AR068632A1 - Alquiltio pirimidinas como antagonistas de crth2 - Google Patents
Alquiltio pirimidinas como antagonistas de crth2Info
- Publication number
- AR068632A1 AR068632A1 ARP080104146A ARP080104146A AR068632A1 AR 068632 A1 AR068632 A1 AR 068632A1 AR P080104146 A ARP080104146 A AR P080104146A AR P080104146 A ARP080104146 A AR P080104146A AR 068632 A1 AR068632 A1 AR 068632A1
- Authority
- AR
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- Prior art keywords
- alkyl
- trihalogen
- mono
- substituted
- aryl
- Prior art date
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- C07D239/28—Heterocyclic 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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Abstract
Compuestos de pirimidina sustituida por alquiltio que tienen actividad del antagonista de CRTH2 (receptor quimioatrayente acoplado a proteína G, expresado en células Th2) utiles para el tratamiento o la profilaxis de enfermedades asociadas con la actividad de CRTH2, incluso el tratamiento de enfermedades alérgicas, enfermedades relacionadas con eosinofilo y enfermedades relacionadas con basofilo. Reivindicacion 1: Un compuesto caracterizado porque tiene la formula (1), o su sal, solvato, hidrato, estereoisomero o tautomero farmacéuticamente aceptable, en donde W es una ligadura simple, -(CH2)m-, -O-, -S(O)n-, -NR7-, -C(O)-, -C(O)O-, -C(O)NR7-, -NR7C(O)NR7- o -NR7C(O)O-; R1 es -CO2R9, -C(O)NR8aR8b, nitrilo o tetrazolilo; R2 es (a) hidrogeno; (b) halogeno; (c) alquilo C1-6; (d) alquilo C1-6 sustituido por arilo, hidroxi, carboxi, alcoxi, carbamoil, alquil C1-6carbamoil, di(alquil C1-6)carbamoil, cicloalquil C3-7carbamoil o heterociclil C3-7carbamoil; (e) alquilo C1-6 sustituido por mono-, di- o trihalogeno; (f) cicloalquilo C3-7; (g) -NR8aR8b; (h) -SR3 o (i) alcoxi C1-6 opcionalmente sustituido por mono-, di- o trihalogeno; cada R3 es independientemente (a) hidrogeno; (b) alquilo C1-6 opcionalmente sustituido por mono-, di- o trihalogeno; (c) cicloalquilo C3-7 o (d) -C(O)R9; R4a y R4b son cada uno seleccionado independientemente de hidrogeno o alquilo C1-6; cada R5 es independientemente (a) hidrogeno; (b) halogeno; (c) ciano; (d) nitro; (e) hidroxi; (f) fenilo; (g) feniloxi; (h) bencilo; (i) benciloxi; (j) guanidino; (k) heterociclilo; (l) -NR8aR8b; (m) sulfamoil; (n) alquilsulfonilo C1-6; (o) alquilaminosulfonilo C1-6; (p) dialquilaminosulfonilo C1-6; (q) -C(O)R9; (r) -C(O)OR9; (s) -C(O)NR8aR8b; (t) -OC(O)NR8aR8b; (u) -NR7C(O)OR9 (y) -NR7C(O)R9; (w) alquenilo C2-6; (x) alquilo C1-6 opcionalmente sustituido por mono-, di- o trihalogeno; (y) alcoxi C1-6 opcionalmente sustituido por mono-, di- o trihalogeno; o (z) alquiltio C1-6 opcionalmente sustituido por mono-, di- o trihalogeno; R6 es (a) hidrogeno; (b) alquilo C1-6; (c) alquenilo C2-6; (d) alquinilo C2-6; (e) cicloalquilo C3-7; (f) alquilo C1-6 sustituido por arilo o heteroarilo; (g) alquenilo C2-4 sustituido por arilo o heteroarilo; (h) alquilo C1-6 sustituido por mono-, di- o trihalogeno; (i) alquilo C1-6 sustituido por -C(O)R6a; j) alcoxi C1-6 sustituido por mono-, di- o trihalogeno; (k) alquiltio C1-6 sustituido por mono-, di- o trihalogeno; (l) arilo; (m) o heteroarilo, en donde dicho arilo y heteroarilo son opcionalmente sustituidos en una posicion sustituible con uno o más