JP2011504964A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2011504964A5 JP2011504964A5 JP2010536101A JP2010536101A JP2011504964A5 JP 2011504964 A5 JP2011504964 A5 JP 2011504964A5 JP 2010536101 A JP2010536101 A JP 2010536101A JP 2010536101 A JP2010536101 A JP 2010536101A JP 2011504964 A5 JP2011504964 A5 JP 2011504964A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- pharmaceutically acceptable
- acceptable salt
- complex
- acid
- 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.)
- Granted
Links
- 150000003839 salts Chemical class 0.000 claims 40
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 claims 12
- 150000001721 carbon Chemical group 0.000 claims 9
- 229910052799 carbon Inorganic materials 0.000 claims 9
- 239000000203 mixture Substances 0.000 claims 9
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- NGGMYCMLYOUNGM-CSDLUJIJSA-N fumagillin Chemical class C([C@H]([C@H]([C@@H]1[C@]2(C)[C@H](O2)CC=C(C)C)OC)OC(=O)\C=C\C=C\C=C\C=C\C(O)=O)C[C@@]21CO2 NGGMYCMLYOUNGM-CSDLUJIJSA-N 0.000 claims 8
- 239000003937 drug carrier Substances 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- LMDZBCPBFSXMTL-UHFFFAOYSA-N 1-Ethyl-3-(3-dimethylaminopropyl)carbodiimide Substances CCN=C=NCCCN(C)C LMDZBCPBFSXMTL-UHFFFAOYSA-N 0.000 claims 4
- FPQQSJJWHUJYPU-UHFFFAOYSA-N 3-(dimethylamino)propyliminomethylidene-ethylazanium;chloride Chemical compound Cl.CCN=C=NCCCN(C)C FPQQSJJWHUJYPU-UHFFFAOYSA-N 0.000 claims 4
- 238000001816 cooling Methods 0.000 claims 4
- 125000005647 linker group Chemical group 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- RTBFRGCFXZNCOE-UHFFFAOYSA-N 1-methylsulfonylpiperidin-4-one Chemical compound CS(=O)(=O)N1CCC(=O)CC1 RTBFRGCFXZNCOE-UHFFFAOYSA-N 0.000 claims 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims 3
- JFCQEDHGNNZCLN-UHFFFAOYSA-N anhydrous glutaric acid Natural products OC(=O)CCCC(O)=O JFCQEDHGNNZCLN-UHFFFAOYSA-N 0.000 claims 3
- 238000004581 coalescence Methods 0.000 claims 3
- 239000002552 dosage form Substances 0.000 claims 3
- 239000000945 filler Substances 0.000 claims 3
- 125000000524 functional group Chemical group 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- KRNJGCZJVCWXFN-JGVFFNPUSA-N (2s,3r)-2-methyl-3-(3-methylbut-2-enyl)oxirane Chemical group C[C@@H]1O[C@@H]1CC=C(C)C KRNJGCZJVCWXFN-JGVFFNPUSA-N 0.000 claims 2
- YAQYVSLBYMDWPD-JGVFFNPUSA-N (2s,3r)-2-methyl-3-(3-methylbutyl)oxirane Chemical group CC(C)CC[C@H]1O[C@H]1C YAQYVSLBYMDWPD-JGVFFNPUSA-N 0.000 claims 2
- WXGOLMICHIGDMF-SGAXSIHGSA-N (z)-n-phenylmethoxyethanimine Chemical group C\C=N/OCC1=CC=CC=C1 WXGOLMICHIGDMF-SGAXSIHGSA-N 0.000 claims 2
- IILGVAQPFQYXIO-UHFFFAOYSA-N 2-methylhepta-2,5-diene Chemical group CC=CCC=C(C)C IILGVAQPFQYXIO-UHFFFAOYSA-N 0.000 claims 2
- LXBJRNXXTAWCKU-UHFFFAOYSA-N 6-methylhept-2-ene Chemical group CC=CCCC(C)C LXBJRNXXTAWCKU-UHFFFAOYSA-N 0.000 claims 2
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical group OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 2
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims 2
- OFOBLEOULBTSOW-UHFFFAOYSA-N Malonic acid Chemical compound OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims 2
