JP2014502979A5 - - Google Patents

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Publication number: JP2014502979A5
Authority: JP; Japan
Prior art keywords: alkyl; halo; substituted; aryl; cycloalkyl
Prior art date: 2012-01-19
Legal status (The legal status 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 status listed.): Granted

Application number

JP2013549707A

Other languages

English (en)

Japanese (ja)

Other versions

JP2014502979A (ja

JP6078004B2 (ja

Filing date

2012-01-19

Publication date

2015-02-26

2012-01-19 Application filed filed Critical

2012-01-19 Priority claimed from PCT/CN2012/070597 external-priority patent/WO2012097744A1/en

2014-02-06 Publication of JP2014502979A publication Critical patent/JP2014502979A/ja

2015-02-26 Publication of JP2014502979A5 publication Critical patent/JP2014502979A5/ja

2017-02-08 Application granted granted Critical

2017-02-08 Publication of JP6078004B2 publication Critical patent/JP6078004B2/ja

Status Expired - Fee Related legal-status Critical Current

2032-01-19 Anticipated expiration legal-status Critical

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125000003118 aryl group Chemical group 0.000 claims 51
125000001475 halogen functional group Chemical group 0.000 claims 47
125000000217 alkyl group Chemical group 0.000 claims 41
150000001875 compounds Chemical class 0.000 claims 38
125000000753 cycloalkyl group Chemical group 0.000 claims 34
125000001424 substituent group Chemical group 0.000 claims 22
125000001072 heteroaryl group Chemical group 0.000 claims 19
150000003839 salts Chemical class 0.000 claims 18
125000000623 heterocyclic group Chemical group 0.000 claims 15
239000003814 drug Substances 0.000 claims 6
238000004519 manufacturing process Methods 0.000 claims 6
206010020772 Hypertension Diseases 0.000 claims 4
201000009395 primary hyperaldosteronism Diseases 0.000 claims 4
208000011580 syndromic disease Diseases 0.000 claims 4
125000006163 5-membered heteroaryl group Chemical group 0.000 claims 3
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
SHIPWMSSVUHKSG-UHFFFAOYSA-N 1-[1-[3-(4-chlorophenyl)-2-hydroxy-2-methylpentan-3-yl]indazol-4-yl]-3-methylsulfonylurea Chemical compound N1=CC2=C(NC(=O)NS(C)(=O)=O)C=CC=C2N1C(C(C)(C)O)(CC)C1=CC=C(Cl)C=C1 SHIPWMSSVUHKSG-UHFFFAOYSA-N 0.000 claims 2
201000001320 Atherosclerosis Diseases 0.000 claims 2
208000024172 Cardiovascular disease Diseases 0.000 claims 2
208000016998 Conn syndrome Diseases 0.000 claims 2
206010019280 Heart failures Diseases 0.000 claims 2
206010020571 Hyperaldosteronism Diseases 0.000 claims 2
FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims 2
208000001145 Metabolic Syndrome Diseases 0.000 claims 2
206010028594 Myocardial fibrosis Diseases 0.000 claims 2
208000004880 Polyuria Diseases 0.000 claims 2
ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 claims 2
208000001647 Renal Insufficiency Diseases 0.000 claims 2
206010041277 Sodium retention Diseases 0.000 claims 2
241000209149 Zea Species 0.000 claims 2
235000005824 Zea mays ssp. parviglumis Nutrition 0.000 claims 2
235000002017 Zea mays subsp mays Nutrition 0.000 claims 2
201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 2
125000003342 alkenyl group Chemical group 0.000 claims 2
125000000304 alkynyl group Chemical group 0.000 claims 2
206010003119 arrhythmia Diseases 0.000 claims 2
230000006793 arrhythmia Effects 0.000 claims 2
150000003943 catecholamines Chemical class 0.000 claims 2
235000005822 corn Nutrition 0.000 claims 2
230000003205 diastolic effect Effects 0.000 claims 2
208000035475 disorder Diseases 0.000 claims 2
