公开(公告)号：US09969722B2

公开(公告)日：2018-05-15

申请号：US15373874

申请日：2016-12-09

申请人： SynDevRx, Inc.

发明人： John S. Petersen

IPC分类号： C07D303/00 ,  C07D407/08 ,  C07C309/29

CPC分类号： C07D407/08 ,  C07B2200/13 ,  C07C309/29 ,  C07D303/46

摘要： The present disclosure relates to salts and polymorphs of aminoalkylfumagillol carbamates (e.g., fumagill-6-yl N-(trans-4-aminocyclohexyl)carbamate benzenesulfonic acid salt and fumagill-6-yl N-(trans-4-aminocyclohexyl)carbamate hydroxynaphthoic acid salt). The polymorphs are characterized by X-ray powder diffraction, differential scanning calorimetry, and thermogravimetric analysis, among other methods. The polymorphs and salts can be used as intermediates in the production of fumagillol derivatives (e.g., polymer-conjugated fumagillol derivatives) as well as therapeutic agents for the treatment of various diseases and conditions such as cancer.

公开(公告)号：US09371312B2

公开(公告)日：2016-06-21

申请号：US14178788

申请日：2014-02-12

申请人： Zafgen, Inc.

发明人： Thomas Crawford ,  Hayley A. Reece

IPC分类号： C07D407/04 ,  C07D303/16 ,  C07D407/08

CPC分类号： A61K31/336 ,  C07D303/16 ,  C07D407/04 ,  C07D407/08

摘要： The disclosure is in part directed to crystalline forms of 6-O-(4-dimethylaminoethoxy)cinnamoyl fumagillol and variants thereof.

公开(公告)号：US09365553B2

公开(公告)日：2016-06-14

申请号：US13699892

申请日：2011-05-23

申请人： Makoto Okada ,  Koichi Hasumi ,  Takahiro Nishimoto ,  Miwa Yoshida ,  Kouki Ishitani ,  Tomoji Aotsuka ,  Hashime Kanazawa

发明人： Makoto Okada ,  Koichi Hasumi ,  Takahiro Nishimoto ,  Miwa Yoshida ,  Kouki Ishitani ,  Tomoji Aotsuka ,  Hashime Kanazawa

IPC分类号： C07D401/06 ,  C07D211/46 ,  C07D405/06 ,  C07D213/79 ,  C07D333/40 ,  C07D407/08 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06

CPC分类号： C07D405/06 ,  C07D211/46 ,  C07D213/79 ,  C07D333/40 ,  C07D401/06 ,  C07D407/08 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06

摘要： A heterocyclic compound useful as an antiallergic agent is provided.A compound represented by the following formula (1) or a salt thereof: wherein the ring A is a homocyclic or heterocyclic ring; the ring B is a heterocyclic ring which contains G and nitrogen atom N as constituent atoms thereof, wherein G is CH or N; R1 is a carbonyl group or an alkylene group; R2a and R2b are an alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; X is an oxygen atom or a sulfur atom; Z is a hydroxyl group, an alkoxy group, a cycloalkyloxy group, an aryloxy group, an aralkyloxy group, an amino group, or an N-substituted amino group; and n is 0 or 1; with the proviso that when the ring A is a benzene ring or when the ring B is a piperazine ring, R1 is an alkylene group which may have a substituent.

摘要翻译： 提供了可用作抗过敏剂的杂环化合物。 由下式（1）表示的化合物或其盐：其中环A是稠环或杂环; 环B是含有G和氮原子N作为其构成原子的杂环，其中G是CH或N; R1是羰基或亚烷基; R2a和R2b是烷基，环烷基，芳基或杂环基; X是氧原子或硫原子; Z是羟基，烷氧基，环烷氧基，芳氧基，芳烷氧基，氨基或N-取代氨基; 并且n为0或1; 条件是当环A为苯环时，或当环B为哌嗪环时，R 1为可具有取代基的亚烷基。

