CA3114672A1 - Modulators of alpha-1 antitrypsin - Google Patents
Modulators of alpha-1 antitrypsin Download PDFInfo
- Publication number
- CA3114672A1 CA3114672A1 CA3114672A CA3114672A CA3114672A1 CA 3114672 A1 CA3114672 A1 CA 3114672A1 CA 3114672 A CA3114672 A CA 3114672A CA 3114672 A CA3114672 A CA 3114672A CA 3114672 A1 CA3114672 A1 CA 3114672A1
- Authority
- CA
- Canada
- Prior art keywords
- branched
- linear
- groups
- cyclic
- chosen
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
-
- 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
-
- 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
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
-
- 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
- C07D487/12—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 three hetero rings
- C07D487/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- 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
-
- 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
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Saccharide Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862742148P | 2018-10-05 | 2018-10-05 | |
| US62/742,148 | 2018-10-05 | ||
| US201862768662P | 2018-11-16 | 2018-11-16 | |
| US62/768,662 | 2018-11-16 | ||
| PCT/US2019/054681 WO2020081257A1 (en) | 2018-10-05 | 2019-10-04 | Modulators of alpha-1 antitrypsin |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3114672A1 true CA3114672A1 (en) | 2020-04-23 |
Family
ID=69467663
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3114672A Pending CA3114672A1 (en) | 2018-10-05 | 2019-10-04 | Modulators of alpha-1 antitrypsin |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US11623924B2 (https=) |
| EP (1) | EP3860712A1 (https=) |
| JP (1) | JP2022512588A (https=) |
| KR (1) | KR20210089656A (https=) |
| CN (1) | CN113164761A (https=) |
| AU (1) | AU2019362753A1 (https=) |
| BR (1) | BR112021006392A2 (https=) |
| CA (1) | CA3114672A1 (https=) |
| CO (1) | CO2021005884A2 (https=) |
| IL (1) | IL281884A (https=) |
| JO (1) | JOP20210060A1 (https=) |
| MA (1) | MA53827A (https=) |
| MX (1) | MX2021003819A (https=) |
| TW (1) | TW202024091A (https=) |
| UY (1) | UY38403A (https=) |
| WO (1) | WO2020081257A1 (https=) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3114672A1 (en) | 2018-10-05 | 2020-04-23 | Vertex Pharmaceuticals Incorporated | Modulators of alpha-1 antitrypsin |
| GB201820450D0 (en) | 2018-12-14 | 2019-01-30 | Z Factor Ltd | Compound and its use for the treatment of alpha1-antitryspin deficiency |
| US11884672B2 (en) | 2019-05-14 | 2024-01-30 | Vertex Pharmaceuticals Incorporated | Modulators of alpha-1 antitrypsin |
| 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 |
| GB201918404D0 (en) | 2019-12-13 | 2020-01-29 | Z Factor Ltd | Compounds and their use for the treatment of aplha1-antitrypsin deficiency |
