JP4612628B2 - 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 - Google Patents
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 Download PDFInfo
- Publication number
- JP4612628B2 JP4612628B2 JP2006515870A JP2006515870A JP4612628B2 JP 4612628 B2 JP4612628 B2 JP 4612628B2 JP 2006515870 A JP2006515870 A JP 2006515870A JP 2006515870 A JP2006515870 A JP 2006515870A JP 4612628 B2 JP4612628 B2 JP 4612628B2
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- 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.)
- Expired - Fee Related
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- 0 CN(C(*)=NC1=C2*C(*)=S1)C2=O Chemical compound CN(C(*)=NC1=C2*C(*)=S1)C2=O 0.000 description 10
- NOPFKZSNTRHNQU-UHFFFAOYSA-N CC(N1C)=Nc([s]c2c3CCCC2=O)c3C1=O Chemical compound CC(N1C)=Nc([s]c2c3CCCC2=O)c3C1=O NOPFKZSNTRHNQU-UHFFFAOYSA-N 0.000 description 1
- JOJLHKIVQDSRKX-UHFFFAOYSA-N CCC(N1C)=Nc([s]c2c3CCCC2=O)c3C1=O Chemical compound CCC(N1C)=Nc([s]c2c3CCCC2=O)c3C1=O JOJLHKIVQDSRKX-UHFFFAOYSA-N 0.000 description 1
- RDUGGUBAQYKSMQ-UHFFFAOYSA-N CCOC(C(CCC1=Nc2c3c(CCCC4=O)c4[s]2)CCN1C3=O)=O Chemical compound CCOC(C(CCC1=Nc2c3c(CCCC4=O)c4[s]2)CCN1C3=O)=O RDUGGUBAQYKSMQ-UHFFFAOYSA-N 0.000 description 1
- XZDDZGKJCJKISJ-UHFFFAOYSA-N CCOC(c1c(N)[s]c2c1CCCCC(C)(C)CC2)=O Chemical compound CCOC(c1c(N)[s]c2c1CCCCC(C)(C)CC2)=O XZDDZGKJCJKISJ-UHFFFAOYSA-N 0.000 description 1
- LWBYNHFNVQXTIB-UHFFFAOYSA-N O=C1N(CCCCC2)C2=Nc2c1c(CCCCC1)c1[s]2 Chemical compound O=C1N(CCCCC2)C2=Nc2c1c(CCCCC1)c1[s]2 LWBYNHFNVQXTIB-UHFFFAOYSA-N 0.000 description 1
- XCEQSKRNKVHGPL-UHFFFAOYSA-N O=CC(CCc1c2[s]c(N=C3N4CCC(COCC(CCc5c6[s]c(N=C7N8CCCCC7)c5C8=O)=C6Cl)CC3)c1C4=O)=C2Cl Chemical compound O=CC(CCc1c2[s]c(N=C3N4CCC(COCC(CCc5c6[s]c(N=C7N8CCCCC7)c5C8=O)=C6Cl)CC3)c1C4=O)=C2Cl XCEQSKRNKVHGPL-UHFFFAOYSA-N 0.000 description 1
- OQWFFTTZNIRMIH-UHFFFAOYSA-N O=CC(CCc1c2[s]c(N=C3N4CCCCC3)c1C4=O)=C2S(c1ccccc1)=O Chemical compound O=CC(CCc1c2[s]c(N=C3N4CCCCC3)c1C4=O)=C2S(c1ccccc1)=O OQWFFTTZNIRMIH-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
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- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D495/14—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Psychiatry (AREA)
- Ophthalmology & Optometry (AREA)
- Diabetes (AREA)
- Toxicology (AREA)
- Addiction (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Gynecology & Obstetrics (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Steroid Compounds (AREA)
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 JP2006527227A5 (https=) | 2007-07-26 |
| JP4612628B2 true 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 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
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-
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
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2010
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Also Published As
| Publication number | Publication date |
|---|---|
| US20100249106A1 (en) | 2010-09-30 |
| JP2006527227A (ja) | 2006-11-30 |
| ES2311156T3 (es) | 2009-02-01 |
| HK1087331A1 (zh) | 2006-10-13 |
| BRPI0411319A (pt) | 2006-07-18 |
| AU2004246791A1 (en) | 2004-12-23 |
| SA04250158B1 (ar) | 2007-10-29 |
| ATE401893T1 (de) | 2008-08-15 |
| US20050032778A1 (en) | 2005-02-10 |
| PT1635840E (pt) | 2008-09-17 |
| EP1635840B1 (en) | 2008-07-23 |
| EP1635840A1 (en) | 2006-03-22 |
| DE602004015287D1 (en) | 2008-09-04 |
| AU2004246791B2 (en) | 2010-02-18 |
| US7754709B2 (en) | 2010-07-13 |
| AR044649A1 (es) | 2005-09-21 |
| CA2527591A1 (en) | 2004-12-23 |
| TW200504078A (en) | 2005-02-01 |
| CN100502876C (zh) | 2009-06-24 |
| WO2004110459A1 (en) | 2004-12-23 |
| DK1635840T3 (da) | 2008-09-01 |
| US20080103131A1 (en) | 2008-05-01 |
| CN1784234A (zh) | 2006-06-07 |
| PL1635840T3 (pl) | 2009-01-30 |
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