公开(公告)号：US11505525B2

公开(公告)日：2022-11-22

申请号：US15630986

申请日：2017-06-23

Applicant: Quanta BioDesign, Ltd. ,  University of Washington

Inventor： Paul D. Davis ,  D. Scott Wilbur

IPC: A61K9/00 ,  C07D209/60 ,  C07C271/16 ,  C07C279/24 ,  C07D403/14 ,  C07C317/44 ,  C07C331/28 ,  C07K14/605 ,  C07D257/02 ,  C07C235/08 ,  C07C235/48 ,  C07D207/404 ,  C07D209/48 ,  C07K16/30 ,  C07K16/40 ,  A61K51/10

Abstract: Disclosed are general and “substantially pure” branched discrete polyethylene glycol constructs useful in attaching to a variety of biologically active groups, for example, preferential locators, as well as biologics like enzymes, for use in diagnostics, e.g. imaging, therapeutics, theranostics, and moieties specific for other applications. In its simplest intermediate state, a branched discrete polyethylene glycol construct is terminated at one end by a chemically reactive moiety, “A”, a group that is reactive with a biologic material that creates “A”, which is a biologically reactive group, connected through to a branched core (BC) which has attached at least two dPEG-containing chains, indicated by the solid line, , having terminal groups, which can be charged, non-reactive or reactable moieties and containing between about 2 and 64 dPEG residues.

公开(公告)号：US11174223B2

公开(公告)日：2021-11-16

申请号：US15593540

申请日：2017-05-12

Applicant: Lantheus Medical Imaging, Inc.

Inventor： Ajay Purohit ,  Pedro Benites ,  Heike S. Radeke ,  Joel Lazewatsky ,  L. Veronica Lee

IPC: A61K51/00 ,  A61M36/14 ,  C07C303/30 ,  A61K51/04 ,  C07B59/00 ,  C07C53/06 ,  C07C217/58 ,  C07C255/54 ,  C07C279/10 ,  C07C279/24 ,  C07C309/65 ,  C07C309/66 ,  C07C309/73 ,  C07C277/08 ,  C07C53/10 ,  C07C53/18 ,  C07C63/08 ,  C07C213/02 ,  C07C303/28 ,  C07C309/04 ,  C07C309/30 ,  C07C277/00

Abstract: The present invention generally relates to novel synthetic methods, systems, kits, salts, and precursors useful in medical imaging. In some embodiments, the present invention provides compositions comprising an imaging agent precursor, which may be formed using the synthetic methods described herein. An imaging agent may be converted to an imaging agent using the methods described herein. In some cases, the imaging agent is enriched in 18F. In some cases, an imaging agent including salt forms (e.g., ascorbate salt) may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs.

公开(公告)号：US20200317612A1

公开(公告)日：2020-10-08

申请号：US16597888

申请日：2019-10-10

Applicant: Quanta BioDesign, Ltd ,  University of Washington

Inventor： Paul D. Davis ,  D. Scott Wilbur

IPC: C07D209/60 ,  C07C271/16 ,  C07C279/24 ,  C07D403/14 ,  C07C317/44 ,  C07C331/28 ,  C07K14/605 ,  C07D257/02 ,  C07C235/08 ,  C07C235/48 ,  C07D207/404 ,  C07D209/48 ,  C07K16/30 ,  C07K16/40 ,  A61K51/10 ,  A61K47/60

Abstract: Disclosed are general and “substantially pure” branched discrete polyethylene glycol constructs useful in attaching to a variety of biologically active groups, for example, preferential locators, as well as biologics like enzymes, for use in diagnostics, e.g. imaging, therapeutics, theranostics, and moieties specific for other applications. In its simplest intermediate state, a branched branched discrete polyethylene glycol construct is terminated at one end by a chemically reactive moiety, “A”, a group that is reactive with a biologic material that creates “A”, which is a biologically reactive group, connected through to a branched core (BC) which has attached at least two dPEG-containing chains, indicated by the solid line, , having terminal groups, which can be charged, non-reactive or reactable moieties and containing between about 2 and 64 dPEG residues.

公开(公告)号：US10266485B2

公开(公告)日：2019-04-23

申请号：US16005286

申请日：2018-06-11

Applicant: ModernaTX, Inc.

