JP2006527227A5 - - Google Patents
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- Publication number
- JP2006527227A5 JP2006527227A5 JP2006515870A JP2006515870A JP2006527227A5 JP 2006527227 A5 JP2006527227 A5 JP 2006527227A5 JP 2006515870 A JP2006515870 A JP 2006515870A JP 2006515870 A JP2006515870 A JP 2006515870A JP 2006527227 A5 JP2006527227 A5 JP 2006527227A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- oxo
- substituted
- benzothieno
- 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
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- 150000001875 compounds Chemical class 0.000 claims 23
- 125000003118 aryl group Chemical group 0.000 claims 19
- 125000000217 alkyl group Chemical group 0.000 claims 18
- 229910052739 hydrogen Inorganic materials 0.000 claims 16
- 239000001257 hydrogen Substances 0.000 claims 16
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 14
- 125000004043 oxo group Chemical group O=* 0.000 claims 13
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 12
- 150000002431 hydrogen Chemical class 0.000 claims 11
- 229920006395 saturated elastomer Polymers 0.000 claims 11
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 150000002367 halogens Chemical group 0.000 claims 10
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 10
- 125000004414 alkyl thio group Chemical group 0.000 claims 9
- 125000005110 aryl thio group Chemical group 0.000 claims 9
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 9
- 125000004122 cyclic group Chemical group 0.000 claims 9
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 125000002252 acyl group Chemical group 0.000 claims 8
- 125000004423 acyloxy group Chemical group 0.000 claims 8
- -1 aldehyde compound Chemical class 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 8
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 8
- 150000001408 amides Chemical class 0.000 claims 8
- 125000003710 aryl alkyl group Chemical group 0.000 claims 8
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 8
- 125000004104 aryloxy group Chemical group 0.000 claims 8
- 150000002923 oximes Chemical group 0.000 claims 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 8
- 125000000547 substituted alkyl group Chemical group 0.000 claims 8
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical group C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 7
- 201000010099 disease Diseases 0.000 claims 7
- 208000035475 disorder Diseases 0.000 claims 7
- 125000002947 alkylene group Chemical group 0.000 claims 6
- 230000001419 dependent effect Effects 0.000 claims 6
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 6
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 125000003356 phenylsulfanyl group Chemical group [*]SC1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 6
- 239000003270 steroid hormone Substances 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 6
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 5
