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1. 发明申请

WO2018078005A1 AMIDO-SUBSTITUTED AZASPIRO DERIVATIVES AS TANKYRASE INHIBITORS 审中-公开
标题翻译： AMIDO取代的AZASPIRO衍生物作为TANKYRASE抑制剂
公开(公告)号：WO2018078005A1
公开(公告)日：2018-05-03
申请号：PCT/EP2017/077420
申请日：2017-10-26
申请人： BAYER PHARMA AKTIENGESELLSCHAFT
发明人： BUCHGRABER, Philipp , EIS, Knut , WAGNER, Sarah , SÜLZLE, Detlev , VON NUSSBAUM, Franz , BENDER, Eckhard , LI, Volkhart, Min-Jian , LIU, Ningshu , SIEGEL, Franziska , LIENAU, Philipp
IPC分类号： C07D403/12 , A61K31/4025 , A61K31/4155 , A61K31/4164 , A61K31/4184 , A61K31/4192 , A61K31/4196 , A61K31/422 , A61K31/429 , A61K31/437 , A61K31/4375 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/4725 , A61K31/497 , A61K31/498 , A61K31/501 , A61K31/506 , A61K31/517 , A61K31/519 , C07D219/12 , C07D401/04 , C07D401/12 , C07D405/12 , C07D407/12 , C07D413/12 , C07D417/04 , C07D471/04 , C07D487/04 , C07D513/04
CPC分类号： C07D403/12 , A61K31/4025 , A61K31/403 , A61K31/4155 , A61K31/4164 , A61K31/4184 , A61K31/4192 , A61K31/4196 , A61K31/422 , A61K31/423 , A61K31/427 , A61K31/429 , A61K31/437 , A61K31/4375 , A61K31/4439 , A61K31/4709 , A61K31/497 , A61K31/498 , A61K31/501 , A61K31/506 , A61K31/519 , A61K45/06 , C07D219/12 , C07D401/04 , C07D401/12 , C07D405/12 , C07D407/12 , C07D413/12 , C07D417/04 , C07D471/04 , C07D487/04 , C07D513/04 , A61K2300/00
摘要： The present invention relates to amido-substituted cyclohexane compounds of general formula (I) : in which A, R 4 , R 6 , R 7 , R 8 , R 9 , R 10 and R 11 are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.
摘要翻译：本发明涉及通式（I）的酰氨基取代的环己烷化合物：其中A，R 4，R 6，R R 8，R 9，R 10和R 11的取代基为本文定义的化合物，制备所述化合物的方法，可用于制备所述化合物的中间体化合物，包含所述化合物的药物组合物和组合以及所述化合物用于制备用于治疗或预防疾病的药物组合物的用途，特别是的肿瘤，作为单独的药物或与其他活性成分组合。

