TW201726656A - 包含經取代雜環基團之２－經取代喹唑啉化合物及其使用方法 - Google Patents
包含經取代雜環基團之２－經取代喹唑啉化合物及其使用方法 Download PDFInfo
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- TW201726656A TW201726656A TW105137373A TW105137373A TW201726656A TW 201726656 A TW201726656 A TW 201726656A TW 105137373 A TW105137373 A TW 105137373A TW 105137373 A TW105137373 A TW 105137373A TW 201726656 A TW201726656 A TW 201726656A
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- 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
- C07D403/14—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 three or more hetero rings
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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
- A61K31/495—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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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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
- A61K31/495—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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
- C07D487/10—Spiro-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
- C07D491/10—Spiro-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
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Dermatology (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562255879P | 2015-11-16 | 2015-11-16 | |
| US201662340291P | 2016-05-23 | 2016-05-23 | |
| US201662406247P | 2016-10-10 | 2016-10-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TW201726656A true TW201726656A (zh) | 2017-08-01 |
Family
ID=57472059
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW105137373A TW201726656A (zh) | 2015-11-16 | 2016-11-16 | 包含經取代雜環基團之２－經取代喹唑啉化合物及其使用方法 |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US10414757B2 (enExample) |
| EP (1) | EP3377481A1 (enExample) |
| JP (3) | JP7015059B2 (enExample) |
| KR (3) | KR102932353B1 (enExample) |
| CN (1) | CN108779097A (enExample) |
| AU (1) | AU2016355433C1 (enExample) |
| CA (1) | CA3005089A1 (enExample) |
| EA (1) | EA038635B9 (enExample) |
| MX (1) | MX2018005967A (enExample) |
| TW (1) | TW201726656A (enExample) |
| WO (1) | WO2017087528A1 (enExample) |
Families Citing this family (213)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9227978B2 (en) | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
| JO3805B1 (ar) | 2013-10-10 | 2021-01-31 | Araxes Pharma Llc | مثبطات كراس جي12سي |
| JO3556B1 (ar) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| MX382355B (es) | 2015-04-10 | 2025-03-13 | Araxes Pharma Llc | Compuestos de quinazolina sustituidos y métodos de uso de los mismos. |
| EP3283462B1 (en) | 2015-04-15 | 2020-12-02 | Araxes Pharma LLC | Fused-tricyclic inhibitors of kras and methods of use thereof |
| US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| EP3356349A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| EP3356347A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| WO2017058792A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| EP3356351A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| EP3356354A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| US10689356B2 (en) | 2015-09-28 | 2020-06-23 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| WO2017058728A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| EP3377481A1 (en) * | 2015-11-16 | 2018-09-26 | Araxes Pharma LLC | 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof |
| WO2017100546A1 (en) | 2015-12-09 | 2017-06-15 | Araxes Pharma Llc | Methods for preparation of quinazoline derivatives |
| JP7114076B2 (ja) | 2015-12-22 | 2022-08-08 | シャイ・セラピューティクス・エルエルシー | がん及び炎症性疾患の処置のための化合物 |
| US10822312B2 (en) | 2016-03-30 | 2020-11-03 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use |
| CN109843856B (zh) | 2016-05-18 | 2023-05-02 | 米拉蒂治疗股份有限公司 | Kras g12c抑制剂 |
| US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
| EP3519402A1 (en) | 2016-09-29 | 2019-08-07 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| US10377743B2 (en) | 2016-10-07 | 2019-08-13 | Araxes Pharma Llc | Inhibitors of RAS and methods of use thereof |
| CA3048217A1 (en) * | 2016-12-22 | 2018-06-28 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| WO2018140513A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer |
| US11358959B2 (en) | 2017-01-26 | 2022-06-14 | Araxes Pharma Llc | Benzothiophene and benzothiazole compounds and methods of use thereof |
| CN110382482A (zh) | 2017-01-26 | 2019-10-25 | 亚瑞克西斯制药公司 | 稠合的杂-杂二环化合物及其使用方法 |
| US11136308B2 (en) | 2017-01-26 | 2021-10-05 | Araxes Pharma Llc | Substituted quinazoline and quinazolinone compounds and methods of use thereof |
| EP3573954A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Fused bicyclic benzoheteroaromatic compounds and methods of use thereof |
| JOP20190186A1 (ar) * | 2017-02-02 | 2019-08-01 | Astellas Pharma Inc | مركب كينازولين |
| ES2905676T3 (es) | 2017-05-22 | 2022-04-11 | Amgen Inc | Inhibidores de KRAS G12C y métodos para su uso |
| CN110869358A (zh) * | 2017-05-25 | 2020-03-06 | 亚瑞克西斯制药公司 | Kras的共价抑制剂 |
| CN110831933A (zh) * | 2017-05-25 | 2020-02-21 | 亚瑞克西斯制药公司 | 喹唑啉衍生物作为突变kras、hras或nras的调节剂 |
| JP2020521741A (ja) * | 2017-05-25 | 2020-07-27 | アラクセス ファーマ エルエルシー | がんの処置のための化合物およびその使用の方法 |
| CA3066939A1 (en) | 2017-06-21 | 2018-12-27 | SHY Therapeutics LLC | Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease |
| CN111051306B (zh) * | 2017-09-08 | 2023-01-03 | 美国安进公司 | Kras g12c的抑制剂及其使用方法 |
| KR102861303B1 (ko) | 2017-11-15 | 2025-09-17 | 미라티 테라퓨틱스, 인크. | Ｋｒａｓ ｇ12ｃ 억제제 |
| US10647715B2 (en) | 2017-11-15 | 2020-05-12 | Mirati Therapeutics, Inc. | KRas G12C inhibitors |
| US10597405B2 (en) | 2017-12-08 | 2020-03-24 | Astrazeneca Ab | Chemical compounds |
| CR20200263A (es) | 2017-12-13 | 2020-07-26 | Lupin Ltd | Componentes heterocíclicos bicíclicos sustituidos como inhibidores de prmt5 |
| CN112442031B (zh) * | 2018-01-19 | 2022-07-12 | 勤浩医药（苏州）有限公司 | 作为krasg12c突变蛋白抑制剂的吡啶酮并嘧啶类衍生物 |
| TW201942115A (zh) * | 2018-02-01 | 2019-11-01 | 美商輝瑞股份有限公司 | 作為抗癌藥之經取代的喹唑啉和吡啶並嘧啶衍生物 |
| TW201942116A (zh) * | 2018-02-09 | 2019-11-01 | 美商輝瑞股份有限公司 | 作為抗癌劑之四氫喹唑啉衍生物 |
| CN119569702A (zh) | 2018-04-04 | 2025-03-07 | 阿尔维纳斯运营股份有限公司 | 蛋白水解调节剂及相关使用方法 |
| MX2020010836A (es) | 2018-05-04 | 2021-01-08 | Amgen Inc | Inhibidores de kras g12c y métodos para su uso. |
| ES2995514T3 (en) | 2018-05-04 | 2025-02-10 | Amgen Inc | Kras g12c inhibitors and methods of using the same |
| WO2019217307A1 (en) | 2018-05-07 | 2019-11-14 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| TW202012415A (zh) | 2018-05-08 | 2020-04-01 | 瑞典商阿斯特捷利康公司 | 化學化合物 |
