AR087901A1 - Derivados dihidroquinolina-2-ona como inhibidores de la aldosterona sintasa y procedimiento para su obtencion - Google Patents
Derivados dihidroquinolina-2-ona como inhibidores de la aldosterona sintasa y procedimiento para su obtencionInfo
- Publication number
- AR087901A1 AR087901A1 ARP120103420A ARP120103420A AR087901A1 AR 087901 A1 AR087901 A1 AR 087901A1 AR P120103420 A ARP120103420 A AR P120103420A AR P120103420 A ARP120103420 A AR P120103420A AR 087901 A1 AR087901 A1 AR 087901A1
- Authority
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- Argentina
- Prior art keywords
- substituted
- alkyl
- cycloalkyl
- haloalkyl
- halocycloalkyl
- 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
- 125000000217 alkyl group Chemical group 0.000 abstract 34
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 27
- 125000001188 haloalkyl group Chemical group 0.000 abstract 26
- 125000005347 halocycloalkyl group Chemical group 0.000 abstract 24
- 229910052736 halogen Inorganic materials 0.000 abstract 21
- 150000002367 halogens Chemical class 0.000 abstract 21
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 16
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 11
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 10
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 10
- 229910052757 nitrogen Inorganic materials 0.000 abstract 10
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 9
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 9
- -1 amino, amino Chemical group 0.000 abstract 8
- 125000004432 carbon atom Chemical group C* 0.000 abstract 8
- 125000001072 heteroaryl group Chemical group 0.000 abstract 8
- 125000004994 halo alkoxy alkyl group Chemical group 0.000 abstract 7
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 abstract 6
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 6
- 125000005120 alkyl cycloalkyl alkyl group Chemical group 0.000 abstract 5
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 5
- 125000001424 substituent group Chemical group 0.000 abstract 5
- 125000003545 alkoxy group Chemical group 0.000 abstract 4
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 4
- 125000005083 alkoxyalkoxy group Chemical group 0.000 abstract 3
- 125000005081 alkoxyalkoxyalkyl group Chemical group 0.000 abstract 3
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 3
- 125000005094 alkyl carbonyl amino alkyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 3
- 125000004858 cycloalkoxyalkyl group Chemical group 0.000 abstract 3
- 125000005112 cycloalkylalkoxy group Chemical group 0.000 abstract 3
- 125000004461 halocycloalkylalkyl group Chemical group 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000004043 oxo group Chemical group O=* 0.000 abstract 3
- 125000003884 phenylalkyl group Chemical group 0.000 abstract 3
- 125000003107 substituted aryl group Chemical group 0.000 abstract 3
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000005169 cycloalkylcarbonylamino group Chemical group 0.000 abstract 2
- NFGODEMQGQNUKK-UHFFFAOYSA-M [6-(diethylamino)-9-(2-octadecoxycarbonylphenyl)xanthen-3-ylidene]-diethylazanium;chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCCCCOC(=O)C1=CC=CC=C1C1=C2C=CC(=[N+](CC)CC)C=C2OC2=CC(N(CC)CC)=CC=C21 NFGODEMQGQNUKK-UHFFFAOYSA-M 0.000 abstract 1
- 125000005197 alkyl carbonyloxy alkyl group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- 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
-
- 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
- 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
- C07D401/14—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 three or more hetero rings
