JP2007537147A5 - - Google Patents
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- JP2007537147A5 JP2007537147A5 JP2006547452A JP2006547452A JP2007537147A5 JP 2007537147 A5 JP2007537147 A5 JP 2007537147A5 JP 2006547452 A JP2006547452 A JP 2006547452A JP 2006547452 A JP2006547452 A JP 2006547452A JP 2007537147 A5 JP2007537147 A5 JP 2007537147A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- composition
- unsubstituted
- compound
- 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.)
- Pending
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- 125000000217 alkyl group Chemical group 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 13
- 239000000203 mixture Substances 0.000 claims 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 230000002491 angiogenic Effects 0.000 claims 3
- 125000003710 aryl alkyl group Chemical group 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 206010003816 Autoimmune disease Diseases 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 201000009596 autoimmune hypersensitivity disease Diseases 0.000 claims 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 201000009910 diseases by infectious agent Diseases 0.000 claims 2
- 125000004404 heteroalkyl group Chemical group 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 125000000547 substituted alkyl group Chemical group 0.000 claims 2
- 125000003107 substituted aryl group Chemical group 0.000 claims 2
- 241000222722 Leishmania <genus> Species 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010025310 Other lymphomas Diseases 0.000 claims 1
- 241000224016 Plasmodium Species 0.000 claims 1
- 206010039073 Rheumatoid arthritis Diseases 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000003435 aroyl group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- -1 dialkylsulfinium Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 150000002829 nitrogen Chemical group 0.000 claims 1
- 244000045947 parasites Species 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 201000004681 psoriasis Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 125000005309 thioalkoxy group Chemical group 0.000 claims 1
- 125000005296 thioaryloxy group Chemical group 0.000 claims 1
- 0 C[C@]1(C(CC=C(C)CO)CC1)C([C@](*)[C@@](CC1)C=CC)[C@]11OC1 Chemical compound C[C@]1(C(CC=C(C)CO)CC1)C([C@](*)[C@@](CC1)C=CC)[C@]11OC1 0.000 description 7
Claims (13)
- 請求項1に記載の化合物であって、Bは、式
ここで、
R3は、水素またはアルキルであり;
R4およびR5は、各々、独立して、水素、置換アルキルもしくは非置換アルキル、置換アリールもしくは非置換アリール、置換アリールアルキルもしくは非置換アリールアルキル、置換ヘテロアリールもしくは非置換ヘテロアリールまたは置換ヘテロアルキルもしくは非置換ヘテロアルキルであるか;あるいは
R3およびR5は、一緒になってアルキレン基を形成し;
Zは、−C(O)−または−アルキレン−C(O)−であり;そして
Pは、−OR6または−N(R7)R8であり、ここで、R6、R7およびR8は、各々、独立して、水素、置換アルキルもしくは非置換アルキル、置換アリールもしくは非置換アリールまたは置換アザシクロアルキルもしくは非置換アザシクロアルキルであるか、あるいはR7およびR8は、該R7および該R8が結合する窒素原子と一緒になって、複素環式環構造を形成する、化合物。 - 請求項3に記載の化合物であって、R5は、直鎖C1−C6アルキルまたは分枝C1−C6アルキル、ヒドロキシル置換された直鎖C1−C6アルキルまたはヒドロキシル置換された分枝C1−C6アルキルであり;そして
