RU2493150C2 - 2,4-pyrimidine diamine compounds and use thereof - Google Patents

2,4-pyrimidine diamine compounds and use thereof Download PDF

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RU2493150C2
RU2493150C2 RU2008135563/04A RU2008135563A RU2493150C2 RU 2493150 C2 RU2493150 C2 RU 2493150C2 RU 2008135563/04 A RU2008135563/04 A RU 2008135563/04A RU 2008135563 A RU2008135563 A RU 2008135563A RU 2493150 C2 RU2493150 C2 RU 2493150C2
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Russia
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group
compound according
alkyl
heteroaryl
membered
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RU2008135563/04A
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RU2008135563A (en
Inventor
Раджиндер Сингх
Анкуш АРГАДЕ
Дональд Дж. ПЭЙАН
Сьюзан МОЛИНО
Саша Дж. ХОЛЛАНД
Джеффри КЛАФ
Холгер КАЙМ
Сомасекхар БХАМИДИПАТИ
Катрин СИЛВЭН
Хуэй Ли
Александер Б. РОССИ
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Райджел Фармасьютикалз, Инк
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Abstract

FIELD: chemistry.
SUBSTANCE: invention relates to novel of 2,4-pyrimidine diamine compounds of formula I, which inhibit degranulation of immune cells and can be used in treating cell reactions mediated by FcεRI or FcγRl receptors. In formula
Figure 00000872
(I) each R2 and R4 is independently phenyl substituted with one or more R8 groups or a heteroaryl selected from a group consisting of
Figure 00000873
, where the heteroaryl is optionally substituted with one or more R8 groups and at least one of R2 and R4 is a heteroaryl; R5 is selected from a group consisting of (C1-C6)alkyl, optionally substituted with one or more identical or different R8 groups, -ORd, -SRd, fluorine, (C1-C3)halogenalkyloxy, (C1-C3)perhalogenalkyloxy, -NRcRc, (C1-C3)halogenalkyl, -CN, -NO2, -C(O)Rd, -C(O)ORd, -C(O)NRcRc, -C(NH)NRcRc, -OC(O)Rd, -OC(O)ORd, -OC(O)NRcRc; -OC(NH)NRcRc, - [NHC(O)]nORd, R35 is hydrogen or R8; each Y is independently selected from a group consisting of O, S and NH; each Y1 is independently selected from a group consisting of O, S and NH; each Y2 is independently selected from a group consisting of CH, CH2, S, N, NH and NR37. Other values of radicals are given in the claim.
EFFECT: improved efficiency.
19 cl, 6 tbl.

Description

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The text of the description is given in facsimile form.
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Figure 00000329
Figure 00000330
Figure 00000331
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Figure 00000333
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Figure 00000569
Figure 00000570
Figure 00000571
Figure 00000572
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Figure 00000670
Figure 00000671
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Figure 00000771
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Figure 00000841
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Figure 00000846
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Figure 00000867

Claims (19)

1. Соединение формулы I:
Figure 00000868

каждый R2 и R4 независимо представляют собой фенил, замещенный одним или более R8 группами или гетероарил, выбранный из группы, состоящей из
Figure 00000869

