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HRP20241768T1 - Heterociklički spoj - Google Patents

Heterociklički spoj Download PDF

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Publication number
HRP20241768T1
HRP20241768T1 HRP20241768TT HRP20241768T HRP20241768T1 HR P20241768 T1 HRP20241768 T1 HR P20241768T1 HR P20241768T T HRP20241768T T HR P20241768TT HR P20241768 T HRP20241768 T HR P20241768T HR P20241768 T1 HRP20241768 T1 HR P20241768T1
Authority
HR
Croatia
Prior art keywords
atom
optionally substituted
group optionally
carbon atom
hydroxy groups
Prior art date
Application number
HRP20241768TT
Other languages
English (en)
Inventor
Jun Fujimoto
Xin Liu
Osamu Kurasawa
Terufumi Takagi
Douglas Robert CARY
Hiroshi Banno
Yasutomi Asano
Takuto Kojima
Original Assignee
Takeda Pharmaceutical Company Limited
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 Takeda Pharmaceutical Company Limited filed Critical Takeda Pharmaceutical Company Limited
Publication of HRP20241768T1 publication Critical patent/HRP20241768T1/hr

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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
    • A61K31/437—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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • 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
    • A61K31/4406—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
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    • 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
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
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    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • 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
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    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/42—Radicals substituted by singly-bound nitrogen atoms having hetero atoms attached to the substituent nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/65—One oxygen atom attached in position 3 or 5
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D213/68—One oxygen atom attached in position 4
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/73—Unsubstituted amino or imino radicals
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    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
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    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
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Claims (12)

1. Spoj, naznačen time, da je predstavljen formulom (I): [image] u kojoj prsten A ima formulu: [image] pri čemu kombinacija od X1, X2 i X3 (X1, X2, X3) je (atom ugljika, atom ugljika, atom ugljika) ili (atom ugljika, atom ugljika, atom dušika); R1 je (1) atom klora, atom broma, (2) metil, trifluorometil, ili (3) hidroksi skupina supstituirana s metilom ili trifluorometilom; R2 je (1) atom halogena, (2) C1-6 alkil skupina opcionalno supstituirana s 1 do 3 supstituenta odabrana od atoma halogena i hidroksi skupine, ili (3) C1-6 alkoksi skupina opcionalno supstituirana s 1 do 3 atoma halogena; prsten B je opcionalno dalje supstituiran s 1 do 3 supstituenta odabrana od (1) atoma halogena i (2) C1-6 alkil skupine opcionalno supstituirane s 1 do 3 hidroksi skupine; X6 je atom vodika, atom fluora ili atom klora; X7 je atom fluora ili atom klora; kombinacija od X8 i X9 (X8, X9) je (atom ugljika, atom dušika), (atom dušika, atom ugljika), ili (atom dušika, atom dušika); prsten E je opcionalno dalje supstituiran s 1 do 3 C1-6 alkil skupine; i X10 je amino skupina opcionalno supstituirana s 1 - 2 supstituenta odabrana od (1) C1-6 alkil skupine opcionalno supstituirane s 1 do 3 hidroksi skupine, (2) C3-10 cikloalkil skupine opcionalno supstituirane s 1 do 3 hidroksi skupine, i (3) 3-14-člane nearomatske heterocikličke skupine; ili njegova sol.
