JP2006513169A5 - - Google Patents
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- JP2006513169A5 JP2006513169A5 JP2004553612A JP2004553612A JP2006513169A5 JP 2006513169 A5 JP2006513169 A5 JP 2006513169A5 JP 2004553612 A JP2004553612 A JP 2004553612A JP 2004553612 A JP2004553612 A JP 2004553612A JP 2006513169 A5 JP2006513169 A5 JP 2006513169A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- pharmaceutical composition
- aryl
- alkyl
- group
- 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 37
- 239000008194 pharmaceutical composition Substances 0.000 claims 27
- 125000003118 aryl group Chemical group 0.000 claims 15
- 125000000217 alkyl group Chemical group 0.000 claims 13
- 125000001072 heteroaryl group Chemical group 0.000 claims 11
- 125000003710 aryl alkyl group Chemical group 0.000 claims 9
- 239000003112 inhibitor Substances 0.000 claims 9
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 8
- 238000011282 treatment Methods 0.000 claims 8
- 230000002265 prevention Effects 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 239000012453 solvate Substances 0.000 claims 7
- 239000003795 chemical substances by application Substances 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 5
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 238000010276 construction Methods 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- -1 methylenedioxy Chemical group 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 108010070743 3(or 17)-beta-hydroxysteroid dehydrogenase Proteins 0.000 claims 3
- 201000004384 Alopecia Diseases 0.000 claims 3
- 108010066551 Cholestenone 5 alpha-Reductase Proteins 0.000 claims 3
- 102100034067 Dehydrogenase/reductase SDR family member 11 Human genes 0.000 claims 3
- 229940122117 Potassium channel agonist Drugs 0.000 claims 3
- 239000003098 androgen Substances 0.000 claims 3
- 230000001419 dependent effect Effects 0.000 claims 3
- LKJPYSCBVHEWIU-KRWDZBQOSA-N (R)-bicalutamide Chemical compound C([C@@](O)(C)C(=O)NC=1C=C(C(C#N)=CC=1)C(F)(F)F)S(=O)(=O)C1=CC=C(F)C=C1 LKJPYSCBVHEWIU-KRWDZBQOSA-N 0.000 claims 2
- 101000904173 Homo sapiens Progonadoliberin-1 Proteins 0.000 claims 2
- 108010044467 Isoenzymes Proteins 0.000 claims 2
- 229940124041 Luteinizing hormone releasing hormone (LHRH) antagonist Drugs 0.000 claims 2
- 102000004317 Lyases Human genes 0.000 claims 2
- 108090000856 Lyases Proteins 0.000 claims 2
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 102100024028 Progonadoliberin-1 Human genes 0.000 claims 2
- 229940123934 Reductase inhibitor Drugs 0.000 claims 2
- 102000001854 Steroid 17-alpha-Hydroxylase Human genes 0.000 claims 2
- 108010015330 Steroid 17-alpha-Hydroxylase Proteins 0.000 claims 2
- 101000996723 Sus scrofa Gonadotropin-releasing hormone receptor Proteins 0.000 claims 2
- DRHKJLXJIQTDTD-OAHLLOKOSA-N Tamsulosine Chemical compound CCOC1=CC=CC=C1OCCN[C@H](C)CC1=CC=C(OC)C(S(N)(=O)=O)=C1 DRHKJLXJIQTDTD-OAHLLOKOSA-N 0.000 claims 2
- 239000000556 agonist Substances 0.000 claims 2
- 239000000051 antiandrogen Substances 0.000 claims 2
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 229960000997 bicalutamide Drugs 0.000 claims 2
