公开(公告)号：US20230271917A1

公开(公告)日：2023-08-31

申请号：US18017033

申请日：2021-07-22

Applicant: FOG PHARMACEUTICALS, INC.

Inventor： Ivan Tucker Jewett ,  Lorenzo Josue Alfaro-Lopez ,  Yue-Mei Zhang ,  Brian Halbert White

IPC: C07C271/06 ,  C07C229/10 ,  C07C327/22 ,  C07D249/04

CPC classification number: C07C271/06 ,  C07C229/10 ,  C07C327/22 ,  C07D249/04

Abstract: In some embodiments, the present disclosure provides amino acid compounds that are useful for producing products such as peptides. In some embodiments, the present disclosure provides peptides comprising residues of provided amino acids.

公开(公告)号：US20210115032A1

公开(公告)日：2021-04-22

申请号：US16606397

申请日：2018-04-24

Applicant: Basilea Pharmaceutica International AG

Inventor： Gregor WELTI ,  Markus HEUBES ,  David TAGLIAFERRI

IPC: C07D413/04 ,  C07C271/06 ,  C07C269/06

Abstract: The present invention provides processes for preparing a compound of formula (I) and pharmaceutically acceptable salts thereof, comprising deprotecting a compound of formula (II), wherein each R3 independently represents a tertiary alkyl group, preferably wherein each R3 is tertiary butyl. The invention also provides intermediates useful for preparing compounds of formula (I) and processes for preparing these intermediates. Additionally the invention provides polymorphic forms of the dichloride salt of the compound of formula (I) and their use in the treatment of proliferative disorders.

公开(公告)号：US20190337890A1

公开(公告)日：2019-11-07

申请号：US15970586

申请日：2018-05-03

Applicant: AXALTA COATING SYSTEMS IP CO., LLC

Inventor： Michael Herm ,  Frank-Rainer Boehm ,  Pascal Meiners

IPC: C07C269/02 ,  C09D163/00 ,  C09D175/04 ,  C07C271/06 ,  C07C275/00 ,  C07C273/18 ,  B05D3/02 ,  B05D7/14

Abstract: This invention relates to a crosslinking component for binder resins which is especially suitable to be used together with epoxy-group containing binders and/or (poly)isocyanates such as blocked (poly)isocyanates and which comprises at least two blocked isocyanate groups per molecule of the crosslinking component whereby at least one of the at least two blocked isocyanate groups is a group according to structural unit (I), wherein the ratio of structural units of formula (II), if present, to structural units of formula (I) is 0.40 or below. The cross-linking component may also be self-cross-linkable. The present invention further relates to a coating composition, e.g. a one-component coating composition comprising the crosslinking component and a method of its manufacture.

公开(公告)号：US20110213114A1

公开(公告)日：2011-09-01

申请号：US12714515

申请日：2010-02-28

Applicant: WEN-CHIUNG SU ,  Wei-Ho Ting ,  Chun-Ming Yeh ,  Chia-Cheng Chang ,  Sheng-Hong Dai ,  Ru-Jong Jeng

Inventor： WEN-CHIUNG SU ,  Wei-Ho Ting ,  Chun-Ming Yeh ,  Chia-Cheng Chang ,  Sheng-Hong Dai ,  Ru-Jong Jeng

IPC: C08G18/32 ,  C08G18/24 ,  C07C271/06

CPC classification number: C07C275/40 ,  C08G18/10 ,  C08G18/2825 ,  C08G18/2895 ,  C08G18/3228 ,  C08G18/3275 ,  C08G18/4825 ,  C08G18/4854 ,  C08G18/3831

Abstract: A dendron with hydrophobic functional of end group, a polyurethane with the dendron, and producing methods thereof are disclosed. The dendron with hydrophobic functional of end group in the polyurethane systems, and the honeycomb-like structure thin films were obtained by a breath-figure process. The structures of dendron and dendritic side-chain polyurethanes are respectively expressed in the following. Therein, the end-groups (R) of the dendron are long alkyl chains or perfluoroalkyl derivatives.

