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1. 发明申请

US20230113085A1 NOVEL SMALL MOLECULE INHIBITORS OF TEAD TRANSCRIPTION FACTORS 有权
公开(公告)号：US20230113085A1
公开(公告)日：2023-04-13
申请号：US17439735
申请日：2020-03-13
申请人： The General Hospital Corporation
发明人： Xu Wu , Pranab Maiti , Chandrasekhar Abbineni , Krishna Chaitanya Talluri , Sunil Kumar Panigrahi , Gopala Krishna Jarugumilli , Yang Sun
IPC分类号： C07D471/04 , C07C229/58 , C07C255/58 , C07C211/56 , C07D249/08 , C07D213/74 , C07D213/80 , C07C229/44 , C07C211/55 , C07D215/227 , C07D275/06 , C07C229/48 , C07D207/16 , C07D239/42 , C07D241/28 , C07D211/62 , C07D205/04 , C07D231/56 , C07D235/18 , C07D317/32 , C07D233/61 , C07D401/12 , C07D209/08 , C07D401/06 , C07D295/135 , C07C237/40 , C07C311/44
摘要： The present disclosure compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the TEAD transcription factor, and are useful in the treatment of diseases related to the activity of TEAD transcription factor including, e.g., cancer and other diseases.

2. 发明授权

US11485708B2 Compounds for treatment of PD-L1 diseases 有权
公开(公告)号：US11485708B2
公开(公告)日：2022-11-01
申请号：US16905979
申请日：2020-06-19
申请人： CHEMOCENTRYX, INC.
发明人： Viengkham Malathong , Pingchen Fan , Christopher Lange , Venkat Reddy Mali , Darren J. McMurtrie , Sreenivas Punna , Howard S. Roth , Rajinder Singh , Ju Yang , Penglie Zhang
IPC分类号： C07D217/04 , A61K45/06 , C07D401/12 , A61K31/4725 , C07C217/58 , A61K31/137 , C07D211/58 , A61K31/4468 , A61K31/4545 , C07C229/16 , A61K31/197 , C07D207/06 , A61K31/40 , C07D319/18 , A61K31/357 , C07D213/64 , A61K31/4402 , C07D215/227 , A61K31/4704 , C07C309/14 , A61K31/185 , A61K31/472
摘要： Compounds are provided that are useful as immunomodulators. The compounds have the Formula (I) including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1a, R1b, R1c, R1d, R2a, R2b, R3, R3a, R4, R5, R6, R7, R8 and the subscript n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

3. 发明授权

US11447471B2 α,β-unsaturated amide compound 有权
公开(公告)号：US11447471B2
公开(公告)日：2022-09-20
申请号：US16625446
申请日：2018-06-22
申请人： KYOWA KIRIN CO., LTD.
发明人： Tomohiro Danjo , Hiroki Yamada , Takahiro Nakajima
IPC分类号： A61P35/00 , C07D263/56 , C07D263/57 , C07D267/14 , C07D277/64 , C07D307/83 , C07D307/86 , C07D313/08 , C07D405/12 , C07D213/63 , C07D213/643 , C07D213/75 , C07D215/227 , C07D215/233 , C07D215/26 , C07D215/38 , C07D215/40 , C07D217/02 , C07D311/58 , C07D311/68 , C07D333/66 , C07D401/04 , C07D401/12 , C07D413/12 , C07D471/04 , C07D491/052
摘要： An object of the present invention is to provide an α,β-unsaturated amide compound or a pharmaceutically acceptable salt or the like thereof having anticancer activity and the like. The α,β-unsaturated amide compound represented by the following formula (I) or a pharmaceutically acceptable salt or the like thereof has anticancer activity and the like: [wherein, “A” represents optionally substituted heterocyclic diyl, R1 represents hydrogen atom or optionally substituted lower alkyl, R2 represents optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted aliphatic heterocyclic group or optionally substituted aromatic heterocyclic group, X represents —O—, —S—, —SO2—, —NRX1— (wherein, RX1 represents hydrogen atom or lower alkyl), —CHRX2— (wherein, RX2 represents hydrogen atom or hydroxy), —CH═CH—, −CO— or —NH—CO—, and n1 and n2 are the same or different, and each represents 0 or 1].

