CA3130083A1 - Bicyclic heterocyclyl compounds and uses thereof - Google Patents
Bicyclic heterocyclyl compounds and uses thereof Download PDFInfo
- Publication number
- CA3130083A1 CA3130083A1 CA3130083A CA3130083A CA3130083A1 CA 3130083 A1 CA3130083 A1 CA 3130083A1 CA 3130083 A CA3130083 A CA 3130083A CA 3130083 A CA3130083 A CA 3130083A CA 3130083 A1 CA3130083 A1 CA 3130083A1
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- CA
- Canada
- Prior art keywords
- membered
- alkyl
- compound
- pharmaceutically acceptable
- cycloalkyl
- 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.)
- Pending
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Classifications
-
- 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
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/94—Nitrogen atoms
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962812839P | 2019-03-01 | 2019-03-01 | |
| US62/812,839 | 2019-03-01 | ||
| US201962949785P | 2019-12-18 | 2019-12-18 | |
| US62/949,785 | 2019-12-18 | ||
| PCT/US2020/020609 WO2020180770A1 (en) | 2019-03-01 | 2020-03-02 | Bicyclic heterocyclyl compounds and uses thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3130083A1 true CA3130083A1 (en) | 2020-09-10 |
Family
ID=69941521
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3130083A Pending CA3130083A1 (en) | 2019-03-01 | 2020-03-02 | Bicyclic heterocyclyl compounds and uses thereof |
Country Status (11)
Families Citing this family (72)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2020159942A1 (en) | 2019-01-29 | 2020-08-06 | Tosk, Inc. | Pyrazolopyrimidine modulators of ras gtpase |
| WO2020214537A1 (en) | 2019-04-15 | 2020-10-22 | Tosk, Inc. | Modulators of ras gtpase |
| CN114615981B (zh) | 2019-08-29 | 2024-04-12 | 米拉蒂治疗股份有限公司 | Kras g12d抑制剂 |
| PH12022551102A1 (en) | 2019-11-08 | 2023-11-20 | Revolution Medicines Inc | Bicyclic heteroaryl compounds and uses thereof |
| MX2022006475A (es) | 2019-11-29 | 2022-09-07 | Lupin Ltd | Compuestos triciclicos sustituidos. |
| GEAP202416015A (en) | 2019-12-27 | 2024-04-10 | Lupin Ltd | Substituted tricyclic compounds |
| CN116034106B (zh) | 2020-06-02 | 2025-11-04 | 勃林格殷格翰国际有限公司 | 用于治疗癌症的环状2-氨基-3-氰基噻吩及衍生物 |
| CN113912608B (zh) * | 2020-07-10 | 2023-07-14 | 江苏恒瑞医药股份有限公司 | 嘧啶并嘧啶酮类衍生物、其制备方法及其在医药上的应用 |
| CN116194446B (zh) * | 2020-08-06 | 2026-07-24 | 北京泰德制药股份有限公司 | Sos1抑制剂、包含其的药物组合物及其用途 |
| CA3191279A1 (en) | 2020-08-28 | 2022-03-03 | Yi Liu | Heterocyclic compounds and uses thereof |
| EP4208261A1 (en) | 2020-09-03 | 2023-07-12 | Revolution Medicines, Inc. | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
| IL301298A (en) | 2020-09-15 | 2023-05-01 | Revolution Medicines Inc | Indole derivatives as RAS inhibitors in cancer therapy |
| US20240025863A1 (en) * | 2020-09-16 | 2024-01-25 | Biotheryx, Inc. | Sos1 protein degraders, pharmaceutical compositions thereof, and their therapeutic applications |
| US20230357239A1 (en) | 2020-09-18 | 2023-11-09 | Bayer Aktiengesellschaft | Pyrido[2,3-d]pyrimidin-4-amines as sos1 inhibitors |
| US12180220B2 (en) | 2020-10-14 | 2024-12-31 | Tosk, Inc. | Heteroaryl modulators of RAS GTPase |
| EP4262807A4 (en) * | 2020-12-15 | 2025-04-23 | Mirati Therapeutics, Inc. | Azachinazoline pan-KRAS inhibitors |
| AU2021409816A1 (en) | 2020-12-22 | 2023-07-06 | Qilu Regor Therapeutics Inc. | Sos1 inhibitors and uses thereof |
| US12643886B2 (en) | 2021-01-07 | 2026-06-02 | Ontario Institute for Cancer Research (OICR), The Governing Council of the University of Toronto, Sinai Health System | Isoindolinone aminopyrimidine compounds as inhibitors of NUAK kinases, compositions and uses thereof |
| CN114853812A (zh) * | 2021-02-04 | 2022-08-05 | 四川科伦博泰生物医药股份有限公司 | 含氧化膦基团的化合物、其制备方法及其在医药上的应用 |
| IL305046A (en) * | 2021-02-08 | 2023-10-01 | Wuhan Humanwell Innovative Drug Res And Development Center Limited Company | Pyridopyrimidinone derivative, the method of preparation thereof and its use |
| CN116669738B (zh) * | 2021-02-09 | 2026-04-03 | 苏州阿尔脉生物科技有限公司 | 一种作为sos1抑制剂的嘧啶并吡啶酮类衍生物、其制备方法及用途 |
| WO2022187266A1 (en) * | 2021-03-02 | 2022-09-09 | Viva Star Biosciences (Suzhou) Co., Ltd. | Novel substituted bicycli aza-heterocycles as sos1 inhibitors |
| EP4313151A1 (en) | 2021-03-31 | 2024-02-07 | Sevenless Therapeutics Limited | Sos1 inhibitors and ras inhibitors for use in the treatment of pain |
| GB202104609D0 (en) | 2021-03-31 | 2021-05-12 | Sevenless Therapeutics Ltd | New Treatments for Pain |
| JP2024514127A (ja) | 2021-04-09 | 2024-03-28 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 抗がん剤療法 |
| EP4074317A1 (en) | 2021-04-14 | 2022-10-19 | Bayer AG | Phosphorus derivatives as novel sos1 inhibitors |
| CN115232108B (zh) | 2021-04-23 | 2025-04-18 | 领泰生物医药(绍兴)有限公司 | Sos1降解剂及其制备方法和应用 |