| EP3790886B1 (en) | 2018-05-10 | 2024-06-26 | Amgen Inc. | Kras g12c inhibitors for the treatment of cancer |
| AU2019278998B2 (en) | 2018-06-01 | 2023-11-09 | Amgen Inc. | KRAS G12C inhibitors and methods of using the same |
| MX2020012204A (es) * | 2018-06-11 | 2021-03-31 | Amgen Inc | Inhibidores de kras g12c para tratar el cáncer. |
| CA3100390A1 (en) | 2018-06-12 | 2020-03-12 | Amgen Inc. | Kras g12c inhibitors encompassing piperazine ring and use thereof in the treatment of cancer |
| JP2021176820A (ja) * | 2018-07-31 | 2021-11-11 | アステラス製薬株式会社 | キナゾリン化合物を有効成分とする医薬組成物 |
| JP2021176819A (ja) * | 2018-07-31 | 2021-11-11 | アステラス製薬株式会社 | キナゾリン化合物を有効成分とする医薬組成物 |
| BR112021001709A2 (pt) | 2018-08-01 | 2021-05-04 | Araxes Pharma Llc | compostos espiro heterocíclicos e métodos de uso dos mesmos para o tratamento de câncer |
| CR20210083A (es) | 2018-08-16 | 2021-04-19 | Hoffmann La Roche | Compuestos de anillo fusionado |
| KR102871791B1 (ko) | 2018-09-10 | 2025-10-15 | 미라티 테라퓨틱스, 인크. | 병용 요법 |
| ES3004338T3 (en) | 2018-09-10 | 2025-03-12 | Mirati Therapeutics Inc | Combination therapies |
| WO2020055761A1 (en) | 2018-09-10 | 2020-03-19 | Mirati Therapeutics, Inc. | Combination therapies |
| JP2022500385A (ja) | 2018-09-10 | 2022-01-04 | ミラティ セラピューティクス， インコーポレイテッド | 組み合わせ療法 |
| WO2020061103A1 (en) | 2018-09-18 | 2020-03-26 | Nikang Therapeutics, Inc. | Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors |
| TWI831855B (zh) | 2018-10-26 | 2024-02-11 | 日商大鵬藥品工業股份有限公司 | 新穎吲唑化合物或其鹽 |
| ES3004042T3 (en) | 2018-11-09 | 2025-03-11 | Hoffmann La Roche | Fused ring compounds |
| JP7516029B2 (ja) | 2018-11-16 | 2024-07-16 | アムジエン・インコーポレーテツド | Ｋｒａｓ ｇ１２ｃ阻害剤化合物の重要な中間体の改良合成法 |
| CA3117222A1 (en) | 2018-11-19 | 2020-05-28 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| JP7377679B2 (ja) | 2018-11-19 | 2023-11-10 | アムジエン・インコーポレーテツド | がん治療のためのｋｒａｓｇ１２ｃ阻害剤及び１種以上の薬学的に活性な追加の薬剤を含む併用療法 |
| CA3112129A1 (en) | 2018-12-05 | 2020-06-11 | Mirati Therapeutics, Inc. | Combination therapies |
| EP3898609A1 (en) | 2018-12-19 | 2021-10-27 | Shy Therapeutics LLC | Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease |
| JP7592601B2 (ja) | 2019-01-10 | 2024-12-02 | ミラティ セラピューティクス， インコーポレイテッド | Ｋｒａｓ ｇ１２ｃ阻害剤 |
| CN111499634B (zh) * | 2019-01-31 | 2023-05-12 | 贝达药业股份有限公司 | 一种喹唑啉化合物及其在医药上的应用 |
| US20220152026A1 (en) | 2019-02-12 | 2022-05-19 | Novartis Ag | Pharmaceutical combination comprising tno155 and a krasg12c inhibitor |
| WO2020177629A1 (zh) * | 2019-03-01 | 2020-09-10 | 劲方医药科技(上海)有限公司 | 螺环取代的嘧啶并环类化合物，其制法与医药上的用途 |
| PH12021552083A1 (en) | 2019-03-05 | 2022-06-06 | Astrazeneca Ab | Fused tricyclic compounds useful as anticancer agents |
| CN111662232B (zh) * | 2019-03-06 | 2022-08-02 | 中国科学院上海药物研究所 | 具有2h-吲唑结构的小分子化合物及其合成和应用 |
| AU2020260629A1 (en) * | 2019-04-22 | 2021-12-09 | Betta Pharmaceuticals Co., Ltd | Quinazoline compound and pharmaceutical application thereof |
| EP3738593A1 (en) | 2019-05-14 | 2020-11-18 | Amgen, Inc | Dosing of kras inhibitor for treatment of cancers |
| CN114144414B (zh) | 2019-05-21 | 2025-11-07 | 美国安进公司 | 固态形式 |
| US20220227729A1 (en) | 2019-05-21 | 2022-07-21 | Bayer Aktiengesellschaft | Identification and use of kras inhibitors |
| CN112047948B (zh) * | 2019-06-06 | 2022-08-16 | 山东轩竹医药科技有限公司 | Kras突变体抑制剂 |
| CN112110918B (zh) * | 2019-06-21 | 2023-08-22 | 劲方医药科技(上海)有限公司 | 螺环取代的嘧啶并环类化合物，其制法与医药上的用途 |
| CN114040914B (zh) * | 2019-07-01 | 2024-10-22 | 江苏恒瑞医药股份有限公司 | 喹唑啉酮类衍生物、其制备方法及其在医药上的应用 |
| CN114222743A (zh) * | 2019-08-16 | 2022-03-22 | 劲方医药科技(上海)有限公司 | 氧代六元环并嘧啶类化合物，其制法与医药上的用途 |
| CA3148745A1 (en) | 2019-08-29 | 2021-03-04 | Xiaolun Wang | Kras g12d inhibitors |
| BR112022005193A2 (pt) * | 2019-09-20 | 2022-08-16 | Shanghai Jemincare Pharmaceuticals Co Ltd | Composto de piridona fundido, método de preparação do mesmo e uso do mesmo |
| US12122787B2 (en) | 2019-09-20 | 2024-10-22 | Shanghai Jemincare Pharmaceuticals Co., Ltd | Fused pyridone compound, and preparation method therefor and use thereof |
| CN114761012B (zh) | 2019-09-24 | 2025-03-21 | 米拉蒂治疗股份有限公司 | 组合疗法 |
| WO2021057832A1 (en) * | 2019-09-25 | 2021-04-01 | Jacobio Pharmaceuticals Co., Ltd. | Kras mutant protein inhibitor |
| WO2021058018A1 (en) * | 2019-09-29 | 2021-04-01 | Beigene, Ltd. | Inhibitors of kras g12c |
| WO2021063346A1 (zh) * | 2019-09-30 | 2021-04-08 | 上海迪诺医药科技有限公司 | Kras g12c抑制剂及其应用 |
| CA3158793A1 (en) | 2019-10-28 | 2021-05-06 | Merck Sharp & Dohme Corp. | Small molecule inhibitors of kras g12c mutant |
| PE20221277A1 (es) | 2019-11-04 | 2022-09-05 | Revolution Medicines Inc | Inhibidores de ras |
| WO2021088458A1 (en) * | 2019-11-04 | 2021-05-14 | Jacobio Pharmaceuticals Co., Ltd. | Kras mutant protein inhibitor |
| CN114786777A (zh) | 2019-11-04 | 2022-07-22 | 锐新医药公司 | Ras抑制剂 |
| CN114867735A (zh) | 2019-11-04 | 2022-08-05 | 锐新医药公司 | Ras抑制剂 |
| CA3158188A1 (en) | 2019-11-14 | 2021-05-20 | Amgen Inc. | Improved synthesis of kras g12c inhibitor compound |
| CN114630832A (zh) * | 2019-11-15 | 2022-06-14 | 四川海思科制药有限公司 | 一种嘧啶并环衍生物及其在医药上的应用 |
| EP4065231A1 (en) | 2019-11-27 | 2022-10-05 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
| WO2021106231A1 (en) * | 2019-11-29 | 2021-06-03 | Taiho Pharmaceutical Co., Ltd. | A compound having inhibitory activity against kras g12d mutation |
| WO2021106230A1 (ja) | 2019-11-29 | 2021-06-03 | 大鵬薬品工業株式会社 | 新規なフェノール化合物又はその塩 |
| CN113024544B (zh) * | 2019-12-09 | 2024-07-02 | 武汉誉祥医药科技有限公司 | 一种含氰基并杂环化合物及其用途 |
| KR20220130126A (ko) | 2019-12-20 | 2022-09-26 | 미라티 테라퓨틱스, 인크. | Sos1 억제제 |
| MX2022006609A (es) * | 2019-12-27 | 2022-07-05 | Wigen Biomedicine Tech Shanghai Co Ltd | Compuesto de quinazolina que contiene anillo espiro. |
| WO2021138391A1 (en) | 2019-12-30 | 2021-07-08 | Tyra Biosciences, Inc. | Indazole compounds |
| EP4087843A1 (en) * | 2020-01-10 | 2022-11-16 | Incyte Corporation | Tricyclic compounds as inhibitors of kras |
| WO2021150613A1 (en) | 2020-01-20 | 2021-07-29 | Incyte Corporation | Spiro compounds as inhibitors of kras |
| WO2023205701A1 (en) | 2022-04-20 | 2023-10-26 | Kumquat Biosciences Inc. | Macrocyclic heterocycles and uses thereof |
| JP7462985B2 (ja) * | 2020-02-24 | 2024-04-08 | 上海▲テツ▼▲ギョウ▼生物科技有限公司 | 芳香族化合物および抗腫瘍薬物の調製におけるその使用 |
| CA3170068A1 (en) | 2020-03-25 | 2021-09-30 | Yuli Xie | Spiro ring-containing quinazoline compound |
| EP4132655A1 (en) * | 2020-04-06 | 2023-02-15 | Arvinas Operations, Inc. | Compounds and methods for targeted degradation of kras |
| CA3179692A1 (en) * | 2020-04-16 | 2021-10-21 | Incyte Corporation | Fused tricyclic kras inhibitors |
