PE20181378A1 - Compuestos biciclicos derivados de dihidroquinolina-2-ona como inhibidores de cyp11b - Google Patents
Compuestos biciclicos derivados de dihidroquinolina-2-ona como inhibidores de cyp11bInfo
- Publication number
- PE20181378A1 PE20181378A1 PE2018001330A PE2018001330A PE20181378A1 PE 20181378 A1 PE20181378 A1 PE 20181378A1 PE 2018001330 A PE2018001330 A PE 2018001330A PE 2018001330 A PE2018001330 A PE 2018001330A PE 20181378 A1 PE20181378 A1 PE 20181378A1
- Authority
- PE
- Peru
- Prior art keywords
- dihydroquinoline
- cyp11b
- ona
- inhibitors
- derivative
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 102100024329 Cytochrome P450 11B2, mitochondrial Human genes 0.000 title 1
- 101000761960 Homo sapiens Cytochrome P450 11B1, mitochondrial Proteins 0.000 title 1
- 101000761956 Homo sapiens Cytochrome P450 11B2, mitochondrial Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000001188 haloalkyl group Chemical group 0.000 abstract 2
- 206010007559 Cardiac failure congestive Diseases 0.000 abstract 1
- 208000016998 Conn syndrome Diseases 0.000 abstract 1
- 206010019280 Heart failures Diseases 0.000 abstract 1
- 206010020772 Hypertension Diseases 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 208000020832 chronic kidney disease Diseases 0.000 abstract 1
- 125000005347 halocycloalkyl group Chemical group 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- LVDKZTHQIJVVBW-UHFFFAOYSA-N n-[4-(1-methyl-2-oxo-3,4-dihydroquinolin-6-yl)-5,6,7,8-tetrahydroisoquinolin-8-yl]ethanesulfonamide Chemical compound CN1C(=O)CCC2=CC(C3=CN=CC4=C3CCCC4NS(=O)(=O)CC)=CC=C21 LVDKZTHQIJVVBW-UHFFFAOYSA-N 0.000 abstract 1
- VDEUDSRUMNAXJG-UHFFFAOYSA-N n-[4-(1-methyl-2-oxo-3,4-dihydroquinolin-6-yl)-5,6,7,8-tetrahydroisoquinolin-8-yl]propanamide Chemical compound CN1C(=O)CCC2=CC(C3=CN=CC4=C3CCCC4NC(=O)CC)=CC=C21 VDEUDSRUMNAXJG-UHFFFAOYSA-N 0.000 abstract 1
- 208000013846 primary aldosteronism Diseases 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
- A61P5/42—Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of mineralocorticosteroids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Endocrinology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Emergency Medicine (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Se refiere compuestos biciclicos derivados de dihidroquinolina-2-ona de formula I en los que R1, R2, R3, R4, R5, R8, R9, R10 son H, alquilo, haloalquilo, cicloalquilo, halocicloalquilo; R6, R7, R12, son H, halogeno, alquilo, haloalquilo, cicloalquilo, entre otros; A1 es N o CR13; A2 es NR14, entre otros; A3 es N o CR17; n es cero, 1 o 2. Dichos compuestos son utiles para terapia o profilaxis de enfermedad renal cronica, fallo cardiaco congestivo, hipertension, aldosteronismo primario, entre otros. Entre los compuestos preferidos tenemos los siguientes: (rac)-N-[4-(1-metil-2-oxo-1,2,3,4-tetrahidro-quinolin-6-il)-5,6,7,8-tetrahidro-isoquinolin-8-il)propionamida; (rac)-N-[4-(1-metil-2-oxo-1,2,3,4-tetrahidroquinolin-6-il)-5,6,7,8-tetrahidroisoquinolin-8-il)etanosulfonamida; entre otros.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2011080078 | 2011-09-23 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20181378A1 true PE20181378A1 (es) | 2018-09-05 |
