JP7699389B2 - Ｍａｓｐ－２阻害剤および使用方法 - Google Patents

Ｍａｓｐ－２阻害剤および使用方法 Download PDF

Info

Publication number
JP7699389B2
JP7699389B2 JP2022533455A JP2022533455A JP7699389B2 JP 7699389 B2 JP7699389 B2 JP 7699389B2 JP 2022533455 A JP2022533455 A JP 2022533455A JP 2022533455 A JP2022533455 A JP 2022533455A JP 7699389 B2 JP7699389 B2 JP 7699389B2
Authority
JP
Japan
Prior art keywords
substituted
unsubstituted
compound
alkyl
aryl
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
JP2022533455A
Other languages
English (en)
Japanese (ja)
Other versions
JP2023504544A (ja
JP2023504544A5 (https=
Inventor
ニール エス． カッショール
ジェニファー リン ゲージ
ド ヨン クォン
トーマス エル． リトル
マーカス メッツ
フォン スペヒト ペーター クルト ノラート
ジェニファー ツォン
ジェレマイア エイチ． グエン
メリンダ デービス
ロベルト ウエルタ レムス
サントシュ クマール ケシペディ
サラ レベッカ ゴールドスタイン
Original Assignee
オメロス コーポレーション
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 オメロス コーポレーション filed Critical オメロス コーポレーション
Publication of JP2023504544A publication Critical patent/JP2023504544A/ja
Publication of JP2023504544A5 publication Critical patent/JP2023504544A5/ja
Application granted granted Critical
Publication of JP7699389B2 publication Critical patent/JP7699389B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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
    • C07D471/02—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 two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • C07D471/02—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 two hetero rings
    • C07D471/10—Spiro-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
    • C07D487/02—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—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

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)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2022533455A 2019-12-04 2020-12-04 Ｍａｓｐ－２阻害剤および使用方法 Active JP7699389B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962943599P 2019-12-04 2019-12-04
US62/943,599 2019-12-04
PCT/US2020/063379 WO2021113686A1 (en) 2019-12-04 2020-12-04 Masp-2 inhibitors and methods of use

Publications (3)

Publication Number Publication Date
JP2023504544A JP2023504544A (ja) 2023-02-03
JP2023504544A5 JP2023504544A5 (https=) 2023-11-21
JP7699389B2 true JP7699389B2 (ja) 2025-06-27

Family

ID=73854994

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2022533455A Active JP7699389B2 (ja) 2019-12-04 2020-12-04 Ｍａｓｐ－２阻害剤および使用方法

Country Status (10)

Country Link
US (4) US12110288B2 (https=)
EP (1) EP4069238A1 (https=)
JP (1) JP7699389B2 (https=)
KR (1) KR20220110531A (https=)
CN (1) CN115052604A (https=)
AU (1) AU2020396565C1 (https=)
BR (1) BR112022010890A2 (https=)
CA (1) CA3159176A1 (https=)
IL (1) IL293588B1 (https=)
WO (1) WO2021113686A1 (https=)

Families Citing this family (8)

* 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
BR112021018456A2 (pt) 2019-03-22 2021-11-23 Achillion Pharmaceuticals Inc Compostos farmacêuticos para o tratamento de distúrbios mediados por complemento
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
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
CN119768164A (zh) * 2022-08-11 2025-04-04 阿雷克森制药公司 用于治疗补体介导的病症的药物化合物
EP4626891A1 (en) * 2022-11-30 2025-10-08 Omeros Corporation Fused pyrimidines as masp-2 inhibitors

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001087851A1 (en) 2000-05-18 2001-11-22 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
JP2002516326A (ja) 1998-05-26 2002-06-04 メルク エンド カムパニー インコーポレーテッド イミダゾピリジン系トロンビン阻害薬
JP2002528543A (ja) 1998-10-30 2002-09-03 メルク エンド カムパニー インコーポレーテッド トロンビン阻害剤
JP2002544264A (ja) 1999-05-19 2002-12-24 ファルマシア・コーポレイション 凝固カスケードの選択的阻害に有用な置換多環式アリールおよびヘテロアリールピラジノン
JP2002544263A (ja) 1999-05-19 2002-12-24 ファルマシア・コーポレイション 抗凝血剤としての置換多環式アリールおよびヘテロアリールウラシル
JP2002544262A (ja) 1999-05-19 2002-12-24 ファルマシア・コーポレイション 有用な抗凝血剤としての置換多環式アリールおよびヘテロアリールピリミジノン
JP2004509067A (ja) 2000-05-18 2004-03-25 ファルマシア・コーポレーション 凝固カスケードの選択的阻害に有用な置換多環式アリールとヘテロアリールピラジノン
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
JP2005514332A (ja) 2001-10-03 2005-05-19 ファルマシア・コーポレーション 凝固カスケードの選択阻害に有用な６員不飽和複素環式化合物

Family Cites Families (75)