4. 发明授权

US11312668B2 Organic reactions carried out in aqueous solution in the presence of a hydroxyalkyl(alkyl)cellulose or an alkylcellulose 有权
公开(公告)号：US11312668B2
公开(公告)日：2022-04-26
申请号：US17060801
申请日：2020-10-01
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Wilfried Braje , Katarina Britze , Justin D. Dietrich , Anais Jolit , Johannes Kaschel , Johanna Klee , Tanja Lindner
IPC分类号： C07D213/74 , C07D215/227 , C07D239/26 , C07D239/42 , C07D307/36 , C07D307/81 , C07D311/58 , C07D405/04 , C07D409/04 , C07D471/04 , C07D495/04 , C07B63/04 , C07B43/06 , C07F5/02 , C07B43/04 , C07B37/04 , C07C41/46 , C07C67/62 , C07C209/90 , C07C213/10 , C07C231/22 , C07C253/32 , C07C269/08 , C07C273/18 , C07C303/42 , C07C319/26 , C07D205/04 , C07D207/34 , C07D209/08 , C07D209/48 , C07D211/06
摘要： 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.

5. 发明授权

US11261170B2 Aromatic compound, pharmaceutical composition and use thereof 有权
公开(公告)号：US11261170B2
公开(公告)日：2022-03-01
申请号：US16879204
申请日：2020-05-20
申请人： Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd.
发明人： Jiawang Zhu , Zhiquan Song , Dong Long , Lichun Wang , Jingyi Wang
IPC分类号： C07D401/04 , A61P1/16 , C07D215/14 , C07D215/227 , C07D215/36 , C07D215/38 , C07D333/56 , C07D413/04
摘要： The invention relates to an aromatic compound, pharmaceutical composition comprising the same, and a method for preparing the compound and an intermediate thereof. The invention also relates to use of the compound for the manufacture of a medicament for the prevention or treatment of a PPAR-related disease.

6. 发明申请

US20210340106A1 MODULATORS OF MAS-RELATED G-PROTEIN RECEPTOR X4 AND RELATED PRODUCTS AND METHODS 有权
公开(公告)号：US20210340106A1
公开(公告)日：2021-11-04
申请号：US17231834
申请日：2021-04-15
申请人： Escient Pharmaceuticals, Inc.
发明人： Marcos Sainz , Adam Yeager , Brandon Selfridge , Esther Martinborough , Marcus Boehm , Liming Huang
IPC分类号： C07D215/227 , C07D209/46 , C07D217/24 , C07D209/34 , C07D413/12
摘要： Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4 dependent condition more specifically, by contacting the MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I): or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein m, n, p, t, A, B, Z, R1, R2 and R3 are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.

7. 发明申请

US20210338847A1 RADIOLABELLED COMPOUND OF A QUATERNARY AMMONIUM SALT OF A POLYCYCLIC AROMATIC AMINE AND METHODS OF MANUFACTURING AND DIAGNOSTIC USE THEREOF 有权
公开(公告)号：US20210338847A1
公开(公告)日：2021-11-04
申请号：US17273647
申请日：2019-09-04
申请人： SYNEKTIK S.A.
发明人： Joanna TOWPIK , Seweryn Andrzej KRAJEWSKI , Joanna WLOSTOWSKA , Lukasz Marek STECZEK
IPC分类号： A61K51/04 , C07D215/12 , C07D219/02 , C07D219/08 , C07D215/227 , C07D219/06 , C07B59/00
摘要： The disclosure relates to a radioisotope-labelled compound having a structure according to formula I, wherein a wavy line indicates a single bond between a non-nodal carbon atom of a polycyclic aromatic system and an R1 substituent selected from a hydrogen; a halogen; a hydroxy; a protected hydroxy; a C1-4 alkoxy; a nitro group; an amino group; an amino group having 1 hydrogen replaced with a C1-C6 alkyl group; an amino group having 2 hydrogens replaced with a C1-C6 alkyl group; an amino group having 2 hydrogen atoms replaced with C2-5 alkylene to form a heterocyclic ring; a chain C1-6 carbon group; a chain C1-6 carbon group having a substituent selected from a halogen, carboxyl, a formyl, and a C1-4 alkanesulfonic; a phenyl group; a phenyl group having 1-5 substituents independently selected from halogens, a chain C1-6 carbon, a halogenated chain C1-6 carbon substituent, a hydroxy, a protected hydroxy, a C1-4 alkoxy, and an amino group having 1-2 atoms of hydrogen replaced with C1-6 alkyl; wherein R2 is a chain aliphatic substituent having: a total of 1-16 carbon atoms, an atom of 18F fluorine radioisotope replacing a hydrogen atom at one of the carbon atoms, and a —CH2 fragment as a terminal member of a chain, wherein the chain connects to one of a hydrogen, a phenyl group, and a phenyl group having 1-3 substituents selected from halogens and C1-6 alkyl, and wherein if the chain contains at least 2 carbon atoms and there is a bivalent link between the chain carbon atoms, then the bivalent link is selected from the group consisting of an oxygen atom —O—, a sulfur atom —S—, and a C3-6 cycloalkylene; wherein R3 and R4 are combined to form a bivalent butadienyl-1,3 substituent whose terminal carbon atoms are linked to adjacent non-nodal carbon atoms of a B ring to form an aromatic C ring fused with an A and B ring system, having R1 substituents at non-nodal carbon atoms; wherein n is an integer of 9; wherein X− is a pharmaceutically acceptable counter ion selected from: an anion of a mono-basic inorganic acid, a mononegative anion of a multi-basic inorganic acid, an anion of an alkane carboxylic acid, an anion of an aliphatic sulfonic acid, an anion of an aromatic sulfonic acid, an anion of an acidic amino acid, a hydrate thereof, and a solvate thereof.

