JP2014528451A5 - - Google Patents
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- JP2014528451A5 JP2014528451A5 JP2014534732A JP2014534732A JP2014528451A5 JP 2014528451 A5 JP2014528451 A5 JP 2014528451A5 JP 2014534732 A JP2014534732 A JP 2014534732A JP 2014534732 A JP2014534732 A JP 2014534732A JP 2014528451 A5 JP2014528451 A5 JP 2014528451A5
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- Prior art keywords
- alkylene
- cancer
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- item
- disease
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 4
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims description 4
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- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 2
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- IDLFZVILOHSSID-OVLDLUHVSA-N corticotropin Chemical compound C([C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(O)=O)NC(=O)[C@@H](N)CO)C1=CC=C(O)C=C1 IDLFZVILOHSSID-OVLDLUHVSA-N 0.000 claims description 2
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- HYZJCKYKOHLVJF-UHFFFAOYSA-N c1nc(cccc2)c2[nH]1 Chemical compound c1nc(cccc2)c2[nH]1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 description 1
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161543176P | 2011-10-04 | 2011-10-04 | |
| US61/543,176 | 2011-10-04 | ||
| PCT/US2012/058800 WO2013052699A2 (en) | 2011-10-04 | 2012-10-04 | Novel quinoxaline inhibitors of pi3k |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014528451A JP2014528451A (ja) | 2014-10-27 |
| JP2014528451A5 true JP2014528451A5 (enExample) | 2015-11-26 |
Family
ID=48044399
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014534732A Pending JP2014528451A (ja) | 2011-10-04 | 2012-10-04 | Ｐｉ３ｋの新規キノキサリン阻害剤 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20140235643A1 (enExample) |
| EP (1) | EP2763994A4 (enExample) |
| JP (1) | JP2014528451A (enExample) |
| CN (1) | CN104024257A (enExample) |
| AU (1) | AU2012318580A1 (enExample) |
| CA (1) | CA2850763A1 (enExample) |
| HK (1) | HK1201065A1 (enExample) |
| WO (1) | WO2013052699A2 (enExample) |
Families Citing this family (118)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2458541T5 (en) | 2008-05-02 | 2025-08-04 | Seagen Inc | Methods and compositions for making antibodies and antibody derivatives with reduced core fucosylation |
| EP2448938B9 (en) | 2009-06-29 | 2015-06-10 | Incyte Corporation | Pyrimidinones as pi3k inhibitors |
| GB201007286D0 (en) | 2010-04-30 | 2010-06-16 | Astex Therapeutics Ltd | New compounds |
| GB201020179D0 (en) | 2010-11-29 | 2011-01-12 | Astex Therapeutics Ltd | New compounds |
| TW201249844A (en) | 2010-12-20 | 2012-12-16 | Incyte Corp | N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K inhibitors |
| KR102030609B1 (ko) | 2011-09-02 | 2019-10-11 | 인사이트 홀딩스 코포레이션 | Ｐｉ３ｋ 억제제로서 헤테로시클릴아민 |
