公开(公告)号：US11554094B2

公开(公告)日：2023-01-17

申请号：US17079381

申请日：2020-10-23

Applicant: California Institute of Technology

Inventor： Vanessa M. Marx ,  Robert H. Grubbs

IPC: A61K9/00 ,  C07F9/38 ,  A61K9/107 ,  A61K31/663 ,  A61K9/12 ,  A61N5/02 ,  A61N7/02 ,  C07B41/12 ,  C07B43/06 ,  A61N7/00

Abstract: The present disclosure is directed to fatty-acid glycerol ester derivative compounds containing a targeting bisphosphonate group. The disclosure further includes pharmaceutical or biomedical compositions comprising these compounds, and methods of using these compounds and compositions forming microbubbles. The microbubbles have affinity for metal-containing, especially calcium-containing, bodies and/or biological targets. In certain embodiments, these compositions are useful for providing targeted placement of microbubbles capable of cavitation on application of high frequency energy.

公开(公告)号：US10723714B2

公开(公告)日：2020-07-28

申请号：US16427637

申请日：2019-05-31

Applicant: Aragon Pharmaceuticals, Inc.

Inventor： Cyril Ben Haim ,  Andras Horvath ,  Johan Erwin Edmond Weerts ,  Jennifer Albaneze-Walker

IPC: C07D401/04 ,  B01J31/24 ,  B01J31/26 ,  C07B43/06 ,  C07D213/61 ,  C07D213/84 ,  C07D233/86 ,  C07D235/02

Abstract: Disclosed are processes and intermediates for the preparation of compound (X), which is currently being investigated for the treatment of prostate cancer.

公开(公告)号：US20200148610A1

公开(公告)日：2020-05-14

申请号：US16742523

申请日：2020-01-14

Applicant: AbbVie Deutschland GmbH & Co. KG ,  AbbVie Inc.

Inventor： Wilfried BRAJE ,  Katarina BRITZE ,  Justin D. DIETRICH ,  Anais JOLIT ,  Johannes KASCHEL ,  Johanna KLEE ,  Tanja LINDNER

IPC: C07B63/04 ,  C07B37/04 ,  C07B43/04 ,  C07F5/02 ,  C07B43/06 ,  C07D495/04 ,  C07D471/04 ,  C07D409/04 ,  C07D405/04 ,  C07D311/58 ,  C07D307/81 ,  C07D307/36 ,  C07D239/42 ,  C07D239/26 ,  C07D215/227 ,  C07D213/74 ,  C07D211/06 ,  C07D209/48 ,  C07D209/08 ,  C07D207/34 ,  C07D205/04 ,  C07C319/26 ,  C07C303/42 ,  C07C273/18 ,  C07C269/08 ,  C07C253/32 ,  C07C231/22 ,  C07C213/10 ,  C07C209/90 ,  C07C67/62 ,  C07C41/46

Abstract: The present invention relates to a method of carrying out an organic reaction in aqueous solution in the presence of a hydroxyalkyl(alkyl)cellulose or an alkylcellulose.

公开(公告)号：US10646432B2

公开(公告)日：2020-05-12

申请号：US15737705

申请日：2016-06-20

Applicant: CALIFORINA INSTITUTE OF TECHNOLOGY ,  Vanessa M. Marx ,  Robert H. Grubbs

Inventor： Vanessa M. Marx ,  Robert H. Grubbs

IPC: A61K9/00 ,  C07F9/38 ,  A61K9/107 ,  A61K31/663 ,  A61K9/12 ,  A61N5/02 ,  A61N7/02 ,  C07B41/12 ,  C07B43/06 ,  A61N7/00

Abstract: The present disclosure is directed to fatty-acid glycerol ester derivative compounds containing a targeting bisphosphonate group. The disclosure further include pharmaceutical or biomedical compositions comprising these compounds, and methods of using these compounds and compositions forming microbubbles. The microbubbles have affinity for metal-containing, especially calcium-containing, bodies and/or biological targets. In certain embodiments, these compositions are useful for providing targeted placement of microbubbles capable of cavitation on application of high frequency energy.

公开(公告)号：US10590287B2

公开(公告)日：2020-03-17

申请号：US15736370

申请日：2016-06-10

Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.

Inventor： Taichi Nakazawa ,  Toshiyuki Endo ,  Yuki Takayama

IPC: H01B1/00 ,  C09D5/24 ,  C07C233/00 ,  C07C233/75 ,  C07D209/88 ,  C07C233/80 ,  H01L51/50 ,  H01B1/12 ,  C07B43/06 ,  C07C13/567 ,  C07C25/13

Abstract: Provided is a charge-transporting varnish which comprises an amide compound containing fluorine atoms and represented by formula (1) and a charge-transporting substance. [In the formula, Ar1 represents a group represented by any of formulae (1-1) to (1-9) and Ar2 and Ar3 each represent a given fluorinated aryl or aralkyl group.]

