JP2011016800A5 - - Google Patents
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- JP2011016800A5 JP2011016800A5 JP2010152958A JP2010152958A JP2011016800A5 JP 2011016800 A5 JP2011016800 A5 JP 2011016800A5 JP 2010152958 A JP2010152958 A JP 2010152958A JP 2010152958 A JP2010152958 A JP 2010152958A JP 2011016800 A5 JP2011016800 A5 JP 2011016800A5
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- 0 *[n]1ncc2ccccc12 Chemical compound *[n]1ncc2ccccc12 0.000 description 1
Claims (35)
- 自己免疫疾患を治療するための医薬の調製における、構造式(I)で表される2,4−ピリミジンジアミン化合物:
該自己免疫疾患は、橋本甲状腺炎、自己免疫性溶血性貧血、悪性貧血による自己免疫性萎縮性胃炎、自己免疫性脳脊髄炎、自己免疫性精巣炎、グッドパスチャー病、自己免疫性血小板減少症、交感性眼炎、重症筋無力症、グレーブス病、原発性胆汁性肝硬変、慢性侵攻性肝炎、糸球体腎炎、膜性糸球体腎炎および全身性自己免疫障害を伴う自己免疫疾患からなる群より選択され、ここで、
R2は、R 50 基で3位または5位で一置換されたフェニル、同一もしくは異なったR 51 基で3、4位または3、5位で二置換されたフェニルまたは同一または異なったR 51 基で3、4、5位で三置換されたフェニル、および任意的に置換された5‐15員ヘテロアリールから成る群から選択されており;
R4は、R 50 基で3位、4位または5位で一置換されたフェニル、同一もしくは異なったR 51 基で3、4位または3、5位で二置換されたフェニル、または同一もしくは異なったR 51 基で3、4、5位で三置換されたフェニル、および任意的に置換された5‐15員ヘテロアリールから成る群から選択されており;
R 2 及びR 4 において、前記任意的に置換された5‐15員ヘテロアリールは、互いに独立して、下記からなる群から選択され;
及び
R5は、−CN、−NC、−NO 2 、フルオロ、(C1−C6)アルキル、(C1−C3)ハロアルキル、(C1−C3)ペルハロアルキル、(C1−C3)フルオロアルキル、(C1−C3)ペルフルオロアルキル、−CF 3 、(C1−C3)ハロアルコキシ、(C1−C3)ペルハロアルコキシ、(C1−C3)フルオロアルコキシ、(C1−C3)ペルフルオロアルコキシ、−OCF 3 、−C(O)R a 、−C(O)OR a 、−C(O)CF 3 および−C(O)OCF 3 から成る群から選択されており;
R 8 は、R e 、Rb、一つ以上の同一または異なったRaあるいはRb で置換されたR e 、一つ以上の同一または異なったRaあるいはRbで置換された−ORa、−B(ORa)2、−B(NRcRc)2、−(CH2)m−Rb、−(CHRa)m−Rb、−O−(CH2)m−Rb、−S−(CH2)m−Rb、−O−CHRaRb、−O−CRa(Rb)2、−O−(CHRa)m−Rb、−O−(CH2)m−CH[(CH2)mRb]Rb、−S−(CHRa)m−Rb、−C(O)NH−(CH2)m−Rb、−C(O)NH−(CHRa)m−Rb、−O−(CH2)m−C(O)NH−(CH2)m−Rb、−S−(CH2)m−C(O)NH−(CH2)m−Rb、−O−(CHRa)m−C(O)NH−(CHRa)m−Rb、−S−(CHRa)m−C(O)NH−(CHRa)m−Rb、−NH−(CH2)m−Rb、−NH−(CHRa)m−Rb、−NH[(CH2)mRb]、−N[(CH2)mRb]2、−NH−C(O)−NH−(CH2)m−Rb、−NH−C(O)−(CH2)m−CHRbRbおよび−NH−(CH2)m−C(O)−NH−(CH2)m−Rbから成る群から選択され;
ここで、
pは1から3までの整数であり;
各− − −はそれぞれ独立して単一結合または二重結合を表し;
R 35 は水素あるいはR 8 であり;
各XはCH、NおよびN−Oから成る群から選択され;
各Yは、それぞれO、SおよびNHから成る群から独立して選択され:
各Y 1 は、それぞれO、S、SO、SO 2 、SONR 36 、NHおよびNR 37 から成る群から独立して選択され;
各Y 2 は、それぞれCH、CH 2 、O、S、N、NHおよびNR 37 から成る群から独立して選択され;
各R 36 は水素またはアルキルであり;
各R 37 は、水素並びに、アリール、アリールアルキル、ヘテロアリール、R a 、R b 、−CR a R b −O−C(O)R 8 、−CR a R b− O−PO(OR 8 ) 2 、−CH 2 −O−PO(OR 8 ) 2 、−CH 2 −PO(OR 8 ) 2 、−C(O)−CR a R b −N(CH 3 ) 2 、−CR a R b −O−C(O)−CR a R b −N(CH 3 ) 2 、−C(O)R 8 、−C(O)CF 3 および−C(O)−NR 8 −C(O)R 8 から成る群から選択されたプログループからなる群より選択され;
各R 38 はアルキルおよびアリールから成る群から選択され;
AはO、NHおよびNR 38 から成る群から選択され;
R 9 、R 10 、R 11 およびR 12 はそれぞれに互いに独立して、アルキル、アルコキシ、ハロゲン、ハロアルコキシ、アミノアルキルおよびヒドロキシアルキルから成る群から選択されるか、またはR 9 とR 10 および/もしくはR 11 とR 12 は一緒になって、オキソ基を形成し;
各Zは、ヒドロキシル、アルコキシ、アリールオキシ、エステル、およびカルバメートから成る群から選択され;
各Qは−OH、−OR 8 、−NR c R c 、−NR 39 −CHR 40 −R b 、−NR 39 −(CH 2 ) m −R b および−NR 39 −C(O)−CHR 40 −NR c R c から成る群から選択され;
各R 39 およびR 40 はそれぞれに互いに独立して、水素、アルキル、アリール、アルキルアリール、アリールアルキルおよびNHR 8 から成る群から選択され;
各R 50 は、(C1−C10)アルキル、(C1−C10)分岐アルキル、一つ以上の同一または異なったR b 基で任意的に置換された−OR a 、−O−C(O)OR a 、−O−(CH 2 ) m −C(O)OR a 、−C(O)OR a 、−O−(CH 2 ) m −NR c R c 、−O−C(O)NR c R c 、−O−(CH 2 ) m −C(O)NR c R c 、−O−C(NH)NR c R c 、−O−(CH 2 ) m −C(NH)NR c R c 、及び−NH−(CH 2 ) m −NR c R c からなる群から独立して選択され;
各R 51 は、(C1−C6)アルキル、(C1−C6)アルコキシ、メトキシ、ハロ、クロロ、(C1−C6)ペルハロアルキル、−CF 3 、(C1−C6)ペルハロアルコキシ、及び−OCF 3 からなる群から独立して選択され、
各Raは、水素、(C1−C6)アルキル、(C3−C8)シクロアルキル、シクロヘキシル、(C4−C11)シクロアルキルアルキル、(C5−C10)アリール、フェニル、(C6−C16)アリールアルキル、ベンジル、2‐6員ヘテロアルキル、3‐8員シクロヘテロアルキル、モルホリニル、ピペラジニル、ホモピペラジニル、ピペリジニル、4‐11員シクロヘテロアルキルアルキル、5‐10員ヘテロアリール、および6‐16員ヘテロアリールアルキルから成る群から独立して選択され;
各Rbは、=O、−ORd、(C1−C3)ハロアルキロキシ、=S、−SRd、=NRd、=NORd、−NRcRc、ハロゲン、−CF3、−CN、−NC、−OCN、−SCN、−NO、−NO2、=N2、−N3、−S(O)Rd、−S(O)2Rd、−S(O)2ORd、−S(O)NRcRc、−S(O)2NRcRc、−OS(O)Rd、−OS(O)2Rd、−OS(O)2ORd、−OS(O)2NRcRc、−C(O)Rd、−C(O)ORd、−C(O)NRcRc、−C(NH)NRcRc、−C(NRa)NRcRc、−C(NOH)Ra、−C(NOH)NRcRc、−OC(O)Rd、−OC(O)ORd、−OC(O)NRcRc、−OC(NH)NRcRc、−OC(NRa)NRcRc、−[NHC(O)]nRd、−[NRaC(O)]nRd、−[NHC(O)]nORd、−[NRaC(O)]nORd、−[NHC(O)]nNRcRc、−[NRaC(O)]nNRcRc、−[NHC(NH)]nNRcRc、および−[NRaC(NRa)]nNRcRcから成る群から独立して選択される適切な基であり;
各Rcは、独立してR a であるか、あるいはまた2つのRcは、各々が結合している窒素原子と一まとめになり、一つ以上の同一あるいは異なった追加的へテロ原子を任意的に含み得かつ一つ以上の同一または異なったRaあるいは適切なRb基で任意的に置換され得る、5‐8員シクロヘテロアルキルまたはへテロアリールを形成しており;
各Rdは独立してRaであり;
各R e は、(C1−C6)アルキル、(C3−C8)シクロアルキル、シクロヘキシル、(C4−C11)シクロアルキルアルキル、(C5−C10)アリール、フェニル、(C6−C16)アリールアルキル、ベンジル、2−6員へテロアルキル、3−8員シクロヘテロアルキル、モルホリニル、ピペラジニル、ホモピペラジニル、ピペリジニル、4−11員シクロヘテロアルキルアルキル、5−10員ヘテロアリール、および6−16員ヘテロアリールアルキルから成る群から独立して選択されており;
各mは独立して1から3までの整数であり;そして
各nは独立して0から3までの整数であり、
以下の条件を備えたものである:
R2が置換フェニルである場合、R5はシアノまたは−C(O)NHR以外のものであり、ここでRは、水素または(C1−C6)アルキルである、
使用。 - R2とR4が同一である、請求項1に記載の使用。
- 各R35が独立して水素、Rd、−NRcRc、−(CH2)m−NRcRc、−C(O)NRcRc、−(CH2)m−C(O)NRcRc、−C(O)ORd、−(CH2)m−C(O)ORdおよび−(CH2)m−ORdから成る群から選択されている、請求項1または2に記載の使用。
- 各mが1である、請求項1に記載の使用。
- R2が環の炭素原子により分子の残りの部分に付着している任意的に置換されているヘテロアリールである、請求項1に記載の使用。
- R4が環の炭素原子により分子の残りの部分に付着している任意的に置換されているヘテロアリールである、請求項1に記載の使用。
- Y 1 が酸素、Y 2 がNH、および一つ以上のR 35 部分がアルキル基である、請求項8に記載の使用。
- 同一の炭素原子に結合している二つのR 35 が、それぞれメチルである、請求項9に記載の使用。
- R 5 がフルオロ及び(C1−C3)フルオロアルキルからなる群から選択される、請求項1に記載の使用。
- R 5 がフルオロ及び−CF 3 から選択される、請求項12に記載の使用。
- R2およびR4 の一方または両方が互いに独立して、置換されたフェニルである、請求項1に記載の使用。
- R2およびR4が各々、同一または異なった置換フェニルである、請求項14に記載の使用。
- 前記置換されたフェニルが一置換である、請求項14あるいは15に記載の使用。
- 前記置換されたフェニルが二置換である、請求項14または15に記載の使用。
- 前記置換されたフェニルが三置換である、請求項14または15に記載の使用。
- R2とR4が同一である、請求項15に記載の使用。
- R4が任意的に置換されたヘテロアリールである、請求項22に記載の使用。
- R18が−O−CH2−C(O)−NHCH3である、請求項22に記載の使用。
- 前記2,4−ピリミジンジアミン化合物が、R926891、R940323、R940347、およびR921303からなる群から選択される、請求項1に記載の使用。
- 前記2,4−ピリミジンジアミン化合物が、(S)−R909317、(R)−R909317、R926970、R940361、R940363、R940366、およびR940368からなる群から選択される、請求項1に記載の使用。
- 前記2,4−ピリミジンジアミン化合物が、R908592、R935432、R935461、R940364、R940380、R940395、およびR950423からなる群から選択される、請求項1に記載の使用。
- 前記医薬が、前記化合物および薬学的に使用可能なキャリア、希釈剤あるいは賦形剤を含む薬学的組成物の形態である、請求項1−27のいずれか一項に記載の使用。
- 前記自己免疫疾患が、全身性の自己免疫障害を含む、請求項1−28のいずれか一項に記載の使用。
- 前記自己免疫疾患が、橋本甲状腺炎、自己免疫性溶血性貧血、悪性貧血による自己免疫性萎縮性胃炎、自己免疫性脳脊髄炎、自己免疫性精巣炎、グッドパスチャー病、自己免疫性血小板減少症、交感性眼炎、重症筋無力症、グレーブス病、原発性胆汁性肝硬変、慢性侵攻性肝炎、および膜性糸球体腎炎から成る群から選択されている、請求項1−28のいずれか一項に記載の使用。
- 前記自己免疫疾患が、全身性エリテマトーデス、関節リウマチ、シェーグレン症候群、ライター症候群、多発性筋炎・皮膚筋炎、全身性硬化症、結節性多発性動脈炎、多発性硬化症および水疱性類天疱瘡から成る群より選択されている、請求項1−28のいずれか一項に記載の使用。
- 前記自己免疫疾患が全身性エリテマトーデスである、請求項31に記載の使用。
- 前記自己免疫疾患が関節リウマチである、請求項31に記載の使用。
- 前記自己免疫疾患が多発性硬化症である、請求項31に記載の使用。
- 前記自己免疫疾患が、糸球体腎炎である、請求項1−28のいずれか一項に記載の使用。
Applications Claiming Priority (8)
Application Number | Priority Date | Filing Date | Title |
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US39967302P | 2002-07-29 | 2002-07-29 | |
US60/399,673 | 2002-07-29 | ||
US44394903P | 2003-01-31 | 2003-01-31 | |
US60/443,949 | 2003-01-31 | ||
US45233903P | 2003-03-06 | 2003-03-06 | |
US60/452,339 | 2003-03-06 | ||
US10/631,029 | 2003-07-29 | ||
US10/631,029 US7517886B2 (en) | 2002-07-29 | 2003-07-29 | Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds |
Related Parent Applications (1)