Abstract translation: 公开了具有端基疏水功能的树枝状突起，具有树突的聚氨酯及其制造方法。 在聚氨酯体系中具有端基疏水功能的树枝状体，蜂窝状结构薄膜通过呼吸图法得到。 树枝状和枝状侧链聚氨酯的结构分别表示如下。 其中，树枝状结构基团（R）是长烷基链或全氟烷基衍生物。

公开(公告)号：US20110172421A1

公开(公告)日：2011-07-14

申请号：US13121048

申请日：2009-10-01

Applicant: Isao Yamagami ,  Yoshihiko Maeda ,  Hiroshi Yasuda ,  Katsumi Murofushi

Inventor： Isao Yamagami ,  Yoshihiko Maeda ,  Hiroshi Yasuda ,  Katsumi Murofushi

IPC: C07D265/30 ,  C07C269/00 ,  C07D211/06 ,  C07C271/06

CPC classification number: C07D295/205 ,  C07C269/00 ,  C07C269/02 ,  C07C271/24 ,  C07D211/06 ,  C07D211/16 ,  C07D317/52 ,  C07D317/62

Abstract: An object of the present invention is to provide a novel photobase generator which can sensitively generate a base even by h-ray in place of a conventional 2-nitro-4,5-dimethoxybenzyloxycarbonylamine compound. Disclosed is an N-(α-aromatic group-substituted-2-nitro-4,5-dialkoxybenzyloxycarbonyl)amine compound represented by the following general formula (I). (In the above formula (I), R1 to R9 denote specific groups.)

Abstract translation: 本发明的目的是提供一种新的光碱产生剂，其可以通过h射线代替常规的2-硝基-4,​​5-二甲氧基苄氧羰基胺化合物敏感地产生碱。 公开了由以下通式（I）表示的N-（α-芳族基团取代-2-硝基-4,​​5-二烷氧基苄氧基羰基）胺化合物。 （上式（I）中，R 1〜R 9表示具体的基团。）

公开(公告)号：US20110014715A1

公开(公告)日：2011-01-20

申请号：US12810453

申请日：2009-01-08

Applicant: Hyunil Lee ,  Jung Hyun Min

Inventor： Hyunil Lee ,  Jung Hyun Min

IPC: G01N33/48 ,  C07K9/00 ,  C07C271/06 ,  C08G64/00

CPC classification number: C07H7/00 ,  C07K14/003 ,  Y10T436/143333

Abstract: This invention relates to a peptide nucleic acid (PNA) oligomer which is conjugated with one or more linear-type amino acid containing a plurality of alkyleneglycols and to a synthesis method thereof. In addition, this invention related to a linear amino acid spacer in a device for detection for detecting a target gene using the PNA oligomers which is fixed on a surface of a functionalized solid support. The linear amino acid spacer contains a plurality of alkyleneglycols and maintains enough space between the solid support and PNA oligomer in the device in order to prevent the interference of the interaction between the PNA oligomer and a target gene. Furthermore, this invention relates to a PNA array, a PNA chip and a gene diagnosis kit whereof sensitivity and specificity are improved by being manufactured with the PNA conjugated with the amino acid spacer.

Abstract translation: 本发明涉及与含有多个亚烷基二醇的一种或多种线型氨基酸缀合的肽核酸（PNA）寡聚体及其合成方法。 此外，本发明涉及使用固定在官能化固体支持物表面上的PNA低聚物检测靶基因的检测装置中的线性氨基酸间隔物。 线性氨基酸间隔物包含多个亚烷基二醇并且在该装置中的固体支持物和PNA低聚物之间保持足够的空间，以便防止PNA低聚物与靶基因之间的相互作用的干扰。 此外，本发明涉及一种PNA阵列，PNA芯片和基因诊断试剂盒，其通过用氨基酸间隔基缀合的PNA制备灵敏度和特异性。

