KR101233711B1 - 항염증제로서 유용한 알파-아미노아미드 유도체 - Google Patents
항염증제로서 유용한 알파-아미노아미드 유도체 Download PDFInfo
- Publication number
- KR101233711B1 KR101233711B1 KR1020067003725A KR20067003725A KR101233711B1 KR 101233711 B1 KR101233711 B1 KR 101233711B1 KR 1020067003725 A KR1020067003725 A KR 1020067003725A KR 20067003725 A KR20067003725 A KR 20067003725A KR 101233711 B1 KR101233711 B1 KR 101233711B1
- Authority
- KR
- South Korea
- Prior art keywords
- propanamide
- benzylamino
- fluorobenzyloxy
- inflammatory
- methyl
- Prior art date
- 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.)
- Expired - Lifetime
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- 239000008194 pharmaceutical composition Substances 0.000 claims description 10
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
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Abstract
Description
Claims (7)
- 하기 화학식 I의 알파-아미노아미드 화합물 또는 그의 이성질체, 그의 혼합물, 약제학적으로 허용 가능한 그의 염 또는 에스테르를 활성 약물로서 포함하는 염증성 질환 치료용 약제학적 조성물:[화학식 I]상기 화학식 I에서,■ A는 -CH2-, -CH2-CH2-, -CH2-S-, -CH2-CH2-S-, 또는 -(CH2)n-O-로부터 선택되고, 여기에서 n은 0 내지 5의 정수이고;■ s는 1 또는 2이고;■ R은 할로겐, 메톡시, 또는 트리플루오로메틸로부터 독립적으로 선택된 하나 또는 두 개의 치환기로 선택적으로 치환된 페닐고리이고;■ R1은 수소 또는 C1-C4 알킬이고;■ R2 및 R3 중 하나는 수소이고, 다른 하나는 C1-C4 알킬이거나; R2 및 R3는 모두 메틸이고;■ R4, R5는 각각 독립적으로 수소 또는 C1-C4 알킬이다.
- 삭제
- 제 1 항에 있어서, 상기 활성 약물은 매일 체중당 0.3 내지 100 mg/kg 범위의 용량으로 투여하는 약제학적 조성물.
- 제 1 항에 있어서, 상기 약제학적 조성물은 강직 척추염; 경관절염(cervical arthritis); 섬유근육통; 거트(gut); 소아 류마티스성 관절염; 요천골 관절염; 골관절염; 골다공증; 건선 관절염; 류마티스성 질환; 류마티스성 관절염; 습진; 건선; 피부염; 태양열 화상; 염증성 눈 질환; 포도막염; 결막염; 염증성 폐 질환; 천식; 기관지염; 궤양; 치은염; 크론병; 위축성 위염; 위염 베리알로포르페(gastritis varialoforme); 궤양성 직장염; 셀리악병; 국한회장염; 소화성 궤양; 흉골학작열감(pyresis); 헬리코박터 파이로리(Helicobacter pyoroli)로 인한 GI 경로의 염증; 내장염; 방광자극; 방광염; 중추 또는 말초 신경계의 염증성 신경 질환; 다발성 경화증; 염증성 신경염; 및 AIDS의 신경학적 합병증으로 구성된 그룹에서 선택된 하나 이상의 염증성 질환을 치료하기 위한 약제학적 조성물.
