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PE20220905A1 - Pirroles triciclicos condensados como moduladores de alfa-1 antitripsina - Google Patents

Pirroles triciclicos condensados como moduladores de alfa-1 antitripsina

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Publication number
PE20220905A1
PE20220905A1 PE2021001895A PE2021001895A PE20220905A1 PE 20220905 A1 PE20220905 A1 PE 20220905A1 PE 2021001895 A PE2021001895 A PE 2021001895A PE 2021001895 A PE2021001895 A PE 2021001895A PE 20220905 A1 PE20220905 A1 PE 20220905A1
Authority
PE
Peru
Prior art keywords
linear
cyclic
branched
compounds
independently selected
Prior art date
Application number
PE2021001895A
Other languages
English (en)
Inventor
Upul Keerthi Bandarage
Cavan Mckeon Bligh
Diane Boucher
Michael John Boyd
Michael Aaron Brodney
Michael Philip Clark
Veronique Damagnez
Lev Tyler Dewey Fanning
Robert Francis Fimognari
Gabrielle Simone Fleming
Kevin James Gagnon
Barrantes Pedro Manuel Garcia
Robert Daniel Giacometti
Simon Giroux
Jr Ronald Lee Grey
Samantha Guido
Amy Beth Hall
Sarah Carol Hood
Dennis James Hurley
Jr Mac Arthur Johnson
Peter Jones
Sarathy Kesavan
Mei-Hsiu Lai
Siying Liu
Adam Looker
Brad Maxwell
John Patrick Maxwell
Ales Medek
Philippe Marcel Nuhant
Kirk Alan Overhoff
Setu Roday
Stefanie Roeper
Steven M Ronkin
Rupa Sawant
Yi Shi
Muna Shrestha
Marisa Sposato
Kathy Stavropoulos
Rebecca Jane Swett
Qing Tang
Timothy Lewis Tapley
Stephen Thomson
Jinwang Xu
Mariam Zaky
Kevin Michael Cottrell
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 PE20220905A1 publication Critical patent/PE20220905A1/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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    • A61K31/41—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
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    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
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    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/23—Heterocyclic radicals containing two or more heterocyclic rings condensed among themselves or condensed with a common carbocyclic ring system, not provided for in groups C07H19/14 - C07H19/22
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Abstract

Un compuesto de formula (I) en donde: R0 se selecciona de (a) grupos alquilo C1-C8 lineales, ramificados y ciclicos, entre otros; R1 es (a) hidrogeno, (b) grupos alquilo C1-C8 lineales, entre otros; R2 es anillos hetereociclicos de 5 y 6 miembros y anillos aromaticos de 5 a 6 miembros, entre otros; X 1 y X 2 se seleccionan, independientemente, de hidrogeno, halogenos, ciano, hidroxi, grupos C1-C6 lineales, ramificados y ciclicos; cada uno de W1 y W2 se selecciona, independientemente, de C y N; cada R 3 se selecciona, independientemente, de hidrogeno, halogenos, ciano, grupos alquilo C1-C6 lineales ramificados y ciclicos, y grupos alcoxi C1-C6 lineales ramificados y ciclicos; n es un numero entero seleccionado de 0, 1, 2 y 3; Z1 , Z2 , y Z3 se seleccionan, independientemente, de carbono, nitrogeno, azufre y oxigeno, en donde, cuando Z1 , Z2 , y/o Z3 son carbono o nitrogeno, las valencias de carbono y nitrogeno se completan con atomos de hidrogeno, halogeno, grupos alquilo C1-C6 lineales, 10 ramificados y ciclicos, y grupos alcoxi C1-C6 lineales, ramificados y ciclicos, entre otros. Los compuestos son utiles para tratar la deficiencia de alfa-1 antitripsina (AATD), de acuerdo con la formula (I), tautomeros de estos, sales farmaceuticamente aceptables de los compuestos, sales farmaceuticamente aceptables de los tautomeros, derivados deuterados de los compuestos, derivados deuterados de los tautomeros y derivados deuterados de las sales, formas solidas de esos compuestos y procesos para preparar esos compuestos.