公开(公告)号：USRE41226E1

公开(公告)日：2010-04-13

申请号：US11607078

申请日：2006-12-01

Applicant: Fabio Giannessi ,  Mauro Marzi ,  Patrizia Minetti ,  Francesco De Angelis ,  Maria Ornella Tinti ,  Piero Chiodi ,  Arduino Arduini

Inventor： Fabio Giannessi ,  Mauro Marzi ,  Patrizia Minetti ,  Francesco De Angelis ,  Maria Ornella Tinti ,  Piero Chiodi ,  Arduino Arduini

IPC: A61K31/27 ,  C07C271/06

CPC classification number: C07D257/04 ,  C07C229/22 ,  C07C229/26 ,  C07C271/12 ,  C07C271/22 ,  C07C275/16 ,  C07C311/06 ,  C07C335/08 ,  C07D295/15 ,  C07D453/02 ,  C07F9/5407

Abstract: Compounds of formula (I) wherein the groups are as defined in the description are disclosed. The compounds of formula (I) are endowed with reversible inhibiting activity of carnitine palmitoyl-transferase and are useful in the preparation of medicaments useful in the pathologies related to a hyperactivity of carnitine polymitoyl-transferase, such as hyperglycemia, diabetes and pathologies related thereto, heart failure, ischemia.

Abstract translation: 公开了其中基团如说明书中定义的式（I）化合物。 式（I）化合物具有肉毒碱棕榈酰转移酶的可逆抑制活性，可用于制备与肉碱多聚酰胺转移酶多动症有关的病症，如高血糖症，糖尿病及其相关疾病， 心力衰竭，局部缺血。

公开(公告)号：US20080200511A1

公开(公告)日：2008-08-21

申请号：US10561425

申请日：2004-06-16

Applicant: Martin Griffin ,  Ian George Coutts ,  Robert Edward Saint

Inventor： Martin Griffin ,  Ian George Coutts ,  Robert Edward Saint

IPC: A61K31/27 ,  C07C271/06 ,  A61K31/4164 ,  A61K31/4178 ,  C07D233/54 ,  C07D207/04 ,  A61K31/40 ,  A61K31/445 ,  C07D211/06 ,  C07D403/02 ,  A61P35/00 ,  A61P31/12 ,  A61P37/00 ,  A61P17/00

CPC classification number: C07K5/06026 ,  A61K38/00 ,  C07K5/06034 ,  C07K5/06069 ,  C07K5/06078 ,  C07K5/06086 ,  C07K5/06104 ,  C07K5/06139 ,  C07K5/06165

Abstract: The present invention relates to novel compounds of Formula (I) wherein ‘X’ represents an amino acid group, ‘n’ is an integer between 1 and 4, ‘R1’ represents benzyl, t-butyl or 9-fluorenylmethyl and ‘R2’ represents a tetramethylmercaptoimidazole derivative or —S+R3R4, wherein R3 and R4 each independently represent lower alkyl, or a pharmaceutically and/or veterinarily acceptable derivative thereof. The present invention further relates to pharmaceutical formulations of said compound and the use thereof in the preparation of a medicament for inhibiting diseases in which transglutaminase has been implicated. Advantageously, the medicament is for treating fibrosis, scarring and/or cancer. Additionally, the invention relates to a method of inhibiting autoimmune diseases such as coeliac disease, neurodegeneration and chronic inflammatory diseases (e.g. of the joints including rheumatoid arthritis and osteoarthritis in a subject). The invention further relates to a method for preventing or treating rejection of a transplanted organ.

