JP2006525944A5 - - Google Patents
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- JP2006525944A5 JP2006525944A5 JP2004570427A JP2004570427A JP2006525944A5 JP 2006525944 A5 JP2006525944 A5 JP 2006525944A5 JP 2004570427 A JP2004570427 A JP 2004570427A JP 2004570427 A JP2004570427 A JP 2004570427A JP 2006525944 A5 JP2006525944 A5 JP 2006525944A5
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- Prior art keywords
- alkyl
- pharmaceutically acceptable
- acceptable salt
- compound
- compound according
- Prior art date
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- 125000000217 alkyl group Chemical group 0.000 claims 36
- 150000003839 salts Chemical class 0.000 claims 25
- 239000011780 sodium chloride Substances 0.000 claims 25
- 150000001875 compounds Chemical class 0.000 claims 23
- 239000008194 pharmaceutical composition Substances 0.000 claims 10
- 239000000203 mixture Substances 0.000 claims 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
- 239000002111 antiemetic agent Substances 0.000 claims 6
- 229940121367 non-opioid analgesics Drugs 0.000 claims 6
- 239000000014 opioid analgesic Substances 0.000 claims 6
- 125000005428 anthryl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C3C(*)=C([H])C([H])=C([H])C3=C([H])C2=C1[H] 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 125000001624 naphthyl group Chemical group 0.000 claims 5
- 125000005561 phenanthryl group Chemical group 0.000 claims 5
- -1 -C 3 -C 8 cycloalkyl Chemical group 0.000 claims 4
- 125000002947 alkylene group Chemical group 0.000 claims 4
- 230000003474 anti-emetic Effects 0.000 claims 4
- 239000003793 antidiarrheal agent Substances 0.000 claims 4
- 102000003840 Opioid Receptors Human genes 0.000 claims 3
- 108090000137 Opioid Receptors Proteins 0.000 claims 3
- 206010012735 Diarrhoea Diseases 0.000 claims 2
- 201000008286 diarrhea Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 230000004936 stimulating Effects 0.000 claims 2
- 239000000969 carrier Substances 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 108090001120 delta Opioid Receptors Proteins 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229940079593 drugs Drugs 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 102000029985 nociceptin receptor Human genes 0.000 claims 1
- 108010020615 nociceptin receptor Proteins 0.000 claims 1
- 239000000546 pharmaceutic aid Substances 0.000 claims 1
- 102000005962 receptors Human genes 0.000 claims 1
- 108020003175 receptors Proteins 0.000 claims 1
- 102000037229 δ-opioid receptors Human genes 0.000 claims 1
- 102000037289 κ-opioid receptors Human genes 0.000 claims 1
- 108020001588 κ-opioid receptors Proteins 0.000 claims 1
- 102000037275 μ-opioid receptors Human genes 0.000 claims 1
- 108020001612 μ-opioid receptors Proteins 0.000 claims 1
Claims (35)
- 下記式(Ia)又は(Ib):
Ar1は、−C3〜C8シクロアルキル、フェニル、ナフチル、アントリル、フェナントリル又は−(5員〜7員)ヘテロアリール(これらは、各々、非置換であるか、1又はそれ以上のR2基で置換されている)であり;