где гетероарил необязательно замещен одной или более R8 группами и, по меньшей мере, один из R2 и R4 представляет собой гетероарил;
R5 выбран из группы, состоящей из (C1-C6)алкила, необязательно замещенного одной или более одинаковыми или разными R8 группами,
-ORd, -SRd, фтор, (C1-C3)галогеналкилокси, (C1-C3)пергалогеналкилокси,
-NRcRc, (C1-C3)галогеналкила, -CN, -NO2, -C(O)Rd, -C(O)ORd, -C(O)NRcRc, -C(NH)NRcRc, -OC(O)Rd, -OC(O)ORd, -OC(O)NRcRc; -OC(NH)NRcRc, - [NHC(O)]nORd,
R35 представляет собой водород или R8;
R8 представляет собой Re, Rb, Re, замещенные одной или более одинаковыми или разными Ra или Rb, -ORa, замещенный одной или более одинаковыми или разными Ra или
Rb, -(CH2)m-Rb, -(CHRa)m-Rb, -O-(CH2)m-Rb, -S-(CH2)m-Rb, -O-CHRaRb, -O-CRa(Rb)2,
-O-(CHRa)m-Rb, -O-(CH2)m-CH[(CH2)m-Rb]Rb, -S-(CHRa)m-Rb,
-C(O)NH-(CH2)m-Rb, -C(O)NH-(CHRa)m-Rb, -O-(CH2)m-C(O)NH-(CH2)m-Rb,
-S-(CH2)m-C(O)NH-(CH2)m-Rb,-O-(CHRa)m-C(O)NH-(CHRa)m-Rb,
-S-(CHRa)m-C(O)NH-(CHRa)m-Rb, -NH-(CH2)m-Rb, -NH-(CHRa)m-Rb,
-NH[(CH2)m-Rb], -N[(CH2)mRb]2, -NH-C(O)-NH-(CH2)m-Rb,
-NH-C(O)-(CH2)m-CHRbRb и -NH-(CH2)m-C(O)-NH-(CH2)m-Rb;
каждый Ra независимо выбран группы, состоящей из водорода, (C1-C6)алкила, (C3-C8)циклоалкила, (C4-C11)циклоалкилалкила, фенила или нафтила, (C7-C16)арилалкила, 2-6-членного гетероалкила, включающего 1-3 гетероатома, выбранных из O, S или N, 3-8-членного циклогетероалкила, включающего 1-3 гетероатома, выбранных из O, S или N, 4-11-членного циклогетероалкилалкила, включающего 1-3 гетероатома, выбранных из O, S или N, 5-10-членного гетероарила, включающего 1-3 гетероатома, выбранных из O, N или S, и 6-16-членного гетероарилалкила, где гетероарил представляет собой 5-10-членный гетероарил, включающий 1-3 гетероатома, выбранных из O, N или S;
каждый Rb представляет собой группу, независимо выбранную из группы, состоящей из =O, -ORd, (C1-C3)галогеналкилокси, -OCF3, -NRcRc,
галогена, -CF3, -CN, -NC, -C(O)ORd, -C(NOH)Ra, -OC(O)Rd, -OC(O)ORd-,
-[NHC(O)]nRd, -[NRaC(O)]nRd, - [NHC(O)]nORd, - [NRaC(O)]nORd, -[NHC(O)]nNRcRc, -[NRaC(O)]nNRcRc;
каждый Rc является независимо Ra, или, альтернативно, два Rc, взятые вместе с атомом азота, к которому они присоединены, образуют 5-8-членный циклогетероалкил, включающий 1-3 гетероатома, выбранных из O, S или N, или 5-10-членный гетероарил, включающий 1-3 гетероатома, выбранных из O, N или S, которые необязательно могут включать один или более одинаковых или разных дополнительных гетероатомов и которые необязательно могут быть замещены одним или более одинаковыми или разными Ra или Rb группами;
каждый Rd независимо является Ra;
каждый Re необязательно выбирают из группы, состоящей из (C1-C6)алкила, (C3-C8)циклоалкила, (C4-C11)циклоалкилалкила, фенила или нафтила, (C7-C16) арилалкила, 2-6-членного гетероалкила, включающего 1-3 гетероатома, выбранных из O, S или N, 3-8-членного циклогетероалкила, включающего 1-3 гетероатома, выбранных из O, S или N, 4-11-членного циклогетероалкилалкила, включающего 1-3 гетероатома, выбранных из O, S или N, 5-10-членного гетероарила, включающего 1-3 гетероатома, выбранных из O, N или S, и 6-16-членного гетероарилалкила, где гетероарил представляет собой 5-10-членный гетероарил, включающий 1-3 гетероатома, выбранных из O, N или S;
каждый Y независимо выбран из группы, состоящей из O, S и NH;
каждый Y1 независимо выбран из группы, состоящей из O, S и NH;
каждый Y2 независимо выбран из группы, состоящей из CH, CH2, S, N, NH и NR37;
R36 представляет собой водород или (C1-С6)алкил;
R37 представляет собой водород;
причем в определениях арилалкил - арил представляет собой фенил или нафтил; а алкил - (C1-С6)алкил;
каждый m независимо является целым числом от 1 до 3; и каждый n независимо является целым числом от 0 до 3.1. The compound of formula I:
Figure 00000868

each R 2 and R 4 independently represents phenyl substituted with one or more R 8 groups or heteroaryl selected from the group consisting of
Figure 00000869