-
- 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
-
- 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
-
- 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
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- 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
- C07D471/06—Peri-condensed systems
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- C07—ORGANIC CHEMISTRY
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- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/10—Spiro-condensed systems
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- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
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- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
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- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Composiciones que incluyen los compuestos, y métodos de utilización de los compuestos. Reivindicación 1: Compuestos de fórmula (1), en la que: R¹ es H, halógeno, alquilo, haloalquilo, cicloalquilo o halocicloalquilo; R² es H, halógeno, alquilo, haloalquilo, cicloalquilo o halocicloalquilo; R³ es H, halógeno, alquilo, haloalquilo, cicloalquilo o halocicloalquilo; R⁴ es H, halógeno, alquilo, haloalquilo, cicloalquilo o halocicloalquilo; o R³ y R⁴ conjuntamente con los átomos de carbono a los que se encuentran unidos forman un doble enlace; R⁵ es H, halógeno, alquilo, haloalquilo, cicloalquilo o halocicloalquilo; R⁶ es H o R⁸, en el que, en el caso de que R⁶ sea H, por lo menos uno de A¹ y A³ es N; R⁷ es H, halógeno, alquilo, haloalquilo, cicloalquilo o halocicloalquilo; o R¹ y R⁷ conjuntamente con los átomos de nitrógeno y carbono a los que se encuentran unidos forman un heterocicloalquilo sustituido con uno a tres sustituyentes seleccionados independientemente de entre H, alquilo, haloalquilo, cicloalquilo o halocicloalquilo; R⁸ es -Oₘ-(CR⁹R¹⁰)ₙ-(CR¹¹R¹²)ₚ-(CR¹³R¹⁴)q-NR¹⁵R¹⁶, -NₘR¹⁷-(CR⁹R¹⁰)ₙ-(CR¹¹R¹²)ₚ-(CR¹³R¹⁴)q-NR¹⁵R¹⁶ o -Sₘ(O)ʳ-(CR⁹R¹⁰)ₙ-(CR¹¹R¹²)ₚ-(CR¹³R¹⁴)q-NR¹⁵R¹⁶; R⁹ es H, halógeno, alquilo, haloalquilo, cicloalquilo o halocicloalquilo; R¹⁰ es H, halógeno, alquilo, haloalquilo, cicloalquilo o halocicloalquilo; R¹¹ es H, halógeno, alquilo, haloalquilo, cicloalquilo o halocicloalquilo; o R¹⁰ y R¹¹ conjuntamente con los átomos de carbono a los que se encuentran unidos forman un doble enlace; R¹² es H, halógeno, alquilo, haloalquilo, cicloalquilo o halocicloalquilo; o R¹¹ y R¹² conjuntamente con el átomo de carbono al que se encuentran unidos forman un cicloalquilo o un heterocicloalquilo; R¹³ es H, halógeno, alquilo, haloalquilo, cicloalquilo o halocicloalquilo; R¹⁴ es H, halógeno, alquilo, haloalquilo, cicloalquilo o halocicloalquilo; o R¹⁰ y R¹⁴ conjuntamente forman -(CH₂)ₜ-; R¹⁵ es H, alquilo, haloalquilo, cicloalquilo, halocicloalquilo, alcoxialquilo, haloalcoxialquilo o hidroxialquilo; R¹⁶ es H, alquilo, haloalquilo, cicloalquilo, halocicloalquilo, hidroxialquilo, alcoxialquilo, haloalcoxialquilo, fenilalquilo, fenilalquilo sustituido, arilo, arilo sustituido, heterocicloalquilo, heterocicloalquilo sustituido, heteroarilo, heteroarilo sustituido, -S(O)₂R¹⁸, -S(O)₂OR¹⁸, -S(O)₂NR¹⁸R¹⁹, -C(O)R¹⁸, -C(O)OR¹⁸ o -C(O)NR¹⁸R¹⁹, en la que fenilalquilo sustituido, arilo sustituido, heterocicloalquilo sustituido y heteroarilo sustituido se sustituyen con uno a tres sustituyentes seleccionados independientemente de entre