AR102266A1 - Inhibidores de aldosterona sintasa - Google Patents
Inhibidores de aldosterona sintasaInfo
- Publication number
- AR102266A1 AR102266A1 ARP150103319A ARP150103319A AR102266A1 AR 102266 A1 AR102266 A1 AR 102266A1 AR P150103319 A ARP150103319 A AR P150103319A AR P150103319 A ARP150103319 A AR P150103319A AR 102266 A1 AR102266 A1 AR 102266A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- heterocyclyl
- groups
- sintasa
- Prior art date
Links
- PQSUYGKTWSAVDQ-ZVIOFETBSA-N Aldosterone Chemical compound C([C@@]1([C@@H](C(=O)CO)CC[C@H]1[C@@H]1CC2)C=O)[C@H](O)[C@@H]1[C@]1(C)C2=CC(=O)CC1 PQSUYGKTWSAVDQ-ZVIOFETBSA-N 0.000 title 1
- PQSUYGKTWSAVDQ-UHFFFAOYSA-N Aldosterone Natural products C1CC2C3CCC(C(=O)CO)C3(C=O)CC(O)C2C2(C)C1=CC(=O)CC2 PQSUYGKTWSAVDQ-UHFFFAOYSA-N 0.000 title 1
- 229960002478 aldosterone Drugs 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 9
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 abstract 1
- MESFXNGUDNODTJ-UHFFFAOYSA-N 2h-thiazine 1,1-dioxide Chemical compound O=S1(=O)NC=CC=C1 MESFXNGUDNODTJ-UHFFFAOYSA-N 0.000 abstract 1
- 229910006074 SO2NH2 Inorganic materials 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000002393 azetidinyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 abstract 1
- 125000002757 morpholinyl group Chemical group 0.000 abstract 1
- 125000000160 oxazolidinyl group Chemical group 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 abstract 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4433—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- 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
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- A61P5/40—Mineralocorticosteroids, e.g. aldosterone; Drugs increasing or potentiating the activity of mineralocorticosteroids
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/54—Improvements relating to the production of bulk chemicals using solvents, e.g. supercritical solvents or ionic liquids
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Emergency Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Reivindicación 1: Un compuesto, caracterizado porque tiene la fórmula (1) en donde: R¹ se selecciona de -C(O)NH₂, -C(O)NH(CH₃) y -CN; R² es -(X)-R⁴, en donde -(X)- es un enlace, -CH₂- u -O-; y R⁴ se selecciona de H; alquilo C₁₋₃, opcionalmente sustituido con uno a cuatro grupos seleccionados de -F y -OH; halógeno; -CN; -SO₂-alquilo C₁₋₃; -C(O)N(alquil C₁₋₃)₂, siempre que -(X)- no sea -O-; -NHC(O)R⁵ o -N(CH₃)C(O)R⁵, siempre que -(X)- sea -CH₂- y en donde R⁵ se selecciona de cicloalquilo C₃₋₆ y alquilo C₁₋₃, opcionalmente sustituido con uno a tres grupos -F; -NHSO₂-alquilo C₁₋₃; -CH(ciclopropil)NHSO₂-alquilo C₁₋₃; -OCH₂C(O)N(alquilo C₁₋₃)₂, siempre que -(X)- sea -CH₂-; -S(=O)(=NH)CH₃, siempre que -(X)- sea -CH₂-; heterociclilo seleccionado de tetrahidropiranilo, tetrahidrofuranilo, pirrolidinilo, 1,1-dioxo[1,2]-tiazina, morfolinilo, oxazolidinilo, piperidinilo, azetidinilo, en donde dicho heterociclilo está opcionalmente sustituido con uno a tres grupos seleccionados de -C(O)alquilo C₁₋₃, halógeno, -OH, oxo y alquilo C₁₋₃; -C(O)-heterociclilo, siempre que -(X)- sea -CH₂, en donde dicho heterociclilo se selecciona de morfolin-4-ilo, pirrolidin-1-ilo y piperidin-1-ilo, opcionalmente sustituido con uno o dos grupos seleccionados de -F y -OH; cicloalquilo C₃₋₆ opcionalmente sustituido con -CN u -OH; y fenilo, opcionalmente sustituido con -SO₂NH₂; y R³ es H o alquilo C₁₋₃ opcionalmente sustituido con -OH; o R² y R³ forman juntos un anillo cicloalquilo fusionado de cinco miembros opcionalmente sustituido con -OH; o una de sus sales o estereoisómeros.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462064234P | 2014-10-15 | 2014-10-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR102266A1 true AR102266A1 (es) | 2017-02-15 |
Family
ID=54352516
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP150103319A AR102266A1 (es) | 2014-10-15 | 2015-10-14 | Inhibidores de aldosterona sintasa |
Country Status (33)
| Country | Link |
|---|---|
| US (1) | US9745289B2 (es) |
| EP (1) | EP3207039B1 (es) |
| JP (1) | JP6279812B2 (es) |
| KR (1) | KR102441634B1 (es) |
| CN (1) | CN107108587B (es) |
| AP (1) | AP2017009829A0 (es) |
| AR (1) | AR102266A1 (es) |
| AU (1) | AU2015333611B2 (es) |
| CA (1) | CA2964754C (es) |
| CL (1) | CL2017000827A1 (es) |
| CO (1) | CO2017003305A2 (es) |
| CY (1) | CY1121650T1 (es) |
| DK (1) | DK3207039T3 (es) |
| EA (1) | EA031766B1 (es) |