230000035619 diuresis Effects 0.000 claims 2
230000029142 excretion Effects 0.000 claims 2
201000006370 kidney failure Diseases 0.000 claims 2
239000011777 magnesium Substances 0.000 claims 2
229910052749 magnesium Inorganic materials 0.000 claims 2
208000010125 myocardial infarction Diseases 0.000 claims 2
MFVSIGTZCBDQNQ-UHFFFAOYSA-N n-[1-[1-(4-chlorophenyl)-1-(1-hydroxycyclopropyl)propyl]indol-4-yl]methanesulfonamide Chemical compound C1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(C1(O)CC1)(CC)C1=CC=C(Cl)C=C1 MFVSIGTZCBDQNQ-UHFFFAOYSA-N 0.000 claims 2
WJAQRAZQVWRUDA-UHFFFAOYSA-N n-[1-[1-(4-chlorophenyl)-1-(2-cyanocyclopropyl)propyl]indazol-4-yl]methanesulfonamide Chemical compound C=1C=C(Cl)C=CC=1C(N1C2=CC=CC(NS(C)(=O)=O)=C2C=N1)(CC)C1CC1C#N WJAQRAZQVWRUDA-UHFFFAOYSA-N 0.000 claims 2
CJPUIMBIYSFFNZ-UHFFFAOYSA-N n-[1-[1-(4-chlorophenyl)-1-(3-ethyl-1,2,4-oxadiazol-5-yl)propyl]indol-4-yl]methanesulfonamide Chemical compound CCC1=NOC(C(CC)(C=2C=CC(Cl)=CC=2)N2C3=CC=CC(NS(C)(=O)=O)=C3C=C2)=N1 CJPUIMBIYSFFNZ-UHFFFAOYSA-N 0.000 claims 2
BLEKXSOYNCRHJN-UHFFFAOYSA-N n-[1-[2-(4-chlorophenyl)-1-hydroxybutan-2-yl]-2,3-dihydroindol-4-yl]methanesulfonamide Chemical compound C1CC(C(=CC=C2)NS(C)(=O)=O)=C2N1C(CO)(CC)C1=CC=C(Cl)C=C1 BLEKXSOYNCRHJN-UHFFFAOYSA-N 0.000 claims 2
MFVGPPNQHPWGHH-UHFFFAOYSA-N n-[1-[2-(4-chlorophenyl)-1-hydroxybutan-2-yl]indazol-4-yl]methanesulfonamide Chemical compound N1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(CO)(CC)C1=CC=C(Cl)C=C1 MFVGPPNQHPWGHH-UHFFFAOYSA-N 0.000 claims 2
VAXYUCJZSOERFN-UHFFFAOYSA-N n-[1-[2-amino-3-(4-chlorophenyl)pentan-3-yl]indol-4-yl]methanesulfonamide Chemical compound C1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(C(C)N)(CC)C1=CC=C(Cl)C=C1 VAXYUCJZSOERFN-UHFFFAOYSA-N 0.000 claims 2
MPFHSFBLSWLVNH-UHFFFAOYSA-N n-[1-[3-(4-chlorophenyl)-2-hydroxypentan-3-yl]-6-fluoroindol-4-yl]methanesulfonamide Chemical compound C1=CC2=C(NS(C)(=O)=O)C=C(F)C=C2N1C(C(C)O)(CC)C1=CC=C(Cl)C=C1 MPFHSFBLSWLVNH-UHFFFAOYSA-N 0.000 claims 2
239000008194 pharmaceutical composition Substances 0.000 claims 2
239000011591 potassium Substances 0.000 claims 2
229910052700 potassium Inorganic materials 0.000 claims 2
208000013846 primary aldosteronism Diseases 0.000 claims 2
PQSUYGKTWSAVDQ-ZVIOFETBSA-N Aldosterone Chemical compound C([C@@]1([C@@H](C(=O)CO)CC[C@H]1[C@@H]1CC2)C=O)[C@H](O)[C@@H]1[C@]1(C)C2=CC(=O)CC1 PQSUYGKTWSAVDQ-ZVIOFETBSA-N 0.000 claims 1
PQSUYGKTWSAVDQ-UHFFFAOYSA-N Aldosterone Natural products C1CC2C3CCC(C(=O)CO)C3(C=O)CC(O)C2C2(C)C1=CC(=O)CC2 PQSUYGKTWSAVDQ-UHFFFAOYSA-N 0.000 claims 1
241000124008 Mammalia Species 0.000 claims 1
XKDXIJIYBQRHLO-UHFFFAOYSA-N N1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(C(C)(C)O)(CC)C1=CC=C(C(F)(F)F)C=C1 Chemical compound N1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(C(C)(C)O)(CC)C1=CC=C(C(F)(F)F)C=C1 XKDXIJIYBQRHLO-UHFFFAOYSA-N 0.000 claims 1
239000013543 active substance Substances 0.000 claims 1
229960002478 aldosterone Drugs 0.000 claims 1
201000010099 disease Diseases 0.000 claims 1
239000003937 drug carrier Substances 0.000 claims 1
230000001404 mediated effect Effects 0.000 claims 1
ACWKJSZJAGAKFW-UHFFFAOYSA-N n-[1-(1-cyano-3-phenylpentan-3-yl)-6-fluoroindazol-4-yl]methanesulfonamide Chemical compound N1=CC2=C(NS(C)(=O)=O)C=C(F)C=C2N1C(CCC#N)(CC)C1=CC=CC=C1 ACWKJSZJAGAKFW-UHFFFAOYSA-N 0.000 claims 1
KPNWZECOXIHMCY-RUDMXATFSA-N n-[1-[(e)-3-(4-chlorophenyl)-1-cyanopent-1-en-3-yl]-6-fluoroindazol-4-yl]methanesulfonamide Chemical compound N1=CC2=C(NS(C)(=O)=O)C=C(F)C=C2N1C(\C=C\C#N)(CC)C1=CC=C(Cl)C=C1 KPNWZECOXIHMCY-RUDMXATFSA-N 0.000 claims 1
