AR088810A1 - Moduladores del receptor mas acoplado a la proteina g utiles en el tratamiento de trastornos cardiovasculares y composiciones farmaceuticas que los contienen - Google Patents
Moduladores del receptor mas acoplado a la proteina g utiles en el tratamiento de trastornos cardiovasculares y composiciones farmaceuticas que los contienenInfo
- Publication number
- AR088810A1 AR088810A1 ARP120104218A ARP120104218A AR088810A1 AR 088810 A1 AR088810 A1 AR 088810A1 AR P120104218 A ARP120104218 A AR P120104218A AR P120104218 A ARP120104218 A AR P120104218A AR 088810 A1 AR088810 A1 AR 088810A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkoxy
- heterocyclyl
- cycloalkyl
- substituents
- Prior art date
Links
- 208000024172 Cardiovascular disease Diseases 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 102000004169 proteins and genes Human genes 0.000 title 1
- 108090000623 proteins and genes Proteins 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 11
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 125000003545 alkoxy group Chemical group 0.000 abstract 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 5
- 125000001424 substituent group Chemical group 0.000 abstract 5
- -1 Cquilamino dialkyl Chemical group 0.000 abstract 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 3
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 abstract 2
- 125000002431 aminoalkoxy group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004415 heterocyclylalkyl group Chemical group 0.000 abstract 2
- 208000028867 ischemia Diseases 0.000 abstract 2
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 abstract 2
- 210000004556 brain Anatomy 0.000 abstract 1
- 125000003917 carbamoyl group Chemical class [H]N([H])C(*)=O 0.000 abstract 1
- 208000037765 diseases and disorders Diseases 0.000 abstract 1
- 125000000816 ethylene group Chemical group [H]C([H])([*:1])C([H])([H])[*:2] 0.000 abstract 1
- 210000002216 heart Anatomy 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 210000000987 immune system Anatomy 0.000 abstract 1
- 210000003734 kidney Anatomy 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 230000010410 reperfusion Effects 0.000 abstract 1
- 210000004994 reproductive system Anatomy 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
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- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
- C07D295/135—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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- C—CHEMISTRY; METALLURGY
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- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
- C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
- C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
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- C—CHEMISTRY; METALLURGY
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- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D295/145—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/15—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
- C07F9/6509—Six-membered rings
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- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
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Abstract