| US20250134891A1 (en) * | 2021-05-12 | 2025-05-01 | Revolution Medicines, Inc. | Use of sos1 inhibitors with mtor inhibitors to treat cancers |
| JP2024522768A (ja) * | 2021-06-16 | 2024-06-21 | バイオセリックス, インコーポレイテッド | Sos1タンパク質分解剤、その医薬組成物及びそれらの治療的応用 |
| US20250059182A1 (en) * | 2021-06-21 | 2025-02-20 | Mirati Therapeutics, Inc. | Sos1 inhibitors |
| CN117580836A (zh) * | 2021-06-24 | 2024-02-20 | 四川汇宇制药股份有限公司 | 一种嘧啶并环结构衍生物及其用途 |
| WO2023287730A1 (en) * | 2021-07-13 | 2023-01-19 | Recurium Ip Holdings, Llc | Tricyclic compounds |
| CN116574104A (zh) * | 2021-09-07 | 2023-08-11 | 如东凌达生物医药科技有限公司 | 一类联芳基苄胺类化合物、制备方法和用途 |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| EP4441051A1 (en) | 2021-12-01 | 2024-10-09 | Boehringer Ingelheim International GmbH | Kras degrading compounds comprising annulated 2-amino-3-cyano thiophenes |
| EP4441050A1 (en) | 2021-12-01 | 2024-10-09 | Boehringer Ingelheim International GmbH | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| TW202337432A (zh) | 2021-12-01 | 2023-10-01 | 德商百靈佳殷格翰國際股份有限公司 | 用於治療癌症之環狀2-胺基-3-氰基噻吩及衍生物 |
| TW202340208A (zh) | 2021-12-01 | 2023-10-16 | 德商百靈佳殷格翰國際股份有限公司 | 用於治療癌症之環狀2-胺基-3-氰基噻吩及衍生物 |
| CR20240233A (es) | 2021-12-01 | 2024-07-17 | Univ Vanderbilt | Tiofenos 2-amino-3-ciano anulados y derivados para el tratamiento del cáncer |
| TW202340214A (zh) | 2021-12-17 | 2023-10-16 | 美商健臻公司 | 做為shp2抑制劑之吡唑并吡𠯤化合物 |
| WO2023125737A1 (en) * | 2021-12-29 | 2023-07-06 | Silexon Ai Technology Co., Ltd. | Heterocyclic compounds and use thereof |
| EP4463454A1 (en) | 2022-01-14 | 2024-11-20 | Jazz Pharmaceuticals Ireland Limited | Novel amine-substituted phthalazines and derivatives as sos1 inhibitors |
| EP4227307A1 (en) | 2022-02-11 | 2023-08-16 | Genzyme Corporation | Pyrazolopyrazine compounds as shp2 inhibitors |
| US12419962B2 (en) | 2022-03-16 | 2025-09-23 | Biotheryx, Inc. | Quinazolines, pharmaceutical compositions, and therapeutic applications |
| GB202203976D0 (en) | 2022-03-22 | 2022-05-04 | Jazz Pharmaceuticals Ireland Ltd | Tricyclic phthalazines and derivatives as sos1 inhibitors |
| US20260151410A1 (en) * | 2022-05-30 | 2026-06-04 | Scinnohub Pharmaceutical Co., Ltd | Tetrahydronaphthyridine Derivatives, Medicine Prepared Therefrom, and Applications Thereof in Preventing and Treating Adhesion-related Diseases |
| PE20251235A1 (es) * | 2022-06-10 | 2025-04-29 | Sapiensbio Inc | Compuesto novedoso y composicion farmaceutica que comprende la misma como ingrediente activo |
| EP4536364A1 (en) | 2022-06-10 | 2025-04-16 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| CN117263950A (zh) * | 2022-06-13 | 2023-12-22 | 上海优理惠生医药有限公司 | 一种哒嗪类化合物、其药物组合物及应用 |
| JP2025528836A (ja) | 2022-08-17 | 2025-09-02 | ツリーライン バイオサイエンシズ インコーポレイテッド | ピリドピリミジンKRas阻害剤 |
| WO2024056782A1 (en) | 2022-09-16 | 2024-03-21 | Bayer Aktiengesellschaft | Sulfone-substituted pyrido[3,4-d]pyrimidine derivatives for the treatment of cancer |
| CN120112538A (zh) | 2022-10-13 | 2025-06-06 | 拜耳公司 | Sos1抑制剂 |
| CN117946113A (zh) * | 2022-10-28 | 2024-04-30 | 纽欧申医药(上海)有限公司 | 一种含氮杂环化合物、其药学上可接受的盐及其制备方法与应用 |
| WO2024211712A1 (en) | 2023-04-07 | 2024-10-10 | Revolution Medicines, Inc. | Condensed macrocyclic compounds as ras inhibitors |
| CN121487951A (zh) | 2023-04-07 | 2026-02-06 | 锐新医药公司 | 大环ras抑制剂 |
| AU2024251341A1 (en) | 2023-04-14 | 2025-10-16 | Revolution Medicines, Inc. | Crystalline forms of a ras inhibitor |
| EP4695261A1 (en) | 2023-04-14 | 2026-02-18 | Revolution Medicines, Inc. | Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof |
| WO2024243441A1 (en) | 2023-05-24 | 2024-11-28 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| US20250019385A1 (en) | 2023-05-30 | 2025-01-16 | Boehringer Ingelheim International Gmbh | Spirocyclic annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| EP4735451A1 (en) | 2023-06-30 | 2026-05-06 | Kumquat Biosciences Inc. | Substituted condensed tricyclic amine compounds and uses thereof as ras inhibitors |
| TW202515575A (zh) | 2023-09-11 | 2025-04-16 | 美商金橘生物科技公司 | 細胞增殖調節劑及其用途 |
| WO2025064848A1 (en) | 2023-09-21 | 2025-03-27 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyridine kras inhibitors |
| WO2025090808A1 (en) | 2023-10-25 | 2025-05-01 | Kumquat Biosciences Inc. | Combinations of sos-1 inhibitors with osimertinib and/or met inhibitors to treat cancer |
| WO2025090810A1 (en) | 2023-10-25 | 2025-05-01 | Kumquat Biosciences Inc. | Use of sos1 inhibitors and amivantamab to treat cancer |
| CN117586267B (zh) * | 2023-11-23 | 2026-05-01 | 山东百启生物医药有限公司 | 一种4-溴吡唑[3,4-d]-嘧啶的制备方法 |
| WO2025171055A1 (en) | 2024-02-06 | 2025-08-14 | Kumquat Biosciences Inc. | Heterocyclic conjugates and uses thereof |
| WO2025230971A1 (en) | 2024-04-30 | 2025-11-06 | Kumquat Biosciences Inc. | Macrocyclic heterocycles as anticancer agents |