Ar2は、フェニル、ナフチル、アントリル、フェナントリル又は−(5員〜7員)ヘテロアリール(これらは、各々、非置換であるか、1又はそれ以上のR2基で置換されている)であり;
Gは、−H、−L−(CH2)nCO2R4、−L−(CH2)nR5、−(C1〜C5アルキレン)CO2R4、又は−(C1〜C5アルキレン)R5であり;
L=−C(O)−、−SO2−又は−SO−;
R1=−H、−C(O)NH2、−C(O)NHOH、−CO2R4、−CHO、−CN、−(C1〜C4アルキル)、−C(O)NH(C1〜C4アルキル)、−C(O)N(C1〜C4アルキル)2、
R4=−H、−C1〜C10アルキル、−CH2O(C1〜C4アルキル)、−CH2N(C1〜C4アルキル)2、又は−CH2NH(C1〜C4アルキル);
R5=−NH2、−NHSO2R4、−C(O)NH2、−C(O)NHOH、−SO2NH2、−C(O)NH(C1〜C4アルキル)、−C(O)N(C1〜C4アルキル)2、−SO2NH(C1〜C4アルキル)、−SO2N(C1〜C4アルキル)2、−H、−OH、−CN、−C3〜C8シクロアルキル、フェニル、ナフチル、アントリル、フェナントリル、又は−(5員〜7員)ヘテロアリール(これらは、各々、非置換であるか、1又はそれ以上のR2基で置換されている);
m=0から4の範囲の整数;
n=1から4の範囲の整数;
p=0又は1;
q=0から3の範囲の整数;
r=1から6の範囲の整数)
の化合物又はその薬学的に許容される塩。 - 下記式(Ic)又は(Id):
Ar3は、フェニル、ナフチル、アントリル、フェナントリル又は−(5員〜7員)ヘテロアリール(これらは、各々、非置換であるか、1又はそれ以上のR2基で置換されている)であり;
G=−H、−L(CH2)nC(O)OR4、−L(CH2)nR5、−(C1〜C5アルキレン)COOR4、又は−(C1〜C5アルキレン)R5;
L=−C(O)−、−SO2−、又は−SO−;
R1=−H、−C(O)NH2、−C(O)NHOH、−CO2R4、−CHO、−CN、−(C1〜C4アルキル)、−C(O)NH(C1〜C4アルキル)、−C(O)N(C1〜C4アルキル)2、
R4=−H、−C1〜C10アルキル、−CH2O(C1〜C4アルキル)、−CH2N(C1〜C4アルキル)2、又は−CH2NH(C1〜C4アルキル);
R5=−NH2、−NHSO2R4、−C(O)NH2、−C(O)NHOH、−SO2NH2、−C(O)NH(C1〜C4アルキル)、−C(O)N(C1〜C4アルキル)2、−SO2NH(C1〜C4アルキル)、−SO2N(C1〜C4アルキル)2、−H、−OH、−CN、−C3〜C8シクロアルキル、フェニル、ナフチル、アントリル、フェナントリル、又は−(5員〜7員)ヘテロアリール(これらは、各々、非置換であるか、1又はそれ以上のR2基で置換されている);
m=0から4の範囲の整数;
n=1から4の範囲の整数;
p=0又は1;
q=0から3の範囲の整数;
r=1から6の範囲の整数)
の化合物又はその薬学的に許容される塩。 - Ar1及びAr2がフェニルである、請求項1に記載の化合物又はその化合物の薬学的に許容される塩。
- Ar3がフェニルである、請求項2に記載の化合物又はその化合物の薬学的に許容される塩。
- m=1及びG=Hである請求項1又は2に記載の化合物又はその化合物の薬学的に許容される塩。
- R1が−C(O)NH2、−C(O)NH(C1〜C4アルキル)、−C(O)N(C1〜C4アルキル)(C1〜C4アルキル)又は−CNである、請求項1又は2に記載の化合物又はその化合物の薬学的に許容される塩。
- p=0及びq=0である、請求項1又は2に記載の化合物又はその化合物の薬学的に許容される塩。
- G=−(CH2)2NHSO2H、−CH2C(O)NH2、−CH2C(O)NH(C1〜C4アルキル)、−CH2C(O)N(C1〜C4アルキル)(C1〜C4アルキル)、−(CH2)2C(O)OCH2CH3又は−(CH2)4C(O)OCH2CH3である、請求項1又は2に記載の化合物又はその化合物の薬学的に許容される塩。
- p=1である、請求項1又は2に記載の化合物又はその化合物の薬学的に許容される塩。
- 有効量の請求項1又は2に記載の化合物又はその化合物の薬学的に許容される塩、及び薬学的に許容される担体又は賦形剤を含む組成物。
- オピオイド鎮痛薬、非オピオイド鎮痛薬又は制吐薬を更に含む、請求項10に記載の組成物。
- 請求項1又は2に記載の化合物又はその化合物の薬学的に許容される塩を含む、動物における疼痛を治療するための医薬組成物。
- 有効量のオピオイド鎮痛薬、非オピオイド鎮痛薬又は制吐薬を更に含む、請求項12に記載の医薬組成物。
- 請求項1又は2に記載の化合物又はその化合物の薬学的に許容される塩を含む、細胞におけるオピオイド受容体機能を刺激するための薬剤。
- 請求項1又は2に記載の化合物又はその化合物の薬学的に許容される塩を含む、動物における下痢を治療するための医薬組成物。
- 有効量のオピオイド鎮痛薬、非オピオイド鎮痛薬又は制吐薬を更に含む、請求項15に記載の医薬組成物。
- オピオイド受容体を発現することができる細胞と有効量の請求項1又は2に記載の化合物又はその化合物の薬学的に許容される塩とを接触させることを含む、細胞におけるオピオイド受容体機能をin vitroで刺激するための方法。
- 前記受容体がκ−オピオイド受容体、μ−オピオイド受容体、δ−オピオイド受容体又はORL−1受容体である、請求項17に記載の方法。
- 請求項1又は2に記載の化合物又はその化合物の薬学的に許容される塩と、薬学的に許容される担体又は賦形剤とを混合することを含む、組成物の調製方法。
- 請求項10に記載の組成物、請求項12若しくは15に記載の医薬組成物又は請求項14に記載の薬剤を収容した容器を含むキット。
- 下痢止め薬を更に含む、請求項10に記載の組成物、請求項12若しくは15に記載の医薬組成物又は請求項14に記載の薬剤。
- 下記式:
- 下記式:
- 下記式:
- 下記式:
- 下記式:
- 下記式:
- 下記式:
- 有効量の請求項24に記載の化合物又はその化合物の薬学的に許容される塩を含む組成物。
- オピオイド鎮痛薬、非オピオイド鎮痛薬、制吐薬又は下痢止め薬を更に含む、請求項29に記載の組成物。
- 請求項24に記載の化合物又はその化合物の薬学的に許容される塩を含む、動物における疼痛を治療するための医薬組成物。
- 有効量のオピオイド鎮痛薬、非オピオイド鎮痛薬、制吐薬又は下痢止め薬を更に含む、請求項31に記載の医薬組成物。
- 請求項24に記載の化合物又はその化合物の薬学的に許容される塩を含む、動物における下痢を治療するための医薬組成物。
- 有効量のオピオイド鎮痛薬、非オピオイド鎮痛薬、制吐薬又は下痢止め薬を更に含む、請求項33に記載の医薬組成物。