- 239000003124 biologic agent Substances 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 229940127089 cytotoxic agent Drugs 0.000 claims 2
- 229960002074 flutamide Drugs 0.000 claims 2
- MKXKFYHWDHIYRV-UHFFFAOYSA-N flutamide Chemical compound CC(C)C(=O)NC1=CC=C([N+]([O-])=O)C(C(F)(F)F)=C1 MKXKFYHWDHIYRV-UHFFFAOYSA-N 0.000 claims 2
- XLXSAKCOAKORKW-UHFFFAOYSA-N gonadorelin Chemical compound C1CCC(C(=O)NCC(N)=O)N1C(=O)C(CCCN=C(N)N)NC(=O)C(CC(C)C)NC(=O)CNC(=O)C(NC(=O)C(CO)NC(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C(CC=1NC=NC=1)NC(=O)C1NC(=O)CC1)CC1=CC=C(O)C=C1 XLXSAKCOAKORKW-UHFFFAOYSA-N 0.000 claims 2
- 239000002474 gonadorelin antagonist Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 229960002613 tamsulosin Drugs 0.000 claims 2
- VCKUSRYTPJJLNI-UHFFFAOYSA-N terazosin Chemical compound N=1C(N)=C2C=C(OC)C(OC)=CC2=NC=1N(CC1)CCN1C(=O)C1CCCO1 VCKUSRYTPJJLNI-UHFFFAOYSA-N 0.000 claims 2
- 229960001693 terazosin Drugs 0.000 claims 2
- 229940113178 5 Alpha reductase inhibitor Drugs 0.000 claims 1
- 239000002677 5-alpha reductase inhibitor Substances 0.000 claims 1
- 208000002874 Acne Vulgaris Diseases 0.000 claims 1
- 102000004602 Aldo-Keto Reductase Family 1 Member C3 Human genes 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 101100516563 Caenorhabditis elegans nhr-6 gene Proteins 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 101710088194 Dehydrogenase Proteins 0.000 claims 1
- 206010020112 Hirsutism Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- ZFMITUMMTDLWHR-UHFFFAOYSA-N Minoxidil Chemical group NC1=[N+]([O-])C(N)=CC(N2CCCCC2)=N1 ZFMITUMMTDLWHR-UHFFFAOYSA-N 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 108010065942 Prostaglandin-F synthase Proteins 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 206010000496 acne Diseases 0.000 claims 1
- 239000000951 adrenergic alpha-1 receptor antagonist Substances 0.000 claims 1
- 206010068168 androgenetic alopecia Diseases 0.000 claims 1
- 201000002996 androgenic alopecia Diseases 0.000 claims 1
- 230000003656 anti-hair-loss Effects 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229960004199 dutasteride Drugs 0.000 claims 1
- JWJOTENAMICLJG-QWBYCMEYSA-N dutasteride Chemical compound O=C([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)N[C@@H]4CC3)C)CC[C@@]21C)NC1=CC(C(F)(F)F)=CC=C1C(F)(F)F JWJOTENAMICLJG-QWBYCMEYSA-N 0.000 claims 1
- 229960004039 finasteride Drugs 0.000 claims 1
- DBEPLOCGEIEOCV-WSBQPABSSA-N finasteride Chemical compound N([C@@H]1CC2)C(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)NC(C)(C)C)[C@@]2(C)CC1 DBEPLOCGEIEOCV-WSBQPABSSA-N 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 229960003632 minoxidil Drugs 0.000 claims 1
- 208000025113 myeloid leukemia Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 201000010065 polycystic ovary syndrome Diseases 0.000 claims 1
- 230000003658 preventing hair loss Effects 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 208000021046 prostate intraepithelial neoplasia Diseases 0.000 claims 1
- 230000005855 radiation Effects 0.000 claims 1
