KR20220132601A - 톨-유사 수용체 7 (TLR7) 효능제로서의 1H-피라졸로[4,3-d]피리미딘 화합물 - Google Patents

톨-유사 수용체 7 (TLR7) 효능제로서의 1H-피라졸로[4,3-d]피리미딘 화합물 Download PDF

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KR20220132601A
KR20220132601A KR1020227029360A KR20227029360A KR20220132601A KR 20220132601 A KR20220132601 A KR 20220132601A KR 1020227029360 A KR1020227029360 A KR 1020227029360A KR 20227029360 A KR20227029360 A KR 20227029360A KR 20220132601 A KR20220132601 A KR 20220132601A
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mmol
methyl
alkyl
alkanediyl
cancer
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Korean (ko)
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얌 비. 포우델
매튜 콕스
리치 헤
아쉬비니쿠마르 브이. 가바이
산지브 강와르
마티아스 브뢰케마
크리스틴 엠. 타비
무루가이아 안다판 무루가이아 수바이아
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브리스톨-마이어스 스큅 컴퍼니
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    • 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
    • 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
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • 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
    • A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Microbiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Mycology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020227029360A 2020-01-27 2021-01-26 톨-유사 수용체 7 (TLR7) 효능제로서의 1H-피라졸로[4,3-d]피리미딘 화합물 Ceased KR20220132601A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202062966119P 2020-01-27 2020-01-27
US62/966,119 2020-01-27
PCT/US2021/014982 WO2021154668A1 (en) 2020-01-27 2021-01-26 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS

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KR20220132601A true KR20220132601A (ko) 2022-09-30

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KR1020227029360A Ceased KR20220132601A (ko) 2020-01-27 2021-01-26 톨-유사 수용체 7 (TLR7) 효능제로서의 1H-피라졸로[4,3-d]피리미딘 화합물

Country Status (6)

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US (1) US20230041738A1 (enExample)
EP (1) EP4097106A1 (enExample)
JP (1) JP2023512207A (enExample)
KR (1) KR20220132601A (enExample)
CN (1) CN115151547A (enExample)
WO (1) WO2021154668A1 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021154661A1 (en) * 2020-01-27 2021-08-05 Bristol-Myers Squibb Company 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS
WO2021154662A1 (en) * 2020-01-27 2021-08-05 Bristol-Myers Squibb Company 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS
EP4097104A1 (en) * 2020-01-27 2022-12-07 Bristol-Myers Squibb Company 1h-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (tlr7) agonists
EP4097105A1 (en) * 2020-01-27 2022-12-07 Bristol-Myers Squibb Company 1h-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (tlr7) agonists
AR122043A1 (es) * 2020-05-12 2022-08-03 Bristol Myers Squibb Co Dosificación y administración del anticuerpo anti-ctla-4 activable

