DK2688887T3 - Kondenserede tricykliske dualinhibitorer af cdk 4/6 og flt3 - Google Patents

Kondenserede tricykliske dualinhibitorer af cdk 4/6 og flt3 Download PDF

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DK2688887T3
DK2688887T3 DK12711738.0T DK12711738T DK2688887T3 DK 2688887 T3 DK2688887 T3 DK 2688887T3 DK 12711738 T DK12711738 T DK 12711738T DK 2688887 T3 DK2688887 T3 DK 2688887T3
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alkyl
compound
substituted
pharmaceutically acceptable
hydrate
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DK12711738.0T
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Xiaoqi Chen
Kang Dai
Michael W Gribble Jr
Zhihong Li
Sarah E Lively
Lawrence R Mcgee
Xianghong Wang
Margaret F Weidner
Jian Zhang
Kathleen S Keegan
Jason Duquette
Justin N Huard
Mark L Ragains
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Amgen Inc
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    • 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
    • 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
    • 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
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Claims (26)

1. Forbindelse med formel I:
eller et farmaceutisk acceptabelt salt deraf, et hydrat deraf eller en blanding deraf, hvor: R1 er en gruppe med formel IA, formel IB, formel IC eller formel ID
, hvor JWV symbolet angiver bindingspunktet af gruppen med formel IA, IB, IC eller ID til resten af molekylet; R2 er en C5-C7 cycloalkylgruppe, er en 5- til 7-leddet heterocyclylgruppe, som indeholder 1,2 eller 3 heteroatomer udvalgt fra N, O og S, eller er en C7-C10 bicyklisk gruppe; hvor C5-C7 cycloalkylgruppen, den 5- til 7-leddede hetero- cyclylgruppe eller den C7-C10 bicykliske gruppe er usubstitueret eller er substitueret med 1-3 substituenter uafhængigt udvalgt fra usubstitueret -(C1-C6 alkyl), -OH, halogen, -0-(Ci-C6 alkyl), -C02H, -C(=0)-0-(Ci-C6 alkyl), -C(=0)-NR'R", -NR'R" eller et substitueret -(C1-C4 alkyl), hvor det substituerede -(C1-C4 alkyl) er substitueret med 1-3 substituenter uafhængigt udvalgt fra halogen, -OH, -OCH3, -S(=0)2-CH3 eller-C(=0)-CH3; R3a er udvalgt fra -H, -F eller -Cl, -(CrC3 alkyl) eller -0-(CrC3 alkyl); R3b er -H, halogen, -OH, -0-(Ci-C6 alkyl), usubstitueret -(C1-C6 alkyl), -NR'R", -C(=0)-(Ci-C6 alkyl), -C(=0)-0-(Ci-C6 alkyl), -C(=0)-NR'R" eller et substitueret -(C1-C6 alkyl), hvor det substituerede -(Ci-C6 alkyl) er substitueret med 1-3 substituenter uafhængigt udvalgt fra halogen, -OH, -OCH3, -CN eller -N02; R3c er -H, -(Ci-C3 alkyl) eller halogen; R4 er -H; R5 er -H; R6 er udvalgt fra -H, -(CrC6 alkyl), -C(=0)-(C1-C6 alkyl), -C(=0)-0-(Ci-C6 alkyl), -C(=0)-C(=0)-0H, -C(=0)-NR'R" eller -S(=0)-NR'R", hvor alkylgrup-pen af -(C1-C6 alkyl-), -C(=0)-(Ci-C6 alkyl-) og -C(=0)-0-(Ci-C6 alkyl-) gruppen er usubstitueret eller er substitueret med 1-3 substituenter uafhængigt udvalgt fra -OH, F, -S(=0)2-(Ci-C6 alkyl), -0-(Ci-C6 alkyl), -NR'R" eller -CN; R7a er -H, -CH3 eller halogen; R7b er -H, -(C1-C6 alkyl) eller halogen; eller R7b ikke er til stede, hvis R1 er en gruppe med formel IB eller formel ID; R7c er -H, usubstitueret -(C1-C6 alkyl), halogen, -0-(CrC6 alkyl), -N02, -CN, -NR'R", -C02H, -C(=0)-0-(Ci-C6 alkyl), -C(=0)-NR'R" eller et substitueret -(C1-O3 alkyl), hvor det substituerede -(Ci-C6 alkyl) er substitueret med 1-3 substituenter uafhængigt udvalgt fra -OH, halogen, -0-(CrC6 alkyl), -CN, -NR'R" eller -S(=0)2-CH3; eller R7c ikke er til stede, hvis R1 er en gruppe med formel IA eller formel IC; R8a er -H, usubstitueret -(C1-C6 alkyl) eller et substitueret -(C1-C6 alkyl), hvor det substituerede -(C1-C6 alkyl) er substitueret med 1-3 substituenter uafhængigt udvalgt fra -OH, halogen eller -0-(CrC6 alkyl); R8b er -H, usubstitueret -(C1-C6 alkyl) eller et substitueret -C1-C6 alkyl), hvor det substituerede -(C1-C6 alkyl) er substitueret med 1-3 substituenter uafhængigt udvalgt fra -OH, halogen eller -0-(CrC6 alkyl); eller R8a og R8b, når de er sammen, kan repræsentere =0; R8c er udvalgt fra -H, -OH, usubstitueret -(C1-C6 alkyl) eller et substitueret -(C1-C6 alkyl), hvor det substituerede -(C1-C6 alkyl) er substitueret med 1-3 substituenter uafhængigt udvalgt fra -OH, halogen eller -0-(Ci-C6 alkyl); R8d er -H, usubstitueret -(C1-C6 alkyl) eller et substitueret -(C1-C6 alkyl), hvor det substituerede -(C1-C6 alkyl) er substitueret med 1-3 substituenter uafhængigt udvalgt fra -OH, halogen eller -0-(Ci-C6 alkyl); R8e er -H, usubstitueret -(C1-C6 alkyl) eller et substitueret -(C1-C6 alkyl), hvor det substituerede -(C1-C6 alkyl) er substitueret med 1-3 substituenter uafhængigt udvalgt fra -OH, halogen eller -0-(Ci-C6 alkyl); R8f er -H, usubstitueret -(C1-C6 alkyl) eller et substitueret -(C1-C6 alkyl), hvor det substituerede -(Ci-C6 alkyl) er substitueret med 1-3 substituenter uafhængigt udvalgt fra -OH, halogen eller -0-(Ci-C6 alkyl); eller R8e og R8f, når de er sammen, kan repræsentere =0; og R' og R" uafhængigt er udvalgt fra -H, usubstitueret -(C1-C4 alkyl), eller -(C1-C4 alkyl) substitueret med 1 til 3 substituenter uafhængigt udvalgt fra -OH eller -F.
