TW201623279A - ＴＧＦ－β抑制劑及使用方法 - Google Patents

ＴＧＦ－β抑制劑及使用方法 Download PDF

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TW201623279A
TW201623279A TW104111332A TW104111332A TW201623279A TW 201623279 A TW201623279 A TW 201623279A TW 104111332 A TW104111332 A TW 104111332A TW 104111332 A TW104111332 A TW 104111332A TW 201623279 A TW201623279 A TW 201623279A
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alkyl
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TW104111332A
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拉金徳 辛
索瑪塞克哈 巴米迪帕堤
丁平羽
唐納 帕彥
馬里納 吉爾曼
陶德 金塞拉
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雷傑製藥公司
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    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/535—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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
    • A61K31/635—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
    • 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
    • A61K31/695—Silicon compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/39541—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against normal tissues, cells
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    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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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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    • C07D401/14—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
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    • 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
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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    • 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
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    • 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
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/0803—Compounds with Si-C or Si-Si linkages
    • C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
    • C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
    • C—CHEMISTRY; METALLURGY
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    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
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    • C07K16/2818—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against CD28 or CD152
    • A—HUMAN NECESSITIES
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
TW104111332A 2014-04-08 2015-04-08 ＴＧＦ－β抑制劑及使用方法 TW201623279A (zh)

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US201461976880P 2014-04-08 2014-04-08
US201462019577P 2014-07-01 2014-07-01

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US (2) US10233170B2 (Direct)
EP (1) EP3129367B1 (Direct)
JP (2) JP6767875B2 (Direct)
CN (1) CN106536507B (Direct)
ES (1) ES2759240T3 (Direct)
TW (1) TW201623279A (Direct)
UY (1) UY36068A (Direct)
WO (1) WO2015157093A1 (Direct)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106536507B (zh) * 2014-04-08 2020-04-07 里格尔药品股份有限公司 作为TGF-β抑制剂的2,3-二取代的吡啶化合物及其使用方法
US9981944B2 (en) * 2015-02-20 2018-05-29 Rigel Pharmaceuticals, Inc GDF-8 inhibitors
HK1255330A1 (zh) 2015-08-26 2019-08-16 缆图药品公司 适用於治疗与ntrk相关的病症的化合物和组合物
WO2017087778A1 (en) * 2015-11-19 2017-05-26 Blueprint Medicines Corporation Compounds and compositions useful for treating disorders related to ntrk
AU2016361441B2 (en) * 2015-11-25 2021-08-12 Convergene Llc Bicyclic BET bromodomain inhibitors and uses thereof
CN115969854B (zh) * 2016-03-24 2025-12-23 科瑞华生物技术有限公司 用tg02治疗癌症
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
US11352328B2 (en) 2016-07-12 2022-06-07 Arisan Therapeutics Inc. Heterocyclic compounds for the treatment of arenavirus
WO2018081401A1 (en) * 2016-10-26 2018-05-03 Ichan School Of Medicine At Mount Sinai Method for increasing cell proliferation in pancreatic beta cells, treatmen t method.and composition
ES2928773T3 (es) 2017-01-17 2022-11-22 Heparegenix Gmbh Inhibidores de proteína cinasas para fomentar la regeneración hepática o reducir o prevenir la muerte de hepatocitos
CN110431134A (zh) * 2017-01-23 2019-11-08 锐新医药公司 作为变构shp2抑制剂的吡啶化合物
WO2018161876A1 (zh) * 2017-03-08 2018-09-13 中国科学院上海药物研究所 二氢喹喔啉类溴结构域识别蛋白抑制剂及制备方法和用途
CN107118210A (zh) * 2017-04-28 2017-09-01 贵州大学 一种3‑碘‑6‑（三氟甲基）咪唑并[1,2‑a]吡啶的制备工艺
US11547712B2 (en) 2017-11-20 2023-01-10 Icahn School Of Medicine At Mount Sinai Kinase inhibitor compounds and compositions and methods of use
CN111819193A (zh) 2018-01-05 2020-10-23 西奈山伊坎医学院 增加胰腺β细胞增殖的方法、治疗方法以及组合物
WO2019183245A1 (en) 2018-03-20 2019-09-26 Icahn School Of Medicine At Mount Sinai Kinase inhibitor compounds and compositions and methods of use
US12419865B2 (en) 2018-12-06 2025-09-23 Arisan Therapeutics Inc. Compounds for the treatment of arenavirus infection
BR112021007006A2 (pt) 2018-12-27 2021-08-10 Nexys Therapeutics, Inc. derivados de (piridin-2-il)amina como inibidores de tgf-beta r1(alk5) para o tratamento de câncer
WO2020135195A1 (zh) * 2018-12-28 2020-07-02 四川科伦博泰生物医药股份有限公司 氨基吡啶类化合物及其制备方法和用途
EP3949708A4 (en) 2019-03-29 2022-12-07 Sumitomo Chemical Company, Limited HETEROCYCLIC COMPOUND AND COMPOSITION FOR COMBATING HARMFUL ARTHROPODS THEREOF
MA55804A (fr) 2019-04-29 2022-04-06 Solent Therapeutics Llc Dérivés de 1,1-dioxyde de 3-amino-4h-benzo[e][1,2,4]thiadiazine en tant qu'inhibiteurs de mrgx2
WO2021138391A1 (en) 2019-12-30 2021-07-08 Tyra Biosciences, Inc. Indazole compounds
WO2021254464A1 (zh) * 2020-06-19 2021-12-23 南京红云生物科技有限公司 取代喹唑啉类化合物、其制备方法、药物组合及应用
US20230234935A1 (en) * 2020-06-26 2023-07-27 Icahn School Of Medicine At Mount Sinai Kinase inhibitor compounds and compositions and methods of use
JP7704770B2 (ja) 2020-09-30 2025-07-08 住友化学株式会社 複素環化合物及びそれを含有する有害節足動物防除組成物
CN112225736B (zh) * 2020-11-12 2022-04-15 山东省科学院菏泽分院 一种6-溴咪唑并[1.2-a]吡啶-3-甲醛的制备方法
WO2022246025A1 (en) * 2021-05-20 2022-11-24 Dana-Farber Cancer Institute, Inc. Inhibitors and degraders of pip4k protein
CN113416181B (zh) * 2021-08-02 2022-05-03 四川大学 喹唑啉类衍生物及其用途
CN114292259B (zh) * 2021-11-30 2023-06-27 西安交通大学 4-氨基酸侧链取代的喹唑啉衍生物及其应用
EP4444421A2 (en) * 2021-12-10 2024-10-16 Prothena Biosciences Limited Heterocyclic compounds as dyrk1a inhibitors
WO2024071393A1 (ja) 2022-09-30 2024-04-04 住友化学株式会社 複素環化合物及びそれを含有する有害節足動物防除組成物
TW202423290A (zh) 2022-11-04 2024-06-16 日商住友化學股份有限公司 雜環化合物及含有其之有害節肢動物防除組合物

