RU2013143839A - Ингибиторы сериновых/треониновых киназ - Google Patents
Ингибиторы сериновых/треониновых киназ Download PDFInfo
- Publication number
- RU2013143839A RU2013143839A RU2013143839/04A RU2013143839A RU2013143839A RU 2013143839 A RU2013143839 A RU 2013143839A RU 2013143839/04 A RU2013143839/04 A RU 2013143839/04A RU 2013143839 A RU2013143839 A RU 2013143839A RU 2013143839 A RU2013143839 A RU 2013143839A
- Authority
- RU
- Russia
- Prior art keywords
- alkyl
- optionally substituted
- haloalkyl
- hydroxyalkyl
- compound according
- Prior art date
Links
- MTCFGRXMJLQNBG-UHFFFAOYSA-N serine Chemical compound OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 title 2
- 102000009516 Protein Serine-Threonine Kinases Human genes 0.000 title 1
- 108010009341 Protein Serine-Threonine Kinases Proteins 0.000 title 1
- 241001522306 Serinus serinus Species 0.000 title 1
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 27
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 19
- 239000001257 hydrogen Substances 0.000 claims abstract 19
- -1 C-aralkyl Chemical group 0.000 claims abstract 18
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 16
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 14
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract 11
- 150000002431 hydrogen Chemical group 0.000 claims abstract 8
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims abstract 7
- 125000000714 pyrimidinyl group Chemical group 0.000 claims abstract 7
- 125000003118 aryl group Chemical group 0.000 claims abstract 6
- 125000004076 pyridyl group Chemical group 0.000 claims abstract 6
- 125000000335 thiazolyl group Chemical group 0.000 claims abstract 4
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract 3
- 125000002971 oxazolyl group Chemical group 0.000 claims abstract 3
- 125000003373 pyrazinyl group Chemical group 0.000 claims abstract 3
- 125000003226 pyrazolyl group Chemical group 0.000 claims abstract 3
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims abstract 2
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims abstract 2
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims abstract 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims abstract 2
- 125000002883 imidazolyl group Chemical group 0.000 claims abstract 2
- 125000001041 indolyl group Chemical group 0.000 claims abstract 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims abstract 2
- HRDXJKGNWSUIBT-UHFFFAOYSA-N methoxybenzene Chemical group [CH2]OC1=CC=CC=C1 HRDXJKGNWSUIBT-UHFFFAOYSA-N 0.000 claims abstract 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims abstract 2
- 125000000217 alkyl group Chemical group 0.000 claims 24
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 16
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 14
- 125000000623 heterocyclic group Chemical group 0.000 claims 10
- 229910052736 halogen Inorganic materials 0.000 claims 9
- 150000002367 halogens Chemical class 0.000 claims 9
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 6
- 230000003463 hyperproliferative effect Effects 0.000 claims 5
- 125000004485 2-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])([H])C1([H])* 0.000 claims 4
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 4
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 3
- 206010009944 Colon cancer Diseases 0.000 claims 3
- 125000002757 morpholinyl group Chemical group 0.000 claims 3
- 125000004043 oxo group Chemical group O=* 0.000 claims 3
- 125000003386 piperidinyl group Chemical group 0.000 claims 3
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 208000017604 Hodgkin disease Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 102100024193 Mitogen-activated protein kinase 1 Human genes 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 125000004404 heteroalkyl group Chemical group 0.000 claims 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 201000002510 thyroid cancer Diseases 0.000 claims 2
- 125000006594 (C1-C3) alkylsulfony group Chemical group 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000010507 Adenocarcinoma of Lung Diseases 0.000 claims 1
- 208000003200 Adenoma Diseases 0.000 claims 1
- 206010001233 Adenoma benign Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010023347 Keratoacanthoma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 208000008930 Low Back Pain Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 208000033833 Myelomonocytic Chronic Leukemia Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 1