2. Forbindelse ifølge krav 1 eller farmaceutisk acceptabelt salt deraf, hydrat deraf eller blanding deraf, hvor R2 er en C5-C7 cycloalkylgruppe, som er usubstitueret eller er substitueret med 1-3 substituenter uafhængigt udvalgt fra usubstitueret -(C1-C6 alkyl), -OH, halogen, -0-(CrC6 alkyl), -C02H, -C(=0)-0-(Ci-C6 alkyl), -C(=0)-NR'R", -NR'R" eller et substitueret -(C1-C4 alkyl), hvor det substituerede -(C1-C4 alkyl) er substitueret med 1-3 substituenter uafhængigt udvalgt fra halogen, -OH, -OCH3, -S(=0)2-CH3 eller -C(=0)-CH3.
3. Forbindelse ifølge krav 2 eller farmaceutisk acceptabelt salt deraf, hydrat deraf eller blanding deraf, hvor R2 er en cyclohexylgruppe, der er substitueret med en -(C1-C2 alkyl-) gruppe.
4. Forbindelse ifølge krav 3 eller farmaceutisk acceptabelt salt deraf, hydrat deraf eller blanding deraf, hvor R2 er en gruppe med formel
, hvor «Λ/W symbolet angiver bindingspunktet til resten af molekylet.
5. Forbindelse ifølge et af kravene 1-4 eller farmaceutisk acceptabelt salt deraf, hydrat deraf eller blanding deraf, hvor R1 er en gruppe med formel IA eller IB.
6. Forbindelse ifølge krav 5 eller farmaceutisk acceptabelt salt deraf, hydrat deraf eller blanding deraf, hvor R1 er en gruppe med formel IA.
7. Forbindelse ifølge krav 1, hvor: R2 er en C5-C7 cycloalkylgruppe, som er usubstitueret eller er substitueret med 1-3 -(C1-C6 alkyl-) grupper; R3a er udvalgt fra -H, -(C1-C3 alkyl) eller -0-(CrC3 alkyl); R3b er -H; R3c er -H; R4 er -H; R5 er -H; R6 er udvalgt fra -H, -(C1-C6 alkyl), -C(=0)-(CrC6 alkyl) eller -C(=0)-C(=0)-OH, hvor alkylgruppen af -(C1-C6 alkyl-) og -C(=0)-(CrC6 alkyl-) gruppen er usubstitueret eller er substitueret med 1-3 substituenter uafhængigt udvalgt fra -OH, F, -S(=0)2-(Ci-C6 alkyl) eller -0-(Ci-C6 alkyl); R7a er -H; R7b er -H; eller ikke er til stede, hvis R1 er en gruppe med formel IB eller formel ID; R7c er -H; eller ikke er til stede, hvis R1 er en gruppe med formel IA eller formel IC; R8a er -H; R8b er -H; R8c er udvalgt fra -H, -OH eller usubstitueret -(C1-C6 alkyl); R8d er -H; R8e er -H; og R8f er -H, eller farmaceutisk acceptabelt salt deraf, hydrat deraf eller blanding deraf.
8. Forbindelse ifølge krav 1, hvor forbindelsen har formlen IIA
eller farmaceutisk acceptabelt salt deraf, hydrat deraf eller blanding deraf hvor: R3a er udvalgt fra -H, -F eller -Cl, -(C1-C3 alkyl) eller -0-(CrC3 alkyl); R3b er -H, halogen, -OH, -0-(Ci-C6 alkyl), usubstitueret -(C1-C6 alkyl), -NR'R", -C(=0)-(Ci-C6 alkyl), -C(=0)-0-(Ci-C6 alkyl), -C(=0)-NR'R" eller et substitueret -(C1-C6 alkyl), hvor det substituerede -(CrC6 alkyl) er substitueret med 1-3 substituenter uafhængigt udvalgt fra halogen, -OH, -OCH3, -CN eller -NO2; R6 er udvalgt fra -H, -(CrC6 alkyl), -C(=0)-(Ci-C6 alkyl), -C(=0)-C(=0)-0H, -C(=0)-NR'R" eller -S(=0)-NR'R", hvor alkylgruppen af -(C1-C6 alkyl-) og -C(=0)-(Ci-C6 alkyl-) gruppen er usubstitueret eller er substitueret med 1-3 substituenter uafhængigt udvalgt fra -OH, F, -S(=0)2-(CrC6 alkyl), -0-(CrC6 alkyl), -NR'R" eller -CN; og R8c er udvalgt fra -H, -OH, usubstitueret -(CrC6 alkyl) eller et substitueret (C1-C6 alkyl), hvor det substituerede -(C1-C6 alkyl) er substitueret med 1-3 substituenter uafhængigt udvalgt fra -OH, halogen eller -0-(Ci-C6 alkyl).
