ECSP21085481A - Pirroles tricíclicos condensados como moduladores de alfa-1 antitripsina - Google Patents

Pirroles tricíclicos condensados como moduladores de alfa-1 antitripsina

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Publication number
ECSP21085481A
ECSP21085481A ECSENADI202185481A ECDI202185481A ECSP21085481A EC SP21085481 A ECSP21085481 A EC SP21085481A EC SENADI202185481 A ECSENADI202185481 A EC SENADI202185481A EC DI202185481 A ECDI202185481 A EC DI202185481A EC SP21085481 A ECSP21085481 A EC SP21085481A
Authority
EC
Ecuador
Prior art keywords
alpha
antitrypsin
compounds
pyroles
modulators
Prior art date
Application number
ECSENADI202185481A
Other languages
English (en)
Inventor
Robert Daniel Giacometti
Ales Medek
Barrantes Pedro Manuel Garcia
Sarah Carol Hood
Adam Looker
Philippe Marcel Nuhant
Rupa Sawant
Michael Philip Clark
Marisa Sposato
Sarathy Kesavan
Kathy Stavropoulos
Muna Shrestha
Qing Tang
Amy Beth Hall
Yi Shi
Diane Boucher
Setu Roday
Mei-Hsiu Lai
Lev Tyler Dewey Fanning
Jr Ronald Lee Grey
Mariam Zaky
Timothy Lewis Tapley
Steven M Ronkin
Brad Maxwell
Peter Jones
Jr Mac Arthur Johnson
Dennis James Hurley
Stephen Thomson
Cavan Mckeon Bligh
Michael John Boyd
John Patrick Maxwell
Upul Keerthi Bandarage
Kevin James Gagnon
Gabrielle Simone Fleming
Siying Liu
Michael Aaron Brodney
Jinwang Xu
Stefanie Roeper
Samantha Guido
Veronique Damagnez
Kirk Alan Overhoff
Rebecca Jane Swett
Robert Francis Fimognari
Simon Giroux
Original Assignee
Vertex Pharma
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Vertex Pharma filed Critical Vertex Pharma
Publication of ECSP21085481A publication Critical patent/ECSP21085481A/es

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    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
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    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
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Abstract

La descripción proporciona compuestos útiles para tratar la deficiencia de alfa-1 antitripsina (AATD), de acuerdo con la fórmula (I), tautómeros de estos, sales farmacéuticamente aceptables de los compuestos, sales farmacéuticamente aceptables de los tautómeros, derivados deuterados de los compuestos, derivados deuterados de los tautómeros y derivados deuterados de las sales, formas sólidas de esos compuestos y procesos para preparar esos compuestos. (LA FORMULA SE OBSERVA EN LA MEMORIA TECNICA)
ECSENADI202185481A 2019-05-14 2021-11-25 Pirroles tricíclicos condensados como moduladores de alfa-1 antitripsina ECSP21085481A (es)

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PCT/US2020/032832 WO2020247160A1 (en) 2019-05-14 2020-05-14 Condensed tryciclic pyrroles as alpha-1 antitrypsin modulators