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JP2005506142A Division JP2006514989A (ja) | 2002-07-29 | 2003-07-29 | 2,4−ピリミジンジアミン化合物による自己免疫疾患の治療および予防方法 |
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JP2011016800A JP2011016800A (ja) | 2011-01-27 |
JP2011016800A5 true JP2011016800A5 (ja) | 2011-09-29 |
JP5441841B2 JP5441841B2 (ja) | 2014-03-12 |
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JP2005506142A Pending JP2006514989A (ja) | 2002-07-29 | 2003-07-29 | 2,4−ピリミジンジアミン化合物による自己免疫疾患の治療および予防方法 |
JP2010152958A Expired - Fee Related JP5441841B2 (ja) | 2002-07-29 | 2010-07-05 | 2,4−ピリミジンジアミン化合物による自己免疫疾患の処置または予防の方法 |
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Country Status (25)
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US (5) | US7517886B2 (ja) |
EP (1) | EP1534286B1 (ja) |
JP (2) | JP2006514989A (ja) |
CN (2) | CN103169708B (ja) |
AT (1) | ATE451104T1 (ja) |
AU (1) | AU2003265336B8 (ja) |
BR (1) | BR0313059B8 (ja) |
CA (1) | CA2492325C (ja) |
CY (1) | CY1110292T1 (ja) |
DE (1) | DE60330466D1 (ja) |
DK (1) | DK1534286T3 (ja) |
ES (2) | ES2337782T3 (ja) |
HK (2) | HK1079978A1 (ja) |
HR (1) | HRP20050089B1 (ja) |
IL (3) | IL166241A (ja) |
IS (1) | IS2923B (ja) |
MX (1) | MXPA05001096A (ja) |
NO (1) | NO332550B1 (ja) |
NZ (1) | NZ537752A (ja) |
PL (1) | PL216744B1 (ja) |
RS (1) | RS51752B (ja) |
RU (1) | RU2659777C9 (ja) |
SE (1) | SE0500203L (ja) |
SG (1) | SG176311A1 (ja) |
WO (1) | WO2004014382A1 (ja) |
Families Citing this family (172)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
MXPA05001096A (es) * | 2002-07-29 | 2005-11-23 | Rigel Pharmaceuticals Inc | Metodos para tratamiento o prevencion de enfermedades autoinmunes con compuestos de 2,4-diamino-pirimidina. |
CN1717396A (zh) * | 2002-11-28 | 2006-01-04 | 舍林股份公司 | Chk-、Pdk-和Akt-抑制嘧啶,其制备及作为药物的用途 |
UA80767C2 (en) * | 2002-12-20 | 2007-10-25 | Pfizer Prod Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
CL2004000306A1 (es) * | 2003-02-20 | 2005-04-08 | Tibotec Pharm Ltd | Compuestos derivados de pirimidina sustituidas con indano; proceso para su preparacion; composicion farmaceutica que lo comprende; combinacion farmaceutica; y su uso para el tratamiento o profilaxis de una enfermedad infecciosa. |
US8178671B2 (en) * | 2003-07-30 | 2012-05-15 | Rigel Pharmaceuticals, Inc. | Methods of treating or preventing autoimmune diseases with 2, 4-pyrimidinediamine compounds |
AU2004261484A1 (en) * | 2003-07-30 | 2005-02-10 | Cyclacel Limited | 2-aminophenyl-4-phenylpyrimidines as kinase inhibitors |
JP4741491B2 (ja) * | 2003-08-07 | 2011-08-03 | ライジェル ファーマシューティカルズ, インコーポレイテッド | 抗増殖剤としての2,4−ピリミジンジアミン化合物および使用 |
SI1660458T1 (sl) * | 2003-08-15 | 2012-05-31 | Novartis Ag | pirimidindiamini uporabni pri zdravljenju neoplastičnih bolezni vnetnih motenj in motenj imunskega sistema |
RU2006139258A (ru) | 2004-04-08 | 2008-05-20 | Таргеджен, Инк. (US) | Бензотриазиновые ингибиторы киназ |
WO2005118544A2 (en) | 2004-05-18 | 2005-12-15 | Rigel Pharmaceuticals, Inc. | Cycloalkyl substituted pyrimidinediamine compounds and their uses |
AU2005276974B2 (en) | 2004-08-25 | 2012-08-02 | Targegen, Inc. | Heterocyclic compounds and methods of use |
US20060058525A1 (en) * | 2004-09-01 | 2006-03-16 | Rajinder Singh | Synthesis of 2,4-pyrimidinediamine compounds |
RU2007110731A (ru) | 2004-09-23 | 2008-10-27 | Редди Юс Терапевтикс | Новые соединения пиримидина, способ их получения и содержащие их композиции |
GB2420559B (en) | 2004-11-15 | 2008-08-06 | Rigel Pharmaceuticals Inc | Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses |
WO2006068770A1 (en) * | 2004-11-24 | 2006-06-29 | Rigel Pharmaceuticals, Inc. | Spiro-2, 4-pyrimidinediamine compounds and their uses |
MY169441A (en) * | 2004-12-08 | 2019-04-11 | Janssen Pharmaceutica Nv | 2,4, (4,6) pyrimidine derivatives |
US7799778B1 (en) | 2005-01-12 | 2010-09-21 | Alcon, Inc. | 5-substituted 2-aminopyridine analogs for treating allergic and inflammatory diseases |
US7713975B1 (en) | 2005-01-12 | 2010-05-11 | Alcon, Inc. | 3,6-substituted imidazol[1,2-b]pyridazine analogs for treating allergic and inflammatory diseases |
DE602006010979D1 (de) * | 2005-01-19 | 2010-01-21 | Rigel Pharmaceuticals Inc | Prodrugs aus 2,4-pyrimidindiamin-verbindungen und ihre verwendungen |
AU2006209216A1 (en) | 2005-01-25 | 2006-08-03 | Galenea Corp | Substituted arylamine compounds and their use as 5-HT6 modulators |
US8227455B2 (en) * | 2005-04-18 | 2012-07-24 | Rigel Pharmaceuticals, Inc. | Methods of treating cell proliferative disorders |
CA2604551A1 (en) * | 2005-05-03 | 2007-03-08 | Rigel Pharmaceuticals, Inc. | Jak kinase inhibitors and their uses |
US20070203161A1 (en) * | 2006-02-24 | 2007-08-30 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
EP1904457B1 (en) | 2005-06-08 | 2017-09-06 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
CA2607901C (en) | 2005-06-13 | 2016-08-16 | Rigel Pharmaceuticals, Inc. | Methods and compositions for treating degenerative bone disorders using a syk inhibitory 2,4-pyrimidinediamine |
WO2006138304A2 (en) * | 2005-06-14 | 2006-12-28 | Taigen Biotechnology | Pyrimidine compounds |
PT1734251E (pt) * | 2005-06-17 | 2007-03-30 | Magneti Marelli Powertrain Spa | Injector de combustível |
US20070032514A1 (en) * | 2005-07-01 | 2007-02-08 | Zahn Stephan K | 2,4-diamino-pyrimidines as aurora inhibitors |
TW200740805A (en) * | 2005-07-15 | 2007-11-01 | Glaxo Group Ltd | Novel compounds |
WO2007028445A1 (en) * | 2005-07-15 | 2007-03-15 | Glaxo Group Limited | 6-indolyl-4-yl-amino-5-halogeno-2-pyrimidinyl-amino derivatives |
NZ592990A (en) * | 2005-11-01 | 2013-01-25 | Targegen Inc | Bi-aryl meta-pyrimidine inhibitors of kinases |
US8133900B2 (en) | 2005-11-01 | 2012-03-13 | Targegen, Inc. | Use of bi-aryl meta-pyrimidine inhibitors of kinases |
US8604042B2 (en) | 2005-11-01 | 2013-12-10 | Targegen, Inc. | Bi-aryl meta-pyrimidine inhibitors of kinases |
US7713987B2 (en) * | 2005-12-06 | 2010-05-11 | Rigel Pharmaceuticals, Inc. | Pyrimidine-2,4-diamines and their uses |
WO2007111720A2 (en) * | 2005-12-06 | 2007-10-04 | Rigel Pharmaceuticals, Inc. | Formulation of insoluble small molecule therapeutics in lipid-based carriers |
WO2007085540A1 (en) * | 2006-01-27 | 2007-08-02 | Glaxo Group Limited | 1h-indaz0l-4-yl-2 , 4-pyrimidinediamine derivatives |
KR101411695B1 (ko) * | 2006-02-17 | 2014-07-03 | 리겔 파마슈티칼스, 인크. | 자가면역 질환의 치료 또는 예방을 위한 2,4-피리미딘디아민 화합물 |
US8962643B2 (en) | 2006-02-24 | 2015-02-24 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the JAK pathway |
US8623887B2 (en) * | 2006-05-15 | 2014-01-07 | Boehringer Ingelheim International Gmbh | Compounds |
CA2673125C (en) | 2006-10-19 | 2015-04-21 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
