公开(公告)号：US20170166576A1

公开(公告)日：2017-06-15

申请号：US15349872

申请日：2016-11-11

Applicant: MannKind Corporation

Inventor： Qingping Zeng ,  Warren S. Wade ,  John Bruce Patterson

IPC: C07D487/08 ,  C07D207/14 ,  C07D207/08 ,  C07D213/74 ,  C07D295/108 ,  C07D249/06 ,  C07D207/16 ,  C07D401/12 ,  C07D213/38 ,  C07D211/26 ,  C07D211/58 ,  C07D401/04 ,  C07D295/26 ,  C07D295/32 ,  C07D277/12 ,  C07D263/34 ,  C07D409/12 ,  C07D307/68 ,  C07D333/38 ,  C07D277/18 ,  C07D295/112

CPC classification number: C07D487/08 ,  C07C59/74 ,  C07C65/30 ,  C07C69/738 ,  C07C235/78 ,  C07C235/84 ,  C07D207/08 ,  C07D207/14 ,  C07D207/16 ,  C07D211/26 ,  C07D211/58 ,  C07D211/62 ,  C07D211/66 ,  C07D211/98 ,  C07D213/36 ,  C07D213/38 ,  C07D213/74 ,  C07D213/81 ,  C07D213/82 ,  C07D239/26 ,  C07D239/38 ,  C07D249/06 ,  C07D263/34 ,  C07D277/12 ,  C07D277/18 ,  C07D277/42 ,  C07D277/56 ,  C07D295/108 ,  C07D295/112 ,  C07D295/185 ,  C07D295/192 ,  C07D295/26 ,  C07D295/32 ,  C07D307/68 ,  C07D333/38 ,  C07D333/40 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D413/06 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12

Abstract: The invention provides compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.

公开(公告)号：US09440913B2

公开(公告)日：2016-09-13

申请号：US13882647

申请日：2011-11-01

Applicant: Hiroyuki Saimoto ,  Kiyoshi Kita ,  Yoshisada Yabu ,  Masaichi Yamamoto

Inventor： Hiroyuki Saimoto ,  Kiyoshi Kita ,  Yoshisada Yabu ,  Masaichi Yamamoto

IPC: C07C255/53 ,  C07C47/27 ,  C07C49/248 ,  C07C59/90 ,  A61K31/11 ,  A61K31/12 ,  A61K31/192 ,  A61K31/216 ,  A61K31/336 ,  A61K31/351 ,  A61K31/357 ,  A61P33/00 ,  C07C47/56 ,  C07C59/74 ,  C07C69/738 ,  A61K45/06 ,  A61K31/047 ,  C07C47/575 ,  C07C49/258 ,  C07C49/835 ,  C07C49/84

CPC classification number: C07C255/53 ,  A61K31/047 ,  A61K45/06 ,  C07C47/27 ,  C07C47/56 ,  C07C47/575 ,  C07C49/248 ,  C07C49/258 ,  C07C49/835 ,  C07C49/84 ,  C07C59/74 ,  C07C59/90 ,  C07C69/738 ,  A61K2300/00

Abstract: Novel compounds below are useful for preventing or treating diseases caused by protozoans. At least one of a compound represented by Formula (I) (wherein, X represents a hydrogen atom or a halogen atom; R1 represents a hydrogen atom; R2 represents a hydrogen atom or a C1-7 alkyl group; R3 represents —CHO, —C(═O)R5, —COOR5 (wherein R5 represents a C1-7 alkyl group), —CH2OH or —COOH; and R4 represents a C1-16 alkyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s), a C2-16 alkenyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s), or a C2-16 alkynyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s)), an optical isomer thereof, and a pharmaceutically acceptable salt is used.

公开(公告)号：US08669385B2

公开(公告)日：2014-03-11

申请号：US13501666

申请日：2010-10-12

Applicant: Richard G. Blair

Inventor： Richard G. Blair

IPC: C07C51/16

CPC classification number: C07C51/373 ,  B01J8/10 ,  B01J8/16 ,  B01J2219/182 ,  B01J2219/1946 ,  C07C45/36 ,  C07C47/02 ,  C07C47/54 ,  C07C47/21 ,  C07C59/74 ,  C07C59/147 ,  C07C59/153

Abstract: Provided are processes for the oxidative cleavage of a double bond in an unsaturated carboxylic acid. The process includes contacting the unsaturated carboxylic acid with a mild oxidizing agent and agitating the unsaturated carboxylic acid and the mild oxidizing agent for a time sufficient to cleave a double bond of the unsaturated carboxylic acid and produce a product comprising an aldehyde. The process is typically carried out in a mill, such as a ball, hammer, attrition, or jet mill.

Abstract translation: 提供了在不饱和羧酸中双键氧化裂解的方法。 该方法包括使不饱和羧酸与温和的氧化剂接触，并搅拌不饱和羧酸和温和的氧化剂一段足以裂解不饱和羧酸的双键并产生包含醛的产物的时间。 该方法通常在诸如球，锤，磨耗或喷射磨的研磨机中进行。

公开(公告)号：US08410309B2

公开(公告)日：2013-04-02

申请号：US11458331

申请日：2006-07-18

Applicant: Andrea Leone-Bay ,  Kelly Kraft ,  Destardi Moye-Sherman ,  David Gschneidner ,  Maria Aurora P. Boyd ,  Puchun Liu ,  Pingwah Tang ,  Jun Liao ,  John Smart ,  John J. Freeman, Jr.

