CN100513386C - 用于抑制由白介素8诱导的中性粒细胞趋化作用的酰胺 - Google Patents

用于抑制由白介素8诱导的中性粒细胞趋化作用的酰胺 Download PDF

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CN100513386C
CN100513386C CNB018047866A CN01804786A CN100513386C CN 100513386 C CN100513386 C CN 100513386C CN B018047866 A CNB018047866 A CN B018047866A CN 01804786 A CN01804786 A CN 01804786A CN 100513386 C CN100513386 C CN 100513386C
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phenyl
general formula
methyl
acid
alkyl
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Expired - Fee Related
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CN1479715A (zh
Inventor
M·阿莱格蒂
R·贝尔蒂尼
B·辛齐
V·萨巴蒂尼
G·卡塞利
M·C·切斯塔
C·甘多利
F·科洛塔
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Dompe SpA
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Dompe SpA
Dompe PhaRMa SpA
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    • C07ORGANIC CHEMISTRY
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    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P9/00Drugs for disorders of the cardiovascular system
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/02Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • C07C233/11Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to carbon atoms of an unsaturated carbon skeleton containing six-membered aromatic rings
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/16Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C07C233/17Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/22Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
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    • C07C233/00Carboxylic acid amides
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    • C07C233/45Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/46Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/51Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/45Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/52Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/32Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C07C235/34Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
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    • C07C235/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/70Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/72Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms
    • C07C235/76Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton
    • C07C235/78Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton the carbon skeleton containing rings
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/20Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/62Compounds containing any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylcarbamates
    • C07C271/64Y being a hydrogen or a carbon atom, e.g. benzoylcarbamates
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    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
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    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
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    • C07C2601/14The ring being saturated

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  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Polysaccharides And Polysaccharide Derivatives (AREA)
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CNB018047866A 2000-02-11 2001-02-06 用于抑制由白介素8诱导的中性粒细胞趋化作用的酰胺 Expired - Fee Related CN100513386C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IT2000MI000227A IT1317826B1 (it) 2000-02-11 2000-02-11 Ammidi, utili nell'inibizione della chemiotassi dei neutrofiliindotta da il-8.
ITMI2000A000227 2000-02-11

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Publication Number Publication Date
CN1479715A CN1479715A (zh) 2004-03-03
CN100513386C true CN100513386C (zh) 2009-07-15

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CNB018047866A Expired - Fee Related CN100513386C (zh) 2000-02-11 2001-02-06 用于抑制由白介素8诱导的中性粒细胞趋化作用的酰胺

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US (1) US7705050B2 (enExample)
EP (1) EP1255726B1 (enExample)
JP (1) JP4937479B2 (enExample)
KR (1) KR100884417B1 (enExample)
CN (1) CN100513386C (enExample)
AT (1) ATE448195T1 (enExample)
AU (2) AU4412501A (enExample)
BR (2) BRPI0108152B1 (enExample)
CA (1) CA2396937C (enExample)
CY (1) CY1109780T1 (enExample)
CZ (1) CZ302945B6 (enExample)
DE (1) DE60140429D1 (enExample)
DK (1) DK1255726T3 (enExample)
EE (1) EE05284B1 (enExample)
ES (1) ES2336301T3 (enExample)
HU (1) HU229447B1 (enExample)
IL (1) IL150523A0 (enExample)
IT (1) IT1317826B1 (enExample)
MX (1) MXPA02007714A (enExample)
NO (1) NO331460B1 (enExample)
NZ (1) NZ519925A (enExample)
PL (1) PL207126B1 (enExample)
PT (1) PT1255726E (enExample)
RU (1) RU2273630C2 (enExample)
SI (1) SI1255726T1 (enExample)
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WO (1) WO2001058852A2 (enExample)

