HRP20171689T1 - Inhibitori kinazolina aktivirajućih mutantnih oblika receptora epidermalnog faktora rasta - Google Patents
Inhibitori kinazolina aktivirajućih mutantnih oblika receptora epidermalnog faktora rasta Download PDFInfo
- Publication number
- HRP20171689T1 HRP20171689T1 HRP20171689TT HRP20171689T HRP20171689T1 HR P20171689 T1 HRP20171689 T1 HR P20171689T1 HR P20171689T T HRP20171689T T HR P20171689TT HR P20171689 T HRP20171689 T HR P20171689T HR P20171689 T1 HRP20171689 T1 HR P20171689T1
- Authority
- HR
- Croatia
- Prior art keywords
- formula
- pharmaceutically acceptable
- compounds
- acceptable salt
- chloro
- Prior art date
Links
- 230000003213 activating effect Effects 0.000 title claims 2
- 102000001301 EGF receptor Human genes 0.000 title 1
- 108060006698 EGF receptor Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical compound N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 14
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 4
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 4
- 230000001394 metastastic effect Effects 0.000 claims 3
- 206010061289 metastatic neoplasm Diseases 0.000 claims 3
- PDBXHPORMXSXKO-UHFFFAOYSA-N 8-benzyl-7-[2-[ethyl(2-hydroxyethyl)amino]ethyl]-1,3-dimethylpurine-2,6-dione;hydron;chloride Chemical class Cl.N=1C=2N(C)C(=O)N(C)C(=O)C=2N(CCN(CCO)CC)C=1CC1=CC=CC=C1 PDBXHPORMXSXKO-UHFFFAOYSA-N 0.000 claims 2
- 206010027476 Metastases Diseases 0.000 claims 2
- 241001465754 Metazoa Species 0.000 claims 2
- 238000005259 measurement Methods 0.000 claims 2
- 238000000634 powder X-ray diffraction Methods 0.000 claims 2
- XYDNMOZJKOGZLS-NSHDSACASA-N 3-[(1s)-1-imidazo[1,2-a]pyridin-6-ylethyl]-5-(1-methylpyrazol-4-yl)triazolo[4,5-b]pyrazine Chemical compound N1=C2N([C@H](C3=CN4C=CN=C4C=C3)C)N=NC2=NC=C1C=1C=NN(C)C=1 XYDNMOZJKOGZLS-NSHDSACASA-N 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 229940045513 CTLA4 antagonist Drugs 0.000 claims 1
- -1 Compounds 4-[(3-chloro-2-fluorophenyl)amino]-7-methoxyquinazolin-6-yl (2R)-2-methylpiperazine-1-carboxylate Chemical class 0.000 claims 1
- 206010059282 Metastases to central nervous system Diseases 0.000 claims 1
- 206010051696 Metastases to meninges Diseases 0.000 claims 1
- 102100022153 Tumor necrosis factor receptor superfamily member 4 Human genes 0.000 claims 1
- 101710165473 Tumor necrosis factor receptor superfamily member 4 Proteins 0.000 claims 1
- MXDSJQHFFDGFDK-CYBMUJFWSA-N [4-(3-chloro-2-fluoroanilino)-7-methoxyquinazolin-6-yl] (2r)-2,4-dimethylpiperazine-1-carboxylate Chemical compound C=12C=C(OC(=O)N3[C@@H](CN(C)CC3)C)C(OC)=CC2=NC=NC=1NC1=CC=CC(Cl)=C1F MXDSJQHFFDGFDK-CYBMUJFWSA-N 0.000 claims 1
- IFVBAZHARMVMRV-BTQNPOSSSA-N [4-(3-chloro-2-fluoroanilino)-7-methoxyquinazolin-6-yl] (2r)-2,4-dimethylpiperazine-1-carboxylate;hydrochloride Chemical compound Cl.C=12C=C(OC(=O)N3[C@@H](CN(C)CC3)C)C(OC)=CC2=NC=NC=1NC1=CC=CC(Cl)=C1F IFVBAZHARMVMRV-BTQNPOSSSA-N 0.000 claims 1
- 230000001270 agonistic effect Effects 0.000 claims 1
- 230000001093 anti-cancer Effects 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 1
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- CYOHGALHFOKKQC-UHFFFAOYSA-N selumetinib Chemical compound OCCONC(=O)C=1C=C2N(C)C=NC2=C(F)C=1NC1=CC=C(Br)C=C1Cl CYOHGALHFOKKQC-UHFFFAOYSA-N 0.000 claims 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
- A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
- A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- 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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Microbiology (AREA)
- Mycology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Claims (16)
1. Spojevi formule (I):
[image]
ili njegova farmaceutski prihvatljiva sol.