- 229930195725 Mannitol Natural products 0.000 claims 2
- KKEYFWRCBNTPAC-UHFFFAOYSA-N Terephthalic acid Chemical compound OC(=O)C1=CC=C(C(O)=O)C=C1 KKEYFWRCBNTPAC-UHFFFAOYSA-N 0.000 claims 2
- WNLRTRBMVRJNCN-UHFFFAOYSA-N adipic acid Chemical compound OC(=O)CCCCC(O)=O WNLRTRBMVRJNCN-UHFFFAOYSA-N 0.000 claims 2
- 239000011203 carbon fibre reinforced carbon Substances 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- QQVIHTHCMHWDBS-UHFFFAOYSA-N isophthalic acid Chemical compound OC(=O)C1=CC=CC(C(O)=O)=C1 QQVIHTHCMHWDBS-UHFFFAOYSA-N 0.000 claims 2
- 239000000594 mannitol Substances 0.000 claims 2
- 235000010355 mannitol Nutrition 0.000 claims 2
- BDJRBEYXGGNYIS-UHFFFAOYSA-N nonanedioic acid Chemical compound OC(=O)CCCCCCCC(O)=O BDJRBEYXGGNYIS-UHFFFAOYSA-N 0.000 claims 2
- XNGIFLGASWRNHJ-UHFFFAOYSA-N phthalic acid Chemical compound OC(=O)C1=CC=CC=C1C(O)=O XNGIFLGASWRNHJ-UHFFFAOYSA-N 0.000 claims 2
- WLJVNTCWHIRURA-UHFFFAOYSA-N pimelic acid Chemical compound OC(=O)CCCCCC(O)=O WLJVNTCWHIRURA-UHFFFAOYSA-N 0.000 claims 2
- 229920000642 polymer Polymers 0.000 claims 2
- CXMXRPHRNRROMY-UHFFFAOYSA-N sebacic acid Chemical compound OC(=O)CCCCCCCCC(O)=O CXMXRPHRNRROMY-UHFFFAOYSA-N 0.000 claims 2
- 125000006850 spacer group Chemical group 0.000 claims 2
- TYFQFVWCELRYAO-UHFFFAOYSA-N suberic acid Chemical compound OC(=O)CCCCCCC(O)=O TYFQFVWCELRYAO-UHFFFAOYSA-N 0.000 claims 2
- -1 substituted Chemical class 0.000 claims 2
- 239000004094 surface-active agent Substances 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- 125000006727 (C1-C6) alkenyl group Chemical group 0.000 claims 1
- QDIIYWBIGXHQNO-UHFFFAOYSA-N 3-carboxyoxypropanoic acid Chemical compound OC(=O)CCOC(O)=O QDIIYWBIGXHQNO-UHFFFAOYSA-N 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- 229920000858 Cyclodextrin Polymers 0.000 claims 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims 1
- 108090000790 Enzymes Proteins 0.000 claims 1
- 102000004190 Enzymes Human genes 0.000 claims 1
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims 1
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims 1
- 102100023174 Methionine aminopeptidase 2 Human genes 0.000 claims 1
- 108090000192 Methionyl aminopeptidases Proteins 0.000 claims 1
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 claims 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims 1
- DHKHKXVYLBGOIT-UHFFFAOYSA-N acetaldehyde Diethyl Acetal Natural products CCOC(C)OCC DHKHKXVYLBGOIT-UHFFFAOYSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 239000001361 adipic acid Substances 0.000 claims 1
- 235000011037 adipic acid Nutrition 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- CKLJMWTZIZZHCS-REOHCLBHSA-N aspartic acid group Chemical group N[C@@H](CC(=O)O)C(=O)O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims 1
- 150000001602 bicycloalkyls Chemical group 0.000 claims 1
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- CREMABGTGYGIQB-UHFFFAOYSA-N carbon carbon Chemical group C.C CREMABGTGYGIQB-UHFFFAOYSA-N 0.000 claims 1
- 238000003776 cleavage reaction Methods 0.000 claims 1
- 239000012141 concentrate Substances 0.000 claims 1
- 238000010276 construction Methods 0.000 claims 1