| WO2025245127A1 (en) | 2024-05-21 | 2025-11-27 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| US20260146049A1 (en) | 2024-11-27 | 2026-05-28 | Boehringer Ingelheim International Gmbh | Spirocyclic annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| US20260146050A1 (en) | 2024-11-27 | 2026-05-28 | Boehringer Ingelheim International Gmbh | Kras degrading compounds comprising spirocyclic annulated 2 amino-3-cyano thiophenes |
| WO2026114957A1 (en) | 2024-11-27 | 2026-06-04 | Boehringer Ingelheim International Gmbh | Spirocyclic annulated 2-amino-3-cyano thiophene derivatives as kras degraders for the treatment of cancer |
| WO2026114918A1 (en) | 2024-11-27 | 2026-06-04 | Boehringer Ingelheim International Gmbh | Spirocyclic annulated 2-amino-3-cyano thiophene derivatives as kras inhibitors for the treatment of cancer |
Family Cites Families (214)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2918591A1 (de) * | 1979-05-09 | 1980-11-20 | Hoechst Ag | Neue 4-substituierte 5,6,7,8-tetrahydrochinoline, ihre herstellung und verwendung |
| PH20344A (en) * | 1981-01-29 | 1986-12-04 | Sankyo Co | Aminopyrimidine derivatives, processes for their preparation, and fungicidal, insecticidal and acaricidal compositions containing them |
| GB8827305D0 (en) | 1988-11-23 | 1988-12-29 | British Bio Technology | Compounds |
| US5858358A (en) | 1992-04-07 | 1999-01-12 | The United States Of America As Represented By The Secretary Of The Navy | Methods for selectively stimulating proliferation of T cells |
| US6352694B1 (en) | 1994-06-03 | 2002-03-05 | Genetics Institute, Inc. | Methods for inducing a population of T cells to proliferate using agents which recognize TCR/CD3 and ligands which stimulate an accessory molecule on the surface of the T cells |
| US6905680B2 (en) | 1988-11-23 | 2005-06-14 | Genetics Institute, Inc. | Methods of treating HIV infected subjects |
| US6534055B1 (en) | 1988-11-23 | 2003-03-18 | Genetics Institute, Inc. | Methods for selectively stimulating proliferation of T cells |
| JP2762522B2 (ja) | 1989-03-06 | 1998-06-04 | 藤沢薬品工業株式会社 | 血管新生阻害剤 |
| US5112946A (en) | 1989-07-06 | 1992-05-12 | Repligen Corporation | Modified pf4 compositions and methods of use |
| PT98990A (pt) | 1990-09-19 | 1992-08-31 | American Home Prod | Processo para a preparacao de esteres de acidos carboxilicos de rapamicina |
| US5892112A (en) | 1990-11-21 | 1999-04-06 | Glycomed Incorporated | Process for preparing synthetic matrix metalloprotease inhibitors |
| US5120842A (en) | 1991-04-01 | 1992-06-09 | American Home Products Corporation | Silyl ethers of rapamycin |
| US5100883A (en) | 1991-04-08 | 1992-03-31 | American Home Products Corporation | Fluorinated esters of rapamycin |
| US5118678A (en) | 1991-04-17 | 1992-06-02 | American Home Products Corporation | Carbamates of rapamycin |
| DE69222637T2 (de) | 1991-05-10 | 1998-02-26 | Rhone Poulenc Rorer Int | Bis mono- und bicyclische aryl- und heteroarylderivate mit inhibierender wirkung auf die egf und/oder pdgf-rezeptor tyrosinkinase |
| US5118677A (en) | 1991-05-20 | 1992-06-02 | American Home Products Corporation | Amide esters of rapamycin |
| NZ243082A (en) | 1991-06-28 | 1995-02-24 | Ici Plc | 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof |
| US5151413A (en) | 1991-11-06 | 1992-09-29 | American Home Products Corporation | Rapamycin acetals as immunosuppressant and antifungal agents |
| GB9125660D0 (en) | 1991-12-03 | 1992-01-29 | Smithkline Beecham Plc | Novel compound |
| AU661533B2 (en) | 1992-01-20 | 1995-07-27 | Astrazeneca Ab | Quinazoline derivatives |
| US5521184A (en) | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| ZA935111B (en) | 1992-07-17 | 1994-02-04 | Smithkline Beecham Corp | Rapamycin derivatives |
| ZA935112B (en) | 1992-07-17 | 1994-02-08 | Smithkline Beecham Corp | Rapamycin derivatives |
| US5256790A (en) | 1992-08-13 | 1993-10-26 | American Home Products Corporation | 27-hydroxyrapamycin and derivatives thereof |
| GB9221220D0 (en) | 1992-10-09 | 1992-11-25 | Sandoz Ag | Organic componds |
| US5262564A (en) | 1992-10-30 | 1993-11-16 | Octamer, Inc. | Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents |
| US5258389A (en) | 1992-11-09 | 1993-11-02 | Merck & Co., Inc. | O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives |
| PT669929E (pt) | 1992-11-13 | 2007-04-30 | Immunex Corp | Ligando de elk, uma citoquina |
| US5455258A (en) | 1993-01-06 | 1995-10-03 | Ciba-Geigy Corporation | Arylsulfonamido-substituted hydroxamic acids |
| US5629327A (en) | 1993-03-01 | 1997-05-13 | Childrens Hospital Medical Center Corp. | Methods and compositions for inhibition of angiogenesis |
| US5516658A (en) | 1993-08-20 | 1996-05-14 | Immunex Corporation | DNA encoding cytokines that bind the cell surface receptor hek |
| AU693475B2 (en) | 1993-10-01 | 1998-07-02 | Novartis Ag | Pyrimidineamine derivatives and processes for the preparation thereof |
