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1. 发明申请

WO2021157590A1 ジフルオロメチル置換芳香族複素環化合物の製造方法审中-公开
公开(公告)号：WO2021157590A1
公开(公告)日：2021-08-12
申请号：PCT/JP2021/003821
申请日：2021-02-03
申请人：ＡＧＣ株式会社
发明人：野村　好廷 , 安樂　英一郎
IPC分类号： C07D213/26 , C07D215/12 , C07D215/16 , C07D233/22 , C07D233/26 , C07D237/30 , C07D241/42 , C07D277/64
摘要：本発明の目的は、簡便かつ安価な方法で、ジフルオロメチル置換芳香族複素環化合物を製造できる方法を提供することにある。　本発明は、芳香族炭化水素溶媒、エステル溶媒およびエーテル溶媒から選択される溶媒中、式（Ｉ）で表される部分構造を有するＮ－オキシド芳香族複素環化合物を、テトラフルオロエチレンと反応させることを特徴とする、式（ＩＩ）で表される部分構造を有するジフルオロメチル置換芳香族複素環化合物の製造方法に関する。［式中の各記号は、明細書に記載の通りである。］

2. 发明申请

WO2020252383A2 COMPOUNDS FOR THE MODULATION OF PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9) 审中-公开
公开(公告)号：WO2020252383A2
公开(公告)日：2020-12-17
申请号：PCT/US2020/037591
申请日：2020-06-12
申请人： SRX CARDIO, LLC
发明人： BOWERS, Simeon , KARBARZ, Mark , ZHU, Jiang , BARTA, Thomas E. , BOURNE, Jonathan William , PANDEY, Anjali
IPC分类号： C07D253/02 , A61K31/53 , C07D207/08 , C07D211/14 , C07D211/18 , C07D211/38 , C07D211/42 , C07D211/56 , C07D233/10 , C07D233/22 , C07D265/30 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D471/14 , C07D498/04
摘要： The present disclosure relates to novel compounds capable of binding to PCSK9, thereby modulating PCSK9 biological activity. Also provided are compositions comprising these compounds, methods of preparing the compounds, and methods for use of the compounds in the treatment of PCSK9-related conditions and diseases.

3. 发明申请

WO2016198374A1 AROMATIC SULFONAMIDE DERIVATIVES 审中-公开
标题翻译：芳香磺酰胺衍生物
公开(公告)号：WO2016198374A1
公开(公告)日：2016-12-15
申请号：PCT/EP2016/062841
申请日：2016-06-07
申请人： BAYER PHARMA AKTIENGESELLSCHAFT
发明人： WERNER, Stefan , MESCH, Stefanie , BRÄUER, Nico , POOK, Elisabeth , DAHLLÖF, Henrik , NUBBEMEYER, Reinhard , OSMERS, Maren , KALTHOF, Bernd
IPC分类号： C07D213/71 , C07D213/75 , C07D309/06 , C07D213/84 , C07D309/08 , C07D309/12 , C07D317/64 , C07D319/12 , C07D319/18 , C07C303/38 , C07D231/18 , C07C303/40 , C07D231/20 , C07D333/32 , A61P29/00 , A61P25/04 , C07D233/22 , C07D333/48 , C07D233/60 , C07B59/00 , C07C311/17 , C07C311/46 , C07D239/26 , C07C317/22 , C07D239/34 , C07D417/04 , C07D249/08 , C07D257/04 , C07D263/24 , C07C235/84 , C07D205/04 , C07D265/32 , C07D207/12 , C07D207/24 , C07D207/27 , C07D277/24 , C07D211/40 , C07D211/42 , C07D295/096 , C07D211/46 , C07D295/185 , C07D295/192 , C07D213/46 , C07D213/56 , C07D213/61 , C07D305/06 , C07D305/08 , C07D213/643 , C07D213/65 , C07D213/68 , C07D213/69 , C07D307/12 , C07C51/367 , C07D307/77 , C07D307/79
CPC分类号： C07D213/71 , C07B59/001 , C07B2200/05 , C07C235/84 , C07C311/17 , C07C311/46 , C07C317/22 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D205/04 , C07D207/12 , C07D207/24 , C07D207/27 , C07D211/40 , C07D211/42 , C07D211/46 , C07D213/46 , C07D213/56 , C07D213/61 , C07D213/643 , C07D213/65 , C07D213/68 , C07D213/69 , C07D213/75 , C07D213/84 , C07D231/18 , C07D231/20 , C07D233/22 , C07D233/60 , C07D239/26 , C07D239/34 , C07D249/08 , C07D257/04 , C07D263/24 , C07D265/32 , C07D277/24 , C07D295/096 , C07D295/185 , C07D295/192 , C07D305/06 , C07D305/08 , C07D307/12 , C07D307/77 , C07D307/79 , C07D309/06 , C07D309/08 , C07D309/12 , C07D317/64 , C07D319/12 , C07D319/18 , C07D333/32 , C07D333/48 , C07D417/04
摘要： Substituted aromatic sulfonamides of formula (I) pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease.
摘要翻译：式（I）的取代的芳族磺酰胺包含所述化合物的药物组合物和组合以及用于制备用于治疗或预防疾病的药物组合物的所述化合物的用途。

