AR026990A1 - Antagonistas de neurokinina selectivos - Google Patents
Antagonistas de neurokinina selectivosInfo
- Publication number
- AR026990A1 AR026990A1 ARP000106707A ARP000106707A AR026990A1 AR 026990 A1 AR026990 A1 AR 026990A1 AR P000106707 A ARP000106707 A AR P000106707A AR P000106707 A ARP000106707 A AR P000106707A AR 026990 A1 AR026990 A1 AR 026990A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cycloalkyl
- heteroaryl
- selective
- conr13r14
- Prior art date
Links
- 239000005557 antagonist Substances 0.000 title abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 1
- -1 -NR17R13 Chemical group 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/06—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D239/08—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms directly attached in position 2
- C07D239/10—Oxygen or sulfur atoms
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- C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
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- C07C45/68—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms
- C07C45/70—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction with functional groups containing oxygen only in singly bound form
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Abstract
Se describe el compuesto representado por la formula estructural (1)o su sal farmacéuticamente aceptable, en donde Ar1 y Ar2 son heteroarilo optativamentesustituido o fenilo optativamente sustituido: X1 es -O-, -S-, -SO-, -SO2-, -NR12-, -NCOR12- o -N R12SO2R15-; Q se selecciona entre el grupo que consiste en laformula (2) X2 es -O-, -S-o NR5-; Y es =O, =S o =NR11; Y 1 es H alquilo C1-6, -NR17R13, -SCH3, R19-aril(CH2(n6-, R19-heteroaril-(CH2)n6-, (CH2)n6-heterocicloalquil, -(C1-C3)alquil-NH-C(O)O( C1-6)alquilo o -NHC(O)R15, R5 es H o -(CH2)n1-G, en donde n1 es 0-5, G es H, -CF3, -CHF2, -CH2F, OH, -O-(alquilo C1-6), -SO2R13, -O-(cicloalquilo C3-8), NR13R14, -SO2NR13R14, -NR13SO2R15, -NR13COR12, -NR12(CONR13R14), -CONR13R14, -COOR12, cicloalquil o C3-8, R19-heteroarilo,y siempre y cuando n1=O, G no es H; R1, R2, R3 y R7 SON h, alquilo, cicloalquilo, -CHF2, -CH2F o -CF3; o R1 y R2, junto con el carbono al cual están unidos,forman un anillo alquileno; o R1 y R2 juntos son =O; R6 es R7 o OH; y las variables restantes son como se definieron en la memoria descriptiva, también sedescriben métodos paa el tratamietno de enfermedades susceptibles de tratamiento con antagonistas de neurokinina con dichos compuestos, y composicionesfarmacéuticas q ue comprenden dichos compuestos. También se describen composiciones farmacéuticas que comprenden una cantidad efectiva de uncompuesto de acuerdocon al reivindicacion 1, por lo meno sun portador farmacéuticamente aceptable, y en combinacion con una ca ntidad efectiva de un inhibidor de la recaptacion deserotonina selectivo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US17248999P | 1999-12-17 | 1999-12-17 |
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AR026990A1 true AR026990A1 (es) | 2003-03-05 |
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ARP000106707A AR026990A1 (es) | 1999-12-17 | 2000-12-15 | Antagonistas de neurokinina selectivos |