CA2669111C (en) | 2006-10-23 | 2016-04-12 | Cephalon, Inc. | Fused bicyclic derivatives of 2,4-diaminopyrimidine as alk and c-met inhibitors |
ES2380551T3 (es) | 2006-11-21 | 2012-05-16 | Rigel Pharmaceuticals, Inc. | Sales de profármaco de compuestos de 2,4-pirimidindiamina y sus usos |
WO2008118822A1 (en) | 2007-03-23 | 2008-10-02 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
US7834024B2 (en) | 2007-03-26 | 2010-11-16 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the JAK pathway |
RU2455994C2 (ru) | 2007-04-16 | 2012-07-20 | Хатчисон Медифарма Энтерпрайзис Лимитед | Пиримидиновые производные |
EA016679B1 (ru) | 2007-04-18 | 2012-06-29 | Пфайзер Продактс Инк. | Сульфониламидные производные для лечения аномального роста клеток |
WO2008135786A1 (en) * | 2007-05-04 | 2008-11-13 | Astrazeneca Ab | Amino-thiazolyl- pyrimidine derivatives and their use for the treatment of cancer |
CN101903357A (zh) | 2007-07-17 | 2010-12-01 | 里格尔药品股份有限公司 | 作为pkc抑制剂的环状胺取代的嘧啶二胺 |
DK2178870T3 (en) * | 2007-08-17 | 2018-10-22 | Lg Chemical Ltd | INDOLE AND INDAZOLIC COMPOUNDS AS AN INHIBITOR OF CELLULAR NECROSE |
US20090088371A1 (en) * | 2007-08-28 | 2009-04-02 | Rigel Pharmaceuticals, Inc. | Combination therapy with syk kinase inhibitor |
CA2710118A1 (en) | 2007-12-20 | 2009-07-02 | Cellzome Limited | Sulfamides as zap-70 inhibitors |
JP5749017B2 (ja) | 2008-01-22 | 2015-07-15 | ダウ アグロサイエンシィズ エルエルシー | 5−フルオロピリミジン誘導体 |
CA2715658C (en) | 2008-02-15 | 2016-07-19 | Rigel Pharmaceuticals, Inc. | Pyrimidine-2-amine compounds and their use as inhibitors of jak kinases |
US20110098288A1 (en) * | 2008-03-11 | 2011-04-28 | Jeremy Major | Sulfonamides as zap-70 inhibitors |
WO2009136995A2 (en) | 2008-04-16 | 2009-11-12 | Portola Pharmaceuticals, Inc. | Inhibitors of syk protein kinase |
US8138339B2 (en) | 2008-04-16 | 2012-03-20 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
BRPI0910921B1 (pt) | 2008-04-16 | 2022-06-21 | Portola Pharmaceuticals, Inc | Inibidores de proteína syk quinase, composição farmacêutica, kit e usos dos referidos inibidores |
JP2011518219A (ja) | 2008-04-22 | 2011-06-23 | ポートラ ファーマシューティカルズ, インコーポレイテッド | タンパク質キナーゼの阻害剤 |
US7829574B2 (en) | 2008-05-09 | 2010-11-09 | Hutchison Medipharma Enterprises Limited | Substituted quinazoline compounds and their use in treating angiogenesis-related diseases |
US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
SI2300013T1 (en) | 2008-05-21 | 2018-03-30 | Adriad Pharmacaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
US11351168B1 (en) | 2008-06-27 | 2022-06-07 | Celgene Car Llc | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
ES2711249T3 (es) | 2008-06-27 | 2019-04-30 | Celgene Car Llc | Compuestos de heteroarilo y usos de los mismos |
US8426430B2 (en) | 2008-06-30 | 2013-04-23 | Hutchison Medipharma Enterprises Limited | Quinazoline derivatives |
CN101659659B (zh) * | 2008-08-29 | 2013-01-02 | 和记黄埔医药(上海)有限公司 | 嘧啶衍生物及其医药用途 |
TW201008933A (en) | 2008-08-29 | 2010-03-01 | Hutchison Medipharma Entpr Ltd | Pyrimidine compounds |
EP2161259A1 (de) | 2008-09-03 | 2010-03-10 | Bayer CropScience AG | 4-Halogenalkylsubstituierte Diaminopyrimidine als Fungizide |
ES2542884T3 (es) * | 2008-09-23 | 2015-08-12 | Rigel Pharmaceuticals, Inc. | Inhibidores de JAK de carbamato tricíclico |
EP2382210B1 (en) | 2008-12-30 | 2017-03-01 | Rigel Pharmaceuticals, Inc. | Pyrimidinediamine kinase inhibitors |
EP2389373B1 (en) | 2009-01-21 | 2017-05-17 | Rigel Pharmaceuticals, Inc. | Derivatives of n2-(3-pyridyl or phenyl)-n4-(4-piperidyl)-2,4-pyrimidinediamine useful in the treatment of inflammatory, autoimmune or proliferative diseases |
MX2011007750A (es) * | 2009-01-23 | 2011-09-29 | Rigel Pharmaceuticals Inc | Composiciones y metodos para inhibicion de la ruta jak. |
KR101705158B1 (ko) | 2009-05-05 | 2017-02-09 | 다나-파버 캔서 인스티튜트 인크. | Egfr 억제제 및 질환 치료방법 |
WO2010129802A1 (en) | 2009-05-06 | 2010-11-11 | Portola Pharmaceuticals, Inc. | Inhibitors of jak |
JP5657578B2 (ja) | 2009-06-09 | 2015-01-21 | 武田薬品工業株式会社 | 新規な縮合環化合物およびその用途 |
CA2763717A1 (en) * | 2009-06-10 | 2010-12-16 | Cellzome Limited | Pyrimidine derivatives as zap-70 inhibitors |
UA108077C2 (xx) | 2009-07-02 | 2015-03-25 | Синтез динатрієвої солі n4-(2,2-диметил-4-$(дигідрофосфонокси)метил]-3-оксо-5-піридо$1,4]оксазин-6-іл)-5-фтор-n2-(3,4,5-триметоксифеніл)-2,4-піримідиндіаміну | |
WO2011009075A2 (en) | 2009-07-17 | 2011-01-20 | Rigel Pharmaceuticals, Inc. | Deuterated 2, 4-pyrimidinediamine compounds and prodrugs thereof and their uses |
AU2010281404A1 (en) * | 2009-07-28 | 2012-02-09 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the JAK pathway |
AU2010284255B2 (en) | 2009-08-17 | 2016-11-17 | Memorial Sloan-Kettering Cancer Center | Heat shock protein binding compounds, compositions, and methods for making and using same |
ES2524127T3 (es) | 2009-11-20 | 2014-12-04 | Rigel Pharmaceuticals, Inc. | Compuestos de 2,4-pirimidinodiamina y sus profármacos y sus usos |
WO2011068898A1 (en) | 2009-12-01 | 2011-06-09 | Rigel Pharmaceuticals, Inc. | Protein kinase c inhibitors and uses thereof |
EP2558474B1 (en) | 2010-04-13 | 2015-11-25 | Rigel Pharmaceuticals, Inc. | 2, 4-pyrimidinediamine compounds and prodrugs thereof and their uses |
BR112012029647A2 (pt) * | 2010-05-21 | 2016-08-02 | Chemilia Ab | novos derivados de pirimidinas |
KR101580714B1 (ko) | 2010-06-03 | 2016-01-04 | 파마싸이클릭스 엘엘씨 | 브루톤 티로신 인산화효소(btk)의 억제제의 용도 |
US8710223B2 (en) | 2010-07-21 | 2014-04-29 | Rigel Pharmaceuticals, Inc. | Protein kinase C inhibitors and uses thereof |
PT2598500T (pt) | 2010-07-28 | 2021-07-22 | Rigel Pharmaceuticals Inc | Composições e métodos para a inibição da via jak |
KR20130099040A (ko) | 2010-08-10 | 2013-09-05 | 셀진 아빌로믹스 리서치, 인코포레이티드 | Btk 억제제의 베실레이트 염 |
EP2635557A2 (en) | 2010-11-01 | 2013-09-11 | Portola Pharmaceuticals, Inc. | Nicotinamides as jak kinase modulators |
US20130317029A1 (en) | 2010-11-01 | 2013-11-28 | Portola Pharmaceuticals, Inc. | Oxypyrimidines as syk modulators |
ES2635713T3 (es) | 2010-11-01 | 2017-10-04 | Celgene Car Llc | Compuestos de heteroarilo y usos de los mismos |
EP2635556B1 (en) | 2010-11-01 | 2017-06-21 | Portola Pharmaceuticals, Inc. | Benzamides and nicotinamides as syk modulators |
NZ609957A (en) | 2010-11-01 | 2015-08-28 | Celgene Avilomics Res Inc | Heterocyclic compounds and uses thereof |
WO2012060847A1 (en) | 2010-11-07 | 2012-05-10 | Targegen, Inc. | Compositions and methods for treating myelofibrosis |
JP5957003B2 (ja) | 2010-11-10 | 2016-07-27 | セルジーン アヴィロミクス リサーチ, インコーポレイテッド | 変異体選択的egfr阻害剤およびその使用 |
US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
EP2489663A1 (en) | 2011-02-16 | 2012-08-22 | Almirall, S.A. | Compounds as syk kinase inhibitors |