4. 发明申请

WO2016105449A1 COMPOUNDS FOR USE AS PAIN THERAPEUTICS 审中-公开
标题翻译：用作止痛药的化合物
公开(公告)号：WO2016105449A1
公开(公告)日：2016-06-30
申请号：PCT/US2015/000154
申请日：2015-12-22
申请人： LEDERMAN, Seth , DAUGHERTY, Bruce
发明人： LEDERMAN, Seth , DAUGHERTY, Bruce
IPC分类号： C07D263/28 , C07D207/22 , C07D233/06 , C07D233/20 , C07D233/22 , C07D233/24 , C07D233/88 , C07D233/50 , C07D263/48 , C07D401/04 , C07D403/04 , C07D403/12 , C07D417/12 , C07D471/04 , C07C211/38 , C07D405/04 , C07C211/08 , C07C211/21 , C07C211/42 , C07C279/22 , C07C279/04 , C07H19/052 , A61K31/13 , A61K31/155 , A61K31/40 , A61K31/4164 , A61K31/4168 , A61K31/4178 , A61K31/421 , A61K31/43 , A61K31/4725 , A61K31/506 , A61K31/7028 , A61P29/00 , A61P29/02 , A61P43/00 , C07C279/12 , A61K31/417 , A61K31/4174
CPC分类号： C07H19/052 , A61K31/047 , A61K31/13 , A61K31/155 , A61K31/167 , A61K31/192 , A61K31/40 , A61K31/4164 , A61K31/4166 , A61K31/4168 , A61K31/417 , A61K31/4174 , A61K31/4178 , A61K31/421 , A61K31/427 , A61K31/437 , A61K31/4725 , A61K31/506 , A61K31/522 , A61K31/616 , A61K31/7008 , Y02A50/401 , A61K2300/00
摘要： This disclosure provides compounds and compositions for use as analgesics and for the treatment of one or more conditions selected from: pain; psychic pain; psychological pain; psychiatric pain; depression; allodynia; fibromyalgia; fibromyalgia-ness; central sensitization; centralization; regional pain syndrome; temporomandibular joint syndrome (TMJ); lower back pain; interstitial cystitis; Gulf War syndrome; visceral pain; phantom limb painj.kidney stones; gout; neuropathic pain; post-herpetic neuralgia; diabetic neuropathy; sickle cell pain; priapism; nociceptive pain; post-operative pain; orthopedic injury pain; bunionectomy; dental extraction; pain after severed spinal cord injury; osteoarthritis; rheumatoid arthritis; Lyme disease; Parkinson's disease; opioid-induced constipation; an opioid withdrawal symptom; pain associated with post-traumatic stress disorder (PTSD); and combinations of any of the foregoing conditions. This disclosure also provides compounds that are ligands, and in some embodiments, modulators (e.g., agonists), for the imidazoline receptor type 1.
摘要翻译：本公开提供用作止痛剂和用于治疗选自以下的一种或多种病症的化合物和组合物：疼痛; 精神痛苦心理上的痛苦; 精神病痛萧条; 异常性疼痛; 纤维肌痛; 纤维肌痛的烦躁; 中心致敏; 集权; 区域性疼痛综合征; 颞下颌关节综合征（TMJ）; 腰背痛间质性膀胱炎海湾战争综合症; 内脏痛幻肢四肢痛痛风; 神经性疼痛疱疹后神经痛糖尿病性神经病变镰状细胞性疼痛阴茎异常勃起; 伤害性疼痛术后疼痛; 矫形外伤性疼痛; 拇囊炎切除; 牙科提取; 切断脊髓损伤后疼痛; 骨关节炎; 类风湿关节炎; 莱姆病; 帕金森病阿片样物质引起的便秘阿片样物质戒断症状与创伤后应激障碍（PTSD）相关的疼痛; 以及任何上述条件的组合。本公开还提供了作为咪唑啉受体1型的配体，在一些实施方案中为调节剂（例如激动剂）的化合物。