8. 发明申请

US20210017100A1 ORGANIC REACTIONS CARRIED OUT IN AQUEOUS SOLUTION IN THE PRESENCE OF A HYDROXYALKYL(ALKYL)CELLULOSE OR AN ALKYLCELLULOSE 有权
公开(公告)号：US20210017100A1
公开(公告)日：2021-01-21
申请号：US17060801
申请日：2020-10-01
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Wilfried BRAJE , Katarina BRITZE , Justin D. DIETRICH , Anais JOLIT , Johannes KASCHEL , Johanna KLEE , Tanja LINDNER
IPC分类号： C07B63/04 , C07B43/06 , C07F5/02 , C07B43/04 , C07B37/04 , C07C41/46 , C07C67/62 , C07C209/90 , C07C213/10 , C07C231/22 , C07C253/32 , C07C269/08 , C07C273/18 , C07C303/42 , C07C319/26 , C07D205/04 , C07D207/34 , C07D209/08 , C07D209/48 , C07D211/06 , C07D213/74 , C07D215/227 , C07D239/26 , C07D239/42 , C07D307/36 , C07D307/81 , C07D311/58 , C07D405/04 , C07D409/04 , C07D471/04 , C07D495/04
摘要： 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.

9. 发明授权

US10717739B2 Methods and compositions for inhibition of bromodomain-containing proteins 有权
公开(公告)号：US10717739B2
公开(公告)日：2020-07-21
申请号：US16385606
申请日：2019-04-16
申请人： ConverGene LLC
发明人： Hariprasad Vankayalapati , Makoto Yoshioka , Jeffrey William Strovel , Janak Khimchand Padia
IPC分类号： A61K31/47 , C07D487/04 , C07D401/14 , C07D413/14 , C07D215/227 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/06 , C07D409/06 , C07D409/14 , C07D413/04 , C07D471/04 , C07D265/22 , C07D265/26 , C07D261/08 , C07C217/84 , C07D215/22 , C07D215/38
摘要： The present invention relates to compounds that bind to and otherwise modulate the activity of bromodomain-containing proteins, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders.

10. 发明授权

US10703746B2 Mutant IDH1 inhibitors useful for treating cancer 有权
公开(公告)号：US10703746B2
公开(公告)日：2020-07-07
申请号：US15538570
申请日：2015-12-22
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICE , THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL
发明人： Matthew Brian Boxer , Jason Matthew Rohde , Rajan Pragani , Li Liu , Mindy Irene Emily Davis , Kyle Ryan Brimacombe , Min Shen , Anton Simeonov , Surendra Karavadhi , Daniel Jason Urban , Ajit Jadhav , Xiaodong Wang , Andrew Louis McIver
IPC分类号： C07D417/04 , A61K31/4709 , A61K31/496 , A61K31/4439 , C07D417/14 , A61K31/4375 , C07D471/04 , A61K31/435 , A61K31/4545 , A61K31/551 , A61K31/437 , A61K31/5377 , A61K31/4704 , C07D215/54 , C07D401/04 , A61K31/506 , C07D215/227 , C07D491/048 , C07D213/82 , C07D487/10 , C07D451/02 , A61K31/46 , A61K31/499 , C07D413/14 , C07D215/22 , C07D491/052 , C07D401/14 , C07D491/107 , C07D487/08 , C07D413/04 , C07D471/14 , A61P35/00
摘要： Compounds of Formula I and Formula II and the pharmaceutically acceptable salts thereof are disclosed The variables A, B, Y, Z, X1, X2, R1-4 and R13-18 are disclosed herein. The compounds are useful for treating cancer disorders, especially those involving mutant IDH1 enzymes. Pharmaceutical compositions containing compounds of Formula I or Formula II and methods of treatment comprising administering compounds of Formula I and Formula II are also disclosed.

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