- 제1항, 제3항 및 제4항 중 어느 한 항에 있어서, 하나 이상의 하기 화합물로 구성된 그룹에서 선택된 화합물 또는 그의 이성질체, 그의 혼합물, 또는 약제학적으로 허용 가능한 그의 염을 활성 약물로서 포함하는, 염증성 질환 치료용 약제학적 조성물:2-(4-벤질옥시벤질아미노)-프로판아미드;2-[4-(2-메톡시벤질옥시)-벤질아미노]-프로판아미드;2-[4-(2-플루오로벤질옥시)-벤질아미노]-프로판아미드 ;(S)-(+)-2-[4-(2-플루오로벤질옥시)-벤질아미노]-프로판아미드;2-[4-(2-플루오로벤질옥시)-벤질아미노]-2-메틸-프로판아미드;(S)-(+)-2-[4-(3-플루오로벤질옥시)-벤질아미노]-프로판아미드;2-[4-(2-플루오로벤질옥시)-벤질아미노]-N-메틸-프로판아미드;2-[4-(3-메톡시벤질옥시)-벤질아미노]-프로판아미드;2-[4-(3-플루오로벤질옥시)-벤질아미노]-프로판아미드;2-[4-(3-플루오로벤질옥시)-벤질아미노]-2-메틸-프로판아미드;2-[4-(3-플루오로벤질옥시)-벤질아미노]-N-메틸-프로판아미드;2-[4-(4-플루오로벤질옥시)-벤질아미노]-프로판아미드;2-[4-(3-플루오로벤질옥시)-벤질아미노]-2-메틸-프로판아미드;2-[4-(2-클로로벤질옥시)-벤질아미노]-프로판아미드;2-[4-(3-클로로벤질옥시)-벤질아미노l-프로판아미드;2-[4-(3-클로로벤질옥시)-페닐에틸아미노]-프로판아미드;2-{4-[2-(3-플루오로페닐)-에틸옥시]벤질아미노}-프로판아미드;2-{4-[2-(3-플루오로페닐)-에틸]벤질아미노}-프로판아미드;2-[N-(4-벤질옥시벤질)-N-메틸아미노]-프로판아미드;2-{4-[(3-클로로벤질옥시)-페닐에틸]-아미노}-프로판아미드;2-[4-벤질티오벤질아미노]-프로판아미드;2-[4-(2-플루오로벤질티오)-벤질아미노]-프로판아미드;2-[4-(3-플루오로벤질티오)-벤질아미노]-프로판아미드;2-[4-(3-페닐프로필옥시)-벤질아미노]-프로판아미드;2-[4-(4-페닐부틸옥시)-벤질아미노]-프로판아미드;2-[4-(5-페닐펜틸옥시)-벤질아미노]-프로판아미드;2-(4-벤질옥시벤질아미노)-3-메틸-N-메틸-부탄아미드.
- 제 1 항에 있어서, 상기 알파-아미노아미드 화합물은 (S)-(+)-2-[4-(2-플루오로벤질옥시)-벤질아미노]-프로판아미드인 약제학적 조성물.
- 삭제
Applications Claiming Priority (3)
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US49772203P | 2003-08-25 | 2003-08-25 | |
US60/497,722 | 2003-08-25 | ||
PCT/IB2004/001574 WO2005018627A1 (en) | 2003-08-25 | 2004-04-22 | Alpha-aminoamide derivatives useful as anti-inflammatory agents |
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US (2) | US20070276046A1 (ko) |
EP (1) | EP1658062B1 (ko) |
JP (1) | JP5042625B2 (ko) |
KR (1) | KR101233711B1 (ko) |
CN (1) | CN1842328A (ko) |
AT (1) | ATE457724T1 (ko) |
AU (1) | AU2004266494B2 (ko) |
BR (1) | BRPI0413982A (ko) |
CA (1) | CA2536764C (ko) |
CY (1) | CY1109992T1 (ko) |
DE (1) | DE602004025586D1 (ko) |
DK (1) | DK1658062T3 (ko) |
ES (1) | ES2339021T3 (ko) |
IL (1) | IL173886A (ko) |
NO (1) | NO335245B1 (ko) |
NZ (1) | NZ545502A (ko) |
PL (1) | PL1658062T3 (ko) |
PT (1) | PT1658062E (ko) |
RU (1) | RU2396251C2 (ko) |
SI (1) | SI1658062T1 (ko) |
WO (1) | WO2005018627A1 (ko) |
Families Citing this family (10)
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US20070276046A1 (en) * | 2003-08-25 | 2007-11-29 | Patricia Salvati | Alpha-Aminoamide Derivatives Useful as Anti-Inflammatory Agents |
EP1557166A1 (en) | 2004-01-21 | 2005-07-27 | Newron Pharmaceuticals S.p.A. | Alpha-aminoamide derivatives useful in the treatment of lower urinary tract disorders |
PT1809271E (pt) * | 2004-09-10 | 2010-08-30 | Newron Pharm Spa | Utilização de (halogenobenziloxi)benzilamino-propanamidas para o fabrico de medicamentos activos como moduladores selectivos dos canais de sódio e/ou de cálcio |
DK1963280T3 (en) | 2005-12-22 | 2015-12-14 | Newron Pharm Spa | 2-phenylethylamine derivatives by calcium and / or sodium channel |
JP5240476B2 (ja) | 2006-06-19 | 2013-07-17 | ニユーロン・フアーマシユーテイカルズ・エツセ・ピー・アー | 2−[4−(3−及び2−フルオロベンジルオキシ)ベンジルアミノ]プロパンアミドの製造方法 |
CN101687773B (zh) | 2007-06-15 | 2014-07-30 | 纽朗制药有限公司 | 取代的2-[2-(苯基)乙氨基]烷酰胺衍生物及其作为钠和/或钙通道调节剂的应用 |