| US5656643A (en) | 1993-11-08 | 1997-08-12 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase |
| EP0729471A1 (en) | 1993-11-19 | 1996-09-04 | Abbott Laboratories | Semisynthetic analogs of rapamycin (macrolides) being immunomodulators |
| BR9408323A (pt) | 1993-12-17 | 1997-08-19 | Sandoz Ag | Derivados de rapamicina |
| US5700823A (en) | 1994-01-07 | 1997-12-23 | Sugen, Inc. | Treatment of platelet derived growth factor related disorders such as cancers |
| IL112249A (en) | 1994-01-25 | 2001-11-25 | Warner Lambert Co | Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds |
| IL112248A0 (en) | 1994-01-25 | 1995-03-30 | Warner Lambert Co | Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them |
| WO1995024190A2 (en) | 1994-03-07 | 1995-09-14 | Sugen, Inc. | Receptor tyrosine kinase inhibitors for inhibiting cell proliferative disorders and compositions thereof |
| EP0756627A1 (en) | 1994-04-15 | 1997-02-05 | Amgen Inc. | Hek5, hek7, hek8, hek11, new eph-like receptor protein tyrosine kinases |
| ES2109796T3 (es) | 1994-05-03 | 1998-01-16 | Ciba Geigy Ag | Derivados de pirrolopirimidilo con efecto antiproliferante. |
| US7175843B2 (en) | 1994-06-03 | 2007-02-13 | Genetics Institute, Llc | Methods for selectively stimulating proliferation of T cells |
| US6303769B1 (en) | 1994-07-08 | 2001-10-16 | Immunex Corporation | Lerk-5 dna |
| US5919905A (en) | 1994-10-05 | 1999-07-06 | Immunex Corporation | Cytokine designated LERK-6 |
| US6057124A (en) | 1995-01-27 | 2000-05-02 | Amgen Inc. | Nucleic acids encoding ligands for HEK4 receptors |
| US5863949A (en) | 1995-03-08 | 1999-01-26 | Pfizer Inc | Arylsulfonylamino hydroxamic acid derivatives |
| ATE446955T1 (de) | 1995-03-30 | 2009-11-15 | Pfizer Prod Inc | Chinazolinone derivate |
| JP4249804B2 (ja) | 1995-04-03 | 2009-04-08 | ノバルティス・アクチエンゲゼルシャフト | ピラゾール誘導体およびその製造法 |
| CA2218503C (en) | 1995-04-20 | 2001-07-24 | Pfizer Inc. | Arylsulfonyl hydroxamic acid derivatives |
| GB9508538D0 (en) | 1995-04-27 | 1995-06-14 | Zeneca Ltd | Quinazoline derivatives |
| US6692964B1 (en) | 1995-05-04 | 2004-02-17 | The United States Of America As Represented By The Secretary Of The Navy | Methods for transfecting T cells |
| US7067318B2 (en) | 1995-06-07 | 2006-06-27 | The Regents Of The University Of Michigan | Methods for transfecting T cells |
| US5747498A (en) | 1996-05-28 | 1998-05-05 | Pfizer Inc. | Alkynyl and azido-substituted 4-anilinoquinazolines |
| US5880141A (en) | 1995-06-07 | 1999-03-09 | Sugen, Inc. | Benzylidene-Z-indoline compounds for the treatment of disease |
| US5650415A (en) | 1995-06-07 | 1997-07-22 | Sugen, Inc. | Quinoline compounds |
| DE69624921T2 (de) | 1995-06-09 | 2003-09-11 | Novartis Ag, Basel | Rapamycinderivate |
| PL188959B1 (pl) | 1995-07-06 | 2005-05-31 | Novartis Ag | Pirolopirymidyny i sposoby ich wytwarzania |
| DE19534177A1 (de) | 1995-09-15 | 1997-03-20 | Merck Patent Gmbh | Cyclische Adhäsionsinhibitoren |
| AR004010A1 (es) | 1995-10-11 | 1998-09-30 | Glaxo Group Ltd | Compuestos heterociclicos |
| GB9523675D0 (en) | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
| DK0780386T3 (da) | 1995-12-20 | 2003-02-03 | Hoffmann La Roche | Matrixmetalloproteaseinhibitorer |
| US6140317A (en) | 1996-01-23 | 2000-10-31 | Novartis Ag | Pyrrolopyrimidines and processes for their preparation |
| JP3406763B2 (ja) | 1996-01-30 | 2003-05-12 | 東レ・ダウコーニング・シリコーン株式会社 | シリコーンゴム組成物 |
| GB9603095D0 (en) | 1996-02-14 | 1996-04-10 | Zeneca Ltd | Quinazoline derivatives |
| GB9603097D0 (en) | 1996-02-14 | 1996-04-10 | Zeneca Ltd | Quinazoline compounds |
| DE19608588A1 (de) | 1996-03-06 | 1997-09-11 | Thomae Gmbh Dr K | Pyrimido [5,4-d]pyrimidine, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| DE19629652A1 (de) | 1996-03-06 | 1998-01-29 | Thomae Gmbh Dr K | 4-Amino-pyrimidin-Derivate, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| DE59710417D1 (de) | 1996-03-15 | 2003-08-14 | Novartis Ag | N-7 HETEROCYCLYL-PYRROLO[ 2,3-d]PYRIMIDINE UND IHRE VERWENDUNG |
| CN100503580C (zh) | 1996-04-12 | 2009-06-24 | 沃尼尔·朗伯公司 | 酪氨酸激酶的不可逆抑制剂 |
| GB9607729D0 (en) | 1996-04-13 | 1996-06-19 | Zeneca Ltd | Quinazoline derivatives |
| BR9709959A (pt) | 1996-06-24 | 2000-05-09 | Pfizer | Derivados tricìclicos de fenilamino substituìdo para o tratamento de doenças hiperproliferativas |
| WO1998002441A2 (en) | 1996-07-12 | 1998-01-22 | Ariad Pharmaceuticals, Inc. | Non immunosuppressive antifungal rapalogs |
| 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 |
| US6391874B1 (en) | 1996-07-13 | 2002-05-21 | Smithkline Beecham Corporation | Fused heterocyclic compounds as protein tyrosine kinase inhibitors |
| HRP970371A2 (en) | 1996-07-13 | 1998-08-31 | Kathryn Jane Smith | Heterocyclic compounds |
