JP5763077B2 - トール様受容体のモジュレーター - Google Patents
トール様受容体のモジュレーター Download PDFInfo
- Publication number
- JP5763077B2 JP5763077B2 JP2012528926A JP2012528926A JP5763077B2 JP 5763077 B2 JP5763077 B2 JP 5763077B2 JP 2012528926 A JP2012528926 A JP 2012528926A JP 2012528926 A JP2012528926 A JP 2012528926A JP 5763077 B2 JP5763077 B2 JP 5763077B2
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- heteroalkyl
- heterocyclyl
- 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
Links
- 0 CCCCOc(nc1N)cc(N(CC2=CC=C([C@](*C)C=CC(CN3CCCC3)=C)[C@@](CC)C2)C2=O)c1NC2=O Chemical compound CCCCOc(nc1N)cc(N(CC2=CC=C([C@](*C)C=CC(CN3CCCC3)=C)[C@@](CC)C2)C2=O)c1NC2=O 0.000 description 5
- GNOUIXFCVVMFKH-UHFFFAOYSA-N C=NCc1ccc(C2C=C(CN3CCCC3)C=CC2)cc1 Chemical compound C=NCc1ccc(C2C=C(CN3CCCC3)C=CC2)cc1 GNOUIXFCVVMFKH-UHFFFAOYSA-N 0.000 description 1
- AKQLICZDOCQKRA-UHFFFAOYSA-N CC1(C)OB(c2cc(CN3CCCC3)ccc2)OC1(C)C Chemical compound CC1(C)OB(c2cc(CN3CCCC3)ccc2)OC1(C)C AKQLICZDOCQKRA-UHFFFAOYSA-N 0.000 description 1
- AJRWXBRPWUDPBK-AWQFTUOYSA-N CCCCOC/C=C(\C(N1)=C(N)N)/N(Cc2cccc(CN3CCCC3)c2)CC1=O Chemical compound CCCCOC/C=C(\C(N1)=C(N)N)/N(Cc2cccc(CN3CCCC3)c2)CC1=O AJRWXBRPWUDPBK-AWQFTUOYSA-N 0.000 description 1
- HNIWUOUJDMLJCR-BBYZMDQCSA-N NC(CCCCCC1)/C=C\C=C1\C1=C=C1 Chemical compound NC(CCCCCC1)/C=C\C=C1\C1=C=C1 HNIWUOUJDMLJCR-BBYZMDQCSA-N 0.000 description 1
- PKVISXNITYTURG-UHFFFAOYSA-N NCc1ccc(CCN2CCCC2)cc1 Chemical compound NCc1ccc(CCN2CCCC2)cc1 PKVISXNITYTURG-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
- A61P11/02—Nasal agents, e.g. decongestants
-
- 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
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Pulmonology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Biotechnology (AREA)
- Otolaryngology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24219409P | 2009-09-14 | 2009-09-14 | |
| US61/242,194 | 2009-09-14 | ||
| PCT/US2010/048424 WO2011031965A1 (en) | 2009-09-14 | 2010-09-10 | Modulators of toll-like receptors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013504593A JP2013504593A (ja) | 2013-02-07 |
| JP2013504593A5 JP2013504593A5 (enExample) | 2013-10-31 |
| JP5763077B2 true JP5763077B2 (ja) | 2015-08-12 |
Family
ID=43332257
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012528926A Active JP5763077B2 (ja) | 2009-09-14 | 2010-09-10 | トール様受容体のモジュレーター |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US8476270B2 (enExample) |
| EP (1) | EP2477987B1 (enExample) |
| JP (1) | JP5763077B2 (enExample) |
| AU (1) | AU2010292102B2 (enExample) |
| CA (1) | CA2772253C (enExample) |
| ES (1) | ES2661850T3 (enExample) |
| NO (1) | NO2477987T3 (enExample) |
| NZ (1) | NZ598384A (enExample) |
| PL (1) | PL2477987T3 (enExample) |
| PT (1) | PT2477987T (enExample) |
| SI (1) | SI2477987T1 (enExample) |
| WO (1) | WO2011031965A1 (enExample) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UY32306A (es) | 2008-12-09 | 2010-07-30 | Gilead Sciences Inc | Derivados de pteridinona y pirimidinodiazepinona y composiciones farmacéuticas que modulan en forma selectiva los receptores tipo toll, métodos y usos |
| BR112012019459A2 (pt) | 2010-02-03 | 2017-10-17 | Signal Pharm Llc | identificação de mutação de lkb1 como um biomarcador preditivo para sensibilidade para inibidores de tor quinase. |
