公开(公告)号：US20230331718A1

公开(公告)日：2023-10-19

申请号：US18162085

申请日：2023-01-31

Applicant: Skyhawk Therapeutics, Inc.

Inventor： Michael Luzzio ,  Brian Lucas ,  Tiansheng Wang

IPC: C07D451/04 ,  C07D498/08 ,  C07D453/06

CPC classification number: C07D451/04 ,  C07D453/06 ,  C07D498/08 ,  C07B2200/05

Abstract: Described herein are small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, and methods of use of the small molecule splicing modulator compounds for modulating splicing and treating diseases and conditions.

公开(公告)号：US20200009090A1

公开(公告)日：2020-01-09

申请号：US16511577

申请日：2019-07-15

Applicant: The University of Melbourne

Inventor： Paul Stephen DONNELLY ,  Stacey Erin RUDD ,  Spencer John WILLIAMS

IPC: A61K31/18 ,  C07K17/06 ,  A61K51/10 ,  C07C259/06 ,  C07C309/14 ,  C07C311/19 ,  C07C311/29 ,  C07C311/42 ,  C07C311/46 ,  C07D207/48 ,  C07D211/60 ,  C07D211/96 ,  C07D213/42 ,  C07D213/74 ,  C07D213/89 ,  C07D215/36 ,  C07D223/06 ,  C07D277/06 ,  C07D277/80 ,  C07D279/12 ,  C07D295/13 ,  C07D309/06 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D453/06 ,  C07D471/08 ,  C07D487/08 ,  C07C323/60

Abstract: The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours.

公开(公告)号：US09266904B2

公开(公告)日：2016-02-23

申请号：US14279716

申请日：2014-05-16

Applicant: Hoffmann-La Roche Inc.

Inventor： Lei Guo ,  Taishan Hu ,  Yimin Hu ,  Buelent Kocer ,  Buyu Kou ,  Gangqin Li ,  Xianfeng Lin ,  Haixia Liu ,  Hong Shen ,  Houguang Shi ,  Guolong Wu ,  Zhisen Zhang ,  Mingwei Zhou ,  Wei Zhu

IPC: A61K31/506 ,  C07D498/08 ,  C07D417/14 ,  C07D498/18 ,  C07D491/08 ,  C07D487/08 ,  C07D513/08 ,  C07D498/20 ,  C07D453/06 ,  C07D471/08 ,  C07D491/18

CPC classification number: C07D498/18 ,  A61K31/506 ,  C07D417/14 ,  C07D453/06 ,  C07D471/08 ,  C07D487/08 ,  C07D491/08 ,  C07D491/18 ,  C07D498/08 ,  C07D498/20 ,  C07D513/08

Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as or pharmaceutically acceptable salts, or tautomerism isomers, or enantiomers, or diastereomers thereof. The invention also contains compositions including the compounds and methods of using the compounds.

Abstract translation: 本发明提供具有以下通式的新化合物：其中R 1，R 2，R 3和R 4如说明书和权利要求书中所定义，以及其药学上可接受的盐或互变异构体异构体或其对映异构体或非对映异构体。 本发明还包含包含化合物的组合物和使用该化合物的方法。

公开(公告)号：US07705152B2

公开(公告)日：2010-04-27

申请号：US11943836

申请日：2007-11-21

Applicant: Yoshiharu Iwabuchi ,  Masatoshi Shibuya ,  Masaki Tomizawa

Inventor： Yoshiharu Iwabuchi ,  Masatoshi Shibuya ,  Masaki Tomizawa

IPC: C07D453/06

CPC classification number: C07D453/06 ,  C07C45/30 ,  C07C2601/14 ,  C07D487/04 ,  C07D493/20 ,  C07C47/228 ,  C07C49/657 ,  C07C49/603 ,  C07C49/76 ,  C07C49/04

Abstract: An alcohol oxidation catalyst which is an organic oxidation catalyst to oxidize an alcohol, which contains azabicyclo[3.3.1]nonane N-oxyl represented by the following formula (1) having an N-oxyl group incorporated in a bicycle[3.3.1]nonane skeleton: wherein X is H2, O or NOH.