| GB201918410D0 (en) | 2019-12-13 | 2020-01-29 | Z Factor Ltd | Compounds and their use for the treatment of alpha1-antitrypsin deficiency |
| GB201918416D0 (en) | 2019-12-13 | 2020-01-29 | Z Factor Ltd | Compounds and their use for the treatment of Alpha1-Antitrypsin deficiency |
| GB201918414D0 (en) | 2019-12-13 | 2020-01-29 | Z Factor Ltd | Compounds and their use for the treatment of Alpha1-Antitrypsin deficiency |
| GB201918413D0 (en) | 2019-12-13 | 2020-01-29 | Z Factor Ltd | Compounds and their use for the treatment of alpha1-antitrypsin deficiency |
| CN115776984A (zh) * | 2020-04-03 | 2023-03-10 | 弗特克斯药品有限公司 | 作为用于治疗α-1抗胰蛋白酶缺乏症(AATD)的α-1-抗胰蛋白酶调节剂的吡咯并[2,3-f]吲唑和2,4,5,10-四氮杂三环[7.3.0.03,7]十二碳-1,3(7),5,8,11-五烯衍生物 |
| WO2021203025A1 (en) * | 2020-04-03 | 2021-10-07 | Vertex Pharmaceuticals Incorporated | 1 h-pyrazolo[4,3-g]isoquinoline and 1 h-pyrazolo[4,3-g]quinoline derivatives as alpha-1 -antitrypsin modulators for treating alpha-1 -antitrypsin deficiency (aatd) |
| JP7732999B2 (ja) | 2020-04-03 | 2025-09-02 | バーテックス ファーマシューティカルズ インコーポレイテッド | アルファ１－アンチトリプシンのモジュレーター |
| GB202009074D0 (en) | 2020-06-15 | 2020-07-29 | Z Factor Ltd | Compound |
| WO2022026372A2 (en) | 2020-07-27 | 2022-02-03 | Vertex Pharmaceuticals Incorporated | Processes for preparing modulators of alpha-1 antitrypsin |
| WO2022104353A1 (en) | 2020-11-12 | 2022-05-19 | Vertex Pharmaceuticals Incorporated | Methods of monitoring alpha-1 antitrypsin (aat) deficiency by measuring polymerised aat |
| AU2021381509A1 (en) * | 2020-11-17 | 2023-06-22 | Vertex Pharmaceuticals Incorporated | Solid forms of 4-(5-(4-fluorophenyl)-6-tetrahydro-2h-pyran-4-yl)- 1,5-dihydropyrrolo[2,3-f]indazol-7-yl)benzoic acid |
| GB202108523D0 (en) | 2021-06-15 | 2021-07-28 | Z Factor Ltd | Compositions and their use for the treatment of alpha1-antitrypsin deficiency |
| 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 |
| CN114605385B (zh) * | 2022-03-25 | 2023-09-08 | 河南大学 | 吲哚哌啶脲类trpv1拮抗/faah抑制双靶点药物及制备方法和应用 |
| WO2025090827A1 (en) | 2023-10-27 | 2025-05-01 | Sub21, Inc. | A1at modulators |
| 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 (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE790679A (fr) * | 1971-11-03 | 1973-04-27 | Ici Ltd | Derives de l'indole |
| DK158590D0 (da) | 1990-07-02 | 1990-07-02 | Lundbeck & Co As H | Indolderivater |
| JP2000072751A (ja) | 1998-08-26 | 2000-03-07 | Tanabe Seiyaku Co Ltd | イソキノリノン誘導体 |
| JP2000281654A (ja) | 1999-03-26 | 2000-10-10 | Tanabe Seiyaku Co Ltd | イソキノリン誘導体 |
| GB9913083D0 (en) | 1999-06-04 | 1999-08-04 | Novartis Ag | Organic compounds |
| FR2802532A1 (fr) | 1999-12-17 | 2001-06-22 | Sanofi Synthelabo | Derives de 2-phenyl-quinoleine, leur preparation et leur application en therapeutique |
| US6638929B2 (en) | 1999-12-29 | 2003-10-28 | Wyeth | Tricyclic protein kinase inhibitors |
| EP1305308B1 (en) | 2000-07-26 | 2006-12-20 | Smithkline Beecham Plc | Aminopiperidine quinolines and their azaisosteric analogues with antibacterial activity |