| WO2021218110A1 (zh) * | 2020-04-29 | 2021-11-04 | 上海凌达生物医药有限公司 | 一类苯并噻唑基联芳基类化合物、制备方法和用途 |
| WO2021231526A1 (en) | 2020-05-13 | 2021-11-18 | Incyte Corporation | Fused pyrimidine compounds as kras inhibitors |
| KR20230042600A (ko) | 2020-06-18 | 2023-03-28 | 레볼루션 메디슨즈, 인크. | Ras 억제제에 대한 획득된 저항성을 지연, 예방, 및 치료하는 방법 |
| EP4175947A4 (en) * | 2020-06-30 | 2024-07-03 | InventisBio Co., Ltd. | QUINAZOLINE COMPOUNDS, THEIR PREPARATION PROCESSES AND THEIR USES |
| BR112023002591A2 (pt) * | 2020-08-12 | 2023-04-04 | Genentech Inc | Processo para a preparação de um composto e composto |
| US11999752B2 (en) | 2020-08-28 | 2024-06-04 | Incyte Corporation | Vinyl imidazole compounds as inhibitors of KRAS |
| CA3187757A1 (en) | 2020-09-03 | 2022-03-24 | Ethan AHLER | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
| US12286431B2 (en) | 2020-09-11 | 2025-04-29 | Mirati Therapeutics, Inc. | Crystalline forms of a KRas G12C inhibitor |
| AU2021345111B2 (en) | 2020-09-15 | 2025-11-27 | Revolution Medicines, Inc. | Indole derivatives as Ras inhibitors in the treatment of cancer |
| MX2023003338A (es) | 2020-09-23 | 2023-06-14 | Erasca Inc | Piridonas y pirimidonas tricíclicas. |
| US20230365563A1 (en) * | 2020-09-30 | 2023-11-16 | Shanghai Pharmaceuticals Holding Co., Ltd. | Quinazoline compound and application thereof |
| WO2022072783A1 (en) | 2020-10-02 | 2022-04-07 | Incyte Corporation | Bicyclic dione compounds as inhibitors of kras |
| CN116322697A (zh) * | 2020-10-21 | 2023-06-23 | 贝达药业股份有限公司 | 一种喹唑啉化合物及其药物组合物 |
| CN120887884A (zh) * | 2020-11-06 | 2025-11-04 | 泰励生物科技（上海）有限公司 | 用于癌症治疗的KRas抑制剂 |
| WO2022105855A1 (en) * | 2020-11-20 | 2022-05-27 | Jacobio Pharmaceuticals Co., Ltd. | Kras g12d inhibitors |
| CN112574127B (zh) * | 2020-12-09 | 2022-11-01 | 深圳湾实验室 | 喹唑啉类化合物及其制备方法、药物组合物及其应用 |
| US12398154B2 (en) | 2020-12-15 | 2025-08-26 | Mirati Therapeutics, Inc. | Azaquinazoline pan-KRas inhibitors |
| EP4262803A4 (en) | 2020-12-16 | 2025-03-12 | Mirati Therapeutics, Inc. | Tetrahydropyridopyrimidine pan-kras inhibitors |
| US20230107642A1 (en) | 2020-12-18 | 2023-04-06 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| US20240100172A1 (en) | 2020-12-21 | 2024-03-28 | Hangzhou Jijing Pharmaceutical Technology Limited | Methods and compounds for targeted autophagy |
| AU2021407653B9 (en) * | 2020-12-22 | 2025-06-05 | Shanghai Kechow Pharma, Inc | Preparation and application method of heterocyclic compound as kras inhibitor |
| IL303661A (en) | 2020-12-22 | 2023-08-01 | Nikang Therapeutics Inc | Compounds for degrading cyclin-dependent kinase 2 via ubiquitin proteosome pathway |
| JP2024501507A (ja) * | 2020-12-25 | 2024-01-12 | スーチュアン ハイスーク ファーマシューティカル カンパニー リミテッド | ケトヘキソキナーゼ阻害剤及びその用途 |
| WO2022152233A1 (en) * | 2021-01-15 | 2022-07-21 | Beigene, Ltd. | Kras g12c inhibitors |
| WO2022152313A1 (zh) * | 2021-01-18 | 2022-07-21 | 成都百裕制药股份有限公司 | 嘧啶衍生物及其在医药上的应用 |
| WO2022204112A1 (en) | 2021-03-22 | 2022-09-29 | Incyte Corporation | Imidazole and triazole kras inhibitors |
| CN115124524A (zh) * | 2021-03-26 | 2022-09-30 | 浙江海正药业股份有限公司 | 三环类衍生物及其制备方法和用途 |
| AR125782A1 (es) | 2021-05-05 | 2023-08-16 | Revolution Medicines Inc | Inhibidores de ras |
| CR20230558A (es) | 2021-05-05 | 2024-01-24 | Revolution Medicines Inc | Inhibidores de ras para el tratamiento del cáncer |
| WO2022247760A1 (zh) * | 2021-05-22 | 2022-12-01 | 上海科州药物研发有限公司 | 作为kras抑制剂的杂环化合物，及其制备和治疗用途 |
| WO2022266206A1 (en) | 2021-06-16 | 2022-12-22 | Erasca, Inc. | Kras inhibitor conjugates |
| TW202317100A (zh) | 2021-06-23 | 2023-05-01 | 瑞士商諾華公司 | 包含ｋｒａｓ ｇ１２ｃ抑制劑的藥物組合及其用於治療癌症之用途 |
| AU2022306671A1 (en) | 2021-07-07 | 2024-01-25 | Incyte Corporation | Tricyclic compounds as inhibitors of kras |
| JP2024529347A (ja) * | 2021-07-14 | 2024-08-06 | インサイト・コーポレイション | Ｋｒａｓの阻害剤としての三環式化合物 |
| CN117980310A (zh) | 2021-07-14 | 2024-05-03 | 尼坎治疗公司 | 作为kras抑制剂的亚烷基衍生物 |
| IL310291A (en) | 2021-07-23 | 2024-03-01 | Theras Inc | Compositions and methods for inhibition of ras |
| MX2024000965A (es) | 2021-07-27 | 2024-02-09 | Toray Industries | Medicamento para el tratamiento y/o prevencion de cancer. |
| JP2024534187A (ja) | 2021-08-31 | 2024-09-18 | インサイト・コーポレイション | Ｋｒａｓの阻害剤としてのナフチリジン化合物 |
| EP4395769A1 (en) | 2021-09-01 | 2024-07-10 | Novartis AG | Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers |
| EP4389751A1 (en) | 2021-09-03 | 2024-06-26 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| WO2023049697A1 (en) | 2021-09-21 | 2023-03-30 | Incyte Corporation | Hetero-tricyclic compounds as inhibitors of kras |
| EP4408536A1 (en) | 2021-10-01 | 2024-08-07 | Incyte Corporation | Pyrazoloquinoline kras inhibitors |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| KR20240101561A (ko) | 2021-10-14 | 2024-07-02 | 인사이트 코포레이션 | Kras의 저해제로서의 퀴놀린 화합물 |
| WO2023066371A1 (zh) | 2021-10-22 | 2023-04-27 | 江苏恒瑞医药股份有限公司 | 含氮的四环化合物、其制备方法及其在医药上的应用 |
| WO2023114733A1 (en) * | 2021-12-13 | 2023-06-22 | Quanta Therapeutics, Inc. | Kras modulators and uses thereof |
| WO2023114954A1 (en) | 2021-12-17 | 2023-06-22 | Genzyme Corporation | Pyrazolopyrazine compounds as shp2 inhibitors |
| US20250188085A1 (en) * | 2022-01-06 | 2025-06-12 | Theras, Inc. | Compositions and methods for inhibition of ras |
| US20250084079A1 (en) * | 2022-01-06 | 2025-03-13 | Theras, Inc. | Compositions and methods for inhibition of ras |
| EP4475956A1 (en) | 2022-02-09 | 2024-12-18 | Quanta Therapeutics, Inc. | Kras modulators and uses thereof |
| US20250154170A1 (en) | 2022-02-10 | 2025-05-15 | Bayer Aktiengesellschaft | Fused pyrimidines as kras inhibitors |
| EP4227307A1 (en) | 2022-02-11 | 2023-08-16 | Genzyme Corporation | Pyrazolopyrazine compounds as shp2 inhibitors |
| WO2023172940A1 (en) | 2022-03-08 | 2023-09-14 | Revolution Medicines, Inc. | Methods for treating immune refractory lung cancer |
| KR20240167846A (ko) | 2022-03-28 | 2024-11-28 | 니캉 테라퓨틱스 인코포레이티드 | 사이클린 의존적 키나제 2 억제제로서의 설폰아미도 유도체 |
| WO2023199180A1 (en) | 2022-04-11 | 2023-10-19 | Novartis Ag | Therapeutic uses of a krasg12c inhibitor |
| WO2023225252A1 (en) * | 2022-05-20 | 2023-11-23 | Theras, Inc. | Compositions and methods for inhibition of ras |
| WO2023230190A1 (en) | 2022-05-25 | 2023-11-30 | Quanta Therapeutics, Inc. | Pyrimidine based modulators and uses thereof |
| EP4536363A1 (en) | 2022-06-08 | 2025-04-16 | Nikang Therapeutics, Inc. | Sulfamide derivatives as cyclin-dependent kinase 2 inhibitors |