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Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20210089656A (ko) * 2018-10-05 2021-07-16 버텍스 파마슈티칼스 인코포레이티드 알파-1 항트립신 조절제
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
GB201918410D0 (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
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
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.
EP4126877A1 (en) * 2020-04-03 2023-02-08 Vertex Pharmaceuticals Incorporated Pyrrolo[2,3-f]indazole and 2,4,5,10-tetrazatricyclo[7.3.0.03,7]dodeca-1,3(7),5,8,11-pentaene derivatives as alpha-1-antitrypsin modulators for treating alpha-1-antitrypsin deficiency (aatd)
WO2021203014A1 (en) 2020-04-03 2021-10-07 Vertex Pharmaceuticals Incorporated Pyrano[4,3-b]l ndole derivatives as alpha-1 -antitrypsin modulators for treating alpha-1 -antitrypsin deficiency (aatd)
CA3190103A1 (en) 2020-07-27 2022-02-03 Vertex Pharmaceuticals Incorporated Processes for preparing modulators of alpha-1 antitrypsin
US20240012010A1 (en) 2020-11-12 2024-01-11 Vertex Pharmaceuticals Incorporated Methods of monitoring alpha-1 antitrypsin (aat) deficiency by measuring polymerised aat
US20240002386A1 (en) 2020-11-17 2024-01-04 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
US20250302809A1 (en) * 2022-05-11 2025-10-02 Eli Lilly And Company Glp1 pharmaceutical compositions
CN120166990A (zh) * 2022-09-09 2025-06-17 弗特克斯药品有限公司 α-1抗胰蛋白酶的调节剂
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
CN100432055C (zh) 1999-12-29 2008-11-12 惠氏公司 三环蛋白激酶抑制剂
US6638929B2 (en) 1999-12-29 2003-10-28 Wyeth Tricyclic protein kinase inhibitors
HUP0300721A3 (en) 2000-07-26 2006-02-28 Smithkline Beecham Plc Aminopiperidine quinolines and their azaisosteric analogues with antibacterial activity, process for producing them, pharmaceutical compositions containing them and use thereof
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
JPWO2002094790A1 (ja) 2001-05-23 2004-09-09 三菱ウェルファーマ株式会社 縮合ヘテロ環化合物およびその医薬用途
HUP0501067A2 (en) 2001-11-14 2006-02-28 Teva Pharma Amorphous and crystalline forms of losartan potassium and process for their preparation
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
WO2005009435A1 (en) 2003-07-25 2005-02-03 Pfizer Inc. Aminopyrazole compounds and use as chk1 inhibitors
US7208601B2 (en) 2003-08-08 2007-04-24 Mjalli Adnan M M Aryl and heteroaryl compounds, compositions, and methods of use
KR20070083484A (ko) 2004-07-14 2007-08-24 피티씨 테라퓨틱스, 인크. Ｃ형 간염 치료 방법
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
HUE025471T2 (hu) 2008-04-16 2016-03-29 Karobio Ab Új ösztrogén receptor ligandumok
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
CN102892764B (zh) 2010-03-25 2016-07-06 弗特克斯药品有限公司 (r)-1(2,2-二氟苯并[d][1,3]间二氧杂环戊烯-5-基)-n-(1-(2,3-二羟基丙基)-6-氟-2-(1-羟基-2-甲基丙-2-基)-1h-吲哚-5-基)环丙烷甲酰胺的固体形式
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
TWI526445B (zh) 2010-08-04 2016-03-21 固朗索有限公司 含有６’－氟－（Ｎ－甲基－或Ｎ，Ｎ－二甲基－）－４－苯基－４’，９’－二氫－３’Ｈ－螺［環己烷－１，１’－哌喃並［３，４－ｂ］吲哚］－４－胺之藥學劑型
BR112013008602B1 (pt) 2010-09-24 2020-11-17 Grifols Therapeutics Inc. dispositivo imunocromatográfico, método para a determinação de um carreador gênico, método para o diagnóstico, dispositivo para ensaio imunológico, método para a detecção e determinação da presença de uma proteína e kit
US20130167932A1 (en) 2010-11-08 2013-07-04 Nec Corporation Indole compound, and photoelectric conversion dye using same, semiconductor electrode, photoelectric conversion element, and photoelectrochemical cell
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
EP2723370A4 (en) 2011-06-24 2015-06-03 Univ Colorado Regents COMPOSITIONS, PROCESS AND USE OF ALPHA-1-ANTITRYPHIN FUSION MOLECULES
MX2016000258A (es) 2013-07-10 2016-04-28 Bayer Pharma AG Bencil-1h-pirazolo[3,4-b]piridinas y su uso.