| AR007855A1 (es) | 1996-07-13 | 1999-11-24 | Glaxo Group Ltd | Compuestos heterociclicos fusionados como inhibidores de proteina tirosina quinasa, sus metodos de preparacion, intermediarios, uso en medicinay composiciones farmaceuticas que los contienen |
| EP0923585B1 (en) | 1996-07-18 | 2002-05-08 | Pfizer Inc. | Phosphinate based inhibitors of matrix metalloproteases |
| US6111090A (en) | 1996-08-16 | 2000-08-29 | Schering Corporation | Mammalian cell surface antigens; related reagents |
| DK0920505T3 (da) | 1996-08-16 | 2008-09-08 | Schering Corp | Pattedyrcelleoverfladeantigener og tilhörende reagenser |
| PT938486E (pt) | 1996-08-23 | 2008-03-27 | Novartis Ag | Pirrolopirimidinas substituídas e processos para a sua preparação |
| EP0922030A1 (en) | 1996-08-23 | 1999-06-16 | Pfizer Inc. | Arylsulfonylamino hydroxamic acid derivatives |
| WO1998014449A1 (en) | 1996-10-02 | 1998-04-09 | Novartis Ag | Fused pyrazole derivatives and processes for their preparation |
| ID18494A (id) | 1996-10-02 | 1998-04-16 | Novartis Ag | Turunan pirazola leburan dan proses pembuatannya |
| CA2266519C (en) | 1996-10-02 | 2007-01-23 | Novartis Ag | Pyrimidine derivatives and processes for the preparation thereof |
| EP0837063A1 (en) | 1996-10-17 | 1998-04-22 | Pfizer Inc. | 4-Aminoquinazoline derivatives |
| GB9621757D0 (en) | 1996-10-18 | 1996-12-11 | Ciba Geigy Ag | Phenyl-substituted bicyclic heterocyclyl derivatives and their use |
| US6077864A (en) | 1997-01-06 | 2000-06-20 | Pfizer Inc. | Cyclic sulfone derivatives |
| HUP0000852A2 (hu) | 1997-02-03 | 2001-05-28 | Pfizer Products Inc. | Aril-szulfonil-amino-hidroxámsav-származékok, valamint e vegyületeket tartalmazó gyógyászati készítmények |
| ES2301194T3 (es) | 1997-02-05 | 2008-06-16 | Warner-Lambert Company Llc | Pirido 2,3-d pirimidinas y 4-aminopirimidinas como inhibidores de la proliferacion celular. |
| JP2000507975A (ja) | 1997-02-07 | 2000-06-27 | ファイザー・インク | N−ヒドロキシ−β−スルホニルプロピオンアミド誘導体類及びそれらのマトリックスメタロプロテイナーゼ阻害薬としての使用 |
| NZ336836A (en) | 1997-02-11 | 2001-02-23 | Pfizer | Arylsulfonyl hydroxamic acid derivatives suitable for a broad range of medicinal treatments |
| CO4950519A1 (es) | 1997-02-13 | 2000-09-01 | Novartis Ag | Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion |
| US6150395A (en) | 1997-05-30 | 2000-11-21 | The Regents Of The University Of California | Indole-3-carbinol (I3C) derivatives and methods |
| WO1999007701A1 (en) | 1997-08-05 | 1999-02-18 | Sugen, Inc. | Tricyclic quinoxaline derivatives as protein tyrosine kinase inhibitors |
| TR200000368T2 (tr) | 1997-08-08 | 2000-07-21 | Pfizer Products Inc. | Ariloksiariarilsülfonilamino hidroksamik asit türevleri. |
| CA2308114A1 (en) | 1997-10-21 | 1999-04-29 | Human Genome Sciences, Inc. | Human tumor necrosis factor receptor-like proteins tr11, tr11sv1, and tr11sv2 |
| GB9725782D0 (en) | 1997-12-05 | 1998-02-04 | Pfizer Ltd | Therapeutic agents |
| RS49779B (sr) | 1998-01-12 | 2008-06-05 | Glaxo Group Limited, | Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze |
| GB9800575D0 (en) | 1998-01-12 | 1998-03-11 | Glaxo Group Ltd | Heterocyclic compounds |
| JP2002502607A (ja) | 1998-02-09 | 2002-01-29 | ジェネンテク・インコーポレイテッド | 新規な腫瘍壊死因子レセプター相同体及びそれをコードする核酸 |
| DE69940808D1 (de) | 1998-03-04 | 2009-06-10 | Bristol Myers Squibb Co | Heterocyclen substituierte imidazopyrazine als protein- tyrosin-kinase-inhibitoren |
| 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 |
| KR100743287B1 (ko) | 1998-05-29 | 2007-07-26 | 수젠, 인크. | 피롤기로 치환된 2-인돌리논 단백질 인산화 효소 억제제 |
| UA60365C2 (uk) | 1998-06-04 | 2003-10-15 | Пфайзер Продактс Інк. | Похідні ізотіазолу, спосіб їх одержання, фармацевтична композиція та спосіб лікування гіперпроліферативного захворювання у ссавця |
| AU747427B2 (en) | 1998-07-10 | 2002-05-16 | Merck & Co., Inc. | Novel angiogenesis inhibitors |
| CA2341409A1 (en) | 1998-08-31 | 2000-03-09 | Merck And Co., Inc. | Novel angiogenesis inhibitors |
| EP1004578B1 (en) | 1998-11-05 | 2004-02-25 | Pfizer Products Inc. | 5-oxo-pyrrolidine-2-carboxylic acid hydroxamide derivatives |
| ATE329596T1 (de) | 1999-03-30 | 2006-07-15 | Novartis Pharma Gmbh | Phthalazinderivate zur behandlung von entzündlicher erkrankungen |
| GB9912961D0 (en) | 1999-06-03 | 1999-08-04 | Pfizer Ltd | Metalloprotease inhibitors |
| NZ516258A (en) | 1999-06-07 | 2004-02-27 | Immunex Corp | Tek antagonists |
| US6521424B2 (en) | 1999-06-07 | 2003-02-18 | Immunex Corporation | Recombinant expression of Tek antagonists |
| ATE376837T1 (de) | 1999-07-12 | 2007-11-15 | Genentech Inc | Stimulierung oder hemmung von angiogenese und herzvaskularisierung mit tumor nekrose faktor ligand/rezeptor homologen |
| IL147803A0 (en) | 1999-08-24 | 2002-08-14 | Ariad Gene Therapeutics Inc | 28-epirapalogs |
| PT1244647E (pt) | 1999-11-05 | 2006-10-31 | Astrazeneca Ab | Derivados de quinazolina como inibidores de vegf |
