)(=O)[*])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000000160 oxazolidinyl group Chemical group 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 229940127557 pharmaceutical product Drugs 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- OJAWOLWHEQUTDE-UHFFFAOYSA-N Cc1c[n](C)nn1 Chemical compound Cc1c[n](C)nn1 OJAWOLWHEQUTDE-UHFFFAOYSA-N 0.000 description 12
- 0 C[C@@]1(CC2)C(*)(*)CC(C****)[C@@]1[C@@]1[C@]2c2cc(*)c(*)cc2CC1 Chemical compound C[C@@]1(CC2)C(*)(*)CC(C****)[C@@]1[C@@]1[C@]2c2cc(*)c(*)cc2CC1 0.000 description 5
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP06125138.5 | 2006-11-30 | ||
| EP06125138 | 2006-11-30 | ||
| PCT/EP2007/062856 WO2008065100A1 (en) | 2006-11-30 | 2007-11-27 | Substituted estratrien derivatives as 17beta hsd inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010511010A JP2010511010A (ja) | 2010-04-08 |
| JP2010511010A5 true JP2010511010A5 (cg-RX-API-DMAC7.html) | 2010-11-18 |
| JP5264760B2 JP5264760B2 (ja) | 2013-08-14 |
Family
ID=38198108
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009538695A Expired - Fee Related JP5264760B2 (ja) | 2006-11-30 | 2007-11-27 | １７β−ＨＳＤインヒビターとしての置換エストラトリエン誘導体 |
Country Status (8)
| Country | Link |
|---|---|
| EP (1) | EP2099814A1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP5264760B2 (cg-RX-API-DMAC7.html) |
| CN (1) | CN101568547B (cg-RX-API-DMAC7.html) |
| AU (1) | AU2007327653B2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2671075A1 (cg-RX-API-DMAC7.html) |
| MX (1) | MX2009005201A (cg-RX-API-DMAC7.html) |
| RU (1) | RU2453554C2 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2008065100A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11072632B2 (en) | 2011-03-25 | 2021-07-27 | UNIVERSITé LAVAL | Inhibitors of 17β-HSD1, 17β-HSD3 and 17β-HSD10 |
| DE102011083725A1 (de) | 2011-09-29 | 2013-04-04 | Bayer Pharma AG | Estra-1,3,5(10),16-tetraen-3-carboxamid-Derivate, Verfahren zu ihrer Herstellung, pharmazeutische Präparate die diese enthalten, sowie deren Verwendung zur Herstellung von Arzneimitteln |
| WO2013078413A1 (en) * | 2011-11-22 | 2013-05-30 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Modulators of lipid storage |
| PE20150353A1 (es) | 2012-07-10 | 2015-03-28 | Bayer Pharma AG | Derivados de estra-1,3,5(10),16-tetraeno 3-sustituidos, metodos para su preparacion, preparaciones farmaceuticas que los contienen, asi como su uso para la preparacion de medicamentos |
| ES2678993T3 (es) | 2013-02-21 | 2018-08-21 | Bayer Pharma Aktiengesellschaft | Estra-1,3,5(10),16-tetraeno-3-carboxamidas para la inhibición de la 17beta-hidroxiesteroide deshidrogenada (AKR1C3) |
| TW201512215A (zh) * | 2013-06-25 | 2015-04-01 | Forendo Pharma Ltd | 治療活性雌三烯噻唑衍生物 |
| JP6556125B2 (ja) * | 2013-06-25 | 2019-08-07 | フォレンド ファーマ リミテッド | １７β−ヒドロキシステロイドデヒドロゲナーゼの阻害剤としての治療的に活性な１７−窒素置換エストラトリエンチアゾール誘導体 |
| JP6456373B2 (ja) * | 2013-06-25 | 2019-01-23 | フォレンド ファーマ リミテッド | １７β−ヒドロキシステロイドデヒドロゲナーゼ タイプ１の阻害剤として治療活性のあるエストラトリエンチアゾール誘導体 |
| US10112962B2 (en) * | 2014-07-02 | 2018-10-30 | Xavier University | Boron-based prodrug strategy for increased bioavailability and lower-dosage requirements for drug molecules containing at least one phenol (or aromatic hydroxyl) group |
| CN107207561B (zh) * | 2014-12-23 | 2020-03-31 | 佛恩多制药有限公司 | 17β-HSD1–抑制剂的前药 |
| JP6545266B2 (ja) | 2014-12-23 | 2019-07-17 | フォレンド ファーマ リミテッド | １７β‐ＨＳＤ１抑制剤のプロドラッグ |
| CZ307437B6 (cs) | 2016-06-07 | 2018-08-22 | Ăšstav organickĂ© chemie a biochemie AV ÄŚR, v.v.i. | 15β-substituované deriváty estronu jako selektivní inhibitory 17β-hydroxysteoiddehydrogenáz |
| HRP20240679T1 (hr) | 2017-06-08 | 2024-08-16 | Organon R&D Finland Ltd | 17-oksimi 15.beta.-[3-propanamido]-supstituiranih etera-1,3,5(10)-trien-17-ona za uporabu u inhibiciji 17.beta.-hidroksisteroid dehidrogenaza |
| JP7417608B2 (ja) | 2018-12-05 | 2024-01-18 | フォレンド ファーマ リミテッド | １７－ｈｓｄ１阻害剤としての１６（１７）位でピラゾール環と縮合しているエストラ－１，３，５（１０）－トリエン化合物 |
| IT201900004041A1 (it) * | 2019-03-20 | 2020-09-20 | Farmabios Spa | Procedimento per la preparazione di un derivato del fulvestrant |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5571933A (en) * | 1994-11-17 | 1996-11-05 | Duquesne University Of The Holy Ghost | Derivatives of estra 1,3,5(10)triene-17-one, 3-amino compounds and their use |
| HUP0101809A3 (en) * | 1998-03-11 | 2002-07-29 | Endorech Inc Sainte Foy | Inhibitors of type 5 and type 3 17betha-hydroxysteroid dehydrogenase and methods for their use |
| GB0025788D0 (en) * | 2000-10-20 | 2000-12-06 | Sterix Ltd | Use |
| TWI331154B (en) * | 2003-11-12 | 2010-10-01 | Solvay Pharm Gmbh | Novel 17-hydroxysteroid dehydrogenase type i inhibitors |
| US8030298B2 (en) * | 2005-05-26 | 2011-10-04 | Abbott Products Gmbh | 17β-HSD1 and STS inhibitors |
| CN101189251B (zh) * | 2005-05-26 | 2012-09-12 | 索尔瓦药物有限公司 | 17β-HSD1和STS抑制剂 |
-
2007
- 2007-11-27 AU AU2007327653A patent/AU2007327653B2/en not_active Ceased
- 2007-11-27 CA CA002671075A patent/CA2671075A1/en not_active Abandoned
- 2007-11-27 RU RU2009124589/04A patent/RU2453554C2/ru not_active IP Right Cessation
- 2007-11-27 EP EP07847383A patent/EP2099814A1/en not_active Withdrawn
- 2007-11-27 MX MX2009005201A patent/MX2009005201A/es active IP Right Grant
- 2007-11-27 CN CN200780048224.8A patent/CN101568547B/zh not_active Expired - Fee Related
- 2007-11-27 WO PCT/EP2007/062856 patent/WO2008065100A1/en not_active Ceased
- 2007-11-27 JP JP2009538695A patent/JP5264760B2/ja not_active Expired - Fee Related
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