AU2020395306B2 - MASP-2 inhibitors and methods of use - Google Patents

MASP-2 inhibitors and methods of use Download PDF

Info

Publication number
AU2020395306B2
AU2020395306B2 AU2020395306A AU2020395306A AU2020395306B2 AU 2020395306 B2 AU2020395306 B2 AU 2020395306B2 AU 2020395306 A AU2020395306 A AU 2020395306A AU 2020395306 A AU2020395306 A AU 2020395306A AU 2020395306 B2 AU2020395306 B2 AU 2020395306B2
Authority
AU
Australia
Prior art keywords
substituted
unsubstituted
heterocyclyl
heteroaryl
compound
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.)
Active
Application number
AU2020395306A
Other languages
English (en)
Other versions
AU2020395306A1 (en
Inventor
Neil S. Cutshall
Jennifer Lynn Gage
Sara Rebecca GOLDSTEIN
Do Yeon Kwon
Thomas L. Little
Markus Metz
Peter Kurt NOLLERT VON SPECHT
Jennifer TSOUNG
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Omeros Corp
Original Assignee
Omeros Medical Systems Inc
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 Omeros Medical Systems Inc filed Critical Omeros Medical Systems Inc
Publication of AU2020395306A1 publication Critical patent/AU2020395306A1/en
Application granted granted Critical
Publication of AU2020395306B2 publication Critical patent/AU2020395306B2/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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 two hetero rings
    • C07D471/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2020395306A 2019-12-04 2020-12-04 MASP-2 inhibitors and methods of use Active AU2020395306B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962943629P 2019-12-04 2019-12-04
US62/943,629 2019-12-04
PCT/US2020/063391 WO2021113698A1 (en) 2019-12-04 2020-12-04 Masp-2 inhibitors and methods of use

Publications (2)

Publication Number Publication Date
AU2020395306A1 AU2020395306A1 (en) 2022-06-30
AU2020395306B2 true AU2020395306B2 (en) 2025-04-24

Family

ID=74106147

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2020395306A Active AU2020395306B2 (en) 2019-12-04 2020-12-04 MASP-2 inhibitors and methods of use

Country Status (6)

Country Link
US (4) US12030853B2 (https=)
EP (1) EP4069676A1 (https=)
JP (1) JP7721142B2 (https=)
AU (1) AU2020395306B2 (https=)
CA (1) CA3159159A1 (https=)
WO (1) WO2021113698A1 (https=)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL311042B1 (en) 2018-05-29 2026-04-01 Omeros Corp MASP-2 inhibitors and methods of use
EP4069676A1 (en) * 2019-12-04 2022-10-12 Omeros Corporation Masp-2 inhibitors and methods of use
IL293588B1 (en) 2019-12-04 2026-04-01 Omeros Corp 3-Amino-1-methylpyrazin-2(H1)-one derivatives as MASP-2 inhibitors, compositions containing them and uses thereof
EP4069678A1 (en) 2019-12-04 2022-10-12 Omeros Corporation Masp-2 inhibitors and methods of use
BR112022010895A2 (pt) 2019-12-04 2022-09-06 Omeros Corp Composto, composição farmacêutica, e, método para tratar uma doença ou distúrbio associado à serina protease-2 associada à lectina de ligação ao manan
TWI834025B (zh) 2020-03-06 2024-03-01 美商奥默羅斯公司 用於治療和/或預防冠狀病毒誘導的急性呼吸窘迫症候群的抑制masp-2的方法

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008085608A1 (en) * 2007-01-10 2008-07-17 Irm Llc Compounds and compositions as channel activating protease inhibitors
WO2012093101A1 (en) * 2011-01-04 2012-07-12 Novartis Ag Indole compounds or analogues thereof useful for the treatment of age-related macular degeneration (amd)
WO2015130784A1 (en) * 2014-02-25 2015-09-03 Achillion Pharmaceuticals, Inc. Alkyne compounds for treatment of complement mediated disorders
WO2019186164A1 (en) * 2018-03-29 2019-10-03 University Of Leeds Factor xiia inhibitors
WO2019211585A1 (en) * 2018-04-30 2019-11-07 University Of Leeds FACTOR XIIa INHIBITORS
WO2021032933A1 (en) * 2019-08-21 2021-02-25 Kalvista Pharmaceuticals Limited Enzyme inhibitors