Inventor： Andrea Leone-Bay ,  Kelly Kraft ,  Destardi Moye-Sherman ,  David Gschneidner ,  Maria Aurora P. Boyd ,  Puchun Liu ,  Pingwah Tang ,  Jun Liao ,  John Smart ,  John J. Freeman, Jr.

IPC: C07C59/90 ,  C07C62/32 ,  C07C65/40

CPC classification number: C07C59/64 ,  C07C59/42 ,  C07C59/56 ,  C07C59/74 ,  C07C59/84 ,  C07C59/90 ,  C07C63/14

Abstract: Phenoxy carboxylic acid compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Abstract translation: 提供了苯氧基羧酸化合物和用于递送活性剂的组合物。 也提供给药和制备方法。

公开(公告)号：US20120264956A1

公开(公告)日：2012-10-18

申请号：US13501666

申请日：2010-10-12

Applicant: Richard G. Blair

Inventor： Richard G. Blair

IPC: C07C51/373 ,  C07C59/74 ,  C07C59/147

CPC classification number: C07C51/373 ,  B01J8/10 ,  B01J8/16 ,  B01J2219/182 ,  B01J2219/1946 ,  C07C45/36 ,  C07C47/02 ,  C07C47/54 ,  C07C47/21 ,  C07C59/74 ,  C07C59/147 ,  C07C59/153

Abstract: Provided are processes for the oxidative cleavage of a double bond in an unsaturated carboxylic acid. The process includes contacting the unsaturated carboxylic acid with a mild oxidizing agent and agitating the unsaturated carboxylic acid and the mild oxidizing agent for a time sufficient to cleave a double bond of the unsaturated carboxylic acid and produce a product comprising an aldehyde. The process is typically carried out in a mill, such as a ball, hammer, attrition, or jet mill.

Abstract translation: 提供了在不饱和羧酸中双键氧化裂解的方法。 该方法包括使不饱和羧酸与温和的氧化剂接触，并搅拌不饱和羧酸和温和的氧化剂一段足以裂解不饱和羧酸的双键并产生包含醛的产物的时间。 该方法通常在诸如球，锤，磨耗或喷射磨的研磨机中进行。

公开(公告)号：US07858819B2

公开(公告)日：2010-12-28

申请号：US12304085

申请日：2007-06-11

Applicant: Akira Yoshitomo ,  Tatsuya Iwai

Inventor： Akira Yoshitomo ,  Tatsuya Iwai

IPC: C07C47/57 ,  C07C59/74 ,  C07C69/66 ,  C07C69/76

CPC classification number: C07C47/57 ,  C07C39/15 ,  C07C59/74 ,  C07C69/712

Abstract: A new tris(formylphenyl) of the following general formula and polynuclear phenol derived therefrom:

Abstract translation: 一种新的三（甲酰基苯基）下列通式和由其衍生的多核苯酚：

公开(公告)号：US07635716B2

公开(公告)日：2009-12-22

申请号：US11569369

申请日：2006-01-10

Applicant: David W. Old ,  Todd S. Gac ,  Vinh X. Ngo

Inventor： David W. Old ,  Todd S. Gac ,  Vinh X. Ngo

IPC: A61K31/215 ,  A61K31/5575 ,  C07C69/612

CPC classification number: C07C405/00 ,  A61K31/192 ,  A61K31/216 ,  A61K31/222 ,  C07C59/72 ,  C07C59/74 ,  C07C59/90 ,  C07C69/736 ,  C07C69/738 ,  C07C2601/08

Abstract: Novel compounds, and therapeutic methods, compositions and medicament related thereto are disclosed herein.

Abstract translation: 本文公开了新颖的化合物及其相关的治疗方法，组合物和药物。

公开(公告)号：US4731473A

公开(公告)日：1988-03-15

申请号：US848078

申请日：1986-04-04

Applicant: Donald J. Abraham ,  Otto W. Woltersdorf, Jr. ,  Edward J. Cragoe, Jr.

Inventor： Donald J. Abraham ,  Otto W. Woltersdorf, Jr. ,  Edward J. Cragoe, Jr.

IPC: C07C45/46 ,  C07C49/835 ,  C07C59/74 ,  C07C59/90 ,  C07C59/92 ,  C07C65/30 ,  C07C205/32 ,  C07C205/33 ,  C07C205/54 ,  C07C65/40

CPC classification number: C07C205/54 ,  C07C205/32 ,  C07C205/33 ,  C07C45/46 ,  C07C49/835 ,  C07C59/74 ,  C07C59/90 ,  C07C59/92 ,  C07C65/30

Abstract: The present invention is directed to compounds of the general formula I and pharmaceutically acceptable salts thereof: ##STR1## wherein: R=ethyl, propyl or isopropyl; andA=(CH.sub.2).sub.n wherein n is 2, 4 or 5, and C(CH.sub.2).sub.3.