EP2229351B1 (en) | 2007-12-11 | 2017-11-08 | Newron Pharmaceuticals S.p.A. | Process for the production of 2-[4-(3- or 2-fluorobenzyloxy)benzylamino]propanamides with high purity degree |
EA021389B1 (ru) | 2010-04-27 | 2015-06-30 | Ньюрон Фармасьютикалс С.П.А. | Способ получения метансульфонатных солей ралфинамида или их r-энантиомеров |
RU2449805C1 (ru) | 2011-01-27 | 2012-05-10 | Общество С Ограниченной Ответственностью "Гармония" | Пептидная фармацевтическая композиция, средство на ее основе для лечения гастродуоденальных заболеваний, вызываемых helicobacter pylori, и способ его использования |
DE102012108965B4 (de) | 2012-09-24 | 2014-08-14 | Exscitron Gmbh | Stromquelle mit verbesserter Dimmvorrichtung |
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WO2003020273A2 (en) * | 2001-09-03 | 2003-03-13 | Newron Pharmaceuticals Spa | Pharmaceutical composition comprising gabapentin or an analogue thereof and an $g(a)-aminoamide and its analgesic use |
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IL94466A (en) * | 1989-05-25 | 1995-01-24 | Erba Carlo Spa | Pharmaceutical preparations containing the history of A-amino carboxamide N-phenylalkyl are converted into such new compounds and their preparation |
GB9726987D0 (en) * | 1997-12-22 | 1998-02-18 | Glaxo Group Ltd | Compounds |
GB9727523D0 (en) * | 1997-12-31 | 1998-02-25 | Pharmacia & Upjohn Spa | Alpha-aminoamide derivatives useful as analgesic agents |
SE9801494D0 (sv) * | 1998-04-28 | 1998-04-28 | Astra Pharma Prod | Novel use |
RU2164512C1 (ru) * | 1999-07-27 | 2001-03-27 | Всероссийский научный центр по безопасности биологически активных веществ | Производные аминокислот, проявляющие антиаритмическую активность |
GB9930079D0 (en) * | 1999-12-20 | 2000-02-09 | Glaxo Group Ltd | Medicaments |
AU2001278045B2 (en) * | 2000-07-27 | 2006-08-03 | Pharmacia Corporation | Epoxy-steroidal aldosterone antagonist and calcium channel blocker combination therapy for treatment of congestive heart failure |
JP2005514412A (ja) * | 2001-12-27 | 2005-05-19 | オーソ−マクニール・フアーマシユーチカル・インコーポレーテツド | 中枢神経系疾患を処置するために有用なアロイルピロールヘテロアリールおよびメタノール類 |
EP1438956A1 (en) * | 2003-01-16 | 2004-07-21 | Newron Pharmaceuticals S.p.A. | Alpha-aminoamide derivatives useful as antimigraine agents |
EP1589959A2 (en) * | 2003-01-30 | 2005-11-02 | Dynogen Pharmaceuticals Inc. | Methods of treating lower urinary tract disorders using sodium channel modulators |
JP2006515326A (ja) * | 2003-01-30 | 2006-05-25 | ダイノジェン ファーマシューティカルズ, インコーポレイテッド | 胃腸管障害を処置するためのナトリウムチャネルモジュレーターの使用 |
AR044007A1 (es) * | 2003-04-11 | 2005-08-24 | Newron Pharmaceuticals Inc | Metodos para el tratamiento de la enfermedad de parkinson |
US20070276046A1 (en) * | 2003-08-25 | 2007-11-29 | Patricia Salvati | Alpha-Aminoamide Derivatives Useful as Anti-Inflammatory Agents |
EP1588704A1 (en) * | 2004-04-22 | 2005-10-26 | Newron Pharmaceuticals S.p.A. | Alpha-aminoamide derivatives useful in the treatment of restless legs syndrome and addictive disorders |
PT1809271E (pt) * | 2004-09-10 | 2010-08-30 | Newron Pharm Spa | Utilização de (halogenobenziloxi)benzilamino-propanamidas para o fabrico de medicamentos activos como moduladores selectivos dos canais de sódio e/ou de cálcio |