2. Spojevi formule (I) prema patentnom zahtjevu 1 koje je 4-[(3-kloro-2-fluorofenil)amino]-7-metoksikinazolin-6-il (2R)-2,4-dimetilpiperazin-1-karboksilat.
3. Farmaceutski prihvatljiva sol spoja formule (I) prema patentnom zahtjevu 1 koja je 4-[(3-kloro-2-fluorofenil)amino]-7-metoksikinazolin-6-il (2R)-2,4-dimetilpiperazin-1-karboksilat hidroklorid.
4. Spojevi formule (I), ili njegova farmaceutski prihvatljiva sol, prema bilo kojem od patentnih zahtjeva 1-3 u kristalnom obliku.
5. Mono-HCl sol spoja formule (I), prema patentnom zahtjevu 3, u kristalnom obliku koji ima obrazac rentgenske difrakcije praha sa najmanje dva specifična pika na 2-teta = 12.3° i 13.9° sa greškom mjerenja za svaki difrakcijski kut koji je plus ili minus 0.2°.
6. Mono-HCl so spoja formule (I), prema patentnom zahtjevu 3, u kristalnom obliku koji ima obrazac rentgenske difrakcije praha sa specifičnim pikovima na 2-teta = 12.3, 13.9, 9.3, 23.3, 18.7, 16.0, 24.6, 26.8, 28.0° sa greškom mjerenja za svaki difrakcijski kut koji je plus ili minus 0.2°.
7. Farmaceutska kompozicija koja sadrži spojeve formule (I), ili njegovu farmaceutski prihvatljivu sol, prema bilo kojem od patentnih zahtjeva 1-6, zajedno s farmaceutski prihvatljivim razblaživačem ili nosačem.
8. Spojevi formule (I), ili njegova farmaceutski prihvatljiva sol, prema bilo kojem od patentnih zahtjeva 1-6, za upotrebu kao lijek.
9. Spojevi formule (I), ili njegova farmaceutski prihvatljiva sol, prema bilo kojem od patentnih zahtjeva 1-6, za upotrebu u inhibiciji aktivirajućeg mutantnog EGFR kod toplokrvne životinje kao što je čovjek.
10. Spojevi formule (I), ili njegova farmaceutski prihvatljiva sol, prema bilo kojem od patentnih zahtjeva 1-6, za upotrebu u proizvodnji anti-kancerskog efekta kod toplokrvne životinje, kao što je čovjek.
11. Spojevi formule (I), ili njegova farmaceutski prihvatljiva sol, prema bilo kojem od patentnih zahtjeva 1-6, za upotrebu u liječenju nesitnostaničnog raka pluća.
12. Spojevi formule (I), ili njegova farmaceutski prihvatljiva sol, prema bilo kojem od patentnih zahtjeva 1-6, za upotrebu u liječenju metastatskog nesitnostaničnog raka pluća.
13. Spojevi formule (I), ili njegova farmaceutski prihvatljiva sol, za upotrebu u liječenju metastatskog nesitnostaničnog raka pluća prema patentnom zahtjevu 12, naznačeno time što, metastaze su metastaze na mozgu.