- 239000001530 fumaric acid Substances 0.000 claims 1
- 235000011087 fumaric acid Nutrition 0.000 claims 1
- 235000013922 glutamic acid Nutrition 0.000 claims 1
- 239000004220 glutamic acid Substances 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 150000003949 imides Chemical class 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 150000002576 ketones Chemical class 0.000 claims 1
- 239000008176 lyophilized powder Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 239000000178 monomer Substances 0.000 claims 1
- 235000006408 oxalic acid Nutrition 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 229960000502 poloxamer Drugs 0.000 claims 1
- 229920001983 poloxamer Polymers 0.000 claims 1
- 229950008882 polysorbate Drugs 0.000 claims 1
- 229920000136 polysorbate Polymers 0.000 claims 1
- 230000007017 scission Effects 0.000 claims 1
- 239000000600 sorbitol Substances 0.000 claims 1
- 238000003860 storage Methods 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 235000002906 tartaric acid Nutrition 0.000 claims 1
- 239000011975 tartaric acid Substances 0.000 claims 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims 1
- JRACLRIYQYGWAJ-LYGWUWPISA-N C[C@]1(C([C@@H]([C@@H](CC2)OC(NCc(cc3)ccc3N)=O)OC)[C@]22OC2)O[C@@H]1CC=C(C)C Chemical compound C[C@]1(C([C@@H]([C@@H](CC2)OC(NCc(cc3)ccc3N)=O)OC)[C@]22OC2)O[C@@H]1CC=C(C)C JRACLRIYQYGWAJ-LYGWUWPISA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US458207P | 2007-11-28 | 2007-11-28 | |
| US61/004,582 | 2007-11-28 | ||
| PCT/US2008/084539 WO2009073445A2 (en) | 2007-11-28 | 2008-11-24 | Biocompatible biodegradable fumagillin analog conjugates |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011504964A JP2011504964A (ja) | 2011-02-17 |
| JP2011504964A5 true JP2011504964A5 (cg-RX-API-DMAC10.html) | 2012-12-20 |
| JP5557746B2 JP5557746B2 (ja) | 2014-07-23 |
Family
ID=40600044
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010536101A Expired - Fee Related JP5557746B2 (ja) | 2007-11-28 | 2008-11-24 | 生体適合性生分解性フマギリンアナログ複合体 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US8399512B2 (cg-RX-API-DMAC10.html) |
| EP (1) | EP2217283A2 (cg-RX-API-DMAC10.html) |
| JP (1) | JP5557746B2 (cg-RX-API-DMAC10.html) |
| CN (1) | CN101990441A (cg-RX-API-DMAC10.html) |
| AU (1) | AU2008331516B2 (cg-RX-API-DMAC10.html) |
| BR (1) | BRPI0820229A2 (cg-RX-API-DMAC10.html) |
| CA (1) | CA2706914A1 (cg-RX-API-DMAC10.html) |
| EA (1) | EA020251B1 (cg-RX-API-DMAC10.html) |
| IL (1) | IL206057A0 (cg-RX-API-DMAC10.html) |
| MX (1) | MX2010005857A (cg-RX-API-DMAC10.html) |
| NZ (2) | NZ600039A (cg-RX-API-DMAC10.html) |
| WO (1) | WO2009073445A2 (cg-RX-API-DMAC10.html) |
| ZA (1) | ZA201003819B (cg-RX-API-DMAC10.html) |
Families Citing this family (87)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2004270251B2 (en) * | 2003-09-05 | 2011-03-31 | The General Hospital Corporation | Polyacetal drug conjugates as release system |
| BRPI0820229A2 (pt) | 2007-11-28 | 2017-05-09 | A Stevenson Cheri | conjugados de análogos de fumagilina biodegradáveis biocompatíveis |
| EP2317845A4 (en) * | 2008-07-18 | 2011-11-09 | Zafgen Inc | METHOD FOR TREATING AN OVERWEIGHT OR FATABLE PERSON |