9. Forbindelse ifølge krav 8, hvor: R3a er udvalgt fra -H, -(C1-C3 alkyl) eller -0-(CrC3 alkyl); R3b er -H; R6 er udvalgt fra -H, -(Ci-C6 alkyl), -C(=0)-(Ci-C6 alkyl) eller -0(=0)-0(=0)-OH, hvor alkylgruppen af -(CrC6 alkyl-) og -C(=0)-(Ci-C6 alkyl-) gruppen er usubstitueret eller er substitueret med 1-3 substituenter uafhængigt udvalgt fra -OH, F, -S(=0)2-(CrC6 alkyl) eller -0-(CrC6 alkyl); og R8c er udvalgt fra -H, usubstitueret -(C1-C6 alkyl) eller -OH, eller farmaceutisk acceptabelt salt deraf, hydrat deraf eller blanding deraf.
10. Forbindelse ifølge krav 8 eller krav 9 eller farmaceutisk acceptabelt salt deraf, hydrat deraf eller blanding deraf, hvor R8c er udvalgt fra -H, -CH3 eller -OH.
11. Forbindelse ifølge krav 10 eller farmaceutisk acceptabelt salt deraf, hydrat deraf eller blanding deraf, hvor R8c er -H.
12. Forbindelse ifølge krav 11 eller farmaceutisk acceptabelt salt deraf, hydrat deraf eller blanding deraf, hvor R3a er -H.
13. Forbindelse ifølge et af kravene 7-12 eller farmaceutisk acceptabelt salt deraf, hydrat deraf eller blanding deraf, hvor R6 er udvalgt fra -H, -C(=0)-CH3, -CH2CH2OH, -CH2CH2CH2OH, -C(=0)-CH20H, -C(=0)-C(=0)-0H, -CH2CH2CF3, -CH2CH2F, -CH2CH2S(=0)2-CH3 eller -CH2CH2OCH3.
14. Forbindelse ifølge krav 13 eller farmaceutisk acceptabelt salt deraf, hydrat deraf eller blanding deraf, hvor R6 er udvalgt fra -C(=0)-CH3 eller -C(=0)-CH20H.
15. Forbindelse ifølge krav 1, hvor forbindelsen er udvalgt fra
eller farmaceutisk acceptabelt salt eller hydrat deraf.
16. Forbindelse ifølge krav 1, hvor forbindelsen er
eller farmaceutisk acceptabelt salt eller hydrat deraf.
17. Forbindelse ifølge krav 1, hvor forbindelsen er
eller farmaceutisk acceptabelt salt eller hydrat deraf.
18. Forbindelse ifølge krav 1, hvor forbindelsen er
eller farmaceutisk acceptabelt salt eller hydrat deraf.
19. Forbindelse ifølge krav 1, hvor forbindelsen er udvalgt fra
eller farmaceutisk acceptabelt salt eller hydrat deraf.
20. Forbindelse ifølge et af kravene 1-19 i en neutral form.
21. Farmaceutisk acceptabelt salt eller hydrat deraf ifølge et af kravene 1-19.
22. Farmaceutisk acceptabelt salt eller hydrat deraf ifølge krav 21, hvor det farmaceutisk acceptable salt eller hydratet deraf er udvalgt fra et chloridsalt, et methansulfonatsalt eller et benzensulfonatsalt.
23. Farmaceutisk sammensætning, hvor den farmaceutiske sammensætning omfatter en terapeutisk virksom mængde af forbindelsen, farmaceutisk acceptabelt salt, hydrat deraf eller blanding deraf ifølge et af kravene 1-22 og mindst en farmaceutisk acceptabelt excipiens, bærer eller fortyndingsmiddel.
24. Forbindelse ifølge et af kravene 1-22 eller farmaceutisk acceptabelt salt eller hydrat deraf eller blanding deraf eller farmaceutisk sammensætning ifølge krav 23 til anvendelse ved behandling af cancer.
25. Forbindelse ifølge krav 24 eller farmaceutisk acceptabelt salt eller hydrat deraf eller blanding deraf til anvendelse ved behandling af cancer, hvor canceren er udvalgt fra akut myeloid leukæmi, akut lymfoblastisk leukæmi, mye-lodysplastisk syndrom, myelomatose, kronisk myeloid leukæmi, akut lymfa-tisk leukæmi, kronisk lymfatisk leukæmi, non-Hodgkin-lymfom, andet lymfom, andet myelom eller anden leukæmi.
26. Forbindelse ifølge krav 24 eller farmaceutisk acceptabelt salt eller hydrat deraf eller blanding deraf til anvendelse ved behandling af cancer, hvor canceren er akut myeloid leukæmi.