Abstract translation: 作为氧化醇的有机氧化催化剂的醇氧化催化剂，其含有结合在自行车中的具有N-氧基的由下式（1）表示的氮杂双环[3.3.1]壬烷N-氧基[3.3.1] 壬烷骨架：其中X是H 2，O或NOH。

公开(公告)号：US20080234316A1

公开(公告)日：2008-09-25

申请号：US11970698

申请日：2008-01-08

Applicant: Maria QUINONES

Inventor： Maria QUINONES

IPC: A61K31/439 ,  A61P11/00 ,  C07D453/06

CPC classification number: C07D487/08 ,  C07D453/02

Abstract: New quinuclidine amide derivatives having the chemical structure of general formula (I) and pharmaceutically acceptable salts thereof including quaternary salts of formula (II) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as antagonists of M3 muscarinic receptors.

Abstract translation: 公开了具有通式（I）的化学结构的新的奎宁环酰胺衍生物及其药学上可接受的盐，包括式（II）的季盐; 以及其制备方法，包含它们的药物组合物及其在治疗中作为M3毒蕈碱受体的拮抗剂的用途。

公开(公告)号：US20050009808A1

公开(公告)日：2005-01-13

申请号：US10495370

申请日：2002-11-13

Applicant: Takuya Hiruma ,  Koji Kobayashi ,  Shinji Inomata

Inventor： Takuya Hiruma ,  Koji Kobayashi ,  Shinji Inomata

IPC: A61K8/49 ,  A61K31/403 ,  A61K31/439 ,  A61K31/4439 ,  A61K31/55 ,  A61P1/02 ,  A61P1/04 ,  A61P17/00 ,  A61P17/16 ,  A61P19/02 ,  A61P19/04 ,  A61P19/08 ,  A61P19/10 ,  A61P25/00 ,  A61P27/02 ,  A61P29/00 ,  A61P35/04 ,  A61P43/00 ,  A61Q19/00 ,  A61Q19/08 ,  C07D209/52 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D405/14 ,  C07D451/06 ,  C07D453/06 ,  C07D471/08 ,  C07D453/02 ,  A61K31/4745

CPC classification number: A61Q19/08 ,  A61K8/0212 ,  A61K8/492 ,  A61K31/403 ,  A61K31/439 ,  A61K31/4439 ,  A61K31/55 ,  A61K2800/782 ,  A61Q1/02 ,  A61Q19/00 ,  C07D209/52 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D405/14 ,  C07D451/06 ,  C07D453/06 ,  C07D471/08

Abstract: An azabicyclo compound (I) or a salt thereof in accordance with the present invention has an excellent inhibiting action on matrix metalloproteases (MMPs) activity, and is useful for pharmaceutical, cosmetic and skin external compositions. wherein R is H, alkyl, heteroalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, acyl, COOR1, carbamoyl or SO2R2 (wherein R1 and R2 each are alkyl, heteroalkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl); X is methylene, ethylene or propylene; and is a single bond or a double bond.

Abstract translation: 根据本发明的氮杂二环化合物（I）或其盐对基质金属蛋白酶（MMPs）活性具有优异的抑制作用，并且可用于药物，化妆品和皮肤外用组合物。 其中R是H，烷基，杂烷基，芳基，杂芳基，芳基烷基，杂芳基烷基，酰基，COOR 1，氨基甲酰基或SO 2 R 2（其中R 1和R 2各自是烷基，杂烷基，芳基，杂芳基 ，芳基烷基或杂芳基烷基）; X是亚甲基，亚乙基或亚丙基; 并且是单键或双键。

公开(公告)号：US6156752A

公开(公告)日：2000-12-05

申请号：US133580

申请日：1998-08-13

Applicant: Takafumi Ikeda ,  Mitsuhiro Kawamura ,  Yu-Ting Ge

Inventor： Takafumi Ikeda ,  Mitsuhiro Kawamura ,  Yu-Ting Ge

IPC: C07D487/04 ,  A61K31/4427 ,  A61K31/455 ,  A61K31/55 ,  A61P1/00 ,  A61P3/08 ,  A61P9/00 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P17/00 ,  A61P25/04 ,  A61P25/28 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P35/00 ,  A61P37/08 ,  A61P43/00 ,  C07D211/90 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D451/02 ,  C07D451/04 ,  C07D453/02 ,  C07D453/06 ,  A61K31/497