14. Spojevi formula (I), ili njegova farmaceutski prihvatljiva sol, za upotrebu u liječenju metastatskog nesitnostaničnog raka pluća prema patentnom zahtjevu 12, naznačeno time što, metastaze su leptomeningealne metastaze.
15. Spojevi formula (I), ili njegova farmaceutski prihvatljiva sol, prema bilo kojem od patentnih zahtjeva 1-6, u kombinaciji s anti-tumorskim sredstvom izabranim od:
(i) anti-CTLA-4 antitijela;
(ii) (2-hidroksietoksi)-amida 6-(4-bromo-2-kloro-fenilamino)-7-fluoro-3-metil-3H-benzoimidazol-5-karboksilne kiseline ili njegove farmaceutski prihvatljive soli;
(iii) anti-PD-L1 antitijela;
(iv) 1-[(1S)-1-(imidazo[1,2-a]pyridin-6-il)etil]-6-(1-metil-1H-pirazol-4-il)-1H-[1,2,3]triazolo[4,5-b]pirazina ili njegove farmaceutski prihvatljive soli;
(v) anti-PD-1 antitijela; ili
(vi) OX40 agonističkog antitijela.
16. Spojevi 4-[(3-kloro-2-fluorofenil)amino]-7-metoksikinazolin-6-il (2R)-2-metilpiperazin-1-karboksilat:
[image]
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN2013072250 | 2013-03-06 | ||
PCT/GB2014/050655 WO2014135876A1 (en) | 2013-03-06 | 2014-03-05 | Quinazoline inhibitors of activating mutant forms of epidermal growth factor receptor |
EP14710620.7A EP2964638B1 (en) | 2013-03-06 | 2014-03-05 | Quinazoline inhibitors of activating mutant forms of epidermal growth factor receptor |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20171689T1 true HRP20171689T1 (hr) | 2018-02-23 |
Family
ID=50288181
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20171689TT HRP20171689T1 (hr) | 2013-03-06 | 2017-11-06 | Inhibitori kinazolina aktivirajućih mutantnih oblika receptora epidermalnog faktora rasta |
Country Status (42)
Families Citing this family (36)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2901269C (en) * | 2013-03-06 | 2022-01-18 | Astrazeneca Ab | Quinazoline inhibitors of activating mutant forms of epidermal growth factor receptor |
EP3035936B1 (en) | 2013-08-23 | 2019-03-13 | NeuPharma, Inc. | Certain chemical entities, compositions, and methods |
US10011591B2 (en) | 2014-10-01 | 2018-07-03 | Sun Pharmaceutical Industries Limited | Crystalline form of afatinib dimaleate |
US10947201B2 (en) | 2015-02-17 | 2021-03-16 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
CN105859641B (zh) | 2015-05-05 | 2018-11-16 | 杭州华东医药集团新药研究院有限公司 | 喹唑啉巴豆基化合物二马来酸盐的晶体及其制备方法和用途 |
CN105503906B (zh) * | 2015-12-09 | 2018-09-11 | 上海宣创生物科技有限公司 | 一种三唑并吡嗪衍生物a晶型及其制备方法 |
CN105503905B (zh) * | 2015-12-09 | 2018-09-11 | 上海宣创生物科技有限公司 | 一种三唑并吡嗪衍生物b晶型及其制备方法 |
AU2017312561B2 (en) | 2016-08-15 | 2022-06-30 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
CN108658946B (zh) * | 2017-03-28 | 2020-06-16 | 焦玉奇 | 新颖的喹唑啉抑制剂 |
CN107400094B (zh) * | 2017-09-08 | 2020-04-03 | 贾玉庆 | 喹唑啉基羧酸酯类化合物及其用途 |