DK12711738.0T 2011-03-23 2012-03-21 Kondenserede tricykliske dualinhibitorer af cdk 4/6 og flt3 DK2688887T3 (da)

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US201161466841P 2011-03-23 2011-03-23
PCT/US2012/030007 WO2012129344A1 (en) 2011-03-23 2012-03-21 Fused tricyclic dual inhibitors of cdk 4/6 and flt3

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US (3) US8623885B2 (da)
EP (2) EP2937349B1 (da)
JP (1) JP5647374B2 (da)
KR (2) KR20160035613A (da)
CN (1) CN103703000B (da)
AR (1) AR085544A1 (da)
AU (1) AU2012230896B9 (da)
CA (1) CA2830516C (da)
DK (2) DK2688887T3 (da)
ES (2) ES2620521T3 (da)
HK (2) HK1191014A1 (da)
JO (1) JO3073B1 (da)
MX (1) MX2013010871A (da)
MY (1) MY161199A (da)
PT (2) PT2688887E (da)
SG (1) SG193580A1 (da)
TW (1) TWI438204B (da)
UY (1) UY33969A (da)
WO (1) WO2012129344A1 (da)

Families Citing this family (115)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI1879573T1 (sl) 2005-05-10 2013-04-30 Incyte Corporation Experimental Station Modulatorji indolamin 2,3-dioksigenaze in postopki za uporabo le-te
KR20100095020A (ko) * 2007-12-19 2010-08-27 암젠 인크 세포 주기 억제제로서의 융합된 피리딘, 피리미딘 및 트리아진 화합물
NO2824100T3 (da) 2008-07-08 2018-07-21
PT2688887E (pt) 2011-03-23 2015-07-06 Amgen Inc Inibidores duais tricíclicos fusionados de cdk 4/6 e flt3
SG10201610416TA (en) 2012-06-13 2017-01-27 Incyte Corp Substituted tricyclic compounds as fgfr inhibitors
WO2014109858A1 (en) 2013-01-14 2014-07-17 Amgen Inc. Methods of using cell-cycle inhibitors to modulate one or more properties of a cell culture
JP6435315B2 (ja) * 2013-03-15 2018-12-05 ジー１、セラピューティクス、インコーポレイテッドＧ１ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． 高活性抗新生物薬及び抗増殖剤
CN108283644B (zh) 2013-03-15 2022-03-18 G1治疗公司 在化学疗法期间对正常细胞的瞬时保护
EP2986740B1 (en) 2013-04-16 2020-01-15 Memorial Sloan-Kettering Cancer Center Companion diagnostic for cdk4 inhibitors
SI2986610T1 (en) 2013-04-19 2018-04-30 Incyte Holdings Corporation Bicyclic heterocycles as inhibitors of FGFR
US9603927B2 (en) 2014-02-28 2017-03-28 Janssen Biotech, Inc. Combination therapies with anti-CD38 antibodies
US9732154B2 (en) 2014-02-28 2017-08-15 Janssen Biotech, Inc. Anti-CD38 antibodies for treatment of acute lymphoblastic leukemia
EP3172214B1 (en) * 2014-07-26 2020-05-13 Sunshine Lake Pharma Co., Ltd. 2-amino-pyrido[2,3-d]pyrimidin-7(8h)-one derivatives as cdk inhibitors and uses thereof
ES2890669T3 (es) 2014-09-09 2022-01-21 Janssen Biotech Inc Terapias de combinación con anticuerpos anti-CD38
EP3191098A4 (en) 2014-09-12 2018-04-25 G1 Therapeutics, Inc. Combinations and dosing regimes to treat rb-positive tumors
KR102597989B1 (ko) * 2014-12-04 2023-11-02 얀센 바이오테크 인코포레이티드 급성 골수성 백혈병을 치료하기 위한 항-cd38 항체
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
MX2020004108A (es) 2015-02-20 2022-01-03 Incyte Corp Heterociclos biciclicos como inhibidores de receptores del factor de crecimiento fibroblastico (fgfr).
JP6793401B2 (ja) * 2015-03-11 2020-12-02 国立研究開発法人理化学研究所 難治性白血病治療薬
CA2978363A1 (en) * 2015-03-11 2016-09-15 Charles Z. Ding Substituted 2-hydrogen-pyrazole derivative serving as anticancer drugs
US9840503B2 (en) 2015-05-11 2017-12-12 Incyte Corporation Heterocyclic compounds and uses thereof
US10766965B2 (en) 2015-05-20 2020-09-08 Janssen Biotech, Inc. Anti-CD38 antibodies for treatment of light chain amyloidosis and other CD38-positive hematological malignancies
CR20170587A (es) 2015-06-22 2018-04-03 Janssen Biotech Inc Terapias de combinación para enfermedades malignas hematológicas con anticuerpos anti-cd38 e inhibidores de survivina
US20170044265A1 (en) 2015-06-24 2017-02-16 Janssen Biotech, Inc. Immune Modulation and Treatment of Solid Tumors with Antibodies that Specifically Bind CD38
US9708333B2 (en) 2015-08-12 2017-07-18 Incyte Corporation Fused bicyclic 1,2,4-triazine compounds as TAM inhibitors
US10053465B2 (en) 2015-08-26 2018-08-21 Incyte Corporation Pyrrolopyrimidine derivatives as TAM inhibitors
US10781261B2 (en) 2015-11-03 2020-09-22 Janssen Biotech, Inc. Subcutaneous formulations of anti-CD38 antibodies and their uses
WO2017079150A1 (en) 2015-11-03 2017-05-11 Janssen Biotech, Inc. Subcutaneous formulations of anti-cd38 antibodies and their uses
US11921116B2 (en) 2016-03-09 2024-03-05 Memorial Sloan Kettering Cancer Center Enigma and CDH18 as companion diagnostics for CDK4 inhibitors
SG10202009423QA (en) 2016-03-28 2020-11-27 Incyte Corp Pyrrolotriazine compounds as tam inhibitors
JP7190425B2 (ja) 2016-08-23 2022-12-15 エーザイ・アール・アンド・ディー・マネジメント株式会社 肝細胞癌の治療のための併用療法
JP7044801B2 (ja) 2016-12-16 2022-03-30 シーストーン・ファーマスーティカルズ・（スージョウ）・カンパニー・リミテッド Ｃｄｋ４／６阻害剤
TW201829386A (zh) 2016-12-22 2018-08-16 美商全球血液治療公司 組蛋白甲基轉移酶抑制劑
US10954216B2 (en) 2016-12-27 2021-03-23 Riken BMP-signal-inhibiting compound
US11395821B2 (en) 2017-01-30 2022-07-26 G1 Therapeutics, Inc. Treatment of EGFR-driven cancer with fewer side effects
MA47776A (fr) 2017-03-16 2020-01-22 Eisai R&D Man Co Ltd Polythérapies pour le traitement du cancer du sein
CN107021965B (zh) * 2017-05-16 2019-08-13 无锡捷化医药科技有限公司 一种合成5,6,7,8-四氢-1,6-萘啶-2胺的方法
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
MX2019014759A (es) * 2017-06-09 2020-02-12 Global Blood Therapeutics Inc Compuestos de azaindol como inhibidores de metiltransferasa de histona.