Abstract translation: 本发明涉及新的式（I）化合物，其中“X”表示氨基酸，“n”是1至4之间的整数，“R”1“表示苄基，叔丁基 或9-芴基甲基，'R 2'表示四甲基巯基咪唑衍生物或-S-O，R 3 R 4， 其中R 3和R 4各自独立地表示低级烷基或其药学上和/或兽医学上可接受的衍生物。 本发明还涉及所述化合物的药物制剂及其在制备用于抑制其中涉及转谷氨酰胺酶的疾病的药物中的用途。 有利地，药物用于治疗纤维化，瘢痕形成和/或癌症。 此外，本发明涉及抑制自身免疫性疾病如乳糜泻，神经变性和慢性炎症性疾病（例如关节中包括类风湿关节炎和受试者中的骨关节炎）的方法。 本发明还涉及一种预防或治疗移植器官排斥反应的方法。

公开(公告)号：US20080153899A1

公开(公告)日：2008-06-26

申请号：US11839911

申请日：2007-08-16

Applicant: Charles S. Swindell ,  Glenn G. Fegley

Inventor： Charles S. Swindell ,  Glenn G. Fegley

IPC: A61K31/337 ,  C07C271/06 ,  C07D493/22 ,  A61P35/00 ,  A61K31/27

CPC classification number: C07D209/48 ,  C07C265/06 ,  C07C271/12 ,  C07C275/20 ,  C07D243/38 ,  C07D305/14 ,  C07D405/04 ,  C07D473/24 ,  C07D519/04 ,  C07F9/65583 ,  C07F9/65616 ,  C07H15/252 ,  C07H19/06

Abstract: The invention provides conjugates of fatty amines and pharmaceutical agents useful in treating cancer, viruses, psychiatric disorders. Compositions, pharmaceutical preparations, and methods of preparations of the fatty amine-pharmaceutical agent conjugates are provided.

Abstract translation: 本发明提供脂肪胺和可用于治疗癌症，病毒，精神疾病的药物的缀合物。 提供了组合物，药物制剂和脂肪胺 - 药剂缀合物的制备方法。

公开(公告)号：US20080026407A1

公开(公告)日：2008-01-31

申请号：US11786792

申请日：2007-04-12

Applicant: Keith Wood ,  Dieter Klaubert ,  Georgyi Los ,  Robert Bulleit ,  Mark McDougall ,  Chad Zimprich

Inventor： Keith Wood ,  Dieter Klaubert ,  Georgyi Los ,  Robert Bulleit ,  Mark McDougall ,  Chad Zimprich

IPC: C12Q1/02 ,  C07C233/00 ,  C07C271/06 ,  C07D209/00 ,  C07D209/34 ,  G01N33/573 ,  C07D221/00 ,  C07D311/02 ,  C07D311/82 ,  C07D403/00

CPC classification number: C12Q1/34 ,  C07C217/08 ,  C07C271/16 ,  C07D209/48 ,  C07D233/64 ,  C07D311/78 ,  C07D311/82 ,  C07D405/06 ,  C07D493/10 ,  C07D495/04 ,  C07F5/022 ,  C12N9/14 ,  C12N9/86 ,  C12Y308/01005 ,  G01N33/5005 ,  G01N33/58 ,  Y10S436/80

Abstract: A mutant hydrolase optionally fused to a protein of interest is provided. The mutant hydrolase is capable of forming a bond with a substrate for the corresponding nonmutant (wild-type) hydrolase which is more stable than the bond formed between the wild-type hydrolase and the substrate. Substrates for hydrolases comprising one or more functional groups are also provided, as well as methods of using the mutant hydrolase and the substrates of the invention. Also provided is a fusion protein capable of forming a stable bond with a substrate and cells which express the fusion protein.

Abstract translation: 提供任选融合到感兴趣的蛋白质的突变体水解酶。 突变体水解酶能够与相应的非突变（野生型）水解酶的底物形成键，其比野生型水解酶和底物之间形成的键更稳定。 还提供了包含一个或多个官能团的水解酶的底物，以及使用本发明的突变体水解酶和底物的方法。 还提供能够与底物形成稳定结合的融合蛋白和表达融合蛋白的细胞。