alquilo, hidroxialquilo, haloalquilo, cicloalquilo, alquilcicloalquilo, halocicloalquilo, alquilcicloalquilalquilo, halocicloalquilalquilo, cicloalquilalquilo, cicloalquilalcoxi, cicloalcoxi, cicloalcoxialquilo, cicloalquilalcoxialquilo, alcoxi, alcoxialquilo, haloalcoxi, haloalcoxialquilo, alcoxialcoxi, alcoxialcoxialquilo, alcoxicarbonilo, halógeno, hidroxi, oxo, ciano, triazolilalquilo, tetrazolilalquilo, amino, amino sustituido, aminoalquilo, aminoalquilo sustituido, aminocarbonilo, aminocarbonilo sustituido, alquilcarbonilamino, cicloalquilcarbonilamino, alquilcarbonilaminoalquilo y cicloalquilcarbonilaminoalquilo, en la que amino sustituido, aminoalquilo sustituido y aminocarbonilo sustituido se sustituyen en el átomo de nitrógeno con uno a dos sustituyentes seleccionados independientemente de entre alquilo, cicloalquilo, alquilcicloalquilo, cicloalquilalquilo, alquilcicloalquilalquilo, hidroxialquilo y alcoxialquilo, en la que, en el caso de que R¹⁵ sea H o alquilo y R¹⁶ sea H o alquilo, la suma de n, p y q es de por lo menos 1; o R¹⁵ y R¹⁶ conjuntamente con el átomo de nitrógeno al que se encuentran unidos forman un heterocicloalquilo sustituido o un heteroarilo sustituido, en la que el heterocicloalquilo sustituido y el heteroarilo sustituido se sustituyen con R²³, R²⁴ y R²⁵; o R¹³ y R¹⁵ conjuntamente con los átomos de nitrógeno y carbono a los que se encuentran unidos forman un heterocicloalquilo sustituido, en la que el heterocicloalquilo sustituido se sustituye con R²³, R²⁴ y R²⁵; o R¹¹ y R¹⁵ conjuntamente con los átomos de nitrógeno y carbono a los que se encuentran unidos forman un heterocicloalquilo sustituido, en la que el heterocicloalquilo sustituido se sustituye con R²³, R²⁴ y R²⁵; o R⁹ y R¹⁵ conjuntamente con los átomos de nitrógeno y carbono a los que se encuentran unidos forman un heterocicloalquilo sustituido, en la que el heterocicloalquilo sustituido se sustituye con R²³, R²⁴ y R²⁵; R¹⁷ es H, halógeno, alquilo, haloalquilo, cicloalquilo o halocicloalquilo; R¹⁸ es alquilo, cicloalquilo, haloalquilo, halocicloalquilo, hidroxialquilo, halohidroxialquilo, alcoxialquilo, haloalcoxialquilo, alquilcarboniloxialquilo, arilo, arilo sustituido, heterocicloalquilo, heterocicloalquilo sustituido, heteroarilo, heteroarilo sustituido, en la que arilo sustituido, heterocicloalquilo sustituido y heteroarilo sustituido se sustituyen con uno a tres sustituyentes seleccionados independientemente de entre alquilo, hidroxialquilo, haloalquilo, cicloalquilo, alquilcicloalquilo, halocicloalquilo, alquilcicloalquilalquilo, halocicloalquilalquilo, cicloalquilalquilo, cicloalquilalcoxi, cicloalcoxi, cicloalcoxialquilo, cicloalquilalcoxialquilo, alcoxi, alcoxialquilo, haloalcoxi, haloalcoxialquilo, alcoxialcoxi, alcoxialcoxialquilo, alcoxicarbonilo, halógeno, hidroxi, oxo, ciano, triazolilalquilo, tetrazolilalquilo, amino, amino sustituido, aminoalquilo, aminoalquilo sustituido, aminocarbonilo, aminocarbonilo sustituido, alquilocarbonilamino, cicloalquilcarbonilamino, alquilcarbonilaminoalquilo y cicloalquilcarbonilaminoalquilo, en la que amino sustituido, aminoalquilo sustituido y aminocarbonilo sustituido se sustituyen en el átomo de nitrógeno con uno a dos sustituyentes seleccionados independientemente de entre alquilo, cicloalquilo, alquilcicloalquilo, cicloalquilalquilo, alquilocicloalquilalquilo, hidroxialquilo y alcoxialquilo; R¹⁹ es H, halógeno, alquilo, haloalquilo, cicloalquilo o halocicloalquilo; A¹ es CR²⁰ o N; A² es CR²¹ o N; A³ es CR²² o N; R²⁰ es H, halógeno, alquilo, haloalquilo, cicloalquilo o halocicloalquilo; R²¹ es H, halógeno, alquilo, haloalquilo, cicloalquilo o halocicloalquilo; R²² es H, halógeno, alquilo, haloalquilo, cicloalquilo o halocicloalquilo; R²³, R²⁴ y R²⁵ se seleccionan, cada uno independientemente, de entre