Family Cites Families (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2232871T3 (es) 1996-07-03 2005-06-01 Sumitomo Pharmaceuticals Company, Limited Nuevos derivados de purina.
TW572758B (en) 1997-12-22 2004-01-21 Sumitomo Pharma Type 2 helper T cell-selective immune response inhibitors comprising purine derivatives
US7157465B2 (en) 2001-04-17 2007-01-02 Dainippon Simitomo Pharma Co., Ltd. Adenine derivatives
WO2003037860A2 (en) 2001-10-30 2003-05-08 Conforma Therapeutics Corporation Purine analogs having hsp90-inhibiting activity
US20070142449A1 (en) * 2002-03-29 2007-06-21 Yung Shin Pharmaceutical Ind. Co., Ltd. Angiogenesis inhibitors
MXPA05003193A (es) 2002-09-27 2005-06-08 Sumitomo Pharma Compuesto de adenina novedoso y uso del mismo.
JP2004137157A (ja) 2002-10-16 2004-05-13 Sumitomo Pharmaceut Co Ltd 新規アデニン誘導体を有効成分として含有する医薬
GB0327319D0 (en) * 2003-11-24 2003-12-24 Pfizer Ltd Novel pharmaceuticals
WO2005092892A1 (ja) 2004-03-26 2005-10-06 Dainippon Sumitomo Pharma Co., Ltd. ８−オキソアデニン化合物
AU2006242920A1 (en) 2005-05-04 2006-11-09 Pfizer Limited 2-amido-6-amino-8-oxopurine derivatives as Toll-Like receptor modulators for the treatment of cancer and viral infections, such as hepatitis C
JP4584335B2 (ja) 2005-09-02 2010-11-17 ファイザー・インク ヒドロキシ置換１ｈ−イミダゾピリジンおよび方法
US20090105212A1 (en) 2005-09-22 2009-04-23 Dainippon Sumitomo Pharma Co., Ltd. a corporation of Japan Novel adenine compound
JPWO2007034817A1 (ja) 2005-09-22 2009-03-26 大日本住友製薬株式会社 新規アデニン化合物
JP2009528989A (ja) 2006-02-17 2009-08-13 ファイザー・リミテッド Ｔｌｒ７変調剤としての３−デアザプリン誘導体
CN101790380B (zh) 2007-02-07 2013-07-10 加利福尼亚大学董事会 合成tlr激动剂的缀合物及其应用
AR065784A1 (es) 2007-03-20 2009-07-01 Dainippon Sumitomo Pharma Co Derivados de 8-oxo adenina,medicamentos que los contienen y usos como agentes terapeuticos para enfermedades alergicas, antivirales o antibacterianas.
EP2132207A2 (en) 2007-03-23 2009-12-16 Amgen Inc. Heterocyclic compounds and their uses
CA2691444C (en) 2007-06-29 2016-06-14 Gilead Sciences, Inc. Purine derivatives and their use as modulators of toll-like receptor 7
ES2359123T3 (es) 2007-08-03 2011-05-18 Pfizer Limited Imidazopiridinonas.
RS53347B (sr) 2008-12-09 2014-10-31 Gilead Sciences, Inc. Modulatori toll-sličnih receptora
KR20110117705A (ko) 2009-02-11 2011-10-27 더 리전트 오브 더 유니버시티 오브 캘리포니아 톨-유사 수용체 조정제 및 질병의 치료
JP5694345B2 (ja) 2009-10-22 2015-04-01 ギリアード サイエンシーズ， インコーポレイテッド Ｔｏｌｌ様受容体の調節因子
AU2011247358B2 (en) 2010-04-30 2014-10-30 Urogen Pharma Ltd. Phospholipid drug analogs
JP2013525431A (ja) 2010-04-30 2013-06-20 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア 合成ｔｌｒ７アゴニストのリン脂質結合体の使用
US20120003298A1 (en) 2010-04-30 2012-01-05 Alcide Barberis Methods for inducing an immune response
WO2012038058A1 (en) 2010-09-21 2012-03-29 Telormedix Sa Treatment of conditions by toll-like receptor modulators
TW201247706A (en) 2011-03-08 2012-12-01 Baylor Res Inst Novel vaccine adjuvants based on targeting adjuvants to antibodies directly to antigen-presenting cells
JP6349256B2 (ja) 2011-11-09 2018-06-27 ヤンセン・サイエンシズ・アイルランド・ユーシー ウイルス感染の治療のためのプリン誘導体
EA035790B1 (ru) 2012-07-13 2020-08-11 Янссен Сайенсиз Айрлэнд Юси Макроциклические пурины для лечения вирусных инфекций
EA026354B1 (ru) 2012-08-24 2017-03-31 ГЛАКСОСМИТКЛАЙН ЭлЭлСи Пиразолопиримидиновые соединения
DK2906563T3 (en) 2012-10-10 2018-06-06 Janssen Sciences Ireland Uc PYRROLO [3,2-D] PYRIMIDINE DERIVATIVES FOR TREATING VIRUS INFECTIONS AND OTHER DISEASES