R3、R7およびR8は、各々、水素である、化合物。 - 請求項1または請求項2に記載の化合物および薬学的に受容可能なキャリアを含む、薬学的組成物。
- 被験体における脈管形成疾患を処置するための組成物であって、該組成物が、治療的に有効な量の請求項1または請求項2に記載の化合物を含有する、組成物。
- 前記脈管形成疾患が、癌である、請求項7に記載の組成物。
- 前記脈管形成疾患が、リンパ腫である、請求項8に記載の組成物。
- 被験体における自己免疫疾患を処置するための組成物であって、該組成物が、治療的に有効な量の請求項1または請求項2に記載の化合物を含有する、組成物。
- 前記自己免疫疾患が、慢性関節リウマチ、乾癬または多発性硬化症である、請求項10に記載の組成物。
- 被験体における寄生生物による感染を処置するための組成物であって、該組成物が、治療的に有効な量の請求項1または請求項2に記載の化合物を含有する、組成物。
- 前記感染が、Plasmodium種およびLeishmania種からなる群より選択される寄生生物による、請求項12に記載の組成物。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US53343103P | 2003-12-29 | 2003-12-29 | |
PCT/US2004/043586 WO2005066197A2 (en) | 2003-12-29 | 2004-12-29 | Inhibitors of methionine aminopeptidase-2 and uses thereof |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2007537147A JP2007537147A (ja) | 2007-12-20 |
JP2007537147A5 true JP2007537147A5 (ja) | 2008-02-07 |
Family
ID=34748901
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2006547452A Pending JP2007537147A (ja) | 2003-12-29 | 2004-12-29 | メチオニンアミノペプチダーゼ−2のインヒビターおよびその使用 |
Country Status (9)
Country | Link |
---|---|
US (1) | US20050239878A1 (ja) |
EP (1) | EP1699812A2 (ja) |
JP (1) | JP2007537147A (ja) |
KR (1) | KR20060130077A (ja) |
CN (1) | CN1902215A (ja) |
AU (1) | AU2004312512A1 (ja) |
CA (1) | CA2550873A1 (ja) |
NO (1) | NO20062812L (ja) |
WO (1) | WO2005066197A2 (ja) |
Families Citing this family (37)
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JP4514455B2 (ja) * | 2002-04-11 | 2010-07-28 | チルドレンズ メディカル センター コーポレーション | Tnp−470ポリマー複合体及びその使用 |
WO2003086178A2 (en) * | 2002-04-11 | 2003-10-23 | Children's Medical Center Corporation | Methods for inhibiting vascular hyperpermeability |
US20070254843A1 (en) * | 2006-04-18 | 2007-11-01 | Praecis Pharmaceuticals Incorporated | Methods for treating bone associated diseases by the use of methionine aminopeptidase-2 inhibitors |
WO2008066641A2 (en) * | 2006-11-06 | 2008-06-05 | Praecis Pharmaceuticals Incorporated | Methods for treating mitf associated diseases by the use of methionine aminopeptidase-2 inhibitors |
JP2010531896A (ja) * | 2007-06-26 | 2010-09-30 | チルドレンズ メディカル センター コーポレーション | 治療的投与のためのMetAP−2阻害剤ポリマーソーム |
AU2009270799B2 (en) * | 2008-07-18 | 2016-05-19 | Zafgen, Inc. | Methods of treating an overweight or obese subject |
WO2013055385A2 (en) | 2011-10-03 | 2013-04-18 | Zafgen Corporation | Methods of treating age related disorders |
US8642650B2 (en) | 2008-12-04 | 2014-02-04 | Zafgen, Inc. | Methods of treating an overweight or obese subject |
WO2010065877A2 (en) | 2008-12-04 | 2010-06-10 | Zafgen Corporation | Methods of treating an overweight or obese subject |
AU2010303270A1 (en) | 2009-10-09 | 2012-05-03 | Zafgen Corporation | Sulphone compounds for use in the treatment of obesity |
WO2011085198A1 (en) | 2010-01-08 | 2011-07-14 | Zafgen Corporation | Metap-2 inhibitor for use in treating benign prostatic hypertrophy (bph) |
EP2521719B1 (en) | 2010-01-08 | 2015-07-29 | Zafgen, Inc. | Fumagillol type compounds and methods of making and using same |