- 請求項29に記載の組成物を収容した容器を含むキット。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US42738102P | 2002-11-18 | 2002-11-18 | |
US46027803P | 2003-04-03 | 2003-04-03 | |
US48848803P | 2003-07-17 | 2003-07-17 | |
US10/714,066 US7202259B2 (en) | 2002-11-18 | 2003-11-13 | Therapeutic agents useful for treating pain |
PCT/US2003/036742 WO2004046132A1 (en) | 2002-11-18 | 2003-11-17 | 4-tetrazolyl-4phenylpiperidine derivatives for treating pain |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2010056560A Division JP2010163452A (ja) | 2002-11-18 | 2010-03-12 | 疼痛治療用4−テトラゾリル−4フェニルピペリジン誘導体 |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2006525944A JP2006525944A (ja) | 2006-11-16 |
JP2006525944A5 true JP2006525944A5 (ja) | 2007-01-11 |
JP4601429B2 JP4601429B2 (ja) | 2010-12-22 |
Family
ID=32777221
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2004570427A Expired - Fee Related JP4601429B2 (ja) | 2002-11-18 | 2003-11-17 | 疼痛治療用4−テトラゾリル−4フェニルピペリジン誘導体 |
JP2010056560A Pending JP2010163452A (ja) | 2002-11-18 | 2010-03-12 | 疼痛治療用4−テトラゾリル−4フェニルピペリジン誘導体 |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2010056560A Pending JP2010163452A (ja) | 2002-11-18 | 2010-03-12 | 疼痛治療用4−テトラゾリル−4フェニルピペリジン誘導体 |
Country Status (37)
Country | Link |
---|---|
US (3) | US7202259B2 (ja) |
EP (2) | EP1803718B1 (ja) |
JP (2) | JP4601429B2 (ja) |
KR (1) | KR20050115221A (ja) |
CN (2) | CN100567288C (ja) |
AP (1) | AP2210A (ja) |
AR (1) | AR047008A1 (ja) |
AT (2) | ATE358674T1 (ja) |
AU (2) | AU2003294313B2 (ja) |
BR (1) | BR0316305A (ja) |
CA (1) | CA2506242C (ja) |
CO (1) | CO5690588A2 (ja) |
CR (2) | CR7877A (ja) |
CY (2) | CY1107682T1 (ja) |
DE (2) | DE60322451D1 (ja) |
DK (2) | DK1803718T3 (ja) |
EA (1) | EA008621B1 (ja) |
EC (1) | ECSP055840A (ja) |
ES (2) | ES2285235T3 (ja) |
GE (1) | GEP20084539B (ja) |
HK (1) | HK1086829A1 (ja) |
IL (1) | IL209352A0 (ja) |
IS (2) | IS2720B (ja) |
MA (1) | MA27565A1 (ja) |
ME (1) | MEP48108A (ja) |
MX (1) | MXPA05004669A (ja) |
MY (1) | MY135647A (ja) |
NI (1) | NI200500087A (ja) |
NO (1) | NO20052894L (ja) |
NZ (2) | NZ540068A (ja) |
OA (1) | OA13010A (ja) |
PT (2) | PT1562932E (ja) |
RS (1) | RS51047B (ja) |
SG (1) | SG165998A1 (ja) |
SI (2) | SI1803718T1 (ja) |
TW (2) | TWI343917B (ja) |
WO (1) | WO2004046132A1 (ja) |
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US10550088B2 (en) | 2013-12-27 | 2020-02-04 | Purdue Pharma L.P. | 6-substituted and 7-substituted morphinan analogs and the use thereof |
EP3148535A4 (en) | 2014-05-27 | 2017-11-29 | Purdue Pharma LP | Spirocyclic morphinans and use thereof |
MA40171A (fr) | 2014-06-13 | 2017-04-19 | Purdue Pharma Lp | Dérivés d'azamophinan et leur utilisation |
MA41125A (fr) | 2014-12-05 | 2017-10-10 | Purdue Pharma Lp | Dérivés de 6.7-cyclomorphinane et leur utilisation |
AU2017238208B2 (en) | 2016-03-22 | 2022-01-06 | Regents Of The University Of Minnesota | Combination for treating pain |
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