| AU2023285116A1 (en) | 2022-06-10 | 2024-12-19 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| US20260034123A1 (en) * | 2022-07-28 | 2026-02-05 | Cedilla Therapeutics, Inc. | Cdk2 inhibitors and methods of using the same |
| WO2024036270A1 (en) * | 2022-08-11 | 2024-02-15 | Bristol-Myers Squibb Company | Kras inhibitors |
| CN120659773A (zh) | 2022-11-09 | 2025-09-16 | 锐新医药公司 | 化合物、复合物以及其制备方法和用途 |
| AU2023375457A1 (en) | 2022-11-11 | 2025-05-01 | Nikang Therapeutics, Inc. | Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 via ubiquitin proteasome pathway |
| WO2024158778A1 (en) * | 2023-01-24 | 2024-08-02 | Theras, Inc. | Compositions and methods for inhibition of ras |
| CN121419983A (zh) | 2023-01-26 | 2026-01-27 | 阿尔维纳斯运营股份有限公司 | 基于小脑蛋白的kras降解protac及其相关用途 |
| AU2024234154A1 (en) | 2023-03-15 | 2025-09-25 | Quanta Therapeutics, Inc. | Kras modulators and uses thereof |
| AU2024241633A1 (en) | 2023-03-30 | 2025-11-06 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| WO2024211663A1 (en) | 2023-04-07 | 2024-10-10 | Revolution Medicines, Inc. | Condensed macrocyclic compounds as ras inhibitors |
| EP4688790A1 (en) | 2023-04-07 | 2026-02-11 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| AU2024252105A1 (en) | 2023-04-14 | 2025-10-16 | Revolution Medicines, Inc. | Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof |
| WO2024216016A1 (en) | 2023-04-14 | 2024-10-17 | Revolution Medicines, Inc. | Crystalline forms of a ras inhibitor |
| CN121712509A (zh) | 2023-05-04 | 2026-03-20 | 锐新医药公司 | 用于ras相关疾病或病症的组合疗法 |
| EP4720059A1 (en) | 2023-05-24 | 2026-04-08 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| CN121219016A (zh) | 2023-06-02 | 2025-12-26 | 第一三共株式会社 | 抗-her3抗体-药物缀合物和rasg12c抑制剂的组合 |
| WO2025007000A1 (en) | 2023-06-30 | 2025-01-02 | Kumquat Biosciences Inc. | Substituted condensed tricyclic amine compounds and uses thereof as ras inhibitors |
| WO2025016899A1 (en) | 2023-07-19 | 2025-01-23 | Bayer Aktiengesellschaft | Spirocyclic compounds for the treatment of cancer |
| WO2025026903A1 (en) | 2023-07-31 | 2025-02-06 | Bayer Aktiengesellschaft | Imidazo pyrimidine compounds for the treatment of cancer |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025072462A1 (en) | 2023-09-27 | 2025-04-03 | Nikang Therapeutics, Inc. | Sulfonamide derivatives as cyclin-dependent kinase 2 inhibitors |
| IL327306A (en) | 2023-10-12 | 2026-05-01 | Revolution Medicines Inc | Macrocyclic RAS inhibitors |
| WO2025085748A1 (en) | 2023-10-20 | 2025-04-24 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras proteins |
| TW202527955A (zh) | 2023-11-27 | 2025-07-16 | 美商尼坎醫療公司 | 用於經由泛素蛋白酶體途徑降解週期蛋白依賴性激酶２和週期蛋白依賴性激酶４的含有２，５－取代的嘧啶衍生物的雙功能化合物 |
| WO2025117981A1 (en) | 2023-12-02 | 2025-06-05 | Nikang Therapeutics, Inc. | Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 via ubiquitin proteasome pathway |
| WO2025171055A1 (en) | 2024-02-06 | 2025-08-14 | Kumquat Biosciences Inc. | Heterocyclic conjugates and uses thereof |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025212828A1 (en) | 2024-04-03 | 2025-10-09 | Nikang Therapeutics, Inc. | Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 and cyclin-dependent kinase 4 via ubiquitin proteasome pathway |
| WO2025230971A1 (en) | 2024-04-30 | 2025-11-06 | Kumquat Biosciences Inc. | Macrocyclic heterocycles as anticancer agents |
| WO2025240536A1 (en) | 2024-05-15 | 2025-11-20 | Nikang Therapeutics, Inc. | Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 and/or cyclin-dependent kinase 4 via ubiquitin proteasome pathway |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026035947A1 (en) | 2024-08-07 | 2026-02-12 | Tesseract Medicines Us, Llc | Kras-targeting covalent-induced drug conjugates comprising a topoisomerase payload |
| WO2026035945A1 (en) | 2024-08-07 | 2026-02-12 | Tesseract Medicines Us, Llc | Covalent-induced drug conjugates targeting kras and comprising a topoisomerase payload |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026064527A1 (en) | 2024-09-19 | 2026-03-26 | Tesseract Medicines Us, Llc | Kras-targeting covalent-induced drug conjugates comprising a tubulin inhibitor payload |
| WO2026064520A1 (en) | 2024-09-19 | 2026-03-26 | Tesseract Medicines Us, Llc | Covalent-induced drug conjugates targeting kras and comprising a tubulin inhibitor payload |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
| WO2026090116A2 (en) | 2024-10-21 | 2026-04-30 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026090245A1 (en) | 2024-10-22 | 2026-04-30 | Revolution Medicines, Inc. | Use of ras inhibitors for treating cancer |
| US20260108528A1 (en) | 2024-10-22 | 2026-04-23 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
Family Cites Families (220)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB939516A (en) | 1961-05-29 | 1963-10-16 | British Drug Houses Ltd | Sulphonyl ureas |
| US3702849A (en) | 1967-10-26 | 1972-11-14 | Pfizer | 4-(isoquinolin-1-yl) piperazine-1-carboxylic acid esters |
| US3752660A (en) | 1971-03-15 | 1973-08-14 | Allied Chem | Chlorophenoxyacetyloxazolidone herbicides and preparation thereof |
| US4439606A (en) | 1982-05-06 | 1984-03-27 | American Cyanamid Company | Antiatherosclerotic 1-piperazinecarbonyl compounds |
| EP0094498A3 (en) | 1982-05-06 | 1985-04-03 | American Cyanamid Company | Antiatherosclerotic 1-piperazine derivatives |
| US4656181A (en) | 1982-11-24 | 1987-04-07 | Cermol S.A. | Esters of 1,4-dihydropyridines, processes for the preparation of the new esters, and medicaments containing the same |
| JPS59163372A (ja) | 1983-03-09 | 1984-09-14 | Showa Denko Kk | ピラゾ−ル誘導体とその製造法及び除草剤 |
| JPS60193955A (ja) | 1984-03-13 | 1985-10-02 | Mitsui Toatsu Chem Inc | 環式不飽和アミド置換エ−テル化合物及びその製造方法 |
| JPS6143190A (ja) | 1984-08-06 | 1986-03-01 | Mitsui Petrochem Ind Ltd | ピリドピリミジン誘導体およびその製法 |
| US4911920A (en) | 1986-07-30 | 1990-03-27 | Alcon Laboratories, Inc. | Sustained release, comfort formulation for glaucoma therapy |
| FR2588189B1 (fr) | 1985-10-03 | 1988-12-02 | Merck Sharp & Dohme | Composition pharmaceutique de type a transition de phase liquide-gel |
| US5052558A (en) | 1987-12-23 | 1991-10-01 | Entravision, Inc. | Packaged pharmaceutical product |
| US5033252A (en) | 1987-12-23 | 1991-07-23 | Entravision, Inc. | Method of packaging and sterilizing a pharmaceutical product |
| US5010175A (en) | 1988-05-02 | 1991-04-23 | The Regents Of The University Of California | General method for producing and selecting peptides with specific properties |
| GB8827305D0 (en) | 1988-11-23 | 1988-12-29 | British Bio Technology | Compounds |
| US5925525A (en) | 1989-06-07 | 1999-07-20 | Affymetrix, Inc. | Method of identifying nucleotide differences |
