JP2003528871A5 - - Google Patents
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- Publication number
- JP2003528871A5 JP2003528871A5 JP2001570654A JP2001570654A JP2003528871A5 JP 2003528871 A5 JP2003528871 A5 JP 2003528871A5 JP 2001570654 A JP2001570654 A JP 2001570654A JP 2001570654 A JP2001570654 A JP 2001570654A JP 2003528871 A5 JP2003528871 A5 JP 2003528871A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- hydrogen
- halo
- independently hydrogen
- pyrrolidinyl
- 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.)
- Ceased
Links
- 125000000217 alkyl group Chemical group 0.000 description 11
- 229910052739 hydrogen Inorganic materials 0.000 description 11
- 239000001257 hydrogen Substances 0.000 description 11
- 150000002431 hydrogen Chemical class 0.000 description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 5
- -1 bromo, iodo Chemical group 0.000 description 5
- 125000001475 halogen functional group Chemical group 0.000 description 4
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 description 3
- 125000001188 haloalkyl group Chemical group 0.000 description 3
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 description 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 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 description 3
- 125000003710 aryl alkyl group Chemical group 0.000 description 1
- 125000003118 aryl group Chemical group 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
Description
個々のR1及びR3は独立して、水素、ハロ、アルキル、ハロアルキル、ニトロ、アラルコキシ、-OR 8 , -R11-OR 8 , -N(R8)R9, -C(O)OR8, -R11-C(O)OR8, -C(O)N(R8)R9, -R11-C(O)N(R8)R9, -C(O)N(R8)CH2C(O)N(R8)R9, -N(R8)C(O)N(R8)R9, -N(R8)C(O)R9, -N(R8)S(O)2R10及び-N(R8)C(O)N(R8)-CH2C(O)N(R8)R9から成る群から選択され;
R2は、水素、アルキル、ブロモ、ヨード、-N(R7)-(CH2)p-N(R8)R9(ここでpは1〜4)である)、-(CH2)q-N(R7)-CH2-C(O)-OR8(ここでqは0〜3である)、4−モルホリニル、1−ピペリジニル、1−ピペラジニル又は1−ピロリジニルであり;
個々のR4は独立して、水素又はアルキルであり;
R2は、水素、アルキル、ブロモ、ヨード、-N(R7)-(CH2)p-N(R8)R9(ここでpは1〜4)である)、-(CH2)q-N(R7)-CH2-C(O)-OR8(ここでqは0〜3である)、4−モルホリニル、1−ピペリジニル、1−ピペラジニル又は1−ピロリジニルであり;
個々のR4は独立して、水素又はアルキルであり;
個々のR5は独立して、水素、ハロ、ハロアルキル、アルキル、ニトロ、-OR8, -C(O)OR8, -C(O)N(R8)R9, -N(R8)R9, -N(R8)C(O)R8又は-N(H)S(O)2R10であり;
個々のR6は独立して、水素、アルキル、アリール、アラルキル、ハロ、-N(R8)R9, -N(R7)-(CH2)p-N(R8)R9(ここでpは1〜4である)、-(CH2)q-N(R7)-CH2-C(O)OR8(ここでqは0〜3である)、4−モルホリニル、1−ピペリジニル、1−ピペラジニル又は1−ピロリジニルであり;
個々のR7は、水素又はアルキルである;
個々のR6は独立して、水素、アルキル、アリール、アラルキル、ハロ、-N(R8)R9, -N(R7)-(CH2)p-N(R8)R9(ここでpは1〜4である)、-(CH2)q-N(R7)-CH2-C(O)OR8(ここでqは0〜3である)、4−モルホリニル、1−ピペリジニル、1−ピペラジニル又は1−ピロリジニルであり;
個々のR7は、水素又はアルキルである;
R2が、水素、アルキル、ブロモ、ヨード、-N(R7)-(CH2)p-N(R8)R9(ここでpは1〜4である)、-(CH2)q-N(R7)-CH2-C(O)-OR8(ここでqは0〜3である)、4−モルホリニル、1−ピペリジニル、1−ピペラジニル又は1−ピロリジニルであり;
R4が、水素又はアルキルであり;
R5が、水素、ハロ、ハロアルキル、アルキル、ニトロ、-OR8, -C(O)OR8, -C(O)N(R8)R9, -N(R8)R9, -N(R8)C(O)R8又は-N(H)S(O)2R10であり;