| US20120004162A1 (en) | 2008-12-04 | 2012-01-05 | Vath James E | Methods of Treating an Overweight or Obese Subject |
| US8642650B2 (en) | 2008-12-04 | 2014-02-04 | 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 |
| AR074584A1 (es) * | 2008-12-10 | 2011-01-26 | Mersana Therapeutics Inc | Formulaciones farmaceuticas de conjugados camtotecina-polimero biocompatibles biodegradables |
| JP2012528240A (ja) * | 2009-05-28 | 2012-11-12 | メルサナ セラピューティックス， インコーポレイテッド | 可変速度放出リンカーを含むポリアル−薬物コンジュゲート |
| WO2011044506A2 (en) | 2009-10-09 | 2011-04-14 | Zafgen Corporation | Sulphone compounds and methods of making and using same |
| WO2011085198A1 (en) | 2010-01-08 | 2011-07-14 | Zafgen Corporation | Metap-2 inhibitor for use in treating benign prostatic hypertrophy (bph) |
| BR112012016793A2 (pt) | 2010-01-08 | 2018-07-31 | Zafgen Corp | compostos tipo fumagilol e métodos de fazer e usar os mesmos |
| US8349308B2 (en) | 2010-03-26 | 2013-01-08 | Mersana Therapeutics, Inc. | Modified polymers for delivery of polynucleotides, method of manufacture, and methods of use thereof |
| WO2011127304A2 (en) | 2010-04-07 | 2011-10-13 | Zafgen Corporation | Methods of treating an overweight subject |
| US9895449B2 (en) * | 2010-05-25 | 2018-02-20 | Syndevrx, Inc. | Polymer-conjugated MetAP2 inhibitors, and therapeutic methods of use thereof |
| WO2011150022A2 (en) | 2010-05-25 | 2011-12-01 | Syndevrx, Inc. | Polymer-conjugated metap2 inhibitors, and therapeutic methods of use thereof |
| BR112013001613A2 (pt) | 2010-07-22 | 2016-05-24 | Zafgen Inc | compostos tricíclicos e métodos para fazer e usar os mesmos. |
| PH12013500934A1 (en) | 2010-11-09 | 2022-10-24 | Zafgen Inc | Crystalline solids of a metap-2 inhibitor and methods of making and using same |
| JP2013543899A (ja) | 2010-11-29 | 2013-12-09 | ザフゲン，インコーポレイテッド | ６−ｏ−（４−ジメチルアミノエトキシ）シンナモイルフマギロールの非連日投与を用いた肥満の治療 |
| US9321740B2 (en) | 2011-01-26 | 2016-04-26 | Zafgen, Inc. | Tetrazole compounds and methods of making and using same |
| AU2012225531B2 (en) | 2011-03-08 | 2017-03-30 | Zafgen, Inc | Oxaspiro (2.5) octane derivatives and analogs |
| US9290472B2 (en) | 2011-05-06 | 2016-03-22 | Zafgen, Inc. | Partially saturated tricyclic compounds and methods of making and using same |
| WO2012154679A1 (en) | 2011-05-06 | 2012-11-15 | Zafgen Corporation | Tricyclic pyrazole sulfonamide compounds and methods of making and using same |
| AU2012253759B2 (en) | 2011-05-06 | 2016-01-21 | Zafgen Inc. | Tricyclic sulfonamide compounds and methods of making and using same |
| EP2717916B1 (en) | 2011-06-10 | 2017-03-08 | Mersana Therapeutics, Inc. | Protein-polymer-drug conjugates |
| US8815226B2 (en) | 2011-06-10 | 2014-08-26 | Mersana Therapeutics, Inc. | Protein-polymer-drug conjugates |
| ES2697674T3 (es) | 2011-11-01 | 2019-01-25 | Bionomics Inc | Procedimientos para bloquear el crecimiento de células madre cancerosas |
| WO2013096901A1 (en) * | 2011-12-23 | 2013-06-27 | Mersana Therapeutics, Inc. | Pharmaceutical formulations for fumagillin derivative-phf conjugates |
| BR112014017673A8 (pt) | 2012-01-18 | 2017-07-11 | Zafgen Inc | Compostos de sulfonamida tricíclicos e métodos para fazer e usar os mesmos |
