JP2005534620A5 - - Google Patents
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- Publication number
- JP2005534620A5 JP2005534620A5 JP2003582140A JP2003582140A JP2005534620A5 JP 2005534620 A5 JP2005534620 A5 JP 2005534620A5 JP 2003582140 A JP2003582140 A JP 2003582140A JP 2003582140 A JP2003582140 A JP 2003582140A JP 2005534620 A5 JP2005534620 A5 JP 2005534620A5
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- JP
- Japan
- Prior art keywords
- group
- formula
- alkyl
- hydrogen
- substituted
- 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.)
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- 125000005843 halogen group Chemical group 0.000 claims 10
- 150000001875 compounds Chemical class 0.000 claims 8
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 7
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 125000004433 nitrogen atoms Chemical class N* 0.000 claims 5
- -1 1,2,3,4-tetrahydronaphthalen-1-yl groups Chemical group 0.000 claims 4
- 125000004429 atoms Chemical group 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 4
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 150000004677 hydrates Chemical class 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000011780 sodium chloride Substances 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- 125000002252 acyl group Chemical group 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000002837 carbocyclic group Chemical group 0.000 claims 2
- 125000005842 heteroatoms Chemical group 0.000 claims 2
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 1
- YJTKZCDBKVTVBY-UHFFFAOYSA-N 1,3-Diphenylbenzene Chemical group C1=CC=CC=C1C1=CC=CC(C=2C=CC=CC=2)=C1 YJTKZCDBKVTVBY-UHFFFAOYSA-N 0.000 claims 1
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000005113 hydroxyalkoxy group Chemical group 0.000 claims 1
- 125000004129 indan-1-yl group Chemical group [H]C1=C([H])C([H])=C2C(=C1[H])C([H])([H])C([H])([H])C2([H])* 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000000467 secondary amino group Chemical group [H]N([*:1])[*:2] 0.000 claims 1
Claims (7)
- 式:
− R1は、水素または(C1-C4)アルキルを表し;
− R2は:
・ (C3-C7)アルキル基、
・ インダン-1-イルまたは1,2,3,4-テトラヒドロナフタレン-1-イル基を表し、これらの基は非置換であるかまたはハロゲン原子および/またはメチル基で置換されている;
・ 5〜7原子の飽和の窒素1個の複素環式基を表し、この窒素原子は(C1-C4)アルキル、ベンジル、(C1-C3)アルコキシカルボニルまたは(C1-C4)アルカノイル基で置換されている;
・ 基NR9R10;
・ 基(CH2)nR11、CH(CH3)R11、(CH2)mN(CH3)R11;
・ 非置換または1以上のメチル基で置換されたC3-C12非芳香性炭素環式基、;
を表すか、
− あるいは、R1およびR2は、それらが結合している窒素原子と一緒になって、フェニルもしくはベンジル基により4位において置換されたピペラジン-1-イル基、またはフェニルもしくはベンジル基、および(C1-C4)アルキルもしくは(C1-C3)アルカノイル基により4位において二置換されたピペリジン-1-イル基を形成し;このピペラジン-1-イル基またはピペリジン-1-イル基上のフェニルもしくはベンジル置換基は、非置換であるかまたはハロゲン原子および/またはメチル基で置換されている;
− R3、R4、R5、R6、R7およびR8は、それぞれ互いに独立して、水素もしくはハロゲン原子、または(C1-C6)アルキル、(C1-C6)アルコキシまたはトリフルオロメチル基を表し;
− R9およびR10は、それらが結合している窒素原子と一緒になって、OおよびNから選択される第2のヘテロ原子を含むか含まない、5〜10原子の飽和または不飽和の複素環式基を形成し、該基は非置換であるか、または1以上の(C1-C4)アルキル、ヒドロキシもしくは(C1-C4)アルコキシ基で置換されている;
− R11は:
・ 非置換であるか、またはハロゲン原子およびメチル基から選択される1以上の置換基で置換されたフェニル;
・ 1以上の窒素原子を含む6〜10原子のヘテロアリール基;
を表し
− nは、1、2または3を表し;
− mは、0、2または3を表す]
の化合物、ならびにそれらの塩、それらの溶媒和物およびそれらの水和物。 - 式(I):
(式中、
− R1が、水素原子または(C1-C4)アルキル基を表し;
− R2が、基NR9R10、または非置換または1以上のメチル基で置換された非芳香性C3-C12炭素環式基を表し;
− R3、R4、R5、R6、R7およびR8が、それぞれ互いに独立して、水素もしくはハロゲン原子、または(C1-C6)アルキル、(C1-C6)アルコキシもしくはトリフルオロメチル基を表し;
− R9およびR10が、それらが結合している窒素原子と一緒になって、OおよびNから選択される第2のヘテロ原子を含むか含まない、5〜10原子の飽和または不飽和の複素環式基を形成し、該基は非置換であるか、または1以上の(C1-C4)アルキル基で置換されている)
の請求項1に記載の化合物、ならびにそれらの塩、それらの溶媒和物およびそれらの水和物。 - 式(I):
(式中、
− R1が、水素原子を表し;そして/または
