PE20152033A1 - Heterociclos bicicliclos como inhibidores de fgfr - Google Patents

Heterociclos bicicliclos como inhibidores de fgfr

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Publication number
PE20152033A1
PE20152033A1 PE2015002236A PE2015002236A PE20152033A1 PE 20152033 A1 PE20152033 A1 PE 20152033A1 PE 2015002236 A PE2015002236 A PE 2015002236A PE 2015002236 A PE2015002236 A PE 2015002236A PE 20152033 A1 PE20152033 A1 PE 20152033A1
Authority
PE
Peru
Prior art keywords
heterocycles
bicycle
halo
alkyl
fgfr inhibitors
Prior art date
Application number
PE2015002236A
Other languages
English (en)
Inventor
Chunhong He
Liang Lu
Ding-Quan Qian
Yaping Sun
Jincong Zhuo
Meizhong Xu
Wenqing Yao
Fenglei Zhang
Liangxing Wu
Original Assignee
Incyte Holdings Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Incyte Holdings Corp filed Critical Incyte Holdings Corp
Publication of PE20152033A1 publication Critical patent/PE20152033A1/es

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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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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

Abstract

La presente invencion se refiere a heterociclos biciclicos de formula (I), y composiciones farmaceuticas de estos, que son inhibidores de una o mas enzimas del FGFR y son utiles en el tratamiento de enfermedades relacionadas con el FGFR, como el cancer, donde: W es R9, etc. R1 es alquilo C1-C6, etc. R2, R3 y R5 son H, halo, etc. R4 es H, halo, etc. R6 es H, halo, etc. R7 y R8 son H, alquilo C1-C6, etc.R9 es H, alquilo C1-6,etc. los compuestos preferidos son entre otros:7-amino-3- (2,6-difluoro-3,5-dimetoxifenil)-1,8-dimetil-3,4-dihidropirido [4,3-d]pirimidin-2 (1H)-ona;7-amino-3-(2,6- difluoro-3,5-dimetoxifenil)-8-etil-1-metil-3,4-dihidropirido[4,.3-d] pirimidin-2 (1H)-ona
PE2015002236A 2013-04-19 2014-04-18 Heterociclos bicicliclos como inhibidores de fgfr PE20152033A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361813782P 2013-04-19 2013-04-19

Publications (1)

Publication Number Publication Date
PE20152033A1 true PE20152033A1 (es) 2016-01-21

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PE2015002236A PE20152033A1 (es) 2013-04-19 2014-04-18 Heterociclos bicicliclos como inhibidores de fgfr

Country Status (35)

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US (5) US9533984B2 (es)
EP (2) EP3318564B1 (es)
JP (3) JP6449244B2 (es)
KR (2) KR102469849B1 (es)
CN (3) CN109912594A (es)
AR (1) AR096097A1 (es)
AU (3) AU2014253798C1 (es)
BR (1) BR112015026307B1 (es)
CA (2) CA2909207C (es)
CL (1) CL2015003089A1 (es)
CR (1) CR20150578A (es)
CY (1) CY1120556T1 (es)
DK (1) DK2986610T5 (es)
EA (2) EA035095B1 (es)
EC (1) ECSP15048555A (es)
ES (2) ES2657451T3 (es)
HK (2) HK1255159A1 (es)
HR (1) HRP20180365T2 (es)
HU (1) HUE036571T2 (es)
IL (2) IL241982B (es)
LT (1) LT2986610T (es)
ME (1) ME03015B (es)
MX (2) MX367878B (es)
MY (1) MY181497A (es)
NO (1) NO3087075T3 (es)
PE (1) PE20152033A1 (es)
PH (2) PH12015502383A1 (es)
PL (1) PL2986610T4 (es)
PT (1) PT2986610T (es)
RS (1) RS56924B9 (es)
SG (2) SG10201708520YA (es)
SI (1) SI2986610T1 (es)
TW (2) TWI649318B (es)
UA (1) UA120087C2 (es)
WO (1) WO2014172644A2 (es)

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LT2986610T (lt) 2018-04-10
AU2014253798C1 (en) 2019-02-07
AU2014253798A1 (en) 2015-10-29
CR20150578A (es) 2016-02-29
US20140315902A1 (en) 2014-10-23
PL2986610T3 (pl) 2018-05-30
BR112015026307B1 (pt) 2022-03-22
TWI649318B (zh) 2019-02-01
TW201920173A (zh) 2019-06-01
DK2986610T3 (en) 2018-02-12
NO3087075T3 (es) 2018-07-14
MX2015014683A (es) 2016-07-05
HUE036571T2 (hu) 2018-07-30
AR096097A1 (es) 2015-12-09
HRP20180365T2 (hr) 2019-06-28
ES2657451T9 (es) 2018-12-11
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