wherein heteroaryl is optionally substituted with one or more R 8 groups and at least one of R 2 and R 4 is heteroaryl;
R 5 is selected from the group consisting of (C1-C6) alkyl optionally substituted with one or more identical or different R 8 groups,
-OR d , -SR d , fluoro, (C1-C3) haloalkyloxy, (C1-C3) perhaloalkyloxy,
-NR c R c , (C1-C3) haloalkyl, -CN, -NO 2 , -C (O) R d , -C (O) OR d , -C (O) NR c R c , -C (NH ) NR c R c , -OC (O) R d , -OC (O) OR d , -OC (O) NR c R c ; —OC (NH) NR c R c , - [NHC (O)] n OR d ,
R 35 represents hydrogen or R 8 ;
R 8 represents R e , R b , R e substituted by one or more identical or different R a or R b , -OR a substituted by one or more identical or different R a or
R b , - (CH 2 ) m -R b , - (CHR a ) m -R b , -O- (CH 2 ) m -R b , -S- (CH 2 ) m -R b , -O- CHR a R b , -O-CR a (R b ) 2 ,
-O- (CHR a ) m -R b , -O- (CH 2 ) m -CH [(CH 2 ) m -R b ] R b , -S- (CHR a ) m -R b ,
-C (O) NH- (CH 2 ) m -R b , -C (O) NH- (CHR a ) m -R b , -O- (CH 2 ) m -C (O) NH- (CH 2 ) m -R b ,
-S- (CH 2 ) m -C (O) NH- (CH 2 ) m -R b , -O- (CHR a ) m -C (O) NH- (CHR a ) m -R b ,
-S- (CHR a ) m -C (O) NH- (CHR a ) m -R b , -NH- (CH 2 ) m -R b , -NH- (CHR a ) m -R b ,
-NH [(CH 2 ) m -R b ], -N [(CH 2 ) m R b ] 2 , -NH-C (O) -NH- (CH 2 ) m -R b ,
-NH-C (O) - (CH 2 ) m -CHR b R b and -NH- (CH 2 ) m -C (O) -NH- (CH 2 ) m -R b ;
each R a is independently selected from the group consisting of hydrogen, (C1-C6) alkyl, (C3-C8) cycloalkyl, (C4-C11) cycloalkylalkyl, phenyl or naphthyl, (C7-C16) arylalkyl, 2-6 membered heteroalkyl, comprising 1-3 heteroatoms selected from O, S or N, a 3-8 membered cycloheteroalkyl, comprising 1-3 heteroatoms selected from O, S or N, a 4-11 membered cycloheteroalkylalkyl comprising 1-3 heteroatoms selected from O, S or N, a 5-10 membered heteroaryl comprising 1-3 heteroatoms selected from O, N or S, and a 6-16 membered heteroarylalkyl, wherein the heteroaryl is a 5-10 membered hetero aryl comprising 1-3 heteroatoms selected from O, N or S;
each R b represents a group independently selected from the group consisting of = O, -OR d , (C1-C3) haloalkyloxy, -OCF 3 , -NR c R c ,
halogen, —CF 3 , —CN, —NC, —C (O) OR d , —C (NOH) R a , —OC (O) R d , —OC (O) OR d -,
- [NHC (O)] n R d , - [NR a C (O)] n R d , - [NHC (O)] n OR d , - [NR a C (O)] n OR d , - [ NHC (O)] n NR c R c , - [NR a C (O)] n NR c R c ;
each R c is independently R a , or, alternatively, two R c , taken together with the nitrogen atom to which they are attached, form a 5-8 membered cycloheteroalkyl comprising 1-3 heteroatoms selected from O, S or N, or 5-10 membered heteroaryl, including 1-3 heteroatoms selected from O, N or S, which optionally may include one or more identical or different additional heteroatoms and which may optionally be substituted with one or more identical or different R a or R b in groups;
each R d is independently R a ;
each R e is optionally selected from the group consisting of (C1-C6) alkyl, (C3-C8) cycloalkyl, (C4-C11) cycloalkylalkyl, phenyl or naphthyl, (C7-C16) arylalkyl, 2-6 membered heteroalkyl, including 1-3 heteroatoms selected from O, S or N, a 3-8 membered cycloheteroalkyl, including 1-3 heteroatoms selected from O, S or N, a 4-11 membered cycloheteroalkylalkyl comprising 1-3 heteroatoms selected from O , S or N, a 5-10 membered heteroaryl comprising 1-3 heteroatoms selected from O, N or S, and a 6-16 membered heteroarylalkyl, wherein the heteroaryl is a 5-10 membered hetero Ryl comprising 1-3 heteroatoms selected from O, N or S;
each Y is independently selected from the group consisting of O, S, and NH;