WO2011088055A2 (en) | 2010-01-12 | 2011-07-21 | Zafgen Corporation | Methods and compositions for treating cardiovascular disorders |
US20130266578A1 (en) | 2010-04-07 | 2013-10-10 | Thomas E. Hughes | Methods of treating an overweight subject |
BR112013001613A2 (pt) | 2010-07-22 | 2016-05-24 | Zafgen Inc | compostos tricíclicos e métodos para fazer e usar os mesmos. |
KR101892768B1 (ko) | 2010-11-09 | 2018-08-28 | 자프겐 인크. | Metap-2 저해제의 결정질 고체 및 그의 제조 및 이용 방법 |
US20140073691A1 (en) * | 2010-11-10 | 2014-03-13 | Zafgen, Inc. | Methods and composition for Treating Thyroid Hormone Related Disorders |
WO2012074968A1 (en) | 2010-11-29 | 2012-06-07 | Zafgen Corporation | Methods of reducing risk of hepatobiliary dysfunction during rapid weight loss with metap-2 inhibitors |
EP2646016B1 (en) | 2010-11-29 | 2017-05-17 | Zafgen, Inc. | Treatment if obesity using non-daily administration of 6-0-(4-dimethylaminoethoxy)cinnamoyl fumagillol |
US9189078B2 (en) | 2010-12-20 | 2015-11-17 | Apple Inc. | Enhancing keycap legend visibility with optical components |
US9321740B2 (en) | 2011-01-26 | 2016-04-26 | Zafgen, Inc. | Tetrazole compounds and methods of making and using same |
KR101875988B1 (ko) * | 2011-03-08 | 2018-07-06 | 자프겐 인크. | 옥사스피로[2.5]옥탄 유도체 및 유사체 |
BR112013028665A2 (pt) | 2011-05-06 | 2016-09-06 | Zafgen Inc | compostos de sulfonamida tricíclicos e métodos para fazer e usar os mesmos |
KR101979039B1 (ko) | 2011-05-06 | 2019-05-15 | 자프겐 인크. | 부분 포화된 삼환식 화합물 및 그리고 그의 제조방법 및 그를 이용하는 방법 |
MX343688B (es) | 2011-05-06 | 2016-11-16 | Zafgen Inc | Compuestos tricíclicos de sulfonamida y pirazolo y métodos para su fabricación y uso. |
US9440943B2 (en) | 2012-01-18 | 2016-09-13 | Zafgen, Inc. | Tricyclic sulfone compounds and methods of making and using same |
JP6035347B2 (ja) | 2012-01-18 | 2016-11-30 | ザフゲン,インコーポレイテッド | 三環式スルホンアミド化合物ならびにその作製および使用方法 |
KR20150016303A (ko) | 2012-05-07 | 2015-02-11 | 자프겐 인크. | 6-o-(4-디메틸아미노에톡시) 신나모일 푸마지롤의 옥살레이트 염의 다형체 염 및 이의 제조 및 사용 방법 |
CA2872876A1 (en) | 2012-05-08 | 2013-11-14 | Zafgen, Inc. | Treating hypothalamic obesity with metap2 inhibitors |
KR20150016534A (ko) | 2012-05-09 | 2015-02-12 | 자프겐 인크. | 푸마지롤형 화합물 및 이의 제조 및 사용 방법 |
KR20150080614A (ko) | 2012-11-05 | 2015-07-09 | 자프겐 인크. | 비만의 치료 및/또는 제어에서 사용하기 위한 트리시클릭 화합물 |
NZ707773A (en) | 2012-11-05 | 2019-05-31 | Zafgen Inc | Methods of treating liver diseases |
MX2015005732A (es) | 2012-11-05 | 2015-12-16 | Zafgen Inc | Compuestos tricíclicos y métodos para hacer y utilizar los mismos. |
KR20150126924A (ko) | 2013-03-14 | 2015-11-13 | 자프겐 인크. | 신장 질환 및 기타 장애의 치료 방법 |
AR105671A1 (es) | 2015-08-11 | 2017-10-25 | Zafgen Inc | Compuestos heterocíclicos de fumagillol y sus métodos de elaboración y uso |
CN106432255A (zh) | 2015-08-11 | 2017-02-22 | 扎夫根公司 | 烟曲霉素醇螺环化合物和制备和使用其的方法 |
WO2018148638A1 (en) * | 2017-02-10 | 2018-08-16 | Zafgen, Inc. | Pharmaceutical compositions of metap-2 inhibitors |