2. 发明申请

WO02008193A2 THERAPEUTIC ACRIDONE AND ACRIDINE COMPOUNDS 审中-公开
标题翻译：治疗阿司匹林和阿司匹林化合物
公开(公告)号：WO02008193A2
公开(公告)日：2002-01-31
申请号：PCT/GB2001/003046
申请日：2001-07-06
IPC分类号： A61K31/473 , A61K31/496 , A61K31/5377 , A61K31/55 , A61P35/00 , C07D219/06 , C07D219/08 , C07D219/10 , C07D219/12 , C07D401/12 , C07D219/00
CPC分类号： C07D219/08 , C07D219/06 , C07D219/10
摘要： The present invention pertains to acridone and acridine compounds of formula (I), wherein either: (a) K is =O, L is -H, alpha is a single bond, beta is a double bond, gamma is a single bond (acridones); or, (b) K is a 9-substituent, L is absent, alpha is a double bond, beta is a single bond, gamma is a double bond (acridines); and wherein: J is a 2- or 3-substituent; J is a 6- or 7-substituent; J and J are each independently a group of the formula -NHCO(CH2)nNR R , wherein: n is an integer from 1 to 5; and, R and R are independently hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, or R and R , taken together with the nitrogen atom to which they are attached, form a heterocyclic ring having from 3 to 8 ring atoms; and wherein, when K is a 9-substituent, K is a group of the formula -N(R )Q, wherein: R is an amino substituent and is hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl; and, Q is C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, and is optionally substituted; and pharmaceutically acceptable salts, esters, amides, solvates, hydrates, and protected forms thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo , to inhibit telomerase, to regulate cell prol iferation, and in the treatment of proliferative conditions, such as cancer.
摘要翻译：本发明涉及式（I）的吖啶酮和吖啶化合物，其中：（a）K是= O，L是-H，α是单键，β是双键，γ是单键（吖啶酮）; 或（b）K是9取代基，L不存在，α是双键，β是单键，γ是双键（吖啶）; 并且其中：J 1是2-或3-取代基; J 2是6-或7-取代基; J 1和J 2各自独立地是式-NHCO（CH 2）n NRR R 2的基团，其中：n是1至5的整数; 和R 1和R 2独立地是氢，C 1-7烷基，C 3-20杂环基或C 5-20芳基，或R 1和R 2与它们所连接的氮原子一起形成具有3至8个环原子的杂环; 并且其中当K是9-取代基时，K是式-N（R N）Q的基团，其中：R N是氨基取代基并且是氢，C 1-7烷基，C 3-20杂环基，或C5-20芳基; 且Q为C 1-7烷基，C 3-20杂环基或C 5-20芳基，并且任选被取代; 和其药学上可接受的盐，酯，酰胺，溶剂合物，水合物及其保护形式。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内均用于抑制端粒酶的调控，以调节细胞细胞治疗增生性疾病如癌症。

3. 发明申请

WO2021142065A1 ACRIDIN-9-YL-AMINE, QUINOLIN-9-YL-AMINE, 1 -AMINO-9H-THIOXANTHENE-9-ONE AND BENZO[B][1,5]NAPHTHYRI DIN-10-YL-AMINE DERIVATIVES AS AUTOPHAGY INHIBITORS FOR TREATING CANCER 审中-公开
公开(公告)号：WO2021142065A1
公开(公告)日：2021-07-15
申请号：PCT/US2021/012424
申请日：2021-01-07
申请人： REYOUNG CORPORATION , REYOUNG DRUG DISCOVERY CO., LTD.
发明人： HOU, Frank Shujie , XUE, Jian , ZHAO, Yushan , MIAO, Dezu
IPC分类号： C07D401/14 , C07D401/12 , C07D409/14 , C07D409/12 , C07D471/04 , C07D219/12 , C07D221/08 , A61K31/473 , A61K31/4709 , A61K31/496 , A61K31/4745 , A61K31/382 , A61K31/444 , A61K31/4192 , A61P35/00 , A61P35/02 , A61P35/04
摘要： This disclosure provides a cridin-9-yl-amine, quinolin-9-yl-amine, 1- amino-9H-thioxanthene-9-one and benzo[b][l,5]naphthyridin-10- yl-amine derivatives and structurally related compounds for use as autophagy inhibitors for treating cancer. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 77 to 155; examples 1 to 22; compound A; compounds 1 to 21; tables 1 to 3).