Family
ID=46963698
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2018001330A PE20181378A1 (es) | 2011-09-23 | 2012-09-20 | Compuestos biciclicos derivados de dihidroquinolina-2-ona como inhibidores de cyp11b |
| PE2014000393A PE20141042A1 (es) | 2011-09-23 | 2012-09-20 | Nuevos derivados biciclicos de dihidroquinolina-2-ona |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2014000393A PE20141042A1 (es) | 2011-09-23 | 2012-09-20 | Nuevos derivados biciclicos de dihidroquinolina-2-ona |
Country Status (34)
| Country | Link |
|---|---|
| US (1) | US9353081B2 (es) |
| EP (1) | EP2758388B1 (es) |
| JP (1) | JP6012737B2 (es) |
| KR (1) | KR101723276B1 (es) |
| CN (1) | CN103827101B (es) |
| AR (1) | AR087984A1 (es) |
| AU (1) | AU2012311582B2 (es) |
| BR (1) | BR112014006660B1 (es) |
| CA (1) | CA2845170C (es) |
| CL (1) | CL2014000663A1 (es) |
| CO (1) | CO6870035A2 (es) |
| CR (1) | CR20140089A (es) |
| DK (1) | DK2758388T3 (es) |
| EA (1) | EA035108B1 (es) |
| EC (1) | ECSP14013264A (es) |
| ES (1) | ES2666802T3 (es) |
| HR (1) | HRP20180592T1 (es) |
| HU (1) | HUE038773T2 (es) |
| IL (1) | IL230874A (es) |
| LT (1) | LT2758388T (es) |
| MX (1) | MX366095B (es) |
| MY (1) | MY186165A (es) |
| NO (1) | NO2758388T3 (es) |
| PE (2) | PE20181378A1 (es) |
| PH (1) | PH12014500584A1 (es) |
| PL (1) | PL2758388T3 (es) |
| PT (1) | PT2758388T (es) |
| RS (1) | RS57139B1 (es) |
| SG (1) | SG2014010599A (es) |
| SI (1) | SI2758388T1 (es) |
| TW (1) | TWI576342B (es) |
| UA (1) | UA115972C2 (es) |
| WO (1) | WO2013041591A1 (es) |
| ZA (1) | ZA201401577B (es) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA117092C2 (uk) | 2011-09-06 | 2018-06-25 | Байєр Інтеллектуал Проперті Гмбх | Амінозаміщені імідазопіридазини |
| EP2838883B1 (en) * | 2012-04-17 | 2017-11-08 | F. Hoffmann-La Roche AG | New phenyl-tetrahydroisoquinoline derivatives |
| US9783543B2 (en) | 2012-11-19 | 2017-10-10 | Bayer Pharma Aktiengesellschaft | Aminoimidazopyridazines |
| BR112015023280A2 (pt) * | 2013-03-14 | 2017-07-18 | Hoffmann La Roche | derivados de dihidroquinolin-2-ona para utilização como inibidores da aldosterona sintase |
| DK3004077T3 (da) * | 2013-05-27 | 2020-01-13 | Hoffmann La Roche | Nye 3,4-dihydro-2H-isoquinolin-1-on- og 2,3-dihydro-isoindol-1-on-forbindelser |
| KR102217285B1 (ko) * | 2013-05-27 | 2021-02-22 | 에프. 호프만-라 로슈 아게 | 신규한 3,4-다이하이드로-2h-이소퀴놀린-1-온 및 2,3-다이하이드로-이소인돌-1-온 화합물 |
| RS59663B1 (sr) * | 2013-05-27 | 2020-01-31 | Hoffmann La Roche | Nova jedinjenja 3,4-dihidro-2h-izokinolin-1-on i 2,3-dihidro-izoindol-1-on |
| CN105593212B (zh) * | 2013-10-17 | 2019-06-04 | 豪夫迈·罗氏有限公司 | 作为醛固酮合酶抑制剂的苯基-二氢吡啶衍生物 |