− R2が、ピペリジン-1-イル、ピロリジン-1-イル、シクロヘキシル、スピロ[5.5]ウンデカニルおよび1,3,3-トリメチルビシクロ[2.2.1]ヘプタン-2-イルから選択される基を表し;そして/または
− 置換基R3、R4およびR5の少なくとも一つが、ハロゲン原子またはトリフルオロメチル基を表し;そして/または
− 置換基R6、R7およびR8の少なくとも一つが、ハロゲン原子を表す)
の請求項1または2に記載の化合物。 - 式(IIbis):
(式中、
− R3が4位にあって、ハロゲン原子またはトリフルオロメチル基を表し;
− R6が2位にあって、水素またはハロゲン原子を表し;
− R7が4位にあって、ハロゲン原子を表し;
− R4、R5およびR8が水素である)
の請求項5に記載の化合物。 - 請求項1〜3のいずれか一つに記載の式(I)の化合物、またはその医薬的に許容される塩、水和物または溶媒和物の一つ、および少なくとも一つの医薬的に許容される賦形剤を含むことを特徴とする医薬組成物。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR0204567A FR2838439B1 (fr) | 2002-04-11 | 2002-04-11 | Derives de terphenyle, leur preparation, les compositions pharmaceutqiues en contenant |
PCT/FR2003/001134 WO2003084943A2 (fr) | 2002-04-11 | 2003-04-10 | Derives de terphenyle, leur preparation, les compositions pharmaceutiques en contenant |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2005534620A JP2005534620A (ja) | 2005-11-17 |
JP2005534620A5 true JP2005534620A5 (ja) | 2006-06-01 |
JP4634717B2 JP4634717B2 (ja) | 2011-02-16 |
Family
ID=28459770
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2003582140A Expired - Fee Related JP4634717B2 (ja) | 2002-04-11 | 2003-04-10 | テルフェニル誘導体、それらの製造およびそれらを含む組成物 |
Country Status (13)
Country | Link |
---|---|
US (1) | US7390924B2 (ja) |
EP (1) | EP1497274B1 (ja) |
JP (1) | JP4634717B2 (ja) |
CN (1) | CN100432062C (ja) |
AT (1) | ATE339408T1 (ja) |
AU (1) | AU2003246811A1 (ja) |
BR (1) | BR0309106A (ja) |
CA (1) | CA2481392A1 (ja) |
DE (1) | DE60308349T2 (ja) |
FR (1) | FR2838439B1 (ja) |
MX (1) | MXPA04009981A (ja) |
PL (1) | PL374024A1 (ja) |
WO (1) | WO2003084943A2 (ja) |
Families Citing this family (58)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1492784A4 (en) | 2002-03-28 | 2006-03-29 | Merck & Co Inc | SUBSTITUTED 2,3-DIPHENYLPYRIDINES |
EP1546115A4 (en) | 2002-09-27 | 2010-08-04 | Merck Sharp & Dohme | SUBSTITUTED PYRIMIDINES |
US7129239B2 (en) | 2002-10-28 | 2006-10-31 | Pfizer Inc. | Purine compounds and uses thereof |
US7247628B2 (en) | 2002-12-12 | 2007-07-24 | Pfizer, Inc. | Cannabinoid receptor ligands and uses thereof |
US7772188B2 (en) | 2003-01-28 | 2010-08-10 | Ironwood Pharmaceuticals, Inc. | Methods and compositions for the treatment of gastrointestinal disorders |
US7176210B2 (en) | 2003-02-10 | 2007-02-13 | Pfizer Inc. | Cannabinoid receptor ligands and uses thereof |
US7141669B2 (en) | 2003-04-23 | 2006-11-28 | Pfizer Inc. | Cannabiniod receptor ligands and uses thereof |
US7145012B2 (en) | 2003-04-23 | 2006-12-05 | Pfizer Inc. | Cannabinoid receptor ligands and uses thereof |
US7268133B2 (en) | 2003-04-23 | 2007-09-11 | Pfizer, Inc. Patent Department | Cannabinoid receptor ligands and uses thereof |
US7232823B2 (en) | 2003-06-09 | 2007-06-19 | Pfizer, Inc. | Cannabinoid receptor ligands and uses thereof |
FR2856684B1 (fr) * | 2003-06-26 | 2008-04-11 | Sanofi Synthelabo | Derives de diphenylpyridine, leur preparation et leur application en therapeutique |
MXPA06008391A (es) | 2004-01-28 | 2006-08-25 | Hoffmann La Roche | Nuevos compuestos espiro-pentaciclicos. |
EP1574211A1 (en) | 2004-03-09 | 2005-09-14 | Inserm | Use of antagonists of the CB1 receptor for the manufacture of a composition useful for the treatment of hepatic diseases |
WO2005097127A2 (en) | 2004-04-02 | 2005-10-20 | Merck & Co., Inc. | Method of treating men with metabolic and anthropometric disorders |
TW200602314A (en) | 2004-05-28 | 2006-01-16 | Tanabe Seiyaku Co | A novel pyrrolidine compound and a process for preparing the same |