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 230000005764 inhibitory process Effects 0.000 claims 4
- 201000004384 Alopecia Diseases 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000004429 atom Chemical group 0.000 claims 3
- 125000001309 chloro group Chemical group Cl* 0.000 claims 3
- 125000006413 ring segment Chemical group 0.000 claims 3
- 125000003396 thiol group Chemical class [H]S* 0.000 claims 3
- 108010070743 3(or 17)-beta-hydroxysteroid dehydrogenase Proteins 0.000 claims 2
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 2
- 208000002874 Acne Vulgaris Diseases 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 208000002177 Cataract Diseases 0.000 claims 2
- 206010009944 Colon cancer 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
- 208000001132 Osteoporosis Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 2
- 206010039792 Seborrhoea Diseases 0.000 claims 2
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 2
- 206010046788 Uterine haemorrhage Diseases 0.000 claims 2
- 206010046798 Uterine leiomyoma Diseases 0.000 claims 2
- 206010000496 acne Diseases 0.000 claims 2
- 239000013543 active substance Substances 0.000 claims 2
- 125000005157 alkyl carboxy group Chemical group 0.000 claims 2
- 231100000360 alopecia Toxicity 0.000 claims 2
- 239000003098 androgen Substances 0.000 claims 2
- 125000001246 bromo group Chemical group Br* 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 125000000950 dibromo group Chemical group Br* 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 230000004064 dysfunction Effects 0.000 claims 2
- 201000009274 endometriosis of uterus Diseases 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 239000003112 inhibitor Substances 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
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 125000004817 pentamethylene group Chemical group [H]C([H])([*:2])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[*:1] 0.000 claims 2
- 201000010065 polycystic ovary syndrome Diseases 0.000 claims 2
- 230000035935 pregnancy Effects 0.000 claims 2
- 230000002028 premature Effects 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 201000001514 prostate carcinoma Diseases 0.000 claims 2
- 201000007094 prostatitis Diseases 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 208000008742 seborrheic dermatitis Diseases 0.000 claims 2
- 230000021595 spermatogenesis Effects 0.000 claims 2
- 125000000383 tetramethylene group Chemical group [H]C([H])([*:1])C([H])([H])C([H])([H])C([H])([H])[*:2] 0.000 claims 2
- 230000000451 tissue damage Effects 0.000 claims 2
- 231100000827 tissue damage Toxicity 0.000 claims 2
- 230000002485 urinary effect Effects 0.000 claims 2
- 206010046766 uterine cancer Diseases 0.000 claims 2
- 201000007954 uterine fibroid Diseases 0.000 claims 2
- 230000037303 wrinkles Effects 0.000 claims 2
- LWBYNHFNVQXTIB-UHFFFAOYSA-N 1,2,3,4,5,8,9,10,11,12-decahydro-14h-cyclohepta[4',5']thieno[2',3':4,5]pyrimido[1,2-a]azepin-14-one Chemical compound C1CCCCC2=C1SC1=C2C(=O)N(CCCCC2)C2=N1 LWBYNHFNVQXTIB-UHFFFAOYSA-N 0.000 claims 1