CN109721551B (zh) * | 2017-10-30 | 2022-09-20 | 上海北卡医药技术有限公司 | 一种3,4-二氢-7-甲氧基-4-氧代喹唑啉-6-醇乙酸酯的制备方法 |
CN109721552B (zh) * | 2017-10-30 | 2022-09-20 | 上海北卡医药技术有限公司 | 一种吉非替尼的制备方法 |
EP3749310A4 (en) * | 2018-02-08 | 2021-08-18 | Neupharma, Inc. | CERTAIN CHEMICAL SUBSTANCES, COMPOSITIONS AND PROCEDURES |
CN109438423A (zh) * | 2018-09-12 | 2019-03-08 | 通化师范学院 | 一种肺癌靶向化合物azd-3759的合成工艺的新方法 |
KR20210061371A (ko) * | 2018-09-14 | 2021-05-27 | 스펙트럼 파마슈티컬즈 인크 | 암 치료용 키트 및 방법 |
CN110903283B (zh) * | 2018-09-17 | 2021-01-01 | 南京雷正医药科技有限公司 | 一种取代的喹唑啉类化合物、包含该化合物的药物组合物和该化合物的用途 |
WO2020057403A1 (zh) * | 2018-09-18 | 2020-03-26 | 北京越之康泰生物医药科技有限公司 | 吲哚衍生物及其在医药上的应用 |
AU2020250832A1 (en) | 2019-03-29 | 2021-11-11 | Astrazeneca Ab | Osimertinib for use in the treatment of non-small cell lung cancer |
CN111747950B (zh) * | 2019-03-29 | 2024-01-23 | 深圳福沃药业有限公司 | 用于治疗癌症的嘧啶衍生物 |
CN110590683B (zh) * | 2019-10-11 | 2022-08-19 | 山东四环药业股份有限公司 | 一种靶向药物azd3759中间体的制备方法 |
US20210161897A1 (en) | 2019-11-12 | 2021-06-03 | Astrazeneca Ab | Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer |
CN114980883A (zh) | 2020-01-20 | 2022-08-30 | 阿斯利康(瑞典)有限公司 | 用于治疗癌症的表皮生长因子受体酪氨酸激酶抑制剂 |
US20210369709A1 (en) | 2020-05-27 | 2021-12-02 | Astrazeneca Ab | EGFR TKIs FOR USE IN THE TREATMENT OF NON-SMALL CELL LUNG CANCER |
CN111662273A (zh) * | 2020-06-22 | 2020-09-15 | 通化师范学院 | 一种酪氨酸激酶抑制剂azd3759的制备方法 |
CN111675700A (zh) * | 2020-06-22 | 2020-09-18 | 通化师范学院 | 一种抗癌新药azd3759的制备方法 |
CN111848584A (zh) * | 2020-07-10 | 2020-10-30 | 江南大学 | 一种多取代喹唑啉类化合物及其应用 |
CN113943273A (zh) * | 2020-07-17 | 2022-01-18 | 上海天慈国际药业有限公司 | 一种肺癌药物azd3759的制备方法 |
CN113135901A (zh) * | 2021-04-12 | 2021-07-20 | 南京雷正医药科技有限公司 | 氘代的喹唑啉类盐酸盐化合物的晶型及其制备和应用 |
WO2023187037A1 (en) | 2022-03-31 | 2023-10-05 | Astrazeneca Ab | Epidermal growth factor receptor (egfr) tyrosine kinase inhibitors in combination with an akt inhibitor for the treatment of cancer |
WO2023209088A1 (en) | 2022-04-28 | 2023-11-02 | Astrazeneca Ab | Bicyclic heteroaromatic compounds and their use in the treatment of cancer |
WO2023209090A1 (en) | 2022-04-28 | 2023-11-02 | Astrazeneca Ab | Bicyclic heteroaromatic compounds and their application in the treatment of cancer |
WO2023209084A1 (en) | 2022-04-28 | 2023-11-02 | Astrazeneca Ab | Condensed bicyclic heteroaromatic compounds and their use in the treatment of cancer |
US20240116926A1 (en) | 2022-04-28 | 2024-04-11 | Astrazeneca Ab | Heteroaromatic compounds |
WO2024002938A1 (en) | 2022-06-27 | 2024-01-04 | Astrazeneca Ab | Combinations involving epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer |
CN115813927A (zh) * | 2022-07-06 | 2023-03-21 | 江苏晨泰医药科技有限公司 | 受体酪氨酸激酶抑制剂与联苯环辛二稀木脂素的联合用药及其用途 |