CPC classification number: C07D451/04 ,  C07D211/90 ,  C07D401/06 ,  C07D401/12 ,  C07D453/06

Abstract: This invention provides a compound of the formula (I): ##STR1## and its pharmaceutically acceptable salts, wherein A.sup.1 and A.sup.2 are each halo; R.sup.1 and R.sup.2 are independently C.sub.1-4 alkyl; R.sup.3 is substituted or unsubstituted, phenyl or naphthyl; Y is heterocyclic group selected from C.sub.5-10 azacycloalkyl, C.sub.6-10 diazacycloalkyl, C.sub.7-10 azabicycloalkyl and the like; and R.sup.4 is selected from (a) substituted or unsubstituted C.sub.1-8 alkyll; (b) substituted or unsubstituted amino; (c) substituted or unsubstituted C.sub.2-6 alkanoyl; (d) substituted or unsubstituted C.sub.3-8 cycloalkyl or C.sub.7-14 bicycloalkyl; (e) substituted or unsubstituted C.sub.5-10 azacycloalkyl or C.sub.6-10 diazacycloalkyl, and (f) substituted or unsubstituted C.sub.7-14 mono- or di-azabicycloalkyl. These compounds are useful for the treatment of medical conditions caused by bradykinin such as inflammation, cardiovascular disease, pain, etc. This invention also provides a pharmaceutical composition comprising the above compound, and intermediates of the above compounds.

Abstract translation: 本发明提供式（I）化合物及其药学上可接受的盐，其中A1和A2各自为卤素; R1和R2独立地为C1-4烷基; R3是取代或未取代的，苯基或萘基; Y是选自C5-10氮杂环烷基，C6-10二氮杂环烷基，C7-10氮杂双环烷基等的杂环基; 并且R 4选自（a）取代或未取代的C 1-8烷基; （b）取代或未取代的氨基; （c）取代或未取代的C 2-6烷酰基; （d）取代或未取代的C 3-8环烷基或C 7-14双环烷基; （e）取代或未取代的C 5-10二氮杂环烷基或C 6-10二氮杂环烷基，和（f）取代或未取代的C 7-14单 - 或二 - 氮杂双环烷基。 这些化合物可用于治疗由缓激肽引起的疾病如炎症，心血管疾病，疼痛等。本发明还提供包含上述化合物的药物组合物和上述化合物的中间体。

公开(公告)号：US6124460A

公开(公告)日：2000-09-26

申请号：US441515

申请日：1999-11-17

Applicant: Tsuyoshi Tomiyama ,  Akira Tomiyama ,  Takeyuki Imamaki ,  Naoto Ueyama ,  Motoharu Sonegawa ,  Satoru Takeuchi

Inventor： Tsuyoshi Tomiyama ,  Akira Tomiyama ,  Takeyuki Imamaki ,  Naoto Ueyama ,  Motoharu Sonegawa ,  Satoru Takeuchi

IPC: A61K31/00 ,  A61K31/435 ,  A61K31/439 ,  A61K31/47 ,  A61K31/4709 ,  A61P3/00 ,  A61P3/06 ,  A61P43/00 ,  C07D453/06

CPC classification number: C07D453/06

Abstract: New therapeutic agents of isoquinuclidine derivatives are represented by the following formula or its hydrochloride salts. ##STR1## (wherein R.sub.1 is hydrogen, carboxyl group, ethoxycarbonyl group, 4-(ethoxycarbonyl)phenyl group, 4-(carboxy)phenyl group, 2-(carboxy)-thiophene-5-yl group, quinoline-5-yl group, 4-(quinoline-5-yl)phenyl group or 4-(3-oxo-2-azabicyclo[2.2.2]octane-2-yl)-phenyl group; R.sub.2 is hydrogen or allyl group; Both X.sub.1 and X.sub.2 are hydrogen and X.sub.1 and X.sub.2 may form an oxo group; m stands for an integer of 0 to 2.) These compounds, have excellent inhibitory activities against squalene synthase, and are useful as a treatment agent for hypercholesterolemia.