* 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
US6011158A (en) 1994-12-13 2000-01-04 Corvas International, Inc. Aromatic heterocyclic derivatives as enzyme inhibitors
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
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
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
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
US7919094B2 (en) 2004-06-10 2011-04-05 Omeros Corporation Methods for treating conditions associated with MASP-2 dependent complement activation
US8840893B2 (en) 2004-06-10 2014-09-23 Omeros Corporation Methods for treating conditions associated with MASP-2 dependent complement activation
US20140056873A1 (en) 2004-06-10 2014-02-27 University Of Leicester 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
KR20080002832A (ko) * 2005-03-16 2008-01-04 얀센 파마슈티카 엔.브이. 보체 매개성 질병 및 이상을 치료하기 위한 신규한 티오펜설폭시민
RS51644B (sr) 2007-01-10 2011-10-31 Irm Llc. Jedinjenja i preparati kao inhibitori kanal aktivirajuće proteaze
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
GB201805174D0 (en) 2018-03-29 2018-05-16 Univ Leeds Innovations Ltd Compounds
GB201807014D0 (en) 2018-04-30 2018-06-13 Univ Leeds Innovations Ltd Factor xlla inhibitors
US11584714B2 (en) 2018-05-29 2023-02-21 Omeros Corporation MASP-2 inhibitors and methods of use
IL311042B1 (en) 2018-05-29 2026-04-01 Omeros Corp MASP-2 inhibitors and methods of use
EP4069678A1 (en) 2019-12-04 2022-10-12 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
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
WO2022035997A1 (en) 2020-08-11 2022-02-17 Avilar Therapeutics, Inc. In vivo assembly of asgpr binding therapeutics

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002516326A (ja) 1998-05-26 2002-06-04 メルク エンド カムパニー インコーポレーテッド イミダゾピリジン系トロンビン阻害薬
JP2002528543A (ja) 1998-10-30 2002-09-03 メルク エンド カムパニー インコーポレーテッド トロンビン阻害剤
JP2002544264A (ja) 1999-05-19 2002-12-24 ファルマシア・コーポレイション 凝固カスケードの選択的阻害に有用な置換多環式アリールおよびヘテロアリールピラジノン
JP2002544263A (ja) 1999-05-19 2002-12-24 ファルマシア・コーポレイション 抗凝血剤としての置換多環式アリールおよびヘテロアリールウラシル
JP2002544262A (ja) 1999-05-19 2002-12-24 ファルマシア・コーポレイション 有用な抗凝血剤としての置換多環式アリールおよびヘテロアリールピリミジノン
WO2001087851A1 (en) 2000-05-18 2001-11-22 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
JP2004509067A (ja) 2000-05-18 2004-03-25 ファルマシア・コーポレーション 凝固カスケードの選択的阻害に有用な置換多環式アリールとヘテロアリールピラジノン
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
JP2005514332A (ja) 2001-10-03 2005-05-19 ファルマシア・コーポレーション 凝固カスケードの選択阻害に有用な６員不飽和複素環式化合物

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
PARLOW, J. J. et al.，Design, Parallel Synthesis, and Crystal Structures of Pyrazinone Antithrombotics as Selective Inhibitors of the Tissue Factor VIIa Complex，Journal of Medicinal Chemistry，2003年，Vol.46, No.19，pp.4050-4062，DOI:10.1021/jm030131l
SANDERSON, P. E. et al.，Azaindoles: moderately basic P1 groups for enhancing the selectivity of thrombin inhibitors，Bioorganic & Medicinal Chemistry Letters，2003年，Vol.13, No.5，pp.795-798
コロンビア特許出願公開5160330号明細書，2002年05月30日，CA 2021:953157
大熊浩一、他，血液凝固系と補体系のクロストーク，血栓止血誌，2011年，Vol.2, No.4，pp.171-185
遠藤雄一，補体クレアチン経路と凝固系の協調作用－補体系研究の新展開，血栓止血誌，2011年，Vol.22, No.4，pp.164-170

Also Published As

Publication number Publication date
US20250243198A1 (en) 2025-07-31
BR112022010890A2 (pt) 2022-08-16
JP2023504544A (ja) 2023-02-03
IL293588B1 (en) 2026-04-01
CA3159176A1 (en) 2021-06-10
CN115052604A (zh) 2022-09-13
AU2020396565C1 (en) 2025-05-15
AU2024223991A1 (en) 2024-10-24
IL293588A (en) 2022-08-01
WO2021113686A1 (en) 2021-06-10
EP4069238A1 (en) 2022-10-12
KR20220110531A (ko) 2022-08-08
US20240391917A1 (en) 2024-11-28
US20210179612A1 (en) 2021-06-17
US12110288B2 (en) 2024-10-08
AU2020396565B2 (en) 2025-01-09
US20250011323A1 (en) 2025-01-09
AU2020396565A1 (en) 2022-06-30

Similar Documents

Publication Publication Date Title
JP7699389B2 (ja) Ｍａｓｐ－２阻害剤および使用方法
JP7737153B2 (ja) Ｍａｓｐ－２阻害剤および使用方法
JP7721143B2 (ja) Ｍａｓｐ－２阻害剤および使用方法
JP7721142B2 (ja) Ｍａｓｐ－２阻害剤および使用方法
WO2019231935A1 (en) Masp-2 inhibitors and methods of use
AU2024223991B2 (en) MASP-2 inhibitors and methods of use
US20240228499A1 (en) Masp-2 inhibitors and methods of use
US20250122225A1 (en) Masp-2 inhibitors and methods of use

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20220808

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20221021

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20231113

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20231113

RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20240215

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20241017

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20241108

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20250206

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20250217

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20250519

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20250610

R150 Certificate of patent or registration of utility model

Ref document number: 7699389

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150