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Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020081257A1 (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
GB201918413D0 (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
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
GB201918404D0 (en) 2019-12-13 2020-01-29 Z Factor Ltd Compounds and their use for the treatment of aplha1-antitrypsin deficiency
MX2022009197A (es) * 2020-01-30 2022-10-13 Vertex Pharma Metodos de tratamiento para deficiencia de alfa-1 antitripsina.
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
MX2022012095A (es) * 2020-04-03 2023-01-11 Vertex Pharma Moduladores de alfa-1-antitripsina.
JP2023535766A (ja) 2020-07-27 2023-08-21 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調節因子を調製するためのプロセス
US20240012010A1 (en) 2020-11-12 2024-01-11 Vertex Pharmaceuticals Incorporated Methods of monitoring alpha-1 antitrypsin (aat) deficiency by measuring polymerised aat
JP2023550345A (ja) * 2020-11-17 2023-12-01 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 ４－（５－（４－フルオロフェニル）－６－（テトラヒドロ－２ｈ－ピラン－４－イル）－１，５－ジヒドロピロロ［２，３－ｆ］インダゾール－７－イル）安息香酸の固体形態
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
EP4522129A1 (en) * 2022-05-11 2025-03-19 Eli Lilly And Co. Glp1 pharmaceutical compositions
GEAP202516730A (en) 2022-09-09 2025-07-25 Vertex Pharma Modulators of alpha-i antitrypsin
WO2025090827A1 (en) 2023-10-27 2025-05-01 Sub21, Inc. A1at modulators
WO2025193777A1 (en) 2024-03-13 2025-09-18 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions of alpha-1 antitrypsin 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 (69)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3404157A (en) 1965-02-24 1968-10-01 American Cyanamid Co Substituted pyrroloindazole compounds
US4198415A (en) 1979-01-22 1980-04-15 Eli Lilly And Company Prolactin inhibiting octahydro pyrazolo[3,4-g]quinolines
US4647667A (en) 1982-11-03 1987-03-03 Eli Lilly And Company Octa- and deca-hydroquinoline intermediates
US4778894A (en) 1983-09-26 1988-10-18 Eli Lilly And Company 6 oxo-decahydroquinolines
DK158590D0 (da) * 1990-07-02 1990-07-02 Lundbeck & Co As H Indolderivater
US5639780A (en) 1995-05-22 1997-06-17 Merck Frosst Canada, Inc. N-benzyl indol-3-yl butanoic acid derivatives as cyclooxygenase inhibitors
US20020017295A1 (en) 2000-07-07 2002-02-14 Weers Jeffry G. Phospholipid-based powders for inhalation
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
MXPA02006086A (es) 1999-12-29 2004-08-23 Wyeth Corp Inhibidores triciclicos de proteina-cinasas.
IL154107A0 (en) 2000-07-26 2003-07-31 Smithkline Beecham Plc Aminopiperidine quinolines and their azaisosteric analogues with antibacterial activity
US6777400B2 (en) 2000-08-05 2004-08-17 Smithkline Beecham Corporation Anti-inflammatory androstane derivative compositions
US6906192B2 (en) 2000-11-07 2005-06-14 Bristol Myers Squibb Company Processes for the preparation of acid derivatives useful as serine protease inhibitors
US20030212085A1 (en) 2001-04-17 2003-11-13 Mccall Robert B. Treatment of fibromyalgia and chronic fatigue syndrome
US20040176361A1 (en) 2001-05-23 2004-09-09 Masakazu Fujio Fused heterocyclic compound and medicinal use thereof
MXPA04004657A (es) 2001-11-14 2004-08-13 Teva Pharma Formas amorfas y cristalinas de potasio de losartan y proceso para su preparacion.
US6706423B2 (en) 2001-12-27 2004-03-16 Lightronik Technology Inc. Organic EL device
TW200400963A (en) 2002-05-21 2004-01-16 Wyeth Corp R-enantiomers of pyranoindole derivatives and the use thereof for the treatment of hepatitis C virus infection or disease
WO2004108120A1 (en) 2003-06-11 2004-12-16 Pfizer Products Inc. Use of growth hormone secretagogues for treatment of fibromyalgia
BRPI0412820A (pt) 2003-07-25 2006-09-26 Pfizer compostos de aminopirazol e utilização como inibidores de chk1
US7208601B2 (en) 2003-08-08 2007-04-24 Mjalli Adnan M M Aryl and heteroaryl compounds, compositions, and methods of use
JP2008506702A (ja) 2004-07-14 2008-03-06 ピーティーシー セラピューティクス，インコーポレーテッド Ｃ型肝炎を治療するための方法
US8097644B2 (en) 2006-03-28 2012-01-17 Allergan, Inc. Indole compounds having sphingosine-1-phosphate (S1P) receptor antagonist
TW200813054A (en) 2006-06-02 2008-03-16 Elan Pharm Inc Fused, tricyclic sulfonamide inhibitors of gamma secretase