Que son útiles para tratar y aliviar enfermedades y trastornos del corazón, cerebro, riñón, sistema inmune y reproductivo que resultan de isquemia o reperfusión posterior a isquemia y cualquier complicación o complicaciones posteriores relacionadas con los mismos. Reivindicación 1: Un compuesto que se selecciona de compuestos de fórmula (1) y sales, solvatos e hidratos farmacéuticamente aceptables de los mismos, en donde: X es CH₂ o CH₂CH₂; o X está ausente; R⁴, R⁵, R⁶ y R⁷ se selecciona cada uno independientemente de: H y halógeno; y (A) R¹ se selecciona de: H, alquilo C₁₋₆, alquil C₁₋₆-O-alquilo C₁₋₆, cicloalquilo C₃₋₇, cicloalquil C₄₋₁₃alquilo, heteroarilo, heteroarilalquilo C₁₋₆, heterociclilo y heterociclil-alquilo C₁₋₆, cada uno opcionalmente sustituido por uno o más sustituyentes que se seleccionan de: alcoxi C₁₋₆carbonilamino, amino-alcoxi C₁₋₆, alcoxi C₁₋₆carbonilo, alquilo C₁₋₆, alquil C₁₋₆carboxamida, alquil C₁₋₆sulfinilo, amino, carboxamida, carboxilo, ciano, dialquil C₂₋₆amino, hidroxilo, hidroxi-alquilo C₁₋₆, imino, oxo, fenilo y fosfonooxi; R² se selecciona de: H y alquilo C₁₋₆, en donde dicho alquilo C₁₋₆ está opcionalmente sustituido por uno o más sustituyentes que se seleccionan de: hidroxilo y ciano; y R³ se selecciona de: H y halógeno; o (B) R¹ y R² junto con el átomo de nitrógeno al que ambos están unidos forman un grupo que se selecciona de: heteroarilo y heterociclilo, cada uno opcionalmente sustituido por uno o más sustituyentes que se seleccionan de: alcoxi C₁₋₆carbonilo, alcoxi C₁₋₆carbonilamino, alquilo C₁₋₆, alquil C₁₋₆carboxamida, alquil C₁₋₆sulfonilo, amino, cicloalquilo C₃₋₇, cicloalquil C₄₋₁₃alquilo, carboxamida, carboxilo, dialquil C₂₋₆amino, dialquil C₂₋₆carboxamida, heteroarilalquilo C₁₋₆, heterociclilo, heterociclil-alquilo C₁₋₆, hidroxilo, hidroxiheterociclilo y oxo, en donde dicho alquilo C₁₋₆ y alquil C₁₋₆carboxamida se sustituye cada uno opcionalmente por uno o más sustituyentes que se seleccionan de: carboxilo, hidroxilo y oxo; y R³ se selecciona de: H y halógeno; o (C) R¹ se selecciona de: H, alquilo C₁₋₆, alquil C₁₋₆-O-alquilo C₁₋₆, cicloalquilo C₃₋₇, cicloalquil C₄₋₁₃alquilo, heteroarilo, heteroarilalquilo C₁₋₆, heterociclilo y heterociclil-alquilo C₁₋₆, cada uno opcionalmente sustituido por uno o más sustituyentes que se seleccionan de: alcoxi C₁₋₆carbonilamino, amino-alcoxi C₁₋₆, alcoxi C₁₋₆carbonilo, alquilo C₁₋₆, alquil C₁₋₆carboxamida, alquil C₁₋₆sulfinilo, amino, carboxamida, carboxilo, ciano, dialquil C₂₋₆amino, hidroxilo, hidroxi-alquilo C₁₋₆, imino, oxo, fenilo y fosfonooxi; y R² y R³ juntos forman CH₂.
Applications Claiming Priority (2)
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| US201161557088P | 2011-11-08 | 2011-11-08 | |
| US201261718290P | 2012-10-25 | 2012-10-25 |
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| EP (1) | EP2776407A1 (es) |
| JP (1) | JP2015501788A (es) |
| KR (1) | KR20140083058A (es) |
| CN (1) | CN104105691A (es) |
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| BR (1) | BR112014011163A2 (es) |
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| SG (1) | SG11201401743RA (es) |
| TW (1) | TW201326143A (es) |
| WO (1) | WO2013070657A1 (es) |
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| CA2867577C (en) | 2012-03-20 | 2019-07-02 | Raytheon Company | Routing a data packet in a communication network |
| WO2014182688A1 (en) * | 2013-05-07 | 2014-11-13 | Arena Pharmaceuticals, Inc. | Modulators of the g protein-coupled mas receptor and the treatment of disorders related thereto |
| WO2014182673A1 (en) * | 2013-05-07 | 2014-11-13 | Arena Pharmaceuticals, Inc. | Modulators of the g protein-coupled mas receptor and the treatment of disorders related thereto |