- 206010057644 Testis cancer Diseases 0.000 claims 1
- 206010045515 Undifferentiated sarcoma Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000008385 Urogenital Neoplasms Diseases 0.000 claims 1
- 206010052428 Wound Diseases 0.000 claims 1
- 208000027418 Wounds and injury Diseases 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000004442 acylamino group Chemical group 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims 1
- 125000004966 cyanoalkyl group Chemical group 0.000 claims 1
- 229940127089 cytotoxic agent Drugs 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 125000004995 haloalkylthio group Chemical group 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical compound C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000003849 large cell carcinoma Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000005249 lung adenocarcinoma Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- LVWZTYCIRDMTEY-UHFFFAOYSA-N metamizole Chemical compound O=C1C(N(CS(O)(=O)=O)C)=C(C)N(C)N1C1=CC=CC=C1 LVWZTYCIRDMTEY-UHFFFAOYSA-N 0.000 claims 1
- 208000025113 myeloid leukemia Diseases 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 125000003566 oxetanyl group Chemical group 0.000 claims 1
- 201000010198 papillary carcinoma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 201000003068 rheumatic fever Diseases 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 208000000649 small cell carcinoma Diseases 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 208000001608 teratocarcinoma Diseases 0.000 claims 1
- 201000003120 testicular cancer Diseases 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 208000030901 thyroid gland follicular carcinoma Diseases 0.000 claims 1
- 125000004306 triazinyl group Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 208000022810 undifferentiated (embryonal) sarcoma Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- GVNVAWHJIKLAGL-UHFFFAOYSA-N 2-(cyclohexen-1-yl)cyclohexan-1-one Chemical compound O=C1CCCCC1C1=CCCCC1 GVNVAWHJIKLAGL-UHFFFAOYSA-N 0.000 abstract 1
- FZSXKNJOKINZSF-UHFFFAOYSA-N 2-pyridin-2-yl-1,3-thiazole Chemical compound C1=CSC(C=2N=CC=CC=2)=N1 FZSXKNJOKINZSF-UHFFFAOYSA-N 0.000 abstract 1
- 101150065749 Churc1 gene Proteins 0.000 abstract 1
- 102100038239 Protein Churchill Human genes 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161447587P | 2011-02-28 | 2011-02-28 | |
| US61/447,587 | 2011-02-28 | ||
| PCT/US2012/027009 WO2012118850A1 (en) | 2011-02-28 | 2012-02-28 | Serine/threonine kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2013143839A true RU2013143839A (ru) | 2015-04-10 |
Family
ID=45852719
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2013143839/04A RU2013143839A (ru) | 2011-02-28 | 2012-02-28 | Ингибиторы сериновых/треониновых киназ |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US9133187B2 (enExample) |
| EP (1) | EP2681215B1 (enExample) |
| JP (1) | JP6085866B2 (enExample) |
| KR (1) | KR101961500B1 (enExample) |
| CN (1) | CN103635472B (enExample) |
| BR (1) | BR112013021896A2 (enExample) |
| CA (1) | CA2828478C (enExample) |
| ES (1) | ES2543050T3 (enExample) |
| MX (1) | MX339873B (enExample) |
| RU (1) | RU2013143839A (enExample) |
| WO (1) | WO2012118850A1 (enExample) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9133187B2 (en) | 2011-02-28 | 2015-09-15 | Array Biopharma Inc. | Serine/threonine kinase inhibitors |
| AP2013007331A0 (en) | 2011-06-24 | 2013-12-31 | Amgen Inc | TRPM8 antagonists and their use in treatments |
| EP2723718A1 (en) | 2011-06-24 | 2014-04-30 | Amgen Inc. | Trpm8 antagonists and their use in treatments |
| ES2552989T3 (es) * | 2011-08-04 | 2015-12-03 | Array Biopharma, Inc. | Compuestos de quinazolina como inhibidores de la cinasa de serina / treonina |
| RU2632659C2 (ru) * | 2011-12-27 | 2017-10-09 | Байо-Фарм Солюшнс Ко., Лтд. | Фенилкарбаматные соединения для применения в предупреждении или лечении эпилепсии |
| PE20150666A1 (es) | 2012-03-01 | 2015-05-06 | Array Biopharma Inc | Inhibidores de serina/treonina cinasa |
| US8952009B2 (en) | 2012-08-06 | 2015-02-10 | Amgen Inc. | Chroman derivatives as TRPM8 inhibitors |
| CA2882750A1 (en) | 2012-08-27 | 2014-03-06 | Jim Blake | Serine/threonine kinase inhibitors for the treatment of hyperproliferative|diseases |