| IE66205B1 (en) | 1990-06-14 | 1995-12-13 | Paul A Bartlett | Polypeptide analogs |
| US5650489A (en) | 1990-07-02 | 1997-07-22 | The Arizona Board Of Regents | Random bio-oligomer library, a method of synthesis thereof, and a method of use thereof |
| DK0495421T3 (da) | 1991-01-15 | 1996-12-09 | Alcon Lab Inc | Anvendelse af carragenaner i topiske ophthalmiske sammensætninger |
| US5212162A (en) | 1991-03-27 | 1993-05-18 | Alcon Laboratories, Inc. | Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions |
| US6017696A (en) | 1993-11-01 | 2000-01-25 | Nanogen, Inc. | Methods for electronic stringency control for molecular biological analysis and diagnostics |
| US6051380A (en) | 1993-11-01 | 2000-04-18 | Nanogen, Inc. | Methods and procedures for molecular biological analysis and diagnostics |
| US5573905A (en) | 1992-03-30 | 1996-11-12 | The Scripps Research Institute | Encoded combinatorial chemical libraries |
| US5323907A (en) | 1992-06-23 | 1994-06-28 | Multi-Comp, Inc. | Child resistant package assembly for dispensing pharmaceutical medications |
| US5288514A (en) | 1992-09-14 | 1994-02-22 | The Regents Of The University Of California | Solid phase and combinatorial synthesis of benzodiazepine compounds on a solid support |
| US5455258A (en) | 1993-01-06 | 1995-10-03 | Ciba-Geigy Corporation | Arylsulfonamido-substituted hydroxamic acids |
| US5605798A (en) | 1993-01-07 | 1997-02-25 | Sequenom, Inc. | DNA diagnostic based on mass spectrometry |
| US5858659A (en) | 1995-11-29 | 1999-01-12 | Affymetrix, Inc. | Polymorphism detection |
| US6045996A (en) | 1993-10-26 | 2000-04-04 | Affymetrix, Inc. | Hybridization assays on oligonucleotide arrays |
| US6068818A (en) | 1993-11-01 | 2000-05-30 | Nanogen, Inc. | Multicomponent devices for molecular biological analysis and diagnostics |
| US5538848A (en) | 1994-11-16 | 1996-07-23 | Applied Biosystems Division, Perkin-Elmer Corp. | Method for detecting nucleic acid amplification using self-quenching fluorescence probe |
| IL111730A (en) | 1993-11-29 | 1998-12-06 | Fujisawa Pharmaceutical Co | Piperazine derivatives processes for the preparation thereof and pharmaceutical compositions containing the same |
| DE69531542T2 (de) | 1994-02-07 | 2004-06-24 | Beckman Coulter, Inc., Fullerton | Ligase/polymerase-vermittelte analyse genetischer elemente von einzelnukleotid-polymorphismen und ihre verwendung in der genetischen analyse |
| US5593853A (en) | 1994-02-09 | 1997-01-14 | Martek Corporation | Generation and screening of synthetic drug libraries |
| US5539083A (en) | 1994-02-23 | 1996-07-23 | Isis Pharmaceuticals, Inc. | Peptide nucleic acid combinatorial libraries and improved methods of synthesis |
| US6309853B1 (en) | 1994-08-17 | 2001-10-30 | The Rockfeller University | Modulators of body weight, corresponding nucleic acids and proteins, and diagnostic and therapeutic uses thereof |
| EP0786997A4 (en) | 1994-10-27 | 1998-03-11 | Merck & Co Inc | MUSCARINE ANTAGONISTS |
| US5863949A (en) | 1995-03-08 | 1999-01-26 | Pfizer Inc | Arylsulfonylamino hydroxamic acid derivatives |
| JP3053222B2 (ja) | 1995-04-20 | 2000-06-19 | ファイザー・インコーポレーテッド | Ｍｍｐおよびｔｎｆ抑制剤としてのアリールスルホニルヒドロキサム酸誘導体 |
| FR2734816B1 (fr) | 1995-05-31 | 1997-07-04 | Adir | Nouveaux aryl (alkyl) propylamides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| DE69638269D1 (de) | 1995-06-14 | 2010-11-18 | Univ California | Hochaffine humane antikörper gegen tumorantigene |
| ATE225343T1 (de) | 1995-12-20 | 2002-10-15 | Hoffmann La Roche | Matrix-metalloprotease inhibitoren |
| US6011029A (en) | 1996-02-26 | 2000-01-04 | Bristol-Myers Squibb Company | Inhibitors of farnesyl protein transferase |
| EP0818442A3 (en) | 1996-07-12 | 1998-12-30 | Pfizer Inc. | Cyclic sulphone derivatives as inhibitors of metalloproteinases and of the production of tumour necrosis factor |
| CA2260898C (en) | 1996-07-18 | 2002-05-14 | Pfizer Limited | Phosphinate based inhibitors of matrix metalloproteases |
| PL331895A1 (en) | 1996-08-23 | 1999-08-16 | Pfizer | Arylosulphonylamino derivatives of hydroxamic acid |
| US5777324A (en) | 1996-09-19 | 1998-07-07 | Sequenom, Inc. | Method and apparatus for maldi analysis |
| DE69730151T2 (de) | 1997-01-06 | 2005-08-04 | Pfizer Inc. | Cyclische sulfonderivate |
| AU721748B2 (en) | 1997-02-03 | 2000-07-13 | Pfizer Products Inc. | Arylsulfonylamino hydroxamic acid derivatives |
| GB9702194D0 (en) | 1997-02-04 | 1997-03-26 | Lilly Co Eli | Sulphonide derivatives |
| CA2279863A1 (en) | 1997-02-07 | 1998-08-13 | Pfizer Inc. | N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases |
| WO1998034918A1 (en) | 1997-02-11 | 1998-08-13 | Pfizer Inc. | Arylsulfonyl hydroxamic acid derivatives |
| US6291464B1 (en) | 1997-02-17 | 2001-09-18 | Fujisawa Pharmaceutical Co., Ltd. | Aminopiperazine derivatives |
| US6002008A (en) | 1997-04-03 | 1999-12-14 | American Cyanamid Company | Substituted 3-cyano quinolines |
| UA73073C2 (uk) | 1997-04-03 | 2005-06-15 | Уайт Холдінгз Корпорейшн | Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція |
| US5919626A (en) | 1997-06-06 | 1999-07-06 | Orchid Bio Computer, Inc. | Attachment of unmodified nucleic acids to silanized solid phase surfaces |
| AU8253598A (en) | 1997-06-17 | 1999-01-04 | Schering Corporation | Novel n-substituted urea inhibitors of farnesyl-protein transferase |
| ID23668A (id) | 1997-08-08 | 2000-05-11 | Pfizer Prod Inc | Turunan asam ariloksiarilsulfonilamino hidroksamat |
| GB9725782D0 (en) | 1997-12-05 | 1998-02-04 | Pfizer Ltd | Therapeutic agents |
| US6903118B1 (en) | 1997-12-17 | 2005-06-07 | Klinge Pharma Gmbh | Piperazinyl-substituted pyridylalkane, alkene and alkine carboxamides |
| DE19756236A1 (de) | 1997-12-17 | 1999-07-01 | Klinge Co Chem Pharm Fab | Neue piperazinylsubstituierte Pyridylalkan-, alken- und -alkincarbonsäureamide |
| CA2314401A1 (en) | 1997-12-22 | 1999-07-01 | Du Pont Pharmaceuticals Company | Nitrogen containing heteroaromatics with ortho-substituted p1's as factor xa inhibitors |
| GB9801690D0 (en) | 1998-01-27 | 1998-03-25 | Pfizer Ltd | Therapeutic agents |
| PA8469501A1 (es) | 1998-04-10 | 2000-09-29 | Pfizer Prod Inc | Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico |
| PA8469401A1 (es) | 1998-04-10 | 2000-05-24 | Pfizer Prod Inc | Derivados biciclicos del acido hidroxamico |
| US7060431B2 (en) | 1998-06-24 | 2006-06-13 | Illumina, Inc. | Method of making and decoding of array sensors with microspheres |
| DK1004578T3 (da) | 1998-11-05 | 2004-06-28 | Pfizer Prod Inc | 5-oxo-pyrrolidin-2-carboxylsyrehydroxamidderivater |
