IL296920A - Indole derivatives as alpha-1-antitrypsin modulators for the treatment of alpha-1-antitrypsin deficiency (aatd) - Google Patents

Indole derivatives as alpha-1-antitrypsin modulators for the treatment of alpha-1-antitrypsin deficiency (aatd)

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Publication number
IL296920A
IL296920A IL296920A IL29692022A IL296920A IL 296920 A IL296920 A IL 296920A IL 296920 A IL296920 A IL 296920A IL 29692022 A IL29692022 A IL 29692022A IL 296920 A IL296920 A IL 296920A
Authority
IL
Israel
Prior art keywords
alkyl
compound
pharmaceutically acceptable
compounds
cyano
Prior art date
Application number
IL296920A
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English (en)
Hebrew (he)
Original Assignee
Vertex Pharma
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Filing date
Publication date
Application filed by Vertex Pharma filed Critical Vertex Pharma
Publication of IL296920A publication Critical patent/IL296920A/en

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    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
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    • 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
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    • 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
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    • A—HUMAN NECESSITIES
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    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
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    • A61P11/10—Expectorants
    • A—HUMAN NECESSITIES
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    • 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
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    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
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    • C07D209/20—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals substituted additionally by nitrogen atoms, e.g. tryptophane
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    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
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    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the 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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    • C07D401/06—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 linked by a carbon chain containing only aliphatic carbon atoms
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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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    • C07D403/06—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 linked by a carbon chain containing only aliphatic carbon atoms
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IL296920A 2020-04-03 2021-04-02 Indole derivatives as alpha-1-antitrypsin modulators for the treatment of alpha-1-antitrypsin deficiency (aatd) IL296920A (en)

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US202063004717P 2020-04-03 2020-04-03
PCT/US2021/025614 WO2021203023A1 (en) 2020-04-03 2021-04-02 Indole derivatives as alpha-1 -antitrypsin modulators for treating alpha-1 -antitrypsin deficiency (aatd)

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IL296920A true IL296920A (en) 2022-12-01

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US (1) US20230159502A1 (enExample)
EP (1) EP4132908A1 (enExample)
JP (1) JP2023520400A (enExample)
KR (1) KR20220165260A (enExample)
CN (1) CN115916748A (enExample)
AR (1) AR121745A1 (enExample)
AU (1) AU2021246526A1 (enExample)
BR (1) BR112022019792A2 (enExample)
CA (1) CA3177531A1 (enExample)
IL (1) IL296920A (enExample)
MX (1) MX2022011829A (enExample)
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Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3114672A1 (en) 2018-10-05 2020-04-23 Vertex Pharmaceuticals Incorporated Modulators of alpha-1 antitrypsin
US11884672B2 (en) 2019-05-14 2024-01-30 Vertex Pharmaceuticals Incorporated Modulators of alpha-1 antitrypsin
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
WO2022104353A1 (en) 2020-11-12 2022-05-19 Vertex Pharmaceuticals Incorporated Methods of monitoring alpha-1 antitrypsin (aat) deficiency by measuring polymerised aat
TW202440093A (zh) * 2023-03-06 2024-10-16 香港商英矽智能科技知識產權有限公司 Cdk8/19雙重抑制劑及其使用方法
EP4687883A2 (en) * 2023-04-05 2026-02-11 Caraway Therapeutics, Inc. Modulators of trpml, their compositions and methods of use

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5639780A (en) * 1995-05-22 1997-06-17 Merck Frosst Canada, Inc. N-benzyl indol-3-yl butanoic acid derivatives as cyclooxygenase inhibitors
AU2002211901A1 (en) * 2000-10-10 2002-04-22 Smithkline Beecham Corporation Substituted indoles, pharmaceutical compositions containing such indoles and their use as PPAR-gamma binding agents
US6706423B2 (en) * 2001-12-27 2004-03-16 Lightronik Technology Inc. Organic EL device
US7223785B2 (en) * 2003-01-22 2007-05-29 Boehringer Ingelheim International Gmbh Viral polymerase inhibitors
US20070203209A1 (en) * 2005-08-18 2007-08-30 Wilmin Bartolini Useful indole compounds
BRPI0710527B8 (pt) * 2006-04-04 2021-05-25 Fibrogen Inc compostos de pirrolo- e tiazolo-piridina e composição farmacêutica que os compreende
SG176477A1 (en) * 2006-08-07 2011-12-29 Ironwood Pharmaceuticals Inc Indole compounds
GB0803017D0 (en) * 2008-02-19 2008-03-26 Glaxo Group Ltd Compounds
HUE025471T2 (hu) * 2008-04-16 2016-03-29 Karobio Ab Új ösztrogén receptor ligandumok
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
JPWO2012111610A1 (ja) * 2011-02-14 2014-07-07 日本電気株式会社 チアゾール系化合物及びその用途
MX2020013853A (es) * 2018-06-22 2021-05-27 Ucl Business Ltd Compuestos innovadores.
TWI748194B (zh) * 2018-06-28 2021-12-01 德商菲尼克斯 Ｆｘｒ有限責任公司 含有雙環核心部分之新穎lxr調節劑
AU2021246104A1 (en) * 2020-04-03 2022-10-20 Vertex Pharmaceuticals Incorporated Modulators of alpha-1 antitrypsin

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