公开(公告)号：US20190135775A9

公开(公告)日：2019-05-09

申请号：US15537859

申请日：2015-12-17

Applicant: Aragon Pharmaceuticals, Inc.

Inventor： Cyril Ben Haim ,  Andras Horvath ,  Johan Erwin Edmond Weerts ,  Jennifer Albaneze-Walker

IPC: C07D401/04 ,  C07D235/02 ,  C07D233/86 ,  C07D213/84 ,  B01J31/24 ,  C07B43/06 ,  B01J31/26 ,  C07D213/61

Abstract: Disclosed are processes and intermediates for the preparation of compound (X), which is currently being investigated for the treatment of prostate cancer.

公开(公告)号：US10150733B2

公开(公告)日：2018-12-11

申请号：US15574967

申请日：2016-05-18

Applicant: SUN PHARMA ADVANCED RESEARCH COMPANY LTD.

Inventor： Hemant Ashvinbhai Chokshi ,  Sabbirhusen Yusufbhai Chimanwala ,  Varun Anilkumar Mehta ,  Prabal Sengupta ,  Chitturi Trinadha Rao

IPC: C07D213/75 ,  C07D401/12 ,  C07B43/06

Abstract: The present invention relates to novel amidoheteroaryl aroyl hydrazide ethynes as tyrosine kinase inhibitors, process of preparation thereof, and use of the compounds for preparation of pharmaceutical compositions in the therapeutic treatment of disorders related to tyrosine kinases in humans.

公开(公告)号：US09656927B2

公开(公告)日：2017-05-23

申请号：US15033323

申请日：2014-11-03

Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH

Inventor： Pragati Kishore Prasad ,  Arumugam Sudalai

IPC: C07B41/12 ,  C07C67/00 ,  C07D311/76 ,  C07D491/052 ,  C07D209/46 ,  C07C51/00 ,  C07D307/88 ,  C07D307/89 ,  C07C201/12 ,  C07C231/12 ,  C07D311/10 ,  C07C231/10 ,  C07D209/48 ,  C07B43/06

CPC classification number: C07B41/12 ,  C07B43/06 ,  C07C51/00 ,  C07C67/00 ,  C07C201/12 ,  C07C231/10 ,  C07C231/12 ,  C07D209/46 ,  C07D209/48 ,  C07D307/88 ,  C07D307/89 ,  C07D311/10 ,  C07D311/76 ,  C07D491/052 ,  C07C63/06 ,  C07C69/92 ,  C07C69/78 ,  C07C233/66 ,  C07C205/56 ,  C07C205/57 ,  C07C233/65 ,  C07C233/75

Abstract: The present invention discloses one-pot synthesis of various carboxylic acid derivatives using copper catalyst and sodium cyanide as the cyanide source for bringing in carbonylative coupling in a single step.

公开(公告)号：US20150284417A1

公开(公告)日：2015-10-08

申请号：US14702641

申请日：2015-05-01

Applicant: YEDA RESEARCH AND DEVELOPMENT CO., LTD.

Inventor： David MILSTEIN ,  Ekambaram BALARAMAN ,  Chidambaram GUNANATHAN ,  Boopathy GNANAPRAKASAM ,  Jing ZHANG

IPC: C07F15/00 ,  C07D305/06 ,  C07D307/44 ,  C07D295/023 ,  C07K5/12 ,  C07C29/149 ,  C07C213/02 ,  C07C67/00 ,  C07C231/10 ,  C07D307/52 ,  C07D295/185 ,  C07C51/00 ,  C07D309/30 ,  C07D307/33 ,  C07D307/83 ,  C07D241/12 ,  C07K1/00 ,  C07B41/08 ,  C07B41/02 ,  C07B41/12 ,  C07B43/06 ,  C07B43/04 ,  B01J31/24 ,  C07C209/62

