AR121744A1 - MODULADORES DE a 1-ANTITRIPSINA - Google Patents
MODULADORES DE a 1-ANTITRIPSINAInfo
- Publication number
- AR121744A1 AR121744A1 ARP210100864A ARP210100864A AR121744A1 AR 121744 A1 AR121744 A1 AR 121744A1 AR P210100864 A ARP210100864 A AR P210100864A AR P210100864 A ARP210100864 A AR P210100864A AR 121744 A1 AR121744 A1 AR 121744A1
- Authority
- AR
- Argentina
- Prior art keywords
- groups
- alkyl
- membered
- hydroxy
- substituted
- Prior art date
Links
- 239000002753 trypsin inhibitor Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 6
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 208000006682 alpha 1-Antitrypsin Deficiency Diseases 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000002843 carboxylic acid group Chemical group 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
- C07H17/02—Heterocyclic radicals containing only nitrogen as ring hetero atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- 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
- A61P11/10—Expectorants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/02—Local antiseptics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07D471/12—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 three hetero rings
- C07D471/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Gastroenterology & Hepatology (AREA)
- Dermatology (AREA)
- Nutrition Science (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Saccharide Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Compuestos y composiciones novedosos, y métodos novedosos para usarlos y prepararlos, que pueden ser útiles para tratar la deficiencia de a-1 antitripsina (AATD). Reivindicación 1: Un compuesto de la fórmula (1), un tautómero de este, un derivado deuterado de ese compuesto o tautómero, o una sal farmacéuticamente aceptable de cualquiera de los anteriores, caracterizado porque: Z¹ se selecciona de entre CRZ y N; RZ se selecciona de entre hidrógeno y halógeno; R¹ se selecciona de entre anillos aromáticos de 5 a 6 miembros y anillos heteroaromáticos de 5 a 6 miembros, cada uno de los cuales está sustituido con 0 - 2 grupos RA; cada RA se selecciona independientemente de entre halógeno, hidroxi, alquilo C₁₋₆, alcoxi C₁₋₆, y haloalcoxi C₁₋₆; R² se selecciona de entre grupos alquilo C₁₋₆, cicloalquilo C₃₋₆ y heterociclilo de 4 a 6 miembros, cada uno de los cuales está sustituido con 0 - 1 grupos RB; cada RB se selecciona independientemente de entre grupos halógeno, hidroxi, alcoxi C₁₋₆, alquilo C₁₋₆, y ciano; R³ se selecciona de entre grupos alquilo C₁₋₆, cicloalquilo C₃₋₇, y heterociclilo de 4 a 6 miembros, cada uno de los cuales está sustituido con 0 - 3 grupos RC; cada RC se selecciona independientemente de entre RY, grupos hidroxi, alcoxi C₁₋₆, alquilo C₁₋₆, y ácido carboxílico, en donde los grupos alquilo C₁₋₆ están sustituidos con 0 - 2 grupos seleccionados independientemente de entre oxo, hidroxi y ácido carboxílico, o dos grupos RC tomados juntos forman un grupo cicloalquilo de 3 a 6 miembros; y RY es un compuesto de fórmula (2).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063004636P | 2020-04-03 | 2020-04-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR121744A1 true AR121744A1 (es) | 2022-07-06 |
Family
ID=75690656
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP210100864A AR121744A1 (es) | 2020-04-03 | 2021-04-05 | MODULADORES DE a 1-ANTITRIPSINA |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20230159580A1 (es) |