WO2019029663A1 (zh) * 2017-08-11 2019-02-14 晟科药业（江苏）有限公司 1h-吡唑并[4,3-h]喹唑啉类化合物作为蛋白激酶抑制剂
TWI821200B (zh) 2017-09-27 2023-11-11 美商英塞特公司 Tam抑制劑之鹽
AU2018359527A1 (en) 2017-10-31 2020-05-07 Janssen Biotech, Inc. Methods of treating high risk multiple myeloma
WO2019136451A1 (en) 2018-01-08 2019-07-11 G1 Therapeutics, Inc. G1t38 superior dosage regimes
CR20200441A (es) 2018-02-27 2021-03-15 Incyte Corp Imidazopirimidinas y triazolopirimidinas como inhibidores de a2a / a2b
WO2019213544A2 (en) 2018-05-04 2019-11-07 Incyte Corporation Solid forms of an fgfr inhibitor and processes for preparing the same
TW201946630A (zh) 2018-05-04 2019-12-16 美商英塞特公司 Fgfr抑制劑之鹽
MX2020012376A (es) 2018-05-18 2021-03-09 Incyte Corp Derivados de pirimidina fusionados como inhibidores de los receptores de adenosina a2a/a2b.
US11241438B2 (en) 2018-06-29 2022-02-08 Incyte Corporation Formulations of an AXL/MER inhibitor
TW202402759A (zh) 2018-07-05 2024-01-16 美商英塞特公司 作為a2a/a2b抑制劑之稠合吡嗪衍生物
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
CN111377922B (zh) * 2018-12-29 2021-12-17 武汉光谷通用名药物研究院有限公司 稠合三环类化合物及其用途
TWI829857B (zh) 2019-01-29 2024-01-21 美商英塞特公司 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶
CA3130210A1 (en) 2019-02-15 2020-08-20 Incyte Corporation Cyclin-dependent kinase 2 biomarkers and uses thereof
WO2020168197A1 (en) 2019-02-15 2020-08-20 Incyte Corporation Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors
CN113767100A (zh) 2019-03-01 2021-12-07 锐新医药公司 双环杂芳基化合物及其用途
WO2020180770A1 (en) 2019-03-01 2020-09-10 Revolution Medicines, Inc. Bicyclic heterocyclyl compounds and uses thereof
TW202100520A (zh) 2019-03-05 2021-01-01 美商英塞特公司 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11919904B2 (en) 2019-03-29 2024-03-05 Incyte Corporation Sulfonylamide compounds as CDK2 inhibitors
WO2020223558A1 (en) 2019-05-01 2020-11-05 Incyte Corporation Tricyclic amine compounds as cdk2 inhibitors
US11440914B2 (en) 2019-05-01 2022-09-13 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
AU2020319875A1 (en) 2019-08-01 2022-02-17 Incyte Corporation A dosing regimen for an IDO inhibitor
KR20220064369A (ko) 2019-08-14 2022-05-18 인사이트 코포레이션 Cdk2 저해제로서의 이미다졸릴 피리디미딘일아민 화합물
BR112022006977A2 (pt) 2019-10-11 2022-09-20 Incyte Corp Aminas bicíclicas como inibidores de cdk2
IL291901A (en) 2019-10-14 2022-06-01 Incyte Corp Bicyclyl heterocycles as fgr suppressors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
BR112022008565A2 (pt) 2019-11-04 2022-08-09 Revolution Medicines Inc Composto, composição farmacêutica, conjugado, métodos para tratar câncer e um distúrbio relativo à proteína ras
JP2022553859A (ja) 2019-11-04 2022-12-26 レボリューション メディシンズ インコーポレイテッド Ｒａｓ阻害剤
TW202132315A (zh) 2019-11-04 2021-09-01 美商銳新醫藥公司 Ras 抑制劑
CN114901662A (zh) 2019-11-08 2022-08-12 锐新医药公司 双环杂芳基化合物及其用途
WO2021113462A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Derivatives of an fgfr inhibitor
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
JP2023509701A (ja) 2020-01-07 2023-03-09 レヴォリューション・メディスンズ，インコーポレイテッド Ｓｈｐ２阻害剤投薬およびがんを処置する方法
CN115697343A (zh) 2020-03-06 2023-02-03 因赛特公司 包含axl/mer和pd-1/pd-l1抑制剂的组合疗法
TW202202495A (zh) 2020-03-26 2022-01-16 匈牙利商羅特格登公司 作為ｇａｍｍａ－胺基丁酸Ａ受體次單元ａｌｐｈａ ５受體調節劑之㖠啶及吡啶并〔３，４－ｃ〕嗒𠯤衍生物
WO2021211864A1 (en) 2020-04-16 2021-10-21 Incyte Corporation Fused tricyclic kras inhibitors
WO2021231526A1 (en) 2020-05-13 2021-11-18 Incyte Corporation Fused pyrimidine compounds as kras inhibitors
US10988479B1 (en) 2020-06-15 2021-04-27 G1 Therapeutics, Inc. Morphic forms of trilaciclib and methods of manufacture thereof
IL299131A (en) 2020-06-18 2023-02-01 Revolution Medicines Inc Methods for delaying, preventing and treating acquired resistance to RAS inhibitors
US20220064188A1 (en) 2020-08-28 2022-03-03 Incyte Corporation Vinyl imidazole compounds as inhibitors of kras
EP4208261A1 (en) 2020-09-03 2023-07-12 Revolution Medicines, Inc. Use of sos1 inhibitors to treat malignancies with shp2 mutations
EP4214209A1 (en) 2020-09-15 2023-07-26 Revolution Medicines, Inc. Indole derivatives as ras inhibitors in the treatment of cancer
CN112043710A (zh) * 2020-09-28 2020-12-08 广州智睿医药科技有限公司 一种治疗或预防与lrrk2激酶或异常lrrk2突变激酶活性相关疾病的药物
WO2022072783A1 (en) 2020-10-02 2022-04-07 Incyte Corporation Bicyclic dione compounds as inhibitors of kras
AR124449A1 (es) 2020-12-22 2023-03-29 Qilu Regor Therapeutics Inc Inhibidores de sos1 y usos de los mismos
WO2022155941A1 (en) 2021-01-25 2022-07-28 Qilu Regor Therapeutics Inc. Cdk2 inhibitors
WO2022206888A1 (en) 2021-03-31 2022-10-06 Qilu Regor Therapeutics Inc. Cdk2 inhibitors and use thereof
WO2022221170A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
EP4334321A1 (en) 2021-05-05 2024-03-13 Revolution Medicines, Inc. Ras inhibitors