| ES (1) | ES2724555T3 (es) |
| HR (1) | HRP20190896T1 (es) |
| HU (1) | HUE043783T2 (es) |
| IL (1) | IL251200B (es) |
| LT (1) | LT3207039T (es) |
| ME (1) | ME03381B (es) |
| MX (1) | MX369025B (es) |
| NZ (1) | NZ729688A (es) |
| PE (1) | PE20170696A1 (es) |
| PH (1) | PH12017500595A1 (es) |
| PL (1) | PL3207039T3 (es) |
| PT (1) | PT3207039T (es) |
| RS (1) | RS58651B1 (es) |
| SG (1) | SG11201701850UA (es) |
| SI (1) | SI3207039T1 (es) |
| TR (1) | TR201907755T4 (es) |
| TW (1) | TWI731842B (es) |
| UA (1) | UA118717C2 (es) |
| WO (1) | WO2016061161A1 (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| WO2020223267A1 (en) | 2019-05-01 | 2020-11-05 | Boehringer Ingelheim International Gmbh | (r)-(2-methyloxiran-2-yl)methyl 4-bromobenzenesulfonate |
| EP4211171A2 (en) | 2020-09-10 | 2023-07-19 | Precirix N.V. | Antibody fragment against fap |
| CA3236890A1 (en) | 2021-12-14 | 2023-06-22 | Boehringer Ingelheim International Gmbh | Aldosterone synthase inhibitors for treating chronic kidney disease |
| WO2023203135A1 (en) | 2022-04-22 | 2023-10-26 | Precirix N.V. | Improved radiolabelled antibody |
| WO2023213801A1 (en) | 2022-05-02 | 2023-11-09 | Precirix N.V. | Pre-targeting |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR073629A1 (es) * | 2008-10-07 | 2010-11-17 | Schering Corp | Analogos de benzodioxano moduladores de receptores adrenergicos alfa 2c, composiciones farmaceuticas que los contienen y uso de los mismos para tratar enfermedades respiratorias, alergicas, cardiacas, parkinson y/o alzheimer, entre otras |
| BRPI1010600A2 (pt) * | 2009-05-15 | 2016-03-15 | Novartis Ag | aril piridina como inibidores de aldosterona sintase |
| BR112014013136B1 (pt) * | 2011-11-30 | 2020-05-26 | F. Hoffmann-La Roche Ag | Novos derivados de dihidroisoquinolina-1-ona biciclicos |
| JP6496246B2 (ja) * | 2012-10-05 | 2019-04-03 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | アルドステロンシンターゼインヒビター関連用途としてのインドリン化合物 |
| CN104994848A (zh) | 2013-02-22 | 2015-10-21 | 默沙东公司 | 抗糖尿病二环化合物 |
| EP2991985B1 (en) * | 2013-04-30 | 2018-06-13 | Boehringer Ingelheim International GmbH | Aldosterone synthase inhibitors |
| ES2684050T3 (es) * | 2014-07-24 | 2018-10-01 | Boehringer Ingelheim International Gmbh | Inhibidores de aldosterona sintasa |
-
2015
- 2015-10-14 KR KR1020177012975A patent/KR102441634B1/ko active IP Right Grant
- 2015-10-14 DK DK15785014.0T patent/DK3207039T3/en active
- 2015-10-14 CA CA2964754A patent/CA2964754C/en active Active
- 2015-10-14 AU AU2015333611A patent/AU2015333611B2/en active Active
- 2015-10-14 TW TW104133758A patent/TWI731842B/zh active
- 2015-10-14 WO PCT/US2015/055421 patent/WO2016061161A1/en active Application Filing
- 2015-10-14 EA EA201790830A patent/EA031766B1/ru not_active IP Right Cessation
- 2015-10-14 AP AP2017009829A patent/AP2017009829A0/en unknown
- 2015-10-14 SI SI201530696T patent/SI3207039T1/sl unknown
- 2015-10-14 AR ARP150103319A patent/AR102266A1/es unknown
- 2015-10-14 SG SG11201701850UA patent/SG11201701850UA/en unknown
- 2015-10-14 UA UAA201704599A patent/UA118717C2/uk unknown
- 2015-10-14 PT PT15785014T patent/PT3207039T/pt unknown
- 2015-10-14 HU HUE15785014A patent/HUE043783T2/hu unknown
- 2015-10-14 ES ES15785014T patent/ES2724555T3/es active Active
- 2015-10-14 NZ NZ729688A patent/NZ729688A/en unknown
- 2015-10-14 TR TR2019/07755T patent/TR201907755T4/tr unknown
- 2015-10-14 EP EP15785014.0A patent/EP3207039B1/en active Active
- 2015-10-14 CN CN201580053796.XA patent/CN107108587B/zh active Active
- 2015-10-14 JP JP2017520427A patent/JP6279812B2/ja active Active
- 2015-10-14 PE PE2017000710A patent/PE20170696A1/es unknown
- 2015-10-14 PL PL15785014T patent/PL3207039T3/pl unknown
- 2015-10-14 LT LTEP15785014.0T patent/LT3207039T/lt unknown
- 2015-10-14 RS RS20190501A patent/RS58651B1/sr unknown
- 2015-10-14 US US14/882,486 patent/US9745289B2/en active Active
- 2015-10-14 MX MX2017004852A patent/MX369025B/es active IP Right Grant
- 2015-10-14 ME MEP-2019-121A patent/ME03381B/me unknown
-
2017
- 2017-03-15 IL IL251200A patent/IL251200B/en active IP Right Grant
- 2017-03-31 PH PH12017500595A patent/PH12017500595A1/en unknown
- 2017-04-05 CL CL2017000827A patent/CL2017000827A1/es unknown
- 2017-04-05 CO CONC2017/0003305A patent/CO2017003305A2/es unknown
-
2019
- 2019-05-14 HR HRP20190896TT patent/HRP20190896T1/hr unknown
- 2019-05-24 CY CY20191100554T patent/CY1121650T1/el unknown
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