PT2683385T (pt) | 2011-03-10 | 2018-10-19 | Rigel Pharmaceuticals Inc | Pirimidinadiaminas 2,4-substituídas para utilização no lúpus discoide |
RU2013147417A (ru) | 2011-03-24 | 2015-04-27 | Кемилиа Аб | Новые производные пиримидина |
US9249124B2 (en) | 2011-03-30 | 2016-02-02 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Aurora kinase inhibitors and methods of making and using thereof |
CN111499580A (zh) | 2011-04-22 | 2020-08-07 | 西格诺药品有限公司 | 取代的二氨基甲酰胺和二氨基甲腈嘧啶,其组合物,和用其治疗的方法 |
EA201391626A1 (ru) | 2011-05-04 | 2014-03-31 | Ариад Фармасьютикалз, Инк. | Соединения для ингибирования клеточной пролиферации в egfr-стимулированных типах рака |
ES2710423T3 (es) | 2011-07-28 | 2019-04-25 | Rigel Pharmaceuticals Inc | Formulaciones de (trimetoxifenilamino) pirimidinilo nuevas |
EP3392252B1 (en) | 2011-08-23 | 2023-10-04 | Libertas Bio, Inc. | Pyrimido- pyridazinone compounds and use thereof |
JP2014532658A (ja) | 2011-10-28 | 2014-12-08 | セルジーン アヴィロミクス リサーチ, インコーポレイテッド | ブルトン型チロシンキナーゼ疾患または障害を治療する方法 |
CA2856301C (en) | 2011-11-23 | 2020-10-06 | Portola Pharmaceuticals, Inc. | Pyrazine kinase inhibitors |
ES2880109T3 (es) | 2012-03-15 | 2021-11-23 | Celgene Car Llc | Formas sólidas de un inhibidor de la cinasa del receptor del factor de crecimiento epidérmico |
SG10201700799WA (en) | 2012-03-15 | 2017-02-27 | Celgene Avilomics Res Inc | Salts of an epidermal growth factor receptor kinase inhibitor |
JP6469567B2 (ja) | 2012-05-05 | 2019-02-13 | アリアド・ファーマシューティカルズ・インコーポレイテッド | Egfr発動性がんの細胞増殖阻害用化合物 |
WO2013173506A2 (en) | 2012-05-16 | 2013-11-21 | Rigel Pharmaceuticals, Inc. | Method of treating muscular degradation |
ME03300B (me) | 2012-06-13 | 2019-07-20 | Incyte Holdings Corp | Supsтituisana triciklična jedinjenja као inhibiтori fgfr |
EP2861059B1 (en) | 2012-06-15 | 2017-05-03 | Commonwealth Scientific and Industrial Research Organisation | Production of long chain polyunsaturated fatty acids in plant cells |
KR101446742B1 (ko) | 2012-08-10 | 2014-10-01 | 한국화학연구원 | N2,n4-비스(4-(피페라진-1-일)페닐)피리미딘-2,4-디아민 유도체 또는 이의 약학적으로 허용가능한 염 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물 |
US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
WO2014043257A1 (en) | 2012-09-12 | 2014-03-20 | Rigel Pharmaceuticals, Inc. | Treatment for vitiligo |
EP2903970A4 (en) | 2012-10-08 | 2016-11-30 | Portola Pharm Inc | SUBSTITUTED PYRIMIDINYL KINASE INHIBITORS |
US9748604B2 (en) | 2012-10-19 | 2017-08-29 | The University Of North Carolina At Chapel Hill | Ion conducting polymers and polymer blends for alkali metal ion batteries |
JP6466171B2 (ja) * | 2012-10-31 | 2019-02-06 | 富士フイルム富山化学株式会社 | 新規アミン誘導体またはその塩 |
EP2928891B1 (en) | 2012-12-04 | 2019-02-20 | Rigel Pharmaceuticals, Inc. | Protein kinase c inhibitors and uses thereof |
US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
EP2935226A4 (en) | 2012-12-21 | 2016-11-02 | Celgene Avilomics Res Inc | HETEROARYL COMPOUNDS AND USES THEREOF |
US20140213555A1 (en) | 2013-01-25 | 2014-07-31 | Rigel Pharmaceuticals, Inc. | Compounds and method for treating autoimmune diseases |
WO2014124230A2 (en) | 2013-02-08 | 2014-08-14 | Celgene Avilomics Research, Inc. | Erk inhibitors and uses thereof |
DK2970138T3 (en) | 2013-03-13 | 2019-03-25 | Canadian Blood Services | PYRAZOLD DERIVATIVES AND THEIR USE THEREOF |
JP6421170B2 (ja) | 2013-03-14 | 2018-11-07 | ライジェル ファーマシューティカルズ, インコーポレイテッド | プロテインキナーゼc阻害剤およびその使用 |
KR20150139827A (ko) | 2013-04-01 | 2015-12-14 | 더 유니버시티 오브 노쓰 캐롤라이나 엣 채플 힐 | 알칼리 금속 이온 배터리를 위한 이온 전도성 플루오로중합체 카르보네이트 |
US9611283B1 (en) | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
ES2657451T3 (es) | 2013-04-19 | 2018-03-05 | Incyte Holdings Corporation | Heterocíclicos bicíclicos como inhibidores del FGFR |
US9492471B2 (en) | 2013-08-27 | 2016-11-15 | Celgene Avilomics Research, Inc. | Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase |
TWI667233B (zh) * | 2013-12-19 | 2019-08-01 | 德商拜耳製藥公司 | 新穎吲唑羧醯胺,其製備方法、含彼等之醫藥製劑及其製造醫藥之用途 |
US9415049B2 (en) | 2013-12-20 | 2016-08-16 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
NZ715903A (en) | 2014-01-30 | 2017-06-30 | Signal Pharm Llc | Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use |
EA201692155A1 (ru) | 2014-05-13 | 2017-04-28 | Мемориал Слоун-Кеттеринг Кэнсэ Сентр | МОДУЛЯТОРЫ Hsp70 И СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ |
EP3179858B1 (en) | 2014-08-13 | 2019-05-15 | Celgene Car Llc | Forms and compositions of an erk inhibitor |
US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
WO2016100308A1 (en) | 2014-12-16 | 2016-06-23 | Signal Pharmaceuticals, Llc | Methods for measurement of inhibition of c-jun n-terminal kinase in skin |
EA033530B1 (ru) | 2014-12-16 | 2019-10-31 | Signal Pharm Llc | Композиции 2-(трет-бутиламино)-4-((1r,3r,4r)-3-гидрокси-4-метилциклогексиламино)пиримидин-5-карбоксамида |
WO2016123291A1 (en) | 2015-01-29 | 2016-08-04 | Signal Pharmaceuticals, Llc | Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide |
US10077231B2 (en) | 2015-02-03 | 2018-09-18 | Blue Current, Inc. | Functionalized fluoropolymers and electrolyte compositions |
ES2751669T3 (es) | 2015-02-20 | 2020-04-01 | Incyte Corp | Heterociclos bicíclicos como inhibidores FGFR |
MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
JP6853234B2 (ja) * | 2015-07-09 | 2021-03-31 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung | Btk阻害剤としてのピリミジン誘導体及びその使用 |
JP6805232B2 (ja) | 2015-07-24 | 2020-12-23 | セルジーン コーポレイション | (1r,2r,5r)−5−アミノ−2−メチルシクロヘキサノール塩酸塩の合成方法及びそれに有用な中間体 |
US10428030B2 (en) | 2015-10-30 | 2019-10-01 | Trillium Therapeutics | Heterocycle derivatives and their use for the treatment of CNS disorders |
PL3442947T3 (pl) * | 2016-04-15 | 2023-10-02 | Epizyme, Inc. | Związki arylowe lub heteroarylowe podstawione aminą jako inhibitory ehmt1 i ehmt2 |
MD3448859T2 (ro) | 2017-03-20 | 2020-03-31 | Forma Therapeutics Inc | Compoziții de pirolopirol în calitate de activatori ai piruvatkinazei (PKR) |
EP3612181A4 (en) | 2017-04-21 | 2021-01-06 | Epizyme, Inc. | COMBINATION THERAPIES WITH EHMT2 INHIBITORS |
AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
EP3647311B1 (en) * | 2017-06-30 | 2023-11-01 | Beijing Tide Pharmaceutical Co., Ltd. | Rho-associated protein kinase inhibitor, pharmaceutical composition comprising same, and preparation method and use thereof |
CN107417611A (zh) * | 2017-07-25 | 2017-12-01 | 广州大学 | 一种3‑(4‑甲氧基苯基)‑6‑甲氧基‑4‑氯‑5,7‑二溴喹啉的合成方法 |
CR20200590A (es) | 2018-05-04 | 2021-04-26 | Incyte Corp | Formas sólidas de un inhibidor de fgfr y procesos para prepararlas |
JP2021523118A (ja) | 2018-05-04 | 2021-09-02 | インサイト・コーポレイションIncyte Corporation | Fgfr阻害剤の塩 |
BR112021005188A2 (pt) | 2018-09-19 | 2021-06-08 | Forma Therapeutics, Inc. | tratamento de anemia falciforme com um composto de ativação de piruvato cinase r |