| US6429027B1 (en) | 1998-12-28 | 2002-08-06 | Illumina, Inc. | Composite arrays utilizing microspheres |
| US6511993B1 (en) | 1999-06-03 | 2003-01-28 | Kevin Neil Dack | Metalloprotease inhibitors |
| GB9912961D0 (en) | 1999-06-03 | 1999-08-04 | Pfizer Ltd | Metalloprotease inhibitors |
| EP1081137A1 (en) | 1999-08-12 | 2001-03-07 | Pfizer Products Inc. | Selective inhibitors of aggrecanase in osteoarthritis treatment |
| CA2384838C (en) | 1999-09-13 | 2006-07-18 | Nugen Technologies, Inc. | Methods and compositions for linear isothermal amplification of polynucleotide sequences |
| TWI271406B (en) | 1999-12-13 | 2007-01-21 | Eisai Co Ltd | Tricyclic condensed heterocyclic compounds, preparation method of the same and pharmaceuticals comprising the same |
| IL151249A0 (en) | 2000-03-13 | 2003-04-10 | American Cyanamid Co | Use of cyanoquinolines for treating or inhibiting colonic polyps |
| SK13352002A3 (sk) | 2000-03-21 | 2003-05-02 | The Procter & Gamble Company | Metaloproteázové inhibítory s vedľajším heterocyklickým reťazcom |
| BR0111280A (pt) | 2000-06-05 | 2003-06-10 | Dong A Pharm Co Ltd | Novos derivados de oxazolidinona e um processo para a preparação dos mesmos |
| TWI227231B (en) | 2000-07-12 | 2005-02-01 | Novartis Ag | 4-benzoyl-piperidine derivatives for treating conditions mediated by CCR-3 |
| EP1964839A3 (en) | 2000-08-18 | 2008-11-05 | Millennium Pharmaceuticals, Inc. | Quinazoline derivatives as kinase inhibitors |
| US6890747B2 (en) | 2000-10-23 | 2005-05-10 | Warner-Lambert Company | Phosphoinositide 3-kinases |
| US7429599B2 (en) | 2000-12-06 | 2008-09-30 | Signal Pharmaceuticals, Llc | Methods for treating or preventing an inflammatory or metabolic condition or inhibiting JNK |
| US20020169300A1 (en) | 2001-01-30 | 2002-11-14 | Waterman Marian L. | Method of detection and treatment of colon cancer by analysis of beta-catenin-sensitive isoforms of lymphoid enhancer factor-1 |
| US7259157B2 (en) | 2001-04-03 | 2007-08-21 | Merck & Co., Inc. | N-substituted nonaryl-heterocyclo amidyl NMDA/NR2B Antagonists |
| JP4310109B2 (ja) | 2001-04-26 | 2009-08-05 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | ピラゾリル基を置換基として有する含窒素縮合環化合物およびその医薬組成物 |
| JP2002371078A (ja) | 2001-06-12 | 2002-12-26 | Sankyo Co Ltd | キノリン誘導体及びキノロン誘導体 |
| ATE449090T1 (de) | 2001-07-02 | 2009-12-15 | High Point Pharmaceuticals Llc | Substituierte piperazin- und diazepanderivate zur verwendung als histamin h3 rezeptormodulatoren |
| WO2003053958A1 (en) | 2001-12-20 | 2003-07-03 | Celltech R & D Limited | Quinazolinedione derivatives |
| EP1348434A1 (en) | 2002-03-27 | 2003-10-01 | Fujisawa Deutschland GmbH | Use of pyridyl amides as inhibitors of angiogenesis |
| KR20050051691A (ko) | 2002-10-11 | 2005-06-01 | 아스트라제네카 아베 | 1,4-이치환 피페리딘 유도체 및 11-베타ｈｓｄ1억제제로서의 이들의 용도 |
| JP4608852B2 (ja) | 2002-10-15 | 2011-01-12 | チッソ株式会社 | 液晶性ビニルケトン誘導体およびその重合体 |
| CA2516234A1 (en) | 2003-02-21 | 2004-09-02 | Pfizer Inc. | N-heterocyclyl-substituted amino-thiazole derivatives as protein kinase inhibitors |
| AU2004220321B2 (en) | 2003-03-12 | 2010-02-25 | Kudos Pharmaceuticals Ltd | Phthalazinone derivatives |
| US20050119266A1 (en) | 2003-10-01 | 2005-06-02 | Yan Shi | Pyrrolidine and piperidine derivatives as factor Xa inhibitors |
| SE0302811D0 (sv) | 2003-10-23 | 2003-10-23 | Astrazeneca Ab | Novel compounds |
| JP4923380B2 (ja) | 2003-12-22 | 2012-04-25 | Ｊｎｃ株式会社 | 低屈折率異方性化合物、組成物およびそれらの重合体または重合体組成物 |
| JP4932495B2 (ja) | 2004-01-23 | 2012-05-16 | アムゲン インコーポレイテッド | 化合物及び使用方法 |
| WO2005082892A2 (en) | 2004-02-17 | 2005-09-09 | Dr. Reddy's Laboratories Ltd. | Triazole compounds as antibacterial agents and pharmaceutical compositions containing them |
| EP1723146A1 (en) | 2004-03-01 | 2006-11-22 | Eli Lilly And Company | Fused pyrazole derivatives as tgf-beta signal transduction inhibitors for the treatment of fibrosis and neoplasms |
| WO2005095327A1 (ja) | 2004-03-31 | 2005-10-13 | Ajinomoto Co., Inc. | アニリン誘導体 |
| US20060167044A1 (en) | 2004-12-20 | 2006-07-27 | Arnaiz Damian O | Piperidine derivatives and their use as anti-inflammatory agents |
| US20090264415A2 (en) | 2004-12-30 | 2009-10-22 | Steven De Jonghe | Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for medical treatment |
| GB0428475D0 (en) | 2004-12-30 | 2005-02-02 | 4 Aza Bioscience Nv | Pyrido(3,2-D)pyrimidine derivatives and pharmaceutical compositions useful as medicines for the treatment of autoimmune disorders |
| TW200643015A (en) | 2005-03-11 | 2006-12-16 | Akzo Nobel Nv | 2-(4-oxo-4H-quinazolin-3-yl)acetamide derivatives |
| JP4955646B2 (ja) | 2005-03-16 | 2012-06-20 | エフ．ホフマン−ラ ロシュ アーゲー | シス−２，４，５−トリアリール−イミダゾリン及びそれらの抗癌薬としての使用 |
| JP2007016011A (ja) | 2005-06-10 | 2007-01-25 | Nippon Soda Co Ltd | 抗酸化活性を有する新規な含窒素ヘテロ環化合物、及び該化合物を含有する抗酸化薬 |
| JP2008543888A (ja) | 2005-06-24 | 2008-12-04 | ギリアード サイエンシーズ， インコーポレイテッド | ピリド（３，２−ｄ）ピリミジン、およびＣ型肝炎を治療するのに有用な医薬組成物 |
| CN102304075A (zh) | 2005-10-11 | 2012-01-04 | 因特蒙公司 | 病毒复制抑制剂 |
| EP1966132A2 (en) | 2005-12-15 | 2008-09-10 | Boehringer Ingelheim International Gmbh | Compounds which modulate the cb2 receptor |
| PE20070978A1 (es) | 2006-02-14 | 2007-11-15 | Novartis Ag | COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks) |
| MX2008012617A (es) | 2006-03-31 | 2008-10-10 | Novartis Ag | Compuestos organicos. |
| US20090124636A1 (en) | 2006-04-12 | 2009-05-14 | Pfizer Inc. | Chemical compounds |
| JP2009539937A (ja) | 2006-06-16 | 2009-11-19 | ハイ ポイント ファーマシューティカルズ，リミティド ライアビリティ カンパニー | 置換型ピペリジンカルボキサミドの医薬的使用 |
| US20080039450A1 (en) | 2006-06-22 | 2008-02-14 | Jensen Annika J | Compounds |
| FR2903101B1 (fr) | 2006-06-30 | 2008-09-26 | Servier Lab | Nouveaux derives naphtaleniques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| WO2008009078A2 (en) | 2006-07-20 | 2008-01-24 | Gilead Sciences, Inc. | 4,6-dl- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections |
| EP1903038A1 (de) | 2006-09-07 | 2008-03-26 | Bayer Schering Pharma Aktiengesellschaft | N-(1-Hetaryl-piperidin-4-yl)-(het)arylamide als EP2-Rezeptor Modulatoren |
| JP2010503676A (ja) | 2006-09-15 | 2010-02-04 | シェーリング コーポレイション | 疼痛、糖尿病および脂質代謝の障害の治療 |
| CN101679261A (zh) | 2007-03-09 | 2010-03-24 | 阿斯利康(瑞典)有限公司 | 哌嗪和哌啶mGluR5增效剂 |
| ES2705599T3 (es) | 2007-04-16 | 2019-03-26 | Abbvie Inc | Indoles sustituidos en la posición 7 como inhibidores de mcl-1 |
| JP5721308B2 (ja) | 2008-03-26 | 2015-05-20 | ローム株式会社 | 半導体装置 |
| EP3269824A1 (en) | 2008-03-28 | 2018-01-17 | Pacific Biosciences Of California, Inc. | Compositions and methods for nucleic acid sequencing |
| EP2133334A1 (en) | 2008-06-09 | 2009-12-16 | DAC S.r.l. | Heterocyclic derivatives as HDAC inhibitors |
| CA2733533C (en) | 2008-08-25 | 2013-12-17 | Irm Llc | Hedgehog pathway modulators |
| WO2010087399A1 (ja) | 2009-01-30 | 2010-08-05 | 第一三共株式会社 | ウロテンシンｉｉ受容体拮抗薬 |
| NZ595073A (en) | 2009-04-20 | 2012-11-30 | Hoffmann La Roche | Proline derivatives as cathepsin inhibitors |
| AU2010239188B2 (en) | 2009-04-22 | 2016-03-31 | Janssen Pharmaceutica Nv | Azetidinyl diamides as monoacylglycerol lipase inhibitors |
| SE533816C2 (sv) | 2009-05-06 | 2011-01-25 | Tetra Laval Holdings & Finance | Förfarande för framställning av kartongflaskor |
| US20120083476A1 (en) | 2009-06-05 | 2012-04-05 | Janssen Pharmaceutica Nv | Heteroaryl-substituted spirocyclic diamine urea modulators of fatty acid amide hydrolase |
| EP2270002A1 (en) * | 2009-06-18 | 2011-01-05 | Vereniging voor Christelijk Hoger Onderwijs, Wetenschappelijk Onderzoek en Patiëntenzorg | Quinazoline derivatives as histamine H4-receptor inhibitors for use in the treatment of inflammatory disorders |
| EP2448581B1 (en) | 2009-06-29 | 2016-12-07 | Agios Pharmaceuticals, Inc. | Therapeutic compositions and related methods of use |
| WO2011016559A1 (ja) | 2009-08-07 | 2011-02-10 | 武田薬品工業株式会社 | 複素環化合物およびその用途 |
| KR101256018B1 (ko) | 2009-08-20 | 2013-04-18 | 한국과학기술연구원 | 단백질 키나아제 저해활성을 갖는 1,3,6-치환된 인돌 화합물 |
| RU2595718C2 (ru) | 2009-09-09 | 2016-08-27 | Селджен Авиломикс Рисерч,Инк. | Ингибиторы pi3-киназы и их применение |
| EP3309152B1 (en) | 2009-12-22 | 2020-09-09 | Vertex Pharmaceuticals Incorporated | Isoindolinone inhibitors of phosphatidylinositol 3-kinase |
| AU2010339456A1 (en) | 2009-12-30 | 2012-07-05 | Celgene Avilomics Research, Inc. | Ligand-directed covalent modification of protein |
| CN102791690B (zh) | 2010-01-29 | 2015-12-02 | 大塚制药株式会社 | 作为抗癌药的二取代吡啶衍生物 |
| EP2542893A2 (en) | 2010-03-03 | 2013-01-09 | OSI Pharmaceuticals, LLC | Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors |
| MX2012010557A (es) | 2010-03-16 | 2012-10-05 | Merck Patent Gmbh | Morfolinilquinazolinas. |
| CA2791020A1 (en) | 2010-04-28 | 2011-11-03 | Daiichi Sankyo Company, Limited | [5,6] heterocyclic compound |
| TW201202230A (en) | 2010-05-24 | 2012-01-16 | Mitsubishi Tanabe Pharma Corp | Novel quinazoline compound |
| WO2011153553A2 (en) | 2010-06-04 | 2011-12-08 | The Regents Of The University Of California | Methods and compositions for kinase inhibition |
| CN103119439A (zh) | 2010-06-08 | 2013-05-22 | 纽亘技术公司 | 用于多重测序的方法和组合物 |
| US8658131B2 (en) | 2010-06-21 | 2014-02-25 | Washington University | Compounds comprising 4-benzoylpiperidine as a sigma-1-selective ligand |
| WO2012016082A1 (en) | 2010-07-30 | 2012-02-02 | Oncotherapy Science, Inc. | Quinoline derivatives and melk inhibitors containing the same |
| CN103068798A (zh) | 2010-09-03 | 2013-04-24 | 詹森药业有限公司 | 作为单酰甘油脂肪酶抑制剂的二-氮杂环丁烷二酰胺 |
| BR112013006953A2 (pt) | 2010-09-29 | 2016-07-26 | Intervet Int Bv | composto, composições farmacêutica e anti-helmíntica, uso de um composto, kit, e, método de tratamento de uma doença |
| CN103260703A (zh) | 2010-10-22 | 2013-08-21 | 詹森药业有限公司 | 作为单酰甘油脂肪酶抑制剂的哌啶-4-基-氮杂环丁烷二酰胺 |
| US20130225524A1 (en) | 2010-11-05 | 2013-08-29 | Deping Chai | Chemical Compounds |
| WO2012174489A2 (en) | 2011-06-15 | 2012-12-20 | The Ohio State University | Small molecule composite surfaces as inhibitors of protein-protein interactions |
| EA201490177A1 (ru) * | 2011-06-29 | 2014-08-29 | Оцука Фармасьютикал Ко., Лтд. | Хиназолины как терапевтические соединения и связанные с ними способы их применения |
| CN103087077B (zh) | 2011-11-03 | 2016-05-18 | 上海希迈医药科技有限公司 | 噻吩并嘧啶和呋喃并嘧啶类衍生物、其制备方法及其在医药上的应用 |
| JP2013107855A (ja) | 2011-11-22 | 2013-06-06 | Mitsubishi Tanabe Pharma Corp | 医薬組成物 |
| US9745631B2 (en) | 2011-12-20 | 2017-08-29 | Dana-Farber Cancer Institute, Inc. | Methods for diagnosing and treating oncogenic kras-associated cancer |
| WO2013096151A1 (en) | 2011-12-22 | 2013-06-27 | Glaxosmithkline Llc | Chemical compounds |
| ES2575604T3 (es) | 2012-01-13 | 2016-06-29 | Bristol-Myers Squibb Company | Compuestos de piridilo sustituidos con tiazolilo o tiadiazolilo útiles como inhibidores cinasa |
| EP2828250B1 (en) | 2012-03-19 | 2021-03-10 | Imperial College Innovations Limited | Quinazoline compounds and their use in therapy |
| WO2013155077A1 (en) | 2012-04-09 | 2013-10-17 | Board Of Regents,The University Of Texas System | Response markers for src inhibitor therapies |
| CN104379563B (zh) | 2012-04-10 | 2018-12-21 | 加利福尼亚大学董事会 | 用于治疗癌症的组合物和方法 |
| CN104685055A (zh) | 2012-05-09 | 2015-06-03 | 格兰达利斯有限公司 | 对单核苷酸KRAS突变特异的双功能短发夹RNA(bi-shRNA) |
| JO3300B1 (ar) | 2012-06-06 | 2018-09-16 | Novartis Ag | مركبات وتركيبات لتعديل نشاط egfr |
| NZ703495A (en) | 2012-07-11 | 2018-02-23 | Blueprint Medicines Corp | Inhibitors of the fibroblast growth factor receptor |
| TW201414737A (zh) | 2012-07-13 | 2014-04-16 | 必治妥美雅史谷比公司 | 作爲激酶抑制劑之咪唑并三□甲腈 |
| US20150299188A1 (en) | 2012-08-24 | 2015-10-22 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| US20150283142A1 (en) | 2013-03-15 | 2015-10-08 | Infinity Pharmaceuticals, Inc. | Treatment of cancers using pi3 kinase isoform modulators |
| WO2014159837A1 (en) | 2013-03-14 | 2014-10-02 | Convergene Llc | Methods and compositions for inhibition of bromodomain-containing proteins |
| TW201524952A (zh) | 2013-03-15 | 2015-07-01 | Araxes Pharma Llc | Ｋｒａｓ ｇ１２ｃ之共價抑制劑 |
| US9745319B2 (en) | 2013-03-15 | 2017-08-29 | Araxes Pharma Llc | Irreversible covalent inhibitors of the GTPase K-Ras G12C |
| US9227978B2 (en) | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
| JP6518656B2 (ja) | 2013-06-13 | 2019-05-22 | バイオデシー， インコーポレイテッド | 標的生体実体を標的にする生化学実体候補をスクリーニングする方法 |
| CN108440515B (zh) | 2013-07-03 | 2022-05-03 | 卡尔约药物治疗公司 | 取代的苯并呋喃基和苯并噁唑基化合物及其用途 |
| EP2832762A1 (en) | 2013-07-30 | 2015-02-04 | Sulzer Chemtech AG | A method for manufacturing poly(2-hydroxyalkanoic acid), and the poly(2-hydroxyalkanoic acid)) obtainable thereby |
| MX367085B (es) | 2013-07-31 | 2019-08-05 | Merck Patent Gmbh | Piridinas, pirimidinas y pirazinas como inhibidores de tirosina cinasa de bruton e inhibidores y usos de las mismas. |
| CN104418860B (zh) | 2013-08-20 | 2016-09-07 | 中国科学院广州生物医药与健康研究院 | 嘧啶并杂环类化合物及其药用组合物和应用 |
| JP6559123B2 (ja) * | 2013-10-10 | 2019-08-14 | アラクセス ファーマ エルエルシー | Ｋｒａｓｇ１２ｃの阻害剤 |
| JO3805B1 (ar) | 2013-10-10 | 2021-01-31 | Araxes Pharma Llc | مثبطات كراس جي12سي |
| US9376559B2 (en) | 2013-11-22 | 2016-06-28 | Exxonmobil Chemical Patents Inc. | Reverse staged impact copolymers |