| JP5336686B2 (ja) | 1999-11-24 | 2013-11-06 | スージェン, インク. | 遊離酸または遊離塩基としてイオン化可能な医薬品のための処方 |
| US6515004B1 (en) | 1999-12-15 | 2003-02-04 | Bristol-Myers Squibb Company | N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases |
| US6727225B2 (en) | 1999-12-20 | 2004-04-27 | Immunex Corporation | TWEAK receptor |
| US6867041B2 (en) | 2000-02-24 | 2005-03-15 | Xcyte Therapies, Inc. | Simultaneous stimulation and concentration of cells |
| HK1052372A1 (zh) | 2000-02-24 | 2003-09-11 | Xcyte Therapies, Inc. | 细胞的同步刺激和富集 |
| US7572631B2 (en) | 2000-02-24 | 2009-08-11 | Invitrogen Corporation | Activation and expansion of T cells |
| US6797514B2 (en) | 2000-02-24 | 2004-09-28 | Xcyte Therapies, Inc. | Simultaneous stimulation and concentration of cells |
| US7074408B2 (en) | 2000-02-25 | 2006-07-11 | Immunex Corporation | Use of integrin antagonists to inhibit angiogenesis |
| US6630500B2 (en) | 2000-08-25 | 2003-10-07 | Cephalon, Inc. | Selected fused pyrrolocarbazoles |
| MXPA03005696A (es) | 2000-12-21 | 2003-10-06 | Glaxo Group Ltd | Pirimidinaminas como moduladores de angiogenesis. |
| CA2432578C (en) * | 2001-01-02 | 2008-04-01 | F. Hoffmann-La Roche Ag | Quinazolone derivatives as alpha 1a/b adrenergic receptor antagonists |
| US6995162B2 (en) | 2001-01-12 | 2006-02-07 | Amgen Inc. | Substituted alkylamine derivatives and methods of use |
| US6878714B2 (en) | 2001-01-12 | 2005-04-12 | Amgen Inc. | Substituted alkylamine derivatives and methods of use |
| US7105682B2 (en) | 2001-01-12 | 2006-09-12 | Amgen Inc. | Substituted amine derivatives and methods of use |
| US7102009B2 (en) | 2001-01-12 | 2006-09-05 | Amgen Inc. | Substituted amine derivatives and methods of use |
| US20020147198A1 (en) | 2001-01-12 | 2002-10-10 | Guoqing Chen | Substituted arylamine derivatives and methods of use |
| AU2003242252A1 (en) * | 2002-06-07 | 2003-12-22 | Kyowa Hakko Kogyo Co., Ltd. | Bicyclic pyrimidine derivatives |
| US7307088B2 (en) | 2002-07-09 | 2007-12-11 | Amgen Inc. | Substituted anthranilic amide derivatives and methods of use |
| TWI329112B (en) | 2002-07-19 | 2010-08-21 | Bristol Myers Squibb Co | Novel inhibitors of kinases |
| AU2004244626A1 (en) | 2003-05-23 | 2004-12-09 | The Government Of The United States Of America As Represented By The Secretary, Department Of Health And Human Services | GITR ligand and GITR ligand-related molecules and antibodies and uses thereof |
| CA2531454C (en) | 2003-07-08 | 2011-10-25 | Novartis Ag | Use of rapamycin and rapamycin derivatives for the treatment of bone loss |
| EP1660126A1 (en) | 2003-07-11 | 2006-05-31 | Schering Corporation | Agonists or antagonists of the clucocorticoid-induced tumour necrosis factor receptor (gitr) or its ligand for the treatment of immune disorders, infections and cancer |
| EP1648900A4 (en) | 2003-07-11 | 2010-02-10 | Ariad Pharma Inc | PHOSPHORUS MACROCYCLES |
| TW200523262A (en) | 2003-07-29 | 2005-07-16 | Smithkline Beecham Corp | Inhibitors of AKT activity |
| ATE542801T1 (de) | 2003-08-15 | 2012-02-15 | Novartis Ag | Zur behandlung von neoplastischen krankheiten, entzündlichen erkrankungen und erkrankungen des immunsystems geeignete 2,4-pyrimidindiamine |
| EP1692318A4 (en) | 2003-12-02 | 2008-04-02 | Genzyme Corp | COMPOSITIONS AND METHODS FOR DIAGNOSIS AND TREATMENT OF LUNG CANCER |
| WO2005094314A2 (en) | 2004-03-26 | 2005-10-13 | The Burnham Institute | Modulators of shp2 tyrosine phosphatase and their use in the treatment of body weight disorders |
| GB0409799D0 (en) | 2004-04-30 | 2004-06-09 | Isis Innovation | Method of generating improved immune response |
| EP1765402A2 (en) | 2004-06-04 | 2007-03-28 | Duke University | Methods and compositions for enhancement of immunity by in vivo depletion of immunosuppressive cell activity |
| JP4242911B2 (ja) | 2004-08-26 | 2009-03-25 | ファイザー・インク | プロテインキナーゼ阻害薬としてのエナンチオピュアなアミノヘテロアリール化合物 |
| TW200626610A (en) | 2004-10-13 | 2006-08-01 | Wyeth Corp | Analogs of 17-hydroxywortmannin as PI3K inhibitors |
| JP5238936B2 (ja) | 2005-03-25 | 2013-07-17 | ジーアイティーアール,インク. | Gitr結合分子およびその使用 |
| JP5198256B2 (ja) * | 2005-05-04 | 2013-05-15 | エボテク エージー | 縮合複素環式化合物、並びにそれらの組成物及び使用 |
| EP3530736A3 (en) | 2005-05-09 | 2019-11-06 | ONO Pharmaceutical Co., Ltd. | Human monoclonal antibodies to programmed death 1 (pd-1) and methods for treating cancer using anti-pd-1 antibodies alone or in combination with other immunotherapeutics |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| CN101267824A (zh) | 2005-09-20 | 2008-09-17 | 辉瑞产品公司 | 使用酪氨酸激酶抑制剂的治疗剂型和方法 |
| WO2007133822A1 (en) | 2006-01-19 | 2007-11-22 | Genzyme Corporation | Gitr antibodies for the treatment of cancer |
| PE20080145A1 (es) * | 2006-03-21 | 2008-02-11 | Janssen Pharmaceutica Nv | Tetrahidro-pirimidoazepinas como moduladores de trpv1 |