WO2024008929A1 (en) | 2022-07-08 | 2024-01-11 | Astrazeneca Ab | Epidermal growth factor receptor tyrosine kinase inhibitors in combination with hgf-receptor inhibitors for the treatment of cancer |
Family Cites Families (43)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU661533B2 (en) | 1992-01-20 | 1995-07-27 | Astrazeneca Ab | Quinazoline derivatives |
US5821332A (en) | 1993-11-03 | 1998-10-13 | The Board Of Trustees Of The Leland Stanford Junior University | Receptor on the surface of activated CD4+ T-cells: ACT-4 |
US6242566B1 (en) | 1994-02-10 | 2001-06-05 | Board Of Trustees Of The Leland Stanford Junior University | Ligand (ACT-4-L) to a receptor on the surface of activated CD4+ T-cells |
GB9508538D0 (en) | 1995-04-27 | 1995-06-14 | Zeneca Ltd | Quinazoline derivatives |
GB9603095D0 (en) | 1996-02-14 | 1996-04-10 | Zeneca Ltd | Quinazoline derivatives |
GB9607729D0 (en) | 1996-04-13 | 1996-06-19 | Zeneca Ltd | Quinazoline derivatives |
DE69939526D1 (de) | 1998-02-24 | 2008-10-23 | Sisters Of Providence In Orego | Zusammensetzungen, die entweder ein ox-40-rezeptor-bindemittel oder eine für ein solches bindemittel kodierende nukleicsäuresequenz enthalten, und verfahren zur verbesserung der antigenspezifischen immunantwort |
US6682736B1 (en) | 1998-12-23 | 2004-01-27 | Abgenix, Inc. | Human monoclonal antibodies to CTLA-4 |
DE19911509A1 (de) | 1999-03-15 | 2000-09-21 | Boehringer Ingelheim Pharma | Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
SK3832002A3 (en) | 1999-09-21 | 2002-11-06 | Astrazeneca Ab | Quinazoline compounds and pharmaceutical compositions containing them |
US6656946B2 (en) | 2000-08-26 | 2003-12-02 | Boehringer Ingelheim Pharma Kg | Aminoquinazolines which inhibit signal transduction mediated by tyrosine kinases |
DE10042058A1 (de) | 2000-08-26 | 2002-03-07 | Boehringer Ingelheim Pharma | Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
TWI324597B (en) | 2002-03-28 | 2010-05-11 | Astrazeneca Ab | Quinazoline derivatives |
AU2003226705B2 (en) * | 2002-03-30 | 2008-11-06 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 4-(N-phenylamino)-quinazolines / quinolines as tyrosine kinase inhibitors |
DE60317677T2 (de) | 2002-06-13 | 2008-10-30 | Crucell Holland B.V. | Ox40 (=cd134) rezeptor agonisten und therapeutische verwendung |
AU2003288675B2 (en) | 2002-12-23 | 2010-07-22 | Medimmune Limited | Antibodies against PD-1 and uses therefor |
MXPA06001079A (es) | 2003-07-29 | 2006-04-11 | Astrazeneca Ab | Derivados de piperidil quinazolina como inhibidores de cinasa de tirosina. |
MXPA06003161A (es) | 2003-09-16 | 2006-06-05 | Astrazeneca Ab | Derivados de quinazolina. |
ATE352550T1 (de) | 2003-09-19 | 2007-02-15 | Astrazeneca Ab | Chinazolinderivate |
EP1670782B1 (en) | 2003-09-19 | 2007-02-14 | AstraZeneca AB | Quinazoline derivatives |