YTFLEIJWHIGTBJ-UHFFFAOYSA-N n-[1-[1-cyano-3-(4-methoxyphenyl)pentan-3-yl]indol-4-yl]methanesulfonamide Chemical compound C1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(CCC#N)(CC)C1=CC=C(OC)C=C1 YTFLEIJWHIGTBJ-UHFFFAOYSA-N 0.000 claims 1
GDMIJALDCNMNQA-UHFFFAOYSA-N n-[1-[1-cyano-3-[4-(trifluoromethyl)phenyl]pentan-3-yl]indazol-4-yl]methanesulfonamide Chemical compound N1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(CCC#N)(CC)C1=CC=C(C(F)(F)F)C=C1 GDMIJALDCNMNQA-UHFFFAOYSA-N 0.000 claims 1
SGVBASQJFIRYMK-UHFFFAOYSA-N n-[1-[2-(4-chlorophenyl)-1-methoxybutan-2-yl]indol-4-yl]methanesulfonamide Chemical compound C1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(COC)(CC)C1=CC=C(Cl)C=C1 SGVBASQJFIRYMK-UHFFFAOYSA-N 0.000 claims 1
GKBSBEVPPBUZJM-UHFFFAOYSA-N n-[1-[2-hydroxy-3-[4-(trifluoromethyl)phenyl]pentan-3-yl]indazol-4-yl]methanesulfonamide Chemical compound N1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(C(C)O)(CC)C1=CC=C(C(F)(F)F)C=C1 GKBSBEVPPBUZJM-UHFFFAOYSA-N 0.000 claims 1
IJYBFZDFUPLFBM-UHFFFAOYSA-N n-[1-[3-(4-chlorophenyl)-1-cyanopentan-3-yl]-6-fluoroindol-4-yl]methanesulfonamide Chemical compound C1=CC2=C(NS(C)(=O)=O)C=C(F)C=C2N1C(CCC#N)(CC)C1=CC=C(Cl)C=C1 IJYBFZDFUPLFBM-UHFFFAOYSA-N 0.000 claims 1
MEYHTWPUOMJOCY-UHFFFAOYSA-N n-[1-[3-(4-chlorophenyl)-1-cyanopentan-3-yl]indazol-4-yl]methanesulfonamide Chemical compound N1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(CCC#N)(CC)C1=CC=C(Cl)C=C1 MEYHTWPUOMJOCY-UHFFFAOYSA-N 0.000 claims 1
YEHIJPNUIZWGGR-UHFFFAOYSA-N n-[1-[3-(4-chlorophenyl)-1-cyanopentan-3-yl]indol-4-yl]methanesulfonamide Chemical compound C1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(CCC#N)(CC)C1=CC=C(Cl)C=C1 YEHIJPNUIZWGGR-UHFFFAOYSA-N 0.000 claims 1
MEWKDHXUQFVKCB-UHFFFAOYSA-N n-[1-[3-(4-chlorophenyl)-1-hydroxypentan-3-yl]indol-4-yl]methanesulfonamide Chemical compound C1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(CCO)(CC)C1=CC=C(Cl)C=C1 MEWKDHXUQFVKCB-UHFFFAOYSA-N 0.000 claims 1
RFDLKVRSKTZRCU-UHFFFAOYSA-N n-[1-[3-(4-chlorophenyl)-2-hydroxy-2-methylpentan-3-yl]-6-fluoroindol-4-yl]methanesulfonamide Chemical compound C1=CC2=C(NS(C)(=O)=O)C=C(F)C=C2N1C(C(C)(C)O)(CC)C1=CC=C(Cl)C=C1 RFDLKVRSKTZRCU-UHFFFAOYSA-N 0.000 claims 1
XTYMFUDXUREQRD-UHFFFAOYSA-N n-[1-[3-(4-chlorophenyl)-2-hydroxy-2-methylpentan-3-yl]indazol-4-yl]methanesulfonamide Chemical compound N1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(C(C)(C)O)(CC)C1=CC=C(Cl)C=C1 XTYMFUDXUREQRD-UHFFFAOYSA-N 0.000 claims 1
JOXVIBCCAPTBEO-UHFFFAOYSA-N n-[1-[3-(4-chlorophenyl)-2-hydroxy-2-methylpentan-3-yl]indol-4-yl]methanesulfonamide Chemical compound C1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(C(C)(C)O)(CC)C1=CC=C(Cl)C=C1 JOXVIBCCAPTBEO-UHFFFAOYSA-N 0.000 claims 1
WPKHBXGUDHAVIU-UHFFFAOYSA-N n-[1-[3-(4-chlorophenyl)-2-oxopentan-3-yl]indazol-4-yl]methanesulfonamide Chemical compound N1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(C(C)=O)(CC)C1=CC=C(Cl)C=C1 WPKHBXGUDHAVIU-UHFFFAOYSA-N 0.000 claims 1
LMIREAGAYXEEGR-UHFFFAOYSA-N n-[1-[3-(4-chlorophenyl)-6-hydroxyhexan-3-yl]indol-4-yl]methanesulfonamide Chemical compound C1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(CCCO)(CC)C1=CC=C(Cl)C=C1 LMIREAGAYXEEGR-UHFFFAOYSA-N 0.000 claims 1
MQLOOLGWCJSOPP-UHFFFAOYSA-N n-[1-[3-(4-chlorophenyl)pentan-3-yl]indol-4-yl]methanesulfonamide Chemical compound C1=CC2=C(NS(C)(=O)=O)C=CC=C2N1C(CC)(CC)C1=CC=C(Cl)C=C1 MQLOOLGWCJSOPP-UHFFFAOYSA-N 0.000 claims 1
230000001575 pathological effect Effects 0.000 claims 1
230000002265 prevention Effects 0.000 claims 1
0 *C(*)(*)[n]1ncc2c1cccc2* Chemical compound *C(*)(*)[n]1ncc2c1cccc2* 0.000 description 1