個々のR7が、水素又はアルキルであり;そして
個々のR8及びR9が独立して、水素又はアルキルであるそのサブグループの化合物である。
R4が、水素又はアルキルであり;
R5が、水素、ハロ、ハロアルキル、アルキル、ニトロ、-OR8, -C(O)OR8, -C(O)N(R8)R9, -N(R8)R9, -N(R8)C(O)R8又は-N(H)S(O)2R10であり;
個々のR7が、水素又はアルキルであり;そして
個々のR8及びR9が独立して、水素又はアルキルであるそのサブグループの化合物である。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US19216800P | 2000-03-27 | 2000-03-27 | |
US60/192,168 | 2000-03-27 | ||
US09/814,787 US6525051B2 (en) | 2000-03-27 | 2001-03-22 | N-heterocyclic derivatives as NOS inhibitors |
US09/814,787 | 2001-03-22 | ||
PCT/US2001/009481 WO2001072744A1 (en) | 2000-03-27 | 2001-03-26 | N-heterocyclic derivatives as nos inhibitors |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2003528871A JP2003528871A (ja) | 2003-09-30 |
JP2003528871A5 true JP2003528871A5 (ja) | 2011-12-15 |
Family
ID=26887800
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2001570654A Ceased JP2003528871A (ja) | 2000-03-27 | 2001-03-26 | Nosインヒビターとしてのn−複素環式誘導体 |
Country Status (13)
Country | Link |
---|---|
US (1) | US6525051B2 (ja) |
EP (1) | EP1268471B1 (ja) |
JP (1) | JP2003528871A (ja) |
AT (1) | ATE252097T1 (ja) |
AU (1) | AU2001245972A1 (ja) |
DE (1) | DE60101000T2 (ja) |
DK (1) | DK1268471T3 (ja) |
ES (1) | ES2208578T3 (ja) |
HK (1) | HK1053834A1 (ja) |
NO (1) | NO20024614L (ja) |
PT (1) | PT1268471E (ja) |
TR (1) | TR200302268T4 (ja) |
WO (1) | WO2001072744A1 (ja) |
Families Citing this family (35)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6432947B1 (en) | 1997-02-19 | 2002-08-13 | Berlex Laboratories, Inc. | N-heterocyclic derivatives as NOS inhibitors |
US7012098B2 (en) * | 2001-03-23 | 2006-03-14 | Pharmacia Corporation | Inhibitors of inducible nitric oxide synthase for chemoprevention and treatment of cancers |
JP2005519034A (ja) * | 2001-11-30 | 2005-06-30 | シンタ ファーマシューティカルズ コーポレーション | ピリミジン化合物 |
TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
EP1795192A3 (en) * | 2002-04-30 | 2008-05-07 | Bayer Schering Pharma Aktiengesellschaft | 1-(Pyridazin-3-yl)-imidazole derivatives as inhibitors of nitric oxide synthase (NOS) |
US6982259B2 (en) * | 2002-04-30 | 2006-01-03 | Schering Aktiengesellschaft | N-heterocyclic derivatives as NOS inhibitors |
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. |
WO2004056807A1 (en) | 2002-12-20 | 2004-07-08 | Pfizer Products Inc. | Pyrimidine derivatives for the treatment of abnormal cell growth |
US7109337B2 (en) | 2002-12-20 | 2006-09-19 | Pfizer Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
US20080058297A1 (en) * | 2003-05-29 | 2008-03-06 | Synta Pharmaceuticals Corp. | Heterocyclic Compounds For Preventing And Treating Disorders Associated With Excessive Bone Loss |
KR20120062863A (ko) * | 2003-07-30 | 2012-06-14 | 리겔 파마슈티칼스, 인크. | 자가면역 질환의 치료 또는 예방에 사용하기 위한 2,4-피리미딘디아민 화합물 |