| US8987474B2 (en) | 2006-04-07 | 2015-03-24 | University Of South Florida | Inhibition of Shp2/PTPN11 protein tyrosine phosphatase by NSC-87877, NSC-117199 and their analogs |
| PE20081679A1 (es) | 2006-12-07 | 2008-12-18 | Hoffmann La Roche | Compuestos del inhibidor de fosfoinositida 3-cinasa y metodos de uso |
| WO2008123963A1 (en) * | 2007-04-02 | 2008-10-16 | Renovis, Inc. | Pyrid-2-yl fused heterocyclic compounds, and compositions and uses thereof |
| WO2008124815A1 (en) | 2007-04-10 | 2008-10-16 | University Of South Florida | Method of activating nk cells |
| US8076345B2 (en) * | 2007-04-17 | 2011-12-13 | Evotec Ag | 2-cyanophenyl-7,8-dihydro-5H-pyrido[4,3-d]pyrimidine compounds, compositions and uses thereof |
| PT2175884T (pt) | 2007-07-12 | 2016-09-21 | Gitr Inc | Terapias de combinação empregando moléculas de ligação a gitr |
| BRPI0816769A2 (pt) | 2007-09-12 | 2016-11-29 | Hoffmann La Roche | combinações de compostos inibidores de fosfoinositida 3-cinase e agentes quimioterapêuticos, e métodos de uso |
| WO2009049098A2 (en) | 2007-10-09 | 2009-04-16 | Indiana University Research & Technology Corporation | Materials and methods for regulating the activity of phosphatases |
| WO2009055730A1 (en) | 2007-10-25 | 2009-04-30 | Genentech, Inc. | Process for making thienopyrimidine compounds |
| WO2009135000A2 (en) | 2008-04-30 | 2009-11-05 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Inhibition of shp2/ptpn11 protein tyrosine phosphatase by nsc-117199 and analogs |
| JP2011526794A (ja) | 2008-07-02 | 2011-10-20 | エマージェント プロダクト デベロップメント シアトル, エルエルシー | TGF−βアンタゴニスト多重標的結合性分子 |
| WO2010011666A2 (en) | 2008-07-21 | 2010-01-28 | University Of South Florida | Indoline scaffold shp-2 inhibitors and cancer treatment method |
| JPWO2010030002A1 (ja) | 2008-09-12 | 2012-02-02 | 国立大学法人三重大学 | 外来性gitrリガンド発現細胞 |
| WO2010121212A2 (en) | 2009-04-17 | 2010-10-21 | H. Lee Moffit Cancer Center And Research Institute, Inc. | Indoline scaffold shp-2 inhibitors and method of treating cancer |
| NZ623069A (en) | 2009-08-17 | 2015-11-27 | Sloan Kettering Inst Cancer | Heat shock protein binding compounds, compositions, and methods for making and using same |
| IN2015DN02826A (cg-RX-API-DMAC10.html) | 2009-09-03 | 2015-09-11 | Merck Sharp & Dohme | |
| GB0919054D0 (en) | 2009-10-30 | 2009-12-16 | Isis Innovation | Treatment of obesity |
| US20130089554A1 (en) | 2009-12-29 | 2013-04-11 | Emergent Product Development Seattle, Llc | RON Binding Constructs and Methods of Use Thereof |
| JP2013530942A (ja) * | 2010-05-07 | 2013-08-01 | カリフォルニア・インスティチュート・オブ・テクノロジー | 移行型小胞体atpアーゼの阻害のための方法および組成物 |
| US8637684B2 (en) | 2010-05-12 | 2014-01-28 | Wisconsin Alumni Research Foundation | Tautomycetin and tautomycetin analog biosynthesis |
| WO2012041524A1 (en) | 2010-10-01 | 2012-04-05 | Max-Delbrück-Centrum Für Molekulare Medizin (Mdc) | Hydrazonopyrazolones as protein tyrosine phosphatase inhibitors |
| KR101606250B1 (ko) | 2011-03-23 | 2016-03-24 | 암젠 인크 | Cdk 4/6 및 flt3의 융합된 트리사이클릭 이중 저해제 |
| US20130108641A1 (en) | 2011-09-14 | 2013-05-02 | Sanofi | Anti-gitr antibodies |
| NZ705040A (en) * | 2012-07-20 | 2017-07-28 | Cleave Biosciences Inc | Fused pyrimidines as inhibitors of p97 complex |
| WO2014113584A1 (en) | 2013-01-16 | 2014-07-24 | Rhode Island Hospital | Compositions and methods for the prevention and treatment of osteolysis and osteoporosis |
| MX366978B (es) | 2013-03-15 | 2019-08-01 | Novartis Ag | Conjugados de anticuerpo - farmaco. |
| CA2944198C (en) | 2013-04-26 | 2021-11-16 | Indiana University Research & Technology Corporation | Hydroxyindole carboxylic acid based inhibitors for oncogenic src homology-2 domain containing protein tyrosine phosphatase-2 (shp2) |
| US9844535B2 (en) | 2013-07-03 | 2017-12-19 | Indiana University Research And Technology Corporation | SHP2 inhibitors and methods of treating autoimmune and/or glomerulonephritis-associated diseases using SHP2 inhibitors |
| EP2826586A1 (en) | 2013-07-18 | 2015-01-21 | Siemens Aktiengesellschaft | A method and a system for machining an object |
| ES2699351T3 (es) | 2014-01-17 | 2019-02-08 | Novartis Ag | Derivados de 1-piridazin/triazin-3-il-piper(-azina)/idina/pirolidina y composiciones de las mismas para inhibir la actividad de SHP2 |
| WO2015107494A1 (en) | 2014-01-17 | 2015-07-23 | Novartis Ag | 1 -(triazin-3-yi_/pyridazin-3-yl)-piper(-azine)idine derivatives and compositions thereof for inhibiting the activity of shp2 |
| WO2015171527A1 (en) * | 2014-05-05 | 2015-11-12 | Global Blood Therapeutics, Inc. | Pyrazolopyridine pyrazolopyrimidine and related compounds |
| WO2016077793A1 (en) | 2014-11-14 | 2016-05-19 | Children's Hospital Medical Center | Sos1 inhibitors for cancer treatment |
| CA3199430A1 (en) * | 2015-01-16 | 2016-07-21 | The General Hospital Corporation | Compounds for improving mrna splicing |