EP2114141A2 (en) 2007-01-10 2009-11-11 University of Florida Compounds and methods for treatment of alpha-1 antitrypsin deficiency
JP5107589B2 (ja) 2007-02-13 2012-12-26 旭化成株式会社 インドール誘導体
DE102008022521A1 (de) * 2008-05-07 2009-11-12 Bayer Schering Pharma Aktiengesellschaft 1,4-Diaryl-pyrimidopyridazin-2,5-dione und ihre Verwendung
PT2276732E (pt) 2008-04-16 2015-09-28 Karobio Ab Novos ligandos do recetor de estrogénio
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
SMT202100051T1 (it) 2010-03-25 2021-03-15 Vertex Pharma Dispersione solida di una forma amorfa di (r)-1-(2,2-difluorobenzo[d][1,3]diossol-5-il)-n-(1-(2,3-diidrossipropil)-6-fluoro-2-(1-idrossi-2-metilpropan-2-il)-1h-indol-5-il)ciclopropan-carbossamide
CN110818724B (zh) 2010-05-07 2020-11-13 吉利德康涅狄格有限公司 吡啶酮和氮杂吡啶酮化合物及使用方法
PE20131106A1 (es) 2010-08-04 2013-10-17 Gruenenthal Chemie Aucforma de dosificacion farmaceutica que comprende 6'-fluoro-(n-metil- o n,n-dimetil)-4-fenil-4',9'-dihidro-3'h-espiro[ciclohexan-1,1'-pirano[3,4,b]indol]-4-amina
WO2012038820A2 (en) 2010-09-24 2012-03-29 Grifols Therapeutics Inc. Immunochromatography devices, methods and kits
JPWO2012063753A1 (ja) 2010-11-08 2014-05-12 日本電気株式会社 インドール系化合物、並びにこれを用いた光電変換用色素、半導体電極、光電変換素子および光電気化学電池
WO2012111610A1 (ja) 2011-02-14 2012-08-23 日本電気株式会社 チアゾール系化合物及びその用途
CA2839917A1 (en) 2011-06-24 2012-12-27 The Regents Of The University Of Colorado, A Body Corporate Compositions, methods and uses for alpha-1 antitrypsin fusion molecules
CA2917682A1 (en) 2013-07-10 2015-01-15 Bayer Pharma Aktiengesellschaft Benzyl-1h-pyrazolo[3,4-b]pyridines and use thereof
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
WO2017035418A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Disubstituted compounds for treatment of immune and inflammatory disorders
EP3397243A1 (en) 2015-12-30 2018-11-07 H. Hoffnabb-La Roche Ag Use of tryptophan derivatives for protein formulations
CA3024556A1 (en) 2016-05-12 2017-11-16 The Regents Of The University Of Michigan Ash1l inhibitors and methods of treatment therewith
JOP20180008A1 (ar) * 2017-02-02 2019-01-30 Gilead Sciences Inc مركبات لعلاج إصابة بعدوى فيروس الالتهاب الكبدي b
CN110546150B (zh) 2017-10-19 2021-12-21 江苏豪森药业集团有限公司 含吡唑基的三并环类衍生物、其制备方法和应用
SG11202003827YA (en) 2017-11-01 2020-05-28 Bristol Myers Squibb Co Bridged bicyclic compounds as farnesoid x receptor modulators
CN107698505A (zh) 2017-11-20 2018-02-16 孙婷婷 一种诺得司他的制备方法
US11459330B2 (en) 2017-12-13 2022-10-04 Lupin Limited Substituted bicyclic heterocyclic compounds as PRMT5 inhibitors
WO2019149522A1 (en) 2018-01-31 2019-08-08 Merck Patent Gmbh Quinoline compounds as irak inhibitors and uses thereof
CN113286586A (zh) 2018-06-22 2021-08-20 Ucl商业有限公司 新化合物
CA3108388A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
WO2020081257A1 (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
MX2022009197A (es) 2020-01-30 2022-10-13 Vertex Pharma Metodos de tratamiento para deficiencia de alfa-1 antitripsina.
MX2022012095A (es) 2020-04-03 2023-01-11 Vertex Pharma Moduladores de alfa-1-antitripsina.
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
US20230339915A1 (en) 2020-04-03 2023-10-26 Vertex Pharmaceuticals Incorporated Modulators of alpha-1 antitrypsin
US20230159521A1 (en) 2020-04-03 2023-05-25 Vertex Pharmaceuticals Incorporated 1h-pyrazolo[4,3-g]isoquinoline and 1h-pyrazolo[4,3-g]quinoline derivatives as alpha-1-antitrypsin modulators for treating alpha-1-antitrypsin deficiency (aatd)
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)
JP7791102B2 (ja) 2020-04-03 2025-12-23 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
JP2023535766A (ja) 2020-07-27 2023-08-21 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調節因子を調製するためのプロセス
US20240012010A1 (en) 2020-11-12 2024-01-11 Vertex Pharmaceuticals Incorporated Methods of monitoring alpha-1 antitrypsin (aat) deficiency by measuring polymerised aat
JP2023550345A (ja) 2020-11-17 2023-12-01 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 ４－（５－（４－フルオロフェニル）－６－（テトラヒドロ－２ｈ－ピラン－４－イル）－１，５－ジヒドロピロロ［２，３－ｆ］インダゾール－７－イル）安息香酸の固体形態
GEAP202516730A (en) 2022-09-09 2025-07-25 Vertex Pharma Modulators of alpha-i antitrypsin

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