4. 发明申请

WO0208193A3 THERAPEUTIC ACRIDONE AND ACRIDINE COMPOUNDS 审中-公开
标题翻译：治疗阿司匹林和阿司匹林化合物
公开(公告)号：WO0208193A3
公开(公告)日：2003-10-02
申请号：PCT/GB0103046
申请日：2001-07-06
申请人： CANCER REC TECH LTD , NEIDLE STEPHEN , HARRISON RICHARD JOHN , KELLAND LLOYD ROYSTON , GOWAN SHARON MICHELE , READ MARTIN , RESZKA TONY
发明人： NEIDLE STEPHEN , HARRISON RICHARD JOHN , KELLAND LLOYD ROYSTON , GOWAN SHARON MICHELE , READ MARTIN , RESZKA TONY
IPC分类号： A61K31/473 , A61K31/496 , A61K31/5377 , A61K31/55 , A61P35/00 , C07D219/06 , C07D219/08 , C07D219/10 , C07D219/12 , C07D401/12
CPC分类号： C07D219/08 , C07D219/06 , C07D219/10
摘要： The present invention pertains to acridone and acridine compounds of formula (I), wherein either: (a) K is =O, L is -H, alpha is a single bond, beta is a double bond, gamma is a single bond (acridones); or, (b) K is a 9-substituent, L is absent, alpha is a double bond, beta is a single bond, gamma is a double bond (acridines); and wherein: J is a 2- or 3-substituent; J is a 6- or 7-substituent; J and J are each independently a group of the formula -NHCO(CH2)nNR R , wherein: n is an integer from 1 to 5; and, R and R are independently hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, or R and R , taken together with the nitrogen atom to which they are attached, form a heterocyclic ring having from 3 to 8 ring atoms; and wherein, when K is a 9-substituent, K is a group of the formula -N(R )Q, wherein: R is an amino substituent and is hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl; and, Q is C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, and is optionally substituted; and pharmaceutically acceptable salts, esters, amides, solvates, hydrates, and protected forms thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit telomerase, to regulate cell prol iferation, and in the treatment of proliferative conditions, such as cancer.
摘要翻译：本发明涉及式（I）的吖啶酮和吖啶化合物，其中：（a）K是= O，L是-H，α是单键，β是双键，γ是单键（吖啶酮）; 或（b）K是9取代基，L不存在，α是双键，β是单键，γ是双键（吖啶）; 并且其中：J 1是2-或3-取代基; J 2是6-或7-取代基; J 1和J 2各自独立地是式-NHCO（CH 2）n NRR R 2的基团，其中：n是1至5的整数; 和R 1和R 2独立地是氢，C 1-7烷基，C 3-20杂环基或C 5-20芳基，或R 1和R 2与它们所连接的氮原子一起形成具有3至8个环原子的杂环; 并且其中当K是9-取代基时，K是式-N（R N）Q的基团，其中：R N是氨基取代基并且是氢，C 1-7烷基，C 3-20杂环基，或C5-20芳基; 且Q为C 1-7烷基，C 3-20杂环基或C 5-20芳基，并且任选被取代; 和其药学上可接受的盐，酯，酰胺，溶剂合物，水合物及其保护形式。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制端粒酶，调节细胞增殖和治疗增殖性疾病如癌症。

5. 发明申请

WO00076982A1 ANTAGONISM OF IMMUNOSTIMULATORY CPG-OLIGONUCLEOTIDES BY 4-AMINOQUINOLINES AND OTHER WEAK BASES 审中-公开
标题翻译： 4-氨基喹啉和其他弱碱对免疫抑制剂CPG-寡核苷酸的拮抗作用
公开(公告)号：WO00076982A1
公开(公告)日：2000-12-21
申请号：PCT/US2000/016723
申请日：2000-06-16
IPC分类号： A61K31/47 , A61K31/4706 , A61K31/4709 , A61K31/473 , A61K31/496 , A61K31/5377 , A61P37/06 , C07D215/22 , C07D215/233 , C07D215/42 , C07D215/44 , C07D215/46 , C07D219/12 , C07D401/12 , C07D409/12
CPC分类号： C07D215/233 , A61K31/47 , A61K31/4706 , A61K31/4709 , A61K31/473 , A61K31/496 , A61K31/5377 , C07D215/42 , C07D215/44 , C07D215/46 , C07D219/12 , C07D401/12 , C07D409/12
摘要： The present invention relates generally to the field of immunology. More particularly it concerns compositions and methods for inhibiting stimulation of the immune system. The compounds and methods comprise compounds that are analogs and derivatives of chloroquine, such as 4-aminoquinolines, and other weak bases. They can be used in preventative and therapeutic treatments of autoimmune diseases and phenomena, transplant rejection such as host-versus-graft disease, and sepsis.
摘要翻译：本发明一般涉及免疫学领域。更具体地，涉及用于抑制免疫系统刺激的组合物和方法。化合物和方法包括氯喹的类似物和衍生物如4-氨基喹啉和其它弱碱的化合物。它们可用于预防和治疗自身免疫性疾病和现象，移植排斥反应如宿主与移植物疾病和败血症。

