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)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Endocrinology (AREA)
- Heart & Thoracic Surgery (AREA)
- Emergency Medicine (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (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 |
|---|---|---|---|
| PE2014000393A PE20141042A1 (es) | 2011-09-23 | 2012-09-20 | Nuevos derivados biciclicos de dihidroquinolina-2-ona |
| PE2018001330A PE20181378A1 (es) | 2011-09-23 | 2012-09-20 | Compuestos biciclicos derivados de dihidroquinolina-2-ona como inhibidores de cyp11b |
Family Applications Before (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) | PE20141042A1 (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 (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA117092C2 (uk) | 2011-09-06 | 2018-06-25 | Байєр Інтеллектуал Проперті Гмбх | Амінозаміщені імідазопіридазини |
| DK2838883T3 (en) * | 2012-04-17 | 2018-01-15 | Hoffmann La Roche | New phenyl-tetrahydroisoquinoline derivatives |
| CA2891644A1 (en) | 2012-11-19 | 2014-05-22 | Bayer Pharma Aktiengesellschaft | Aminoimidazopyridazines |
| JP6117948B2 (ja) * | 2013-03-14 | 2017-04-19 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | アルドステロン合成酵素阻害薬としての使用のためのジヒドロキノリン−２−オン誘導体 |
| CA2903180C (en) * | 2013-05-27 | 2022-03-15 | F. Hoffmann-La Roche Ag | 3,4-dihydro-2h-isoquinoline-1-one and 2,3-dihydro-isoindol-1-one compounds |
| ES2763424T3 (es) * | 2013-05-27 | 2020-05-28 | Hoffmann La Roche | Nuevos compuestos de 3,4-dihidro-2H-isoquinolin-1-ona y 2,3-dihidro-isoindol-1-ona |
| ES2804271T3 (es) * | 2013-05-27 | 2021-02-05 | Hoffmann La Roche | Nuevos compuestos de 3,4-dihidro-2H-isoquinolin-1-ona y 2,3-dihidro-isoindol-1-ona |
| 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 |
| CN105531263B (zh) * | 2013-10-17 | 2019-08-23 | 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 |
| WO2015055604A1 (en) * | 2013-10-17 | 2015-04-23 | F. Hoffmann-La Roche Ag | New phenyl-dihydropyridine derivatives as aldosterone synthase inhibitors |
| WO2016066597A1 (en) * | 2014-10-31 | 2016-05-06 | F. Hoffmann-La Roche Ag | New dihydroquinoline pyrazolyl compounds |
| CN106604917B (zh) * | 2014-10-31 | 2020-10-09 | 豪夫迈·罗氏有限公司 | 作为醛固酮合酶抑制剂的新型二氢喹啉吡唑基化合物 |
| 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 |
| WO2016089800A1 (en) * | 2014-12-02 | 2016-06-09 | Boehringer Ingelheim International Gmbh | Aldosterone synthase inhibitors |
| US20190255199A1 (en) | 2016-06-10 | 2019-08-22 | Nihon Medi-Physics Co., Ltd. | Non-invasive diagnostic imaging agent for heart disease |
| EP3962903A1 (en) | 2019-05-01 | 2022-03-09 | Boehringer Ingelheim International GmbH | (r)-(2-methyloxiran-2-yl)methyl 4-bromobenzenesulfonate |
| KR20240035483A (ko) * | 2021-06-24 | 2024-03-15 | 신코 파마, 인크. | 알도스테론 합성효소 억제제를 사용하는 방법 |
| WO2023063851A1 (en) * | 2021-10-13 | 2023-04-20 | «Target Medicals» Limited Liability Company | Inhibitors of human aldosterone synthase (cyp11b2) |
| CA3236890A1 (en) | 2021-12-14 | 2023-06-22 | Boehringer Ingelheim International Gmbh | Aldosterone synthase inhibitors for treating chronic kidney disease |