| AU2013209719A1 (en) | 2012-01-18 | 2014-08-07 | Zafgen, Inc. | Tricyclic sulfone compounds and methods of making and using same |
| BR112014027808A2 (pt) | 2012-05-07 | 2017-06-27 | Zafgen Inc | sal polimórfico do sal de oxalato de 6-o-(4-dimetilaminoetoxi) cinaroil fumagilol e métodos de produção e utilização do mesmo |
| EP2846792B1 (en) | 2012-05-08 | 2018-08-15 | Zafgen, Inc. | Treating hypothalamic obesity with metap2 inhibitors |
| CN104364251B (zh) | 2012-05-09 | 2017-02-22 | 扎夫根股份有限公司 | 烟曲霉醇型化合物及其制备和使用方法 |
| CN104918928A (zh) | 2012-11-05 | 2015-09-16 | 扎夫根股份有限公司 | 三环化合物及其制备方法和用途 |
| BR112015010225A2 (pt) | 2012-11-05 | 2017-07-11 | Zafgen Inc | compostos tricíclicos e seus métodos de produção e utilização |
| NZ707773A (en) | 2012-11-05 | 2019-05-31 | Zafgen Inc | Methods of treating liver diseases |
| KR20150126924A (ko) | 2013-03-14 | 2015-11-13 | 자프겐 인크. | 신장 질환 및 기타 장애의 치료 방법 |
| EP3574922B1 (en) | 2013-04-10 | 2021-09-15 | Syndevrx, Inc. | Modified or polymer-conjugated fumagillol metap2 inhibitors for use in improving or restoring insulin sensitivity |
| WO2015054659A1 (en) | 2013-10-11 | 2015-04-16 | Mersana Therapeutics, Inc. | Protein-polymer-drug conjugates |
| CA2927022C (en) | 2013-10-11 | 2018-08-21 | Asana Biosciences, Llc | Protein-polymer-drug conjugates |
| JP6493868B2 (ja) * | 2014-09-24 | 2019-04-03 | 日東電工株式会社 | ジグリコールアミド酸型配位子を有するビニルモノマー |
| CA2966005C (en) | 2014-10-31 | 2021-04-27 | Abbvie Biotherapeutics Inc. | Anti-cs1 antibodies and antibody drug conjugates |
| EP3229844B1 (en) | 2014-12-09 | 2020-03-04 | AbbVie Inc. | Antibody drug conjugates with cell permeable bcl-xl inhibitors |
| RU2017123942A (ru) | 2014-12-09 | 2019-01-11 | Эббви Инк. | Ингибирующие bcl-xl соединения, обладающие низкой клеточной проницаемостью, и коньюгаты антитело-лекарственное средство, включающие их |
| TW201636342A (zh) | 2014-12-19 | 2016-10-16 | 武田藥品工業有限公司 | 煙黴醇衍生物 |
| 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 |
| AR105671A1 (es) * | 2015-08-11 | 2017-10-25 | Zafgen Inc | Compuestos heterocíclicos de fumagillol y sus métodos de elaboración y uso |
| EP3383909B1 (en) | 2015-11-30 | 2020-06-17 | AbbVie Inc. | Anti-human lrrc15 antibody drug conjugates and methods for their use |
| JP2019501124A (ja) | 2015-11-30 | 2019-01-17 | アッヴィ・インコーポレイテッド | 抗ｈｕＬＲＲＣ１５抗体薬物コンジュゲート及びその使用方法 |
| KR102849342B1 (ko) | 2015-12-10 | 2025-08-21 | 신데브알엑스, 인크. | 푸마길롤 유도체 및 그의 다형체 |
| AU2017206718B2 (en) | 2016-01-11 | 2021-09-30 | Syndevrx, Inc. | Treatment for tumors driven by metabolic dysfunction |
| US10745487B2 (en) | 2016-03-22 | 2020-08-18 | Bionomics Limited | Method of treating cancer by administering an anti-LGR5 monoclonal antibody |
| RS61659B1 (sr) | 2016-05-17 | 2021-04-29 | Abbvie Biotherapeutics Inc | Konjugati antitelo lek anti-cmet i metode za njihovu upotrebu |
| RS61828B1 (sr) | 2016-06-08 | 2021-06-30 | Abbvie Inc | Anti-b7-h3 antitela i antitelske konjugacije lekova |
| MX2018015284A (es) | 2016-06-08 | 2019-09-18 | Abbvie Inc | Conjugados de anticuerpo anti-egfr y fármaco. |
| CN109562190A (zh) | 2016-06-08 | 2019-04-02 | 艾伯维公司 | 抗egfr抗体药物偶联物 |