| RU2016116435A (ru) * | 2013-10-17 | 2017-11-22 | Ф. Хоффманн-Ля Рош Аг | Производные фенил-дигидропиридина в качестве ингибиторов альдостеронсинтазы |
| CA2915788A1 (en) * | 2013-10-17 | 2015-04-23 | F. Hoffmann-La Roche Ag | New phenyl-dihydropyridine derivatives as aldosterone synthase inhibitors |
| EP3212638B1 (en) * | 2014-10-31 | 2019-11-20 | F.Hoffmann-La Roche Ag | New dihydroquinoline pyrazolyl compounds as aldosterone synthase inhibitors |
| WO2016066597A1 (en) * | 2014-10-31 | 2016-05-06 | F. Hoffmann-La Roche Ag | New dihydroquinoline pyrazolyl compounds |
| JP6669734B2 (ja) * | 2014-10-31 | 2020-03-18 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | ピラゾリル−３，４−ジドヒドロキノリン−２−オン・アルドステロン合成酵素阻害剤 |
| US9890171B2 (en) | 2014-12-02 | 2018-02-13 | Boehringer Ingelheim International Gmbh | Aldosterone synthase inhibitors |
| SG11201810847RA (en) | 2016-06-10 | 2019-01-30 | Nihon Mediphysics Co Ltd | Non-invasive diagnostic imaging agent for heart disease |
| WO2020223267A1 (en) | 2019-05-01 | 2020-11-05 | Boehringer Ingelheim International Gmbh | (r)-(2-methyloxiran-2-yl)methyl 4-bromobenzenesulfonate |
| US20240277698A1 (en) * | 2021-06-24 | 2024-08-22 | Cincor Pharma, Inc. | Methods of using aldosterone synthase inhibitors |
| WO2023063851A1 (en) * | 2021-10-13 | 2023-04-20 | «Target Medicals» Limited Liability Company | Inhibitors of human aldosterone synthase (cyp11b2) |
| CN118401241A (zh) | 2021-12-14 | 2024-07-26 | 勃林格殷格翰国际有限公司 | 用于治疗慢性肾脏病的醛固酮合成酶抑制剂 |
| KR20250057804A (ko) | 2022-09-02 | 2025-04-29 | 애프니메드, 인코포레이티드 (델라웨어) | 수면 무호흡증을 치료하기 위한 방법 및 조성물 |
| EP4574830A1 (en) * | 2022-09-23 | 2025-06-25 | Guangzhou Vinnocent Pharmaceutical Limited | Annelated pyridine steroid synthetase inhibitor, preparation method therefor, and use thereof |
| EP4624464A1 (en) * | 2022-11-23 | 2025-10-01 | Shanghai Hansoh Biomedical Co., Ltd. | Pyridine polycyclic compound inhibitor, preparation method therefor and use thereof |
| TW202446391A (zh) * | 2023-04-28 | 2024-12-01 | 大陸商長春金賽藥業有限責任公司 | Ｃｙｐ１１ｂ２抑制劑化合物、藥物組合物及其用途 |
| WO2024235165A1 (zh) * | 2023-05-12 | 2024-11-21 | 南京明德新药研发有限公司 | 含氮杂环类化合物及其应用 |
| WO2025002335A1 (zh) * | 2023-06-29 | 2025-01-02 | 苏州科睿思制药有限公司 | Baxdrostat的晶型及其制备方法和用途 |
| TW202504603A (zh) * | 2023-07-21 | 2025-02-01 | 大陸商上海翰森生物醫藥科技有限公司 | 三并環類化合物、及其製備方法和應用 |
| US12427185B2 (en) | 2023-09-05 | 2025-09-30 | E-Star Biotech, LLC | Formulations of MANP and uses thereof |
| CN117247371A (zh) * | 2023-09-18 | 2023-12-19 | 上海相辉医药科技有限公司 | 一种cyp11b2抑制剂baxdrostat的制备方法 |
| TW202519227A (zh) * | 2023-11-10 | 2025-05-16 | 大陸商上海齊魯製藥研究中心有限公司 | 稠環衍生物、其製備方法及其在醫藥上的應用 |
| TW202525278A (zh) | 2023-12-15 | 2025-07-01 | 愛爾蘭商阿斯特捷利康愛爾蘭有限公司 | 治療慢性腎病及高血壓之方法 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4792561A (en) * | 1986-05-29 | 1988-12-20 | Syntex (U.S.A.) Inc. | Carbostyril derivatives as combined thromboxane synthetase and cyclic-AMP phosphodiesterase inhibitors |