Family Cites Families (76)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4331647A (en) 1980-03-03 1982-05-25 Goldenberg Milton David Tumor localization and therapy with labeled antibody fragments specific to tumor-associated markers
US4816567A (en) 1983-04-08 1989-03-28 Genentech, Inc. Recombinant immunoglobin preparations
US5453566A (en) 1986-03-28 1995-09-26 Calgene, Inc. Antisense regulation of gene expression in plant/cells
US4946778A (en) 1987-09-21 1990-08-07 Genex Corporation Single polypeptide chain binding molecules
US4987071A (en) 1986-12-03 1991-01-22 University Patents, Inc. RNA ribozyme polymerases, dephosphorylases, restriction endoribonucleases and methods
MC2115A1 (fr) 1987-12-15 1991-07-05 Gene Shears Pty Ltd Ribozynes
US5223409A (en) 1988-09-02 1993-06-29 Protein Engineering Corp. Directed evolution of novel binding proteins
GB8822492D0 (en) 1988-09-24 1988-10-26 Considine J Apparatus for removing tumours from hollow organs of body
US5211657A (en) 1988-11-07 1993-05-18 The United States Government As Represented By The Secretary Of The Department Of Health And Human Services Laminin a chain deduced amino acid sequence, expression vectors and active synthetic peptides
US5530101A (en) 1988-12-28 1996-06-25 Protein Design Labs, Inc. Humanized immunoglobulins
US5549910A (en) 1989-03-31 1996-08-27 The Regents Of The University Of California Preparation of liposome and lipid complex compositions
EP0438803B1 (en) 1990-01-26 1997-03-12 Immunomedics, Inc. Vaccines against cancer and infectious diseases
JP3218637B2 (ja) 1990-07-26 2001-10-15 大正製薬株式会社 安定なリポソーム水懸濁液
US5789573A (en) 1990-08-14 1998-08-04 Isis Pharmaceuticals, Inc. Antisense inhibition of ICAM-1, E-selectin, and CMV IE1/IE2
JP2958076B2 (ja) 1990-08-27 1999-10-06 株式会社ビタミン研究所 遺伝子導入用多重膜リポソーム及び遺伝子捕捉多重膜リポソーム製剤並びにその製法
IL108367A0 (en) 1993-01-27 1994-04-12 Hektoen Inst For Medical Resea Antisense polynzcleotide inhibition of human growth factor-sensitive cancer cells
SE9301911D0 (sv) 1993-06-03 1993-06-03 Ab Astra New peptide derivatives
SE9301916D0 (sv) 1993-06-03 1993-06-03 Ab Astra New peptides derivatives
US5801154A (en) 1993-10-18 1998-09-01 Isis Pharmaceuticals, Inc. Antisense oligonucleotide modulation of multidrug resistance-associated protein
IL112795A (en) 1994-03-04 2001-01-28 Astrazeneca Ab Peptide derivatives as antithrombic agents their preparation and pharmaceutical compositions containing them
US5741516A (en) 1994-06-20 1998-04-21 Inex Pharmaceuticals Corporation Sphingosomes for enhanced drug delivery
US5795587A (en) 1995-01-23 1998-08-18 University Of Pittsburgh Stable lipid-comprising drug delivery complexes and methods for their production
US5738868A (en) 1995-07-18 1998-04-14 Lipogenics Ltd. Liposome compositions and kits therefor
US5739119A (en) 1996-11-15 1998-04-14 Galli; Rachel L. Antisense oligonucleotides specific for the muscarinic type 2 acetylcholine receptor MRNA
US5866573A (en) 1997-04-21 1999-02-02 Merck & Co., Inc. Pyrazinone thrombin inhibitors
AU742178B2 (en) 1998-05-26 2001-12-20 Merck & Co., Inc. Imidazopyridine thrombin inhibitors
KR20000047461A (ko) 1998-12-29 2000-07-25 성재갑 트롬빈 억제제
AU3192500A (en) 1999-03-16 2000-10-04 C & C Research Laboratories Substituted proline derivatives and medicinal compositions containing the same
US7015230B1 (en) 1999-05-19 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
US6664255B1 (en) 1999-05-19 2003-12-16 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
CZ20014115A3 (cs) 1999-05-19 2002-05-15 Pharmacia Corporation Substituované polycyklické aryl a heteroaryl pyrazinony vhodné pro selektivní inhibici koagulační kaskády
US6653316B1 (en) 1999-05-19 2003-11-25 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
US20040072862A1 (en) 1999-06-04 2004-04-15 Bitler Catherine M. Compositions for treating ischemia-related neuronal damage
US6649592B1 (en) 2000-01-14 2003-11-18 Science & Technology Corporation @ Unm Peptide inhibitors of LFA-1/ICAM-1 interaction
WO2001079195A2 (en) 2000-04-14 2001-10-25 Corvas International, Inc. Pyridine and pyrazine derivatives as thrombin inhibitors
SG98393A1 (en) 2000-05-19 2003-09-19 Inst Materials Research & Eng Injectable drug delivery systems with cyclodextrin-polymer based hydrogels
AU2002230836A1 (en) 2000-12-18 2002-07-01 Merck & Co., Inc. Benzylamine derivatives and their use as thrombin inhibitors
MXPA04003167A (es) 2001-10-03 2004-07-08 Pharmacia Corp Compuestos heterociclicos insaturados de 6 miembros utiles para la inhibicion selectiva de la cascada de coagulacion.
JP2005509606A (ja) 2001-10-03 2005-04-14 ファルマシア・コーポレーション 凝血カスケードを選択的に阻害するのに有用な置換された多環式化合物のプロドラッグ