CN117616031A (zh) 2021-05-05 2024-02-27 锐新医药公司 用于治疗癌症的ras抑制剂
CA3220155A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
KR20240032915A (ko) 2021-07-07 2024-03-12 인사이트 코포레이션 Kras의 저해제로서의 삼환식 화합물
EP4370515A1 (en) 2021-07-14 2024-05-22 Incyte Corporation Tricyclic compounds as inhibitors of kras
WO2023034290A1 (en) 2021-08-31 2023-03-09 Incyte Corporation Naphthyridine compounds as inhibitors of kras
US20230151005A1 (en) 2021-09-21 2023-05-18 Incyte Corporation Hetero-tricyclic compounds as inhibitors of kras
CA3234375A1 (en) 2021-10-01 2023-04-06 Incyte Corporation Pyrazoloquinoline kras inhibitors
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
WO2023064857A1 (en) 2021-10-14 2023-04-20 Incyte Corporation Quinoline compounds as inhibitors of kras
US20230226040A1 (en) 2021-11-22 2023-07-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a kras inhibitor
WO2023102184A1 (en) 2021-12-03 2023-06-08 Incyte Corporation Bicyclic amine compounds as cdk12 inhibitors
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
US20230183251A1 (en) 2021-12-10 2023-06-15 Incyte Corporation Bicyclic amines as cdk12 inhibitors
WO2023114954A1 (en) 2021-12-17 2023-06-22 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
TW202340215A (zh) 2021-12-22 2023-10-16 美商英塞特公司 Ｆｇｆｒ抑制劑之鹽及固體形式以及其製備方法
WO2023168686A1 (en) 2022-03-11 2023-09-14 Qilu Regor Therapeutics Inc. Substituted cyclopentanes as cdk2 inhibitors
WO2023116884A1 (en) 2021-12-24 2023-06-29 Qilu Regor Therapeutics Inc. Cdk2 inhibitors and use thereof
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
US20230279004A1 (en) 2022-03-07 2023-09-07 Incyte Corporation Solid forms, salts, and processes of preparation of a cdk2 inhibitor
WO2023172940A1 (en) 2022-03-08 2023-09-14 Revolution Medicines, Inc. Methods for treating immune refractory lung cancer
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2023250430A1 (en) 2022-06-22 2023-12-28 Incyte Corporation Bicyclic amine cdk12 inhibitors
US20240101557A1 (en) 2022-07-11 2024-03-28 Incyte Corporation Fused tricyclic compounds as inhibitors of kras g12v mutants

Family Cites Families (101)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1168290A (en) 1964-08-27 1969-10-22 Allen & Hanburys Ltd Novel Heterocyclic Compounds
US4160452A (en) 1977-04-07 1979-07-10 Alza Corporation Osmotic system having laminated wall comprising semipermeable lamina and microporous lamina
US4256108A (en) 1977-04-07 1981-03-17 Alza Corporation Microporous-semipermeable laminated osmotic system
US4265874A (en) 1980-04-25 1981-05-05 Alza Corporation Method of delivering drug with aid of effervescent activity generated in environment of use
IT1153216B (it) 1981-10-16 1987-01-14 Schering Ag Procedimento per la preparazione di composti cianoeterociclici
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
US5892112A (en) 1990-11-21 1999-04-06 Glycomed Incorporated Process for preparing synthetic matrix metalloprotease inhibitors
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
NZ258697A (en) 1992-11-13 1996-03-26 Immunex Corp Elk-l polypeptide, coding sequence and vector therefor
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
US5700823A (en) 1994-01-07 1997-12-23 Sugen, Inc. Treatment of platelet derived growth factor related disorders such as cancers
EP1464706A3 (en) 1994-04-15 2004-11-03 Amgen Inc., HEK5, HEK7, HEK8, HEK11, EPH-like receptor protein tyrosine kinases
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
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
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
US6846630B2 (en) 1996-10-18 2005-01-25 Takara Shuzo Co., Ltd. Nucleic acid encoding receptor type protein kinase
JP2001507349A (ja) 1996-12-23 2001-06-05 セルテック セラピューティックス リミテッド 縮合多環式２−アミノピリミジン誘導体、それらの製造およびたんぱく質チロシンキナーゼ抑制因子としてのそれらの使用
US6498163B1 (en) 1997-02-05 2002-12-24 Warner-Lambert Company Pyrido[2,3-D]pyrimidines and 4-aminopyrimidines as inhibitors of cellular proliferation
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
WO2000012089A1 (en) 1998-08-31 2000-03-09 Merck & Co., Inc. Novel angiogenesis inhibitors
GB9800569D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
WO1999045009A1 (en) 1998-03-04 1999-09-10 Bristol-Myers Squibb Company Heterocyclo-substituted imidazopyrazine protein tyrosine kinase inhibitors
DK2020408T3 (da) 1998-05-29 2013-09-30 Sugen Inc Pyrrol-substitueret 2-indolinon som proteinkinaseinhibitor
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
JP2002520324A (ja) 1998-07-10 2002-07-09 メルク エンド カムパニー インコーポレーテッド 新規な血管形成インヒビター
JP2002534468A (ja) 1999-01-13 2002-10-15 バイエル コーポレイション ｐ３８キナーゼ阻害剤としてのω−カルボキシアリール置換ジフェニル尿素
DE60028740T2 (de) 1999-03-30 2007-05-24 Novartis Ag Phthalazinderivate zur behandlung von entzündlichen erkrankungen