| KR20160077213A (ko) | 2013-11-14 | 2016-07-01 | 카딜라 핼쓰캐어 리미티드 | 새로운 헤테로시클릭 화합물 |
| WO2015161011A1 (en) * | 2014-04-17 | 2015-10-22 | Merck Sharp & Dohme Corp. | Benzamide cgrp receptor antagonists |
| WO2016198691A1 (en) | 2015-06-11 | 2016-12-15 | Basilea Pharmaceutica Ag | Efflux-pump inhibitors and therapeutic uses thereof |
| WO2018026866A1 (en) * | 2016-08-03 | 2018-02-08 | Neuropore Therapies, Inc. | Lipid-substituted amino 1,2-and 1,3-diol compounds as modulators of tlr2 dimerization |
| WO2018100159A1 (en) * | 2016-12-02 | 2018-06-07 | Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. | Bacterial glutaminyl cyclases and inhibitors thereof for use in the treatment of periodontitis |
| CN110092735B (zh) * | 2018-01-31 | 2021-05-11 | 尚科生物医药(上海)有限公司 | 一种l-丙氨酸衍生物的制备方法 |
| US20220047553A1 (en) * | 2018-09-18 | 2022-02-17 | Metacrine, Inc. | Farnesoid x receptor agonists for the treatment of disease |
| GB201820450D0 (en) * | 2018-12-14 | 2019-01-30 | Z Factor Ltd | Compound and its use for the treatment of alpha1-antitryspin deficiency |
| CN110526859B (zh) * | 2019-08-07 | 2021-03-12 | 山东百诺医药股份有限公司 | 一种瑞维那新中间体及其制备方法和瑞维那新的制备方法 |
| GB202010464D0 (en) * | 2020-07-08 | 2020-08-19 | Galapagos Nv | Novel compounds and pharmaceutical compositions thereof for the treatment of diseases |
| CN116406357A (zh) * | 2020-09-25 | 2023-07-07 | 伊赛恩特制药公司 | Mas相关g蛋白受体x2的调节剂及相关产物和方法 |
| KR20230092958A (ko) * | 2020-10-21 | 2023-06-26 | 에시언트 파마슈티컬스 인코포레이티드 | Mas-관련 G-단백질 수용체 X2의 조절제 및 관련 생성물 및 이의 용도 |
| CN114984220B (zh) * | 2022-05-12 | 2023-06-02 | 上海市同济医院 | Mas受体抑制剂在制备预防和治疗急性肝衰竭药物中的应用 |
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| US6270766B1 (en) | 1992-10-08 | 2001-08-07 | The Kennedy Institute Of Rheumatology | Anti-TNF antibodies and methotrexate in the treatment of arthritis and crohn's disease |
| JP2002179651A (ja) * | 1998-06-19 | 2002-06-26 | Wakamoto Pharmaceut Co Ltd | ベンズアニリド誘導体及び医薬組成物 |
| US20070254903A1 (en) | 2003-12-23 | 2007-11-01 | Arena Pharmaceuticals, Inc. | Novel Spiroindoline or Spiroisoquinoline Compounds, Methods of Use and Compositions Thereof |
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2012
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- 2012-11-07 US US14/356,792 patent/US20140309192A1/en not_active Abandoned
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- 2012-11-07 JP JP2014540204A patent/JP2015501788A/ja active Pending
- 2012-11-07 CA CA2853833A patent/CA2853833A1/en not_active Abandoned
- 2012-11-07 MX MX2014005638A patent/MX2014005638A/es not_active Application Discontinuation
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2014
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Also Published As
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| JP2015501788A (ja) | 2015-01-19 |
| DOP2014000096A (es) | 2014-07-15 |
| KR20140083058A (ko) | 2014-07-03 |
| BR112014011163A2 (pt) | 2017-05-09 |
| PH12014500888A1 (en) | 2014-06-09 |
| TW201326143A (zh) | 2013-07-01 |
| CN104105691A (zh) | 2014-10-15 |
| SG11201401743RA (en) | 2014-05-29 |
| WO2013070657A1 (en) | 2013-05-16 |
| MX2014005638A (es) | 2014-11-25 |
| US20140309192A1 (en) | 2014-10-16 |
| EA201490941A1 (ru) | 2014-10-30 |
| IL232334A0 (en) | 2014-06-30 |
| EP2776407A1 (en) | 2014-09-17 |
| CA2853833A1 (en) | 2013-05-16 |
| AU2012335978A1 (en) | 2014-05-22 |
| CO6970607A2 (es) | 2014-06-13 |
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