- TXDYRLZWUVLHQS-UHFFFAOYSA-N 1,2,3,4,6,7,8,9-octahydro-11-thia-5a,10-diaza-benzo[b]fluoren-5-one Chemical compound C1CCCC2=C1SC1=C2C(=O)N(CCCC2)C2=N1 TXDYRLZWUVLHQS-UHFFFAOYSA-N 0.000 claims 1
- NPTZOAKVKKFTTK-UHFFFAOYSA-N 1,2,7,8,9,10,11,13-octahydro-13-oxo-4-(propylthio)[1]benzothieno[2',3':4,5]-pyrimido-[1,2-a]azepine-3-carboxaldehyde Chemical compound N1=C2CCCCCN2C(=O)C2=C1SC1=C2CCC(C=O)=C1SCCC NPTZOAKVKKFTTK-UHFFFAOYSA-N 0.000 claims 1
- UMOBBPSBMBBSTF-UHFFFAOYSA-N 11-oxo-19-thia-2,10-diazatetracyclo[10.7.0.03,10.013,18]nonadeca-1(12),2,4,6,8,13,15,17-octaene-17-carbaldehyde Chemical compound C1=CC=C(C2=C1C1=C(N=C3N(C=CC=CC=C3)C1=O)S2)C=O UMOBBPSBMBBSTF-UHFFFAOYSA-N 0.000 claims 1
- RVKNUVLCOGEBNM-UHFFFAOYSA-N 16-chloro-18-thia-2,9-diazatetracyclo[9.7.0.03,9.012,17]octadeca-1(11),2,12(17),15-tetraen-10-one Chemical compound N1=C2CCCCCN2C(=O)C2=C1SC1=C2CCC=C1Cl RVKNUVLCOGEBNM-UHFFFAOYSA-N 0.000 claims 1
- JHZCPVXSEOVUEZ-UHFFFAOYSA-N 1h-azepine-3-carbaldehyde Chemical compound O=CC1=CNC=CC=C1 JHZCPVXSEOVUEZ-UHFFFAOYSA-N 0.000 claims 1
- FCICWTXGPVBTKU-UHFFFAOYSA-N 2,3,8,9,10,11-hexahydro[1]benzothieno[2',3':4,5]pyrimido[1,2-a]azepine-4,13(1h,7h)-dione Chemical compound N1=C2CCCCCN2C(=O)C2=C1SC1=C2CCCC1=O FCICWTXGPVBTKU-UHFFFAOYSA-N 0.000 claims 1
- NOPFKZSNTRHNQU-UHFFFAOYSA-N 2,3-dimethyl-6,7-dihydro-5h-[1]benzothiolo[2,3-d]pyrimidine-4,8-dione Chemical compound C1=2C(=O)N(C)C(C)=NC=2SC2=C1CCCC2=O NOPFKZSNTRHNQU-UHFFFAOYSA-N 0.000 claims 1
- HQIKQPXFQXSKBA-UHFFFAOYSA-N 2-(dimethylamino)-13-methylidene-18-thia-2,9-diazatetracyclo[9.7.0.03,9.012,17]octadeca-1(11),12(17)-diene-10,16-dione Chemical compound CN(N1C2=C(C(N3C1CCCCC3)=O)C3=C(S2)C(CCC3=C)=O)C HQIKQPXFQXSKBA-UHFFFAOYSA-N 0.000 claims 1
- MSUMKBCBFVSDAS-UHFFFAOYSA-N 3-ethyl-2-methyl-6,7-dihydro-5h-[1]benzothiolo[2,3-d]pyrimidine-4,8-dione Chemical compound C1=2C(=O)N(CC)C(C)=NC=2SC2=C1CCCC2=O MSUMKBCBFVSDAS-UHFFFAOYSA-N 0.000 claims 1
- SHTIGZOXDJWUQG-UHFFFAOYSA-N 3-methyl-6,7-dihydro-5h-[1]benzothiolo[2,3-d]pyrimidine-4,8-dione Chemical compound C1=2C(=O)N(C)C=NC=2SC2=C1CCCC2=O SHTIGZOXDJWUQG-UHFFFAOYSA-N 0.000 claims 1
- NFQJVHLIKXXJST-UHFFFAOYSA-N 8-chloro-3-methyl-4-oxo-5,6-dihydro-[1]benzothiolo[2,3-d]pyrimidine-7-carbaldehyde Chemical compound C1=2C(=O)N(C)C=NC=2SC2=C1CCC(C=O)=C2Cl NFQJVHLIKXXJST-UHFFFAOYSA-N 0.000 claims 1
- 125000004399 C1-C4 alkenyl group Chemical group 0.000 claims 1
- 102100034067 Dehydrogenase/reductase SDR family member 11 Human genes 0.000 claims 1
- 108090000790 Enzymes Proteins 0.000 claims 1
- 102000004190 Enzymes Human genes 0.000 claims 1
- 206010020112 Hirsutism Diseases 0.000 claims 1
- 206010048469 Kidney enlargement Diseases 0.000 claims 1
- KKAAQMYLNZYOGX-UHFFFAOYSA-N N1=C2CCCCCN2C(=O)C2=C1SC1=C2CCC1=O Chemical compound N1=C2CCCCCN2C(=O)C2=C1SC1=C2CCC1=O KKAAQMYLNZYOGX-UHFFFAOYSA-N 0.000 claims 1
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 1