Inventor： Kerry E. Benenato

IPC: A61K48/00 ,  A61K9/127 ,  C07C229/12 ,  C07C271/20 ,  C07C279/12 ,  C07C279/28 ,  C07C279/32 ,  C07D233/72 ,  C07D249/04 ,  C07D263/20 ,  C07D265/33 ,  C07D271/06 ,  C07D271/10 ,  C07D207/27 ,  C07D277/38 ,  C07C275/14 ,  C07C279/24 ,  C07C311/05 ,  C07C229/16 ,  C07C335/08 ,  C07C233/36 ,  C07C235/10 ,  C07C255/24 ,  C07F9/09 ,  A61K9/16 ,  A61K38/18 ,  C07K14/505 ,  A61K9/00 ,  A61K47/54 ,  A61K47/69 ,  C07C227/16 ,  A61K9/51 ,  A61K31/7105 ,  A61K38/17 ,  C07C227/18

Abstract: The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.

公开(公告)号：US10017462B1

公开(公告)日：2018-07-10

申请号：US15911299

申请日：2018-03-05

Applicant: Joong Ho Moon ,  Md Salauddin Ahmed

Inventor： Joong Ho Moon ,  Md Salauddin Ahmed

IPC: C08G73/06 ,  C07C279/24 ,  C07D241/04 ,  C08G71/02

Abstract: A poly(guanylurea) (PGU), comprising the structure where a multiplicity of repeating units are connected by guanylurea groups. The repeating units comprise: linear or cyclic alkylene, heteroatom interrupted alkylene, cycloalkylene, arylene, or heteroarylene; and a linear or cyclic alkylene, one or more heteroatom interrupted alkylene, cycloalkylene, arylene, heteroarylene, or a dinitrogen heterocycle. The PGU can be used as an antimicrobial agent with low toxicity in a pharmaceutical composition, generally as a protonated PGU upon combining with a pharmaceutically acceptable acid.

公开(公告)号：US20170304235A1

公开(公告)日：2017-10-26

申请号：US15517764

申请日：2015-10-09

Applicant: LEAD DISCOVERY SIENA S.R.L.

Inventor： Maurizio BOTTA ,  Giorgio MACCARI ,  Stefania SANFILIPPO ,  Filomena DE LUCA ,  Jean-Denis DOCQUIER ,  Davide DEODATO

IPC: A61K31/155 ,  C07C279/12 ,  C07C279/04 ,  C08K5/31 ,  C07C279/24 ,  C07C2601/02

CPC classification number: A61K31/155 ,  A61K31/17 ,  A61K45/06 ,  C07C279/04 ,  C07C279/12 ,  C07C279/24 ,  C07C2601/02 ,  C08K5/31 ,  Y02A50/473 ,  A61K2300/00

Abstract: The present invention relates to linear guanidine derivatives, methods of preparation, uses and pharmaceutical compositions thereof. The compounds of Formulas 1 or 2 exhibit high antimicrobial activity against Gram positive and Gram negative bacteria.

公开(公告)号：US06875764B1

公开(公告)日：2005-04-05

申请号：US10111376

申请日：2000-10-27

Applicant: Sabrina Muzi ,  Shoaá Abdul Rahman

Inventor： Sabrina Muzi ,  Shoaá Abdul Rahman

IPC: A23K1/16 ,  A23K1/18 ,  C07C275/30 ,  C07C275/34 ,  C07C275/38 ,  C07C275/40 ,  C07C275/42 ,  C07C279/24 ,  C07C279/28 ,  C07C281/16 ,  C07C281/18 ,  C07C335/16 ,  C07C335/18 ,  C07C335/22 ,  C07C335/28 ,  C07C335/42 ,  C07D209/54 ,  C07D213/71 ,  C07D213/75 ,  C07D215/38 ,  C07D217/24 ,  C07D233/84 ,  C07D241/20 ,  C07D265/24 ,  C07D265/30 ,  C07D277/48 ,  C07D277/82 ,  C07D295/215 ,  C07D401/12 ,  C07D405/04 ,  C07D413/12 ,  C07D417/14 ,  C07D275/28 ,  A61K31/17 ,  A61K31/425 ,  C07D295/16