| CN109641962A (zh) | 2016-06-08 | 2019-04-16 | 艾伯维公司 | 抗b7-h3抗体和抗体药物偶联物 |
| JP2019526529A (ja) | 2016-06-08 | 2019-09-19 | アッヴィ・インコーポレイテッド | 抗ｂ７−ｈ３抗体及び抗体薬物コンジュゲート |
| MX2018015268A (es) | 2016-06-08 | 2019-08-12 | Abbvie Inc | Anticuerpos anti-cd98 y conjugados de anticuerpo y farmaco. |
| MX2018015272A (es) | 2016-06-08 | 2019-08-12 | Abbvie Inc | Anticuerpos anti-cd98 y conjugados de anticuerpo y farmaco. |
| WO2017214456A1 (en) | 2016-06-08 | 2017-12-14 | Abbvie Inc. | Anti-cd98 antibodies and antibody drug conjugates |
| CN116059201A (zh) | 2016-06-08 | 2023-05-05 | 艾伯维公司 | 抗egfr抗体药物偶联物 |
| WO2018031877A1 (en) * | 2016-08-11 | 2018-02-15 | Zafgen, Inc. | Fumagillol compounds and methods of making and using same |
| DK3529269T3 (da) | 2016-10-19 | 2026-02-23 | Invenra Inc | Antistof-konstruktioner |
| WO2018115485A1 (en) | 2016-12-22 | 2018-06-28 | Pierfrancesco Tassone | A monoclonal antibody targeting a unique sialoglycosilated cancer-associated epitope of cd43 |
| CN106831662B (zh) * | 2016-12-29 | 2018-12-18 | 中国农业科学院蜜蜂研究所 | 一种胺基多元醇代烟曲霉素及其合成方法与应用 |
| US10772971B2 (en) | 2017-06-22 | 2020-09-15 | Mersana Therpeutics, Inc. | Methods of producing drug-carrying polymer scaffolds and protein-polymer-drug conjugates |
| WO2019118612A1 (en) * | 2017-12-12 | 2019-06-20 | Zafgen, Inc. | Targeting compounds |
| PE20210320A1 (es) | 2018-06-01 | 2021-02-16 | Novartis Ag | Moleculas de union contra bcma y usos de las mismas |
| CN113227127A (zh) | 2018-06-05 | 2021-08-06 | 伦敦大学国王学院 | 向胃肠系统递送酬载的btnl3/8导引构建体 |
| US11612577B2 (en) | 2018-10-26 | 2023-03-28 | Syndevrx, Inc. | Biomarkers of METAP2 inhibitors and applications thereof |
| KR20210099614A (ko) | 2018-12-04 | 2021-08-12 | 노파르티스 아게 | Cd3에 대한 결합 분자 및 이의 용도 |
| US12037378B2 (en) | 2019-05-21 | 2024-07-16 | Novartis Ag | Variant CD58 domains and uses thereof |
| UY38701A (es) | 2019-05-21 | 2020-12-31 | Novartis Ag | Moléculas de unión a cd19, conjugados, composiciones que las comprenden y usos de las mismas |
| CN114585651A (zh) | 2019-08-08 | 2022-06-03 | 再生元制药公司 | 新型抗原结合分子形式 |
| AU2020379735A1 (en) | 2019-11-05 | 2022-05-26 | Regeneron Pharmaceuticals, Inc. | N-terminal SCFV multispecific binding molecules |
| CN115052663B (zh) | 2020-01-08 | 2026-06-09 | 辛瑟斯治疗股份有限公司 | Alk5抑制剂缀合物及其用途 |
| JP7859981B2 (ja) | 2020-03-06 | 2026-05-15 | ジーオー セラピューティクス，インコーポレイテッド | 抗グリコｃｄ４４抗体およびその使用 |
| WO2021195513A1 (en) | 2020-03-27 | 2021-09-30 | Novartis Ag | Bispecific combination therapy for treating proliferative diseases and autoimmune disorders |
| AR124681A1 (es) | 2021-01-20 | 2023-04-26 | Abbvie Inc | Conjugados anticuerpo-fármaco anti-egfr |
| EP4301782A1 (en) | 2021-03-05 | 2024-01-10 | Go Therapeutics, Inc. | Anti-glyco-cd44 antibodies and their uses |
| JP2024531915A (ja) | 2021-08-05 | 2024-09-03 | ジーオー セラピューティクス，インコーポレイテッド | 抗グリコｍｕｃ抗体およびその使用 |
| WO2023034569A1 (en) | 2021-09-03 | 2023-03-09 | Go Therapeutics, Inc. | Anti-glyco-cmet antibodies and their uses |
| JP2024534910A (ja) | 2021-09-03 | 2024-09-26 | ジーオー セラピューティクス，インコーポレイテッド | 抗グリコｌａｍｐ１抗体およびその使用 |
| JP2025508363A (ja) * | 2022-02-16 | 2025-03-26 | イッサム リサーチ ディベロップメント カンパニー オブ ザ ヘブライ ユニバーシティー オブ エルサレム リミテッド | ＭｅｔＡｐ２阻害剤及びその使用 |