- 206010038468 Renal hypertrophy Diseases 0.000 claims 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 1
- 238000005874 Vilsmeier-Haack formylation reaction Methods 0.000 claims 1
- DHKHKXVYLBGOIT-UHFFFAOYSA-N acetaldehyde Diethyl Acetal Natural products CCOC(C)OCC DHKHKXVYLBGOIT-UHFFFAOYSA-N 0.000 claims 1
- 239000012190 activator Substances 0.000 claims 1
- 206010068168 androgenetic alopecia Diseases 0.000 claims 1
- 201000002996 androgenic alopecia Diseases 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- CSXQFDHPOSTQPU-UHFFFAOYSA-N chembl570358 Chemical compound C1=2SC=3N=C4CCCCCN4C(=O)C=3C=2CCC(C=O)=C1SC1CCCC1 CSXQFDHPOSTQPU-UHFFFAOYSA-N 0.000 claims 1
- QGQHJWACZLQAMG-UHFFFAOYSA-N chembl570584 Chemical compound N1=C2CCCCCN2C(=O)C2=C1SC1=C2CCC(C=O)=C1SC(C)(C)C QGQHJWACZLQAMG-UHFFFAOYSA-N 0.000 claims 1
- PUDXJSZZKSDMHW-UHFFFAOYSA-N chembl570585 Chemical compound N1=C2CCCCCN2C(=O)C2=C1SC1=C2CCC(C=O)=C1SC(C)C PUDXJSZZKSDMHW-UHFFFAOYSA-N 0.000 claims 1
- DEPWCDOKLZHUMP-UHFFFAOYSA-N chembl571260 Chemical compound N1=C2CCCCCN2C(=O)C2=C1SC1=C2CCC(C=O)=C1SCCCC DEPWCDOKLZHUMP-UHFFFAOYSA-N 0.000 claims 1
- IKVOPWVOZWRAOT-UHFFFAOYSA-N chembl576266 Chemical compound N1=C2CCCCCN2C(=O)C2=C1SC1=C2CCC(C=O)=C1SCC IKVOPWVOZWRAOT-UHFFFAOYSA-N 0.000 claims 1
- NWAPSCLFPKXCMK-UHFFFAOYSA-N chembl583044 Chemical compound C1=2SC=3N=C4CCCCCN4C(=O)C=3C=2CCC(C=O)=C1SC1CCCCC1 NWAPSCLFPKXCMK-UHFFFAOYSA-N 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 125000004185 ester group Chemical group 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 201000008627 kidney hypertrophy Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000002347 octyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- RLOWWWKZYUNIDI-UHFFFAOYSA-N phosphinic chloride Chemical compound ClP=O RLOWWWKZYUNIDI-UHFFFAOYSA-N 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 125000004434 sulfur atom Chemical group 0.000 claims 1
- 0 CC(Cc1c2[s]c(N=C(*)N3*)c1C3=O)C(C=O)=C2S* Chemical compound CC(Cc1c2[s]c(N=C(*)N3*)c1C3=O)C(C=O)=C2S* 0.000 description 2
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US47701703P | 2003-06-10 | 2003-06-10 | |
| PCT/EP2004/006231 WO2004110459A1 (en) | 2003-06-10 | 2004-06-09 | Thiophenepyrimidinones as 17-beta-hydroxysteroid dehydrogenase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2006527227A JP2006527227A (ja) | 2006-11-30 |
| JP2006527227A5 true JP2006527227A5 (https=) | 2007-07-26 |
| JP4612628B2 JP4612628B2 (ja) | 2011-01-12 |
Family
ID=33551663
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006515870A Expired - Fee Related JP4612628B2 (ja) | 2003-06-10 | 2004-06-09 | １７−β−ヒドロキシステロイドデヒドロゲナーゼのインヒビターとしてのチオフェンピリミジノン |
Country Status (17)
| Country | Link |
|---|---|
| US (3) | US7754709B2 (https=) |
| EP (1) | EP1635840B1 (https=) |
| JP (1) | JP4612628B2 (https=) |
| CN (1) | CN100502876C (https=) |
| AR (1) | AR044649A1 (https=) |
| AT (1) | ATE401893T1 (https=) |
| AU (1) | AU2004246791B2 (https=) |