2. Spoj prema patentnom zahtjevu 1, naznačen time, da prsten A ima formulu: [image] pri čemu kombinacija od X1, X2 i X3 (X1, X2, X3) je (atom ugljika, atom ugljika, atom ugljika) ili (atom ugljika, atom ugljika, atom dušika); R1 je (1) atom klora, atom broma, (2) metil, trifluorometil, ili (3) hidroksi skupina supstituirana s metilom ili trifluorometilom; R2 je (1) atom halogena, (2) C1-6 alkil skupina opcionalno supstituirana s 1 do 3 supstituenta odabrana od atoma halogena i hidroksi skupine, ili (3) C1-6 alkoksi skupina opcionalno supstituirana s 1 do 3 atoma halogena; prsten B je opcionalno dalje supstituiran s 1 do 3 supstituenta odabrana od (1) atoma halogena i (2) C1-6 alkil skupine opcionalno supstituirane s 1 do 3 hidroksi skupine; X6 je atom vodika, atom fluora ili atom klora; X7 je atom fluora ili atom klora; kombinacija od X8 i X9 (X8, X9) je (atom ugljika, atom dušika), (atom dušika, atom ugljika), ili (atom dušika, atom dušika); prsten E je opcionalno dalje supstituiran s 1 do 3 C1-6 alkil skupine; i X10 je amino skupina opcionalno supstituirana s 1 - 2 supstituenta odabrana od (1) C1-6 alkil skupine opcionalno supstituirane s 1 do 3 hidroksi skupine, (2) C3-10 cikloalkil skupine opcionalno supstituirane s 1 do 3 hidroksi skupine, i (3) 3-14-člane nearomatske heterocikličke skupine; ili njegova sol, uz uvjet da prsten B je dalje supstituiran s 1 do 3 supstituenta odabrana od (1) atoma halogena i (2) C1-6 alkil skupine opcionalno supstituirane s 1 do 3 hidroksi skupine, kada 1) X1, X2 i X3 (X1, X2, X3) je (atom ugljika, atom ugljika, atom ugljika) i 2) X9 i X10 su spojeni jedan za drugoga da tvore 5-14-člani aromatski heterocikl.
3. Spoj prema patentnom zahtjevu 1, naznačen time, da prsten A ima formulu: [image] pri čemu kombinacija od X1, X2 i X3 (X1, X2, X3) je (atom ugljika, atom ugljika, atom ugljika) ili (atom ugljika, atom ugljika, atom dušika); R1 je (1) atom klora, atom broma, (2) metil, trifluorometil, ili (3) hidroksi skupina supstituirana s metilom ili trifluorometilom; R2 je (1) atom halogena, (2) C1-6 alkil skupina opcionalno supstituirana s 1 do 3 supstituenta odabrana od atoma halogena i hidroksi skupine, ili (3) C1-6 alkoksi skupina opcionalno supstituirana s 1 do 3 atoma halogena; prsten B je opcionalno dalje supstituiran s 1 do 3 supstituenta odabrana od (1) atoma halogena i (2) C1-6 alkil skupine opcionalno supstituirane s 1 do 3 hidroksi skupine; X6 je atom vodika, atom fluora ili atom klora; X7 je atom fluora ili atom klora; kombinacija od X8 i X9 (X8, X9) je (atom ugljika, atom dušika); prsten E je opcionalno dalje supstituiran s 1 do 3 C1-6 alkil skupine; i X10 je amino skupina opcionalno supstituirana s 1 - 2 supstituenta odabrana od (1) C1-6 alkil skupine opcionalno supstituirane s 1 do 3 hidroksi skupine, (2) C3-10 cikloalkil skupine opcionalno supstituirane s 1 do 3 hidroksi skupine, i (3) 3-14-člane nearomatske heterocikličke skupine; ili njegova sol.
