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NZ775003B2 - Fused ring compounds - Google Patents
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NZ775003B2 - Fused ring compounds - Google Patents

Fused ring compounds Download PDF

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Publication number
NZ775003B2
NZ775003B2 NZ775003A NZ77500319A NZ775003B2 NZ 775003 B2 NZ775003 B2 NZ 775003B2 NZ 775003 A NZ775003 A NZ 775003A NZ 77500319 A NZ77500319 A NZ 77500319A NZ 775003 B2 NZ775003 B2 NZ 775003B2
Authority
NZ
New Zealand
Prior art keywords
compound
acceptable salt
pharmaceutically acceptable
halo
group
Prior art date
Application number
NZ775003A
Other versions
NZ775003A (en
Inventor
Steven Do
Sushant Malhotra
Jack Terrett
Jianfeng Xin
Original Assignee
F Hoffmann La Roche Ag
Filing date
Publication date
Application filed by F Hoffmann La Roche Ag filed Critical F Hoffmann La Roche Ag
Priority claimed from PCT/US2019/060578 external-priority patent/WO2020097537A2/en
Publication of NZ775003A publication Critical patent/NZ775003A/en
Publication of NZ775003B2 publication Critical patent/NZ775003B2/en

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems

Abstract

This invention pertains to fused ring compounds of Formula (II), as further detailed herein, which are used for the inhibition of Ras proteins, as well as compositions comprising these compounds and methods of treatment by their administration.

Claims (16)

1. A compound of Formula (II): or a pharmaceutically acceptable salt thereof; wherein, R is NH ; R is H; R is H or C alkyl; 4 1-6 R is CF ; R is selected from the group consisting of H, cyano, and halo; R and R are each independently selected from the group consisting of H, C alkyl, 8 9 1-6 C haloalkyl, C hydroxyalkyl, cyano, and halo; wherein C alkyl is optionally substituted 1-6 1-6 1-6 with one substituent selected from the group consisting of: methanesulfonyl (mesyl), p- toluenesulfonyl (tosyl), an alkyl or aryl sulfonate leaving group, C alkanoylamino, C 1-6 1-6 alkoxy, C alkylamino, C alkylsulfonylamino, C dialkylamino, and C haloalkoxy; 1-6 1-6 6-12 1-6 X is piperazinyl optionally substituted with 1 to 4 substituents, wherein each substituent is independently selected from the group consisting of cyano, C alkyl, C cyanoalkyl, and 1-6 1-6 C haloalkyl; Y is , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , U is C(R ), wherein R is H; 6a 6a V is C(R ), wherein R is H or halo; 6b 6b W is C(R ), wherein R is H or halo ; 6c 6c n is 0.
2. The compound or pharmaceutically acceptable salt thereof of claim 1, wherein X , , , , , , , , , , , , , or .
3. The compound of claim 1 or 2, or pharmaceutically acceptable salt thereof, wherein Y is or .
4. The compound of claim 1, having Formula (IV): or a pharmaceutically acceptable salt thereof; wherein, R is , , , , or ; X is , , , , , , , , , , , , , or Y is or ; U is C(R ), wherein R is H; 6a 6a V is C(R ), wherein R is H or halo; 6b 6b W is C(R ), wherein R is H or halo; 6c 6c n is 0; and R is selected from the group consisting of: , , , , , , , and , .
5. The compound of claim 4, or a pharmaceutically acceptable salt thereof, wherein R is , or .
6. The compound of claim 4, or a pharmaceutically acceptable salt thereof, wherein R is .
7. The compound of any one of claims 4-6, or a pharmaceutically acceptable salt thereof, wherein R is , , or .
8. The compound of any one of claims 4-7, or a pharmaceutically acceptable salt thereof, wherein R is
9. The compound of any one of claims 4-6, or a pharmaceutically acceptable salt thereof, wherein R11 is , , or .
10. The compound of any one of claims 1-9, or a pharmaceutically acceptable salt thereof, wherein R is halo.
11. The compound of any one of claims 1-9, or a pharmaceutically acceptable salt thereof, wherein R is hydrogen.
12. The compound of any one of claims 1-11, or a pharmaceutically acceptable salt thereof, wherein R is halo.
13. The compound of any one of claims 1-12, or a pharmaceutically acceptable salt thereof, wherein X is , , or .
14. The compound of claim 1 having a Formula : (Ia); (Ib); (Ic); (Ih); or (Il), or a pharmaceutically acceptable salt thereof.
15. The compound of claim 1 or 4 having formula: (IVa); (IVb); (IVc); (IVd); or (IVg), or a pharmaceutcially acceptable salt thereof.
16. The compound of claim 1, having formula: °Y^ °Y^ °Y^ Cl Cl Cl N^O N^O N^O h2n. .n h2n. .n h2n^ ^n. 5^ V' V' / / / 'CF3 'CF3 'CF3 , , , O^Y^^F QY^^f Cl Cl Cl N^O N^O N^O H2N. .N, H2Nv.N H2Nv-N s"'.. >. S"'.. F F N—' F N^y / / / CF3 cf3 cf3 , , , . ^Nk ^ ,N-. f^fci fJ1 Cl N^O F s"'.. NH2 nh2 nh2 , , , QY'^k F^VN> F FCI nh2 nh2 nh2 , , , fJ^ci F. Cl N r n H2N. .N Or* L> nh2 nh2 , , , / <-J ¦Z Z— C _j~i. o z—i' z /--- \ •z z—(/ z z z^/ LK •z z z Z—<' z o o N—/ \\ /“V \\ /r^ o jr% o z \ \ LL \ \ LL- •z Z—v / \ K K z z-(/ z ^ W5 ¦z z-!/ Z Z—v z \\ ^“V \\ //^v LL? LjCO o zr^ X X X , , , , , HzN^N. CF3 / Cl r n H2N. .N h2n_n •s: / ¦cf3 / h2n^n HjN^N n^Xqy":. r>0Et ¦CF3 ¦CF3 Cl Cl H2N N. h2n_n y"'-. ¦cf3 ‘CF3 h2n^n. CX0X h2n M N*...O oCfF O N N~V ¦CF3 / CF3 , , , Cl Cl h2n
NZ775003A 2019-11-08 Fused ring compounds NZ775003B2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2018114788 2018-11-09
PCT/US2019/060578 WO2020097537A2 (en) 2018-11-09 2019-11-08 Fused ring compounds

Publications (2)

Publication Number Publication Date
NZ775003A NZ775003A (en) 2024-07-05
NZ775003B2 true NZ775003B2 (en) 2024-10-08

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