| BR (1) | BRPI0411319A (https=) |
| CA (1) | CA2527591A1 (https=) |
| DE (1) | DE602004015287D1 (https=) |
| DK (1) | DK1635840T3 (https=) |
| ES (1) | ES2311156T3 (https=) |
| PL (1) | PL1635840T3 (https=) |
| PT (1) | PT1635840E (https=) |
| SA (1) | SA04250158B1 (https=) |
| TW (1) | TW200504078A (https=) |
| WO (1) | WO2004110459A1 (https=) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7524853B2 (en) | 2003-06-10 | 2009-04-28 | Solvay Pharmaceuticals B.V. | Compounds and their use in therapy |
| JP2008517061A (ja) * | 2004-10-20 | 2008-05-22 | コンパス ファーマシューティカルズ リミティド ライアビリティ カンパニー | 抗腫瘍剤としての化合物及びそれらの使用 |
| BRPI0419229A (pt) * | 2004-12-13 | 2007-12-18 | Solvay Pharm Gmbh | derivados de tiofenopirimidinona substituìdos como inibidores de 17beta-hidroxiesteróide-desidrogenase, uso e composição farmacêutica |
| GB0513702D0 (en) | 2005-07-04 | 2005-08-10 | Sterix Ltd | Compound |
| EP2013176A2 (en) * | 2006-02-27 | 2009-01-14 | Sterix Limited | Diaryl compounds as non-steroidal inhibitors of 17-beta hydroxysteroid dehydrogenase and/or steroid sulphatase for the treatment of oestrogen-related diseases such as hormone dependent breast cancer |
| EP1990335A4 (en) | 2006-03-02 | 2009-11-11 | Astellas Pharma Inc | 17-BETA-HSD-type-5 INHIBITOR |
| 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 |
| DE102007015169A1 (de) | 2007-03-27 | 2008-10-02 | Universität des Saarlandes Campus Saarbrücken | 17Beta-Hydroxysteroid-Dehydrogenase-Typ1-Inhibitoren zur Behandlung hormonabhängiger Erkrankungen |
| DE102007040243A1 (de) | 2007-08-25 | 2009-02-26 | Universität des Saarlandes | 17Beta-Hydroxysteriod-Dehydrogenase Typ1 Inhibitoren zur Behandlung hormonabhängiger Erkrankungen |
| GB0722779D0 (en) | 2007-11-20 | 2008-01-02 | Sterix Ltd | Compound |
| NZ589691A (en) * | 2008-05-05 | 2012-11-30 | Merck Patent Gmbh | Compounds and methods for inhibiting NHE-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders |
| WO2012025638A1 (en) | 2010-08-27 | 2012-03-01 | Universität des Saarlandes | Selective 17beta-hydroxysteroid dehydrogenase type 1 inhibitors |
| WO2012119605A1 (en) * | 2011-03-10 | 2012-09-13 | Akar Yahya Ahmed Abdellhafeez Salem | New disperse dye with potent anticancer activity |
| WO2014207311A1 (en) | 2013-06-25 | 2014-12-31 | Forendo Pharma Ltd | Therapeutically active estratrienthiazole derivatives as inhibitors of 17.beta.-hydroxy-steroid dehydrogenase, type 1 |
| US10377791B2 (en) | 2013-06-25 | 2019-08-13 | Forendo Pharma Ltd. | Therapeutically active estratrienthiazole derivatives as inhibitors of 17 B-hydroxysteroid dehydrogenase, type 1 |
| KR20160042873A (ko) | 2013-06-25 | 2016-04-20 | 포렌도 파마 리미티드 | 17.베타.-하이드록시스테로이드 탈수소효소의 억제제로서 치료적 활성 17-질소 치환된 에스트라트리엔티아졸 유도체 |
| EP3089969A2 (en) | 2014-01-03 | 2016-11-09 | Elexopharm GmbH | Inhibitors of 17beta-hydroxysteroid dehydrogenases type 1 and type 2 |
| WO2016042775A1 (en) * | 2014-09-18 | 2016-03-24 | Sunovion Pharmaceuticals Inc. | Tricyclic derivative |