| KR20250057804A (ko) | 2022-09-02 | 2025-04-29 | 애프니메드, 인코포레이티드 (델라웨어) | 수면 무호흡증을 치료하기 위한 방법 및 조성물 |
| WO2024061371A1 (zh) * | 2022-09-23 | 2024-03-28 | 广州威诺森医药科技有限公司 | 一种骈环吡啶类甾体合成酶抑制剂及其制备方法和应用 |
| CN120187713A (zh) * | 2022-11-23 | 2025-06-20 | 上海翰森生物医药科技有限公司 | 吡啶多环类化合物抑制剂、及其制备方法和应用 |
| WO2024222814A1 (zh) * | 2023-04-28 | 2024-10-31 | 长春金赛药业有限责任公司 | Cyp11b2抑制剂化合物、药物组合物及其应用 |
| 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 |
| WO2025021062A1 (zh) * | 2023-07-21 | 2025-01-30 | 上海翰森生物医药科技有限公司 | 三并环类化合物、及其制备方法和应用 |
| WO2025098465A1 (zh) * | 2023-11-10 | 2025-05-15 | 上海齐鲁制药研究中心有限公司 | 稠环衍生物、其制备方法及其在医药上的应用 |
| WO2025125513A1 (en) | 2023-12-15 | 2025-06-19 | AstraZeneca Ireland Limited | Sglt2 inhibitors and baxdrostat for treating chronic kidney disease and hypertension |
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 |
| AU2006326662B2 (en) | 2005-12-09 | 2011-07-28 | Amgen Inc. | Quinolone based compounds exhibiting prolyl hydroxylase inhibitory activity, and compositions, and uses thereof |
| 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 MX MX2014002624A patent/MX366095B/es active IP Right Grant
- 2012-09-20 SG SG2014010599A patent/SG2014010599A/en unknown
- 2012-09-20 PE PE2014000393A patent/PE20141042A1/es active IP Right Grant
- 2012-09-20 LT LTEP12766628.7T patent/LT2758388T/lt unknown
- 2012-09-20 PT PT127666287T patent/PT2758388T/pt unknown
- 2012-09-20 PL PL12766628T patent/PL2758388T3/pl unknown
- 2012-09-20 JP JP2014531214A patent/JP6012737B2/ja active Active
- 2012-09-20 UA UAA201404207A patent/UA115972C2/uk unknown
- 2012-09-20 MY MYPI2014700679A patent/MY186165A/en unknown
- 2012-09-20 ES ES12766628.7T patent/ES2666802T3/es active Active
- 2012-09-20 BR BR112014006660-4A patent/BR112014006660B1/pt active IP Right Grant
- 2012-09-20 CA CA2845170A patent/CA2845170C/en active Active
- 2012-09-20 AU AU2012311582A patent/AU2012311582B2/en active Active
- 2012-09-20 PE PE2018001330A patent/PE20181378A1/es unknown
- 2012-09-20 PH PH1/2014/500584A patent/PH12014500584A1/en unknown
- 2012-09-20 SI SI201231277T patent/SI2758388T1/en unknown
- 2012-09-20 WO PCT/EP2012/068472 patent/WO2013041591A1/en active Application Filing
- 2012-09-20 EA EA201490567A patent/EA035108B1/ru not_active IP Right Cessation
- 2012-09-20 HU HUE12766628A patent/HUE038773T2/hu unknown
- 2012-09-20 RS RS20180446A patent/RS57139B1/sr unknown
- 2012-09-20 EP EP12766628.7A patent/EP2758388B1/en active Active
- 2012-09-20 DK DK12766628.7T patent/DK2758388T3/en active
- 2012-09-20 NO NO12766628A patent/NO2758388T3/no unknown
- 2012-09-20 CN CN201280045785.3A patent/CN103827101B/zh active Active
- 2012-09-20 KR KR1020147010662A patent/KR101723276B1/ko active Active
- 2012-09-20 HR HRP20180592TT patent/HRP20180592T1/hr unknown
- 2012-09-21 TW TW101134790A patent/TWI576342B/zh active
- 2012-09-21 AR ARP120103485A patent/AR087984A1/es active IP Right Grant
-
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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