公开(公告)号：US08962575B2

公开(公告)日：2015-02-24

申请号：US13402675

申请日：2012-02-22

申请人： Matthias Gehling ,  Torsten Grothe ,  Ernst Roemer ,  Peter Reinemer ,  Kathrin Reinhardt ,  Annie George ,  Nur Hanisah Mohtar ,  Noorsyarida Mohd Sapiai

发明人： Matthias Gehling ,  Torsten Grothe ,  Ernst Roemer ,  Peter Reinemer ,  Kathrin Reinhardt ,  Annie George ,  Nur Hanisah Mohtar ,  Noorsyarida Mohd Sapiai

IPC分类号： A61K31/70 ,  A61K31/34 ,  C07D407/08 ,  C07D407/04 ,  C07H17/08

CPC分类号： C07D407/08 ,  C07D407/04 ,  C07H17/08

摘要： The use or methods of use of extracts comprising one or more special clerodane compounds against inflammatory (including allergic) diseases or conditions, as well as novel compounds of this type, said clerodane derivatives for use against inflammatory (including allergic) diseases or conditions, pharmaceutical formulations comprising them especially for use against inflammatory disease or conditions, and related embodiments; said extract and/or compound(s) for use in the treatment or in the preparation of a medicament (including a nutraceutical) for the prophylactic and/or therapeutic treatment of said disease or condition, as well as their preparation; pharmaceutical or nutraceutical formulations comprising said extract and/or natural compound(s) which are useful in said prophylactic and/or therapeutic treatment, and related embodiments.

摘要翻译： 使用或使用包含一种或多种抗炎症（特别是过敏性）疾病或病症的特殊克洛膦酸化合物的提取物以及这种新型化合物的用途，所述用于抗炎症（包括过敏性）疾病或病症的氯化丹烷衍生物，药物 包含它们的制剂，特别是用于抗炎性疾病或病症，以及相关实施方案; 所述提取物和/或化合物用于治疗或制备用于预防和/或治疗所述疾病或病症的药物（包括营养药物）及其制备; 包含可用于所述预防和/或治疗性治疗的所述提取物和/或天然化合物的药物或营养制剂以及相关实施方案。

公开(公告)号：US20180291010A1

公开(公告)日：2018-10-11

申请号：US15946899

申请日：2018-04-06

申请人： SynDevRx, Inc.

发明人： John S. Petersen

IPC分类号： C07D407/08 ,  C07D303/46 ,  C07C309/29

CPC分类号： C07D407/08 ,  C07B2200/13 ,  C07C309/29 ,  C07D303/46

摘要： The present disclosure relates to salts and polymorphs of aminoalkylfumagillol carbamates (e.g., fumagill-6-yl N-(trans-4-aminocyclohexyl)carbamate benzenesulfonic acid salt and fumagill-6-yl N-(trans-4-aminocyclohexyl)carbamate hydroxynaphthoic acid salt). The polymorphs are characterized by X-ray powder diffraction, differential scanning calorimetry, and thermogravimetric analysis, among other methods. The polymorphs and salts can be used as intermediates in the production of fumagillol derivatives (e.g., polymer-conjugated fumagillol derivatives) as well as therapeutic agents for the treatment of various diseases and conditions such as cancer.

公开(公告)号：US20170166556A1

公开(公告)日：2017-06-15

申请号：US15373874

申请日：2016-12-09

申请人： SynDevRx, Inc.

发明人： John S. Petersen

IPC分类号： C07D407/08 ,  C07C309/29

CPC分类号： C07D407/08 ,  C07B2200/13 ,  C07C309/29 ,  C07D303/46

摘要： The present disclosure relates to salts and polymorphs of aminoalkylfumagillol carbamates (e.g., fumagill-6-yl N-(trans-4-aminocyclohexyl)carbamate benzenesulfonic acid salt and fumagill-6-yl N-(trans-4-aminocyclohexyl)carbamate hydroxynaphthoic acid salt). The polymorphs are characterized by X-ray powder diffraction, differential scanning calorimetry, and thermogravimetric analysis, among other methods. The polymorphs and salts can be used as intermediates in the production of fumagillol derivatives (e.g., polymer-conjugated fumagillol derivatives) as well as therapeutic agents for the treatment of various diseases and conditions such as cancer.