sustituyentes seleccionados del grupo que consiste en (a) halogeno; (b) ciano; (c) nitro; (d) hidroxi; (e) guanidino; (f) heterociclilo; (g) fenilo; (h) feniloxi; (i) bencilo; (j) benciloxi; (k) -NR8aR8b; (l) -C(O)R9; (m) -C(O)NR8aR8b; (n) -OC(O)NR8aR8b; (o) -C(O)OR9; (p) -NR7C(O)OR9; (q) -NR7C(O)R9; (r) sulfamoil; (s) alquilsulfonilo C1-6; (t) alquilaminosulfonilo C1-6; (u) dialquilaminosulfonilo C1-6; (y) alquilo C1-6 opcionalmente sustituido por mono-, di- o trihalogeno; (w) alcoxi C1-6 opcionalmente sustituido por mono-, di- o trihalogeno; y (x) alquiltio C1-6 opcionalmente sustituido por mono-, di- o trihalogeno; R6a es (a) hidrogeno; (b) alquilo C1-6; (c) alquenilo C2-6; (d) alquinilo C2-6; (e) cicloalquilo C3-7; (f) alquilo C1-6 sustituido por arilo o heteroarilo; (g) alquenilo C2-4 sustituido por arilo o heteroarilo; (h) alquilo C1-6 sustituido por mono-, di- o trihalogeno; (i) alcoxi C1-6 sustituido por mono-, di- o trihalogeno; (j) alquiltio C1-6 sustituido por mono-, di- o trihalogeno; (k) arilo; (l) o heteroarilo, en donde dicho arilo y heteroarilo son opcionalmente sustituidos en una posicion sustituible por uno o más sustituyentes seleccionados del grupo que consiste en (a) halogeno; (b) ciano; (c) nitro; (d) hidroxi; (e) guanidino; (f) heterociclilo; (g) fenilo; (h) feniloxi; (i) bencilo; j) benciloxi; (k) NR8aR8b; (l) -C(O)R9; (m) -C(O)NR8aR8b; (n) -OC(O)NR8aR8b; (o) -C(O)OR9 (p) -NR7C(O)OR9; (q) -NR7C(O)R9 (r) sulfamoil; (s) alquilsulfonilo C1-6; (t) alquilaminosulfonilo C1-6; (J) dialquilaminosulfonilo C1-6; (y) alquilo C1-6 opcionalmente sustituido por mono-, di- o trihalogeno; (w) alcoxi C1-6 opcionalmente sustituido por mono, di- o trihalogeno; y (x) alquiltio C1-6 opcionalmente sustituido por mono-, di- o trihalogeno; R7 es (a) hidrogeno; (b) alquilo C1-6; (c) fenilo; (d) alquilo C1-6 sustituido por arilo, hidroxi, carboxi, alcoxi, carbamoil, alquil C1-6carbamoil, di(alquil)carbamoil C1-6, cicloalquil C3-7carbamoil C3-7 o heterociclil C3-7carbamoil; (e) alquilo C1-6 sustituido por mono-, di- o trihalogeno; o (f) cicloalquilo C3-7; en cada caso, independientemente, R8a y R8b se seleccionan de (i) o (ii) de la siguiente manera, (i) R8a y R8b son cada uno seleccionado independientemente de (a) hidrogeno; (b) alquilo C1-6; (e) fenilo; (d) alquilo C1-6 sustituido por arilo, hidroxi, carboxi, alcoxi, carbamoil, alquil C1-6carbamoil, di(alquil C1-6)carbamoil, cicloalquil C3-7carbamoil o heterociclil C3-7carbamoil; (e) alquilo C1-6 sustituido por mono-, di- o trihalogeno; o (f) cicloalquilo C3-7; o (ii) cada R8a y R8b, junto con el N al cual se encuentran ligados, independientemente pueden formar un anillo saturado o no saturado de 3 a miembros que opcionalmente contiene en el anillo uno o más átomos O o S, o uno o más átomos N adicionales; cada R9 es independientemente (a) hidrogeno; (b) alquilo C1-6; (c) fenilo; o (d) alquilo C1-6 sustituido por arilo, alcoxi o mono-, di-, o trihalogeno; k es 0, 1 o 2; m es 1, 2, 3 o 4; y n es 0, 1 o 2.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US99538607P | 2007-09-25 | 2007-09-25 |
Publications (1)
Publication Number | Publication Date |
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AR068632A1 true AR068632A1 (es) | 2009-11-25 |
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Application Number | Title | Priority Date | Filing Date |