JP7450610B2 (ja) | 2018-09-19 | 2024-03-15 | ノヴォ・ノルディスク・ヘルス・ケア・アーゲー | ピルビン酸キナーゼrの活性化 |
CN111362928A (zh) * | 2018-12-26 | 2020-07-03 | 上海喆邺生物科技有限公司 | 2,4-二氨基嘧啶衍生物 |
US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
US11091467B2 (en) | 2019-05-08 | 2021-08-17 | Aligos Therapeutics, Inc. | Modulators of THR-β and methods of use thereof |
US20200377518A1 (en) | 2019-05-29 | 2020-12-03 | Rigel Pharmaceuticals, Inc. | Method of preventing and treating thrombosis |
WO2020257495A1 (en) * | 2019-06-18 | 2020-12-24 | Purdue Research Foundation | Inhibitors of erythrocyte band 3 tyrosine phosphorylation and uses thereof |
US11529350B2 (en) | 2019-07-03 | 2022-12-20 | Sumitomo Pharma Oncology, Inc. | Tyrosine kinase non-receptor 1 (TNK1) inhibitors and uses thereof |
US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
MX2022001596A (es) | 2019-08-08 | 2022-03-11 | Rigel Pharmaceuticals Inc | Compuestos y metodos para tratar sindrome de liberacion de citocinas. |
MX2022001890A (es) | 2019-08-14 | 2022-04-26 | Rigel Pharmaceuticals Inc | Metodo para bloquear o mejorar el sindrome de liberacion de citocinas. |
CN110746402B (zh) * | 2019-09-21 | 2021-01-15 | 温州医科大学 | 一种2-n-芳基-4-n-芳基-5-氟嘧啶类化合物及其制备方法和应用 |
IL291901A (en) | 2019-10-14 | 2022-06-01 | Incyte Corp | Bicyclyl heterocycles as fgr suppressors |
US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
JP2023505257A (ja) | 2019-12-04 | 2023-02-08 | インサイト・コーポレイション | Fgfr阻害剤の誘導体 |
JP2023505258A (ja) | 2019-12-04 | 2023-02-08 | インサイト・コーポレイション | Fgfr阻害剤としての三環式複素環 |
CN112920124B (zh) * | 2021-01-29 | 2024-03-01 | 安徽医科大学 | 一种嘧啶-2,4-二胺类化合物及其制备方法与应用 |
CA3220274A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
Family Cites Families (198)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3159547A (en) | 1963-06-28 | 1964-12-01 | Abbott Lab | Method of lowering blood pressure with 4-(2-amino-4-pyrimidylamino)-benzene-sulfonamide |
US3320256A (en) | 1965-04-09 | 1967-05-16 | Hoffmann La Roche | Fluorinated imidazoo[1, 2-c]pyrimidines and pyrimido[1, 2-c]pyrimidines |
EP0139613A1 (de) | 1983-08-29 | 1985-05-02 | Ciba-Geigy Ag | N-(2-Nitrophenyl)-4-aminopyrimidin-Derivate, deren Herstellung und Verwendung |
DE3618353A1 (de) | 1986-05-31 | 1987-12-03 | Hoechst Ag | Schaedlingsbekaempfungsmittel auf der basis von aminopyrimidin-derivaten sowie neue aminopyrimidin-verbindungen |
US4968781A (en) | 1987-04-02 | 1990-11-06 | Ciba-Geigy Corporation | Fiber-reactive dyes comprising a halopyrimidine for which a vinylsulfonyl or the like moiety is attached via a bridge member |
SU1499883A1 (ru) | 1987-11-24 | 1991-10-23 | Научно-исследовательский институт фармакологии АМН СССР | Дихлоргидрат 2,4-бис-(п-трет-бутиланилино)-5-окси-6-метилпиримидина, обладающий анальгетической и противовоспалительной активностью |
HU206337B (en) | 1988-12-29 | 1992-10-28 | Mitsui Petrochemical Ind | Process for producing pyrimidine derivatives and pharmaceutical compositions |
IE63502B1 (en) | 1989-04-21 | 1995-05-03 | Zeneca Ltd | Aminopyrimidine derivatives useful for treating cardiovascular disorders |
US4983608A (en) | 1989-09-05 | 1991-01-08 | Hoechst-Roussell Pharmaceuticals, Inc. | N-substituted-4-pyrimidinamines and pyrimidinediamines |
US5179204A (en) | 1989-09-05 | 1993-01-12 | Hoechst-Roussel Pharmaceuticals Incorporated | N-substituted-4-pyrimidinamines and pyrimidinediamines |
JPH03127790A (ja) | 1989-10-11 | 1991-05-30 | Morishita Pharmaceut Co Ltd | N―(1h―テトラゾール―5―イル)―2―アニリノ―5―ピリミジンカルボキシアミド類及びその合成中間体 |
TW224941B (ja) | 1989-11-08 | 1994-06-11 | Yamanouchi Pharma Co Ltd | |
GB9012592D0 (en) | 1990-06-06 | 1990-07-25 | Smithkline Beecham Intercredit | Compounds |
DE4029650A1 (de) | 1990-09-19 | 1992-03-26 | Hoechst Ag | 2-anilino-pyrimidine, verfahren zu ihrer herstellung, sie enthaltene mittel und ihre verwendung als fungizide |
CA2074864A1 (en) | 1991-07-30 | 1993-01-31 | Carmen Almansa | Tetralones with pharmacological activity |
US5728536A (en) | 1993-07-29 | 1998-03-17 | St. Jude Children's Research Hospital | Jak kinases and regulation of Cytokine signal transduction |
US5521184A (en) | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
TW287160B (ja) | 1992-12-10 | 1996-10-01 | Hoffmann La Roche | |
CA2174080A1 (en) | 1993-10-12 | 1995-04-20 | Paul Edward Aldrich | 1n-alkyl-n-arylpyrimidinamines and derivatives thereof |
IL112290A (en) | 1994-01-12 | 1999-01-26 | Novartis Ag | Transformed aryl and the troiryl pyrimidines and herbicides containing them |
CA2150609C (en) | 1994-06-01 | 1998-12-08 | Mikiro Yanaka | Pyrimidine derivatives and pharmaceutical composition |
US5733932A (en) | 1995-01-06 | 1998-03-31 | The Picower Institute For Medical Research | Compounds and methods of use to derivatize neighboring lysine residues in proteins under physiological conditions |
GB9516121D0 (en) | 1995-08-05 | 1995-10-04 | Pfizer Ltd | Organometallic addition to ketones |
GB9523675D0 (en) | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
TW440563B (en) | 1996-05-23 | 2001-06-16 | Hoffmann La Roche | Aryl pyrimidine derivatives and a pharmaceutical composition thereof |
GB9619284D0 (en) | 1996-09-16 | 1996-10-30 | Celltech Therapeutics Ltd | Chemical compounds |
US6004985A (en) | 1996-10-09 | 1999-12-21 | Berlex Laboratories, Inc. | Thio acid derived monocylic N-heterocyclics as anticoagulants |
DE19710435A1 (de) * | 1997-03-13 | 1998-09-17 | Hoechst Ag | Verwendung von Pyrimidinderivaten zur Prävention von Krebs allein oder in Kombination mit anderen therapeutischen Maßnahmen |
GB9705361D0 (en) | 1997-03-14 | 1997-04-30 | Celltech Therapeutics Ltd | Chemical compounds |
US6022884A (en) | 1997-11-07 | 2000-02-08 | Amgen Inc. | Substituted pyridine compounds and methods of use |
GB9723859D0 (en) | 1997-11-12 | 1998-01-07 | Zeneca Ltd | Compound,composition and use |
DE19750701A1 (de) | 1997-11-15 | 1999-05-20 | Dystar Textilfarben Gmbh & Co | Verfahren zur Umsetzung von fluorsubstituierten Heterocyclen mit Aminen in Gegenwart von Phasentransfer-Katalysatoren |
US6432963B1 (en) | 1997-12-15 | 2002-08-13 | Yamanouchi Pharmaceutical Co., Ltd. | Pyrimidine-5-carboxamide derivatives |
JP2001527083A (ja) | 1997-12-31 | 2001-12-25 | ザ・ユニバーシティ・オブ・カンザス | 第二級および第三級アミン含有薬剤の水溶性プロドラッグおよびその製造方法 |
JP2002503662A (ja) | 1998-02-17 | 2002-02-05 | テュラリク インコーポレイテッド | 抗ウイルス性ピリミジン誘導体 |
ATE296812T1 (de) * | 1998-03-09 | 2005-06-15 | Vertex Pharma | 1,2-diazepanderivate als inhibitoren des interleukin-1beta umwandelnden enzyms |
JP2002506873A (ja) | 1998-03-18 | 2002-03-05 | アリアド・ファーマシューティカルズ・インコーポレイテッド | 複素環式シグナル伝達阻害剤、それを含む組成物 |
SK287996B6 (sk) | 1998-03-27 | 2012-09-03 | Janssen Pharmaceutica N. V. | Pyrimide compound, pharmaceutical composition the compound is comprised, method for preparation thereof, combination and product containing the composition and use of the pyrimide compound |
