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公开(公告)号：US20240352007A1
公开(公告)日：2024-10-24
申请号：US18390071
申请日：2023-12-20
发明人： Gregor WELTI , Markus HEUBES , David TAGLIAFERRI
IPC分类号： C07D413/04 , C07C269/06 , C07C271/06
CPC分类号： C07D413/04 , C07C269/06 , C07C271/06 , C07B2200/13
摘要： 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：US20240351975A1
公开(公告)日：2024-10-24
申请号：US18676957
申请日：2024-05-29
申请人： XWPHARMA LTD.
发明人： JIA-NING XIANG , HAO-WEI SHIH , XIAOMING WU , XUAN ZHANG , JAMES TIEN
IPC分类号： C07C229/08 , C07C227/16 , C07C227/18 , C07C227/20 , C07C269/06 , C07C271/22
CPC分类号： C07C229/08 , C07C227/16 , C07C227/18 , C07C227/20 , C07C269/06 , C07C271/22
摘要： The present disclosure is directed synthetic methods for the preparation of 4-valyloxybutyric acid. The synthetic methods described herein employ a diverse array of protecting group strategies and reaction conditions. Additionally, the present disclosure is directed to compounds useful as synthetic intermediates in the preparation of 4-valyloxybutyric acid.
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公开(公告)号：US11780970B2
公开(公告)日：2023-10-10
申请号：US18184439
申请日：2023-03-15
申请人： Galderma Holding SA
发明人： Hotan Mojarradi , Johan Olsson , Craig Harris , Jean-Guy Boiteau , Thibaut Gerfaud , Loïc Tomas
IPC分类号： A61K8/04 , A61K8/73 , A61P17/00 , A61Q19/00 , A61K9/00 , C08B37/08 , C08K5/09 , C08K5/08 , C07C209/62 , C07C7/08 , C07C213/00 , C08J3/24 , C08J3/075 , C08L5/00 , C08J7/14 , C07C269/06 , C08B37/00 , C08L5/08 , C07F7/08
CPC分类号： C08J3/075 , A61K8/042 , A61K8/73 , A61K8/735 , A61K9/0019 , A61Q19/00 , C07C209/62 , C07C213/00 , C07C269/06 , C07F7/083 , C08B37/0063 , C08B37/0069 , C08B37/0072 , C08J3/24 , C08J7/14 , C08K5/09 , C08L5/00 , C08L5/08 , C07C2603/18 , C08J2305/00 , C08J2305/08
摘要： The invention relates to a hydrogel product comprising glycosaminoglycan molecules as the swellable polymer, wherein the glycosaminoglycan molecules are covalently crosslinked via crosslinks comprising a spacer group selected from the group consisting of di-, tri-, tetra-, and oligosaccharides.
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公开(公告)号：US20230102685A1
公开(公告)日：2023-03-30
申请号：US17839202
申请日：2022-06-13
申请人： Synaffix B.V.
IPC分类号： C07C33/16 , A61K49/00 , C07C29/147 , C07C29/58 , C07C29/62 , C07C67/347 , C07C271/12 , G01N33/532 , G01N33/58 , A61K47/54 , C07C62/30 , C07C269/06 , C07C271/20 , C07D311/82 , C07D495/04 , C07K14/47 , G01N21/64
摘要： The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.
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公开(公告)号：US11613514B2
公开(公告)日：2023-03-28
申请号：US17155162
申请日：2021-01-22
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , University of Maryland, Baltimore
发明人： Craig Thomas , Carlos Zarate , Ruin Moaddel , Todd Gould , Panos Zanos , Patrick Morris
IPC分类号： C07C225/20 , C07C221/00 , C07C269/06
摘要： The disclosure provides a method for synthesizing free base forms of (2R,6R)-hydroxynorketamine (HNK) and (2S,6S)-hydroxynorketamine. In an embodiment synthesis of (2R,6R)-hydroxynorketamine (HNK) includes preparation of (R)-norketamine via chiral resolution from racemic norketamine via a chiral resolution with L-pyroglutamic acid. The disclosure also provided crystal forms of the corresponding (2R,6R)-hydroxynorketamine (HNK) and (2S,6S)-hydroxynorketamine hydrochloride salts.
