PE20212111A1 - Moduladores calpaina y usos terapeuticos de los mismos - Google Patents
Moduladores calpaina y usos terapeuticos de los mismosInfo
- Publication number
- PE20212111A1 PE20212111A1 PE2020001468A PE2020001468A PE20212111A1 PE 20212111 A1 PE20212111 A1 PE 20212111A1 PE 2020001468 A PE2020001468 A PE 2020001468A PE 2020001468 A PE2020001468 A PE 2020001468A PE 20212111 A1 PE20212111 A1 PE 20212111A1
- Authority
- PE
- Peru
- Prior art keywords
- optionally substituted
- group
- membered heteroaryl
- aryl
- membered
- Prior art date
Links
- 108010032088 Calpain Proteins 0.000 title abstract 3
- 102000007590 Calpain Human genes 0.000 title abstract 3
- 230000001225 therapeutic effect Effects 0.000 title 1
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 abstract 5
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 abstract 2
- 102100025172 Calpain-1 catalytic subunit Human genes 0.000 abstract 1
- 102100032537 Calpain-2 catalytic subunit Human genes 0.000 abstract 1
- 102100030003 Calpain-9 Human genes 0.000 abstract 1
- 102100035037 Calpastatin Human genes 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 101000934069 Homo sapiens Calpain-1 catalytic subunit Proteins 0.000 abstract 1
- 101000867692 Homo sapiens Calpain-2 catalytic subunit Proteins 0.000 abstract 1
- 101000793680 Homo sapiens Calpain-9 Proteins 0.000 abstract 1
- -1 alpha-ketoamide compounds Chemical class 0.000 abstract 1
- 108010044208 calpastatin Proteins 0.000 abstract 1
- ZXJCOYBPXOBJMU-HSQGJUDPSA-N calpastatin peptide Ac 184-210 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H](CCSC)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CC(O)=O)NC(C)=O)[C@@H](C)O)C1=CC=C(O)C=C1 ZXJCOYBPXOBJMU-HSQGJUDPSA-N 0.000 abstract 1
- 125000004452 carbocyclyl group Chemical group 0.000 abstract 1
- 230000009137 competitive binding Effects 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000003176 fibrotic effect Effects 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
- C07D285/10—1,2,5-Thiadiazoles; Hydrogenated 1,2,5-thiadiazoles
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- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
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- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
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- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or 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
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- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
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- C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or 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
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- C07D295/027—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 containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring
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- 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
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- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
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- 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
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- Public Health (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Referido a compuestos de formula I, en donde A1 se selecciona del grupo que consiste de heterociclilo de 5-10 miembros opcionalmente sustituido; heteroarilo de 5-, 8- o 9- miembros opcionalmente sustituido; y C3-10 carbociclilo opcionalmente sustituido; A2 se selecciona del grupo que consiste de heterociclilo de 3-10 miembros opcionalmente sustituido, C6-10 arilo opcionalmente sustituido, entre otros; A4 se selecciona del grupo que consiste de C6-10 arilo opcionalmente sustituido, heteroarilo de 5-10 miembros opcionalmente sustituido, entre otros; A3 se selecciona del grupo que consiste de C6-10arilo opcionalmente sustituido, heteroarilo de 5-10 miembros opcionalmente sustituido, entre otros; A5 se selecciona del grupo que consiste de heterociclilo de 3-10 miembros opcionalmente sustituido, C6-10 arilo opcionalmente sustituido, heteroarilo de 5-10 miembros opcionalmente sustituido, entre otros; A6 se selecciona del grupo que consiste de C6-10 arilo opcionalmente sustituido, heteroarilo de 5-10 miembros opcionalmente sustituido, entre otros; A7 se selecciona del grupo que consiste de C6-10 arilo opcionalmente sustituido, heteroarilo de 5-10 miembros opcionalmente sustituido, entre otros; A8 es un miembro de anillo de A1 y se selecciona del grupo que consiste de C y N; R2 se selecciona independientemente de -H, C1-4 alquilo opcionalmente sustituido, C1-8alcoxialquilo opcionalmente sustituido, entre otros; R6 se selecciona independientemente de -H y C1-4alquilo opcionalmente sustituido; y cada n se selecciona independientemente para que sea un numero entero de 0 a 3; o una sal farmaceuticamente aceptable de los mismos. Estos compuestos alfa-cetoamidas no macrociclicas actuan como moduladores calpaina, inhiben la calpaina o la union competitiva con calpastatina al ponerlos en contacto con enzimas como CAPN1, CAPN2 y/o CAPN9. Tambien se refiere a una composicion farmaceutica y a metodos de tratamiento de una enfermedad fibrotica o condicion secundaria.