JP4760139B2 (ja) * | 2004-05-28 | 2011-08-31 | 田辺三菱製薬株式会社 | ピロリジン誘導体およびその製法 |
US20060025448A1 (en) | 2004-07-22 | 2006-02-02 | Cadila Healthcare Limited | Hair growth stimulators |
GB0416508D0 (en) * | 2004-07-23 | 2004-08-25 | Merck Sharp & Dohme | Therapeutic agents |
FR2876691B1 (fr) * | 2004-10-18 | 2006-12-29 | Sanofi Aventis Sa | Derives de pyridine, leur preparation, leur application en therapeutique |
EP1812418B1 (en) | 2004-11-09 | 2010-10-27 | F. Hoffmann-La Roche AG | Dibenzosuberone derivatives |
US7914859B2 (en) * | 2005-01-25 | 2011-03-29 | Merck Patent Gmbh | Mesogenic compounds, liquid crystal medium and liquid crystal display |
BRPI0613505A2 (pt) | 2005-06-30 | 2011-01-11 | Prosidion Ltd | agonistas de gpcr |
FR2899899A1 (fr) * | 2006-04-14 | 2007-10-19 | Sanofi Aventis Sa | Derives d'aminomethyl pyridine, leur preparation et leur application en therapeutique |
ATE445586T1 (de) * | 2006-04-21 | 2009-10-15 | Cellzome Ltd | Terphenylderivate zur alzheimerbehandlung |
BRPI0715160A2 (pt) | 2006-08-08 | 2013-06-11 | Sanofi Aventis | imidazolidina-2,4-dionas substituÍdas por arilamimoaril-alquil-, processo para preparÁ-las, medicamentos compeendendo estes compostos, e seu uso |
WO2008081208A1 (en) | 2007-01-04 | 2008-07-10 | Prosidion Limited | Piperidine gpcr agonists |
GB0700122D0 (en) | 2007-01-04 | 2007-02-14 | Prosidion Ltd | GPCR agonists |
DK2114933T3 (da) | 2007-01-04 | 2012-01-02 | Prosidion Ltd | Piperidin-GPCR-agonister |
AR064736A1 (es) | 2007-01-04 | 2009-04-22 | Prosidion Ltd | Agonistas de gpcr |
AR064735A1 (es) | 2007-01-04 | 2009-04-22 | Prosidion Ltd | Agonistas de gpcr y composicion farmaceutica en base al compuesto |
GB0702862D0 (en) * | 2007-02-14 | 2007-03-28 | Univ Aberdeen | Therapeutic compounds |
EA020466B1 (ru) | 2007-06-04 | 2014-11-28 | Синерджи Фармасьютикалз Инк. | Агонисты гуанилатциклазы, пригодные для лечения желудочно-кишечных нарушений, воспаления, рака и других заболеваний |
US8969514B2 (en) | 2007-06-04 | 2015-03-03 | Synergy Pharmaceuticals, Inc. | Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases |
EP2025674A1 (de) | 2007-08-15 | 2009-02-18 | sanofi-aventis | Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
GB0720390D0 (en) | 2007-10-18 | 2007-11-28 | Prosidion Ltd | G-Protein coupled receptor agonists |
GB0720389D0 (en) | 2007-10-18 | 2008-11-12 | Prosidion Ltd | G-Protein Coupled Receptor Agonists |
EP2810951B1 (en) | 2008-06-04 | 2017-03-15 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders |
WO2010003624A2 (en) | 2008-07-09 | 2010-01-14 | Sanofi-Aventis | Heterocyclic compounds, processes for their preparation, medicaments comprising these compounds, and the use thereof |
ES2624828T3 (es) | 2008-07-16 | 2017-07-17 | Synergy Pharmaceuticals Inc. | Agonistas de la guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros |
WO2010068601A1 (en) | 2008-12-08 | 2010-06-17 | Sanofi-Aventis | A crystalline heteroaromatic fluoroglycoside hydrate, processes for making, methods of use and pharmaceutical compositions thereof |
EP2470552B1 (en) | 2009-08-26 | 2013-11-13 | Sanofi | Novel crystalline heteroaromatic fluoroglycoside hydrates, pharmaceuticals comprising these compounds and their use |
EP2582709B1 (de) | 2010-06-18 | 2018-01-24 | Sanofi | Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen |
US9616097B2 (en) | 2010-09-15 | 2017-04-11 | Synergy Pharmaceuticals, Inc. | Formulations of guanylate cyclase C agonists and methods of use |