Abstract translation: 本发明涉及通式I的化合物及其药学上可接受的盐：其中：R =乙基，丙基或异丙​​基; 和A =（CH 2）n，其中n为2,4或5，和C（CH 2）3。

公开(公告)号：US4535183A

公开(公告)日：1985-08-13

申请号：US332246

申请日：1981-12-18

Applicant: Geoffrey Kneen

Inventor： Geoffrey Kneen

IPC: A61K31/215 ,  A61K31/10 ,  A61K31/11 ,  A61K31/165 ,  A61K31/19 ,  A61K31/195 ,  A61K31/41 ,  A61P7/00 ,  A61P7/06 ,  A61P11/00 ,  A61P43/00 ,  C07C43/205 ,  C07C43/225 ,  C07C45/00 ,  C07C45/51 ,  C07C45/60 ,  C07C45/71 ,  C07C47/575 ,  C07C51/347 ,  C07C59/00 ,  C07C59/125 ,  C07C59/74 ,  C07C65/30 ,  C07C67/00 ,  C07C213/00 ,  C07C223/06 ,  C07C231/00 ,  C07C231/12 ,  C07C233/00 ,  C07C233/33 ,  C07C233/43 ,  C07C235/20 ,  C07C235/46 ,  C07C253/00 ,  C07C253/30 ,  C07C255/13 ,  C07C255/53 ,  C07C255/54 ,  C07C301/00 ,  C07C303/40 ,  C07C311/02 ,  C07C311/51 ,  C07D229/00 ,  C07D257/04 ,  C07D307/79 ,  C07C65/40

CPC classification number: C07D257/04 ,  C07C255/00 ,  C07C43/205 ,  C07C43/225 ,  C07C45/00 ,  C07C45/515 ,  C07C45/60 ,  C07C45/71 ,  C07C47/575 ,  C07C59/74 ,  C07C65/30 ,  C07D307/79 ,  Y10S514/815

Abstract: This invention is directed to novel ether compounds of formula (I) ##STR1## which are of value in medicine in the palliation of haemoglobinopathies, in particular sickle-cell anemia, and also in the palliation of pulmonary dyefunction, protection from the effects of hypoxia and the radio-sensitization of tumours. The invention is also directed to methods for the preparation of the ether compounds, to pharmaceutical formulations containing them, the preparation of such formulations and the use of the compounds in human medicine. Also provided by the invention are intermediates of value in the preparation of the ether compounds, by the methods described, and the preparation of the intermediates.

Abstract translation: 本发明涉及式（I）的新型醚化合物（I），其在血红蛋白病，尤其是镰状细胞性贫血的缓解中以及在肺部染色功能的缓解中在药物中具有价值， 缺氧的影响和肿瘤的放射敏感性。 本发明还涉及制备醚化合物的方法，含有它们的药物制剂，这些制剂的制备以及该化合物在人类药物中的用途。 本发明还提供了通过所述方法和中间体的制备在制备醚化合物中有价值的中间体。

公开(公告)号：US4410537A

公开(公告)日：1983-10-18

申请号：US271950

申请日：1981-06-09

Applicant: Geoffrey Kneen

Inventor： Geoffrey Kneen

IPC: C07C59/125 ,  A61K9/08 ,  A61K9/28 ,  A61K9/48 ,  A61K31/16 ,  A61K31/19 ,  A61K31/215 ,  A61K31/235 ,  A61K31/275 ,  A61K31/395 ,  A61P7/00 ,  A61P7/06 ,  A61P11/00 ,  A61P43/00 ,  C07C51/00 ,  C07C59/74 ,  C07C65/21 ,  C07C65/30 ,  C07C67/00 ,  C07C69/712 ,  C07C69/76 ,  C07C231/00 ,  C07C231/02 ,  C07C231/12 ,  C07C235/20 ,  C07C235/34 ,  C07C253/00 ,  C07C255/13 ,  C07C255/54 ,  C07D257/04 ,  A61K31/41 ,  C07C121/75

CPC classification number: C07C65/30 ,  C07C59/74

Abstract: This invention is directed to novel ether compounds of formula (I) ##STR1## which are of value in medicine in the palliation of haemoglobinopathies, in particular sickle-cell anaemia, and also in the palliation of pulmonary dysfunction, protection from the effects of hypoxia and the radio-sensitization of tumors. The invention is also directed to methods for the preparation of the ether compounds, to pharmaceutical formulations containing them, the preparation of such formulations and the use of the compounds in human medicine. Also provided by the invention are intermediates of value in the preparation of the ether compounds, by the methods described, and the preparation of the intermediates.

Abstract translation: 本发明涉及式（I）的新型醚化合物，其在药物中在减轻血红蛋白病，特别是镰状细胞性贫血中以及在肺功能障碍的缓解中具有价值， 缺氧的影响和肿瘤的放射敏感性。 本发明还涉及制备醚化合物的方法，含有它们的药物制剂，这些制剂的制备以及该化合物在人类药物中的用途。 本发明还提供了通过所述方法和中间体的制备在制备醚化合物中有价值的中间体。