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7320789B2 (en) * 2001-09-26 2008-01-22 Wyeth Antibody inhibitors of GDF-8 and uses thereof
EP1720855A4 (en) * 2004-03-02 2008-12-17 Smithkline Beecham Corp HEMMER OF ACT ACTIVITY
EP1804801A2 (en) * 2004-10-15 2007-07-11 Biogen Idec MA, Inc. Methods of treating vascular injuries
US9259426B2 (en) * 2006-07-20 2016-02-16 Gilead Sciences, Inc. 4,6-di- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections
US8143253B2 (en) 2007-07-26 2012-03-27 Novartis Ag Organic compounds
WO2009032653A1 (en) 2007-08-31 2009-03-12 Smith Kline Beecham Corporation Inhibitors of akt activity
JP5675850B2 (ja) * 2010-02-05 2015-02-25 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ ヘタリール−［１，８］ナフチリジン誘導体
US9051318B2 (en) * 2011-03-09 2015-06-09 Merck Patent Gmbh Pyrido [2, 3-B] pyrazine compounds and their therapeutical uses such as for inhibiting ATP consuming proteins and treating diseases associated therewith
PT2731949T (pt) * 2011-07-13 2018-06-15 Tiumbio Co Ltd Imidazóis substituídos com 2-piridilo como inibidores de alk5 e/ou alk4
EP2903978B1 (en) 2012-10-05 2022-12-07 Rigel Pharmaceuticals, Inc. Gdf-8 inhibitors
CN106536507B (zh) * 2014-04-08 2020-04-07 里格尔药品股份有限公司 作为TGF-β抑制剂的2,3-二取代的吡啶化合物及其使用方法

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WO2015157093A1 (en) 2015-10-15
JP2017515802A (ja) 2017-06-15
US20190284155A1 (en) 2019-09-19
ES2759240T3 (es) 2020-05-08
US20170096409A1 (en) 2017-04-06
US10233170B2 (en) 2019-03-19
CN106536507B (zh) 2020-04-07
EP3129367B1 (en) 2019-09-04
US10858335B2 (en) 2020-12-08
JP6767875B2 (ja) 2020-10-14
JP2019196387A (ja) 2019-11-14
EP3129367A1 (en) 2017-02-15
UY36068A (es) 2015-10-30

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