5. 发明申请

WO2013045431A1 SULFONAMIDE COMPOUNDS AND THEIR USE IN THE MODULATION RETINOID - RELATED ORPHAN RECEPTOR 审中-公开
标题翻译：磺酰胺化合物及其在调节反应物中的用途 - 相关的ORPAN受体
公开(公告)号：WO2013045431A1
公开(公告)日：2013-04-04
申请号：PCT/EP2012/068845
申请日：2012-09-25
申请人： GLAXO GROUP LIMITED , BIRAULT, Véronique , CAMPBELL, Amanda, Jennifer , HARRISON, Stephen , LE, Joelle
发明人： BIRAULT, Véronique , CAMPBELL, Amanda, Jennifer , HARRISON, Stephen , LE, Joelle
IPC分类号： A61K31/18 , A61K31/33 , C07D213/30 , C07D213/38 , C07D213/61 , C07D213/65 , C07D213/68 , C07D213/75 , C07D233/22 , C07D239/28 , C07D249/08 , C07D257/04 , C07D261/08 , C07C311/21 , C07C311/29
CPC分类号： C07C311/44 , C07C311/21 , C07C311/29 , C07C2101/16 , C07C2601/16 , C07D213/30 , C07D213/38 , C07D213/42 , C07D213/61 , C07D213/65 , C07D213/68 , C07D213/73 , C07D213/75 , C07D231/12 , C07D233/22 , C07D233/64 , C07D239/26 , C07D239/28 , C07D239/34 , C07D249/08 , C07D257/04 , C07D261/08
摘要： The present invention is directed to novel retinoid-related orphan receptor gamma (RORy) modulators of formula (I), processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by RORy wherein R 1 to R 7 are as defined in claim 1.
摘要翻译：本发明涉及式（I）的类视黄醇相关孤儿受体γ（RORY）调节剂，其制备方法，含有这些调节剂的药物组合物及其在治疗由RORy介导的炎性，代谢和自身免疫性疾病中的用途其中R 1至R 7如权利要求1中所定义。

6. 发明申请

WO2010132629A1 GRANULAR FABRIC SOFTENING COMPOSITIONS COMPRISING A DI-ALKYL SUBSTITUTED IMIDAZOLINE DERIVATIVES 审中-公开
标题翻译：包含二烷基取代的咪唑啉衍生物的颗粒织物组合物
公开(公告)号：WO2010132629A1
公开(公告)日：2010-11-18
申请号：PCT/US2010/034642
申请日：2010-05-13
申请人： THE PROCTER & GAMBLE COMPANY , DEMEYERE, Hugo, Jean Marie
发明人： DEMEYERE, Hugo, Jean Marie
IPC分类号： C07D233/22
CPC分类号： C11D3/28 , C11D1/46 , C11D1/835
摘要： The present invention describes a granular fabric softening composition comprising a di-alkyl substituted imidazoline derivative according to the formula : (I) wherein; X 1 is a C2-3 alkylene group; X 2 and X 3 are independently C1-6 linear or branched alkylene or alkenylene groups; R 1 and R 2 are independently C8-22 linear or branched alkyl or alkenyl groups; characterized in that; A and B are independently O-(C=O)-.
摘要翻译：本发明描述了一种颗粒织物软化组合物，其包含根据下式的（I）的二烷基取代的咪唑啉衍生物，其中： X1是C2-3亚烷基; X 2和X 3独立地为C 1-6直链或支链亚烷基或亚烯基; R1和R2独立地为C8-22直链或支链烷基或烯基; 其特征在于： A和B独立地为O-（C = O） - 。