| EP1396488A1 (en) | 2001-05-23 | 2004-03-10 | Mitsubishi Pharma Corporation | Fused heterocyclic compound and medicinal use thereof |
| ES2234451T1 (es) | 2001-11-14 | 2005-07-01 | Teva Pharmaceutical Industries Ltd. | Formas cristalinas y amorfas de losartan potasio y procedimiento para su preparacion. |
| US7208601B2 (en) | 2003-08-08 | 2007-04-24 | Mjalli Adnan M M | Aryl and heteroaryl compounds, compositions, and methods of use |
| WO2009158587A1 (en) * | 2008-06-26 | 2009-12-30 | Inspire Pharmaceuticals, Inc. | Method for treating pulmonary diseases using rho kinase inhibitor compounds |
| WO2011056222A1 (en) | 2009-11-05 | 2011-05-12 | University Of Pittsburgh - Of The Commonwealth System Of Higher Education | Methods of treating disorders associated with protein aggregation |
| WO2011110852A1 (en) | 2010-03-10 | 2011-09-15 | Astrazeneca Ab | Polymorphic forms of 6- [2- (4 -cyanophenyl) - 2h - pyrazol - 3 - yl] - 5 -methyl - 3 - oxo - 4 - (trifluoromethyl - phenyl) 3,4-dihydropyrazine-2-carboxylic acid ethylamide |
| US9572794B2 (en) | 2014-08-06 | 2017-02-21 | Vanderbilt University | Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists |
| WO2016154051A1 (en) | 2015-03-20 | 2016-09-29 | University Of Florida Research Foundation, Inc. | Combination therapy for treating infections diseases |
| ES2910787T3 (es) | 2016-05-12 | 2022-05-13 | Univ Michigan Regents | Inhibidores de ASH1L y métodos de tratamiento con los mismos |
| US20200247815A1 (en) | 2017-10-19 | 2020-08-06 | Jiangsu Hansoh Pharmaceutical Group Co., Ltd. | Pyrazolyl-containing tricyclic derivative, preparation method therefor and use thereof |
| PE20201170A1 (es) | 2017-11-01 | 2020-10-28 | Bristol Myers Squibb Co | Compuestos biciclicos en puente como moduladores del receptor farnesoide x |
| CN107698505A (zh) | 2017-11-20 | 2018-02-16 | 孙婷婷 | 一种诺得司他的制备方法 |
| SMT202200396T1 (it) | 2017-12-13 | 2022-11-18 | Lupin Ltd | Composti eterociclici biciclici sostituiti come inibitori di prmt5 |
| CN111971278B (zh) | 2018-01-31 | 2023-08-11 | 默克专利有限公司 | 用作irak抑制剂的喹啉化合物及其用途 |
| MX2020013853A (es) | 2018-06-22 | 2021-05-27 | Ucl Business Ltd | Compuestos innovadores. |
| US12173026B2 (en) | 2018-08-07 | 2024-12-24 | Merck Sharp & Dohme Llc | PRMT5 inhibitors |
| CA3114672A1 (en) | 2018-10-05 | 2020-04-23 | Vertex Pharmaceuticals Incorporated | Modulators of alpha-1 antitrypsin |
| CN110776459B (zh) | 2019-03-19 | 2023-01-24 | 江苏知原药业股份有限公司 | 7-羟基-2-喹诺酮-二硫代氨基甲酸酯类胆碱酯酶抑制剂 |
| US11884672B2 (en) | 2019-05-14 | 2024-01-30 | Vertex Pharmaceuticals Incorporated | Modulators of alpha-1 antitrypsin |
| 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 |
| BR112022014861A2 (pt) | 2020-01-30 | 2022-09-20 | Vertex Pharma | Métodos de tratamento para deficiência de alfa-1 antittripsina |