| 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 |
| US10626140B2 (en) | 2014-12-23 | 2020-04-21 | Forendo Pharma Ltd | Prodrugs of 17β-HSD1-inhibitors |
| IL314915B1 (en) | 2017-01-23 | 2026-02-01 | Regeneron Pharma | Variants of 17-beta-hydroxysteroid dehydrogenase and their uses |
| KR20190139869A (ko) | 2017-04-11 | 2019-12-18 | 리제너론 파마슈티칼스 인코포레이티드 | 하이드록시스테로이드 (17-베타) 탈수소효소(hsd17b) 패밀리의 구성원의 조절인자의 활성도를 스크리닝하기 위한 검정 |
| FI3634975T3 (fi) | 2017-06-08 | 2024-05-03 | Organon R&D Finland Ltd | 15-beeta-[3-propanamido]substituoitujen estra-1,3,5(10)-trien-17-onien 17-oksiimeja käytettäväksi 17-beeta-hydroksisteroididehydrogenaasien inhiboimisessa |
| US10961583B2 (en) | 2017-10-11 | 2021-03-30 | Regeneron Phramaceuticals, Inc. | Inhibition of HSD17B13 in the treatment of liver disease in patients expressing the PNPLA3 I148M variation |
| JP7507093B2 (ja) | 2018-03-21 | 2024-06-27 | リジェネロン・ファーマシューティカルズ・インコーポレイテッド | １７β－水酸化ステロイド脱水素酵素１３型（ＨＳＤ１７Ｂ１３）ｉＲＮＡ組成物およびその使用方法 |
| US10285998B1 (en) | 2018-04-04 | 2019-05-14 | The Menopause Method, Inc. | Composition and method to aid in hormone replacement therapy |
| MX2021003077A (es) | 2018-09-19 | 2021-05-27 | Arrowhead Pharmaceuticals Inc | Agentes de arni para inhibir la expresion de 17beta-hsd tipo 13 (hsd17b13), composiciones de dichos agentes, y metodos de uso. |
| CN109180702B (zh) * | 2018-10-29 | 2021-11-30 | 四川大学 | 一种噻吩并嘧啶酮化合物及其用途 |
| BR112021010598A2 (pt) | 2018-12-05 | 2021-08-24 | Forendo Pharma Ltd | Compostos, método para preparação de um composto e composição farmacêutica |
| JP7612682B2 (ja) | 2019-10-15 | 2025-01-14 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 新規なテトラゾール |
| PH12022550846A1 (en) * | 2019-10-15 | 2023-03-27 | Boehringer Ingelheim Pharma | Thienopyrimidones as trpa1 inhibitors |
| CA3210965A1 (en) | 2021-04-14 | 2022-10-20 | Boehringer Ingelheim International Gmbh | 3h,4h-thieno[2,3-d]pyrimidin-4-one derivatives as trpa1 inhibitors |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| JPS4742271B1 (https=) * | 1968-06-20 | 1972-10-25 | ||
| DE2411273A1 (de) * | 1974-03-06 | 1975-09-18 | Schering Ag | Neue thieno eckige klammer auf 2,3-d eckige klammer zu pyrimidinone und verfahren zu ihrer herstellung |
| US5395842A (en) * | 1988-10-31 | 1995-03-07 | Endorecherche Inc. | Anti-estrogenic compounds and compositions |
| US5364847A (en) * | 1989-03-10 | 1994-11-15 | Endorecherche | Inhibitors of sex steroid biosynthesis and methods for their production and use |
| US5597823A (en) * | 1995-01-27 | 1997-01-28 | Abbott Laboratories | Tricyclic substituted hexahydrobenz [e]isoindole alpha-1 adrenergic antagonists |
| JP3783810B2 (ja) | 1997-01-14 | 2006-06-07 | 第一製薬株式会社 | 新規ベンゾフラノン誘導体及びその製造方法 |
| JPH10273467A (ja) | 1997-01-29 | 1998-10-13 | Snow Brand Milk Prod Co Ltd | 新規テトラロン又はベンゾピラノン誘導体及びその製造方法 |
| JP4166433B2 (ja) | 1997-09-11 | 2008-10-15 | 第一製薬株式会社 | ホルモン依存性疾患治療剤 |