H, alquilo, hidroxialquilo, haloalquilo, cicloalquilo, alquilcicloalquilo, halocicloalquilo, alquilcicloalquilalquilo, halocicloalquilalquilo, cicloalquilalquilo, cicloalquilalcoxi, cicloalcoxi, cicloalcoxialquilo, cicloalquilalcoxialquilo, alcoxi, alcoxialquilo, haloalcoxi, haloalcoxialquilo, alcoxialcoxi, alcoxialcoxialquilo, alcoxicarbonilo, -S(O)₂R¹⁸, -C(O)R¹⁸, halógeno, hidroxi, oxo, ciano, triazolilalquilo, tetrazolilalquilo, amino, amino sustituido, aminoalquilo, aminoalquilo sustituido, aminocarbonilo, aminocarbonilo sustituido, alquilcarbonilamino, cicloalquilcarbonilamino, alquilcarbonilaminoalquilo y cicloalquilcarbonilaminoalquilo, en la que amino sustituido, aminoalquilo sustituido y aminocarbonilo sustituido se sustituyen en el átomo de nitrógeno con uno a dos sustituyentes seleccionados independientemente de entre alquilo, cicloalquilo, alquilcicloalquilo, cicloalquilalquilo, alquilcicloalquilalquilo, hidroxialquilo y alcoxialquilo; en la que, en el caso de que m sea 0 y R⁹ y R¹⁵, o R¹¹ y R¹⁵ o R¹³ y R¹⁵ o R¹⁵ y R¹⁶ conjuntamente con los átomos de nitrógeno y carbono a los que se encuentran unidos formen un heterocicloalquilo sustituido o un heteroarilo sustituido, por lo menos uno de R²³, R²⁴, R²⁵ y R¹⁶ es diferente de H, alquilo, haloalquilo, alcoxi, haloalcoxi, halógeno, hidroxi, ciano, amino, amino sustituido, aminocarbonilo, aminocarbonilo sustituido, en la que amino sustituido y aminocarbonilo sustituido se sustituyen en el átomo de nitrógeno con uno a dos alquilos y -C(O)R¹⁸, -S(O)₂R¹⁸, en la que R¹⁸ es alquilo, haloalquilo, hidroxialquilo, halohidroxialquilo, alcoxialquilo o haloalcoxialquilo; m es 0 ó 1 en el que, en el caso de que m sea 1, la suma de n y p es 2, 3 ó 4; n es 0, 1 ó 2; p es 0, 1 ó 2; q es 0, 1 ó 2; r es 0, 1 ó 2, en el que, en el caso de que m sea 0, r es 0; t es 0, 1 ó 2; o sales o esteres farmacéuticamente aceptables.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2011079673 | 2011-09-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR087901A1 true AR087901A1 (es) | 2014-04-23 |
Family
ID=46829775
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120103420A AR087901A1 (es) | 2011-09-15 | 2012-09-17 | Derivados dihidroquinolina-2-ona como inhibidores de la aldosterona sintasa y procedimiento para su obtencion |
Country Status (33)
| Country | Link |
|---|---|
| US (1) | US9260408B2 (es) |
| EP (2) | EP2755963B1 (es) |
| JP (1) | JP6012735B2 (es) |
| KR (1) | KR101785143B1 (es) |
| CN (1) | CN103814021B (es) |
| AR (1) | AR087901A1 (es) |
| AU (1) | AU2012307509B2 (es) |
| BR (1) | BR112014006283B1 (es) |
| CA (1) | CA2846785C (es) |
| CL (1) | CL2014000604A1 (es) |
| CO (1) | CO6890099A2 (es) |
| CR (1) | CR20140091A (es) |
| DK (1) | DK2755963T3 (es) |
| EA (1) | EA035757B1 (es) |
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| CA2897417A1 (en) * | 2013-03-08 | 2014-09-12 | F. Hoffmann-La Roche Ag | New dihydroquinoline-2-one derivatives as aldosterone synthase (cyp11b2 or cyp11b1) inhibitors |
| US9682983B2 (en) | 2013-03-14 | 2017-06-20 | The Brigham And Women's Hospital, Inc. | BMP inhibitors and methods of use thereof |
| KR20150119207A (ko) | 2013-03-14 | 2015-10-23 | 에프. 호프만-라 로슈 아게 | 알도스테론 신타제 억제제로서 사용하기 위한 다이하이드로퀴놀린-2-온 유도체 |
| CN105073732B (zh) * | 2013-03-14 | 2017-07-21 | 豪夫迈·罗氏有限公司 | 用作醛固酮合酶抑制剂的二氢喹啉‑2‑酮衍生物 |
| WO2014179186A1 (en) * | 2013-04-30 | 2014-11-06 | Boehringer Ingelheim International Gmbh | Aldosterone synthase inhibitors |
| JP6581970B2 (ja) * | 2013-05-27 | 2019-09-25 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | 新規３，４−ジヒドロ−２ｈ−イソキノリン−１−オン及び２，３−ジヒドロ−イソインドール−１−オン化合物 |