CPC classification number: C07D213/75 ,  A23K20/105 ,  A23K20/111 ,  A23K20/116 ,  A23K50/75 ,  C07C275/30 ,  C07C275/34 ,  C07C275/38 ,  C07C275/40 ,  C07C275/42 ,  C07C279/24 ,  C07C279/28 ,  C07C281/16 ,  C07C281/18 ,  C07C335/16 ,  C07C335/18 ,  C07C335/22 ,  C07C335/28 ,  C07C335/42 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/42 ,  C07C2603/24 ,  C07C2603/74 ,  C07D209/54 ,  C07D213/71 ,  C07D215/38 ,  C07D217/24 ,  C07D233/84 ,  C07D241/20 ,  C07D265/24 ,  C07D265/30 ,  C07D277/48 ,  C07D277/82 ,  C07D295/215 ,  C07D401/12 ,  C07D405/04 ,  C07D413/12 ,  C07D417/14

Abstract: The present invention relates to novel compounds, pharmaceutical compositions containing the same as well as a method for treatment of parasitic disorders, wherein said compounds are administered. The present compounds are especially well suited for treatment of coccidiosis, particularly in poultry, and they have general formula (I): where Y is S or O and R is as defined in the specification.

Abstract translation: 本发明涉及新化合物，含有该化合物的药物组合物以及治疗寄生虫病的方法，其中施用所述化合物。 本发明化合物特别适用于治疗球虫病，特别是在家禽中，并且它们具有通式（I）：其中Y是S或O，R如说明书中所定义。

公开(公告)号：US06849733B1

公开(公告)日：2005-02-01

申请号：US08916527

申请日：1997-08-22

Applicant: Yufeng Hong ,  Vlad Edward Gregor ,  Anthony Lai Ling ,  Eileen Valenzuela Tompkins

Inventor： Yufeng Hong ,  Vlad Edward Gregor ,  Anthony Lai Ling ,  Eileen Valenzuela Tompkins

IPC: C07D295/12 ,  A61K31/17 ,  A61K31/341 ,  A61K31/351 ,  A61K31/357 ,  A61K31/381 ,  A61K31/397 ,  A61K31/40 ,  A61K31/407 ,  A61K31/4164 ,  A61K31/4184 ,  A61K31/439 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/4468 ,  A61K31/472 ,  A61K31/495 ,  A61K31/505 ,  A61K31/5375 ,  A61P3/04 ,  A61P9/10 ,  A61P9/12 ,  A61P11/08 ,  A61P15/00 ,  A61P25/22 ,  A61P43/00 ,  C07C279/00 ,  C07C279/24 ,  C07D205/00 ,  C07D205/04 ,  C07D207/09 ,  C07D207/27 ,  C07D207/335 ,  C07D211/26 ,  C07D211/62 ,  C07D211/72 ,  C07D213/38 ,  C07D213/40 ,  C07D217/02 ,  C07D217/26 ,  C07D233/61 ,  C07D235/16 ,  C07D239/42 ,  C07D295/20 ,  C07D307/14 ,  C07D307/52 ,  C07D309/14 ,  C07D319/12 ,  C07D333/20 ,  C07D409/12 ,  C07D413/00 ,  C07D453/02 ,  C07D487/08

CPC classification number: C07C279/24 ,  C07D213/40 ,  C07D307/14

Abstract: There are disclosed novel neuropeptide Y ligands having the general formula I Wherein the symbols W, A, D, R1, R2, R3, R4 are further defined in the description. Compounds of formula I are agonists and antagonists of neuropeptide Y, and are therefore useful as regulators.