each Y 1 is independently selected from the group consisting of O, S, and NH;
each Y 2 is independently selected from the group consisting of CH, CH 2 , S, N, NH, and NR 37 ;
R 36 represents hydrogen or (C1-C6) alkyl;
R 37 represents hydrogen;
moreover, in the definitions of arylalkyl - aryl represents phenyl or naphthyl; and alkyl is (C1-C6) alkyl;
each m is independently an integer from 1 to 3; and each n is independently an integer from 0 to 3. 2. Соединение по п.1, где гетероарил выбран из
Figure 00000870
2. The compound according to claim 1, where heteroaryl is selected from
Figure 00000870
 3. Соединение по п.1, где R2 и R4 являются одинаковыми.3. The compound according to claim 1, where R 2 and R 4 are the same. 4. Соединение по п.1, где каждый R35 независимо выбирают из группы, состоящей из водорода, -NRcRc, -(CH2)m-NRcRc, -C(O)ORd, -(CH2)m-C(O)ORd и -(CH2)m-ORd.4. The compound according to claim 1, where each R 35 is independently selected from the group consisting of hydrogen, —NR c R c , - (CH 2 ) m —NR c R c , —C (O) OR d , - (CH 2 ) m —C (O) OR d and - (CH 2 ) m —OR d . 5. Соединение по п.1, где R2 представляет собой фенил, необязательно замещенный одной, двумя или тремя R8 группами.5. The compound according to claim 1, where R 2 represents phenyl, optionally substituted by one, two or three R 8 groups. 6. Соединение по п.1, где R2 представляет собой фенил, необязательно замещенный одной или двумя R8 группами.6. The compound according to claim 1, where R 2 represents phenyl, optionally substituted by one or two R 8 groups. 7. Соединение по пп.1, 2 или 3, где R2 представляет собой тризамещенный фенил.7. The compound according to claims 1, 2 or 3, where R 2 represents trisubstituted phenyl. 8. Соединение по п.1, где R2 представляет собой фенил, замещенный одной R8 группой, выбранной из группы, состоящей из (C1-C6)алкила, -ORd, -O-(CH2)m-NRcRc, -O-C(O)ORa, -O-(CH2)m-C(O)ORa, -O-C(NH)NRcRc, -O-(CH2)m-C(NH)NRcRc, -NH-(CH2)m-NRcRc и -NH-C(O)NRcRc.8. The compound according to claim 1, where R 2 represents phenyl substituted with one R 8 group selected from the group consisting of (C1-C6) alkyl, -OR d , -O- (CH 2 ) m -NR c R c , -OC (O) OR a , -O- (CH 2 ) m -C (O) OR a , -OC (NH) NR c R c , -O- (CH 2 ) m -C (NH) NR c R c , -NH- (CH 2 ) m -NR c R c and -NH-C (O) NR c R c . 9. Соединение по п.1, где R2 представляет собой фенил, замещенный двумя R8 заместителями, выбранными из группы, состоящей из (C1-C6)алкила, -ORd, -O-(CH2)m-NRcRc, -O-C(O)ORa, -O-(CH2)m-C(O)ORa, -O-C(NH)NRcRc, -O-(CH2)m-C(NH)NRcRc, -NH-(CH2)m-NRcRc и -NH-C(O)NRcRc.9. The compound according to claim 1, where R 2 represents phenyl substituted with two R 8 substituents selected from the group consisting of (C1-C6) alkyl, -OR d , -O- (CH 2 ) m -NR c R c , -OC (O) OR a , -O- (CH 2 ) m -C (O) OR a , -OC (NH) NR c R c , -O- (CH 2 ) m -C (NH) NR c R c , -NH- (CH 2 ) m -NR c R c and -NH-C (O) NR c R c . 10. Соединение по п.1, где R2 представляет собой фенил, замещенный тремя R8 заместителями, выбранными из группы, состоящей из (C1-C6)алкила, -ORd, -O-(CH2)m-NRcRc, -O-C(O)ORa, -O-(CH2)m-C(O)ORa, -O-C(NH)NRcRc, -O-(CH2)m-C(NH)NRcRc, -NH-(CH2)m-NRcRc и -NH-C(O)NRcRc.10. The compound according to claim 1, where R 2 represents phenyl substituted with three R 8 substituents selected from the group consisting of (C1-C6) alkyl, -OR d , -O- (CH 2 ) m -NR c R c , -OC (O) OR a , -O- (CH 2 ) m -C (O) OR a , -OC (NH) NR c R c , -O- (CH 2 ) m -C (NH) NR c R c , -NH- (CH 2 ) m -NR c R c and -NH-C (O) NR c R c . 11. Соединение по п.1, где R замещен в 3-, 4- и 5-положениях.11. The compound according to claim 1, where R is substituted at the 3-, 4- and 5-positions. 