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1. 发明申请

US20230002351A1 TRICYCLIC COMPOUNDS AS HISTONE METHYLTRANSFERASE INHIBITORS 有权
公开(公告)号：US20230002351A1
公开(公告)日：2023-01-05
申请号：US16639051
申请日：2018-08-13
申请人： GLOBAL BLOOD THERAPEUTICS, INC.
发明人： ZHE LI , MING YU , QING XU , MANUEL ZANCANELLA
IPC分类号： C07D401/12 , C07D215/42 , C07D401/14 , C07D405/14 , C07D491/056 , C07D491/044 , C07B59/00 , C07D487/04 , C07D413/12 , C07D453/02 , C07D487/08
摘要： The present disclosure provides certain tricyclic compounds that are histone methyltransferases G9a and/or GLP inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of G9a and/or GLP such as cancers and hemoglobinopathies (e.g., beta-thalassemia and sickle cell disease). Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

2. 发明申请

US20220380361A1 MATERIAL AND METHODS FOR THE TREATMENT OF GASTRO-INTESTINAL DISORDERS 有权
公开(公告)号：US20220380361A1
公开(公告)日：2022-12-01
申请号：US17887325
申请日：2022-08-12
申请人： Renexxion, LLC
发明人： Pascal Jean DRUZGALA , Peter MILNER , Jien Heh TIEN
IPC分类号： C07D453/02 , A61K9/00 , A61P1/10 , A61P1/04 , A61K31/439
摘要： Provided herein is a bulk composition comprising the trihydrate form of (3S, 4R, 3′R)-6-[4-(4-amino-5-chloro-2-methoxy-benzoylamino)-3-methoxy-piperidin-1-yl]-hexanoic acid 1-azabicyclo[2.2.2]oct-3′-yl ester di-hydrochloride salt. Provided are also pharmaceutical compositions and dosage forms comprising the trihydrate form, and methods and uses for treating a gastrointestinal disorder in a subject with the trihydrate form. In some embodiments, the gastrointestinal disorder is gastroesophageal reflux disease (GERD), dyspepsia (such as functional dyspepsia or functional motility disorder), gastroparesis, paralytic ileus, post-operative ileus, emesis, nausea, heartburn, intestinal pseudo-obstruction, irritable bowel syndrome (IBS), constipation, enteral feeding intolerance (EFI), or esophagitis. In some embodiments, the gastrointestinal disorder is post-operative ileus, chronic grass sickness, constipation, megacolon, gastritis, gastrointestinal stasis, or abomasal emptying defect.

3. 发明授权

US11427584B2 Process for the preparation of umeclidinium bromide 有权
公开(公告)号：US11427584B2
公开(公告)日：2022-08-30
申请号：US16927574
申请日：2020-07-13
申请人： Hovione Scientia Limited
发明人： Nuno Torres Lourenço , Luis Sobral , Rafael Antunes , Maria Santos , Margarida Espadinha
IPC分类号： C07D471/08 , A61K9/00 , A61K9/14 , C07D211/62 , C07D453/02
摘要： The present invention discloses processes comprising a) reacting ethyl isonipecotate with 1-bromo-2-chloroethane in the presence of an organic base in a solvent to form ethyl 1-(2-chloroethyl)piperidine-4-carboxylate (II) or a salt thereof. Process step a) may be included in a process for preparing umeclidinium bromide that comprises further process steps: b) reacting ethyl 1-(2-chloroethyl)piperidine-4-carboxylate (II) or a salt thereof with lithium diisopropylamide in a solvent to form ethyl 1-azabicyclo[2.2.2]octane-4-carboxylate (III); c) reacting ethyl 1-azabicyclo[2.2.2]octane-4-carboxylate (III) with phenyl lithium in a solvent to form 1-azabicyclo[2.2.2]oct-4-yl(diphenyl)methanol (IV); and d) reacting 1-azabicyclo[2.2.2]oct-4-yl(diphenyl)methanol (IV) with ((2-bromoethoxy)methyl) benzene in a solvent to form 4-[hydroxyl(diphenyl)methyl]-1-[2-(phenylmethyl)oxy]ethyl]-1-azoniabicyclo[2.2.2]octane bromide (I), umeclidinium bromide. A process comprising d) reacting 1-azabicyclo[2.2.2]oct-4-yl(diphenyl)methanol with ((2-bromoethoxy)methyl) benzene in a solvent to form 4-[hydroxyl(diphenyl)methyl]-1-[2-(phenylmethyl)oxy]ethyl]-1-azoniabicyclo[2.2.2]octane bromide (I), umeclidinium bromide, wherein the solvent is selected from cyclic ethers such as tetrahydrofuran, aromatic solvents, such as toluene, ketones such as acetone and protic solvents such as water or combinations thereof, optionally wherein the solvent is water is also disclosed. Umeclidinium bromide obtainable from the disclosed processes, ethyl 1-(2-chloroethyl)piperidine-4-carboxylate (II) and pharmaceutical compositions are also disclosed.