| CA2882410A1 (en) * | 2012-09-19 | 2014-03-27 | Novartis Ag | Dihydropyrrolidino-pyrimidines as kinase inhibitors |
| EP2909206A1 (en) | 2012-10-16 | 2015-08-26 | F. Hoffmann-La Roche AG | Serine/threonine kinase inhibitors |
| JPWO2015012328A1 (ja) * | 2013-07-24 | 2017-03-02 | 武田薬品工業株式会社 | 複素環化合物 |
| US9532987B2 (en) | 2013-09-05 | 2017-01-03 | Genentech, Inc. | Use of a combination of a MEK inhibitor and an ERK inhibitor for treatment of hyperproliferative diseases |
| EA031243B1 (ru) | 2013-12-06 | 2018-12-28 | Дженентек, Инк. | Ингибиторы серин/треонинкиназ |
| MX375902B (es) | 2013-12-30 | 2025-03-07 | Genentech Inc | Inhibidores de serina/treonina cinasa. |
| KR102379517B1 (ko) * | 2013-12-30 | 2022-03-25 | 제넨테크, 인크. | 세린/트레오닌 키나아제 억제제 |
| AU2017249229A1 (en) | 2016-04-15 | 2018-10-04 | Genentech, Inc. | Diagnostic and therapeutic methods for cancer |
| ES2863873T3 (es) * | 2016-05-18 | 2021-10-11 | Mirati Therapeutics Inc | Inhibidores de KRAS G12C |
| KR102811888B1 (ko) | 2017-09-08 | 2025-05-27 | 에프. 호프만-라 로슈 아게 | 암의 진단 및 치료 방법 |
| JP6986565B2 (ja) | 2017-09-29 | 2021-12-22 | 田辺三菱製薬株式会社 | 光学活性ピロリジン化合物及びその製造方法 |
| EP3706742B1 (en) | 2017-11-08 | 2023-03-15 | Merck Sharp & Dohme LLC | Prmt5 inhibitors |
| US20210008047A1 (en) | 2018-02-13 | 2021-01-14 | Vib Vzw | Targeting minimal residual disease in cancer with rxr antagonists |
| KR20210145773A (ko) | 2019-03-28 | 2021-12-02 | 지앙수 헨그루이 메디슨 컴퍼니 리미티드 | 티에노헤테로고리형 유도체, 이의 제조 방법 및 이의 의약적 용도 |
| WO2020200069A1 (zh) | 2019-03-29 | 2020-10-08 | 江苏恒瑞医药股份有限公司 | 吡咯并杂环类衍生物、其制备方法及其在医药上的应用 |
| EP3978498A1 (en) | 2019-05-24 | 2022-04-06 | Jiangsu Hengrui Medicine Co., Ltd. | Substituted fused bicyclic derivative, preparation method therefor, and application thereof in medicines |
| CN113874374B (zh) * | 2019-05-24 | 2024-12-27 | 江苏恒瑞医药股份有限公司 | 氢化吡啶并嘧啶类衍生物、其制备方法及其在医药上的应用 |
| CN111170929A (zh) * | 2019-12-12 | 2020-05-19 | 北京达因高科儿童药物研究院有限公司 | 一种由末端烯烃制备β-氨基醇的方法 |
| EP4217356B1 (en) | 2020-09-25 | 2025-05-14 | JANSSEN Pharmaceutica NV | Cyclin-dependent kinase 7 (cdk7) non-covalent inhibitors |
| US20230331731A1 (en) | 2020-09-29 | 2023-10-19 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | Crystal form of pyrrolo heterocyclic derivative and preparation method therefor |
| CN115040522B (zh) * | 2022-06-30 | 2024-02-06 | 牡丹江医学院 | 一种用于治疗肺癌的药物及其制备方法 |
| KR20250091232A (ko) * | 2022-10-25 | 2025-06-20 | 투오지에 바이오텍 (상하이) 컴퍼니 리미티드 | 피페리디노피리미딘계 유도체, 이의 제조 방법 및 이의 의학적 응용 |
| IT202200024963A1 (it) * | 2022-12-05 | 2024-06-05 | Angelini Pharma S P A | Composti attivatori dei canali potassio Kv7.2/Kv7.3 |
| TW202535869A (zh) * | 2023-10-23 | 2025-09-16 | 大陸商上海拓界生物醫藥科技有限公司 | 一種含有噻唑基的哌啶并嘧啶類衍生物、其製備方法及其醫藥上的應用 |
| WO2025223512A1 (zh) * | 2024-04-24 | 2025-10-30 | 江苏恒瑞医药股份有限公司 | 一种二氢吡啶并嘧啶衍生物的可药用盐、结晶形式及用途 |
| WO2026067627A1 (zh) * | 2024-09-26 | 2026-04-02 | 江苏恒瑞医药股份有限公司 | 一种降解剂及其用途 |
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- 2012-02-28 ES ES12709429.0T patent/ES2543050T3/es active Active
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- 2012-02-28 RU RU2013143839/04A patent/RU2013143839A/ru not_active Application Discontinuation
- 2012-02-28 KR KR1020137025269A patent/KR101961500B1/ko not_active Expired - Fee Related
- 2012-02-28 CA CA2828478A patent/CA2828478C/en not_active Expired - Fee Related
- 2012-02-28 WO PCT/US2012/027009 patent/WO2012118850A1/en not_active Ceased
- 2012-02-28 BR BR112013021896A patent/BR112013021896A2/pt not_active Application Discontinuation
- 2012-02-28 CN CN201280020897.3A patent/CN103635472B/zh active Active
- 2012-02-28 JP JP2013556817A patent/JP6085866B2/ja active Active
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| CA2828478A1 (en) | 2012-09-07 |
| EP2681215A1 (en) | 2014-01-08 |
| MX339873B (es) | 2016-06-15 |
| JP2014506930A (ja) | 2014-03-20 |
| ES2543050T3 (es) | 2015-08-14 |
| CN103635472A (zh) | 2014-03-12 |
| WO2012118850A1 (en) | 2012-09-07 |
| KR101961500B1 (ko) | 2019-03-22 |
| US9133187B2 (en) | 2015-09-15 |
| EP2681215B1 (en) | 2015-04-22 |
| US20130338140A1 (en) | 2013-12-19 |
| CA2828478C (en) | 2019-12-31 |
| KR20140014190A (ko) | 2014-02-05 |
| JP6085866B2 (ja) | 2017-03-01 |
| CN103635472B (zh) | 2018-01-12 |
| BR112013021896A2 (pt) | 2016-11-08 |
| MX2013009877A (es) | 2014-02-11 |
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| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
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