Family Cites Families (14)
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FR2546163B1 (fr) * | 1983-05-16 | 1987-10-09 | Centre Nat Rech Scient | Nouveaux derives acyles hydrosolubles de peptides ou d'amino-acides, leur preparation et leur application |
US5135919A (en) * | 1988-01-19 | 1992-08-04 | Children's Medical Center Corporation | Method and a pharmaceutical composition for the inhibition of angiogenesis |
PH26256A (en) * | 1988-08-12 | 1992-04-01 | Fujisawa Pharmaceutical Co | Oxaspiro [2,5] octane derivative |
DE68927904T2 (de) * | 1988-09-01 | 1997-09-04 | Takeda Chemical Industries Ltd | Fumagillol-Derivate |
US5180738A (en) * | 1988-09-01 | 1993-01-19 | Takeda Chemical Industries | Fumagillol derivatives and pharmaceutical compositions thereof |
US5290807A (en) * | 1989-08-10 | 1994-03-01 | Children's Medical Center Corporation | Method for regressing angiogenesis using o-substituted fumagillol derivatives |
US6017954A (en) * | 1989-08-10 | 2000-01-25 | Children's Medical Center Corp. | Method of treating tumors using O-substituted fumagillol derivatives |
EP0415294A3 (en) * | 1989-08-31 | 1991-06-12 | Takeda Chemical Industries, Ltd. | Cyclohexanol derivatives, production and use thereof |
JPH06157344A (ja) * | 1992-02-07 | 1994-06-03 | Childrens Medical Center Corp:The | 血管新生阻害のための医薬製剤及び血管新生阻害方法 |
DE69311278T2 (de) * | 1992-12-16 | 1997-10-30 | Takeda Chemical Industries Ltd | Stabile pharmazeutische Zubereitung mit Fumagillolderivaten |
FR2733498B1 (fr) * | 1995-04-27 | 1997-05-30 | Adir | Nouveaux composes cyclohexaniques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
WO1998056372A1 (en) * | 1997-06-09 | 1998-12-17 | Massachusetts Institute Of Technology | TYPE 2 METHIONINE AMINOPEPTIDASE (MetAP2) INHIBITORS AND USES THEROF |
US6548477B1 (en) * | 2000-11-01 | 2003-04-15 | Praecis Pharmaceuticals Inc. | Therapeutic agents and methods of use thereof for the modulation of angiogenesis |
US6919307B2 (en) * | 2000-11-01 | 2005-07-19 | Praecis Pharmaceuticals, Inc. | Therapeutic agents and methods of use thereof for the modulation of angiogenesis |
-
2004
- 2004-12-29 JP JP2006547452A patent/JP2007537147A/ja active Pending
- 2004-12-29 WO PCT/US2004/043586 patent/WO2005066197A2/en active Application Filing
- 2004-12-29 CN CNA2004800393912A patent/CN1902215A/zh active Pending
- 2004-12-29 EP EP04815618A patent/EP1699812A2/en not_active Withdrawn
- 2004-12-29 CA CA002550873A patent/CA2550873A1/en not_active Abandoned
- 2004-12-29 US US11/025,568 patent/US20050239878A1/en not_active Abandoned
- 2004-12-29 AU AU2004312512A patent/AU2004312512A1/en not_active Abandoned
- 2004-12-29 KR KR1020067012422A patent/KR20060130077A/ko not_active Application Discontinuation
-
2006
- 2006-06-15 NO NO20062812A patent/NO20062812L/no not_active Application Discontinuation
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