ES2361146T3 (es) | 1998-03-27 | 2011-06-14 | Janssen Pharmaceutica Nv | Derivados de la piramidina inhibitatoria de vih. |
GB9806739D0 (en) | 1998-03-28 | 1998-05-27 | Univ Newcastle Ventures Ltd | Cyclin dependent kinase inhibitors |
WO1999050249A2 (en) | 1998-04-01 | 1999-10-07 | Du Pont Pharmaceuticals Company | Pyrimidines and triazines as integrin antagonists |
KR20010025087A (ko) | 1998-05-22 | 2001-03-26 | 스튜어트 알. 수터 | 신규한 2-알킬 치환된 이미다졸 화합물 |
US6093743A (en) * | 1998-06-23 | 2000-07-25 | Medinox Inc. | Therapeutic methods employing disulfide derivatives of dithiocarbamates and compositions useful therefor |
WO2000000202A1 (en) | 1998-06-30 | 2000-01-06 | Parker Hughes Institute | Method for inhibiting c-jun expression using jak-3 inhibitors |
DE69924500T2 (de) | 1998-08-21 | 2006-02-09 | Parker Hughes Institute, St. Paul | Chinazolinderivate |
DE69933680T2 (de) | 1998-08-29 | 2007-08-23 | Astrazeneca Ab | Pyrimidine verbindungen |
DE19851421A1 (de) | 1998-11-07 | 2000-05-11 | Boehringer Ingelheim Pharma | Neue Pyrimidine, deren Herstellung und Verwendung |
HU230394B1 (hu) | 1998-11-10 | 2016-04-28 | Janssen Pharmaceutica N.V. | HIV-vírus szaporodását gátló pirimidin-származékok |
US6127376A (en) | 1998-12-04 | 2000-10-03 | Berlex Laboratories, Inc. | Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants |
GB9828511D0 (en) | 1998-12-24 | 1999-02-17 | Zeneca Ltd | Chemical compounds |
US6080747A (en) | 1999-03-05 | 2000-06-27 | Hughes Institute | JAK-3 inhibitors for treating allergic disorders |
CN1344266A (zh) * | 1999-03-26 | 2002-04-10 | 阿斯特拉曾尼卡有限公司 | 新的化合物 |
WO2000059893A1 (en) | 1999-04-06 | 2000-10-12 | Krenitsky Pharmaceuticals Inc. | Neurotrophic thio substituted pyrimidines |
DE19917785A1 (de) | 1999-04-20 | 2000-10-26 | Bayer Ag | 2,4-Diamino-pyrimidin-Derivate |
AU5108000A (en) | 1999-06-10 | 2001-01-02 | Yamanouchi Pharmaceutical Co., Ltd. | Novel nitrogen-contaiing heterocyclic derivatives or salts thereof |
GB9914258D0 (en) | 1999-06-18 | 1999-08-18 | Celltech Therapeutics Ltd | Chemical compounds |
GB9918035D0 (en) | 1999-07-30 | 1999-09-29 | Novartis Ag | Organic compounds |
DE19945982A1 (de) | 1999-09-24 | 2001-03-29 | Knoll Ag | Geschwindigkeitsbestimmte Partikel |
AU775360B2 (en) | 1999-09-24 | 2004-07-29 | Janssen Pharmaceutica N.V. | Antiviral compositions |
US6506762B1 (en) | 1999-09-30 | 2003-01-14 | Neurogen Corporation | Certain alkylene diamine-substituted heterocycles |
AU1026901A (en) | 1999-10-29 | 2001-05-08 | Syngenta Participations Ag | Novel herbicides |
WO2001045641A2 (en) | 1999-11-30 | 2001-06-28 | Parker Hughes Institute | Inhibitors of thrombin induced platelet aggregation |
PL218519B1 (pl) | 1999-12-10 | 2014-12-31 | Pfizer Prod Inc | Związki pirolo [2,3-d] pirymidynowe, środek farmaceutyczny zawierający te związki oraz ich zastosowanie |
US20020065270A1 (en) | 1999-12-28 | 2002-05-30 | Moriarty Kevin Joseph | N-heterocyclic inhibitors of TNF-alpha expression |
CA2396693A1 (en) * | 1999-12-28 | 2001-07-05 | Stephen T. Wrobleski | Cytokine, especially tnf-alpha, inhibitors |
US6362172B2 (en) | 2000-01-20 | 2002-03-26 | Bristol-Myers Squibb Company | Water soluble prodrugs of azole compounds |
CA2400447C (en) * | 2000-02-17 | 2008-04-22 | Amgen Inc. | Kinase inhibitors |
GB0004890D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
GB0004887D0 (en) * | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
GB0004888D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
GB0004886D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
US6525051B2 (en) | 2000-03-27 | 2003-02-25 | Schering Aktiengesellschaft | N-heterocyclic derivatives as NOS inhibitors |
AU782948B2 (en) | 2000-05-08 | 2005-09-15 | Janssen Pharmaceutica N.V. | Prodrugs of HIV replication inhibiting pyrimidines |
EP1282606B1 (en) | 2000-05-08 | 2015-04-22 | Janssen Pharmaceutica NV | Hiv replication inhibiting pyrimidines and triazines |
YU83302A (sh) | 2000-06-26 | 2005-09-19 | Pfizer Products Inc. | Jedinjenja pirolo (2,3-d) pirimidina kao imunosupresivni agensi |
GB0016877D0 (en) * | 2000-07-11 | 2000-08-30 | Astrazeneca Ab | Chemical compounds |
DE60120193T2 (de) | 2000-09-15 | 2007-03-29 | Vertex Pharmaceuticals Inc., Cambridge | Pyrazolverbindungen als protein-kinasehemmer |
CA2422076A1 (en) * | 2000-09-18 | 2002-03-21 | Idec Pharmaceutical Corporation | Combination therapy for treatment of autoimmune diseases using b cell depleting/immunoregulatory antibody combination |
WO2002043735A1 (en) | 2000-11-29 | 2002-06-06 | Parker Hughes Institute | Inhibitors of thrombin induced platelet aggregation |
US20020137755A1 (en) | 2000-12-04 | 2002-09-26 | Bilodeau Mark T. | Tyrosine kinase inhibitors |
DE60138645D1 (de) | 2000-12-21 | 2009-06-18 | Smithkline Beecham Corp | Pyrimidinamine als angiogenesemodulatoren |
ATE528303T1 (de) | 2000-12-21 | 2011-10-15 | Vertex Pharma | Pyrazoleverbindungen als proteinkinasehemmer |
CA2436487A1 (en) | 2001-01-30 | 2002-08-08 | Cytopia Pty Ltd. | Methods of inhibiting kinases |
WO2002064096A2 (en) | 2001-02-16 | 2002-08-22 | Tularik Inc. | Methods of using pyrimidine-based antiviral agents |
MXPA03007266A (es) | 2001-02-20 | 2003-12-04 | Astrazeneca Ab | 2-arilamino-pirimidinas para tratamiento de desordenes relacionados a glucogeno-sintasa cinasa-3(gsk3). |
GB2373186A (en) * | 2001-02-23 | 2002-09-18 | Astrazeneca Ab | Pharmaceutical combinations of a CCR3 antagonist and a compound which is usefulreatment of asthma, allergic disease or inflammation |
EP1975620A3 (en) | 2001-03-02 | 2008-12-24 | GPC Biotech AG | Three hybrid assay system |
EP1392662B1 (de) | 2001-05-29 | 2009-01-07 | Bayer Schering Pharma Aktiengesellschaft | Cdk inhibitorische pyrimidine, deren herstellung und verwendung als arzneimittel |
US7301023B2 (en) | 2001-05-31 | 2007-11-27 | Pfizer Inc. | Chiral salt resolution |
US6762179B2 (en) | 2001-05-31 | 2004-07-13 | Vertex Pharmaceuticals Incorporated | Thiazole compounds useful as inhibitors of protein kinase |
JP4523271B2 (ja) | 2001-06-01 | 2010-08-11 | バーテックス ファーマシューティカルズ インコーポレイテッド | プロテインキナーゼのインヒビターとして有用なチアゾール化合物 |
ATE432929T1 (de) | 2001-06-15 | 2009-06-15 | Vertex Pharma | 5-(2-aminopyrimidin-4-yl)benzisoxazole als proteinkinasehemmer |
JP2005500294A (ja) | 2001-06-19 | 2005-01-06 | ブリストル−マイヤーズ スクイブ カンパニー | ホスホジエステラーゼ7に対するピリミジン阻害剤 |
EP1408978A4 (en) | 2001-06-21 | 2005-07-13 | Ariad Pharma Inc | NOVEL PHENYLAMINO-PYRIMIDINES AND THEIR USE |
GB0115393D0 (en) | 2001-06-23 | 2001-08-15 | Aventis Pharma Ltd | Chemical compounds |
KR100875380B1 (ko) | 2001-06-23 | 2008-12-23 | 아벤티스 파마슈티칼스 인크. | 단백질 키나제 억제제로서의 피롤로피리미딘 |
AU2002316421B2 (en) * | 2001-06-26 | 2008-05-15 | Bristol-Myers Squibb Company | N-heterocyclic inhibitors of TNF-ALPHA expression |