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公开(公告)号：US11370747B2
公开(公告)日：2022-06-28
申请号：US16607443
申请日：2018-04-25
IPC分类号： C07C231/02 , C07C231/12 , C07C269/06 , B01J31/02 , B01J31/36 , C07C237/12 , C07C271/20 , C07C271/22
摘要： Provided is a novel method for producing amide compounds at high stereochemical selectivities. The method according to the present invention for producing amide compounds is provided with an amidation step for reacting, in the presence of a catalyst comprising a metal compound, an amino compound with an aminoester compound represented by general formula (1) to amidate the ester group in the aminoester compound.
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公开(公告)号：US20220162159A1
公开(公告)日：2022-05-26
申请号：US17265356
申请日：2019-08-09
发明人： Shekhar Bhaskar Bhirud , Samir Naik , Sushanta K. Mishra , Rahul Bhalchadrarao Kawthekar , Deepak Shantaram Patekar , Nitesh Patll
IPC分类号： C07C269/06
摘要： The present invention relates to solriamfetol or novel salts thereof and its process for preparation. More particularly the present invention relates to solriamfetol dibenzoyl-D-tartaric acid salt or solriamfetol di-p-toluoyl-D-tartaric acid salt and their process for preparation. Further the present invention relates to use of solriamfetol dibenzoyl-D-tartaric acid salt or solriamfetol di-p-toluoyl-D-tartaric acid salt for the preparation of solriamfetol hydrochloride.
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8.发明授权公开(公告)号：US11333976B2
公开(公告)日：2022-05-17
申请号：US15545912
申请日：2016-01-25
发明人： Tomoyuki Yuba , Yuki Masuda , Jiake Jin , Ping Li
IPC分类号： G03F7/023 , G03F7/40 , C08G69/32 , C07C209/74 , C07C231/02 , C07D209/48 , C07D263/62 , C07C231/12 , H01L21/027 , C07C41/22 , H01L23/31 , H05K3/34 , C07C213/00 , C07C211/56 , C08G73/10 , G03F7/037 , C09D179/08 , C07C67/307 , C07C269/06 , C09D179/04 , G03F7/039 , C07C25/18 , C07C215/80 , C07D263/56 , C08G73/22 , G03F7/16 , G03F7/20 , G03F7/32 , H01L23/29 , H01L27/12 , H05K1/02 , H01L27/32
摘要： A resin having a small linear thermal expansion coefficient and a low absorbance is provided. The resin is characterized by including at least one structure selected from structures represented by the following general formulae (1) and (2):
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公开(公告)号：US11236076B2
公开(公告)日：2022-02-01
申请号：US16088374
申请日：2017-03-27
申请人： Novartis AG
IPC分类号： C07D405/14 , C07C211/52 , C07C269/06 , C07D241/20 , C07D333/64 , C07D401/04 , C07D403/14 , C07D487/04
摘要： The present invention is directed to reaction mixtures comprising a water-surfactant mixture and a co-solvent. This technology reduced the amount of organic solvents needed for performing chemical reactions. Furthermore, compared to reaction mixtures lacking the co-solvent, solvation of the reactants and products of the chemical reaction is greatly enhanced, leading to a significantly improved yield, purity, reproducibility and robustness.
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公开(公告)号：US20220017451A1
公开(公告)日：2022-01-20
申请号：US17389633
申请日：2021-07-30
申请人： SHENZHEN CATALYS TECHNOLOGY CO., LTD , Shenzhen Innovation Center of Small Molecule Drug Discovery Co., Ltd.
发明人： Qiwei LANG , Xiaobing DING , Shaobai YAN
IPC分类号： C07C209/26 , C07C213/02 , C07C269/06
摘要： The present invention relates to a preparation method of chiral primary amine. The chiral primary amine is prepared through a one-pot method that under the action of a ruthenium-chiral diphosphine catalyst, a simple ketone and an ammonium salt RCOONH4 have reductive amination by adding hydrogen and then are heated and hydrolyzed by adding acid. The present invention has the advantages of good substrate universality, high reaction efficiency and the like
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