JP2006513169A5 - - Google Patents
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- Publication number
- 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 (enExample) | 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 (enExample) |
| EP (1) | EP1562901B1 (enExample) |
| JP (2) | JP4614770B2 (enExample) |
| CN (1) | CN100374421C (enExample) |
| AR (1) | AR042046A1 (enExample) |
| AT (1) | ATE469886T1 (enExample) |
| AU (1) | AU2003290799A1 (enExample) |
| CA (1) | CA2506290C (enExample) |
| CL (1) | CL2003002356A1 (enExample) |
| DE (1) | DE60332862D1 (enExample) |
| ES (1) | ES2345146T3 (enExample) |
| MX (1) | MXPA05005360A (enExample) |
| MY (1) | MY130792A (enExample) |
| PE (1) | PE20040750A1 (enExample) |
| TW (1) | TW200412964A (enExample) |
| WO (1) | WO2004046111A1 (enExample) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2003293555A1 (en) | 2002-12-17 | 2004-07-29 | Schering Corporation | 17 beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases |
| GB0513702D0 (en) | 2005-07-04 | 2005-08-10 | Sterix Ltd | Compound |
| WO2007016496A2 (en) * | 2005-08-02 | 2007-02-08 | 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 |
| AU2014300894A1 (en) | 2013-06-25 | 2016-01-28 | Forendo Pharma Ltd | Therapeutically active 17-nitrogen substituted estratrienthiazole derivatives as inhibitors of 17.beta.-hydroxysteroid dehydrogenase |
| TW201512215A (zh) | 2013-06-25 | 2015-04-01 | Forendo Pharma Ltd | 治療活性雌三烯噻唑衍生物 |
| 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 |
| WO2016102775A1 (en) | 2014-12-23 | 2016-06-30 | Forendo Pharma Ltd | PRODRUGS OF 17β-HSD1 -INHIBITORS |
| US10413557B2 (en) | 2014-12-23 | 2019-09-17 | Forendo Pharma Ltd. | Prodrugs of 17.BETA.-HSD1-inhibitors |
| MA43940A (fr) | 2015-09-02 | 2018-12-12 | Glaxosmithkline Ip No 2 Ltd | Dicarboxamide de pyridinone utilisé comme inhibiteur de bromodomaine |
| SG11201911776PA (en) | 2017-06-08 | 2020-01-30 | Forendo Pharma Ltd | 15.beta.-[3-propanamido]-substituted estra-1,3,5(10)-trien-17-one compounds and their 17-oximes for use in inhibition of 17.beta.-hydroxysteroid dehydrogenases |
| EP3724178B1 (en) | 2017-12-15 | 2024-05-01 | Inthera Bioscience AG | 1-(piperidinocarbonylmethyl)-2-oxopiperazine derivatives for treating cancer |
| CA3122049C (en) | 2018-12-05 | 2023-10-17 | Forendo Pharma Ltd | Estra-1,3,5(10)-triene compounds condensed in position 16(17) with a pyrazole ring as inhibitors of 17-hsd1 |
| US12611406B2 (en) | 2020-06-19 | 2026-04-28 | Inthera Bioscience AG | Oxopiperazine derivatives for the treatment of cancer |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3590389T1 (de) | 1984-08-02 | 1986-08-28 | Schering Corp., Kenilworth, N.J. | Pharmazeutische Zusammensetzung für eine Kombinationstherapie hormon-abhängiger Cancer |
| PH30747A (en) | 1989-03-10 | 1997-10-17 | Endorech Inc | Combination therapy for the treatment of estrogen sensitive disease. |
| DK0595796T3 (da) | 1989-07-07 | 2003-05-05 | Endorech Inc | Fremgangsmåde til behandling af androgen-relaterede sygdomme |
| CA2062973C (en) | 1989-07-07 | 2003-09-23 | Fernand Labrie | Combination therapy for prophylaxsis and/or treatment of benign prostatic hyperplasia |
| US6060503A (en) | 1991-12-02 | 2000-05-09 | Endorecherche, Inc. | Benzopyran-containing compounds and method for their use |
| CZ285893B6 (cs) | 1993-05-17 | 1999-11-17 | Endorecherche Inc. | Antiandrogenní sloučenina, její prekursor a farmaceutický prostředek ji obsahující |
| US6124115A (en) | 1995-09-22 | 2000-09-26 | Endorecherche Inc. | Production and use of isolated type 5 17β-hydroxysteroid dehydrogenase |
| ES2229340T3 (es) * | 1996-09-13 | 2005-04-16 | Schering Corporation | Compuestos triciclicos antitumorales, inhibidores de farnesil-proteina-tranferasa. |
| MXPA00008868A (es) * | 1998-03-11 | 2003-04-25 | Endorech Inc | Inhibidores de dihidrogenasa de 17 -hidroxiesteroide y metodos para su uso. |
| MY141661A (en) * | 2001-09-06 | 2010-05-31 | Schering Corp | 17b-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases |
| ES2347643T3 (es) * | 2001-10-17 | 2010-11-03 | Schering Corporation | Piperin- y piperazinacetamidas como inhibidores de 17beta hidroxiesteroide deshidrogenasa tipo 3 para el tratamiento de enfermedades dependientes de androgenos. |
-
2003
- 2003-11-14 ES ES03783382T patent/ES2345146T3/es not_active Expired - Lifetime
- 2003-11-14 PE PE2003001156A patent/PE20040750A1/es not_active Application Discontinuation
- 2003-11-14 DE DE60332862T patent/DE60332862D1/de not_active Expired - Lifetime
- 2003-11-14 JP JP2004553612A patent/JP4614770B2/ja not_active Expired - Fee Related
- 2003-11-14 CL CL200302356A patent/CL2003002356A1/es unknown
- 2003-11-14 EP EP03783382A patent/EP1562901B1/en not_active Expired - Lifetime
- 2003-11-14 CA CA2506290A patent/CA2506290C/en not_active Expired - Fee Related
- 2003-11-14 CN CNB2003801086673A patent/CN100374421C/zh not_active Expired - Fee Related
- 2003-11-14 AT AT03783382T patent/ATE469886T1/de not_active IP Right Cessation
- 2003-11-14 AR ARP030104210A patent/AR042046A1/es unknown
- 2003-11-14 WO PCT/US2003/036203 patent/WO2004046111A1/en not_active Ceased
- 2003-11-14 AU AU2003290799A patent/AU2003290799A1/en not_active Abandoned
- 2003-11-14 TW TW092131992A patent/TW200412964A/zh unknown
- 2003-11-14 US US10/713,828 patent/US7074795B2/en not_active Expired - Fee Related
- 2003-11-14 MY MYPI20034363A patent/MY130792A/en unknown
- 2003-11-14 MX MXPA05005360A patent/MXPA05005360A/es active IP Right Grant
-
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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