JO3429B1 (ar) | 2001-08-13 | 2019-10-20 | Janssen Pharmaceutica Nv | مشتقات برميدينات مثبطة فيروس الايدز |
US6939874B2 (en) | 2001-08-22 | 2005-09-06 | Amgen Inc. | Substituted pyrimidinyl derivatives and methods of use |
US7115617B2 (en) | 2001-08-22 | 2006-10-03 | Amgen Inc. | Amino-substituted pyrimidinyl derivatives and methods of use |
WO2003030909A1 (en) | 2001-09-25 | 2003-04-17 | Bayer Pharmaceuticals Corporation | 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer |
WO2003026665A1 (en) | 2001-09-26 | 2003-04-03 | Bayer Pharmaceuticals Corporation | 2-phenylamino-4-(5-pyrazolylamino)-pyrimidine derivatives as kinase inhibitors, in particular, src kinase inhibitors |
WO2003040141A1 (en) | 2001-09-28 | 2003-05-15 | Bayer Pharmaceuticals Corporation | Oxazolyl-phenyl-2,4-diamino-pyrimidine compounds and methods for treating hyperproliferative disorders |
EP1438053B1 (de) | 2001-10-17 | 2008-09-10 | Boehringer Ingelheim Pharma GmbH & Co.KG | Pyrimidinderivate, arzneimittel enthaltend diese verbindungen, deren verwendung und verfahren zu ihrer herstellung |
WO2003032994A2 (de) | 2001-10-17 | 2003-04-24 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 5-substituierte 4-amino-2-phenylamino-pyrimidinderivate und ihre verwendung als beta-amyloid modulatoren |
HUP0402657A3 (en) | 2001-11-28 | 2010-03-29 | Btg Int Ltd | Preventives or remedies for alzheimer' s disease or amyloid protein fibrosis inhibitors containing nitrogen-containing heteroaryl compounds |
GT200200234A (es) | 2001-12-06 | 2003-06-27 | Compuestos cristalinos novedosos | |
SE0104140D0 (sv) | 2001-12-07 | 2001-12-07 | Astrazeneca Ab | Novel Compounds |
WO2003055489A1 (en) | 2001-12-21 | 2003-07-10 | Bayer Pharmaceuticals Corporation | 2,4-diamino-pyrimidine derivative compounds as inhibitors of prolylpeptidase, inducers of apoptosis and cancer treatment agents |
WO2003062225A1 (en) | 2002-01-23 | 2003-07-31 | Bayer Pharmaceuticals Corporation | Pyrimidine derivatives as rho-kinase inhibitors |
TWI329105B (en) * | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
US6998391B2 (en) | 2002-02-07 | 2006-02-14 | Supergen.Inc. | Method for treating diseases associated with abnormal kinase activity |
US7459455B2 (en) | 2002-02-08 | 2008-12-02 | Smithkline Beecham Corporation | Pyrimidine compounds |
MXPA04008458A (es) | 2002-03-01 | 2004-12-06 | Smithkline Beecham Corp | Diamino pirimidinas y su uso como inhibidores de angiogenesis. |
WO2003076437A1 (de) * | 2002-03-11 | 2003-09-18 | Schering Aktiengesellschaft | Cdk inhibitorische 2-heteroaryl-pyrimidine, deren herstellung und verwendung als arzneimittel |
US7288547B2 (en) | 2002-03-11 | 2007-10-30 | Schering Ag | CDK-inhibitory 2-heteroaryl-pyrimidines, their production and use as pharmaceutical agents |
GB0206215D0 (en) * | 2002-03-15 | 2002-05-01 | Novartis Ag | Organic compounds |
BR0308737A (pt) | 2002-03-20 | 2005-01-11 | Bristol Myers Squibb Co | Pró-drogas de fosfato de fluoroxindóis |
AU2003301758A1 (en) | 2002-05-06 | 2004-05-25 | Bayer Pharmaceuticals Corporation | Use of pyrimidine derivates for the manifacture of a medicament for the treatment of hyper-proliferative disorders |
WO2003095448A1 (en) | 2002-05-06 | 2003-11-20 | Bayer Pharmaceuticals Corporation | Pyridinyl amino pyrimidine derivatives useful for treating hyper-proliferative disorders |
JP4681302B2 (ja) | 2002-05-06 | 2011-05-11 | バーテックス ファーマシューティカルズ インコーポレイテッド | チアジアゾールまたはオキサジアゾール、およびこれらの、jakプロテインキナーゼのインヒビターとしての使用 |
AR039540A1 (es) | 2002-05-13 | 2005-02-23 | Tibotec Pharm Ltd | Compuestos microbicidas con contenido de pirimidina o triazina |
CA2487679A1 (en) | 2002-05-30 | 2003-12-11 | Vertex Pharmaceuticals Incorporated | Inhibitors of jak and cdk2 protein kinases |
US20060252943A1 (en) | 2002-06-17 | 2006-11-09 | Amogh Boloor | Chemical process |
MXPA04012855A (es) | 2002-06-28 | 2005-04-19 | Yamanouchi Pharma Co Ltd | Derivado de diaminopirimidincarboxiamida. |
MXPA05001096A (es) | 2002-07-29 | 2005-11-23 | Rigel Pharmaceuticals Inc | Metodos para tratamiento o prevencion de enfermedades autoinmunes con compuestos de 2,4-diamino-pirimidina. |
WO2004014384A2 (en) | 2002-08-13 | 2004-02-19 | Warner-Lambert Company Llc | Cyclic compounds containing zinc binding groups as matrix metalloproteinase inhibitors |
WO2004016597A2 (en) | 2002-08-14 | 2004-02-26 | Vertex Pharmaceuticals Incorporated | Protein kinase inhibitors and uses thereof |
JP2006512314A (ja) | 2002-11-01 | 2006-04-13 | バーテックス ファーマシューティカルズ インコーポレイテッド | Jakインヒビターおよび他のプロテインキナーゼインヒビターとしての組成物の使用 |
AU2003295396B2 (en) | 2002-11-04 | 2009-02-26 | Vertex Pharmaceuticals Incorporated | Heteroaryl-pyramidine derivatives as JAK inhibitors |
CA2507406A1 (en) | 2002-11-05 | 2004-05-21 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of jak and other protein kinases |
GB0226582D0 (en) | 2002-11-14 | 2002-12-18 | Cyclacel Ltd | Anti-viral compounds |
GB0226583D0 (en) | 2002-11-14 | 2002-12-18 | Cyclacel Ltd | Compounds |
BR0316470A (pt) | 2002-11-21 | 2005-10-11 | Pfizer Prod Inc | Derivados de 3-amino-piperadina e métodos de preparação |
EP1572213A1 (en) | 2002-11-26 | 2005-09-14 | Pfizer Products Inc. | Method of treatment of transplant rejection |
CN1717396A (zh) | 2002-11-28 | 2006-01-04 | 舍林股份公司 | Chk-、Pdk-和Akt-抑制嘧啶,其制备及作为药物的用途 |
AU2002350719A1 (en) | 2002-11-29 | 2004-06-23 | Janssen Pharmaceutica N.V. | Pharmaceutical compositions comprising a basic respectively acidic drug compound, a surfactant and a physiologically tolerable water-soluble acid respectively base |
WO2004054617A1 (ja) | 2002-12-13 | 2004-07-01 | Kyowa Hakko Kogyo Co., Ltd. | 中枢疾患の予防および/または治療剤 |
US7226919B2 (en) | 2002-12-18 | 2007-06-05 | Vertex Pharmaceuticals Inc. | Compositions useful as inhibitors of protein kinases |
US7098332B2 (en) | 2002-12-20 | 2006-08-29 | Hoffmann-La Roche Inc. | 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones |
UA80767C2 (en) | 2002-12-20 | 2007-10-25 | Pfizer Prod Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
MXPA05008364A (es) | 2003-02-07 | 2005-11-04 | Janssen Pharmaceutica Nv | Derivados de pirimidina para la prevencion de una infeccion por vih. |
JP4634367B2 (ja) | 2003-02-20 | 2011-02-16 | スミスクライン ビーチャム コーポレーション | ピリミジン化合物 |
CL2004000306A1 (es) | 2003-02-20 | 2005-04-08 | Tibotec Pharm Ltd | Compuestos derivados de pirimidina sustituidas con indano; proceso para su preparacion; composicion farmaceutica que lo comprende; combinacion farmaceutica; y su uso para el tratamiento o profilaxis de una enfermedad infecciosa. |
GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
US20050009817A1 (en) | 2003-04-30 | 2005-01-13 | Jennifer Savoy | Substituted heteroaryls |