| GB201118654D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118652D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118675D0 (en) | 2011-10-28 | 2011-12-14 | Astex Therapeutics Ltd | New compounds |
| GB201118656D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| US20150011569A1 (en) * | 2011-12-15 | 2015-01-08 | Philadelphia Health & Education Corporation D/B/A Drexel University College Of Medicine | NOVEL P13K p110 INHIBITORS AND METHODS OF USE THEREOF |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| GB201209609D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201209613D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| US9737521B2 (en) | 2012-11-08 | 2017-08-22 | Rhizen Pharmaceuticals Sa | Pharmaceutical compositions containing a PDE4 inhibitor and a PI3 delta or dual PI3 delta-gamma kinase inhibitor |
| GB201307577D0 (en) | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
| WO2015085075A1 (en) | 2013-12-06 | 2015-06-11 | Dana-Farber Cancer Institute, Inc. | Methods to distinguish waldenström's macroglobulinemia from igm monoclonal gammopathy of undetermined significance |
| JP6879740B2 (ja) | 2013-12-13 | 2021-06-02 | ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド | リンパ形質細胞性リンパ腫を処置する方法 |
| US9908872B2 (en) | 2013-12-13 | 2018-03-06 | Dana-Farber Cancer Institute, Inc. | Methods to treat lymphoplasmacytic lymphoma |
| US10167286B2 (en) | 2014-02-11 | 2019-01-01 | Mitokinin, Inc. | Compositions and methods using the same for treatment of neurodegenerative and mitochondrial disease |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| KR102479696B1 (ko) | 2014-03-26 | 2022-12-22 | 아스텍스 테라퓨틱스 리미티드 | Fgfr 억제제 및 igf1r 억제제의 조합물 |
| HUE053654T2 (hu) | 2014-03-26 | 2021-07-28 | Astex Therapeutics Ltd | FGFR- és CMET-inhibitorok kombinációi a rák kezelésére |
| CN104003982A (zh) * | 2014-05-05 | 2014-08-27 | 成都尔珏科技有限公司 | 一种可用于制备肺癌的化合物 |
| WO2015191677A1 (en) | 2014-06-11 | 2015-12-17 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors |
| PE20170640A1 (es) | 2014-07-04 | 2017-05-26 | Lupin Ltd | Derivados de quinolizinona como inhibidores de pi3k |
| CN105503877A (zh) | 2014-09-24 | 2016-04-20 | 和记黄埔医药（上海）有限公司 | 咪唑并哒嗪类化合物及其用途 |
| WO2016054491A1 (en) | 2014-10-03 | 2016-04-07 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| JP6788583B2 (ja) | 2014-10-22 | 2020-11-25 | ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド | 増殖性疾患を処置するためのチアゾリル含有化合物 |
| US9637488B2 (en) | 2015-01-29 | 2017-05-02 | Fuqiang Ruan | Heterocyclic compounds as inhibitors of class I PI3KS |
| TW201639573A (zh) | 2015-02-03 | 2016-11-16 | 吉李德科學股份有限公司 | 有關治療癌症之合併治療 |
| JOP20200201A1 (ar) | 2015-02-10 | 2017-06-16 | Astex Therapeutics Ltd | تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين |
| DK3831833T3 (da) | 2015-02-27 | 2022-11-14 | Incyte Holdings Corp | Fremgangsmåder til fremstillingen af en pi3k-inhibitor |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