JP4587626B2 (ja) 1999-06-07 2010-11-24 イミュネックス・コーポレーション Ｔｅｋアンタゴニスト
US6521424B2 (en) 1999-06-07 2003-02-18 Immunex Corporation Recombinant expression of Tek antagonists
UA72946C2 (uk) 1999-11-05 2005-05-16 Астразенека Аб Похідні хіназоліну як інгібітори васкулярного ендотеліального фактора росту (vegf)
WO2001037820A2 (en) 1999-11-24 2001-05-31 Sugen, Inc. Ionizable indolinone derivatives and their use as ptk ligands
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
JP2003523768A (ja) 2000-02-25 2003-08-12 イミュネックス・コーポレーション インテグリンアンタゴニスト
IL151480A0 (en) 2000-03-06 2003-04-10 Warner Lambert Co 5-alkylpyrido[2,3-d] pyrimidines tyrosine kinase inhibitors
BR0109161A (pt) 2000-03-15 2002-11-26 Aventis Pharma Gmbh Beta-carbolinas substituìdas com atividade de inibição de ikb-quinase
GB0007371D0 (en) 2000-03-28 2000-05-17 Astrazeneca Uk Ltd Chemical compounds
WO2002002550A1 (fr) 2000-06-30 2002-01-10 Banyu Pharmaceutical Co., Ltd. Nouveaux derives pyrazinone
US6630500B2 (en) 2000-08-25 2003-10-07 Cephalon, Inc. Selected fused pyrrolocarbazoles
SI1343782T1 (sl) 2000-12-21 2009-10-31 Smithkline Beecham Corp Pirimidinamini kot modulatorji angiogeneze
US7102009B2 (en) 2001-01-12 2006-09-05 Amgen Inc. Substituted amine derivatives and methods of use
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
US20020147198A1 (en) 2001-01-12 2002-10-10 Guoqing Chen Substituted arylamine derivatives and methods of use
US7105682B2 (en) 2001-01-12 2006-09-12 Amgen Inc. Substituted amine derivatives and methods of use
US6878714B2 (en) 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
WO2003062246A1 (en) 2002-01-22 2003-07-31 Warner-Lambert Company Llc 2-thia-1,6,8-triaza-naphtalene-2,2-dioxides as cdk inhibitors
CN101001857B (zh) 2002-01-22 2011-06-22 沃尼尔·朗伯有限责任公司 2-(吡啶-2-基氨基)-吡啶并[2,3-d]嘧啶-7-酮
US20030199525A1 (en) 2002-03-21 2003-10-23 Hirst Gavin C. Kinase inhibitors
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
US7563798B2 (en) 2002-09-04 2009-07-21 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
DE602004021558D1 (de) 2003-01-17 2009-07-30 Warner Lambert Co 2-aminopyridin-substituierteheterocyclen als inhibitoren der zellulären proliferation
OA13170A (en) 2003-05-22 2006-12-13 Pharmacia Italia Spa Pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors.
CN1835951B (zh) 2003-07-11 2010-06-02 沃尼尔·朗伯有限责任公司 选择性cdk4抑制剂的羟乙基磺酸盐
AU2004285052A1 (en) 2003-10-31 2005-05-12 Neurogen Corporation 4-amino (AZA) quinoline derivatives as capsaicin receptor agonists
GB0329214D0 (en) 2003-12-17 2004-01-21 Glaxo Group Ltd Novel compounds
JP2007523151A (ja) 2004-02-18 2007-08-16 ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー ２−（ピリジン−３−イルアミノ）−ピリド［２，３−ｄ］ピリミジン−７−オン
GB0403606D0 (en) 2004-02-18 2004-03-24 Novartis Ag Organic compounds
JP2007530654A (ja) 2004-03-30 2007-11-01 ファイザー・プロダクツ・インク シグナル伝達阻害剤の組合せ
MXPA06013250A (es) 2004-05-14 2007-02-28 Abbott Lab Inhibidores de quinasa como agentes terapeuticos.
US7452887B2 (en) 2004-06-04 2008-11-18 Amphora Discovery Corporation Quinoline- and isoquinoline-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions, and uses thereof
CA2569277A1 (en) 2004-06-04 2005-12-15 Pfizer Products Inc. Method for treating abnormal cell growth
WO2006021547A1 (de) 2004-08-26 2006-03-02 Boehringer Ingelheim International Gmbh Pteridinone als plk (polo like kinase) inhibitoren
WO2006042102A2 (en) 2004-10-05 2006-04-20 Neurogen Corporation Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds
CA2583622A1 (en) 2004-10-13 2006-04-27 Merck & Co., Inc. Ophthalmic compositions for treating ocular hypertension
TW200633990A (en) 2004-11-18 2006-10-01 Takeda Pharmaceuticals Co Amide compound
US20060142312A1 (en) 2004-12-23 2006-06-29 Pfizer Inc C6-aryl and heteroaryl substituted pyrido[2,3-D] pyrimidin-7-ones
AU2006205851A1 (en) 2005-01-14 2006-07-20 Janssen Pharmaceutica N.V. 5-membered annelated heterocyclic pyrimidines as kinase inhibitors
WO2006077428A1 (en) 2005-01-21 2006-07-27 Astex Therapeutics Limited Pharmaceutical compounds
JP2008542433A (ja) 2005-06-09 2008-11-27 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 ＣＤＫ−１インヒビターとしてのα−カルボリン
CN101291936A (zh) 2005-08-19 2008-10-22 先灵公司 作为治疗剂的稠合三环mglur1拮抗剂
EP1926734A1 (en) 2005-08-22 2008-06-04 Amgen Inc. Pyrazolopyridine and pyrazolopyrimidine compounds useful as kinase enzymes modulators
CN101360499B (zh) 2005-10-06 2015-10-07 默沙东公司 吡唑并[1,5-a]嘧啶衍生物在制备抑制蛋白激酶的药物中的用途
HUE028504T2 (en) 2006-01-23 2016-12-28 Amgen Inc Aurora kinase modulators and method for their application
MX2008013110A (es) 2006-04-12 2009-03-06 Vertex Pharma 4-5-dihidro-[1,2,4]triazolo[4,3-f]pteridinas como inhibidores de la proteina-cinasa plk1 para el tratamiento de trastornos proliferativos.
