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公开(公告)号:US20240308986A1
公开(公告)日:2024-09-19
申请号:US18661960
申请日:2024-05-13
发明人: Chris MILLER
IPC分类号: C07D403/10 , A61P35/04 , C07D209/30 , C07D333/64 , C07D409/12 , C07D487/04 , C07D495/04
CPC分类号: C07D403/10 , A61P35/04 , C07D209/30 , C07D333/64 , C07D409/12 , C07D487/04 , C07D495/04
摘要: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
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公开(公告)号:US12071404B2
公开(公告)日:2024-08-27
申请号:US17506331
申请日:2021-10-20
申请人: UCB Pharma GmbH
发明人: Christa E. Mueller , Cécile Pegurier , Michael Louis Robert Deligny , Ali El-Tayeb , Joerg Hockemeyer , Marie Ledecq , Joël Mercier , Laurent Provins , Nader M. Boshta , Sanjay Bhattarai , Vigneshwaran Namasivayam , Mario Funke , Lukas Schwach , Sabrina Gollos , Daniel Von Laufenberg , Anaïs Barré
IPC分类号: C07D209/30 , C07D307/82 , C07D333/62 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D421/12 , C07D487/04 , C07D491/056
CPC分类号: C07D209/30 , C07D307/82 , C07D333/62 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D421/12 , C07D487/04 , C07D491/056
摘要: Disclosed are sulfonamide compounds with GPR17 modulating properties, which are useful for treating or preventing a variety of CNS and other diseases, in particular for preventing and treating myelinating diseases or disorders.
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公开(公告)号:US12065459B2
公开(公告)日:2024-08-20
申请号:US16672114
申请日:2019-11-01
发明人: Jason Allan Wiles , Venkat Rao Gadhachanda , Qiuping Wang , Godwin Pais , Akihiro Hashimoto , Dawei Chen , Xiangzhu Wang , Atul Agarwal , Milind Deshpande , Avinash S. Phadke
IPC分类号: C07F9/572 , A61K9/00 , A61K31/404 , A61K31/4045 , A61K31/407 , A61K31/4162 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/549 , A61K31/55 , A61K31/675 , A61K31/683 , C07B59/00 , C07D209/12 , C07D209/14 , C07D209/30 , C07D209/40 , C07D209/42 , C07D209/44 , C07D209/88 , C07D401/14 , C07D403/06 , C07D403/08 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/14 , C07D491/113 , C07D495/04 , C07D513/04 , C07F5/02 , C07F7/08 , C07F9/6558 , C07F9/6561
CPC分类号: C07F9/5728 , A61K9/0014 , A61K9/0019 , A61K9/0048 , A61K9/0053 , A61K31/404 , A61K31/4045 , A61K31/407 , A61K31/4162 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/549 , A61K31/55 , A61K31/675 , A61K31/683 , C07B59/002 , C07D209/12 , C07D209/14 , C07D209/30 , C07D209/40 , C07D209/42 , C07D209/44 , C07D209/88 , C07D401/14 , C07D403/06 , C07D403/08 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/14 , C07D491/113 , C07D495/04 , C07D513/04 , C07F5/025 , C07F5/027 , C07F7/0812 , C07F9/65583 , C07F9/6561 , C07F9/65616 , C07B2200/05
摘要: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.