WO2005097137A2 (en) | 2004-03-31 | 2005-10-20 | The Scripps Research Institute | Advanced quinazoline based protein kinase inhibitors |
DK2447375T3 (da) | 2004-03-31 | 2019-07-29 | Massachusetts Gen Hospital | Fremgangsmåde til bestemmelse af responsiviteten af en tumor på behandlinger med den epidermale vækstfaktor-receptor som mål |
PT2161336E (pt) | 2005-05-09 | 2013-10-03 | Ono Pharmaceutical Co | Anticorpos monoclonais humanos para morte programada 1 (pd-1) e métodos de tratamento do cancro utilizando anticorpos anti- pd-1 sozinhos ou em combinação com outros agentes imunoterapêuticos¿ |
CN101175732B (zh) | 2005-05-12 | 2010-06-16 | 黄文林 | 一种喹唑啉衍生物的制备方法及用作制备治疗肿瘤疾病药物的应用 |
CN101175734B (zh) | 2005-05-12 | 2011-10-12 | 黄文林 | 一种作为抗肿瘤药物的喹唑啉衍生物及其制备方法 |
KR101607288B1 (ko) | 2005-07-01 | 2016-04-05 | 이. 알. 스퀴부 앤드 선즈, 엘.엘.씨. | 예정 사멸 리간드 1 (피디-엘1)에 대한 인간 모노클로날 항체 |
WO2007023073A2 (de) | 2005-08-22 | 2007-03-01 | Boehringer Ingelheim International Gmbh | Bicyclische heterocyclen, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung |
US8648087B2 (en) * | 2005-11-15 | 2014-02-11 | Array Biopharma, Inc. | N4-phenyl-quinazoline-4-amine derivatives and related compounds as ErbB type I receptor tyrosine kinase inhibitors for the treatment of hyperproliferative diseases |
TWI405756B (zh) | 2005-12-21 | 2013-08-21 | Array Biopharma Inc | 新穎硫酸氫鹽 |
BRPI0602275A (pt) | 2006-03-24 | 2007-11-27 | Astrazeneca Ab | derivado de quinazolina, composição farmacêutica, uso de um derivado de quinazolina, métodos para produzir um efeito anti-proliferativo em um animal de sangue quente e para tratar um cáncer em um animal de sangue quente e processo para a preparação de um derivado de quinalizona |
EP2242773B1 (en) | 2008-02-11 | 2017-06-14 | Cure Tech Ltd. | Monoclonal antibodies for tumor treatment |
US8168757B2 (en) | 2008-03-12 | 2012-05-01 | Merck Sharp & Dohme Corp. | PD-1 binding proteins |
CN101367793B (zh) | 2008-09-26 | 2013-09-11 | 中国科学院广州生物医药与健康研究院 | 一种具有抗肿瘤活性的氨基喹唑啉衍生物及其盐类 |
WO2010061208A2 (en) | 2008-11-03 | 2010-06-03 | Astrazeneca Ab | Therapeutic treatment 555 |
EP3929216A1 (en) | 2008-12-09 | 2021-12-29 | F. Hoffmann-La Roche AG | Anti-pd-l1 antibodies and their use to enhance t-cell function |
US9050341B2 (en) | 2009-07-14 | 2015-06-09 | Natco Pharma Limited | Methods of treating drug resistant and other tumors by administering 6,7-dialkoxy quinazoline derivatives |
NO2504364T3 (hr) | 2009-11-24 | 2018-01-06 | ||
PT2719699E (pt) | 2009-12-31 | 2015-09-30 | Hutchison Medipharma Ltd | Certas triazolopirazinas, suas composições e seus métodos de utilização |
CN101857618B (zh) | 2010-06-13 | 2015-11-25 | 中国海洋大学 | 作为蛋白酪氨酸激酶抑制剂的一系列喹唑啉糖衍生物,其制备方法和应用 |