| GB8709448D0 (en) | 1987-04-21 | 1987-05-28 | Pfizer Ltd | Heterobicyclic quinoline derivatives |
| US5246944A (en) * | 1991-08-13 | 1993-09-21 | Merck & Co., Inc. | Quinoline angiotensin ii antagonists incorporating a substituted benzyl element |
| WO2005065050A2 (ja) * | 2003-12-25 | 2005-07-21 | Asahi Kasei Pharma Corporation | ２環化合物 |
| JP5202327B2 (ja) | 2005-12-09 | 2013-06-05 | アムジエン・インコーポレーテツド | プロリルヒドロキシラーゼ阻害活性を示すキノロンベースの化合物、およびこの組成物、およびこの使用 |
| DE102008022221A1 (de) * | 2008-05-06 | 2009-11-12 | Universität des Saarlandes | Inhibitoren der humanen Aldosteronsynthase CYP11B2 |
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2012
- 2012-09-14 US US13/615,901 patent/US9353081B2/en active Active
- 2012-09-20 EA EA201490567A patent/EA035108B1/ru not_active IP Right Cessation
- 2012-09-20 PT PT127666287T patent/PT2758388T/pt unknown
- 2012-09-20 JP JP2014531214A patent/JP6012737B2/ja active Active
- 2012-09-20 KR KR1020147010662A patent/KR101723276B1/ko active Active
- 2012-09-20 MY MYPI2014700679A patent/MY186165A/en unknown
- 2012-09-20 SG SG2014010599A patent/SG2014010599A/en unknown
- 2012-09-20 PE PE2018001330A patent/PE20181378A1/es unknown
- 2012-09-20 AU AU2012311582A patent/AU2012311582B2/en active Active
- 2012-09-20 MX MX2014002624A patent/MX366095B/es active IP Right Grant
- 2012-09-20 UA UAA201404207A patent/UA115972C2/uk unknown
- 2012-09-20 PH PH1/2014/500584A patent/PH12014500584A1/en unknown
- 2012-09-20 PE PE2014000393A patent/PE20141042A1/es active IP Right Grant
- 2012-09-20 NO NO12766628A patent/NO2758388T3/no unknown
- 2012-09-20 HU HUE12766628A patent/HUE038773T2/hu unknown
- 2012-09-20 PL PL12766628T patent/PL2758388T3/pl unknown
- 2012-09-20 RS RS20180446A patent/RS57139B1/sr unknown
- 2012-09-20 BR BR112014006660-4A patent/BR112014006660B1/pt active IP Right Grant
- 2012-09-20 SI SI201231277T patent/SI2758388T1/en unknown
- 2012-09-20 ES ES12766628.7T patent/ES2666802T3/es active Active
- 2012-09-20 CA CA2845170A patent/CA2845170C/en active Active
- 2012-09-20 LT LTEP12766628.7T patent/LT2758388T/lt unknown
- 2012-09-20 HR HRP20180592TT patent/HRP20180592T1/hr unknown
- 2012-09-20 WO PCT/EP2012/068472 patent/WO2013041591A1/en active Application Filing
- 2012-09-20 EP EP12766628.7A patent/EP2758388B1/en active Active
- 2012-09-20 DK DK12766628.7T patent/DK2758388T3/en active
- 2012-09-20 CN CN201280045785.3A patent/CN103827101B/zh active Active
- 2012-09-21 AR ARP120103485A patent/AR087984A1/es active IP Right Grant
- 2012-09-21 TW TW101134790A patent/TWI576342B/zh active
-
2014
- 2014-01-31 CO CO14020664A patent/CO6870035A2/es active IP Right Grant
- 2014-02-06 IL IL230874A patent/IL230874A/en active IP Right Grant
- 2014-02-25 CR CR20140089A patent/CR20140089A/es unknown
- 2014-02-28 ZA ZA2014/01577A patent/ZA201401577B/en unknown
- 2014-03-19 CL CL2014000663A patent/CL2014000663A1/es unknown
- 2014-03-21 EC ECSP14013264 patent/ECSP14013264A/es unknown
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