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公开(公告)号:US11851428B2
公开(公告)日:2023-12-26
申请号:US17328814
申请日:2021-05-24
发明人: Craig W. Lindsley , Joshua M. Wieting , Kevin M. Mcgowan , Jerod S. Denton , Kentaro Yashiro , Haruto Kurata , Yoko Sekioka , Takahiro Mori , Yuzo Iwaki
IPC分类号: C07D213/36 , C07D231/12 , C07D249/08 , C07D401/04 , A61K31/454 , C07D471/04 , C07C255/57 , C07C317/28 , C07D209/30 , C07D213/89 , C07D231/56 , C07D235/16 , C07D237/24 , C07D239/47 , C07D249/18 , C07D257/04 , C07D265/36 , C07D271/10 , C07D285/14 , C07D295/04 , C07D513/04
CPC分类号: C07D471/04 , C07C255/57 , C07C317/28 , C07D209/30 , C07D213/89 , C07D231/56 , C07D235/16 , C07D237/24 , C07D239/47 , C07D249/08 , C07D249/18 , C07D257/04 , C07D265/36 , C07D271/10 , C07D285/14 , C07D295/04 , C07D401/04 , C07D513/04
摘要: Disclosed is a compound of formula (I):
wherein all symbols are defined in the description. Also disclosed are pharmaceutical compositions comprising the compounds, methods of making the compounds, kits comprising the compounds, and methods of using the compounds, compositions and kits for treatment of disorders associated with TREK-1, TREK-2 or both TREK-1 and TREK-2 dysfunction in a mammal.-
公开(公告)号:US20230285598A1
公开(公告)日:2023-09-14
申请号:US17416180
申请日:2019-12-20
发明人: Laura EDGINGTON-MITCHELL , Simon MOUNTFORD , Bethany M. ANDERSON , Monika SZABO , Luigi AURELIO , Philip THOMPSON
IPC分类号: A61K49/00 , C07D209/30 , G01N33/58
CPC分类号: A61K49/0052 , C07D209/30 , G01N33/582 , G01N2333/96466
摘要: The present invention relates to compounds of formula I bearing a sulfoxoniumylide moiety as warhead, or salts thereof. Such compounds can be used as activity-based probes for cysteine proteases such as cathepsin X, in methods of detecting cysteine protease activity and in related diagnostic or therapeutic methods.
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公开(公告)号:US20190241517A1
公开(公告)日:2019-08-08
申请号:US15569221
申请日:2016-10-09
IPC分类号: C07D209/30
CPC分类号: C07D209/30
摘要: The invention discloses a method for the preparation of N-omega-(1,2-dimethylindole-3-sulfonyl)-L-arginine and its derivatives using L-ornithine.
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公开(公告)号:US20180258075A1
公开(公告)日:2018-09-13
申请号:US15760697
申请日:2016-09-12
发明人: Phillip M. Cowley , Yongxin Han
IPC分类号: C07D403/12 , A61K31/4155 , A61K45/06
CPC分类号: C07D403/12 , A61K31/404 , A61K31/4155 , C07D209/30 , A61K2300/00
摘要: Provided is a compound having formula (I): wherein R2 is selected from —C1, —Br and —CN; R1 and R4 are independently selected from H and —F; R631, R632, R641 and R642 are independently selected from —H, —F and substituted or unsubstituted C1-C3 alkyl groups; and R651 and R652 are independently selected from H and substituted or unsubstituted C1-C3 alkyl groups and substituted or unsubstituted phenyl groups; and wherein at least one of R631, R632, R641, R642 and R652 is not —H, or wherein when all of R631, R632, R641, R642 and R652 are —H, R651 is not Me or Et.
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公开(公告)号:US10005802B2
公开(公告)日:2018-06-26
申请号:US15245712
申请日:2016-08-24
发明人: Jason Allan Wiles , Avinash S. Phadke , Milind Deshpande , Atul Agarwal , Dawei Chen , Venkat Rao Gadhachanda , Akihiro Hashimoto , Godwin Pais , Qiuping Wang , Xiangzhu Wang
IPC分类号: C07D209/42 , C07D403/12 , C07D401/14 , C07D471/04 , C07D487/04 , C07D405/14 , C07F9/572 , C07D403/14 , C07D417/06 , C07D403/06 , C07D417/14 , C07F7/08 , C07D413/14 , C07D403/08 , C07D413/06 , C07F5/02 , C07F9/6561 , C07F9/6558 , A61K31/404 , A61K31/407 , A61K31/4162 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/437 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/549 , A61K31/55 , A61K31/675 , A61K31/683 , C07B59/00 , C07D209/14 , C07D209/40 , C07D405/12 , C07D417/12 , C07D487/14 , C07D491/113 , C07D495/04 , C07D513/04
CPC分类号: C07F9/5728 , A61K9/0014 , A61K9/0019 , A61K9/0048 , A61K9/0053 , A61K31/404 , A61K31/4045 , A61K31/407 , A61K31/4162 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/549 , A61K31/55 , A61K31/675 , A61K31/683 , C07B59/002 , C07B2200/05 , C07D209/12 , C07D209/14 , C07D209/30 , C07D209/40 , C07D209/42 , C07D209/44 , C07D209/88 , C07D401/14 , C07D403/06 , C07D403/08 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/14 , C07D491/113 , C07D495/04 , C07D513/04 , C07F5/025 , C07F5/027 , C07F7/0812 , C07F9/65583 , C07F9/6561 , C07F9/65616
摘要: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof, wherein R12 or R13 on the A group is an amide substituent (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade in the alternative complement pathway. The inhibitors of factor D described herein reduce the excessive activation of complement.