12. Соединение по п.1, где R4 представляет собой фенил, необязательно замещенный одной, двумя или тремя R8 группами.12. The compound according to claim 1, where R 4 represents phenyl, optionally substituted by one, two or three R 8 groups. 13. Соединение по п.12, где R4 представляет собой фенил, замещенный в 3-положении, 4-положении, 5-положении, или их комбинации.13. The compound of claim 12, wherein R 4 is phenyl substituted at the 3-position, 4-position, 5-position, or a combination thereof. 14. Соединение по п.13, где R4 представляет собой фенил, замещенный одним R8 заместителем, выбранным из группы, состоящей из (C1-C6)алкила, -ORd, -O-(CH2)m-NRcRc, -O-C(O)ORa, -O-(CH2)m-C(O)ORa, -O-C(NH)NRcRc, -O-(CH2)m-C(NH)NRcRc, -NH-(CH2)m-NRcRc и -NH-C(O)NRcRc.14. The compound of claim 13, wherein R 4 is phenyl substituted with one R 8 with a substituent selected from the group consisting of (C1-C6) alkyl, —OR d , —O- (CH 2 ) m —NR c R c , -OC (O) OR a , -O- (CH 2 ) m -C (O) OR a , -OC (NH) NR c R c , -O- (CH 2 ) m -C (NH) NR c R c , -NH- (CH 2 ) m -NR c R c and -NH-C (O) NR c R c . 15. Соединение по п.12, где R4 представляет собой фенил, замещенный двумя R8 заместителями, выбранными из группы, состоящей из (C1-C6)алкила, -ORd, -O-(CH2)m-NRcRc, -O-C(O)ORa, -O-(CH2)m-C(O)ORa, -O-C(NH)NRcRc, -O-(CH2)m-C(NH)NRcRc, -NH-(CH2)m-NRcRc и -NH-C(O)NRcRc.15. The compound of claim 12, wherein R 4 is phenyl substituted with two R 8 substituents selected from the group consisting of (C1-C6) alkyl, —OR d , —O- (CH 2 ) m —NR c R c , -OC (O) OR a , -O- (CH 2 ) m -C (O) OR a , -OC (NH) NR c R c , -O- (CH 2 ) m -C (NH) NR c R c , -NH- (CH 2 ) m -NR c R c and -NH-C (O) NR c R c . 16. Соединение по п.12, где R4 представляет собой фенил, замещенный тремя R8 заместителями, выбранными из группы, состоящей из (C1-C6)алкил, -ORd, -O-(CH2)m-NRcRc, -O-C(O)ORa, -O-(CH2)m-C(O)ORa, -O-C(NH)NRcRc, -O-(CH2)m-C(NH)NRcRc, -NH-(CH2)m-NRcRc и -NH-C(O)NRcRc.16. The compound of claim 12, wherein R 4 is phenyl substituted with three R 8 substituents selected from the group consisting of (C1-C6) alkyl, -OR d , -O- (CH 2 ) m -NR c R c , -OC (O) OR a , -O- (CH 2 ) m -C (O) OR a , -OC (NH) NR c R c , -O- (CH 2 ) m -C (NH) NR c R c , -NH- (CH 2 ) m -NR c R c and -NH-C (O) NR c R c . 17. Соединение по п.1, где один из R2 и R4 представляет собой фенил, замещенный одной или более R8 группами, а другие R2 и R4 представляют собой гетероарильную группу
Figure 00000871
, причем гетероарильная группа необязательно замещена одной или более R8 группами.17. The compound according to claim 1, where one of R 2 and R 4 represents phenyl substituted with one or more R 8 groups, and the other R 2 and R 4 represent a heteroaryl group
Figure 00000871
wherein the heteroaryl group is optionally substituted with one or more R 8 groups. 18. Фармацевтическая композиция для ингибирования дегрануляции иммунных клеток, включающая эффективное количество соединения по любому из предшествующих пунктов и фармацевтически приемлемый носитель, разбавитель или экципиент.18. A pharmaceutical composition for inhibiting the degranulation of immune cells, comprising an effective amount of a compound according to any one of the preceding paragraphs and a pharmaceutically acceptable carrier, diluent or excipient. 19. Применение соединения по любому из пп.1-17 в лечении клеточных реакций, опосредованных FcεRI или FcγR1 - рецепторами, у животных. 19. The use of the compound according to any one of claims 1 to 17 in the treatment of cellular reactions mediated by FcεRI or FcγR1 receptors in animals.
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