JP2007537235A (ja) | 2004-05-14 | 2007-12-20 | ファイザー・プロダクツ・インク | 異常細胞増殖の治療用ピリミジン誘導体 |
MXPA06013165A (es) | 2004-05-14 | 2007-02-13 | Pfizer Prod Inc | Derivados de pirimidina para el tratamiento de crecimiento de celulas anormal. |
EP1751142A1 (en) | 2004-05-14 | 2007-02-14 | Pfizer Products Incorporated | Pyrimidines derivatives for the treatment of abnormal cell growth |
JP4990766B2 (ja) * | 2004-07-01 | 2012-08-01 | シンタ ファーマシューティカルズ コーポレーション | 二置換型ヘテロアリール化合物 |
CA2584295C (en) * | 2004-11-24 | 2014-08-26 | Rigel Pharmaceuticals, Inc. | Spiro-2, 4-pyrimidinediamine compounds and their uses |
ES2440965T3 (es) * | 2005-01-14 | 2014-01-31 | Chemocentryx, Inc. | Heteroaril-sulfonamidas y CCR2 |
US7622583B2 (en) | 2005-01-14 | 2009-11-24 | Chemocentryx, Inc. | Heteroaryl sulfonamides and CCR2 |
EP2161275A1 (en) | 2005-01-19 | 2010-03-10 | Rigel Pharmaceuticals, Inc. | Prodrugs of 2,4-pyrimidinediamine compounds and their uses |
WO2007027238A2 (en) * | 2005-05-03 | 2007-03-08 | Rigel Pharmaceuticals, Inc. | Jak kinase inhibitors and their uses |
WO2007039578A1 (en) * | 2005-10-05 | 2007-04-12 | Nycomed Gmbh | Imidazolyl-substituted azabenzophenone compounds |
ES2593486T3 (es) | 2007-04-18 | 2016-12-09 | Pfizer Products Inc. | Derivados de sulfonil amida para el tratamiento del crecimiento celular anómalo |
KR101849560B1 (ko) | 2007-07-12 | 2018-04-17 | 케모센트릭스, 인크. | 염증의 치료를 위한 ccr2 조절물질로서 융합된 헤테로아릴 피리딜과 페닐 벤젠술폰아마이드 |
PT2323993E (pt) | 2008-04-16 | 2015-10-12 | Portola Pharm Inc | 2,6-diamino-pirimidina-5-il-carboxamidas como inibidores de quinasses syk ou jak |
US8138339B2 (en) | 2008-04-16 | 2012-03-20 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
HUE035029T2 (en) | 2008-05-21 | 2018-03-28 | Ariad Pharma Inc | Kinase inhibitor phosphorus derivatives |
US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
EA201391626A1 (ru) | 2011-05-04 | 2014-03-31 | Ариад Фармасьютикалз, Инк. | Соединения для ингибирования клеточной пролиферации в egfr-стимулированных типах рака |
AU2012340555B2 (en) | 2011-11-23 | 2016-10-20 | Portola Pharmaceuticals, Inc. | Pyrazine kinase inhibitors |
US20150166591A1 (en) | 2012-05-05 | 2015-06-18 | Ariad Pharmaceuticals, Inc. | Methods and compositions for raf kinase mediated diseases |
US9611283B1 (en) | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
KR20190088513A (ko) | 2016-11-23 | 2019-07-26 | 케모센트릭스, 인크. | 국소 분절 사구체경화증의 치료 방법 |
JP7301758B2 (ja) * | 2017-03-13 | 2023-07-03 | インペティス・バイオサイエンシーズ・リミテッド | 縮合二環式化合物、その組成物及び応用 |
RU2020113612A (ru) | 2017-10-11 | 2021-11-12 | Хемоцентрикс, Инк. | Лечение фокально-сегментарного гломерулосклероза антагонистами ccr2 |
KR102563834B1 (ko) * | 2021-06-28 | 2023-08-04 | 순천대학교 산학협력단 | 세포자멸사를 유도하는 신규한 화합물 및 이를 포함하는 항암용 조성물 |