| WO2014191340A1 (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 |
| CN105143205B (zh) * | 2013-05-27 | 2018-02-02 | 豪夫迈·罗氏有限公司 | 新的3,4‑二氢‑2h‑异喹啉‑1‑酮和2,3‑二氢‑异吲哚‑1‑酮化合物 |
| CN105143204B (zh) * | 2013-05-27 | 2018-02-02 | 豪夫迈·罗氏有限公司 | 3,4‑二氢‑2h‑异喹啉‑1‑酮和2,3‑二氢‑异吲哚‑1‑酮化合物 |
| WO2015125858A1 (ja) * | 2014-02-24 | 2015-08-27 | 日本曹達株式会社 | ヘテロアリール化合物およびその用途 |
| US20170190705A1 (en) * | 2014-03-26 | 2017-07-06 | The Brigham And Woman's Hospital, Inc. | Compositions and Methods for Inhibiting BMP |
| MY176401A (en) | 2014-04-24 | 2020-08-05 | Mitsubishi Tanabe Pharma Corp | Novel disubstituted 1,2,4-triazine compound |
| US10513521B2 (en) | 2014-07-15 | 2019-12-24 | The Brigham And Women's Hospital, Inc. | Compositions and methods for inhibiting BMP |
| CR20170118A (es) * | 2014-10-08 | 2017-07-10 | Hoffmann La Roche | Derivados espirodiamina como inhibidores de la aldosterona sintasa |
| 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 |
| EP3212638B1 (en) * | 2014-10-31 | 2019-11-20 | 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 |
| MY199607A (en) | 2015-08-31 | 2023-11-09 | Dong A Socio Holdings Co Ltd | Heteroaryl compounds and their use as therapeutic drugs |
| JP6314196B2 (ja) * | 2015-10-22 | 2018-04-18 | 田辺三菱製薬株式会社 | 医薬組成物 |
| US10717731B2 (en) | 2015-10-23 | 2020-07-21 | Mitsubishi Tanabe Pharma Corporation | Nitrogen-containing aromatic heterocyclic compound |
| EP3523292B1 (en) * | 2016-10-10 | 2021-12-15 | Dong-A Socio Holdings Co., Ltd. | Heteroaryl compounds and their use as mer inhibitors |
| KR102564643B1 (ko) * | 2016-12-08 | 2023-08-08 | 에프. 호프만-라 로슈 아게 | Gaba a 알파5 pam으로서 신규한 이소옥사졸릴 에터 유도체 |
| WO2020223267A1 (en) | 2019-05-01 | 2020-11-05 | Boehringer Ingelheim International Gmbh | (r)-(2-methyloxiran-2-yl)methyl 4-bromobenzenesulfonate |
| WO2023063851A1 (en) * | 2021-10-13 | 2023-04-20 | «Target Medicals» Limited Liability Company | Inhibitors of human aldosterone synthase (cyp11b2) |
| KR20240122521A (ko) | 2021-12-14 | 2024-08-12 | 베링거 인겔하임 인터내셔날 게엠베하 | 만성 신장 질환 치료용 알도스테론 신타아제 억제제 |
| EP4615843A1 (en) * | 2022-11-10 | 2025-09-17 | «Target Medicals» Limited Liability Company | Inhibitors of human aldosterone synthase (cyp11b2) |
| JP2025540715A (ja) * | 2022-11-23 | 2025-12-16 | 上▲海▼翰森生物医▲薬▼科技有限公司 | ピリジン多環系化合物阻害剤、及びその製造方法と使用 |
| 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 |
| CN120530098A (zh) * | 2023-12-22 | 2025-08-22 | 上海翊石医药科技有限公司 | 一类芳杂环化合物及其制备方法和应用 |
| CN120289471B (zh) * | 2024-03-01 | 2025-10-17 | 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 |
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| US4710507A (en) * | 1983-12-22 | 1987-12-01 | Pfizer Inc. | Quinolone inotropic agents |
| GB8334282D0 (en) * | 1983-12-22 | 1984-02-01 | Pfizer Ltd | Quinolone inotropic agents |
| CN85100796A (zh) * | 1985-04-01 | 1986-10-01 | 辉瑞公司 | 喹啉酮衍生物的制备方法 |
| FR2580646A1 (fr) * | 1985-04-19 | 1986-10-24 | Synthelabo | Derives de 2(1h)-quinolinone, leur preparation et leur application en therapeutique |
| US20080176830A1 (en) | 2005-04-14 | 2008-07-24 | Adams Nicholas D | Compounds, Compositions, and Methods |
| DE102008022221A1 (de) | 2008-05-06 | 2009-11-12 | Universität des Saarlandes | Inhibitoren der humanen Aldosteronsynthase CYP11B2 |
| ES2430088T3 (es) | 2009-05-15 | 2013-11-18 | Novartis Ag | Derivados de benzoxazolona como inhibidores de aldosterona sintasa |
| MY184008A (en) | 2009-05-15 | 2021-03-17 | Novartis Ag | Aryl pyridine as aldosterone synthase inhibitors |
| US8541404B2 (en) * | 2009-11-09 | 2013-09-24 | Elexopharm Gmbh | Inhibitors of the human aldosterone synthase CYP11B2 |
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