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EP (1) | EP1237874B1 (es) |
JP (1) | JP2003522739A (es) |
KR (1) | KR20020067548A (es) |
CN (1) | CN1434805A (es) |
AR (1) | AR026990A1 (es) |
AT (1) | ATE318259T1 (es) |
AU (1) | AU2097601A (es) |
CA (1) | CA2393672A1 (es) |
CO (1) | CO5261559A1 (es) |
DE (1) | DE60026169T2 (es) |
EC (1) | ECSP003828A (es) |
ES (1) | ES2258485T3 (es) |
HK (1) | HK1045308A1 (es) |
HU (1) | HUP0301607A3 (es) |
IL (1) | IL150033A0 (es) |
MX (1) | MXPA02006017A (es) |
PE (1) | PE20011035A1 (es) |
WO (1) | WO2001044200A2 (es) |
ZA (1) | ZA200204395B (es) |
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AR038002A1 (es) | 2001-11-13 | 2004-12-22 | Schering Corp | Antagonistas del receptor de neuroquinina-1, composiciones farmaceuticas y el uso de dichos antagonistas para la preparacion de un medicamento |
PE20030762A1 (es) | 2001-12-18 | 2003-09-05 | Schering Corp | Compuestos heterociclicos como antagonistas nk1 |
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ATE384053T1 (de) * | 2002-04-26 | 2008-02-15 | Lilly Co Eli | Triazolderivate als tachykininrezeptor- antagonisten |
DE60312998T2 (de) * | 2002-07-03 | 2007-12-13 | Schering Corp. | 1-amido-4-phenyl-4-benzyloxymethyl-piperidin derivative und verwandte verbindungen als neurokinin-1 (nk-1) antagonsisten zur behandlung von erbrechen, depressionen, angstzustände und husten |
GB0308968D0 (en) * | 2003-04-17 | 2003-05-28 | Glaxo Group Ltd | Medicaments |
US7592348B2 (en) * | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
FR2873373B1 (fr) * | 2004-07-23 | 2006-09-08 | Sanofi Synthelabo | Derives de 4-arylmorpholin-3-one, leur preparation et leur application en therapeutique |
CN101641099A (zh) | 2007-01-24 | 2010-02-03 | 葛兰素集团有限公司 | 包含3,5-二氨基-6-(2,3-二氯苯基)-1,2,4-三嗪或r(-)-2,4-二氨基-5-(2,3-二氯苯基)-6-氟甲基嘧啶和nk1的药物组合物 |
JP5486928B2 (ja) | 2007-02-26 | 2014-05-07 | ヴァイティー ファーマシューティカルズ,インコーポレイテッド | 11β−ヒドロキシステロイドデヒドロゲナーゼ1のサイクリックウレアおよびカルバメートインヒビター |
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AR069207A1 (es) | 2007-11-07 | 2010-01-06 | Vitae Pharmaceuticals Inc | Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1 |
CA2708303A1 (en) | 2007-12-11 | 2009-06-18 | Vitae Pharmaceuticals, Inc. | Cyclic urea inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1 |
TW200934490A (en) | 2008-01-07 | 2009-08-16 | Vitae Pharmaceuticals Inc | Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1 |
CA2712500A1 (en) | 2008-01-24 | 2009-07-30 | Vitae Pharmaceuticals, Inc. | Cyclic carbazate and semicarbazide inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
EP2252598A2 (en) | 2008-02-11 | 2010-11-24 | Vitae Pharmaceuticals, Inc. | 1,3-oxazepan-2-one and 1,3-diazepan-2-one inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
EP2254872A2 (en) | 2008-02-15 | 2010-12-01 | Vitae Pharmaceuticals, Inc. | Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 |
JP5451752B2 (ja) | 2008-05-01 | 2014-03-26 | ヴァイティー ファーマシューティカルズ,インコーポレイテッド | 11β−ヒドロキシステロイドデヒドロゲナーゼ1の環状インヒビター |
JP5538365B2 (ja) | 2008-05-01 | 2014-07-02 | ヴァイティー ファーマシューティカルズ,インコーポレイテッド | 11β−ヒドロキシステロイドデヒドロゲナーゼ1の環状阻害剤 |
EP2291371B1 (en) | 2008-05-01 | 2015-06-10 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
