KR20220132593A - 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 PDFInfo
- Publication number
- KR20220132593A KR20220132593A KR1020227029272A KR20227029272A KR20220132593A KR 20220132593 A KR20220132593 A KR 20220132593A KR 1020227029272 A KR1020227029272 A KR 1020227029272A KR 20227029272 A KR20227029272 A KR 20227029272A KR 20220132593 A KR20220132593 A KR 20220132593A
- Authority
- KR
- South Korea
- Prior art keywords
- alkyl
- alkanediyl
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- cycloalkyl
- moiety
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- Ceased
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Classifications
-
- 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
- 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
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
- C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
- C07K16/28—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
- C07K16/2803—Immunoglobulins [IG], 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
- C07K16/2818—Immunoglobulins [IG], 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
- C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
- C07K16/28—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
- C07K16/2803—Immunoglobulins [IG], 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
- C07K16/2827—Immunoglobulins [IG], 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 B7 molecules, e.g. CD80, CD86
-
- 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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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Immunology (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202062966144P | 2020-01-27 | 2020-01-27 | |
| US62/966,144 | 2020-01-27 | ||
| US202063058230P | 2020-07-29 | 2020-07-29 | |
| US63/058,230 | 2020-07-29 | ||
| PCT/US2021/014980 WO2021154666A1 (en) | 2020-01-27 | 2021-01-26 | 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20220132593A true KR20220132593A (ko) | 2022-09-30 |
Family
ID=74595468
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020227029272A Ceased KR20220132593A (ko) | 2020-01-27 | 2021-01-26 | 톨-유사 수용체 7 (TLR7) 효능제로서의 1H-피라졸로[4,3-d]피리미딘 화합물 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20230348468A1 (https=) |
| EP (1) | EP4097100A1 (https=) |
| JP (1) | JP2023512206A (https=) |
| KR (1) | KR20220132593A (https=) |
| CN (1) | CN115151548A (https=) |
| WO (1) | WO2021154666A1 (https=) |
Families Citing this family (4)
| 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 |
| 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 |
| CN115279765B (zh) * | 2020-01-27 | 2024-11-12 | 百时美施贵宝公司 | 作为Toll样受体7(TLR7)激动剂的1H-吡唑并[4,3-d]嘧啶化合物 |
Family Cites Families (51)
| 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 |
| 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 |
| 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 |
| US20120003298A1 (en) | 2010-04-30 | 2012-01-05 | Alcide Barberis | Methods for inducing an immune response |
| 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 |
| AU2011247358B2 (en) | 2010-04-30 | 2014-10-30 | Urogen Pharma Ltd. | Phospholipid drug analogs |
| 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 |
| 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 |
| ES2908150T3 (es) | 2014-05-01 | 2022-04-27 | Novartis Ag | Compuestos y composiciones como agonistas del receptor de tipo Toll 7 |
| PL3137470T3 (pl) | 2014-05-01 | 2021-10-11 | Novartis Ag | Związki i kompozycje jako agonisty receptora toll-like 7 |
| 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 |
| US11028090B2 (en) | 2017-01-26 | 2021-06-08 | Dong Wha Pharm. Co., Ltd. | [1,2,4]Triazolo[4,3-a]quinoxaline derivative, method for preparing same, and pharmaceutical composition for preventing or treating BET protein-related diseases, containing same as active ingredient |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
-
2021
- 2021-01-26 EP EP21705396.6A patent/EP4097100A1/en not_active Withdrawn
- 2021-01-26 WO PCT/US2021/014980 patent/WO2021154666A1/en not_active Ceased
- 2021-01-26 JP JP2022545790A patent/JP2023512206A/ja active Pending
- 2021-01-26 KR KR1020227029272A patent/KR20220132593A/ko not_active Ceased
- 2021-01-26 CN CN202180016904.1A patent/CN115151548A/zh active Pending
- 2021-01-26 US US17/793,278 patent/US20230348468A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| WO2021154666A1 (en) | 2021-08-05 |
| EP4097100A1 (en) | 2022-12-07 |
| US20230348468A1 (en) | 2023-11-02 |
| CN115151548A (zh) | 2022-10-04 |
| JP2023512206A (ja) | 2023-03-24 |
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