| CN121002062A (zh) | 2023-01-13 | 2025-11-21 | 再生元制药公司 | Fgfr3结合分子及其使用方法 |
| WO2024258967A1 (en) | 2023-06-13 | 2024-12-19 | Synthis Therapeutics, Inc. | Anti-cd5 antibodies and their uses |
| WO2025240335A1 (en) | 2024-05-13 | 2025-11-20 | Regeneron Pharmaceuticals, Inc. | Fgfr3 binding molecules and methods of use thereof |
Family Cites Families (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2803586A (en) | 1953-06-29 | 1957-08-20 | Abbott Lab | ph control in production of fumagillin |
| US5164410A (en) | 1988-01-09 | 1992-11-17 | Takeda Chemical Industries, Ltd. | Fumagillol derivatives and pharmaceutical compositions thereof |
| PH26256A (en) | 1988-08-12 | 1992-04-01 | Fujisawa Pharmaceutical Co | Oxaspiro [2,5] octane derivative |
| JP2858724B2 (ja) * | 1988-09-01 | 1999-02-17 | 武田薬品工業株式会社 | 血管新生阻害剤 |
| EP0359036B1 (en) | 1988-09-01 | 1997-03-26 | Takeda Chemical Industries, Ltd. | Fumagillol derivatives |
| 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 |
| ATE153854T1 (de) | 1992-12-16 | 1997-06-15 | Takeda Chemical Industries Ltd | Stabile pharmazeutische zubereitung mit fumagillolderivaten |
| NZ304906A (en) | 1995-03-27 | 1999-06-29 | Sanofi Sa | Use of fumagillol or a fumagillol ester and an optionally saturated alkylcarboxylic or alkyldicarboxylic acid to fight intestinal infections |
| US5811510A (en) | 1995-04-14 | 1998-09-22 | General Hospital Corporation | Biodegradable polyacetal polymers and methods for their formation and use |
| WO1998056372A1 (en) | 1997-06-09 | 1998-12-17 | Massachusetts Institute Of Technology | TYPE 2 METHIONINE AMINOPEPTIDASE (MetAP2) INHIBITORS AND USES THEROF |
| WO1999061432A1 (en) | 1998-05-12 | 1999-12-02 | Biochem Pharma Inc. | Fumagillin analogs and their use as angiogenesis inhibitors |
| KR100357541B1 (ko) | 1998-05-15 | 2002-10-18 | 주식회사종근당 | 5-데메톡시 푸마질롤 유도체 및 그 제조방법 |
| KR100357542B1 (ko) | 1998-05-15 | 2002-10-18 | 주식회사종근당 | 푸마질롤 유도체 및 그 제조방법 |
| US6603812B1 (en) | 1998-08-17 | 2003-08-05 | Linear Technology Corporation | Hardware implementation of a decimating finite impulse response filter |
| WO2000018232A1 (en) | 1998-10-01 | 2000-04-06 | Children's Medical Center Corporation | Method of treatment of cardiovascular injuries |
| ATE361757T1 (de) | 1999-02-26 | 2007-06-15 | Sanofi Aventis | Stabile fumagillin-formulierung |
| HUP9901943A2 (hu) | 1999-06-11 | 2001-12-28 | Sanofi-Synthelabo | Eljárás fumagillin előállítására |
| US6822086B1 (en) | 1999-08-09 | 2004-11-23 | The General Hospital Corporation | Drug-carrier complexes and methods of use thereof |
| US8106098B2 (en) | 1999-08-09 | 2012-01-31 | The General Hospital Corporation | Protein conjugates with a water-soluble biocompatible, biodegradable polymer |
| GB0012179D0 (en) | 2000-05-20 | 2000-07-12 | Imp Cancer Res Tech | Assays and drug screening systems |
| US6548477B1 (en) | 2000-11-01 | 2003-04-15 | Praecis Pharmaceuticals Inc. | Therapeutic agents and methods of use thereof for the modulation of angiogenesis |
| US7105482B2 (en) | 2000-11-01 | 2006-09-12 | Praecis Pharmaceuticals, Inc. | Methionine aminopeptidase-2 inhibitors and methods of use thereof |