4. 发明申请

US20220251084A1 PROGRANULIN MODULATORS AND METHODS OF USING THE SAME 有权
公开(公告)号：US20220251084A1
公开(公告)日：2022-08-11
申请号：US17614666
申请日：2020-06-12
申请人： ARKUDA THERAPEUTICS
发明人： Duane A. Burnett , William J. Greenlee , James C. Lanter
IPC分类号： C07D471/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D413/06 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/14 , C07D453/02 , C07D471/10 , C07D487/04 , C07D487/08 , C07D491/048 , C07D498/08 , C07D498/10 , C07D519/00
摘要： Provided herein are compounds that modulate progranulin and methods of using the compounds in progranulin-associated disorders, such as Frontotemporal dementia (FTD).

5. 发明申请

US20220249500A1 PHENOXY(HETERO)ARYL ETHERS OF ANTIPROLIFERACTIVE ACTIVITY 有权
公开(公告)号：US20220249500A1
公开(公告)日：2022-08-11
申请号：US17270652
申请日：2019-08-23
申请人： XENIOPRO GmbH
发明人： Viktoria REINMÜLLER , Roman MARTY , Olivier WAGNIÈRES , Jean-Baptiste GUALTIEROTTI , Verena KÜPPERS
IPC分类号： A61K31/5375 , C07C43/275 , C07D213/647 , A61K31/09 , A61K31/44 , A61P35/02 , A61P35/00 , C07D295/096 , C07D453/02 , A61K31/351 , A61K31/451 , A61K31/495 , A61K31/439 , C07D305/06 , C07D331/04 , C07D205/04 , A61K31/337 , A61K31/38 , A61K31/397 , C07D407/12 , C07D411/12 , C07D405/12 , C07D409/12 , C07D401/12 , A61K31/5377 , A61K31/496 , C07D309/04 , A61K31/12 , A61K31/085 , C07C49/255 , C07C43/295 , C07C205/04 , C07C251/20 , C07C251/48 , A61K31/04 , A61K31/15 , A61K39/39
摘要： The present invention comprises novel aromatic molecules, which can be used in the treatment of pathological conditions, such as cancer, skin diseases, muscle disorders, and immune system-related disorders such as disorders of the haematopoietic system including the haematologic system in human and veterinary medicine.

6. 发明授权

US11230517B2 Method for aromatic fluorination 有权
公开(公告)号：US11230517B2
公开(公告)日：2022-01-25
申请号：US17015775
申请日：2020-09-09
申请人： DOW GLOBAL TECHNOLOGIES LLC , THE REGENTS OF THE UNIVERSITY OF MICHIGAN
发明人： Melanie S. Sanford , Douglas Bland , Patrick S. Hanley , Megan A. Cismesia , Sydonie D. Schimler
IPC分类号： C07C17/02 , C07D453/02 , C07D311/16 , C07C17/093 , C07D209/08 , C07D213/79 , C07D213/61 , C07C231/12 , C07C41/22 , C07C45/63 , C07D213/57 , C07C201/12 , C07C67/307 , C07D213/75 , C07J21/00 , C07D279/16 , C07C253/30 , C07D209/88 , C07D215/18 , C07C25/13 , C07C317/14
摘要： Disclosed is a fluorination method comprising providing an aryl fluorosulfonate and a fluorinating reagent to a reaction mixture; and reacting the aryl fluorosulfonate and the fluorinating reagent to provide a fluorinated aryl species.
Also disclosed is a fluorination method comprising providing, a salt comprising a cation and an aryloxylate, and SO2F2 to a reaction mixture; reacting the SO2F2 and the ammonium salt to provide a fluorinated aryl species.
Further disclosed a fluorination method comprising providing a compound having the structure Ar—OH to a reaction mixture; where Ar is an aryl or heteroaryl; providing SO2F2 to the reaction mixture; providing a fluorinating reagent to the reaction mixture; reacting the SO2F2, the fluorinating reagent and the compound having the structure Ar—OH to provide a fluorinated aryl species having the structure Ar—F.