SG187945A1 (en) | 2010-08-23 | 2013-03-28 | Univ Texas | Anti-ox40 antibodies and methods of using the same |
JP6072771B2 (ja) | 2011-04-20 | 2017-02-01 | メディミューン,エルエルシー | B7−h1およびpd−1に結合する抗体およびその他の分子 |
CN104736168B (zh) | 2012-05-31 | 2018-09-21 | 索伦托治疗有限公司 | 与pd-l1结合的抗原结合蛋白 |
CA2901269C (en) * | 2013-03-06 | 2022-01-18 | Astrazeneca Ab | Quinazoline inhibitors of activating mutant forms of epidermal growth factor receptor |
-
2014
- 2014-03-05 CA CA2901269A patent/CA2901269C/en active Active
- 2014-03-05 NO NO14710620A patent/NO2964638T3/no unknown
- 2014-03-05 MY MYPI2015702970A patent/MY186126A/en unknown
- 2014-03-05 CN CN201480012092.3A patent/CN105209456B/zh active Active
- 2014-03-05 SI SI201430449T patent/SI2964638T1/sl unknown
- 2014-03-05 AP AP2015008696A patent/AP2015008696A0/xx unknown
- 2014-03-05 US US14/197,476 patent/US9066979B2/en active Active
- 2014-03-05 PL PL14710620T patent/PL2964638T3/pl unknown
- 2014-03-05 LT LTEP14710620.7T patent/LT2964638T/lt unknown
- 2014-03-05 ES ES14710620.7T patent/ES2642201T3/es active Active
- 2014-03-05 BR BR112015020787-1A patent/BR112015020787B1/pt active IP Right Grant
- 2014-03-05 UA UAA201508063A patent/UA115686C2/uk unknown
- 2014-03-05 EP EP17179729.3A patent/EP3342770B1/en active Active
- 2014-03-05 EP EP14710620.7A patent/EP2964638B1/en active Active
- 2014-03-05 KR KR1020147021415A patent/KR101645112B1/ko active IP Right Grant
- 2014-03-05 AU AU2014224382A patent/AU2014224382B2/en active Active
- 2014-03-05 PE PE2015001877A patent/PE20152000A1/es active IP Right Grant
- 2014-03-05 MX MX2015011818A patent/MX362247B/es active IP Right Grant
- 2014-03-05 JP JP2015548782A patent/JP5894714B1/ja active Active
- 2014-03-05 PT PT147106207T patent/PT2964638T/pt unknown
- 2014-03-05 ME MEP-2017-259A patent/ME03041B/me unknown
- 2014-03-05 RS RS20171114A patent/RS56566B1/sr unknown
- 2014-03-05 WO PCT/GB2014/050655 patent/WO2014135876A1/en active Application Filing
- 2014-03-05 DK DK14710620.7T patent/DK2964638T3/en active
- 2014-03-05 SG SG11201506487YA patent/SG11201506487YA/en unknown
- 2014-03-05 RU RU2015139513A patent/RU2656597C2/ru active
- 2014-03-05 HU HUE14710620A patent/HUE034568T2/en unknown
- 2014-03-06 UY UY0001035369A patent/UY35369A/es not_active Application Discontinuation
- 2014-03-06 TW TW103107724A patent/TWI543977B/zh active
- 2014-03-06 AR ARP140100737A patent/AR095039A1/es active IP Right Grant
-
2015
- 2015-05-12 US US14/709,900 patent/US9375432B2/en active Active
- 2015-08-11 DO DO2015000189A patent/DOP2015000189A/es unknown
- 2015-08-13 IL IL240578A patent/IL240578B/en active IP Right Grant
- 2015-08-21 CL CL2015002361A patent/CL2015002361A1/es unknown
- 2015-08-27 CR CR20150450A patent/CR20150450A/es unknown