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US201862649451P | 2018-03-28 | 2018-03-28 | |
PCT/US2019/023457 WO2019190885A1 (en) | 2018-03-28 | 2019-03-21 | Calpain modulators and therapeutic uses thereof |
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EP3481835A4 (en) | 2016-07-05 | 2020-02-26 | Blade Therapeutics, Inc. | CALPAIN MODULATORS AND THEIR THERAPEUTIC USES |
PE20191153A1 (es) * | 2016-09-28 | 2019-09-05 | Blade Therapeutics Inc | Moduladores de calpainas y usos terapeuticos de los mismos |
SG11202008773PA (en) * | 2018-03-28 | 2020-10-29 | Blade Therapeutics Inc | Method of treating fibrotic disease |
EP3820864A4 (en) * | 2018-06-28 | 2022-03-30 | Blade Therapeutics, Inc. | METHODS OF TREATMENT OF HEPATIC FIBROSIS USING CALPAIN INHIBITORS |
IL298324A (en) | 2020-06-10 | 2023-01-01 | Aligos Therapeutics Inc | Antiviral compounds for the treatment of coronavirus, picornavirus and novovirus infections |
WO2023283256A1 (en) | 2021-07-09 | 2023-01-12 | Aligos Therapeutics, Inc. | Anti-viral compounds |
WO2023043816A1 (en) | 2021-09-17 | 2023-03-23 | Aligos Therapeutics, Inc. | Anti-viral compounds for treating coronavirus, picornavirus, and norovirus infections |
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SE9102462D0 (sv) * | 1991-08-28 | 1991-08-28 | Astra Ab | New isosteric peptides |
JPH09500087A (ja) * | 1992-06-24 | 1997-01-07 | コーテックス ファーマシューティカルズ インコーポレイテッド | カルパイン活性の増大に関連した健康障害の抑制及び処置におけるカルパイン阻害剤の使用法 |
DE19642591A1 (de) * | 1996-10-15 | 1998-04-16 | Basf Ag | Neue Piperidin-Ketocarbonsäure-Derivate, deren Herstellung und Anwendung |
US6083944A (en) * | 1997-10-07 | 2000-07-04 | Cephalon, Inc. | Quinoline-containing α-ketoamide cysteine and serine protease inhibitors |
JP2002539190A (ja) * | 1999-03-15 | 2002-11-19 | アクシス・ファーマシューティカルズ・インコーポレイテッド | プロテアーゼ阻害剤としての新規化合物および組成物 |
WO2005000793A1 (ja) * | 2003-06-26 | 2005-01-06 | Taisho Pharmaceutical Co., Ltd. | 2位置換シクロアルキルカルボン酸誘導体 |
EP1493739A1 (fr) * | 2003-07-03 | 2005-01-05 | Warner-Lambert Company LLC | Dérivés thiophényliques d'aminoacides, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent |
US7964624B1 (en) * | 2005-08-26 | 2011-06-21 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases |
AR055395A1 (es) * | 2005-08-26 | 2007-08-22 | Vertex Pharma | Compuestos inhibidores de la actividad de la serina proteasa ns3-ns4a del virus de la hepatitis c |
TWI405571B (zh) * | 2006-12-29 | 2013-08-21 | Abbott Gmbh & Co Kg | 羰醯胺化合物及其作為鈣蛋白酶(calpain)抑制劑之用途 |
US9051304B2 (en) * | 2009-12-22 | 2015-06-09 | AbbVie Deutschland GmbH & Co. KG | Carboxamide compounds and their use as calpain inhibitors V |
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SG11202008773PA (en) * | 2018-03-28 | 2020-10-29 | Blade Therapeutics Inc | Method of treating fibrotic disease |
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ECSP20068210A (es) | 2020-11-30 |
KR20200139702A (ko) | 2020-12-14 |
BR112020019560A2 (pt) | 2021-01-05 |
AU2019242387A1 (en) | 2020-11-19 |
RU2020130022A (ru) | 2022-05-04 |
EP3774737A1 (en) | 2021-02-17 |
CO2020012359A2 (es) | 2020-10-30 |
MX2020010033A (es) | 2020-10-14 |
EP3774737A4 (en) | 2021-12-22 |
IL277548A (en) | 2020-11-30 |
CL2020002496A1 (es) | 2021-03-12 |
AR115303A1 (es) | 2020-12-23 |
PH12020551555A1 (en) | 2021-07-12 |
CA3095164A1 (en) | 2019-10-03 |
CN112204014A (zh) | 2021-01-08 |
WO2019190885A1 (en) | 2019-10-03 |
SG11202008750XA (en) | 2020-10-29 |
JP2021519312A (ja) | 2021-08-10 |
TW202003472A (zh) | 2020-01-16 |
US20210009564A1 (en) | 2021-01-14 |
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