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ARP080104146A AR068632A1 (es) | 2007-09-25 | 2008-09-24 | Alquiltio pirimidinas como antagonistas de crth2 |
Country Status (25)
Country | Link |
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US (1) | US8324229B2 (es) |
EP (1) | EP2205569B1 (es) |
JP (1) | JP5524847B2 (es) |
KR (1) | KR20100061747A (es) |
CN (1) | CN101874023A (es) |
AR (1) | AR068632A1 (es) |
AT (1) | ATE547407T1 (es) |
AU (1) | AU2008305632B2 (es) |
BR (1) | BRPI0817319A2 (es) |
CA (1) | CA2700524C (es) |
CL (1) | CL2008002826A1 (es) |
CY (1) | CY1112720T1 (es) |
DK (1) | DK2205569T3 (es) |
ES (1) | ES2383249T3 (es) |
HR (1) | HRP20120377T1 (es) |
IL (1) | IL205647A0 (es) |
MX (1) | MX2010003182A (es) |
NZ (1) | NZ584352A (es) |
PL (1) | PL2205569T3 (es) |
PT (1) | PT2205569E (es) |
RU (1) | RU2491280C2 (es) |
SI (1) | SI2205569T1 (es) |
TW (1) | TW200922587A (es) |
WO (1) | WO2009042138A1 (es) |
ZA (1) | ZA201002173B (es) |
Families Citing this family (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AR068633A1 (es) | 2007-09-25 | 2009-11-25 | Actimis Pharmaceuticals Inc | Pirimidinas sustituidas con 2-s- bencilo como antagonistas de crth2 |
CN101903394B (zh) * | 2007-10-18 | 2013-12-25 | 贝林格尔.英格海姆国际有限公司 | 二氢噻吩并[3,2-d]嘧啶的制备及其中使用的中间体 |
EP2393492A1 (en) * | 2009-02-09 | 2011-12-14 | Boehringer Ingelheim International GmbH | New pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders |
HUE025318T2 (en) * | 2010-01-27 | 2016-02-29 | Boehringer Ingelheim Int | Pyrazole Compounds as CRTH2 antagonists |
JP2013535457A (ja) * | 2010-07-28 | 2013-09-12 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 呼吸器系及び炎症性疾患の治療用医薬組成物 |
EP2457900A1 (en) | 2010-11-25 | 2012-05-30 | Almirall, S.A. | New pyrazole derivatives having CRTh2 antagonistic behaviour |
US8759386B2 (en) | 2011-01-24 | 2014-06-24 | Boehringer Ingelheim International Gmbh | Pyrazole compounds as CRTH2 antagonists |
WO2012130633A1 (en) | 2011-03-25 | 2012-10-04 | Boehringer Ingelheim International Gmbh | Pyrazole compounds as crth2 antagonists |
GB2494277A (en) | 2011-08-29 | 2013-03-06 | Univ Heriot Watt | Electro-spinning nanofibres onto a moving wire card |
CA2856100C (en) * | 2011-11-17 | 2016-09-27 | Kbp Biosciences Co., Ltd. | Nitrogen-containing fused ring compounds as crth2 antagonists |
Family Cites Families (12)
Publication number | Priority date | Publication date | Assignee | Title |
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BE790679A (fr) | 1971-11-03 | 1973-04-27 | Ici Ltd | Derives de l'indole |
GB9125842D0 (en) | 1991-12-04 | 1992-02-05 | Ici Plc | Heterocyclic derivatives |
CA2147275A1 (en) * | 1992-10-16 | 1994-04-28 | Hirokazu Yamada | Pyrimidine derivative |
GB2359078A (en) | 2000-02-11 | 2001-08-15 | Astrazeneca Uk Ltd | Pharmaceutically active pyrimidine derivatives |
JP2001302667A (ja) | 2000-04-28 | 2001-10-31 | Bayer Ag | イミダゾピリミジン誘導体およびトリアゾロピリミジン誘導体 |
US6878522B2 (en) | 2000-07-07 | 2005-04-12 | Baiyong Li | Methods for the identification of compounds useful for the treatment of disease states mediated by prostaglandin D2 |
EP1413306A1 (en) | 2002-10-21 | 2004-04-28 | Warner-Lambert Company LLC | Tetrahydroquinoline derivatives as CRTH2 antagonists |