ES2601143T3 (es) 2002-07-19 2017-02-14 Omeros Corporation Copolímeros tribloque biodegradables, métodos de síntesis de los mismos, e hidrogeles y biomateriales preparados a partir de los mismos
WO2004032834A2 (en) 2002-10-04 2004-04-22 Merck & Co., Inc. Thrombin inhibitors
US7482376B2 (en) 2003-07-03 2009-01-27 3-Dimensional Pharmaceuticals, Inc. Conjugated complement cascade inhibitors
US20140056873A1 (en) 2004-06-10 2014-02-27 University Of Leicester Methods for Treating Conditions Associated with MASP-2 Dependent Complement Activation
US7919094B2 (en) 2004-06-10 2011-04-05 Omeros Corporation Methods for treating conditions associated with MASP-2 dependent complement activation
ES2631127T3 (es) 2004-06-10 2017-08-28 Omeros Corporation Métodos para tratar afecciones asociadas con la activación del complemento dependiente de MASP-2
US8840893B2 (en) 2004-06-10 2014-09-23 Omeros Corporation Methods for treating conditions associated with MASP-2 dependent complement activation
KR20080002832A (ko) * 2005-03-16 2008-01-04 얀센 파마슈티카 엔.브이. 보체 매개성 질병 및 이상을 치료하기 위한 신규한 티오펜설폭시민
TW201100441A (en) 2009-06-01 2011-01-01 Osi Pharm Inc Amino pyrimidine anticancer compounds
DK2488203T3 (en) 2009-10-16 2017-03-13 Omeros Corp METHODS OF TREATING DISSEMINATED INTRAVASCULAR COAGULATION BY INHIBITION OF MASP-2 DEPENDENT COMPLEMENT ACTIVATION
HUP1000366A2 (en) 2010-07-13 2012-03-28 Mta Enzimologiai Intezet Novel proteins, their production process and use tereof
US9644035B2 (en) 2011-04-08 2017-05-09 Omeros Corporation Methods for treating conditions associated with MASP-2 dependent complement activation
BR112013025917A2 (pt) 2011-04-08 2016-12-20 Omeros Corp uso de um anticorpo masp-2 ou fragmento do mesmo que inibe ativação de complemento dependente de masp-2
HUE049154T2 (hu) 2011-05-04 2020-09-28 Omeros Corp Készítmények a MASP-2-függõ komplement-aktiválás gátlására
AU2013201779B2 (en) 2011-05-04 2016-01-07 Omeros Corporation Compositions for inhibiting MASP-2 dependent complement activation
KR102668696B1 (ko) 2012-01-12 2024-05-29 예일 유니버시티 E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법
MX357540B (es) 2012-04-06 2018-07-13 Omeros Corp Composiciones y metodos para inhibir masp-1 y/o masp-2 y/o masp-3 para el tratamiento de la hemoglobinuria paroxistica nocturna.
BR112014031522A2 (pt) 2012-06-18 2017-08-01 Omeros Corp métodos para inibir a ativação de complemento dependente de masp-3, para inibir a ativação de complemento dependente de masp-2 e para fabricar um medicamento
AR091490A1 (es) 2012-06-19 2015-02-11 Bristol Myers Squibb Co Antagonistas de iap
EP2906236A1 (en) 2012-10-10 2015-08-19 Novo Nordisk Health Care AG Liquid pharmaceutical composition of factor vii polypeptide
EP2922535B1 (en) 2012-11-20 2021-11-10 Merck Sharp & Dohme Corp. Thrombin inhibitors
JP2016539919A (ja) 2013-10-17 2016-12-22 オメロス コーポレーション Masp−2依存性補体活性化に関連した状態を治療するための方法
CA2935683A1 (en) 2013-12-30 2015-07-09 Lifesci Pharmaceuticals, Inc. Therapeutic inhibitory compounds
AU2016354117B2 (en) 2015-11-09 2019-11-28 Omeros Corporation Methods for treating conditions associated with MASP-2 dependent complement activation
KR102528260B1 (ko) 2016-01-05 2023-05-04 유니버시티 오브 레스터 필요로 하는 대상체에서 섬유증의 억제 방법
US20170253667A1 (en) 2016-01-05 2017-09-07 University Of Leicester Methods for inhibiting fibrosis in a subject in need thereof
MX2018011648A (es) 2016-03-31 2019-01-30 Omeros Corp Metodos para la inhibicion de fibrosis en un sujeto en necesidad del mismo.
JOP20170170B1 (ar) 2016-08-31 2022-09-15 Omeros Corp صيغ لجسم مضاد تثبيطية لـ masp-2 بتركيز عالي ولزوجة منخفضة وأطقم، وطرق
US20180105604A1 (en) 2016-10-13 2018-04-19 University Of Leicester Methods for reducing proteinuria in a human subject suffering from immunoglobulin a nephropathy
TWI881481B (zh) 2017-08-15 2025-04-21 美商歐米諾斯公司 用於治療和/或預防與造血幹細胞移植有關的移植物抗宿主病和/或瀰漫性肺泡出血和/或靜脈閉塞性病的方法
PE20200924A1 (es) 2017-09-13 2020-09-14 Amgen Inc Compuestos de bisamida sustituida que activan el sarcomero cardiaco
IL311042B1 (en) 2018-05-29 2026-04-01 Omeros Corp MASP-2 inhibitors and methods of use
US11584714B2 (en) 2018-05-29 2023-02-21 Omeros Corporation MASP-2 inhibitors and methods of use
EP4069676A1 (en) * 2019-12-04 2022-10-12 Omeros Corporation Masp-2 inhibitors and methods of use
EP4069678A1 (en) 2019-12-04 2022-10-12 Omeros Corporation Masp-2 inhibitors and methods of use
IL293588B1 (en) 2019-12-04 2026-04-01 Omeros Corp 3-Amino-1-methylpyrazin-2(H1)-one derivatives as MASP-2 inhibitors, compositions containing them and uses thereof
BR112022010895A2 (pt) 2019-12-04 2022-09-06 Omeros Corp Composto, composição farmacêutica, e, método para tratar uma doença ou distúrbio associado à serina protease-2 associada à lectina de ligação ao manan