4. Spoj prema patentnom zahtjevu 1, naznačen time, da prsten A ima formulu: [image] pri čemu kombinacija od X1, X2 i X3 (X1, X2, X3) je (atom ugljika, atom ugljika, atom ugljika); R1 je (1) atom klora, atom broma, (2) metil, trifluorometil, ili (3) hidroksi skupina supstituirana s metilom ili trifluorometilom; R2 je (1) atom halogena, (2) C1-6 alkil skupina opcionalno supstituirana s 1 do 3 supstituenta odabrana od atoma halogena i hidroksi skupine, ili (3) C1-6 alkoksi skupina opcionalno supstituirana s 1 do 3 atoma halogena; prsten B je opcionalno dalje supstituiran s 1 do 3 supstituenta odabrana od (1) atoma halogena i (2) C1-6 alkil skupine opcionalno supstituirane s 1 do 3 hidroksi skupine; X6 je atom vodika, atom fluora ili atom klora; X7 je atom fluora ili atom klora; kombinacija od X8 i X9 (X8, X9) je (atom ugljika, atom dušika); prsten E je opcionalno dalje supstituiran s 1 do 3 C1-6 alkil skupine; i X10 je amino skupina opcionalno supstituirana s 1 - 2 supstituenta odabrana od (1) C1-6 alkil skupine opcionalno supstituirane s 1 do 3 hidroksi skupine, (2) C3-10 cikloalkil skupine opcionalno supstituirane s 1 do 3 hidroksi skupine, i (3) 3-14-člane nearomatske heterocikličke skupine; ili njegova sol.
5. Spoj prema patentnom zahtjevu 1, naznačen time, da prsten A ima formulu: [image] pri čemu kombinacija od X1, X2 i X3 (X1, X2, X3) je (atom ugljika, atom ugljika, atom dušika); R1 je (1) atom klora, atom broma, (2) metil, trifluorometil, ili (3) hidroksi skupina supstituirana s metilom ili trifluorometilom; R2 je (1) atom halogena, (2) C1-6 alkil skupina opcionalno supstituirana s 1 do 3 supstituenta odabrana od atoma halogena i hidroksi skupine, ili (3) C1-6 alkoksi skupina opcionalno supstituirana s 1 do 3 atoma halogena; prsten B je opcionalno dalje supstituiran s 1 do 3 supstituenta odabrana od (1) atoma halogena i (2) C1-6 alkil skupine opcionalno supstituirane s 1 do 3 hidroksi skupine; X6 je atom vodika, atom fluora ili atom klora; X7 je atom fluora ili atom klora; kombinacija od X8 i X9 (X8, X9) je (atom ugljika, atom dušika); prsten E je opcionalno dalje supstituiran s 1 do 3 C1-6 alkil skupine; i X10 je amino skupina opcionalno supstituirana s 1 - 2 supstituenta odabrana od (1) C1-6 alkil skupine opcionalno supstituirane s 1 do 3 hidroksi skupine, (2) C3-10 cikloalkil skupine opcionalno supstituirane s 1 do 3 hidroksi skupine, i (3) 3-14-člane nearomatske heterocikličke skupine; ili njegova sol.
6. Spoj prema patentnom zahtjevu 1, naznačen time, da je N-(3-((2-aminopirimidin-5-il)etinil)-2,4-difluorofenil)-5-kloro-2-metoksipiridin-3-sulfonamid ili njegova sol.
7. Spoj prema patentnom zahtjevu 1, naznačen time, da je 5-kloro-N-(2,4-difluoro-3-((2-((trans-4-hidroksicikloheksil)amino)pirimidin-5-il)etinil)fenil)-2-metoksipiridin-3-sulfonamid ili njegova sol.
8. Spoj prema patentnom zahtjevu 1, naznačen time, da je 2,5-dikloro-N-(2,4-difluoro-3-((2-(((2R)-1-hidroksipropan-2-il)amino)pirimidin-5-il)etinil)fenil)-3-(hidroksimetil)benzensulfonamid ili njegova sol.
9. Lijek, naznačen time, da sadrži spoj prema patentnom zahtjevu 1, ili njegovu sol.
10. Lijek prema patentnom zahtjevu 9, naznačen time, da je to profilaktičko ili terapeutsko sredstvo kod raka.
11. Uporaba spoja prema patentnom zahtjevu 1, ili njegove soli, naznačena time, da je za proizvodnju profilaktičkog ili terapeutskog sredstva za rak.
12. Spoj spoja prema patentnom zahtjevu 1, ili njegova sol, naznačen time, da je za uporabu u profilaksi ili liječenju raka.
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