Family Cites Families (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS6339875A (ja) | 1986-08-05 | 1988-02-20 | Nissin Food Prod Co Ltd | ピリミジン誘導体 |
DE4118720A1 (de) | 1991-06-07 | 1992-12-10 | Bayer Ag | Substituierte imidazolinylpyrimidine |
WO1993017009A1 (en) | 1992-02-28 | 1993-09-02 | Zenyaku Kogyo Kabushiki Kaisha | s-TRIAZINE DERIVATIVE AND REMEDY FOR ESTROGEN-DEPENDENT DISEASES CONTAINING THE SAME AS ACTIVE INGREDIENT |
US5593992A (en) | 1993-07-16 | 1997-01-14 | Smithkline Beecham Corporation | Compounds |
ATE163647T1 (de) | 1993-08-26 | 1998-03-15 | Ono Pharmaceutical Co | 4-aminopyrimidin derivate |
US5426110A (en) | 1993-10-06 | 1995-06-20 | Eli Lilly And Company | Pyrimidinyl-glutamic acid derivatives |
US5629322A (en) | 1994-11-15 | 1997-05-13 | Merck & Co., Inc. | Cyclic amidine analogs as inhibitors of nitric oxide synthase |
WO1996014842A1 (en) | 1994-11-15 | 1996-05-23 | Merck & Co., Inc. | Substituted heterocycles as inhibitors of nitric oxide synthase |
CA2214685C (en) * | 1995-03-10 | 2008-05-20 | Berlex Laboratories, Inc. | Benzamidine derivatives their preparation and their use as anti-coagulants |
DE19541146A1 (de) * | 1995-10-25 | 1997-04-30 | Schering Ag | Imidazolderivate und deren Verwendung als Stickstoffmonoxid-Synthase-Inhibitoren |
ZA977427B (en) | 1996-09-04 | 1998-03-02 | Dainippon Pharmaceutical Co | 2,4-disubstituted pyrimidine derivative, process for preparing the same, and a pharmaceutical composition containing the same. |
JP2001505585A (ja) * | 1996-12-16 | 2001-04-24 | 藤沢薬品工業株式会社 | 新規アミド化合物およびそれらの一酸化窒素シンターゼ阻害剤としての用途 |
CN1100777C (zh) | 1997-02-19 | 2003-02-05 | 伯莱克斯实验室公司 | 作为nos抑制剂的n-杂环衍生物 |
-
2001
- 2001-03-22 US US09/814,787 patent/US6525051B2/en not_active Expired - Fee Related
- 2001-03-26 DE DE60101000T patent/DE60101000T2/de not_active Expired - Lifetime
- 2001-03-26 AT AT01918958T patent/ATE252097T1/de not_active IP Right Cessation
- 2001-03-26 AU AU2001245972A patent/AU2001245972A1/en not_active Abandoned
- 2001-03-26 EP EP01918958A patent/EP1268471B1/en not_active Expired - Lifetime
- 2001-03-26 WO PCT/US2001/009481 patent/WO2001072744A1/en active IP Right Grant
- 2001-03-26 PT PT01918958T patent/PT1268471E/pt unknown
- 2001-03-26 JP JP2001570654A patent/JP2003528871A/ja not_active Ceased
- 2001-03-26 TR TR2003/02268T patent/TR200302268T4/xx unknown
- 2001-03-26 ES ES01918958T patent/ES2208578T3/es not_active Expired - Lifetime
- 2001-03-26 DK DK01918958T patent/DK1268471T3/da active
-
2002
- 2002-09-26 NO NO20024614A patent/NO20024614L/no not_active Application Discontinuation
-
2003
- 2003-07-02 HK HK03104720.6A patent/HK1053834A1/zh unknown
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