| US9732097B2 (en) | 2015-05-11 | 2017-08-15 | Incyte Corporation | Process for the synthesis of a phosphoinositide 3-kinase inhibitor |
| WO2016183063A1 (en) | 2015-05-11 | 2016-11-17 | Incyte Corporation | Crystalline forms of a pi3k inhibitor |
| SG10201912699RA (en) | 2015-07-20 | 2020-02-27 | Genzyme Corp | Colony stimulating factor-1 receptor (csf-1r) inhibitors |
| CA2996857C (en) | 2015-09-23 | 2024-05-21 | Janssen Pharmaceutica Nv | Quinoxaline, quinoline and quinazolinone derivative compounds for the treatment of cancer |
| EP3353164B1 (en) | 2015-09-23 | 2021-11-03 | Janssen Pharmaceutica, N.V. | Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer |
| TW201725044A (zh) | 2015-10-01 | 2017-07-16 | 基利科學股份有限公司 | 用於治療癌症之btk抑制劑及查核點抑制劑之組合 |
| CU20180059A7 (es) | 2015-12-17 | 2018-10-04 | Gilead Sciences Inc | Compuestos inhibidores de la quinasa de unión a tank |
| CA3016081A1 (en) | 2016-03-04 | 2017-09-08 | Gilead Sciences, Inc. | Compositions and combinations of autotaxin inhibitors |
| CA3019003A1 (en) | 2016-04-08 | 2017-10-12 | Gilead Sciences, Inc. | Compositions and methods for treating cancer, inflammatory diseases and autoimmune diseases |
| WO2017214269A1 (en) | 2016-06-08 | 2017-12-14 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| JP6730466B2 (ja) | 2016-06-13 | 2020-07-29 | アイ−エムエービー バイオファーマ ユーエス リミテッド | 抗ｐｄ−ｌ１抗体およびその使用 |
| EP3493797A1 (en) | 2016-08-04 | 2019-06-12 | Gilead Sciences, Inc. | Cobicistat for use in cancer treatments |
| JOP20190052A1 (ar) * | 2016-09-22 | 2019-03-21 | Astrazeneca Ab | 5-[2-(بيريدين-2-يلامينو )-3،1 ثيازول-5-يال]-3،2 – ثنائي هيدرو- 1h- إيزوإندول 1--مشتق واحد واستخدامها كمثبطات مزدوجة للدلتا وغاما فوسفاتيديلينوسيتول 3-كيناز |
| WO2018085069A1 (en) | 2016-11-03 | 2018-05-11 | Gilead Sciences, Inc. | Combination of a bcl-2 inhibitor and a bromodomain inhibitor for treating cancer |
| US20180141939A1 (en) | 2016-11-22 | 2018-05-24 | Gilead Sciences, Inc. | Solid forms of a bet inhibitor |
| PL3383916T3 (pl) | 2017-01-24 | 2023-06-12 | I-Mab Biopharma Us Limited | Przeciwciała anty-cd73 i ich zastosowania |
| AR110998A1 (es) | 2017-02-24 | 2019-05-22 | Gilead Sciences Inc | Inhibidores de la tirosina cinasa de bruton |
| JP2020508326A (ja) | 2017-02-24 | 2020-03-19 | ギリアド サイエンシズ， インコーポレイテッド | ブルトン型チロシンキナーゼの阻害剤 |
| JOP20180040A1 (ar) | 2017-04-20 | 2019-01-30 | Gilead Sciences Inc | مثبطات pd-1/pd-l1 |
| KR20200019228A (ko) | 2017-06-21 | 2020-02-21 | 미토키닌, 인크. | 신경퇴행성 및 미토콘드리아 질환의 치료를 위한 조성물 및 이를 사용하는 방법 |
| CN111511754B (zh) | 2017-12-20 | 2023-09-12 | 捷克共和国有机化学与生物化学研究所 | 活化sting转接蛋白的具有膦酸酯键的2’3’环状二核苷酸 |
| EP3728283B1 (en) | 2017-12-20 | 2023-11-22 | Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. | 3'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein |
| WO2019160882A1 (en) | 2018-02-13 | 2019-08-22 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| TWI818007B (zh) | 2018-04-06 | 2023-10-11 | 捷克科學院有機化學與生物化學研究所 | 2'3'-環二核苷酸 |
| TWI833744B (zh) | 2018-04-06 | 2024-03-01 | 捷克科學院有機化學與生物化學研究所 | 3'3'-環二核苷酸 |
| TW202005654A (zh) | 2018-04-06 | 2020-02-01 | 捷克科學院有機化學與生物化學研究所 | ２，２，─環二核苷酸 |
| WO2019204609A1 (en) | 2018-04-19 | 2019-10-24 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| US20190359645A1 (en) | 2018-05-03 | 2019-11-28 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 2'3'-cyclic dinucleotides comprising carbocyclic nucleotide |
| JP2021523151A (ja) | 2018-05-11 | 2021-09-02 | ホスホレックス、インコーポレイテッド | 負の表面電荷を有するマイクロ粒子及びナノ粒子 |
| US10703733B2 (en) | 2018-05-14 | 2020-07-07 | Gilead Sciences, Inc. | MCL-1 inhibitors |
| CN119258070A (zh) | 2018-06-01 | 2025-01-07 | 因赛特公司 | 治疗pi3k相关病症的给药方案 |
| BR112020026746A2 (pt) | 2018-07-13 | 2021-03-30 | Gilead Sciences, Inc. | Composto, composição farmacêutica, métodos para inibir pd-1, pd-l1 e/ou a interação de pd-1/pd-l1 e para tratar câncer, e, kit para tratar ou prevenir câncer ou uma doença ou condição. |
| US11179397B2 (en) | 2018-10-03 | 2021-11-23 | Gilead Sciences, Inc. | Imidazopyrimidine derivatives |
| CN112955435B (zh) | 2018-10-24 | 2024-09-06 | 吉利德科学公司 | Pd-1/pd-l1抑制剂 |
| KR102658602B1 (ko) | 2018-10-31 | 2024-04-19 | 길리애드 사이언시즈, 인코포레이티드 | Hpk1 억제 활성을 갖는 치환된 6-아자벤즈이미다졸 화합물 |
| FI3873903T3 (fi) | 2018-10-31 | 2024-03-26 | Gilead Sciences Inc | Substituoituja 6-azabentsiimidatsoliyhdisteitä HPK1-inhibiittoreina |
| CA3129011C (en) | 2019-03-07 | 2023-12-19 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3'3'-cyclic dinucleotides and prodrugs thereof |
| EP3934757B1 (en) | 2019-03-07 | 2023-02-22 | Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. | 2'3'-cyclic dinucleotides and prodrugs thereof |
| EP3935065A1 (en) | 2019-03-07 | 2022-01-12 | Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. | 3'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator |
| TWI751517B (zh) | 2019-04-17 | 2022-01-01 | 美商基利科學股份有限公司 | 類鐸受體調節劑之固體形式 |
| TW202210480A (zh) | 2019-04-17 | 2022-03-16 | 美商基利科學股份有限公司 | 類鐸受體調節劑之固體形式 |
| TWI826690B (zh) | 2019-05-23 | 2023-12-21 | 美商基利科學股份有限公司 | 經取代之烯吲哚酮化物及其用途 |
| MX2021015452A (es) | 2019-06-25 | 2022-02-11 | Gilead Sciences Inc | Proteinas de fusion flt3l-fc y metodos de uso. |
| CA3145791A1 (en) | 2019-07-16 | 2021-01-21 | Gilead Sciences, Inc. | Hiv vaccines and methods of making and using |
| KR20220074917A (ko) | 2019-09-30 | 2022-06-03 | 길리애드 사이언시즈, 인코포레이티드 | Hbv 백신 및 hbv를 치료하는 방법 |
| MX2022004370A (es) | 2019-10-18 | 2022-05-06 | Forty Seven Inc | Terapias de combinacion para tratar sindromes mielodisplasicos y leucemia mieloide aguda. |
| WO2021087064A1 (en) | 2019-10-31 | 2021-05-06 | Forty Seven, Inc. | Anti-cd47 and anti-cd20 based treatment of blood cancer |
| TWI778443B (zh) | 2019-11-12 | 2022-09-21 | 美商基利科學股份有限公司 | Mcl1抑制劑 |
