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 (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA117092C2 (uk) | 2011-09-06 | 2018-06-25 | Байєр Інтеллектуал Проперті Гмбх | Амінозаміщені імідазопіридазини |
| TW201345895A (zh) * | 2012-04-17 | 2013-11-16 | Hoffmann La Roche | 新穎苯基－四氫異喹啉衍生物 |
| CA2891644A1 (en) | 2012-11-19 | 2014-05-22 | Bayer Pharma Aktiengesellschaft | Aminoimidazopyridazines |
| RU2015138961A (ru) * | 2013-03-14 | 2017-04-18 | Ф. Хоффманн-Ля Рош Аг | Производные дигидрохинолин-2-она для применения в качестве ингибиторов альдостеронсинтазы |
| LT3004077T (lt) * | 2013-05-27 | 2020-01-27 | F. Hoffmann-La Roche Ag | Nauji 3,4-dihidro-2h-izochinolin-1-ono ir 2,3-dihidro-izoindol-1-ono junginiai |
| WO2014191336A1 (en) * | 2013-05-27 | 2014-12-04 | F. Hoffmann-La Roche Ag | New 3,4-dihydro-2h-isoquinoline-1-one and 2,3-dihydro-isoindol-1-one compounds |
| RU2693698C2 (ru) * | 2013-05-27 | 2019-07-04 | Ф. Хоффманн-Ля Рош Аг | Новые соединения 3,4-дигидро-2н-изохинолин-1-она и 2,3-дигидроизоиндол-1-она |
| RU2016116433A (ru) * | 2013-10-17 | 2017-11-22 | Ф. Хоффманн-Ля Рош Аг | Новые производные фенил-дигидропиридина в качестве ингибиторов альдостерон синтазы |
| EP3057940A1 (en) * | 2013-10-17 | 2016-08-24 | F.Hoffmann-La Roche Ag | Phenyl-dihydropyridine derivatives as inhibitors of aldosterone synthase |
| 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 |
| WO2016066662A1 (en) * | 2014-10-31 | 2016-05-06 | F. Hoffmann-La Roche Ag | New dihydroquinoline pyrazolyl compounds as aldosterone synthase inhibitors |
| EP3212630B1 (en) * | 2014-10-31 | 2022-05-18 | F. Hoffmann-La Roche AG | New dihydroquinoline pyrazolyl compounds |
| CN106660998B (zh) * | 2014-10-31 | 2019-10-25 | 豪夫迈·罗氏有限公司 | 吡唑基-3,4-二氢喹啉-2-酮醛固酮合酶抑制剂 |
| JP6707084B2 (ja) | 2014-12-02 | 2020-06-10 | 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 | アルドステロンシンターゼ阻害薬 |
| 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 |
| JP2024523559A (ja) * | 2021-06-24 | 2024-06-28 | シンコア・ファーマ・インコーポレイテッド | アルドステロン合成酵素阻害剤を使用する方法 |
| 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 |
| AU2023335927A1 (en) | 2022-09-02 | 2025-02-27 | Apnimed, Inc. (Delaware) | Methods and compositions for treating sleep apnea |
| CN119894905A (zh) * | 2022-09-23 | 2025-04-25 | 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 |
| CN120359210A (zh) * | 2023-04-28 | 2025-07-22 | 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 |
| 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 |
| 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 |
| 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 |
| CN120289471A (zh) * | 2024-03-01 | 2025-07-11 | 浙江扬厉医药技术有限公司 | 吡喃并吡啶类化合物、其制备方法、药物组合物及应用 |
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 |
| EP1960363B1 (en) | 2005-12-09 | 2014-01-22 | Amgen, Inc. | Quinolone based compounds exhibiting prolyl hydroxylase inhibitory activity, 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 HR HRP20180592TT patent/HRP20180592T1/hr unknown
- 2012-09-20 JP JP2014531214A patent/JP6012737B2/ja active Active
- 2012-09-20 PL PL12766628T patent/PL2758388T3/pl unknown
- 2012-09-20 MX MX2014002624A patent/MX366095B/es active IP Right Grant
- 2012-09-20 KR KR1020147010662A patent/KR101723276B1/ko active Active
- 2012-09-20 RS RS20180446A patent/RS57139B1/sr unknown
- 2012-09-20 CN CN201280045785.3A patent/CN103827101B/zh active Active
- 2012-09-20 PE PE2018001330A patent/PE20181378A1/es unknown
- 2012-09-20 SG SG2014010599A patent/SG2014010599A/en unknown
- 2012-09-20 WO PCT/EP2012/068472 patent/WO2013041591A1/en active Application Filing
- 2012-09-20 ES ES12766628.7T patent/ES2666802T3/es active Active
- 2012-09-20 LT LTEP12766628.7T patent/LT2758388T/lt unknown
- 2012-09-20 AU AU2012311582A patent/AU2012311582B2/en active Active
- 2012-09-20 HU HUE12766628A patent/HUE038773T2/hu unknown
- 2012-09-20 EA EA201490567A patent/EA035108B1/ru not_active IP Right Cessation
- 2012-09-20 MY MYPI2014700679A patent/MY186165A/en unknown
- 2012-09-20 SI SI201231277T patent/SI2758388T1/en 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 EP EP12766628.7A patent/EP2758388B1/en active Active
- 2012-09-20 NO NO12766628A patent/NO2758388T3/no unknown
- 2012-09-20 PT PT127666287T patent/PT2758388T/pt unknown
- 2012-09-20 DK DK12766628.7T patent/DK2758388T3/en active
- 2012-09-20 CA CA2845170A patent/CA2845170C/en active Active
- 2012-09-20 UA UAA201404207A patent/UA115972C2/uk unknown
- 2012-09-20 BR BR112014006660-4A patent/BR112014006660B1/pt active IP Right Grant
- 2012-09-21 TW TW101134790A patent/TWI576342B/zh active
- 2012-09-21 AR ARP120103485A patent/AR087984A1/es active IP Right Grant
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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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