| TR200002784T2 (tr) | 1998-03-11 | 2000-12-21 | Endorecherche, Inc | Tip 5 ve tip 3 17beta-Hidroksisteroid dehidrojenaz inhibitörleri ve bunların kullanımı için metodlar |
| GB9816729D0 (en) | 1998-08-01 | 1998-09-30 | Hoechst Schering Agrevo Gmbh | Substituted cyclohexylaminopyrimidines |
| GB9929302D0 (en) | 1999-12-11 | 2000-02-02 | Univ Cardiff | Benzyl tetralins compositions and uses thereof |
| AU2001296961A1 (en) | 2000-09-29 | 2002-04-08 | Bayer Pharmaceuticals Corporation | 17-beta-hydroxysteroid dehydrogenase-ii inhibitors |
| WO2003017974A1 (en) | 2001-08-31 | 2003-03-06 | Pantarhei Bioscience B.V. | Method of treating benign gynaecological disorders and a pharmaceutical kit for use in such method |
| AR036492A1 (es) | 2001-09-06 | 2004-09-15 | Schering Corp | Inhibidores de la 17beta-hidroxiesteroide deshidrogenasa tipo 3, composiciones farmaceuticas y el uso de dichos inhibidores para la elaboracion de un medicamento para el tratamiento de enfermedades androgeno dependientes |
| US6750248B2 (en) | 2001-11-09 | 2004-06-15 | National University Of Singapore | Methods for preparing an estrogenic preparation and isolated estrogenic compounds from a plant and uses thereof |
| FI20030393A7 (fi) | 2003-03-14 | 2004-09-15 | Molekyyliendokrinologian Tutkimusyksikkoe | Menetelmiä, joilla voidaan ennustaa rintasyövän kehistyskulku ja yhdisteitä, joita voidaan käyttää sen ehkäisemiseksi tai hoitamiseksi |
| GB0324792D0 (en) * | 2003-10-23 | 2003-11-26 | Sterix Ltd | Compound |
| CN1964956B (zh) * | 2004-05-24 | 2013-03-27 | 安美基公司 | 11-β-羟基类固醇脱氢酶1型的抑制剂 |
-
2004
- 2004-06-07 US US10/861,922 patent/US7754709B2/en not_active Expired - Fee Related
- 2004-06-08 AR ARP040101982A patent/AR044649A1/es not_active Application Discontinuation
- 2004-06-08 TW TW093116412A patent/TW200504078A/zh unknown
- 2004-06-09 PL PL04739738T patent/PL1635840T3/pl unknown
- 2004-06-09 CA CA002527591A patent/CA2527591A1/en not_active Abandoned
- 2004-06-09 DK DK04739738T patent/DK1635840T3/da active
- 2004-06-09 AT AT04739738T patent/ATE401893T1/de active
- 2004-06-09 PT PT04739738T patent/PT1635840E/pt unknown
- 2004-06-09 WO PCT/EP2004/006231 patent/WO2004110459A1/en not_active Ceased
- 2004-06-09 ES ES04739738T patent/ES2311156T3/es not_active Expired - Lifetime
- 2004-06-09 JP JP2006515870A patent/JP4612628B2/ja not_active Expired - Fee Related
- 2004-06-09 BR BRPI0411319-5A patent/BRPI0411319A/pt not_active IP Right Cessation
- 2004-06-09 DE DE602004015287T patent/DE602004015287D1/de not_active Expired - Lifetime
- 2004-06-09 CN CNB2004800126362A patent/CN100502876C/zh not_active Expired - Fee Related
- 2004-06-09 EP EP04739738A patent/EP1635840B1/en not_active Expired - Lifetime
- 2004-06-09 AU AU2004246791A patent/AU2004246791B2/en not_active Ceased
- 2004-06-12 SA SA04250158A patent/SA04250158B1/ar unknown
-
2007
- 2007-12-31 US US11/967,989 patent/US20080103131A1/en not_active Abandoned
-
2010
- 2010-06-08 US US12/796,097 patent/US20100249106A1/en not_active Abandoned
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