- 238000001959 radiotherapy Methods 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 238000001356 surgical procedure Methods 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- SXTNLGBTJOWZIW-IDCGIGBZSA-N CC(C)(C)[C@@H](CN(CC1)C(c2ccccc2)c2ccc(C(C)(C)C)cc2)N1C(NC(CC1)CCN1C(C)=O)=O Chemical compound CC(C)(C)[C@@H](CN(CC1)C(c2ccccc2)c2ccc(C(C)(C)C)cc2)N1C(NC(CC1)CCN1C(C)=O)=O SXTNLGBTJOWZIW-IDCGIGBZSA-N 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US42726302P | 2002-11-18 | 2002-11-18 | |
| PCT/US2003/036203 WO2004046111A1 (en) | 2002-11-18 | 2003-11-14 | 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010058356A Division JP2010138204A (ja) | 2002-11-18 | 2010-03-15 | アンドロゲン依存性疾患を処置するための１７β−ヒドロキシステロイドデヒドロゲナーゼタイプ３インヒビター |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2006513169A JP2006513169A (ja) | 2006-04-20 |
| JP2006513169A5 true JP2006513169A5 (https=) | 2006-10-05 |
| JP4614770B2 JP4614770B2 (ja) | 2011-01-19 |
Family
ID=32326512
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004553612A Expired - Fee Related JP4614770B2 (ja) | 2002-11-18 | 2003-11-14 | アンドロゲン依存性疾患を処置するための１７β−ヒドロキシステロイドデヒドロゲナーゼタイプ３インヒビター |
| JP2010058356A Withdrawn JP2010138204A (ja) | 2002-11-18 | 2010-03-15 | アンドロゲン依存性疾患を処置するための１７β−ヒドロキシステロイドデヒドロゲナーゼタイプ３インヒビター |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010058356A Withdrawn JP2010138204A (ja) | 2002-11-18 | 2010-03-15 | アンドロゲン依存性疾患を処置するための１７β−ヒドロキシステロイドデヒドロゲナーゼタイプ３インヒビター |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US7074795B2 (https=) |
| EP (1) | EP1562901B1 (https=) |
| JP (2) | JP4614770B2 (https=) |
| CN (1) | CN100374421C (https=) |
| AR (1) | AR042046A1 (https=) |
| AT (1) | ATE469886T1 (https=) |
| AU (1) | AU2003290799A1 (https=) |
| CA (1) | CA2506290C (https=) |
| CL (1) | CL2003002356A1 (https=) |
| DE (1) | DE60332862D1 (https=) |
| ES (1) | ES2345146T3 (https=) |
| MX (1) | MXPA05005360A (https=) |
| MY (1) | MY130792A (https=) |
| PE (1) | PE20040750A1 (https=) |
| TW (1) | TW200412964A (https=) |
| WO (1) | WO2004046111A1 (https=) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE60323765D1 (de) | 2002-12-17 | 2008-11-06 | Schering Corp | Inhibitoren der 17 beta-hydroxysteroiddehydrogenase des typs 3 zur behandlung androgenabhängiger krankheiten |
| GB0513702D0 (en) | 2005-07-04 | 2005-08-10 | Sterix Ltd | Compound |
| US7851474B2 (en) * | 2005-08-02 | 2010-12-14 | Neurogen Corporation | Dipiperazinyl ketones and related analogues |
| US8080540B2 (en) | 2006-09-19 | 2011-12-20 | Abbott Products Gmbh | Therapeutically active triazoles and their use |
| US8288367B2 (en) | 2006-11-30 | 2012-10-16 | Solvay Pharmaceuticals Gmbh | Substituted estratriene derivatives as 17BETA HSD inhibitors |
| US8501940B2 (en) * | 2008-07-15 | 2013-08-06 | Hoffmann-La Roche Inc. | Tetrahydrocinnoline derivatives |
| CN106890100A (zh) * | 2011-04-25 | 2017-06-27 | 朴俊炯 | 用于预防脱发和促进毛发生长的局部施用的组合物 |
| 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 |
| 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 |
| 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 |
| JP6532599B2 (ja) | 2015-09-02 | 2019-06-19 | グラクソスミスクライン、インテレクチュアル、プロパティー、（ナンバー２）、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ （Ｎｏ．２） Ｌｉｍｉｔｅｄ | ブロモドメイン阻害薬としての使用のためのピリジノンジカルボキサミド |
| 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 |