JP2013549707A 2011-01-20 2012-01-19 ミネラルコルチコイド受容体拮抗薬 Expired - Fee Related JP6078004B2 (ja)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
US201161434543P	2011-01-20	2011-01-20
US61/434,543		2011-01-20
PCT/CN2012/070597 WO2012097744A1 (en)	2011-01-20	2012-01-19	Mineralocorticoid receptor antagonists

Publications (3)

Publication Number	Publication Date
JP2014502979A JP2014502979A (ja)	2014-02-06
JP2014502979A5 true JP2014502979A5 (2)	2015-02-26
JP6078004B2 JP6078004B2 (ja)	2017-02-08

Family

ID=46515166

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
JP2013549707A Expired - Fee Related JP6078004B2 (ja)	2011-01-20	2012-01-19	ミネラルコルチコイド受容体拮抗薬

Country Status (11)

Country	Link
US (2)	US8933113B2 (2)
EP (1)	EP2665707B1 (2)
JP (1)	JP6078004B2 (2)
KR (1)	KR20140009291A (2)
CN (1)	CN103384661B (2)
AU (1)	AU2012208837B2 (2)
CA (1)	CA2824344A1 (2)
ES (1)	ES2618812T3 (2)
MX (1)	MX351305B (2)
RU (1)	RU2598842C2 (2)
WO (1)	WO2012097744A1 (2)

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- 2012-01-19 CN CN201280005921.6A patent/CN103384661B/zh not_active Expired - Fee Related
- 2012-01-19 EP EP12736795.1A patent/EP2665707B1/en active Active
- 2012-01-19 AU AU2012208837A patent/AU2012208837B2/en not_active Ceased
- 2012-01-19 CA CA2824344A patent/CA2824344A1/en not_active Abandoned
- 2012-01-19 KR KR1020137019134A patent/KR20140009291A/ko not_active Ceased
- 2012-01-19 WO PCT/CN2012/070597 patent/WO2012097744A1/en not_active Ceased
- 2012-01-19 JP JP2013549707A patent/JP6078004B2/ja not_active Expired - Fee Related
- 2012-01-19 ES ES12736795.1T patent/ES2618812T3/es active Active
- 2012-01-19 MX MX2013008431A patent/MX351305B/es active IP Right Grant
- 2012-01-19 US US13/979,875 patent/US8933113B2/en active Active
2014
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