公开(公告)号：US20170087119A1

公开(公告)日：2017-03-30

申请号：US15145403

申请日：2016-05-03

申请人： Zafgen, Inc. ,  Zafgen, Inc.

发明人： Thomas Crawford ,  Hayley A. Reece

IPC分类号： A61K31/336

CPC分类号： A61K31/336 ,  C07D303/16 ,  C07D407/04 ,  C07D407/08

摘要： The disclosure is in part directed to crystalline forms of 6-O-(4-dimethylaminoethoxy)cinnamoyl fumagillol and variants thereof.

公开(公告)号：US20160229811A1

公开(公告)日：2016-08-11

申请号：US15023159

申请日：2014-09-25

申请人： THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS ,  DUKE UNIVERSITY

发明人： John Katzenelienbogen ,  Donald McDonneli ,  John D, Norris ,  Alexander Parent ,  Julie Pollock ,  Jillian Gunther ,  Kathryn E. Carlson ,  Teresa Martin

IPC分类号： C07D239/48 ,  C07D239/47 ,  C07D213/74 ,  C07D401/14 ,  C07D403/14 ,  C07D239/52 ,  C07D239/54 ,  C07D407/08 ,  C07D239/26 ,  C07D239/58 ,  C07D239/30 ,  C07D213/24 ,  C07D241/12 ,  C07D241/16 ,  C07D409/14 ,  C07D239/34 ,  C07D241/18 ,  C07D403/08

CPC分类号： C07D239/48 ,  A61K45/06 ,  C07D213/24 ,  C07D213/74 ,  C07D239/26 ,  C07D239/30 ,  C07D239/34 ,  C07D239/47 ,  C07D239/52 ,  C07D239/54 ,  C07D239/58 ,  C07D241/12 ,  C07D241/16 ,  C07D241/18 ,  C07D401/14 ,  C07D403/08 ,  C07D403/14 ,  C07D407/08 ,  C07D409/08 ,  C07D409/14 ,  F01K5/02 ,  F23G5/04 ,  F23K1/04 ,  F23K3/00 ,  F23K2201/20 ,  F23K2203/103

摘要： The present disclosure provides tetra-substituted cyclobutane inhibitors of Androgen Receptor Action, and methods of using such inhibitors, for the treatment of hormone-refractory cancers.

摘要翻译： 本公开提供了雄激素受体作用的四取代环丁烷抑制剂以及使用这些抑制剂用于治疗激素难治性癌症的方法。

公开(公告)号：US20150111964A1

公开(公告)日：2015-04-23

申请号：US14399387

申请日：2013-05-07

申请人： Zafgen, Inc.

发明人： Thomas Crawford

IPC分类号： C07D407/08

CPC分类号： C07D407/08 ,  C07D303/36

摘要： The disclosure is in part directed to crystalline forms of an oxalate salt of 6-O-(4-dimethylaminoethoxy)cinnamoyl fumagillol.

摘要翻译： 本公开部分涉及6-O-（4-二甲基氨基乙氧基）肉桂酰基烟曲霉醇的草酸盐的结晶形式。

公开(公告)号：US20140275185A1

公开(公告)日：2014-09-18

申请号：US14291709

申请日：2014-05-30

申请人： N30 Pharmaceuticals, Inc.

发明人： Xicheng Sun ,  Jian Qiu

IPC分类号： C07D417/10 ,  C07D405/10 ,  C07D409/04 ,  C07D407/08 ,  C07D335/06 ,  C07D413/10 ,  C07D409/10 ,  C07D311/36 ,  C07D311/22

CPC分类号： A61K31/433 ,  A61K31/352 ,  A61K31/381 ,  A61K31/382 ,  A61K31/41 ,  A61K31/4245 ,  C07D311/22 ,  C07D311/36 ,  C07D311/58 ,  C07D335/06 ,  C07D405/10 ,  C07D407/08 ,  C07D409/04 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10

摘要： The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.

摘要翻译： 本发明涉及S-亚硝基谷胱甘肽还原酶（GSNOR）的抑制剂，包含这种GSNOR抑制剂的药物组合物及其制备和使用方法。