| EP (1) | EP4126877A1 (es) |
| JP (1) | JP2023520398A (es) |
| KR (1) | KR20220163429A (es) |
| CN (1) | CN115776984A (es) |
| AR (1) | AR121744A1 (es) |
| AU (1) | AU2021247282A1 (es) |
| BR (1) | BR112022019794A2 (es) |
| CA (1) | CA3179184A1 (es) |
| IL (1) | IL296750A (es) |
| MX (1) | MX2022012095A (es) |
| TW (1) | TW202204359A (es) |
| WO (1) | WO2021203010A1 (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20210089656A (ko) | 2018-10-05 | 2021-07-16 | 버텍스 파마슈티칼스 인코포레이티드 | 알파-1 항트립신 조절제 |
| UY38696A (es) | 2019-05-14 | 2020-11-30 | Vertex Pharma | Moduladores de alfa-1 antitripsina |
| US12502376B2 (en) | 2020-04-03 | 2025-12-23 | Vertex Pharmaceuticals Incorporated | Pyrano[4,3-b]indole derivatives as alpha-1-antitrypsin modulators for treating alpha-1-antitrypsin deficiency (AATD) |
| US20240012010A1 (en) | 2020-11-12 | 2024-01-11 | Vertex Pharmaceuticals Incorporated | Methods of monitoring alpha-1 antitrypsin (aat) deficiency by measuring polymerised aat |
| CN116813623A (zh) * | 2022-03-21 | 2023-09-29 | 东南大学 | 一种吡咯并[2,3-f]吲唑类化合物的制备方法 |
| WO2024054624A1 (en) | 2022-09-09 | 2024-03-14 | Vertex Pharmaceuticals Incorporated | Modulators of alpha-1 antitrypsin |
| WO2025236095A1 (en) * | 2024-05-17 | 2025-11-20 | Congruence Therapeutics Inc. | Modulators of alpha-1 antitrypsin |
| WO2026014456A1 (ja) * | 2024-07-10 | 2026-01-15 | 株式会社アークメディスン | 化合物、補体ｄ因子阻害剤、及び医薬組成物 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3103920C (en) * | 2018-06-22 | 2025-09-16 | Ucl Business Ltd | COMPOUNDS FOR TREATING DISEASES MEDIATED BY ALPHA-1 ANTITRYPSIN |
| KR20210089656A (ko) * | 2018-10-05 | 2021-07-16 | 버텍스 파마슈티칼스 인코포레이티드 | 알파-1 항트립신 조절제 |
| UY38696A (es) * | 2019-05-14 | 2020-11-30 | Vertex Pharma | Moduladores de alfa-1 antitripsina |
| TW202116303A (zh) * | 2019-10-02 | 2021-05-01 | 美商維泰克斯製藥公司 | α—１抗胰蛋白酶缺乏症之治療方法 |
-
2021
- 2021-04-02 IL IL296750A patent/IL296750A/en unknown
- 2021-04-02 JP JP2022559584A patent/JP2023520398A/ja not_active Withdrawn
- 2021-04-02 US US17/916,481 patent/US20230159580A1/en active Pending
- 2021-04-02 BR BR112022019794A patent/BR112022019794A2/pt not_active Application Discontinuation
- 2021-04-02 WO PCT/US2021/025597 patent/WO2021203010A1/en not_active Ceased
- 2021-04-02 CA CA3179184A patent/CA3179184A1/en active Pending
- 2021-04-02 CN CN202180039946.7A patent/CN115776984A/zh active Pending
- 2021-04-02 EP EP21722013.6A patent/EP4126877A1/en not_active Withdrawn
- 2021-04-02 KR KR1020227038218A patent/KR20220163429A/ko not_active Withdrawn
- 2021-04-02 MX MX2022012095A patent/MX2022012095A/es unknown
- 2021-04-02 AU AU2021247282A patent/AU2021247282A1/en not_active Abandoned
- 2021-04-05 AR ARP210100864A patent/AR121744A1/es not_active Application Discontinuation
- 2021-04-06 TW TW110112373A patent/TW202204359A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20230159580A1 (en) | 2023-05-25 |
| MX2022012095A (es) | 2023-01-11 |
| KR20220163429A (ko) | 2022-12-09 |
| JP2023520398A (ja) | 2023-05-17 |
| IL296750A (en) | 2022-11-01 |
| BR112022019794A2 (pt) | 2022-12-06 |
| CA3179184A1 (en) | 2021-10-07 |
| TW202204359A (zh) | 2022-02-01 |
| EP4126877A1 (en) | 2023-02-08 |
| WO2021203010A1 (en) | 2021-10-07 |
| AU2021247282A1 (en) | 2022-10-27 |
| CN115776984A (zh) | 2023-03-10 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |