MX2017013275A - Inhibidores triciclicos fusionados de kras y metodos de uso de los mismos. - Google Patents
Inhibidores triciclicos fusionados de kras y metodos de uso de los mismos.Info
- Publication number
- MX2017013275A MX2017013275A MX2017013275A MX2017013275A MX2017013275A MX 2017013275 A MX2017013275 A MX 2017013275A MX 2017013275 A MX2017013275 A MX 2017013275A MX 2017013275 A MX2017013275 A MX 2017013275A MX 2017013275 A MX2017013275 A MX 2017013275A
- Authority
- MX
- Mexico
- Prior art keywords
- methods
- compounds
- kras
- fused
- inhibitors
- Prior art date
Links
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
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D219/00—Heterocyclic compounds containing acridine or hydrogenated acridine ring systems
- C07D219/04—Heterocyclic compounds containing acridine or hydrogenated acridine ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
- C07D219/08—Nitrogen atoms
- C07D219/10—Nitrogen atoms attached in position 9
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D219/00—Heterocyclic compounds containing acridine or hydrogenated acridine ring systems
- C07D219/04—Heterocyclic compounds containing acridine or hydrogenated acridine ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
- C07D219/08—Nitrogen atoms
- C07D219/10—Nitrogen atoms attached in position 9
- C07D219/12—Amino-alkylamino radicals attached in position 9
-
- 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
- C07D491/04—Ortho-condensed systems
- C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562147955P | 2015-04-15 | 2015-04-15 | |
| PCT/US2016/027673 WO2016168540A1 (en) | 2015-04-15 | 2016-04-15 | Fused-tricyclic inhibitors of kras and methods of use thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2017013275A true MX2017013275A (es) | 2018-01-26 |
Family
ID=55806883
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2017013275A MX2017013275A (es) | 2015-04-15 | 2016-04-15 | Inhibidores triciclicos fusionados de kras y metodos de uso de los mismos. |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US10428064B2 (enExample) |
| EP (1) | EP3283462B1 (enExample) |
| JP (1) | JP6789239B2 (enExample) |
| CA (1) | CA2982360A1 (enExample) |
| ES (1) | ES2856880T3 (enExample) |
| MX (1) | MX2017013275A (enExample) |
| WO (1) | WO2016168540A1 (enExample) |
Families Citing this family (152)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UY35464A (es) | 2013-03-15 | 2014-10-31 | Araxes Pharma Llc | Inhibidores covalentes de kras g12c. |
| TWI659021B (zh) | 2013-10-10 | 2019-05-11 | 亞瑞克西斯製藥公司 | Kras g12c之抑制劑 |
| JO3556B1 (ar) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| AR102094A1 (es) | 2014-09-25 | 2017-02-01 | Araxes Pharma Llc | Inhibidores de proteínas kras con una mutación g12c |
| US10011600B2 (en) | 2014-09-25 | 2018-07-03 | Araxes Pharma Llc | Methods and compositions for inhibition of Ras |
| EA201792214A1 (ru) | 2015-04-10 | 2018-01-31 | Араксис Фарма Ллк | Соединения замещенного хиназолина |
| US10428064B2 (en) | 2015-04-15 | 2019-10-01 | 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 |
| EP3356353A1 (en) | 2015-09-28 | 2018-08-08 | 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 |
| EP3356359B1 (en) | 2015-09-28 | 2021-10-20 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| WO2017058902A1 (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 |
| EP3356347A1 (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 |
| WO2017070256A2 (en) | 2015-10-19 | 2017-04-27 | Araxes Pharma Llc | Method for screening inhibitors of ras |
| KR20240113606A (ko) | 2015-11-16 | 2024-07-22 | 아락세스 파마 엘엘씨 | 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법 |
| US9988357B2 (en) | 2015-12-09 | 2018-06-05 | Araxes Pharma Llc | Methods for preparation of quinazoline derivatives |
| WO2017172979A1 (en) | 2016-03-30 | 2017-10-05 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use |
| WO2017201161A1 (en) | 2016-05-18 | 2017-11-23 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| 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 |
| CN110036010A (zh) | 2016-09-29 | 2019-07-19 | 亚瑞克西斯制药公司 | Kras g12c突变蛋白的抑制剂 |
| EP3523289A1 (en) | 2016-10-07 | 2019-08-14 | Araxes Pharma LLC | Heterocyclic compounds as inhibitors of ras and methods of use thereof |
| HRP20211642T1 (hr) | 2016-12-22 | 2022-01-21 | Amgen Inc. | Derivati benzizotiazola, izotiazolo[3,4-b]piridina, kinazolina, ftalazina, pirido[2,3-d]piridazina i pirido[2,3-d]pirimidina kao inhibitori kras g12c za liječenje raka pluća, gušterače ili kolorektalnog karcinoma |
| 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 |
| US11136308B2 (en) | 2017-01-26 | 2021-10-05 | Araxes Pharma Llc | Substituted quinazoline and quinazolinone compounds and methods of use thereof |
| JP7327802B2 (ja) | 2017-01-26 | 2023-08-16 | アラクセス ファーマ エルエルシー | 縮合ヘテロ-ヘテロ二環式化合物およびその使用方法 |
| EP3573954A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Fused bicyclic benzoheteroaromatic compounds and methods of use thereof |
| WO2018140599A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | Benzothiophene and benzothiazole compounds and methods of use thereof |
| JOP20190272A1 (ar) | 2017-05-22 | 2019-11-21 | Amgen Inc | مثبطات kras g12c وطرق لاستخدامها |
| EP3630746A1 (en) | 2017-05-25 | 2020-04-08 | Araxes Pharma LLC | Compounds and methods of use thereof for treatment of cancer |
| EP3630747A1 (en) | 2017-05-25 | 2020-04-08 | Araxes Pharma LLC | Quinazoline derivatives as modulators of mutant kras, hras or nras |
| EP3630745A2 (en) | 2017-05-25 | 2020-04-08 | Araxes Pharma LLC | Covalent inhibitors of kras |
| CN109464707A (zh) * | 2017-09-07 | 2019-03-15 | 天津大学 | 用于骨修复的3d打印高强度温敏超分子水凝胶支架 |
| WO2019051291A1 (en) * | 2017-09-08 | 2019-03-14 | Amgen Inc. | Inhibitors of kras g12c and methods of using the same |
| HUE061599T2 (hu) | 2017-11-15 | 2023-07-28 | Mirati Therapeutics Inc | KRas G12C inhibotorok |
| US10647715B2 (en) | 2017-11-15 | 2020-05-12 | Mirati Therapeutics, Inc. | KRas G12C inhibitors |
| TW201938561A (zh) * | 2017-12-08 | 2019-10-01 | 瑞典商阿斯特捷利康公司 | 化學化合物 |
| JP7289839B2 (ja) * | 2018-01-19 | 2023-06-12 | メッドシャイン ディスカバリー インコーポレイテッド | Krasg12c突然変異タンパク質阻害剤としてのピリドン-ピリミジン系誘導体 |
| CA3099118A1 (en) | 2018-05-04 | 2019-11-07 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| JP7266043B2 (ja) | 2018-05-04 | 2023-04-27 | アムジエン・インコーポレーテツド | KRas G12C阻害剤及びそれを使用する方法 |
| 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 |
| JP7361720B2 (ja) | 2018-05-10 | 2023-10-16 | アムジエン・インコーポレーテツド | がんの治療のためのkras g12c阻害剤 |
| EP3802535B1 (en) | 2018-06-01 | 2022-12-14 | Amgen, Inc | Kras g12c inhibitors and methods of using the same |
| AU2019336588B2 (en) | 2018-06-12 | 2022-07-28 | Amgen Inc. | KRAS G12C inhibitors encompassing a piperazine ring and use thereof in the treatment of cancer |
| JP2021532157A (ja) | 2018-08-01 | 2021-11-25 | アラクセス ファーマ エルエルシー | がんを処置するための複素環式スピロ化合物およびその使用方法 |
| AU2019340436B2 (en) | 2018-09-10 | 2025-04-17 | Mirati Therapeutics, Inc. | Combination therapies |
| EP3849536A4 (en) | 2018-09-10 | 2022-06-29 | Mirati Therapeutics, Inc. | Combination therapies |
| WO2020055756A1 (en) | 2018-09-10 | 2020-03-19 | Mirati Therapeutics, Inc. | Combination therapies |
| TWI827677B (zh) | 2018-09-18 | 2024-01-01 | 美商尼坎醫療公司 | 作為src同源-2磷酸酶抑制劑之稠合三環衍生物 |
| WO2020085493A1 (ja) | 2018-10-26 | 2020-04-30 | 大鵬薬品工業株式会社 | 新規なインダゾール化合物又はその塩 |
| 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 |
| 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 |
| AU2019384118B2 (en) | 2018-11-19 | 2025-06-12 | Amgen Inc. | KRAS G12C inhibitors and methods of using the same |
| MX2021002804A (es) | 2018-12-05 | 2021-07-15 | Mirati Therapeutics Inc | Terapias de combinacion. |
| 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 |
| EP4249000A3 (en) | 2019-02-12 | 2023-12-27 | Novartis AG | Pharmaceutical combination comprising tno155 and a krasg12c inhibitor |
| WO2020173935A1 (en) | 2019-02-26 | 2020-09-03 | Boehringer Ingelheim International Gmbh | New isoindolinone substituted indoles and derivatives as ras inhibitors |
| JP7453989B2 (ja) | 2019-03-05 | 2024-03-21 | アストラゼネカ・アクチエボラーグ | 抗癌剤として有用な縮合三環式化合物 |
| EP3738593A1 (en) | 2019-05-14 | 2020-11-18 | Amgen, Inc | Dosing of kras inhibitor for treatment of cancers |
| US20220227729A1 (en) | 2019-05-21 | 2022-07-21 | Bayer Aktiengesellschaft | Identification and use of kras inhibitors |
| NZ782284A (en) | 2019-05-21 | 2024-11-29 | Amgen Inc | Solid state forms |
| CN112300173B (zh) * | 2019-07-30 | 2021-10-01 | 上海凌达生物医药有限公司 | 一类含氮多环类化合物、制备方法和用途 |
| KR20220071193A (ko) | 2019-08-29 | 2022-05-31 | 미라티 테라퓨틱스, 인크. | Kras g12d 억제제 |
| WO2021055728A1 (en) * | 2019-09-18 | 2021-03-25 | Merck Sharp & Dohme Corp. | Small molecule inhibitors of kras g12c mutant |
| US12122787B2 (en) | 2019-09-20 | 2024-10-22 | Shanghai Jemincare Pharmaceuticals Co., Ltd | Fused pyridone compound, and preparation method therefor and use thereof |
| WO2021052499A1 (zh) * | 2019-09-20 | 2021-03-25 | 上海济煜医药科技有限公司 | 稠合吡啶酮类化合物及其制备方法和应用 |
| US11890285B2 (en) | 2019-09-24 | 2024-02-06 | Mirati Therapeutics, Inc. | Combination therapies |
| JP7340100B2 (ja) | 2019-10-28 | 2023-09-06 | メルク・シャープ・アンド・ドーム・エルエルシー | Kras g12c変異型の小分子阻害薬 |
| CA3159559A1 (en) | 2019-11-04 | 2021-05-14 | Revolution Medicines, Inc. | Ras inhibitors |
| CN114867735A (zh) | 2019-11-04 | 2022-08-05 | 锐新医药公司 | Ras抑制剂 |
| KR20250175006A (ko) | 2019-11-04 | 2025-12-15 | 레볼루션 메디슨즈, 인크. | Ras 억제제 |
| CN114980976A (zh) | 2019-11-27 | 2022-08-30 | 锐新医药公司 | 共价ras抑制剂及其用途 |
| 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 |
| EP4076418A4 (en) | 2019-12-20 | 2024-01-24 | Mirati Therapeutics, Inc. | Sos1 inhibitors |
| CN112094269B (zh) * | 2020-01-01 | 2021-12-07 | 上海凌达生物医药有限公司 | 一类饱和六元环并杂环类化合物、制备方法和用途 |
| WO2021150613A1 (en) * | 2020-01-20 | 2021-07-29 | Incyte Corporation | Spiro compounds as inhibitors of kras |
| GB202001344D0 (en) | 2020-01-31 | 2020-03-18 | Redx Pharma Plc | Ras Inhibitors |
| WO2023205701A1 (en) | 2022-04-20 | 2023-10-26 | Kumquat Biosciences Inc. | Macrocyclic heterocycles and uses thereof |
| CN112142735B (zh) * | 2020-04-09 | 2021-09-17 | 上海凌达生物医药有限公司 | 一类稠和氰基吡啶类化合物、制备方法和用途 |
| US11739102B2 (en) | 2020-05-13 | 2023-08-29 | Incyte Corporation | Fused pyrimidine compounds as KRAS inhibitors |
| TW202210633A (zh) | 2020-06-05 | 2022-03-16 | 法商昂席歐公司 | 用於治療癌症之dbait分子與kras抑制劑的組合 |
| MX2022016355A (es) | 2020-06-18 | 2023-04-03 | Revolution Medicines Inc | Metodos para retardar, prevenir, y tratar la resistencia adquirida a inhibidores de ras. |
| WO2022047093A1 (en) | 2020-08-28 | 2022-03-03 | Incyte Corporation | Vinyl imidazole compounds as inhibitors of kras |
| KR20230081726A (ko) | 2020-09-03 | 2023-06-07 | 레볼루션 메디슨즈, 인크. | Shp2 돌연변이가 있는 악성 종양을 치료하기 위한 sos1 억제제의 용도 |
| US12286431B2 (en) | 2020-09-11 | 2025-04-29 | Mirati Therapeutics, Inc. | Crystalline forms of a KRas G12C inhibitor |
| JP2023540388A (ja) | 2020-09-11 | 2023-09-22 | メッドシャイン ディスカバリー インコーポレイテッド | アゼチジン置換化合物の結晶形 |
| IL301298A (en) | 2020-09-15 | 2023-05-01 | Revolution Medicines Inc | Indole derivatives as RAS inhibitors in cancer therapy |
| CA3196277A1 (en) | 2020-09-23 | 2022-03-31 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| US11767320B2 (en) | 2020-10-02 | 2023-09-26 | Incyte Corporation | Bicyclic dione compounds as inhibitors of KRAS |
| CN114539286B (zh) * | 2020-11-24 | 2024-02-02 | 成都百裕制药股份有限公司 | 哌嗪衍生物及其在医药上的应用 |
| AU2021401232A1 (en) | 2020-12-15 | 2023-06-22 | Mirati Therapeutics, Inc. | Azaquinazoline pan-kras inhibitors |
| WO2022133038A1 (en) | 2020-12-16 | 2022-06-23 | Mirati Therapeutics, Inc. | Tetrahydropyridopyrimidine pan-kras inhibitors |
| WO2022133345A1 (en) | 2020-12-18 | 2022-06-23 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| WO2022140246A1 (en) | 2020-12-21 | 2022-06-30 | Hangzhou Jijing Pharmaceutical Technology Limited | Methods and compounds for targeted autophagy |
| AU2021409561A1 (en) | 2020-12-22 | 2023-07-06 | Nikang Therapeutics, Inc. | Compounds for degrading cyclin-dependent kinase 2 via ubiquitin proteosome pathway |
| US12077539B2 (en) | 2021-03-22 | 2024-09-03 | Incyte Corporation | Imidazole and triazole KRAS inhibitors |
| CN115124533A (zh) * | 2021-03-26 | 2022-09-30 | 浙江海正药业股份有限公司 | 四环类衍生物、其制备方法和其医药上的用途 |
| TW202309052A (zh) | 2021-05-05 | 2023-03-01 | 美商銳新醫藥公司 | Ras抑制劑 |
| CN117616031A (zh) | 2021-05-05 | 2024-02-27 | 锐新医药公司 | 用于治疗癌症的ras抑制剂 |
| 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 |
| CA3224674A1 (en) | 2021-07-07 | 2023-01-12 | Pei Gan | Tricyclic compounds as inhibitors of kras |
| US20230114765A1 (en) * | 2021-07-14 | 2023-04-13 | Incyte Corporation | Tricyclic compounds as inhibitors of kras |
| EP4370522A1 (en) | 2021-07-14 | 2024-05-22 | Nikang Therapeutics, Inc. | Alkylidene derivatives as kras inhibitors |
| EP4396187A1 (en) | 2021-08-31 | 2024-07-10 | Incyte Corporation | Naphthyridine compounds as inhibitors of kras |
| US20240374571A1 (en) | 2021-09-01 | 2024-11-14 | 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 |
| AU2022349569A1 (en) | 2021-09-22 | 2024-04-04 | Sichuan Huiyu Pharmaceutical Co., Ltd. | Pyridine derivative and use thereof |
| WO2023056421A1 (en) | 2021-10-01 | 2023-04-06 | Incyte Corporation | Pyrazoloquinoline kras inhibitors |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| CR20240197A (es) | 2021-10-14 | 2024-08-07 | Incyte Corp | Compuestos de quinolina como inhibidores de kras |
| WO2023114954A1 (en) | 2021-12-17 | 2023-06-22 | Genzyme Corporation | Pyrazolopyrazine compounds as shp2 inhibitors |
| 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 |
| JP2025510572A (ja) | 2022-03-08 | 2025-04-15 | レボリューション メディシンズ インコーポレイテッド | 免疫不応性肺癌を治療するための方法 |
| 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 |
| EP4536363A1 (en) | 2022-06-08 | 2025-04-16 | Nikang Therapeutics, Inc. | Sulfamide derivatives as cyclin-dependent kinase 2 inhibitors |
| IL317476A (en) | 2022-06-10 | 2025-02-01 | Revolution Medicines Inc | Macrocyclic RAS inhibitors |
| GB202212641D0 (en) | 2022-08-31 | 2022-10-12 | Jazz Pharmaceuticals Ireland Ltd | Novel compounds |
| WO2024091409A1 (en) * | 2022-10-24 | 2024-05-02 | Nikang Therapeutics, Inc. | Tricyclic derivatives as kras inhibitors |
| KR20250116016A (ko) | 2022-11-09 | 2025-07-31 | 레볼루션 메디슨즈, 인크. | 화합물, 복합체 및 이들의 제조 및 사용 방법 |
| WO2024102849A1 (en) | 2022-11-11 | 2024-05-16 | Nikang Therapeutics, Inc. | Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 via ubiquitin proteasome pathway |
| WO2024206858A1 (en) | 2023-03-30 | 2024-10-03 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| AU2024243852A1 (en) | 2023-04-07 | 2025-11-06 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| WO2024211663A1 (en) | 2023-04-07 | 2024-10-10 | Revolution Medicines, Inc. | Condensed macrocyclic compounds as ras inhibitors |
| US20240352038A1 (en) | 2023-04-14 | 2024-10-24 | 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 |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| AU2024276994A1 (en) | 2023-05-24 | 2025-10-23 | 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 |
| TW202530228A (zh) | 2023-10-12 | 2025-08-01 | 美商銳新醫藥公司 | Ras抑制劑 |
| US12466840B2 (en) | 2023-10-20 | 2025-11-11 | Merck Sharp & Dohme Llc | Small molecule inhibitors of KRAS proteins |
| WO2025117616A1 (en) | 2023-11-27 | 2025-06-05 | 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 |
| 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 |
Family Cites Families (181)
| 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 |
| US5033252A (en) | 1987-12-23 | 1991-07-23 | Entravision, Inc. | Method of packaging and sterilizing a pharmaceutical product |
| US5052558A (en) | 1987-12-23 | 1991-10-01 | Entravision, Inc. | Packaged 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 |
| US6051380A (en) | 1993-11-01 | 2000-04-18 | Nanogen, Inc. | Methods and procedures for molecular biological analysis and diagnostics |
| US6017696A (en) | 1993-11-01 | 2000-01-25 | Nanogen, Inc. | Methods for electronic stringency control 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 |
| DE59304298D1 (de) | 1993-01-04 | 1996-11-28 | Schneider Willi Ingbuero | Schneidmaschine |
| 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 |
| ATE247716T1 (de) | 1994-02-07 | 2003-09-15 | Beckman Coulter Inc | 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 |
| WO1996013262A1 (en) | 1994-10-27 | 1996-05-09 | Merck & Co., Inc. | Muscarine antagonists |
| US5863949A (en) | 1995-03-08 | 1999-01-26 | Pfizer Inc | Arylsulfonylamino hydroxamic acid derivatives |
| DE69519751T2 (de) | 1995-04-20 | 2001-04-19 | Pfizer Inc., New York | Arylsulfonamido-substituierte hydroxamsäure derivate als inhibitoren von mmp und tnf |
| FR2734816B1 (fr) | 1995-05-31 | 1997-07-04 | Adir | Nouveaux aryl (alkyl) propylamides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| EP2258726A1 (en) | 1995-06-14 | 2010-12-08 | The Regents of the University of California | High affinity human antibodies to c-erbB-2 |
| EP0780386B1 (en) | 1995-12-20 | 2002-10-02 | F. Hoffmann-La Roche Ag | Matrix metalloprotease inhibitors |
| 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 |
| SK3799A3 (en) | 1996-07-18 | 2000-03-13 | Pfizer | Phosphinate compounds, pharmaceutical compositions, method for inhibiting of matrix metalloproteases or of producing tnf and method of treatment |
| CN1228083A (zh) | 1996-08-23 | 1999-09-08 | 美国辉瑞有限公司 | 芳基磺酰氨基异羟肟酸衍生物 |
| US5777324A (en) | 1996-09-19 | 1998-07-07 | Sequenom, Inc. | Method and apparatus for maldi analysis |
| ES2224277T3 (es) | 1997-01-06 | 2005-03-01 | Pfizer Inc. | Derivados de sulfonas ciclicas. |
| CA2279276C (en) | 1997-02-03 | 2005-09-13 | Pfizer Products Inc. | Arylsulfonylamino hydroxamic acid derivatives |
| GB9702194D0 (en) | 1997-02-04 | 1997-03-26 | Lilly Co Eli | Sulphonide derivatives |
| AU5493598A (en) | 1997-02-07 | 1998-08-26 | Pfizer Inc. | N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases |
| NZ336836A (en) | 1997-02-11 | 2001-02-23 | Pfizer | Arylsulfonyl hydroxamic acid derivatives suitable for a broad range of medicinal treatments |
| US6291464B1 (en) | 1997-02-17 | 2001-09-18 | Fujisawa Pharmaceutical Co., Ltd. | Aminopiperazine derivatives |
| US5919626A (en) | 1997-06-06 | 1999-07-06 | Orchid Bio Computer, Inc. | Attachment of unmodified nucleic acids to silanized solid phase surfaces |
| HUP0002954A3 (en) | 1997-06-17 | 2002-11-28 | Schering Corp | Novel n-substituted urea inhibitors of farnesyl-protein transferase |
| BR9811868A (pt) | 1997-08-08 | 2000-08-15 | Pfizer Prod Inc | Derivados de ácido ariloxiarilsulfonilamino hidroxâmico |
| 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 |
| IL136637A0 (en) | 1997-12-22 | 2001-06-14 | Du Pont Pharm Co | Nitrogen containing heteroaromatics with ortho-substituted pi's as factor xa inhibitors |
| GB9801690D0 (en) | 1998-01-27 | 1998-03-25 | Pfizer Ltd | Therapeutic agents |
| PA8469401A1 (es) | 1998-04-10 | 2000-05-24 | Pfizer Prod Inc | Derivados biciclicos del acido hidroxamico |
| PA8469501A1 (es) | 1998-04-10 | 2000-09-29 | Pfizer Prod Inc | Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico |
| JP3662850B2 (ja) | 1998-06-24 | 2005-06-22 | イルミナ インコーポレイテッド | 微小球を有するアレイセンサーのデコード |
| ATE260255T1 (de) | 1998-11-05 | 2004-03-15 | Pfizer Prod Inc | 5-oxo-pyrrolidine-2-carbonsäure- hydroxamidderivate |
| US6429027B1 (en) | 1998-12-28 | 2002-08-06 | Illumina, Inc. | Composite arrays utilizing microspheres |
| EP1081137A1 (en) | 1999-08-12 | 2001-03-07 | Pfizer Products Inc. | Selective inhibitors of aggrecanase in osteoarthritis treatment |
| DK1431303T3 (en) | 1999-09-13 | 2014-02-17 | Nugen Technologies Inc | A composition for isothermal linear amplification of polynucleotide sequences |
| AR033356A1 (es) | 2000-03-21 | 2003-12-17 | Procter & Gamble | Compuesto que contiene una cadena lateral heterociclica, composicion farmaceutica que lo comprende y uso de dicho compuesto para la fabricacion de un medicamento |
| CN1433413A (zh) | 2000-06-05 | 2003-07-30 | 东亚制药株式会社 | 新的噁唑烷酮衍生物及其制备方法 |
| TWI227231B (en) | 2000-07-12 | 2005-02-01 | Novartis Ag | 4-benzoyl-piperidine derivatives for treating conditions mediated by CCR-3 |
| DK1315715T3 (da) | 2000-08-18 | 2008-11-17 | Millennium Pharm Inc | Quinazolinderivater som kinaseinhibitorer |
| 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 |
| DE60234453D1 (de) | 2001-07-02 | 2009-12-31 | High Point Pharmaceuticals Llc | Substituierte piperazin- und diazepanderivate zur verwendung als histamin h3 rezeptormodulatoren |
| EP1348434A1 (en) | 2002-03-27 | 2003-10-01 | Fujisawa Deutschland GmbH | Use of pyridyl amides as inhibitors of angiogenesis |
| WO2004033427A1 (en) | 2002-10-11 | 2004-04-22 | Astrazeneca Ab | 1,4-disubstituted piperidine derivatives and their use as 11-betahsd1 inhibitors |
| 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 |
| EP1597256A1 (en) | 2003-02-21 | 2005-11-23 | Pfizer Inc. | N-heterocyclyl-substituted amino-thiazole derivatives as protein kinase inhibitors |
| WO2004080976A1 (en) | 2003-03-12 | 2004-09-23 | Kudos Pharmaceuticals Limited | Phthalazinone derivatives |
| US20050119266A1 (en) | 2003-10-01 | 2005-06-02 | Yan Shi | Pyrrolidine and piperidine derivatives as factor Xa inhibitors |
| 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 |
| EA011402B1 (ru) | 2004-01-23 | 2009-02-27 | Эмджен Инк. | Азотсодержащие гетероциклические производные и их фармацевтические применения |
| WO2005082892A2 (en) | 2004-02-17 | 2005-09-09 | Dr. Reddy's Laboratories Ltd. | Triazole compounds as antibacterial agents and pharmaceutical compositions containing them |
| JP4775259B2 (ja) | 2004-03-31 | 2011-09-21 | 味の素株式会社 | 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 |
| MX2007011151A (es) | 2005-03-16 | 2007-10-17 | Hoffmann La Roche | Cis-2,4,5-triaril-imidazolinas y su uso como medicamentos anticancer. |
| 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 |
| KR20080066949A (ko) | 2005-10-11 | 2008-07-17 | 인터뮨, 인크. | 바이러스 복제 억제제 |
| CA2632030A1 (en) | 2005-12-15 | 2007-06-21 | 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) |
| EP2004643A1 (en) | 2006-03-31 | 2008-12-24 | Novartis AG | Organic compounds |
| US20090124636A1 (en) | 2006-04-12 | 2009-05-14 | Pfizer Inc. | Chemical compounds |
| WO2007144394A2 (en) | 2006-06-16 | 2007-12-21 | High Point Pharmaceuticals, Llc. | Pharmaceutical use of substituted piperidine carboxamides |
| WO2007147874A1 (en) | 2006-06-22 | 2007-12-27 | Biovitrum Ab (Publ) | Pyridine and pyrazine derivatives as mnk kinase inhibitors |
| FR2903101B1 (fr) | 2006-06-30 | 2008-09-26 | Servier Lab | Nouveaux derives naphtaleniques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| US9259426B2 (en) | 2006-07-20 | 2016-02-16 | Gilead Sciences, Inc. | 4,6-di- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections |
| 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 |
| EP3170904B1 (en) | 2008-03-28 | 2017-08-16 | 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 |
| BRPI0917936A2 (pt) | 2008-08-25 | 2017-07-11 | Irm Llc | Moduladores de via hedgehog |
| 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 |
| UA106748C2 (uk) | 2009-04-20 | 2014-10-10 | Ф. Хоффманн-Ля Рош Аг | Похідні проліну як інгібітори катепсину |
| AR076380A1 (es) | 2009-04-22 | 2011-06-08 | Janssen Pharmaceutica Nv | Azetidinil diamidas inhibidoras de monoacilglicerol lipasa(mgl), composiciones farmaceuticas que las contienen y uso de las mismas para el tratamiento de enfermedades y patologias que incluyen dolor inflamatorio. |
| 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 |
| KR101256018B1 (ko) | 2009-08-20 | 2013-04-18 | 한국과학기술연구원 | 단백질 키나아제 저해활성을 갖는 1,3,6-치환된 인돌 화합물 |
| MX339584B (es) | 2009-09-09 | 2016-06-01 | Avila Therapeutics Inc | Inhibidores de pi3 cinasa y usos de los mismos. |
| MX2012007403A (es) | 2009-12-22 | 2012-09-12 | Vertex Pharma | Inhibidores de isoindolinona de fosfatidinositol 3-cinasa. |
| SG181965A1 (en) | 2009-12-30 | 2012-08-30 | Avila Therapeutics Inc | Ligand-directed covalent modification of protein |
| TWI404713B (zh) | 2010-01-29 | 2013-08-11 | Otsuka Pharma Co Ltd | 雜環化合物 |
| EP2547664B1 (de) | 2010-03-16 | 2016-05-04 | Merck Patent GmbH | Morpholinylchinazoline |
| EP2565185A1 (en) | 2010-04-28 | 2013-03-06 | 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 |
| CN103153063B (zh) | 2010-07-30 | 2016-02-17 | 肿瘤疗法科学股份有限公司 | 喹啉衍生物及含有其的melk抑制剂 |
| RU2013114771A (ru) | 2010-09-03 | 2014-10-10 | Янссен Фармацевтика Нв | Диамиды азетидинила как ингибиторы моноацилглицерол липазы |
| 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 |
| CA2815350A1 (en) | 2010-10-22 | 2012-04-26 | Janssen Pharmaceutica Nv | Piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors |
| US9260484B2 (en) | 2011-06-15 | 2016-02-16 | Ohio State Innovation Foundation | Small molecule composite surfaces as inhibitors of protein-protein interactions |
| EP2726485A1 (en) | 2011-06-29 | 2014-05-07 | Otsuka Pharmaceutical Co., Ltd. | Quinazolines as therapeutic compounds and related methods of use |
| 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 |
| WO2013106641A1 (en) | 2012-01-13 | 2013-07-18 | Bristol-Myers Squibb Company | Thiazolyl- or thiadiazolyl-substituted pyridyl compounds useful as kinase inhibitors |
| AU2013237226A1 (en) | 2012-03-19 | 2014-10-09 | Emory University | Quinazoline compounds and their use in therapy |
| JP6399660B2 (ja) | 2012-04-10 | 2018-10-03 | ザ・リージエンツ・オブ・ザ・ユニバーシテイー・オブ・カリフオルニア | 癌治療用組成物および方法 |
| JP6283661B2 (ja) | 2012-05-09 | 2018-02-21 | ストライク バイオ インク.Strike Bio,Inc. | 一塩基KRAS変異に特異的な二機能性低分子ヘアピン型RNA(BI−SHRNA,Bi−functionalShort−HairpinRNA) |
| JO3300B1 (ar) | 2012-06-06 | 2018-09-16 | Novartis Ag | مركبات وتركيبات لتعديل نشاط egfr |
| RU2019102203A (ru) | 2012-07-11 | 2019-03-05 | Блюпринт Медсинс Корпорейшн | Ингибиторы рецептора фактора роста фибробластов |
| US20150299188A1 (en) | 2012-08-24 | 2015-10-22 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| CN105407894A (zh) | 2013-03-14 | 2016-03-16 | 康威基内有限公司 | 用于抑制含布罗莫结构域的蛋白质的方法和组合物 |
| UY35464A (es) | 2013-03-15 | 2014-10-31 | Araxes Pharma Llc | Inhibidores covalentes de kras g12c. |
| WO2014143659A1 (en) * | 2013-03-15 | 2014-09-18 | Araxes Pharma Llc | Irreversible covalent inhibitors of the gtpase k-ras g12c |
| EP2970121B1 (en) * | 2013-03-15 | 2017-12-13 | Araxes Pharma LLC | Covalent inhibitors of kras g12c |
| EP3008465B1 (en) | 2013-06-13 | 2019-08-07 | Biodesy, Inc. | Method of screening candidate biochemical entities targeting a target biochemical entity |
| JP6397010B2 (ja) | 2013-07-03 | 2018-09-26 | カリオファーム セラピューティクス,インコーポレイテッド | 置換されたベンゾフラニル及びベンゾオキサゾリル化合物並びにその使用 |
| NZ715838A (en) | 2013-07-31 | 2020-05-29 | Merck Patent Gmbh | Pyridines, pyrimidines, and pyrazines, as btk inhibitors and uses thereof |
| 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 |
| TWI659021B (zh) | 2013-10-10 | 2019-05-11 | 亞瑞克西斯製藥公司 | Kras g12c之抑制劑 |
| CN106488910B (zh) * | 2013-10-10 | 2020-07-31 | 亚瑞克西斯制药公司 | Kras g12c的抑制剂 |
| US9376559B2 (en) | 2013-11-22 | 2016-06-28 | Exxonmobil Chemical Patents Inc. | Reverse staged impact copolymers |
| US9695165B2 (en) | 2014-01-15 | 2017-07-04 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| EA201691302A1 (ru) | 2014-02-03 | 2017-03-31 | Кадила Хелзкэр Лимитед | Новые гетероциклические соединения |
| CN114989140B (zh) | 2014-03-20 | 2025-03-25 | 卡佩拉医疗公司 | 苯并咪唑衍生物作为erbb酪氨酸激酶抑制剂用于治疗癌症 |
| RU2695815C9 (ru) | 2014-03-24 | 2019-10-28 | Гуандун Чжуншэн Фармасьютикал Ко., Лтд | Хинолиновые производные в качестве ингибиторов smo |
| EP3148981A4 (en) | 2014-05-30 | 2017-11-08 | The Trustees of Columbia University in the City of New York | Multivalent ras binding compounds |
| US10092555B2 (en) | 2014-06-27 | 2018-10-09 | Celgene Corporation | Compositions and methods for inducing conformational changes in cereblon and other E3 ubiquitin ligases |
| JO3556B1 (ar) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| US10011600B2 (en) | 2014-09-25 | 2018-07-03 | Araxes Pharma Llc | Methods and compositions for inhibition of Ras |
| AR102094A1 (es) | 2014-09-25 | 2017-02-01 | Araxes Pharma Llc | Inhibidores de proteínas kras con una mutación g12c |
| WO2016049565A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Compositions and methods for inhibition of ras |
| US9695200B2 (en) | 2015-01-23 | 2017-07-04 | Confluence Life Sciences, Inc. | Heterocyclic ITK inhibitors for treating inflammation and cancer |
| EA201792214A1 (ru) | 2015-04-10 | 2018-01-31 | Араксис Фарма Ллк | Соединения замещенного хиназолина |
| US10428064B2 (en) | 2015-04-15 | 2019-10-01 | 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 |
| CA2993013A1 (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 |
| WO2017058902A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| EP3356353A1 (en) | 2015-09-28 | 2018-08-08 | 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 |
| EP3356349A1 (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 |
| EP3356347A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| EP3356359B1 (en) | 2015-09-28 | 2021-10-20 | 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 |
| HUE068392T2 (hu) | 2015-10-21 | 2024-12-28 | Otsuka Pharma Co Ltd | Benzolaktám vegyületek mint fehérje kináz gátlók |
| KR20240113606A (ko) | 2015-11-16 | 2024-07-22 | 아락세스 파마 엘엘씨 | 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법 |
| US9988357B2 (en) | 2015-12-09 | 2018-06-05 | Araxes Pharma Llc | Methods for preparation of quinazoline derivatives |
| WO2017172979A1 (en) | 2016-03-30 | 2017-10-05 | 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 |
| CN110036010A (zh) | 2016-09-29 | 2019-07-19 | 亚瑞克西斯制药公司 | Kras g12c突变蛋白的抑制剂 |
| EP3523289A1 (en) | 2016-10-07 | 2019-08-14 | Araxes Pharma LLC | Heterocyclic compounds as inhibitors of ras and methods of use thereof |
| EP3630746A1 (en) | 2017-05-25 | 2020-04-08 | Araxes Pharma LLC | Compounds and methods of use thereof for treatment of cancer |
| EP3630745A2 (en) | 2017-05-25 | 2020-04-08 | Araxes Pharma LLC | Covalent inhibitors of kras |
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| CA2982360A1 (en) | 2016-10-20 |
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