| WO2012167423A1 (en) * | 2011-06-08 | 2012-12-13 | Hutchison Medipharma Limited | Substituted pyridopyrazines as novel syk inhibitors |
| EP2744807A4 (en) | 2011-08-15 | 2015-03-04 | Intermune Inc | COMPOUNDS AS LYSOPHOSPHIC ACID RECEPTOR ANTAGONISTS |
| AU2013203714B2 (en) | 2012-10-18 | 2015-12-03 | Signal Pharmaceuticals, Llc | Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity |
| CA2908742C (en) | 2013-04-17 | 2021-06-01 | Signal Pharmaceuticals, Llc | Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer |
| WO2014172425A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Treatment of cancer with dihydropyrazino-pyrazines |
| MY189663A (en) | 2013-04-17 | 2022-02-23 | Signal Pharm Llc | Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer |
| HK1221168A1 (zh) | 2013-04-17 | 2017-05-26 | 西格诺药品有限公司 | 用於治疗癌症的包括tor激酶抑制剂和n-(3-(5-氟-2-(4-(2-甲氧基乙氧基)苯基氨基)嘧啶-4-基氨基)苯基)丙烯醯胺的组合疗法 |
| WO2014172436A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Combination therapy comprising a tor kinase inhibitor and a 5-substituted quinazolinone compound for treating cancer |
| JP6382946B2 (ja) | 2013-04-17 | 2018-08-29 | シグナル ファーマシューティカルズ,エルエルシー | ジヒドロピラジノ−ピラジンによる癌治療 |
| EP3549940A1 (en) | 2013-04-17 | 2019-10-09 | Signal Pharmaceuticals, LLC | Pharmaceutical formulations, of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl) pyridin-3-yl) -3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one |
| CN107474051B (zh) | 2013-05-29 | 2020-10-30 | 西格诺药品有限公司 | 二氢吡嗪并吡嗪化合物的药物组合物、其固体形式和它们的用途 |
| WO2015160880A1 (en) | 2014-04-16 | 2015-10-22 | Signal Pharmaceuticals, Llc | SOLID FORMS COMPRISING 1-ETHYL-7-(2-METHYL-6-(1H-1,2,4-TRIAZOL-3-YL) PYRIDIN-3-YL)-3,4-DIHYDROPYRAZINO(2,3-b)PYRAZIN-2(1H)-ONE, AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF |
| NZ714742A (en) | 2014-04-16 | 2017-04-28 | Signal Pharm Llc | Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use |
| SI3166607T1 (sl) | 2014-07-11 | 2023-01-31 | Gilead Sciences, Inc. | Modulatorji toličnih receptorjev za zdravljenje HIV-a |
| CN110305133A (zh) | 2014-09-16 | 2019-10-08 | 吉利德科学公司 | Toll样受体调节剂的固体形式 |
| CN107074860B (zh) * | 2014-09-16 | 2022-07-15 | 吉利德科学公司 | 制备toll样受体调节剂的方法 |
| WO2016106050A1 (en) | 2014-12-26 | 2016-06-30 | Emory University | N4-hydroxycytidine and derivatives and anti-viral uses related thereto |
| KR20190084991A (ko) | 2016-11-28 | 2019-07-17 | 지앙수 헨그루이 메디슨 컴퍼니 리미티드 | 피라졸로-헤테로아릴 유도체, 이의 제조 방법 및 의학적 용도 |
| WO2018137614A1 (zh) * | 2017-01-24 | 2018-08-02 | 江苏恒瑞医药股份有限公司 | 杂芳基并噻二嗪-2,2-二氧化物类衍生物、其制备方法及其在医药上的应用 |
| BR102018007822A2 (pt) | 2017-04-20 | 2018-11-06 | Gilead Sciences, Inc. | composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição |
| JP2020520379A (ja) | 2017-05-18 | 2020-07-09 | 江▲蘇▼恒瑞医▲薬▼股▲フン▼有限公司Jiangsu Hengrui Medicine Co., Ltd. | ヘテロアリール−ピラゾール誘導体ならびにその調製方法および医学的適用 |
| IL271491B2 (en) | 2017-06-22 | 2023-09-01 | Celgene Corp | Treatment of carcinoma of the liver characterized by hepatitis b virus infection |
| RU2020116571A (ru) | 2017-12-07 | 2021-11-22 | Эмори Юниверсити | N4-гидроксицитидин и производные и связанные с этим противовирусные применения |
| WO2019160882A1 (en) | 2018-02-13 | 2019-08-22 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| KR102591947B1 (ko) | 2018-04-19 | 2023-10-25 | 길리애드 사이언시즈, 인코포레이티드 | Pd-1/pd-l1 억제제 |