ES2401079T3 (es) | 2002-12-20 | 2013-04-16 | Amgen Inc. | Moduladores del asma y de la inflamación alérgica |
DE60303238T2 (de) * | 2003-04-25 | 2006-09-14 | Actimis Pharmaceuticals, Inc., La Jolla | Pyrimidin-Essigsäure Derivate geeignet zur Behandlung von CRTH2-bedingten Krankheiten |
RU2373208C2 (ru) * | 2004-01-31 | 2009-11-20 | Актимис Фармасьютикалз, Инк. | Производные имидазо[1,2-c]пиримидинилуксусной кислоты |
WO2007062677A1 (en) * | 2005-11-30 | 2007-06-07 | 7Tm Pharma A/S | Thiazolyl- and pyrimidinyl-acetic acids and their use as crth2 receptor ligands |
AR068633A1 (es) | 2007-09-25 | 2009-11-25 | Actimis Pharmaceuticals Inc | Pirimidinas sustituidas con 2-s- bencilo como antagonistas de crth2 |
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- 2008-09-24 EP EP08833849A patent/EP2205569B1/en not_active Not-in-force
- 2008-09-24 KR KR1020107008867A patent/KR20100061747A/ko not_active Application Discontinuation
- 2008-09-24 CN CN200880117669A patent/CN101874023A/zh active Pending
- 2008-09-24 AU AU2008305632A patent/AU2008305632B2/en not_active Expired - Fee Related
- 2008-09-24 JP JP2010526927A patent/JP5524847B2/ja active Active
- 2008-09-24 CA CA2700524A patent/CA2700524C/en not_active Expired - Fee Related
- 2008-09-24 AT AT08833849T patent/ATE547407T1/de active
- 2008-09-24 AR ARP080104146A patent/AR068632A1/es not_active Application Discontinuation
- 2008-09-24 ES ES08833849T patent/ES2383249T3/es active Active
- 2008-09-24 WO PCT/US2008/011053 patent/WO2009042138A1/en active Application Filing
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- 2008-09-24 NZ NZ584352A patent/NZ584352A/en not_active IP Right Cessation
- 2008-09-24 PT PT08833849T patent/PT2205569E/pt unknown
- 2008-09-24 CL CL2008002826A patent/CL2008002826A1/es unknown
- 2008-09-24 TW TW097136691A patent/TW200922587A/zh unknown
- 2008-09-24 SI SI200830609T patent/SI2205569T1/sl unknown
- 2008-09-24 MX MX2010003182A patent/MX2010003182A/es active IP Right Grant
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2010
- 2010-03-26 ZA ZA2010/02173A patent/ZA201002173B/en unknown
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2012
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Also Published As
Publication number | Publication date |
---|---|
PL2205569T3 (pl) | 2012-08-31 |
AU2008305632A1 (en) | 2009-04-02 |
IL205647A0 (en) | 2011-07-31 |
JP5524847B2 (ja) | 2014-06-18 |
AU2008305632B2 (en) | 2014-01-30 |
CL2008002826A1 (es) | 2009-08-07 |
EP2205569B1 (en) | 2012-02-29 |
BRPI0817319A2 (pt) | 2015-03-17 |
RU2010116293A (ru) | 2011-11-10 |
WO2009042138A1 (en) | 2009-04-02 |
KR20100061747A (ko) | 2010-06-08 |
DK2205569T3 (da) | 2012-05-21 |
US20100298361A1 (en) | 2010-11-25 |
ZA201002173B (en) | 2011-05-25 |
ES2383249T3 (es) | 2012-06-19 |
EP2205569A1 (en) | 2010-07-14 |
CA2700524A1 (en) | 2009-04-02 |
RU2491280C2 (ru) | 2013-08-27 |
JP2010540520A (ja) | 2010-12-24 |
US8324229B2 (en) | 2012-12-04 |
TW200922587A (en) | 2009-06-01 |
CN101874023A (zh) | 2010-10-27 |
HRP20120377T1 (hr) | 2012-05-31 |
ATE547407T1 (de) | 2012-03-15 |
CY1112720T1 (el) | 2016-02-10 |
CA2700524C (en) | 2017-08-01 |
WO2009042138A9 (en) | 2009-10-15 |
MX2010003182A (es) | 2010-06-02 |
PT2205569E (pt) | 2012-05-25 |
SI2205569T1 (sl) | 2012-06-29 |
NZ584352A (en) | 2012-03-30 |
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