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
SG11201804951SA (en) 2015-12-30 2018-07-30 Genentech Inc 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
US20200247815A1 (en) 2017-10-19 2020-08-06 Jiangsu Hansoh Pharmaceutical Group Co., Ltd. Pyrazolyl-containing tricyclic derivative, preparation method therefor and use thereof
AR113820A1 (es) 2017-11-01 2020-06-17 Bristol Myers Squibb Co Compuestos bicíclicos 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
KR102708147B1 (ko) 2017-12-13 2024-09-19 루핀 리미티드 Prmt5 억제제로서의 치환된 이중 고리형 헤테로 고리 화합물
US11542246B2 (en) 2018-01-31 2023-01-03 Merck Patent Gmbh Quinoline compounds as IRAK inhibitors and uses thereof
SG11202012765PA (en) 2018-06-22 2021-01-28 Ucl Business Ltd Novel compounds
MA53287A (fr) 2018-08-07 2022-05-11 Merck Sharp & Dohme Inhibiteurs de prmt5
KR20210089656A (ko) * 2018-10-05 2021-07-16 버텍스 파마슈티칼스 인코포레이티드 알파-1 항트립신 조절제
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.
WO2021203007A1 (en) 2020-04-03 2021-10-07 Vertex Pharmaceuticals Incorporated Substituted 5-hydroxyindole compounds as modulators of alpha-1 antitrypsin
EP4126877A1 (en) 2020-04-03 2023-02-08 Vertex Pharmaceuticals Incorporated Pyrrolo[2,3-f]indazole and 2,4,5,10-tetrazatricyclo[7.3.0.03,7]dodeca-1,3(7),5,8,11-pentaene derivatives as alpha-1-antitrypsin modulators for treating alpha-1-antitrypsin deficiency (aatd)
AU2021246527A1 (en) 2020-04-03 2022-10-27 Vertex Pharmaceuticals Incorporated Modulators of alpha-1 antitrypsin
JP2023520400A (ja) 2020-04-03 2023-05-17 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－アンチトリプシン欠損症（ａａｔｄ）を治療するためのアルファ－１－アンチトリプシンモジュレーターとしてのインドール誘導体
JP7803872B2 (ja) 2020-04-03 2026-01-21 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モジュレーター
WO2021203014A1 (en) 2020-04-03 2021-10-07 Vertex Pharmaceuticals Incorporated Pyrano[4,3-b]l ndole derivatives as alpha-1 -antitrypsin modulators for treating alpha-1 -antitrypsin deficiency (aatd)
CA3190103A1 (en) 2020-07-27 2022-02-03 Vertex Pharmaceuticals Incorporated Processes for preparing modulators of alpha-1 antitrypsin
US20240012010A1 (en) 2020-11-12 2024-01-11 Vertex Pharmaceuticals Incorporated Methods of monitoring alpha-1 antitrypsin (aat) deficiency by measuring polymerised aat
US20240002386A1 (en) 2020-11-17 2024-01-04 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
CN120166990A (zh) 2022-09-09 2025-06-17 弗特克斯药品有限公司 α-1抗胰蛋白酶的调节剂

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