CPC classification number: C07K5/12 ,  B01J31/18 ,  B01J31/189 ,  B01J31/2404 ,  B01J31/2409 ,  B01J31/248 ,  B01J31/2485 ,  B01J2231/40 ,  B01J2231/49 ,  B01J2231/643 ,  B01J2231/763 ,  B01J2531/0244 ,  B01J2531/821 ,  C07B41/02 ,  C07B41/08 ,  C07B41/12 ,  C07B43/04 ,  C07B43/06 ,  C07C29/136 ,  C07C29/149 ,  C07C29/177 ,  C07C41/16 ,  C07C41/26 ,  C07C45/002 ,  C07C45/006 ,  C07C51/00 ,  C07C51/02 ,  C07C51/23 ,  C07C51/295 ,  C07C67/00 ,  C07C67/03 ,  C07C67/297 ,  C07C209/00 ,  C07C209/62 ,  C07C213/00 ,  C07C213/02 ,  C07C231/02 ,  C07C231/10 ,  C07C2601/08 ,  C07C2601/10 ,  C07C2601/14 ,  C07D207/06 ,  C07D207/08 ,  C07D211/12 ,  C07D213/38 ,  C07D241/08 ,  C07D241/12 ,  C07D295/023 ,  C07D295/027 ,  C07D295/185 ,  C07D305/06 ,  C07D307/14 ,  C07D307/33 ,  C07D307/44 ,  C07D307/52 ,  C07D307/83 ,  C07D309/30 ,  C07D487/14 ,  C07F9/58 ,  C07F9/65583 ,  C07F15/0046 ,  C07F15/0053 ,  C07K1/00 ,  C08G69/00 ,  Y02P20/52 ,  C07C233/05 ,  C07C235/06 ,  C07C233/07 ,  C07C235/16 ,  C07C235/14 ,  C07C235/10 ,  C07C211/27 ,  C07C211/07 ,  C07C211/35 ,  C07C211/46 ,  C07C211/10 ,  C07C215/28 ,  C07C217/58 ,  C07C69/14 ,  C07C69/24 ,  C07C31/125 ,  C07C31/12 ,  C07C49/78 ,  C07C49/04 ,  C07C49/10 ,  C07C49/08 ,  C07C49/403 ,  C07C31/205 ,  C07C31/202 ,  C07C31/04 ,  C07C31/08 ,  C07C33/20 ,  C07C33/22 ,  C07C31/1355 ,  C07C31/10 ,  C07C43/13 ,  C07C69/78 ,  C07C69/75 ,  C07C53/124 ,  C07C53/126 ,  C07C59/125 ,  C07C57/32 ,  C07C61/08 ,  C07C57/30 ,  C07C65/21 ,  C07C63/08 ,  C07C63/06

Abstract: The present invention relates to novel Ruthenium complexes and related borohydride complexes, and their use for (1) hydrogenation of amides (including polyamides) to alcohols and amines; (2) preparing amides from alcohols with amines (including preparing polyamides (e.g., polypeptides) by reacting dialcohols and diamines or by polymerization of amino alcohols); (3) hydrogenation of esters to alcohols (including hydrogenation of cyclic esters (lactones), cyclic di-esters (di-lactones) or polyesters); (4) hydrogenation of organic carbonates (including polycarbonates) to alcohols and of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (5) dehydrogenative coupling of alcohols to esters; (6) hydrogenation of secondary alcohols to ketones; (7) amidation of esters (synthesis of amides from esters and amines); (8) acylation of alcohols using esters; (9) coupling of alcohols with water to form carboxylic acids; and (10) dehydrogenation of beta-amino alcohols to form pyrazines. The present invention further relates to novel uses of certain pyridine Ruthenium complexes.

Abstract translation: 本发明涉及新型钌络合物和相关硼氢化物配合物及其用于（1）将酰胺（包括聚酰胺）氢化成醇和胺的用途; （2）由醇与胺（包括通过使二元醇和二胺反应制备聚酰胺（如多肽）或通过氨基醇的聚合）制备酰胺; （3）将酯氢化成醇（包括环酯（内酯）的加氢，环状二酯（二内酯）或聚酯））; （4）有机碳酸酯（包括聚碳酸酯）对醇和氨基甲酸酯（包括聚氨基甲酸酯）或脲衍生物氢化成醇和胺; （5）醇与酯的脱氢偶联; （6）将仲醇醇化成酮类; （7）酯的酰胺化（由酯和胺合成酰胺）; （8）使用酯酰化醇; （9）将醇与水偶联以形成羧酸; 和（10）β-氨基醇脱氢形成吡嗪。 本发明还涉及某些吡啶钌络合物的新用途。

公开(公告)号：US08729304B2

公开(公告)日：2014-05-20

申请号：US13122440

申请日：2009-09-24

Applicant: Frank Richter

Inventor： Frank Richter

IPC: C07F9/6584 ,  C07B43/06

CPC classification number: C07D251/46 ,  C07B43/06 ,  C07D247/02 ,  C07F9/6584

Abstract: The present invention relates to a 1,4,2-diazaphospholidine of the formula (1) wherein R1, R2 represent, independently of one another, saturated or mono- or polyunsaturated C1-C20-alkyl, -alkenyl, -alkynyl or C5-C40-aryl groups optionally substituted or interrupted by at least one heteroatom selected from the group consisting of N, O, S, and halogen, and X represents identical or different substituents selected from the group consisting of O, S, and N—R2.

Abstract translation: 本发明涉及式（1）的1,4,2-二氮杂磷杂环丁烷，其中R1，R2彼此独立地表示饱和或单或多不饱和C1-C20-烷基， - 烯基， - 炔基或C5- C40-芳基任选被至少一个选自N，O，S和卤素的杂原子取代或间隔，X代表相同或不同的选自O，S和N-R2的取代基。