Abstract translation: 公开了在说明书中进一步定义的符号W，A，D，R 1，R 2，R 3，R 4中具有通式IW的新型神经肽Y配体。 式I化合物是神经肽Y的激动剂和拮抗剂，因此可用作调节剂。

公开(公告)号：US5883132A

公开(公告)日：1999-03-16

申请号：US722168

申请日：1996-10-10

Applicant: Luc Lebreton ,  Patrice Renaut ,  Philippe Durand

Inventor： Luc Lebreton ,  Patrice Renaut ,  Philippe Durand

IPC: A61K31/16 ,  A61P1/00 ,  A61P11/00 ,  A61P29/00 ,  A61P33/02 ,  A61P37/06 ,  C07C247/12 ,  C07C271/20 ,  C07C277/00 ,  C07C279/14 ,  C07C279/24 ,  C07C231/14 ,  C07C231/18

CPC classification number: C07C279/24 ,  C07C247/12 ,  C07C271/20 ,  C07C279/14 ,  Y10S514/825 ,  Y10S514/895 ,  Y10S514/903

Abstract: The present invention relates to compounds selected from the group consisting of:(i) the compounds of the formula ##STR1## in which: R is a hydrogen atom, a group OH, a group OCH.sub.3 or a group CH.sub.2 OH,*C, in the case where R is not a hydrogen atom, is an asymmetric carbon atom of (R,S), (R) or (S) configuration, and**C is an asymmetric carbon atom of (R,S) or (R) configuration; and(ii) their addition salts.It further relates to the method of preparing these compounds, to their use in therapeutics and in the field of analysis, and to intermediates.

Abstract translation: PCT No.PCT / FR96 / 00203 Sec。 371日期：1996年10月10日 102（e）日期1996年10月10日PCT提交1996年2月7日PCT公布。 第WO96 / 24579号公报 日期：1996年8月15日本发明涉及选自以下的化合物：（i）式（I）的化合物，其中：R为氢原子，OH基团，OCH 3或 基团CH 2 OH，* C，在R不是氢原子的情况下，是（R，S），（R）或（S）构型的不对称碳原子，并且** C是（R ，S）或（R）构型; 和（ii）它们的加成盐。 它还涉及制备这些化合物的方法，其用于治疗学和分析领域以及中间体。

公开(公告)号：US5352796A

公开(公告)日：1994-10-04

申请号：US78965

申请日：1993-06-17

Applicant: Carl A. Hoeger ,  Jean E. F. Rivier ,  John S. Porter

Inventor： Carl A. Hoeger ,  Jean E. F. Rivier ,  John S. Porter

IPC: A61K38/04 ,  A61K38/00 ,  C07C277/08 ,  C07C279/18 ,  C07C279/24 ,  C07C279/28 ,  C07C313/30 ,  C07D249/14 ,  C07K1/00 ,  C07K7/02 ,  C07K7/06 ,  C07K7/23

CPC classification number: C07C279/24 ,  C07C277/08 ,  C07C279/28 ,  C07C313/30 ,  C07D249/14 ,  C07K1/006 ,  C07K7/02 ,  C07K7/23 ,  A61K38/00 ,  C07C2101/14 ,  Y02P20/55

Abstract: Unnatural amino acids are provided which can be incorporated into peptides which either inhibit or promote the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. These unnatural amino acids are useful in the synthesis of peptides and have the formula (a): ##STR1## where W is (CH.sub.2).sub.n or ##STR2## n is an integer from 1 to 6; j=1,2 or 3, and preferably, Y is N--CN, X is NH and R.sub.2 is alkyl, modified alkyl, alkenyl, alkynyl, aryl or methyl pyridyl; or the formula (b): ##STR3## where R.sub.11 is H or acyl and W is as defined in (a), and preferably R.sub.11 is H and W is ##STR4## Disclosed are peptides that are analogs of the decapeptide GnRH wherein there is at least one residue of an unnatural amino acid in the 3-, 5-, 6- and/or 8-positions.

Abstract translation: 可以提供非天然氨基酸，其可以并入肽中，其抑制或促进垂体分泌促性腺激素并抑制性腺释放类固醇。 这些非天然氨基酸可用于肽的合成并具有式（a）：其中W为（CH 2）n或 n为1至6的整数; j = 1,2或3，优选Y为N-CN，X为NH，R 2为烷基，改性烷基，烯基，炔基，芳基或甲基吡啶基; 或式（b）：其中R11为H或酰基，W为如（a）中所定义的式（b）：其中R 11为H且W为本文所公开的肽，其为存在十肽GnRH的类似物 在3-，5-，6-和/或8-位的至少一个非天然氨基酸残基。