| MX2020012651A (es) | 2018-05-25 | 2021-02-02 | Jiangsu Hengrui Medicine Co | Forma de cristal de clorhidrato de derivado de pirazoloheteroarilo, y metodo de preparacion. |
| CN112105620B (zh) * | 2018-05-25 | 2026-02-24 | 正大天晴药业集团股份有限公司 | 用于治疗肺癌的tlr7激动剂及其药物组合 |
| PE20210642A1 (es) | 2018-07-13 | 2021-03-23 | Gilead Sciences Inc | Inhibidores de pd-1/pd-l1 |
| US11236085B2 (en) | 2018-10-24 | 2022-02-01 | Gilead Sciences, Inc. | PD-1/PD-L1 inhibitors |
| CN113924114A (zh) | 2019-05-22 | 2022-01-11 | 吉利德科学公司 | Tlr7调节化合物和hiv疫苗的组合 |
| KR102514860B1 (ko) * | 2020-12-01 | 2023-03-29 | 한국과학기술연구원 | 5-ht7 세로토닌 수용체 활성 저해용 바이페닐 피롤리딘 및 바이페닐 다이하이드로이미다졸 유도체 및 이를 유효성분으로 포함하는 약학 조성물 |
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| US263470A (en) * | 1882-08-29 | Grate for boiler-furnaces | ||
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| EA200702235A1 (ru) | 2005-05-04 | 2008-04-28 | Пфайзер Лимитед | Производные 2-амидо-6-амино-8-оксопурина в качестве модуляторов toll-подобных рецепторов для лечения рака и вирусных инфекций, таких как гепатит с |
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| CN101636399B (zh) | 2007-03-22 | 2012-04-18 | 武田药品工业株式会社 | 可用作plk1抑制剂的取代的嘧啶并二氮杂* |
| BRPI0811125A2 (pt) * | 2007-05-08 | 2017-05-09 | Astrazeneca Ab | imidazoquinolinas com propriedades imunomoduladoras |
| EP2170888B1 (en) * | 2007-06-29 | 2015-04-22 | Gilead Sciences, Inc. | Purine derivatives and their use as modulators of toll-like receptor 7 |
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| AU2008287339A1 (en) | 2007-08-15 | 2009-02-19 | Vertex Pharmaceuticals Incorporated | 4-(9-(3, 3-difluorocyclopentyl) -5, 7, 7-trimethyl-6-oxo-6, 7, 8, 9-tetrahydro-5H-pyrimido [4, 5-b][1, 4] diazepin-2-ylamino)-3-methoxybenzamide Derivatives as Inhibitors of the Human Protein Kinases PLK1 to PLK4 for the Treatment of Proliferative Diseases |
| WO2009022185A2 (en) | 2007-08-16 | 2009-02-19 | Astrazeneca Ab | 6, 6-fused heterocycles, their pharmaceutical compositions and methos of use |
| WO2009067547A1 (en) | 2007-11-19 | 2009-05-28 | Takeda Pharmaceutical Company Limited | Polo-like kinase inhibitors |
| UY32306A (es) * | 2008-12-09 | 2010-07-30 | Gilead Sciences Inc | Derivados de pteridinona y pirimidinodiazepinona y composiciones farmacéuticas que modulan en forma selectiva los receptores tipo toll, métodos y usos |
-
2010
- 2010-09-10 WO PCT/US2010/048424 patent/WO2011031965A1/en not_active Ceased
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- 2010-09-10 ES ES10760831.7T patent/ES2661850T3/es active Active
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|---|---|
| NO2477987T3 (enExample) | 2018-06-09 |
| EP2477987A1 (en) | 2012-07-25 |
| CA2772253C (en) | 2018-02-27 |
| EP2477987B1 (en) | 2018-01-10 |
| AU2010292102A1 (en) | 2012-03-15 |
| CA2772253A1 (en) | 2011-03-17 |
| AU2010292102B2 (en) | 2015-04-09 |
| PL2477987T3 (pl) | 2018-06-29 |
| SI2477987T1 (en) | 2018-03-30 |
| NZ598384A (en) | 2014-04-30 |
| WO2011031965A1 (en) | 2011-03-17 |
| US20110124627A1 (en) | 2011-05-26 |
| JP2013504593A (ja) | 2013-02-07 |
| US8476270B2 (en) | 2013-07-02 |
| PT2477987T (pt) | 2018-03-13 |
| ES2661850T3 (es) | 2018-04-04 |
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