PE20190475A1 - Inhibidores de cdk2/4/6 - Google Patents
Inhibidores de cdk2/4/6Info
- Publication number
- PE20190475A1 PE20190475A1 PE2019000359A PE2019000359A PE20190475A1 PE 20190475 A1 PE20190475 A1 PE 20190475A1 PE 2019000359 A PE2019000359 A PE 2019000359A PE 2019000359 A PE2019000359 A PE 2019000359A PE 20190475 A1 PE20190475 A1 PE 20190475A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- fluoroalkyl
- cdk2
- compounds
- pyrimidin
- Prior art date
Links
- 108010024986 Cyclin-Dependent Kinase 2 Proteins 0.000 title abstract 3
- 102000015792 Cyclin-Dependent Kinase 2 Human genes 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000003709 fluoroalkyl group Chemical group 0.000 abstract 3
- 102100036239 Cyclin-dependent kinase 2 Human genes 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- HNHSQOTUDOXEGY-KBXCAEBGSA-N 4-[[6-(2-hydroxyethyl)-8-[(1R,2S)-2-methylcyclopentyl]-7-oxopyrido[2,3-d]pyrimidin-2-yl]amino]-N-methylpiperidine-1-sulfonamide Chemical compound OCCC1=CC2=C(N=C(N=C2)NC2CCN(CC2)S(=O)(=O)NC)N(C1=O)[C@H]1[C@H](CCC1)C HNHSQOTUDOXEGY-KBXCAEBGSA-N 0.000 abstract 1
- PPTJJWQOPWUCOH-UHFFFAOYSA-N 8-cyclopentyl-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrido[2,3-d]pyrimidin-7-one Chemical compound C1(CCCC1)N1C(C=CC2=C1N=C(N=C2)NC1CCN(CC1)S(=O)(=O)C)=O PPTJJWQOPWUCOH-UHFFFAOYSA-N 0.000 abstract 1
- 206010006187 Breast cancer Diseases 0.000 abstract 1
- 208000026310 Breast neoplasm Diseases 0.000 abstract 1
- 108010025464 Cyclin-Dependent Kinase 4 Proteins 0.000 abstract 1
- 108010025468 Cyclin-Dependent Kinase 6 Proteins 0.000 abstract 1
- 102100036252 Cyclin-dependent kinase 4 Human genes 0.000 abstract 1
- 102100026804 Cyclin-dependent kinase 6 Human genes 0.000 abstract 1
- 206010033128 Ovarian cancer Diseases 0.000 abstract 1
- 206010061535 Ovarian neoplasm Diseases 0.000 abstract 1
- 230000002159 abnormal effect Effects 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 210000000481 breast Anatomy 0.000 abstract 1
- 230000010261 cell growth Effects 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Se refiere a compuestos de las formulas (I) o una sal farmaceuticamente aceptable del mismo, en donde: R1 es heterociclilo de 3 a 10 miembros sustituido; R2 es independientemente F, OH, alquilo de C1-C4, entre otros; R3 es H, F, Cl, NH2, alquilo de C1-C4 o fluoroalquilo de C1-C4, en donde el alquilo de C1-C4 y fluoroalquilo de C1-C4 se sustituyen opcionalemente por OH; CN, alcoxi de C1-C4, entre otros; R4 es H, alquilo de C1-C2 o fluoroalquilo de C1-C2; R2A y R2B son independientemente H, OH o alquilo de C1-C4; p es 0,1, 2, 3 o 4; q es 0,1, 2 o 3; r es 0, 1 o 2. Son compuestos preferidos 8-ciclopentil-2-{[1-(metilsulfonil) piperidin-4-il] amino}pirido[2,3-d]pirimidin-7(8H)-ona; 4-({6-(2-hidroxietil)-8-[(1R,2S)-2-metilciclopentil]-7-oxo-7,8-dihidropirido[2,3-d]pirimidin-2-il}amino)-N-metilpiperidin-1-sulfonamida. Dichos compuestos pueden inhibir la actividad de CDK2, incluyendo CDK2, CDK4 y/o CDK6. Tambien se refiere a una composicion farmaceutica que es util para el tratamiento de crecimiento celular anormal, en particular el cancer de mama y ovario.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662371602P | 2016-08-15 | 2016-08-15 | |
| US201762533347P | 2017-07-17 | 2017-07-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20190475A1 true PE20190475A1 (es) | 2019-04-04 |
Family
ID=59631834
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2019000359A PE20190475A1 (es) | 2016-08-15 | 2017-07-31 | Inhibidores de cdk2/4/6 |
Country Status (43)
Families Citing this family (49)
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| JP2020097562A (ja) * | 2018-09-25 | 2020-06-25 | ファイザー・インク | ピリド［２，３−ｄ］ピリミジン−７（８ｈ）−オンの合成 |
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| EP3903828A4 (en) | 2018-12-21 | 2022-10-05 | Daiichi Sankyo Company, Limited | ANTIBODY-DRUG CONJUGATE AND KINAS INHIBITOR COMBINATION |
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| US20200316064A1 (en) * | 2019-02-15 | 2020-10-08 | Incyte Corporation | Cyclin-dependent kinase 2 biomarkers and uses thereof |
| US11384083B2 (en) | 2019-02-15 | 2022-07-12 | Incyte Corporation | Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors |
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| US11447494B2 (en) | 2019-05-01 | 2022-09-20 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
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| AU2020328025A1 (en) | 2019-08-14 | 2022-03-03 | Incyte Corporation | Imidazolyl pyrimidinylamine compounds as CDK2 inhibitors |
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2017
- 2017-07-31 AU AU2017311645A patent/AU2017311645B2/en active Active
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