6. 发明申请

WO00007591A1 INDOLE sPLA2 INHIBITORS 审中-公开
标题翻译： INDOLE sPLA2抑制剂
公开(公告)号：WO00007591A1
公开(公告)日：2000-02-17
申请号：PCT/US1999/017460
申请日：1999-08-02
IPC分类号： A61K31/405 , A61K31/403 , A61K31/404 , A61P1/18 , A61P7/00 , A61P9/10 , A61P11/00 , A61P19/02 , A61P19/06 , A61P27/16 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/08 , A61P43/00 , C07D209/18 , C07D209/22 , C07D231/12 , C07D233/54 , C07D233/56 , C07D233/58 , C07D249/08 , A61K31/335 , A61K31/38 , A61K31/395 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/535 , C07D205/02 , C07D209/04 , C07D209/12 , C07D209/14 , C07D209/82 , C07D211/26 , C07D211/30 , C07D211/86 , C07D213/36 , C07D213/50 , C07D213/56 , C07D215/12 , C07D219/12 , C07D231/54 , C07D231/56 , C07D237/30 , C07D239/26 , C07D241/04 , C07D241/42 , C07D249/04 , C07D251/22 , C07D261/08 , C07D263/32 , C07D275/02 , C07D277/02 , C07D285/04 , C07D285/06 , C07D285/08 , C07D285/10 , C07D285/12 , C07D317/26 , C07D317/28 , C07D319/12 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14
CPC分类号： C07D209/18 , C07D209/22
摘要： A class of novel acylsulfonamide substituted indole compounds is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of inflammatory diseases such as septic shock.
摘要翻译：公开了一类新的酰基磺酰胺取代的吲哚化合物以及这些化合物用于抑制sPLA2介导的脂肪酸释放以治疗炎症性疾病如败血性休克的用途。

7. 发明申请

WO1993016996A1 INDOLE DERIVATIVES AS TESTOSTERONE-5-ALPHA-REDUCTASE INHIBITORS 审中-公开
标题翻译：作为TESTOSTERONE-5-ALPHA-REDUCTASE抑制剂的吲哚衍生物
公开(公告)号：WO1993016996A1
公开(公告)日：1993-09-02
申请号：PCT/JP1993000201
申请日：1993-02-18
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , OKADA, Satoshi , SAWADA, Kozo , KURODA, Akio , WATANABE Shinya , TANAKA, Hirokazu
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07D219/12
CPC分类号： C07D209/12
摘要： A compound of formula (I), wherein R is carboxy or protected carboxy, R is hydrogen, lower alkyl or halogen, R is aryl which may have suitable substituent(s), A is lower alkylene, X is methylene, -O- or -NH-, and Y is lower alkylene substituted by lower alkoxy, lower alkenylene or lower alkynylene; or Y-R is alkyl, and a pharmaceutically acceptable salt thereof. The compound of the present invention is useful as a testosteron 5 alpha -reductase inhibitor and effective to testosteron 5 alpha -reductase mediated diseases such as prostatism, prostatic hypertrophy, prostatic cancer, alopecia, hirsutism (e.g. female hirsutism, etc.), androgenic alopecia (or malepattern baldness), acne (e.g. acne vulgaris, pimple, etc.), other hyperandrogenism, and the like.
摘要翻译：式（I）化合物，其中R 1为羧基或被保护的羧基，R 2为氢，低级烷基或卤素，R 3为可具有合适取代基的芳基，A为低级亚烷基，X为亚甲基，-O-或-NH-，Y为被低级烷氧基，低级亚烯基或低级亚炔基取代的低级亚烷基; 或Y-R 3为烷基，及其药学上可接受的盐。本发明的化合物可用作睾丸激素5α-还原酶抑制剂，并且对睾酮5α-还原酶介导的疾病如前列腺增生，前列腺肥大，前列腺癌，脱发，多毛症（例如雌性多毛症等）有效，雄激素性脱发（或恶病质秃发），痤疮（例如寻常痤疮，疙瘩等），其他雄激素过多症等。