DK1963280T3 (en) * | 2005-12-22 | 2015-12-14 | Newron Pharm Spa | 2-phenylethylamine derivatives by calcium and / or sodium channel |
EP1870097A1 (en) * | 2006-06-15 | 2007-12-26 | Newron Pharmaceuticals S.p.A. | Alpha-aminoamide derivatives useful in the treatment of cognitive disorders |
JP5240476B2 (ja) * | 2006-06-19 | 2013-07-17 | ニユーロン・フアーマシユーテイカルズ・エツセ・ピー・アー | 2−[4−(3−及び2−フルオロベンジルオキシ)ベンジルアミノ]プロパンアミドの製造方法 |
CN101687773B (zh) * | 2007-06-15 | 2014-07-30 | 纽朗制药有限公司 | 取代的2-[2-(苯基)乙氨基]烷酰胺衍生物及其作为钠和/或钙通道调节剂的应用 |
EP2229351B1 (en) * | 2007-12-11 | 2017-11-08 | Newron Pharmaceuticals S.p.A. | Process for the production of 2-[4-(3- or 2-fluorobenzyloxy)benzylamino]propanamides with high purity degree |
EP2222290B1 (en) * | 2007-12-19 | 2021-06-16 | Newron Pharmaceuticals S.p.A. | Alpha-aminoamide derivatives for the treatment of psychiatric disorders |
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2004
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- 2004-04-22 KR KR1020067003725A patent/KR101233711B1/ko not_active Expired - Lifetime
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- 2004-04-22 CN CNA2004800242753A patent/CN1842328A/zh active Pending
- 2004-04-22 JP JP2006524432A patent/JP5042625B2/ja not_active Expired - Lifetime
- 2004-04-22 SI SI200431379T patent/SI1658062T1/sl unknown
- 2004-04-22 AT AT04728870T patent/ATE457724T1/de active
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2006
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2009
- 2009-08-20 US US12/544,456 patent/US20100016440A1/en not_active Abandoned
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Patent Citations (1)
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WO2003020273A2 (en) * | 2001-09-03 | 2003-03-13 | Newron Pharmaceuticals Spa | Pharmaceutical composition comprising gabapentin or an analogue thereof and an $g(a)-aminoamide and its analgesic use |
Also Published As
Publication number | Publication date |
---|---|
PT1658062E (pt) | 2010-03-31 |
RU2006105634A (ru) | 2006-08-10 |
CA2536764A1 (en) | 2005-03-03 |
RU2396251C2 (ru) | 2010-08-10 |
IL173886A (en) | 2012-09-24 |
WO2005018627A8 (en) | 2005-09-01 |
AU2004266494A1 (en) | 2005-03-03 |
EP1658062A1 (en) | 2006-05-24 |
NO20060896L (no) | 2006-03-09 |
CY1109992T1 (el) | 2014-09-10 |
CN1842328A (zh) | 2006-10-04 |
JP2007503424A (ja) | 2007-02-22 |
WO2005018627A1 (en) | 2005-03-03 |
DK1658062T3 (da) | 2010-05-31 |
KR20060128825A (ko) | 2006-12-14 |
ES2339021T3 (es) | 2010-05-14 |
US20100016440A1 (en) | 2010-01-21 |
NO335245B1 (no) | 2014-10-27 |
PL1658062T3 (pl) | 2010-07-30 |
EP1658062B1 (en) | 2010-02-17 |
JP5042625B2 (ja) | 2012-10-03 |
US20070276046A1 (en) | 2007-11-29 |
DE602004025586D1 (de) | 2010-04-01 |
SI1658062T1 (sl) | 2010-05-31 |
ATE457724T1 (de) | 2010-03-15 |
CA2536764C (en) | 2013-09-17 |
IL173886A0 (en) | 2006-07-05 |
NZ545502A (en) | 2010-04-30 |
BRPI0413982A (pt) | 2006-11-07 |
AU2004266494B2 (en) | 2010-04-08 |
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