| US6919307B2 (en) | 2000-11-01 | 2005-07-19 | Praecis Pharmaceuticals, Inc. | Therapeutic agents and methods of use thereof for the modulation of angiogenesis |
| EP1330447A2 (en) | 2000-11-01 | 2003-07-30 | Praecis Pharmaceuticals Incorporated | Peptides as met-ap2 inhibitors |
| ATE440094T1 (de) * | 2001-09-27 | 2009-09-15 | Equispharm Co Ltd | Fumagillolderivate und verfahren zu deren herstellung |
| US6803382B2 (en) | 2001-11-09 | 2004-10-12 | Galderma Research & Development, S.N.C. | Angiogenesis inhibitors and pharmaceutical and cosmetic use thereof |
| WO2003059988A2 (en) | 2002-01-14 | 2003-07-24 | The General Hospital Corporation | Biodegradable polyketal polymers and methods for their formation and use |
| WO2003070823A2 (en) | 2002-02-20 | 2003-08-28 | The General Hospital Corporation | Conjugates comprising a biodegradable polymer and uses therefor |
| 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 |
| AU2003256613A1 (en) * | 2002-07-19 | 2004-02-09 | Amgen Inc. | Protein conjugates with a water-soluble biocompatible, biogradable polymer |
| CA2492803C (en) | 2002-07-19 | 2013-11-05 | The General Hospital Corporation | Oxime conjugates and methods for their formation and use |
| AU2004270251B2 (en) * | 2003-09-05 | 2011-03-31 | The General Hospital Corporation | Polyacetal drug conjugates as release system |
| FR2872511B1 (fr) | 2004-06-30 | 2006-08-11 | Galderma Res & Dev | Nouveaux inhibiteurs de l'angiogenese et leur utilisation pharmaceutique et cosmetique |
| CA2616906A1 (en) | 2005-05-12 | 2006-11-23 | Tapestry Pharmaceuticals, Inc. | Molecular constructs suitable for targeted conjugates |
| JP5364875B2 (ja) | 2007-07-16 | 2013-12-11 | アッヴィ・インコーポレイテッド | タンパク質キナーゼ阻害薬としてのインダゾール類、ベンゾイソオキサゾール類およびベンゾイソチアゾール類 |
| BRPI0820229A2 (pt) | 2007-11-28 | 2017-05-09 | A Stevenson Cheri | conjugados de análogos de fumagilina biodegradáveis biocompatíveis |
| JP2012528240A (ja) | 2009-05-28 | 2012-11-12 | メルサナ セラピューティックス， インコーポレイテッド | 可変速度放出リンカーを含むポリアル−薬物コンジュゲート |
-
2008
- 2008-11-24 BR BRPI0820229A patent/BRPI0820229A2/pt not_active IP Right Cessation
- 2008-11-24 WO PCT/US2008/084539 patent/WO2009073445A2/en not_active Ceased
- 2008-11-24 EA EA201070657A patent/EA020251B1/ru not_active IP Right Cessation
- 2008-11-24 CN CN2008801221269A patent/CN101990441A/zh active Pending
- 2008-11-24 CA CA2706914A patent/CA2706914A1/en not_active Abandoned
- 2008-11-24 EP EP08857683A patent/EP2217283A2/en not_active Withdrawn
- 2008-11-24 NZ NZ600039A patent/NZ600039A/xx not_active IP Right Cessation
- 2008-11-24 JP JP2010536101A patent/JP5557746B2/ja not_active Expired - Fee Related
- 2008-11-24 NZ NZ585547A patent/NZ585547A/xx not_active IP Right Cessation
- 2008-11-24 US US12/276,856 patent/US8399512B2/en not_active Expired - Fee Related
- 2008-11-24 MX MX2010005857A patent/MX2010005857A/es active IP Right Grant
- 2008-11-24 AU AU2008331516A patent/AU2008331516B2/en not_active Ceased
-
2010
- 2010-05-27 IL IL206057A patent/IL206057A0/en unknown
- 2010-05-27 ZA ZA2010/03819A patent/ZA201003819B/en unknown
-
2013
- 2013-02-15 US US13/769,024 patent/US20130158046A1/en not_active Abandoned