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IT1318466B1 (it) * 2000-04-14 2003-08-25 Dompe Spa Ammidi di acidi r-2-(amminoaril)-propionici, utili nella prevenzionedell'attivazione leucocitaria.
TWI243164B (en) 2001-02-13 2005-11-11 Aventis Pharma Gmbh Acylated indanyl amines and their use as pharmaceuticals
ITMI20010395A1 (it) 2001-02-27 2002-08-27 Dompe Spa Omega-amminoalchilammidi di acidi r-2-aril-propionici come inibitori della chemiotassi di cellule polimorfonucleate e mononucleate
ITMI20012025A1 (it) * 2001-09-28 2003-03-28 Dompe Spa Sali di ammonio quaternari di omega-amminoalchilammidi di acidi r 2-aril-propionici e composizioni farmaceutiche che li contengono
ITMI20012434A1 (it) * 2001-11-20 2003-05-20 Dompe Spa Acidi 2-aril-propionici e composizioni farmaceutiche che li contengono
CA2507765C (en) * 2002-12-10 2012-03-20 Dompe S.P.A. Chiral arylketones in the treatment of neutrophil-dependent inflammatory diseases
PT1590314E (pt) 2003-02-06 2015-11-19 Dompã Farmaceutici S P A Ácidos 2-aril-acéticos, seus derivados e composições farmacêuticas que os contêm
EP1457485A1 (en) * 2003-03-14 2004-09-15 Dompé S.P.A. Sulfonic acids, their derivatives and pharmaceutical compositions containing them
ATE521589T1 (de) * 2003-09-25 2011-09-15 Dompe Spa Amidine und derivate davon und pharmazeutische zusammensetzungen, die diese enthalten
CN1934077B (zh) 2004-03-23 2010-09-29 冬姆佩制药股份公司 2-苯基丙酸衍生物及含有它们的药物组合物
EP1856031B1 (en) * 2004-12-15 2009-02-25 DOMPE' pha.r.ma s.p.a. 2-arylpropionic acid derivatives and pharmaceutical compositions containing them
EP1676834A1 (en) 2004-12-30 2006-07-05 Sanofi-Aventis Deutschland GmbH Fused bicyclic carboxamide derivates for use as CXCR2 inhibitors in the treatment of inflammation
DE602006007210D1 (de) * 2005-01-25 2009-07-23 Dompe Pha R Ma Spa Res & Mfg Metaboliten aus 2-arylpropionsäure-derivaten und pharmazeutische zusammensetzungen damit
US7652169B2 (en) * 2006-05-18 2010-01-26 Dompe' Pha. R. Ma S.p.A. (2R)-2-[(4-sulfonyl) aminophenyl] propanamides and pharmaceutical compositions containing them
JP5237938B2 (ja) 2006-06-28 2013-07-17 サノフイ 新規なcxcr2阻害剤
JP5352454B2 (ja) 2006-06-28 2013-11-27 サノフイ Cxcr2アンンタゴニスト
EP2040690B1 (en) 2006-06-28 2014-08-06 Sanofi Inhibitors of cxcr2
JP5352455B2 (ja) 2006-06-30 2013-11-27 サノフイ Cxcr2阻害剤
US20090238763A1 (en) 2006-07-09 2009-09-24 Chongxi Yu High penetration compositions and uses thereof
US20090221703A1 (en) 2006-07-09 2009-09-03 Chongxi Yu High penetration composition and uses thereof
CN103772259B (zh) * 2006-08-08 2016-08-31 于崇曦 具有快速皮肤穿透速度的带正电荷的芳基和杂芳基乙酸类前药
CN101506160A (zh) * 2006-08-08 2009-08-12 于崇曦 具有快速皮肤穿透速度的带正电荷的芳基和杂芳基乙酸类前药
CN103772258B (zh) * 2006-08-08 2016-09-28 于崇曦 具有快速皮肤穿透速度的带正电荷的芳基和杂芳基乙酸类前药
JP5424880B2 (ja) * 2006-08-15 2014-02-26 テックフィールズ バイオケム カンパニー リミテッド 非常に速い皮膚透過率を有するアリール−及びヘテロアリールプロピオン酸の正荷電水溶性プロドラッグ
KR20210103586A (ko) 2007-06-04 2021-08-23 테크필즈 인크 매우 높은 피부 및 막 침투율을 가지는 비스테로이드성 소염제(nsaia) 약물전구체 및 이들의 새로운 의약적 용도
EP3546452A1 (en) * 2007-10-08 2019-10-02 MMV Medicines for Malaria Venture Antimalarial compounds with flexible side-chains
JP2011507909A (ja) 2007-12-20 2011-03-10 エンビボ ファーマシューティカルズ インコーポレイテッド 四置換ベンゼン
EP2166006A1 (en) * 2008-09-18 2010-03-24 Dompe' S.P.A. 2-aryl-propionic acids and derivatives and pharmaceutical compositions containing them
CN107320732B (zh) 2008-12-04 2021-09-07 于崇曦 高穿透性组合物及其应用
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