| CA2986732A1 (en) | 2015-05-22 | 2016-12-01 | Allosta Pharmaceuticals | Methods to prepare and employ binding site models for modulation of phosphatase activity and selectivity determination |
| WO2016196591A1 (en) | 2015-06-01 | 2016-12-08 | Indiana University Research & Technology Corporation | Protein tyrosine phosphatases or shp2 inhibitors and uses thereof |
| ES2824576T3 (es) | 2015-06-19 | 2021-05-12 | Novartis Ag | Compuestos y composiciones para inhibir la actividad de SHP2 |
| WO2016203406A1 (en) | 2015-06-19 | 2016-12-22 | Novartis Ag | Compounds and compositions for inhibiting the activity of shp2 |
| EP3310779B1 (en) | 2015-06-19 | 2019-05-08 | Novartis AG | Compounds and compositions for inhibiting the activity of shp2 |
| JP6689297B2 (ja) * | 2015-07-23 | 2020-04-28 | 武田薬品工業株式会社 | 複素環化合物 |
| WO2017078499A2 (ko) | 2015-11-06 | 2017-05-11 | 경북대학교 산학협력단 | 단백질 타이로신 탈인산화효소 억제제를 포함하는 신경염증성 질환의 예방 또는 치료용 조성물 |
| US11008372B2 (en) | 2015-11-07 | 2021-05-18 | Board Of Regents, The University Of Texas System | Targeting proteins for degradation |
| WO2017100279A1 (en) | 2015-12-09 | 2017-06-15 | West Virginia University | Chemical compound for inhibition of shp2 function and for use as an anti-cancer agent |
| WO2017156397A1 (en) | 2016-03-11 | 2017-09-14 | Board Of Regents, The University Of Texas Sysytem | Heterocyclic inhibitors of ptpn11 |
| WO2017210134A1 (en) | 2016-05-31 | 2017-12-07 | Board Of Regents, University Of Texas System | Heterocyclic inhibitors of ptpn11 |
| KR102218333B1 (ko) | 2016-06-07 | 2021-02-22 | 자코바이오 파마슈티칼스 컴퍼니 리미티드 | Shp2 억제제로서 유용한 신규한 헤테로환형 유도체 |
| IL311645B2 (en) | 2016-07-12 | 2025-11-01 | Revolution Medicines Inc | 2,5- disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines asallosteric shp2 inhibitors |
| EP3558979B1 (en) * | 2016-12-22 | 2021-02-17 | Boehringer Ingelheim International GmbH | Novel benzylamino substituted quinazolines and derivatives as sos1 inhibitors |
| WO2018129402A1 (en) | 2017-01-06 | 2018-07-12 | Oregon Health & Science University | Compositions and methods used in diagnosing and treating colorectal cancer |
| CN110730678B (zh) | 2017-01-10 | 2022-07-15 | 诺华股份有限公司 | 包含alk抑制剂和shp2抑制剂的药物组合 |
| CN110446709B (zh) | 2017-01-23 | 2023-09-12 | 锐新医药公司 | 作为变构shp2抑制剂的二环化合物 |
| CA3051054A1 (en) | 2017-01-23 | 2018-07-26 | Revolution Medicines, Inc. | Pyridine compounds as allosteric shp2 inhibitors |
| WO2018160731A1 (en) | 2017-02-28 | 2018-09-07 | Novartis Ag | Shp inhibitor compositions and uses for chimeric antigen receptor therapy |
| CA3056970A1 (en) * | 2017-03-21 | 2018-09-27 | Bayer Pharma Aktiengesellschaft | 2-methyl-quinazolines |
| SG11201908820VA (en) | 2017-03-23 | 2019-10-30 | Jacobio Pharmaceuticals Co Ltd | Novel heterocyclic derivatives useful as shp2 inhibitors |
| CA3061907A1 (en) | 2017-05-02 | 2018-11-08 | Revolution Medicines, Inc. | Rapamycin analogs as mtor inhibitors |
| TWI852912B (zh) | 2017-09-07 | 2024-08-21 | 美商銳新醫藥公司 | Shp2抑制劑組合物以及治療癌症的方法 |
| JP7447002B2 (ja) | 2017-09-11 | 2024-03-11 | クルーゾン・ファーマシューティカルズ・インコーポレイテッド | SHP2のオクタヒドロシクロペンタ[c]ピロールのアロステリック阻害剤 |
| US10683280B2 (en) * | 2018-01-26 | 2020-06-16 | Rapt Therapeutics, Inc. | Chemokine receptor modulators and uses thereof |
| PL3788049T3 (pl) | 2018-05-01 | 2023-06-19 | Revolution Medicines, Inc. | Połączone z C40, C28 i C32 analogi rapamycyny jako inhibitory mTOR |
| EP3788050B1 (en) | 2018-05-01 | 2024-08-28 | Revolution Medicines, Inc. | C26-linked rapamycin analogs as mtor inhibitors |
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2020
- 2020-03-02 US US17/310,932 patent/US20230096028A1/en not_active Abandoned
- 2020-03-02 AU AU2020232616A patent/AU2020232616A1/en not_active Abandoned
- 2020-03-02 CA CA3130083A patent/CA3130083A1/en active Pending
- 2020-03-02 SG SG11202109422WA patent/SG11202109422WA/en unknown
- 2020-03-02 CN CN202080031627.7A patent/CN113727758A/zh active Pending
- 2020-03-02 KR KR1020217027943A patent/KR20210146288A/ko not_active Ceased
- 2020-03-02 EP EP20713492.5A patent/EP3930845A1/en not_active Withdrawn
- 2020-03-02 WO PCT/US2020/020609 patent/WO2020180770A1/en not_active Ceased
- 2020-03-02 MX MX2021010323A patent/MX2021010323A/es unknown
- 2020-03-02 JP JP2021551777A patent/JP2022522778A/ja active Pending
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2021
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|---|---|
| US20230096028A1 (en) | 2023-03-30 |
| AU2020232616A1 (en) | 2021-09-09 |
| WO2020180770A1 (en) | 2020-09-10 |
| CN113727758A (zh) | 2021-11-30 |
| EP3930845A1 (en) | 2022-01-05 |
| JP2022522778A (ja) | 2022-04-20 |
| SG11202109422WA (en) | 2021-09-29 |
| MX2021010323A (es) | 2021-12-10 |
| IL285820A (en) | 2021-10-31 |
| KR20210146288A (ko) | 2021-12-03 |
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