| JP7711068B2 (ja) | 2019-12-24 | 2025-07-22 | カルナバイオサイエンス株式会社 | ジアシルグリセロールキナーゼ調節化合物 |
| IL295023A (en) | 2020-02-14 | 2022-09-01 | Jounce Therapeutics Inc | Antibodies and fusion proteins that bind to ccr8 and their uses |
| CR20220547A (es) | 2020-05-01 | 2022-12-15 | Gilead Sciences Inc | Compuestos de 2,4-dioxopirimidina inhibidores de cd73 |
| CN114258393B (zh) * | 2020-07-21 | 2024-11-22 | 中国医药研究开发中心有限公司 | 具有磷脂酰肌醇3-激酶δ和γ的双重抑制剂活性的杂环化合物及其医药用途 |
| TW202302145A (zh) | 2021-04-14 | 2023-01-16 | 美商基利科學股份有限公司 | ＣＤ４７／ＳＩＲＰα結合及ＮＥＤＤ８活化酶Ｅ１調節次單元之共抑制以用於治療癌症 |
| TW202313094A (zh) | 2021-05-18 | 2023-04-01 | 美商基利科學股份有限公司 | 使用ＦＬＴ３Ｌ—Ｆｃ融合蛋白之方法 |
| AU2022299051B2 (en) | 2021-06-23 | 2025-03-13 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| AU2022298639C1 (en) | 2021-06-23 | 2025-07-17 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| KR20240005901A (ko) | 2021-06-23 | 2024-01-12 | 길리애드 사이언시즈, 인코포레이티드 | 디아실글리세롤 키나제 조절 화합물 |
| KR20240025616A (ko) | 2021-06-23 | 2024-02-27 | 길리애드 사이언시즈, 인코포레이티드 | 다이아실글리세롤 키나제 조절 화합물 |
| JP2024539252A (ja) | 2021-10-28 | 2024-10-28 | ギリアード サイエンシーズ， インコーポレイテッド | ピリジジン－３（２ｈ）－オン誘導体 |
| CA3235986A1 (en) | 2021-10-29 | 2023-05-04 | Gilead Science, Inc. | Cd73 compounds |
| WO2023107954A1 (en) | 2021-12-08 | 2023-06-15 | Dragonfly Therapeutics, Inc. | Antibodies targeting 5t4 and uses thereof |
| US20230203202A1 (en) | 2021-12-08 | 2023-06-29 | Dragonfly Therapeutics, Inc. | Proteins binding nkg2d, cd16 and 5t4 |
| EP4667056A1 (en) | 2021-12-22 | 2025-12-24 | Gilead Sciences, Inc. | Ikaros zinc finger family degraders and uses thereof |
| EP4452414A2 (en) | 2021-12-22 | 2024-10-30 | Gilead Sciences, Inc. | Ikaros zinc finger family degraders and uses thereof |
| TW202340168A (zh) | 2022-01-28 | 2023-10-16 | 美商基利科學股份有限公司 | Ｐａｒｐ７抑制劑 |
| LT4245756T (lt) | 2022-03-17 | 2024-11-25 | Gilead Sciences, Inc. | Ikaros cinko pirštų šeimos skaidymo medžiagos ir jų panaudojimas |
| AU2023240346A1 (en) | 2022-03-24 | 2024-09-19 | Gilead Sciences, Inc. | Combination therapy for treating trop-2 expressing cancers |
| TWI876305B (zh) | 2022-04-05 | 2025-03-11 | 美商基利科學股份有限公司 | 用於治療結腸直腸癌之組合療法 |
| US20230374036A1 (en) | 2022-04-21 | 2023-11-23 | Gilead Sciences, Inc. | Kras g12d modulating compounds |
| IL317958A (en) | 2022-07-01 | 2025-02-01 | Gilead Sciences Inc | CD73 compounds |
| JP2025523043A (ja) | 2022-07-12 | 2025-07-17 | ギリアード サイエンシーズ， インコーポレイテッド | Ｈｉｖ免疫原性ポリペプチド及びワクチン、並びにその使用 |
| WO2024064668A1 (en) | 2022-09-21 | 2024-03-28 | Gilead Sciences, Inc. | FOCAL IONIZING RADIATION AND CD47/SIRPα DISRUPTION ANTICANCER COMBINATION THERAPY |
| EP4638436A1 (en) | 2022-12-22 | 2025-10-29 | Gilead Sciences, Inc. | Prmt5 inhibitors and uses thereof |
| EP4695260A1 (en) | 2023-04-11 | 2026-02-18 | Gilead Sciences, Inc. | Kras modulating compounds |
| KR20250175331A (ko) | 2023-04-21 | 2025-12-16 | 길리애드 사이언시즈, 인코포레이티드 | Prmt5 억제제 및 이의 용도 |