GB2486631A (en) * | 2010-12-01 | 2012-06-27 | Univ Sheffield | Phenol/quinone boronic acids/esters and method of preparation thereof |
US8871758B2 (en) | 2011-03-08 | 2014-10-28 | Sanofi | Tetrasubstituted oxathiazine derivatives, method for producing them, their use as medicine and drug containing said derivatives and the use thereof |
EP2683702B1 (de) | 2011-03-08 | 2014-12-24 | Sanofi | Neue substituierte phenyl-oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
WO2012120055A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
US8828994B2 (en) | 2011-03-08 | 2014-09-09 | Sanofi | Di- and tri-substituted oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
US8828995B2 (en) | 2011-03-08 | 2014-09-09 | Sanofi | Branched oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
WO2012120052A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Mit carbozyklen oder heterozyklen substituierte oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
WO2012120057A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Neue substituierte phenyl-oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
EP2683698B1 (de) | 2011-03-08 | 2017-10-04 | Sanofi | Mit adamantan- oder noradamantan substituierte benzyl-oxathiazinderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
EP2683701B1 (de) | 2011-03-08 | 2014-12-24 | Sanofi | Mit benzyl- oder heteromethylengruppen substituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
CA2905438A1 (en) | 2013-03-15 | 2014-09-25 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase and their uses |
CA2905435A1 (en) | 2013-03-15 | 2014-09-25 | Synergy Pharmaceuticals Inc. | Compositions useful for the treatment of gastrointestinal disorders |
PT3004138T (pt) | 2013-06-05 | 2024-06-18 | Bausch Health Ireland Ltd | Agonistas ultrapuros de guanilato ciclase c, método de produção e utilização dos mesmos |
CN105175241B (zh) * | 2015-08-28 | 2017-09-29 | 浙江工业大学 | 三联苯类化合物及其制备方法和应用 |
WO2018159650A1 (ja) * | 2017-02-28 | 2018-09-07 | 東レ株式会社 | グアニジン誘導体及びその医薬用途 |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4916145A (en) * | 1987-07-10 | 1990-04-10 | Hoffmann-La Roche Inc. | Substituted n-[(pyridyl)alkyl]aryl-carboxamide |
FR2800375B1 (fr) * | 1999-11-03 | 2004-07-23 | Sanofi Synthelabo | Derives tricycliques d'acide pyrazolecarboxylique, leur preparation, les compositions pharmaceutiques en contenant |
-
2002
- 2002-04-11 FR FR0204567A patent/FR2838439B1/fr not_active Expired - Fee Related
-
2003
- 2003-04-10 BR BR0309106-6A patent/BR0309106A/pt not_active IP Right Cessation
- 2003-04-10 EP EP03745842A patent/EP1497274B1/fr not_active Expired - Lifetime
- 2003-04-10 DE DE60308349T patent/DE60308349T2/de not_active Expired - Lifetime
- 2003-04-10 AU AU2003246811A patent/AU2003246811A1/en not_active Abandoned
- 2003-04-10 MX MXPA04009981A patent/MXPA04009981A/es active IP Right Grant
- 2003-04-10 US US10/511,040 patent/US7390924B2/en not_active Expired - Fee Related
- 2003-04-10 CA CA002481392A patent/CA2481392A1/fr not_active Abandoned
- 2003-04-10 JP JP2003582140A patent/JP4634717B2/ja not_active Expired - Fee Related
- 2003-04-10 CN CNB038130068A patent/CN100432062C/zh not_active Expired - Fee Related
- 2003-04-10 PL PL03374024A patent/PL374024A1/xx not_active Application Discontinuation
- 2003-04-10 WO PCT/FR2003/001134 patent/WO2003084943A2/fr active IP Right Grant
- 2003-04-10 AT AT03745842T patent/ATE339408T1/de not_active IP Right Cessation
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