GB0311276D0 (en) | 2003-05-16 | 2003-06-18 | Astrazeneca Ab | Chemical compounds |
GB0311274D0 (en) | 2003-05-16 | 2003-06-18 | Astrazeneca Ab | Chemical compounds |
EP1651595A2 (en) | 2003-05-30 | 2006-05-03 | Rigel Pharmaceuticals, Inc. | Ubiquitin ligase inhibitors |
CN1820001A (zh) | 2003-07-10 | 2006-08-16 | 神经能质公司 | 经取代的杂环二芳基胺类似物 |
CN100549014C (zh) | 2003-07-16 | 2009-10-14 | 詹森药业有限公司 | 作为糖原合酶激酶3抑制剂的三唑并嘧啶衍生物 |
CA2531333A1 (en) | 2003-07-16 | 2005-02-10 | Janssen Pharmaceutica N.V. | Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors |
WO2005009980A1 (en) | 2003-07-22 | 2005-02-03 | Neurogen Corporation | Substituted pyridin-2-ylamine analogues |
US7442698B2 (en) * | 2003-07-24 | 2008-10-28 | Amgen Inc. | Substituted heterocyclic compounds and methods of use |
US8178671B2 (en) * | 2003-07-30 | 2012-05-15 | Rigel Pharmaceuticals, Inc. | Methods of treating or preventing autoimmune diseases with 2, 4-pyrimidinediamine compounds |
AU2004261484A1 (en) | 2003-07-30 | 2005-02-10 | Cyclacel Limited | 2-aminophenyl-4-phenylpyrimidines as kinase inhibitors |
JP4741491B2 (ja) | 2003-08-07 | 2011-08-03 | ライジェル ファーマシューティカルズ, インコーポレイテッド | 抗増殖剤としての2,4−ピリミジンジアミン化合物および使用 |
SI1660458T1 (sl) | 2003-08-15 | 2012-05-31 | Novartis Ag | pirimidindiamini uporabni pri zdravljenju neoplastičnih bolezni vnetnih motenj in motenj imunskega sistema |
US7223759B2 (en) | 2003-09-15 | 2007-05-29 | Anadys Pharmaceuticals, Inc. | Antibacterial 3,5-diaminopiperidine-substituted aromatic and heteroaromatic compounds |
GB0321710D0 (en) | 2003-09-16 | 2003-10-15 | Novartis Ag | Organic compounds |
CA2538413A1 (en) | 2003-09-18 | 2005-03-24 | Novartis Ag | 2,4-di (phenylamino) pyrimidines useful in the treatment of proliferative disorders |
WO2005027848A2 (en) | 2003-09-19 | 2005-03-31 | Barnes-Jewish Hospital | Methods for screening osteogenic compounds targeting syk kinase and/or vav3 and uses of syk modulators and/or vav modulators |
EP1668011B1 (en) | 2003-09-25 | 2011-03-02 | Janssen Pharmaceutica NV | Hiv replication inhibiting purine derivatives |
DE10349423A1 (de) | 2003-10-16 | 2005-06-16 | Schering Ag | Sulfoximinsubstituierte Parimidine als CDK- und/oder VEGF-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel |
RU2006122853A (ru) | 2003-11-28 | 2008-01-10 | Новартис АГ (CH) | Производные диарилмочевины для лечения заболеваний, зависимых от протеинкиназы |
MY141255A (en) | 2003-12-11 | 2010-03-31 | Memory Pharm Corp | Phosphodiesterase 4 inhibitors, including n-substituted diarylamine analogs |
US7511137B2 (en) | 2003-12-19 | 2009-03-31 | Rigel Pharmaceuticals, Inc. | Stereoisomers and stereoisomeric mixtures of 1-(2,4-pyrimidinediamino)-2-cyclopentanecarboxamide synthetic intermediates |
ZA200602666B (en) | 2004-01-12 | 2007-09-26 | Cytopia Res Pty Ltd | Selective kinase inhibitors |
GB0402653D0 (en) | 2004-02-06 | 2004-03-10 | Cyclacel Ltd | Compounds |
PL1713806T3 (pl) | 2004-02-14 | 2013-09-30 | Irm Llc | Związki i kompozycje jako inhibitory kinaz białkowych |
US7607424B2 (en) * | 2004-02-17 | 2009-10-27 | Planet Eclipse Limited | Electro-magnetically operated rotating projectile loader |
US7745625B2 (en) | 2004-03-15 | 2010-06-29 | Bristol-Myers Squibb Company | Prodrugs of piperazine and substituted piperidine antiviral agents |
WO2005107760A1 (en) | 2004-04-30 | 2005-11-17 | Irm Llc | Compounds and compositions as inducers of keratinocyte differentiation |
WO2005118544A2 (en) | 2004-05-18 | 2005-12-15 | Rigel Pharmaceuticals, Inc. | Cycloalkyl substituted pyrimidinediamine compounds and their uses |
GB0419161D0 (en) | 2004-08-27 | 2004-09-29 | Novartis Ag | Organic compounds |
US20060047135A1 (en) | 2004-08-30 | 2006-03-02 | Chadwick Scott T | Process for preparing chloromethyl di-tert-butylphosphate |
US20060058525A1 (en) * | 2004-09-01 | 2006-03-16 | Rajinder Singh | Synthesis of 2,4-pyrimidinediamine compounds |
EP1794134A1 (de) | 2004-09-29 | 2007-06-13 | Bayer Schering Pharma Aktiengesellschaft | Substituierte 2-anilinopyrimidine als zellzyklus -kinase oder rezeptortyrosin-kinase inhibitoren, deren herstellung und verwendung als arzneimittel |
US7585883B2 (en) | 2004-10-29 | 2009-09-08 | Rigel Pharmaceuticals, Inc. | Substituted pyridines and their uses |
WO2006068770A1 (en) * | 2004-11-24 | 2006-06-29 | Rigel Pharmaceuticals, Inc. | Spiro-2, 4-pyrimidinediamine compounds and their uses |
US7442716B2 (en) | 2004-12-17 | 2008-10-28 | Merck Frosst Canada Ltd. | 2-(phenyl or heterocyclic)-1H-phenantrho[9,10-d]imidazoles as mPGES-1 inhibitors |
AU2005322855B2 (en) | 2004-12-30 | 2012-09-20 | Exelixis, Inc. | Pyrimidine derivatives as kinase modulators and method of use |
DE602006010979D1 (de) * | 2005-01-19 | 2010-01-21 | Rigel Pharmaceuticals Inc | Prodrugs aus 2,4-pyrimidindiamin-verbindungen und ihre verwendungen |
CA2604551A1 (en) | 2005-05-03 | 2007-03-08 | Rigel Pharmaceuticals, Inc. | Jak kinase inhibitors and their uses |
EP1904457B1 (en) * | 2005-06-08 | 2017-09-06 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
US20070203161A1 (en) * | 2006-02-24 | 2007-08-30 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
CA2607901C (en) | 2005-06-13 | 2016-08-16 | Rigel Pharmaceuticals, Inc. | Methods and compositions for treating degenerative bone disorders using a syk inhibitory 2,4-pyrimidinediamine |
WO2007006926A2 (fr) | 2005-07-11 | 2007-01-18 | Sanofi-Aventis | Nouveaux derives de 2,4-dianilinopyrimidines, leur preparation, a titre de medicaments, compositions pharmaceutiques et notamment comme inhibiteurs de ikk |
PT1913009E (pt) | 2005-07-28 | 2010-06-25 | Intervet Int Bv | Novos (tio)carbamatos de benzimidazole com actividade antiparasitária e sua síntese |
JP4981673B2 (ja) | 2005-09-13 | 2012-07-25 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 安定性が改善されたクロロメチルフォスフェイト誘導体を含む組成物およびその製造方法 |
CA2627242A1 (en) * | 2005-10-31 | 2007-05-10 | Rigel Pharmaceuticals, Inc. | Compositions and methods for treating inflammatory disorders |
NZ592990A (en) | 2005-11-01 | 2013-01-25 | Targegen Inc | Bi-aryl meta-pyrimidine inhibitors of kinases |
US7713987B2 (en) * | 2005-12-06 | 2010-05-11 | Rigel Pharmaceuticals, Inc. | Pyrimidine-2,4-diamines and their uses |
TW200736232A (en) | 2006-01-26 | 2007-10-01 | Astrazeneca Ab | Pyrimidine derivatives |
WO2007085540A1 (en) | 2006-01-27 | 2007-08-02 | Glaxo Group Limited | 1h-indaz0l-4-yl-2 , 4-pyrimidinediamine derivatives |
KR101411695B1 (ko) * | 2006-02-17 | 2014-07-03 | 리겔 파마슈티칼스, 인크. | 자가면역 질환의 치료 또는 예방을 위한 2,4-피리미딘디아민 화합물 |
US8962643B2 (en) * | 2006-02-24 | 2015-02-24 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the JAK pathway |
US7776855B2 (en) | 2006-07-27 | 2010-08-17 | Janssen Pharmaceutica N.V. | Antimicrobial oxazolidinone prodrugs |
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