7. 发明申请

US20210369710A1 MODULATORS OF MYC FAMILY PROTO-ONCOGENE PROTEIN 有权
公开(公告)号：US20210369710A1
公开(公告)日：2021-12-02
申请号：US17404529
申请日：2021-08-17
申请人： Nalo Therapeutics
发明人： Keith Wilson , William Greenlee , Ken Brameld , Anand Kumar Raichurkar , Prashant Latthe , Ganesh Babu Karunakaran
IPC分类号： A61K31/506 , A61K45/06 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/14 , C07D409/14 , C07D493/08 , C07D403/14 , C07D451/04 , C07D453/02
摘要： Disclosed herein are compounds and compositions having potency in the modulation of Myc family proteins. Such compounds and compositions can be used in the treatment of proliferative diseases, such as cancer, or in the treatment of disease where modulation of Myc family proteins is desired. Also disclosed herein are methods of using said compounds and compositions.

8. 发明授权

US11117900B2 Compounds useful as inhibitors of ATR kinase 有权
公开(公告)号：US11117900B2
公开(公告)日：2021-09-14
申请号：US16532596
申请日：2019-08-06
申请人： Vertex Pharmaceuticals Incorporated
发明人： Nadia Ahmad , Dean Boyall , Jean-Damien Charrier , Chris Davis , Rebecca Davis , Steven Durrant , Gorka Etxebarria I Jardi , Damien Fraysse , Juan-Miguel Jimenez , David Kay , Ronald Knegtel , Donald Middleton , Michael O'Donnell , Maninder Panesar , Francoise Pierard , Joanne Pinder , David Shaw , Pierre-Henri Storck , John Studley , Heather Twin
IPC分类号： C07D487/04 , C07D453/02 , C07D471/08 , C07D487/08 , C07D491/107 , C07D498/04 , C07D498/10
摘要： The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.
The compounds of this invention have formula I: or a pharmaceutically acceptable salt, wherein the variables are as devined herein. Moreover, The compounds of this invention have formula I-A: or a pharmaceutically acceptable salt, wherein the variables are as defined herein.

9. 发明申请

US20210261557A1 GLUCOSYLCERAMIDE SYNTHASE INHIBITORS 有权
公开(公告)号：US20210261557A1
公开(公告)日：2021-08-26
申请号：US17242016
申请日：2021-04-27
申请人： GENZYME CORPORATION
发明人： Elyse BOURQUE , Mario CABRERA-SALAZAR , Cassandra CELATKA , Seng CHENG , Mary A. CROMWELL , Andrew GOOD , Bradford HIRTH , Katherine JANCSICS , John P. LEONARD , Lingyun LI , James LILLIE , Hanlan LIU , Elina MAKINO , John MARSHALL , Paul MASON , Markus METZ , Fazeela MORSHED , Thomas O'SHEA , Ronald SCHEULE , Renato SKERLJ , Bing WANG , Yibin XIANG , Zhong ZHAO
IPC分类号： C07D487/08 , A61K31/439 , A61K31/454 , A61K38/47 , C07D453/02 , C07D453/00 , A61K31/46 , A61K31/506 , A61K31/551 , C07D455/02
摘要： The invention relates to inhibitors of glucosylceramide synthase (GCS) useful for the treatment of metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, and for the treatment of cancer.

10. 发明授权

US11028082B2 Process for the preparation of a novel umeclidinium synthesis intermediate 有权
公开(公告)号：US11028082B2
公开(公告)日：2021-06-08
申请号：US16617928
申请日：2018-05-28
申请人： OLON S.P.A.
发明人： Giorgio Bertolini , Corrado Colli , Filippo Nisic , Mara Sada , Stefania Bertuolo , Silvano Ronzoni , Stefano Maiorana , Romano Di Fabio
IPC分类号： C07D453/02
摘要： The present invention relates to a process for the preparation of a novel and versatile synthesis intermediate and its use in the preparation of umeclidinium. The invention also relates to some reference standards allowing to detect impurity traces recurring in the preparation of umeclidinium and a process for their preparation.

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