KR20110002492A (ko) | 2008-05-01 | 2011-01-07 | 비타이 파마슈티컬즈, 인코포레이티드 | 11베타-하이드록시스테로이드 탈수소효소 1의 고리형 억제제 |
WO2010010157A2 (en) | 2008-07-25 | 2010-01-28 | Boehringer Ingelheim International Gmbh | INHIBITORS OF 11beta-HYDROXYSTEROID DEHYDROGENASE 1 |
CN102105454A (zh) | 2008-07-25 | 2011-06-22 | 贝林格尔.英格海姆国际有限公司 | 合成1型11β-羟基类固醇脱氢酶的抑制剂 |
CN102119160B (zh) | 2008-07-25 | 2014-11-05 | 贝林格尔·英格海姆国际有限公司 | 11β-羟基类固醇脱氢酶1的环状抑制剂 |
CN102203062B (zh) | 2008-09-05 | 2014-12-17 | 欧科生医股份有限公司 | 用于合成8-[{1-(3,5-双-(三氟甲基)苯基)-乙氧基}-甲基]-8-苯基-1,7-二氮杂-螺[4.5]癸-2-酮化合物的方法和中间体 |
WO2010089303A1 (en) | 2009-02-04 | 2010-08-12 | Boehringer Ingelheim International Gmbh | CYCLIC INHIBITORS OF 11 β-HYDROXYSTEROID DEHYDROGENASE 1 |
US8680093B2 (en) | 2009-04-30 | 2014-03-25 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
EP2440537A1 (en) | 2009-06-11 | 2012-04-18 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 based on the 1,3 -oxazinan- 2 -one structure |
US8883778B2 (en) | 2009-07-01 | 2014-11-11 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11 beta-hydroxysteroid dehydrogenase 1 |
BR112012003263A2 (pt) | 2009-08-14 | 2015-09-22 | Opko Health Inc | formulações intravenosas de antagonistas de neuroquinina-1 |
US8552212B2 (en) | 2009-11-05 | 2013-10-08 | Boehringer Ingelheim International Gmbh | Chiral phosphorus ligands |
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JP5860042B2 (ja) | 2010-06-16 | 2016-02-16 | ヴァイティー ファーマシューティカルズ,インコーポレイテッド | 置換5、6及び7員複素環、そのような化合物を含有する医薬及びそれらの使用 |
WO2011161128A1 (en) | 2010-06-25 | 2011-12-29 | Boehringer Ingelheim International Gmbh | Azaspirohexanones as inhibitors of 11-beta-hsd1 for the treatment of metabolic disorders |
AU2011325286B2 (en) | 2010-11-02 | 2015-04-16 | Boehringer Ingelheim International Gmbh | Pharmaceutical combinations for the treatment of metabolic disorders |
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EP3822265A1 (en) | 2019-11-15 | 2021-05-19 | Bayer AG | Substituted hydantoinamides as adamts7 antagonists |
EP3822268A1 (en) | 2019-11-15 | 2021-05-19 | Bayer Aktiengesellschaft | Substituted hydantoinamides as adamts7 antagonists |
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DE69327541T2 (de) * | 1992-10-28 | 2000-08-10 | Merck Sharp & Dohme Ltd., Hoddesdon | 4-arylmethyloxymethyl piperidine als tachykinin antagonisten |
GB9601680D0 (en) * | 1996-01-27 | 1996-03-27 | Pfizer Ltd | Therapeutic agents |
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CO5261559A1 (es) | 2003-03-31 |
HUP0301607A3 (en) | 2004-03-29 |
ECSP003828A (es) | 2002-02-25 |
CA2393672A1 (en) | 2001-06-21 |
CN1434805A (zh) | 2003-08-06 |
KR20020067548A (ko) | 2002-08-22 |
EP1237874A2 (en) | 2002-09-11 |
WO2001044200A3 (en) | 2001-12-13 |
IL150033A0 (en) | 2002-12-01 |
HUP0301607A2 (hu) | 2003-12-29 |
AU2097601A (en) | 2001-06-25 |
ES2258485T3 (es) | 2006-09-01 |
HK1045308A1 (zh) | 2002-11-22 |
DE60026169T2 (de) | 2006-11-09 |
ATE318259T1 (de) | 2006-03-15 |
MXPA02006017A (es) | 2002-12-05 |
EP1237874B1 (en) | 2006-02-22 |
ZA200204395B (en) | 2003-11-26 |
PE20011035A1 (es) | 2001-10-13 |
DE60026169D1 (de) | 2006-04-27 |
JP2003522739A (ja) | 2003-07-29 |
WO2001044200A2 (en) | 2001-06-21 |
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