| AU2021246104A1 (en) | 2020-04-03 | 2022-10-20 | Vertex Pharmaceuticals Incorporated | Modulators of alpha-1 antitrypsin |
| CN115697969A (zh) | 2020-04-03 | 2023-02-03 | 弗特克斯药品有限公司 | 作为用于治疗α-1抗胰蛋白酶缺乏症(AATD)的α-1抗胰蛋白酶调节剂的7-或8-羟基-异喹啉和7-或8-羟基-喹啉衍生物 |
| IL296920A (en) | 2020-04-03 | 2022-12-01 | Vertex Pharma | Indole derivatives as alpha-1-antitrypsin modulators for the treatment of alpha-1-antitrypsin deficiency (aatd) |
| CN115776984A (zh) | 2020-04-03 | 2023-03-10 | 弗特克斯药品有限公司 | 作为用于治疗α-1抗胰蛋白酶缺乏症(AATD)的α-1-抗胰蛋白酶调节剂的吡咯并[2,3-f]吲唑和2,4,5,10-四氮杂三环[7.3.0.03,7]十二碳-1,3(7),5,8,11-五烯衍生物 |
| WO2021203025A1 (en) | 2020-04-03 | 2021-10-07 | Vertex Pharmaceuticals Incorporated | 1 h-pyrazolo[4,3-g]isoquinoline and 1 h-pyrazolo[4,3-g]quinoline derivatives as alpha-1 -antitrypsin modulators for treating alpha-1 -antitrypsin deficiency (aatd) |
| JP7732999B2 (ja) | 2020-04-03 | 2025-09-02 | バーテックス ファーマシューティカルズ インコーポレイテッド | アルファ１－アンチトリプシンのモジュレーター |
| WO2022026372A2 (en) | 2020-07-27 | 2022-02-03 | Vertex Pharmaceuticals Incorporated | Processes for preparing modulators of alpha-1 antitrypsin |
-
2019
- 2019-10-04 CA CA3114672A patent/CA3114672A1/en active Pending
- 2019-10-04 EP EP19848828.0A patent/EP3860712A1/en not_active Withdrawn
- 2019-10-04 WO PCT/US2019/054681 patent/WO2020081257A1/en not_active Ceased
- 2019-10-04 BR BR112021006392A patent/BR112021006392A2/pt unknown
- 2019-10-04 JO JOP/2021/0060A patent/JOP20210060A1/ar unknown
- 2019-10-04 KR KR1020217013514A patent/KR20210089656A/ko not_active Withdrawn
- 2019-10-04 AU AU2019362753A patent/AU2019362753A1/en not_active Abandoned
- 2019-10-04 MX MX2021003819A patent/MX2021003819A/es unknown
- 2019-10-04 CN CN201980078980.8A patent/CN113164761A/zh active Pending
- 2019-10-04 MA MA053827A patent/MA53827A/fr unknown
- 2019-10-04 JP JP2021518181A patent/JP2022512588A/ja active Pending
- 2019-10-04 US US16/593,118 patent/US11623924B2/en active Active
- 2019-10-05 TW TW108136173A patent/TW202024091A/zh unknown
- 2019-10-07 UY UY0001038403A patent/UY38403A/es not_active Application Discontinuation
-
2021
- 2021-03-29 IL IL281884A patent/IL281884A/en unknown
- 2021-05-05 CO CONC2021/0005884A patent/CO2021005884A2/es unknown
-
2023
- 2023-02-09 US US18/107,786 patent/US20230265080A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| AU2019362753A1 (en) | 2021-05-20 |
| MX2021003819A (es) | 2021-06-23 |
| KR20210089656A (ko) | 2021-07-16 |
| JP2022512588A (ja) | 2022-02-07 |
| EP3860712A1 (en) | 2021-08-11 |
| CO2021005884A2 (es) | 2021-05-20 |
| US20230265080A1 (en) | 2023-08-24 |
| US20210179587A1 (en) | 2021-06-17 |
| US11623924B2 (en) | 2023-04-11 |
| JOP20210060A1 (ar) | 2023-01-30 |
| UY38403A (es) | 2020-04-30 |
| IL281884A (en) | 2021-05-31 |
| WO2020081257A1 (en) | 2020-04-23 |
| MA53827A (fr) | 2021-09-15 |
| TW202024091A (zh) | 2020-07-01 |
| CN113164761A (zh) | 2021-07-23 |
| BR112021006392A2 (pt) | 2021-07-06 |
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