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Cyp11b, cyp17, and/or cyp21 inhibitors

A technology of heteroaryl compounds, applied in the field of C-17-heteroaryl steroid compounds as CYP11B, CYP17 and/or CYP21 inhibitors, can solve problems such as toxicity

Inactive Publication Date: 2013-09-04
BIOMARIN PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Reasons that such non-specific activity is believed to be responsible for the clinically significant toxicity of these drugs

Method used

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  • Cyp11b, cyp17, and/or cyp21 inhibitors
  • Cyp11b, cyp17, and/or cyp21 inhibitors
  • Cyp11b, cyp17, and/or cyp21 inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0210] Example 1: In another example, compounds of formula (Z) having the structure of formula (I) are disclosed:

[0211]

[0212] in For -CH-CH=CH-, -C=CH-CH 2 -, -CH-CH 2 -CH 2 -, -CH-CH(OH)-CH 2 -, -CH-C(O)CH 2 -,or

[0213] each are independently single or double bonds;

[0214] A is composed of 1, 2, 3 or 4 R as the case may be 4 Substituted heteroaryl;

[0215] Each R 4 When present, independently selected from halo, cyano, hydroxy, alkoxy, alkyl, alkenyl, haloalkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C(O)R 13a , alkoxycarbonyl, -C(O)NR A R B , -NR 13 S(O) 2 R 13a , -NR 13a C(O)R 13a and -NR A R B composed of groups;

[0216] R A and R B independently selected from the group consisting of hydrogen, alkyl, haloalkyl, alkoxyalkyl, cycloalkyl, aryl, arylalkyl, heteroaryl and heteroarylalkyl; or

[0217] R A and R B Together with the nitrogen atom, a 4- to 7-membered heterocyclic ring having one or two heteroatoms is formed;

[02...

Embodiment 1a

[0230] Example 1a: Compounds of Formula I conform to Formula IH

[0231]

[0232] in

[0233] Q 2 for CH 2 , CH(OH) or C(O);

[0234] D is (CH 2 ) d , where d is an integer from 1 to 3;

[0235] E for CH 2 、CR 14 R 14a , O, NR 1 , N-COR 1 , N-S(O) 0-2 (Alkyl) or N-COOR 1 ;

[0236] G is CH(CH 3 ), C(CH 3 ) 2 or (CH 2 ) e , where e is an integer from 1 to 3,

[0237] The restriction is that when E is CH 2 And when d+e is 3, then A is not unsubstituted furyl, unsubstituted thienyl, oxadiazolyl substituted by alkyl or phenyl or thiadiazolyl substituted by alkyl;

[0238] A is composed of 1, 2, 3 or 4 R as the case may be 4 Substituted heteroaryl;

[0239] Each R 1 independently selected from the group consisting of hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, alkoxyalkyl, hydroxy and haloalkoxyalkyl; wherein alkyl, cycloalkyl, alkenyl, alkynyl , alkoxyalkyl and haloalkoxyalkyl optionally consist of 1, 2 or 3 independently selected from halo, alkyl, al...

Embodiment 1f

[0255] Example 1f: Compounds of formula I conform to formula IJ

[0256]

[0257] in

[0258] D is (CH 2 ) d , where d is an integer from 1 to 3;

[0259] E for CH 2 、CR 14 R 14a , O, NR 1 , N-COR 1 , N-S(O) 0-2 (Alkyl) or N-COOR 1 ;

[0260] G is CH(CH 3 ), C(CH 3 ) 2 or (CH 2 ) e , where e is an integer from 1 to 3,

[0261] The restriction is that when E is CH 2 And when d+e is 3, then A is not unsubstituted furyl, unsubstituted thienyl, oxadiazolyl substituted by alkyl or phenyl or thiadiazolyl substituted by alkyl;

[0262] A is composed of 1, 2, 3 or 4 R as the case may be 4 Substituted heteroaryl;

[0263] Each R 1 independently selected from the group consisting of hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, alkoxyalkyl, hydroxy and haloalkoxyalkyl; wherein alkyl, cycloalkyl, alkenyl, alkynyl , alkoxyalkyl and haloalkoxyalkyl optionally consist of 1, 2 or 3 independently selected from halo, alkyl, alkenyl, aryl, heteroaryl, alkoxy, alkoxycarb...

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PUM

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Abstract

Provided herein are inhibitors of CYP11B, CYP17, and / or CYP21 enzymes of Formula (Z), (IX), (X), (XI), (XII), (XIII), (XIV), (XV), (XVI), or (XVII). Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat androgen-dependent diseases, disorders and conditions. Formula (Z).

Description

technical field [0001] Described herein are compounds, methods of making the compounds, pharmaceutical compositions and medicaments containing the compounds, and methods of using the compounds to treat androgen-dependent diseases or conditions. Background technique [0002] 17α-Hydroxylase / C 17-20 The lyase complex is essential for androgen biosynthesis. CYP17 is a bifunctional enzyme with C 17,20 - Lyase activity and C17-hydroxylase activity. These two alternating enzymatic activities of CYP17 lead to the formation of severely distinct intermediates in steroid biosynthesis, and each activity appears to be regulated differently and is developmentally regulated. [0003] In the testes and adrenal glands, the final step in testosterone biosynthesis involves two key reactions that occur sequentially and are both mediated by a single enzyme (cytochrome 6P450 monooxygenase 17α-hydroxylase / C 17,20 - Lyase (P450 17 or CYP17)) catalyzed. CYP17 is a key enzyme in androgen biosy...

Claims

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Application Information

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IPC IPC(8): C07D401/08C07D403/08C07D405/08C07D413/08C07D471/04C07J43/00C07J61/00C07J63/00C07J73/00A61P5/26A61P5/42A61P5/46A61P35/00A61K31/56
CPCC07D401/08C07D403/08C07D405/08C07D413/08C07D471/04C07J43/003C07J61/00C07J1/0011C07J13/005C07J21/005C07J31/006C07J73/003C07J63/002C07J73/005C07J73/008A61P13/08A61P15/08A61P17/00A61P17/14A61P35/00A61P35/02A61P43/00A61P5/26A61P5/28A61P5/42A61P5/46
Inventor 朱添和王兵叶涛
Owner BIOMARIN PHARMA INC
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