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公开(公告)号:US20180155286A1
公开(公告)日:2018-06-07
申请号:US15798545
申请日:2017-10-31
发明人: Snezna ROGELJ , Liliya FROLOVA , Alexander KORNIENKO , Leslie D. EDWARDS , Cody CHAMPION , Kailee ZINGLER , Danielle Nicole Turner
IPC分类号: C07D209/42 , C07D209/40 , A61K31/404 , C07D209/30 , C07D209/10 , A61K41/00 , A61K38/14 , A61K38/12 , A61K31/7048 , A61K31/7036 , A61K31/655 , A61K31/65 , A61K31/496 , A61K31/431 , A61K31/43 , C07D209/36
CPC分类号: C07D209/42 , A61K31/404 , A61K31/43 , A61K31/431 , A61K31/496 , A61K31/65 , A61K31/655 , A61K31/7036 , A61K31/7048 , A61K38/12 , A61K38/14 , A61K41/0057 , A61P31/00 , C07D209/10 , C07D209/30 , C07D209/36 , C07D209/40 , Y02A50/473 , A61K2300/00
摘要: The present disclosure describes a method to treat conditions, including bacterial infections and cancer, using a photosensitive compound that, upon exposure to white light, can be activated. The photosensitive compound can also interact synergistically with antibiotics used concomitantly to kill drug-resistant bacteria. The photosensitive compounds can also be used to inhibit the proliferation of cancer cells.
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公开(公告)号:US20180072762A1
公开(公告)日:2018-03-15
申请号:US15818559
申请日:2017-11-20
发明人: Jason Allan Wiles , Godwin Pais , Akihiro Hashimoto , Venkat Rao Gadhachanda , Qiuping Wang , Dawei Chen , Xiangzhu Wang , Atul Agarwal , Milind Deshpande , Avinash S. Phadke
IPC分类号: C07F9/572 , A61K31/404 , C07F9/6558 , C07F9/6561 , C07F7/08 , C07F5/02 , C07D513/04 , C07D495/04 , C07D491/113 , C07D487/14 , C07D487/04 , C07D471/04 , C07D417/14 , C07D417/12 , C07D417/06 , C07D413/14 , C07D413/06 , C07D405/14 , C07D405/12 , C07D403/14 , C07D403/12 , C07D403/08 , C07D403/06 , C07D401/14 , C07D209/42 , C07D209/40 , C07D209/14 , C07B59/00 , A61K31/683 , A61K31/675 , A61K31/55 , A61K31/549 , A61K31/506 , A61K31/496 , A61K31/4709 , A61K31/4439 , A61K31/437 , A61K31/4192 , A61K31/4188 , A61K31/4184 , A61K31/4178 , A61K31/4162 , A61K31/407
CPC分类号: C07F9/5728 , A61K9/0014 , A61K9/0019 , A61K9/0048 , A61K9/0053 , A61K31/404 , A61K31/4045 , A61K31/407 , A61K31/4162 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/549 , A61K31/55 , A61K31/675 , A61K31/683 , C07B59/002 , C07B2200/05 , C07D209/12 , C07D209/14 , C07D209/30 , C07D209/40 , C07D209/42 , C07D209/44 , C07D209/88 , C07D401/14 , C07D403/06 , C07D403/08 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/14 , C07D491/113 , C07D495/04 , C07D513/04 , C07F5/025 , C07F5/027 , C07F7/0812 , C07F9/65583 , C07F9/6561 , C07F9/65616
摘要: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof, wherein R12 or R13 on the A group is an alkyne (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.
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