EP2732825B1 (en) 2012-11-19 2015-07-01 Invivogen Conjugates of a TLR7 and/or TLR8 agonist and a TLR2 agonist
US9295732B2 (en) 2013-02-22 2016-03-29 Invivogen Conjugated TLR7 and/or TLR8 and TLR2 polycationic agonists
CN110590809B (zh) 2013-03-29 2022-04-19 爱尔兰詹森科学公司 用于治疗病毒感染的大环脱氮-嘌呤酮
PT3030563T (pt) 2013-06-27 2017-11-15 Janssen Sciences Ireland Uc Derivados de pirrolo[3,2-d]pirimidina para o tratamento de infeções virais e outras doenças
EP3033089A2 (en) 2013-08-16 2016-06-22 The Regents of The University of California Uses of phospholipid conjugates of synthetic tlr7 agonists
WO2015036044A1 (en) 2013-09-13 2015-03-19 Telormedix Sa Cationic lipid vehicles for delivery of tlr7 agonists for specific targeting of human cd14+ monocytes in whole blood
PL3137470T3 (pl) 2014-05-01 2021-10-11 Novartis Ag Związki i kompozycje jako agonisty receptora toll-like 7
ES2908150T3 (es) 2014-05-01 2022-04-27 Novartis Ag Compuestos y composiciones como agonistas del receptor de tipo Toll 7
US9917227B1 (en) 2014-05-07 2018-03-13 Soraa, Inc. Controlling oxygen concentration levels during processing of highly-reflective contacts
HRP20210927T1 (hr) 2014-08-15 2021-09-03 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Spojevi pirolopirimidina koje se koriste kao agonist tlr7
CN105732635A (zh) 2014-12-29 2016-07-06 南京明德新药研发股份有限公司 一类Toll样受体7激动剂
EP3368092B9 (en) 2015-10-29 2020-07-29 Novartis AG Antibody conjugates comprising toll-like receptor agonist
UA121345C2 (uk) 2015-11-05 2020-05-12 Чіа Тай Тяньцин Фармасьютікал Груп Ко., Лтд. 7-(тіазол-5-іл)піролопіримідин як агоніст рецептора tlr7
CA3025746A1 (en) 2016-06-16 2017-12-21 Janssen Pharmaceutica Nv Azabenzimidazole derivatives as pi3k beta inhibitors
WO2018095426A1 (zh) * 2016-11-28 2018-05-31 江苏恒瑞医药股份有限公司 吡唑并杂芳基类衍生物、其制备方法及其在医药上的应用
US10472361B2 (en) * 2017-08-16 2019-11-12 Bristol-Myers Squibb Company Toll-like receptor 7 (TLR7) agonists having a benzotriazole moiety, conjugates thereof, and methods and uses therefor
US10487084B2 (en) * 2017-08-16 2019-11-26 Bristol-Myers Squibb Company Toll-like receptor 7 (TLR7) agonists having a heterobiaryl moiety, conjugates thereof, and methods and uses therefor
US10457681B2 (en) 2017-08-16 2019-10-29 Bristol_Myers Squibb Company Toll-like receptor 7 (TLR7) agonists having a tricyclic moiety, conjugates thereof, and methods and uses therefor
US10508115B2 (en) * 2017-08-16 2019-12-17 Bristol-Myers Squibb Company Toll-like receptor 7 (TLR7) agonists having heteroatom-linked aromatic moieties, conjugates thereof, and methods and uses therefor
US10494370B2 (en) 2017-08-16 2019-12-03 Bristol-Myers Squibb Company Toll-like receptor 7 (TLR7) agonists having a pyridine or pyrazine moiety, conjugates thereof, and methods and uses therefor
CN111757755A (zh) 2017-12-21 2020-10-09 大日本住友制药株式会社 包含tlr7激动剂的组合药物
WO2019209811A1 (en) 2018-04-24 2019-10-31 Bristol-Myers Squibb Company Macrocyclic toll-like receptor 7 (tlr7) agonists
US11554120B2 (en) * 2018-08-03 2023-01-17 Bristol-Myers Squibb Company 1H-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (TLR7) agonists and methods and uses therefor

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WO2021154668A1 (en) 2021-08-05
EP4097106A1 (en) 2022-12-07
JP2023512207A (ja) 2023-03-24
US20230041738A1 (en) 2023-02-09
CN115151547A (zh) 2022-10-04

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