| AU2024306338A1 (en) | 2023-06-30 | 2026-01-08 | Gilead Sciences, Inc. | Kras modulating compounds |
| AU2024300557A1 (en) | 2023-07-26 | 2026-02-05 | Gilead Sciences, Inc. | Parp7 inhibitors |
| AU2024297978A1 (en) | 2023-07-26 | 2026-02-05 | Gilead Sciences, Inc. | Parp7 inhibitors |
| WO2025054530A1 (en) | 2023-09-08 | 2025-03-13 | Gilead Sciences, Inc. | Pyrimidine-containing polycyclic derivatives as kras g12d modulating compounds |
| US20250101042A1 (en) | 2023-09-08 | 2025-03-27 | Gilead Sciences, Inc. | Kras g12d modulating compounds |
| US20250154172A1 (en) | 2023-11-03 | 2025-05-15 | Gilead Sciences, Inc. | Prmt5 inhibitors and uses thereof |
| WO2025137640A1 (en) | 2023-12-22 | 2025-06-26 | Gilead Sciences, Inc. | Azaspiro wrn inhibitors |
| WO2025245003A1 (en) | 2024-05-21 | 2025-11-27 | Gilead Sciences, Inc. | Prmt5 inhibitors and uses thereof |
| WO2026039365A1 (en) | 2024-08-12 | 2026-02-19 | Gilead Sciences, Inc. | Kras modulating compounds |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1247804A1 (en) * | 1993-11-12 | 2002-10-09 | PHARMACIA & UPJOHN COMPANY | Pyrimidine-thioalkyl and alkylether compounds |
| WO2000042026A1 (en) * | 1999-01-15 | 2000-07-20 | Novo Nordisk A/S | Non-peptide glp-1 agonists |
| US6927214B1 (en) * | 1999-01-15 | 2005-08-09 | Novo Nordisk A/S | Non-peptide GLP-1 agonists |
| US7705018B2 (en) * | 2007-03-23 | 2010-04-27 | Amgen Inc. | Substituted quinolines and their uses in treatment of inflammatory and related conditions |
| EP2132207A2 (en) * | 2007-03-23 | 2009-12-16 | Amgen Inc. | Heterocyclic compounds and their uses |
| AU2008231304B2 (en) * | 2007-03-23 | 2011-05-12 | Amgen Inc. | Heterocyclic compounds and their uses |
| NZ580009A (en) * | 2007-04-11 | 2012-06-29 | Exelixis Inc | Combination therapies comprising quinoxaline inhibitors of pi3k-alpha for use in the treatment of cancer |
| US8399483B2 (en) * | 2007-12-21 | 2013-03-19 | Ucb Pharma S.A. | Quinoxaline and quinoline derivatives as kinase inhibitors |
| WO2010036380A1 (en) * | 2008-09-26 | 2010-04-01 | Intellikine, Inc. | Heterocyclic kinase inhibitors |
| US8754113B2 (en) * | 2009-12-15 | 2014-06-17 | Shionogi & Co., Ltd. | Oxadiazole derivative having endothelial lipase inhibitory activity |
| TWI642670B (zh) * | 2010-09-14 | 2018-12-01 | 伊塞利克斯公司 | Ｐｉ３ｋ-德爾塔抑制劑以及其應用和生產方法 |
-
2012
- 2012-10-04 CN CN201280049200.5A patent/CN104024257A/zh active Pending
- 2012-10-04 EP EP12838127.4A patent/EP2763994A4/en not_active Withdrawn
- 2012-10-04 CA CA2850763A patent/CA2850763A1/en not_active Abandoned
- 2012-10-04 US US14/350,039 patent/US20140235643A1/en not_active Abandoned
- 2012-10-04 WO PCT/US2012/058800 patent/WO2013052699A2/en not_active Ceased
- 2012-10-04 JP JP2014534732A patent/JP2014528451A/ja active Pending
- 2012-10-04 AU AU2012318580A patent/AU2012318580A1/en not_active Abandoned
- 2012-10-04 HK HK15101538.0A patent/HK1201065A1/xx unknown