- 2015-08-28 TN TN2015000368A patent/TN2015000368A1/en unknown
- 2015-09-04 GT GT201500251A patent/GT201500251A/es unknown
- 2015-09-04 NI NI201500123A patent/NI201500123A/es unknown
- 2015-09-04 MA MA38380A patent/MA38380A1/fr unknown
- 2015-09-04 PH PH12015501965A patent/PH12015501965A1/en unknown
- 2015-10-05 ZA ZA2015/07353A patent/ZA201507353B/en unknown
-
2016
- 2016-04-15 HK HK16104323.2A patent/HK1216315A1/zh unknown
- 2016-05-24 US US15/162,816 patent/US9718806B2/en active Active
-
2017
- 2017-06-23 US US15/631,230 patent/US20180016259A1/en not_active Abandoned
- 2017-10-18 CY CY20171101087T patent/CY1119487T1/el unknown
- 2017-11-06 HR HRP20171689TT patent/HRP20171689T1/hr unknown
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
HRP20171689T1 (hr) | Inhibitori kinazolina aktivirajućih mutantnih oblika receptora epidermalnog faktora rasta | |
HRP20200624T1 (hr) | Derivati 2-(2,4,5-supstituiranog-anilino)pirimidina kao modulatori egfr korisni za liječenje raka | |
HRP20231614T1 (hr) | Spojevi pirolotriazina kao tam inhibitori | |
HRP20220255T1 (hr) | Derivati 6,7,8,9-tetrahidro-3h-pirazolo[4,3-f]izokinolina koji su korisni u liječenju raka | |
AU2015369983B2 (en) | Thieno[2,3-c]pyrrol-4-one derivatives as ERK inhibitors | |
HRP20210871T1 (hr) | Piridopirimdinonski inhibitori cdk2/4/6 | |
HRP20171748T1 (hr) | 6-amino kinazolina ili 3-cijano derivati kinolina, postupci priprave i njihova farmaceutska uporaba | |
HRP20210770T1 (hr) | PIROLO[2,3-d]PIRIMIDINIL-, PIROLO[2,3-b]PIRAZINIL- I PIROLO[2,3-d]PIRIDINILAKRILAMIDI | |
HRP20150868T1 (hr) | Derivati kinolina i kinoksalina kao inhibitori kinaze | |
HRP20191027T1 (hr) | Derivati imidazopiridina kao inhibitori tiposinskih receptora kinaza | |
JP2018012712A5 (hr) | ||
JP2017528524A5 (hr) | ||
WO2017223414A1 (en) | HETEROCYCLIC COMPOUNDS AS PI3K-γ INHIBITORS | |
JP2017521394A5 (hr) | ||
HRP20201400T1 (hr) | Spojevi 6-aril-4-(morfolin-4-il)-1h-piridin-2-ona korisni za liječenje karcinoma i dijabetesa | |
JP2014505735A5 (hr) | ||
GEP201706774B (en) | Heterocyclyl compounds | |
HRP20220840T1 (hr) | Inhibitori receptora faktora rasta fibroblasta | |
HRP20140807T1 (hr) | Derivati pirolo[2,3-d]pirimidina kao inhibitori protein kinaze b | |
EA201492125A1 (ru) | НОВЫЕ 4-(ЗАМЕЩЕННЫЙ АМИНО)-7Н-ПИРРОЛО[2,3-d]ПИРИМИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ LRRK2 | |
MX2022000826A (es) | Composiciones de forma de dosificacion que comprenden un inhibidor de tirosina cinasa de bruton. | |
JP2019511526A5 (hr) | ||
EP4132524A1 (en) | Oral compositions of mk2 pathway inhibitor for treatment of immune conditions | |
US11529350B2 (en) | Tyrosine kinase non-receptor 1 (TNK1) inhibitors and uses thereof | |
HRP20220520T1 (hr) | Ciklički dinukleotidi kao agensi protiv raka |