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008085608A1 (en) * 2007-01-10 2008-07-17 Irm Llc Compounds and compositions as channel activating protease inhibitors
WO2012093101A1 (en) * 2011-01-04 2012-07-12 Novartis Ag Indole compounds or analogues thereof useful for the treatment of age-related macular degeneration (amd)
WO2015130784A1 (en) * 2014-02-25 2015-09-03 Achillion Pharmaceuticals, Inc. Alkyne compounds for treatment of complement mediated disorders
WO2019186164A1 (en) * 2018-03-29 2019-10-03 University Of Leeds Factor xiia inhibitors
WO2019211585A1 (en) * 2018-04-30 2019-11-07 University Of Leeds FACTOR XIIa INHIBITORS
WO2021032933A1 (en) * 2019-08-21 2021-02-25 Kalvista Pharmaceuticals Limited Enzyme inhibitors

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
CAS Registry Entry 1348395-03-8, index name not yet assigned. 05 Dec 2011 *
CAS Registry Entry 1348431-17-3, index name not yet assigned. 04 Dec 2011 *
CAS Registry Entry 1348728-96-0, index name not yet assigned. 05 Dec 2011 *
CAS Registry Entry 1348730-54-0, index name not yet assigned. 04 Dec 2011 *

Also Published As

Publication number Publication date
EP4069676A1 (en) 2022-10-12
US20240317682A1 (en) 2024-09-26
US12030853B2 (en) 2024-07-09
US20210171461A1 (en) 2021-06-10
JP2023504541A (ja) 2023-02-03
US20250197349A1 (en) 2025-06-19
JP7721142B2 (ja) 2025-08-12
CA3159159A1 (en) 2021-06-10
AU2020395306A1 (en) 2022-06-30
WO2021113698A1 (en) 2021-06-10
US20240351980A1 (en) 2024-10-24

Similar Documents

Publication Publication Date Title
AU2020395306B2 (en) MASP-2 inhibitors and methods of use
AU2020398241B2 (en) MASP-2 inhibitors and methods of use
AU2020397894B2 (en) MASP-2 inhibitors and methods of use
AU2020396565B2 (en) MASP-2 inhibitors and methods of use
AU2023266363A1 (en) MASP-2 inhibitors and methods of use
TW202523310A (zh) Masp-2抑制劑及其使用方法
US20240228499A1 (en) Masp-2 inhibitors and methods of use

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)