8. 发明申请

WO2022250971A1 SMALL MOLECULE INHIBITORS OF AUTOPHAGY AND HISTONE DEACTYLASES AND USES THEREOF 审中-公开
公开(公告)号：WO2022250971A1
公开(公告)日：2022-12-01
申请号：PCT/US2022/028970
申请日：2022-05-12
申请人： ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA
发明人： CAREW, Jennifer , NAWROCKI, Steffan , WANG, Wei
IPC分类号： A61K31/473 , C07D219/10 , C07D219/12 , A61P31/12
摘要： This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a tetrahydroacridine (or similar) structure, an acridine (or similar) structure, a benzonaphthyridine (or similar) structure, or a tetrahydrobenzonaphthyridine (or similar) structure which function as autophagy inhibitors and/or histone deactylase inhibitors, and their use as therapeutics for the treatment of conditions characterized with aberrant autophagy activity and/or aberrant HDAC activity (e.g., cancer, pulmonary hypertension, diabetes, neurodegenerative disorders, aging, heart disease, rheumatoid arthritis, infectious diseases, conditions and symptoms caused by a viral infection (e.g., COVID-19)).

9. 发明申请

WO2008010984A3 ACRIDINE ACTIVATION OF P53 AND USES THEREOF 审中-公开
标题翻译： ACRIDINE激活P53及其用途
公开(公告)号：WO2008010984A3
公开(公告)日：2008-08-14
申请号：PCT/US2007016122
申请日：2007-07-16
申请人： UNIV PENNSYLVANIA , EL-DEIRY WAFIK S
发明人： EL-DEIRY WAFIK S
IPC分类号： C07D413/12 , A61K31/473 , A61K31/496 , A61K31/5355 , C07D219/12 , C07D401/12 , C07D403/12
CPC分类号： A61K31/5377 , A61K9/0019 , A61K31/473 , A61K31/496 , A61K31/5355 , C07D219/12
摘要： This invention relates to the stabilization of p53 in cells, thereby inducing eitrher cell cycle arrest or apoptosis or both and the consequence of such stabilization on the treatment of cancer. Specifically, the use of acridine and its derivatives in stabilizing p53 through blockage of its ubiquitation, thereby inducing cell cycle arrest or apoptosis in a cell; and the use of these compounds in the treatment of cancer.
摘要翻译：本发明涉及细胞中p53的稳定化，由此诱导细胞周期阻滞或细胞凋亡或两者，以及这种稳定化对癌症治疗的结果。具体而言，吖啶及其衍生物通过阻断其泛素化来稳定p53，从而诱导细胞中的细胞周期停滞或凋亡; 以及这些化合物在治疗癌症中的用途。

10. 发明申请

WO03039488A3 A METHOD FOR TREATING INFLAMMATORY BOWEL DISEASE 审中-公开
标题翻译：一种治疗炎性肠病的方法
公开(公告)号：WO03039488A3
公开(公告)日：2003-07-17
申请号：PCT/US0236354
申请日：2002-11-12
申请人： CHAROUS LAUREN
发明人： CHAROUS LAUREN
IPC分类号： C07D215/40 , A61K9/00 , A61K9/22 , A61K9/48 , A61K9/52 , A61K31/136 , A61K31/47 , A61K31/4706 , A61K31/4709 , A61K31/473 , A61K45/00 , A61P1/04 , C07D215/46 , C07D219/12 , C07D401/06 , A61K31/675 , A01N25/00 , A61K31/66
CPC分类号： A61K31/47 , A61K9/0004 , A61K9/4808 , A61K31/4706
摘要： The present invention is directed to a method for treating inflammatory bowel disease in a patient comprising administering to said patient a pharmaceutical compositions comprising a pharmaceutically effective amount of an anti-malarial compound in association with a pharmaceutically acceptable carrier and/or excipient that delays and targets the release of the anti-malarial compound in the gastrointestinal tract of the patient. It is also directed to the pharmaceutical composition comprising a pharmaceutically effective amount of the anti-malarial compound in association with a pharmaceutically acceptable carrier or excipient that delays and target the release of the anti-malarial compound in the gastrointestinal tract.
摘要翻译：本发明涉及治疗患者的炎性肠病的方法，其包括向所述患者施用药物组合物，所述药物组合物包含药学有效量的抗疟疾化合物以及延迟和靶向的药学可接受的载体和/或赋形剂抗疟疾化合物在患者胃肠道中的释放。本发明还涉及药物组合物，其包含药学有效量的抗疟疾化合物以及延迟和靶向抗疟疾化合物在胃肠道中的释放的药学上可接受的载体或赋形剂。

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