| WO2015108992A1 (en) | 2014-01-15 | 2015-07-23 | Blueprint Medicines Corporation | Heterobicyclic compounds and their use as fgfr4 receptor inhibitors |
| CN105916859A (zh) | 2014-02-03 | 2016-08-31 | 卡迪拉保健有限公司 | 杂环化合物 |
| CA3175724C (en) | 2014-03-20 | 2024-01-09 | Capella Therapeutics, Inc. | Benzimidazole derivatives, and pharmaceutical compositions and methods of use thereof |
| PE20170331A1 (es) | 2014-03-24 | 2017-04-28 | Guangdong Zhongsheng Pharmaceutical Co Ltd | Derivados quinolina como inhibidores smo |
| MA40074A (fr) | 2014-05-30 | 2015-12-03 | Univ Columbia | Composés liant ras multivalents |
| EP3160486B1 (en) | 2014-06-27 | 2020-11-18 | Celgene Corporation | Compositions and methods for inducing conformational changes in cereblon other e3 ubiquitin ligases |
| JO3556B1 (ar) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| WO2016049568A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Methods and compositions for inhibition of ras |
| WO2016049565A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Compositions and methods for inhibition of ras |
| JP2017528498A (ja) | 2014-09-25 | 2017-09-28 | アラクセス ファーマ エルエルシー | Ｋｒａｓ ｇ１２ｃ変異体タンパク質のインヒビター |
| HK1245677A1 (zh) | 2015-01-23 | 2018-08-31 | Aclaris Therapeutics, Inc. | 用於治疗炎症和癌症的杂环itk抑制剂 |
| MX382355B (es) * | 2015-04-10 | 2025-03-13 | Araxes Pharma Llc | Compuestos de quinazolina sustituidos y métodos de uso de los mismos. |
| EP3283462B1 (en) | 2015-04-15 | 2020-12-02 | Araxes Pharma LLC | Fused-tricyclic inhibitors of kras and methods of use thereof |
| WO2017015562A1 (en) | 2015-07-22 | 2017-01-26 | Araxes Pharma Llc | Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins |
| US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| EP3356351A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| WO2017058728A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| EP3356354A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| EP3356349A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| WO2017058792A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| US10689356B2 (en) | 2015-09-28 | 2020-06-23 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| EP3356347A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| WO2017070256A2 (en) | 2015-10-19 | 2017-04-27 | Araxes Pharma Llc | Method for screening inhibitors of ras |
| US10457669B2 (en) | 2015-10-21 | 2019-10-29 | Otsuka Pharmaceutical Co., Ltd. | Benzolactam compounds as protein kinase inhibitors |
| EP3377481A1 (en) * | 2015-11-16 | 2018-09-26 | Araxes Pharma LLC | 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof |
| WO2017100546A1 (en) | 2015-12-09 | 2017-06-15 | Araxes Pharma Llc | Methods for preparation of quinazoline derivatives |
| US10822312B2 (en) | 2016-03-30 | 2020-11-03 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use |
| US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
| EP3519402A1 (en) | 2016-09-29 | 2019-08-07 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| US10377743B2 (en) | 2016-10-07 | 2019-08-13 | Araxes Pharma Llc | Inhibitors of RAS and methods of use thereof |
| KR102540515B1 (ko) | 2016-11-03 | 2023-06-05 | 코버스 파마슈티칼스, 인크. | 인터류킨-2-유도성 t-세포 키나제를 조절하기 위한 화합물 및 방법 |
| US11136308B2 (en) | 2017-01-26 | 2021-10-05 | Araxes Pharma Llc | Substituted quinazoline and quinazolinone compounds and methods of use thereof |
| US11358959B2 (en) | 2017-01-26 | 2022-06-14 | Araxes Pharma Llc | Benzothiophene and benzothiazole compounds and methods of use thereof |
| CN110382482A (zh) | 2017-01-26 | 2019-10-25 | 亚瑞克西斯制药公司 | 稠合的杂-杂二环化合物及其使用方法 |
| WO2018140513A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer |
| EP3573966A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Fused n-heterocyclic compounds and methods of use thereof |
| EP3573954A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Fused bicyclic benzoheteroaromatic compounds and methods of use thereof |
| JOP20190186A1 (ar) | 2017-02-02 | 2019-08-01 | Astellas Pharma Inc | مركب كينازولين |
| CN110869358A (zh) | 2017-05-25 | 2020-03-06 | 亚瑞克西斯制药公司 | Kras的共价抑制剂 |
| JP2020521741A (ja) | 2017-05-25 | 2020-07-27 | アラクセス ファーマ エルエルシー | がんの処置のための化合物およびその使用の方法 |
| CN110831933A (zh) | 2017-05-25 | 2020-02-21 | 亚瑞克西斯制药公司 | 喹唑啉衍生物作为突变kras、hras或nras的调节剂 |
| MX2020010836A (es) | 2018-05-04 | 2021-01-08 | Amgen Inc | Inhibidores de kras g12c y métodos para su uso. |
| BR112021001709A2 (pt) | 2018-08-01 | 2021-05-04 | Araxes Pharma Llc | compostos espiro heterocíclicos e métodos de uso dos mesmos para o tratamento de câncer |
| WO2020086739A1 (en) | 2018-10-24 | 2020-04-30 | Araxes Pharma Llc | 2-(2-acryloyl-2,6-diazaspiro[3.4]octan-6-yl)-6-(1h-indazol-4-yl)-benzonitrile derivatives and related compounds as inhibitors of g12c mutant kras protein for inhibiting tumor metastasis |
| KR20210097715A (ko) | 2018-11-29 | 2021-08-09 | 아락세스 파마 엘엘씨 | 암 치료용 화합물 및 이의 사용 방법 |
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2016
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- 2016-11-16 KR KR1020247022782A patent/KR102932353B1/ko active Active
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- 2016-11-16 JP JP2018524781A patent/JP7015059B2/ja active Active
- 2016-11-16 US US15/353,402 patent/US10414757B2/en active Active
- 2016-11-16 KR KR1020187016874A patent/KR20180081596A/ko not_active Ceased
- 2016-11-16 MX MX2018005967A patent/MX2018005967A/es unknown
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- 2016-11-16 EA EA201891191A patent/EA038635B9/ru unknown
- 2016-11-16 TW TW105137373A patent/TW201726656A/zh unknown
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| US20200181123A1 (en) | 2020-06-11 |
| EA201891191A1 (ru) | 2018-12-28 |
| KR20260047240A (ko) | 2026-04-07 |
| US10414757B2 (en) | 2019-09-17 |
| KR20180081596A (ko) | 2018-07-16 |
| EA038635B9 (ru) | 2021-10-26 |
| AU2016355433B2 (en) | 2021-05-20 |
| KR102932353B1 (ko) | 2026-02-27 |
| WO2017087528A1 (en) | 2017-05-26 |
| JP2022050628A (ja) | 2022-03-30 |
| US20170197945A1 (en) | 2017-07-13 |
| CN108779097A (zh) | 2018-11-09 |
| US11021470B2 (en) | 2021-06-01 |
| JP7015059B2 (ja) | 2022-02-15 |
| CA3005089A1 (en) | 2017-05-26 |
| JP2024028804A (ja) | 2024-03-05 |
| EA038635B1 (ru) | 2021-09-27 |
| AU2016355433C1 (en) | 2021-12-16 |
| EP3377481A1 (en) | 2018-09-26 |
| AU2016355433B9 (en) | 2021-06-03 |
| JP2018533611A (ja) | 2018-11-15 |
| MX2018005967A (es) | 2018-08-29 |
| KR20240113606A (ko) | 2024-07-22 |
| AU2016355433A1 (en) | 2018-06-28 |
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