| AU2018386327B2 (en) * | 2017-12-15 | 2023-04-13 | Inthera Bioscience AG | 1 -(piperidinocarbonylmethyl)-2-oxopiperazine derivatives for treating cancer |
| 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 |
| EP4168014A1 (en) | 2020-06-19 | 2023-04-26 | Inthera Bioscience AG | Oxopiperazine derivatives for the treatment of cancer |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IE58836B1 (en) | 1984-08-02 | 1993-11-17 | Labrie Fernand | Pharmaceutical composition for combination therapy of hormone dependent cancers |
| ZA901847B (en) | 1989-03-10 | 1991-10-30 | Endorecherche Inc | Combination therapy for the treatment of estrogen sensitive diseases |
| ATE230994T1 (de) | 1989-07-07 | 2003-02-15 | Endorech Inc | Methode zur behandlung androgenbedingter krankheiten |
| DE69034148T2 (de) | 1989-07-07 | 2005-06-30 | Endorecherche Inc., Ste-Foy | Kombinationstherapie zur Prophylaxe und/oder Behandlung von gutartiger prostatischer Hyperplasie |
| US6060503A (en) | 1991-12-02 | 2000-05-09 | Endorecherche, Inc. | Benzopyran-containing compounds and method for their use |
| ATE197458T1 (de) | 1993-05-17 | 2000-11-11 | Endorech Inc | Verbesserte antiandrogene |
| US6124115A (en) | 1995-09-22 | 2000-09-26 | Endorecherche Inc. | Production and use of isolated type 5 17β-hydroxysteroid dehydrogenase |
| AU4801197A (en) * | 1996-09-13 | 1998-04-02 | Schering Corporation | Tricyclic antitumor compounds being farnesyl protein transferase inhibit ors |
| 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 |
| PE20030703A1 (es) | 2001-09-06 | 2003-08-21 | Schering Corp | Inhibidores de la 17b-hidroxiesteroide deshidrogenasa tipo 3 |
| EP1436281B1 (en) * | 2001-10-17 | 2010-06-16 | Schering Corporation | Piperidine- and piperazineacetamides as 17beta hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases |
-
2003
- 2003-11-14 WO PCT/US2003/036203 patent/WO2004046111A1/en not_active Ceased
- 2003-11-14 DE DE60332862T patent/DE60332862D1/de not_active Expired - Lifetime
- 2003-11-14 TW TW092131992A patent/TW200412964A/zh unknown
- 2003-11-14 AT AT03783382T patent/ATE469886T1/de not_active IP Right Cessation
- 2003-11-14 CN CNB2003801086673A patent/CN100374421C/zh not_active Expired - Fee Related
- 2003-11-14 JP JP2004553612A patent/JP4614770B2/ja not_active Expired - Fee Related
- 2003-11-14 AR ARP030104210A patent/AR042046A1/es unknown
- 2003-11-14 AU AU2003290799A patent/AU2003290799A1/en not_active Abandoned
- 2003-11-14 US US10/713,828 patent/US7074795B2/en not_active Expired - Fee Related
- 2003-11-14 CA CA2506290A patent/CA2506290C/en not_active Expired - Fee Related
- 2003-11-14 MX MXPA05005360A patent/MXPA05005360A/es active IP Right Grant
- 2003-11-14 PE PE2003001156A patent/PE20040750A1/es not_active Application Discontinuation
- 2003-11-14 CL CL200302356A patent/CL2003002356A1/es unknown
- 2003-11-14 MY MYPI20034363A patent/MY130792A/en unknown
- 2003-11-14 ES ES03783382T patent/ES2345146T3/es not_active Expired - Lifetime
- 2003-11-14 EP EP03783382A patent/EP1562901B1/en not_active Expired - Lifetime
-
2006
- 2006-02-24 US US11/362,217 patent/US7476681B2/en not_active Expired - Fee Related
-
2010
- 2010-03-15 JP JP2010058356A patent/JP2010138204A/ja not_active Withdrawn
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