JP2009535393A (ja) 2006-05-01 2009-10-01 ファイザー・プロダクツ・インク 置換２−アミノ縮合複素環式化合物
EP2026805A1 (en) 2006-05-08 2009-02-25 Astex Therapeutics Limited Pharmaceutical combinations of diazole derivatives for cancer treatment
US7893058B2 (en) 2006-05-15 2011-02-22 Janssen Pharmaceutica Nv Imidazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases
US20070270362A1 (en) 2006-05-18 2007-11-22 The University Of Washington Methods and compositions for prevention or treatment of inflammatory-related diseases and disorders
JO3235B1 (ar) 2006-05-26 2018-03-08 Astex Therapeutics Ltd مركبات بيررولوبيريميدين و استعمالاتها
EP2035436B1 (en) 2006-06-26 2011-05-25 UCB Pharma S.A. Fused thiazole derivatives as kinase inhibitors
BRPI0716880A2 (pt) 2006-09-08 2013-10-15 Pfizer Prod Inc Síntese de 2-(piridin-2-ilamino)-pirido[2,3-d]pirimidin-7-onas
AU2007333791A1 (en) 2006-12-14 2008-06-26 Panacea Pharmaceuticals, Inc. Methods of neuroprotection by cyclin-dependent kinase inhibition
JP2010513495A (ja) 2006-12-20 2010-04-30 シェーリング コーポレイション 新規なｊｎｋ阻害剤
US20080234262A1 (en) 2007-03-21 2008-09-25 Wyeth Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors
WO2009014642A1 (en) 2007-07-19 2009-01-29 Amgen Inc. Combination of a de novo purine biosynthesis inhibitor and a cyclin dependent kinase inhibitor for the treatment of cancer
US7982035B2 (en) 2007-08-27 2011-07-19 Duquesne University Of The Holy Spirit Tricyclic compounds having antimitotic and/or antitumor activity and methods of use thereof
US7960400B2 (en) 2007-08-27 2011-06-14 Duquesne University Of The Holy Ghost Tricyclic compounds having cytostatic and/or cytotoxic activity and methods of use thereof
US9259399B2 (en) 2007-11-07 2016-02-16 Cornell University Targeting CDK4 and CDK6 in cancer therapy
CN101903396A (zh) 2007-11-07 2010-12-01 先灵公司 新的细胞周期关卡调节剂和它们与关卡激酶抑制剂的联合应用
KR20100095020A (ko) * 2007-12-19 2010-08-27 암젠 인크 세포 주기 억제제로서의 융합된 피리딘, 피리미딘 및 트리아진 화합물
US20110014191A1 (en) 2007-12-28 2011-01-20 Ipsogen Breast cancer expression profiling
AR070127A1 (es) 2008-01-11 2010-03-17 Novartis Ag Pirrolo - pirimidinas y pirrolo -piridinas
ATE531372T1 (de) 2008-04-07 2011-11-15 Amgen Inc Gem-disubstituierte und spirocyclische aminopyridine/pyrimidine als zellcyclus- inhibitoren
AU2009238590A1 (en) * 2008-04-22 2009-10-29 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
PT2688887E (pt) 2011-03-23 2015-07-06 Amgen Inc Inibidores duais tricíclicos fusionados de cdk 4/6 e flt3

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PT2688887E (pt) 2015-07-06
EP2937349B1 (en) 2016-12-28
TWI438204B (zh) 2014-05-21
EP2688887B1 (en) 2015-05-13
HK1216889A1 (zh) 2016-12-09
DK2937349T3 (da) 2017-02-20
ES2620521T3 (es) 2017-06-28
US8623885B2 (en) 2014-01-07
EP2688887A1 (en) 2014-01-29
KR20130140150A (ko) 2013-12-23
TW201302750A (zh) 2013-01-16
CA2830516C (en) 2017-01-24
CN103703000A (zh) 2014-04-02
US20140163052A1 (en) 2014-06-12
US20160368933A1 (en) 2016-12-22
HK1191014A1 (en) 2014-07-18
MY161199A (en) 2017-04-14
JP5647374B2 (ja) 2014-12-24
MX2013010871A (es) 2014-01-31
AU2012230896B9 (en) 2015-06-18
AU2012230896B2 (en) 2015-05-28
PT2937349T (pt) 2017-03-24
SG193580A1 (en) 2013-10-30
UY33969A (es) 2012-10-31
WO2012129344A1 (en) 2012-09-27
JP2014508808A (ja) 2014-04-10
KR20160035613A (ko) 2016-03-31
ES2543569T3 (es) 2015-08-20
AR085544A1 (es) 2013-10-09
CN103703000B (zh) 2015-11-25
US20120244110A1 (en) 2012-09-27
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AU2012230896A1 (en) 2013-10-03
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EP2937349A1 (en) 2015-10-28
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