Abstract translation: 异喹啉衍生物的新治疗剂由下式表示，或其盐酸盐。 （羧基）苯基，2-（羧基） - 噻吩-5-基，喹啉-5-基，4-（乙氧基羰基）苯基， （喹啉-5-基）苯基或4-（3-氧代-2-氮杂双环[2.2.2]辛烷-2-基） - 苯基; R2是氢或烯丙基; X1和X2都是氢和X1 X2可以形成氧基，m表示0〜2的整数。）这些化合物对角鲨烯合酶的抑制活性优异，可用作高胆固醇血症的治疗剂。

公开(公告)号：US6100269A

公开(公告)日：2000-08-08

申请号：US306497

申请日：1999-05-06

Applicant: Merouane Bencherif ,  William Scott Caldwell ,  Gary Maurice Dull ,  Patrick Michael Lippiello

Inventor： Merouane Bencherif ,  William Scott Caldwell ,  Gary Maurice Dull ,  Patrick Michael Lippiello

IPC: C07D401/04 ,  C07D453/06 ,  A61K31/505 ,  A61K31/44

CPC classification number: C07D401/04 ,  C07D453/06

Abstract: Patients susceptible to or suffering from central nervous system disorders (e.g., neurodegenerative diseases including presenile dementia, senile dementia of the Alzheimer's type, and Parkinsonism including Parkinson's disease, and other CNS disorders including attention deficit disorder, schizophrenia and Tourette's syndrome) are treated by administering an effective amount of 2-azabicyclo [2.2.1] heptane and 2-azabicyclo [2.2.2] octane compounds.

Abstract translation: 患有中枢神经系统疾病（例如，老年性痴呆，老年痴呆症，阿尔茨海默氏型老年痴呆，帕金森综合征，包括帕金森病，其他CNS疾病，包括注意力缺陷障碍，精神分裂症和图雷特氏综合症）的易感或患中枢神经系统疾病的患者， 有效量的2-氮杂双环[2.2.1]庚烷和2-氮杂双环[2.2.2]辛烷化合物。

公开(公告)号：US5886175A

公开(公告)日：1999-03-23

申请号：US352310

申请日：1994-12-08

Applicant: Phaik-Eng Sum ,  Ving J. Lee ,  Joseph J. Hlavka ,  Raymond T. Testa

Inventor： Phaik-Eng Sum ,  Ving J. Lee ,  Joseph J. Hlavka ,  Raymond T. Testa

IPC: A61K31/65 ,  A61P31/00 ,  A61P31/04 ,  C07C20060101 ,  C07C237/26 ,  C07C239/18 ,  C07C243/20 ,  C07C245/20 ,  C07C247/18 ,  C07C255/41 ,  C07C271/24 ,  C07C271/60 ,  C07C309/39 ,  C07C309/65 ,  C07C317/28 ,  C07C323/59 ,  C07D205/04 ,  C07D207/16 ,  C07D209/52 ,  C07D221/22 ,  C07D231/14 ,  C07D233/61 ,  C07D233/96 ,  C07D241/12 ,  C07D249/04 ,  C07D249/08 ,  C07D249/10 ,  C07D249/16 ,  C07D257/04 ,  C07D261/08 ,  C07D265/30 ,  C07D265/36 ,  C07D279/12 ,  C07D295/08 ,  C07D295/14 ,  C07D295/20 ,  C07D295/22 ,  C07D307/18 ,  C07D333/06 ,  C07D333/36 ,  C07D453/06 ,  C07D471/08 ,  C07D487/08 ,  C07C231/12 ,  C07C233/64

CPC classification number: C07C237/26 ,  C07C243/20 ,  C07C245/20 ,  C07C247/18 ,  C07C271/24 ,  C07C271/60 ,  C07C309/65 ,  C07C2103/46

Abstract: The invention provides compounds of the formulas ##STR1## which are useful as intermediates for the preparation of 6-demethyl-6-deotetracycline antibiotic agents.

Abstract translation: 本发明提供了可用作制备6-去甲基-6-反四环素类抗生素的中间体的式（VI）VI和VI的化合物。