7. 发明申请

WO2010125402A1 IMIDAZOLE DERIVATIVES AND THEIR USE AS MODULATORS OF CYCLIN DEPENDENT KINASES 审中-公开
标题翻译：咪唑衍生物及其作为细胞周期调节因子的调节剂
公开(公告)号：WO2010125402A1
公开(公告)日：2010-11-04
申请号：PCT/GB2010/050725
申请日：2010-04-30
申请人： NOVARTIS AG , ASTEX THERAPEUTICS LIMITED , HOWARD, Steven , MORTENSON, Paul Neil , HISCOCK, Steven Douglas , WOOLFORD, Alison Jo-Anne , WOODHEAD, Andrew James , CHESSARI, Gianni , O'REILLY, Marc , CONGREVE, Miles Stuart , DAGOSTIN, Claudio , CHO, Young Shin , YANG, Fan , CHEN, Christine Hiu-Tung , BRAIN, Christopher Thomas , LAGU, Bharat , WANG, Yaping , KIM, Sunkyu , GRIALDES, John , LUZZIO, Michael Joseph , PEREZ, Lawrence Blas
发明人： HOWARD, Steven , MORTENSON, Paul Neil , HISCOCK, Steven Douglas , WOOLFORD, Alison Jo-Anne , WOODHEAD, Andrew James , CHESSARI, Gianni , O'REILLY, Marc , CONGREVE, Miles Stuart , DAGOSTIN, Claudio , CHO, Young Shin , YANG, Fan , CHEN, Christine Hiu-Tung , BRAIN, Christopher Thomas , LAGU, Bharat , WANG, Yaping , KIM, Sunkyu , GRIALDES, John , LUZZIO, Michael Joseph , PEREZ, Lawrence Blas
IPC分类号： C07D233/22 , C07D235/12 , C07D401/06 , C07D401/10 , C07D401/14 , C07D409/10 , C07D409/14 , C07D413/14 , C07D417/10 , A61K31/4164 , A61K31/4178 , A61P35/00
CPC分类号： C07D471/04 , C07D233/22 , C07D233/24 , C07D235/12 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D487/04 , C07D519/00
摘要： The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N + -O - or CR 3 ; Y is N, N + -O - or CR 3a ; R 1 and R 2 are independently selected from hydrogen and various substituents as defined in the claims; or R 1 and R 2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R 3 is selected from hydrogen and various substituents; and R 3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.
摘要翻译：本发明提供式（I）化合物及其盐，互变异构体，溶剂化物和N-氧化物; 其中Q是CH或N; X是N，N + -O-或CR 3; Y是N，N + -O-或CR3a; R 1和R 2独立地选自氢和权利要求中定义的各种取代基; 或R 1和R 2与它们所连接的原子一起连接以形成任选取代的4至7个成员的碳环或杂环芳族或非芳族环; R3选自氢和各种取代基; 并且R 3a选自氢和权利要求中定义的各种取代基。还提供含有式（I）化合物，制备化合物的方法和化合物的医疗用途的药物组合物。式（I）化合物具有作为CDK激酶抑制剂的活性，并且可用于治疗尤其是增殖性疾病如癌症。

8. 发明申请

WO2010074776A2 COMPOUNDS FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：用于治疗癌症的化合物
公开(公告)号：WO2010074776A2
公开(公告)日：2010-07-01
申请号：PCT/US2009/047572
申请日：2009-06-16
申请人： THE UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION , OHIO STATE UNIVERSITY RESEARCH FOUNDATION
发明人： MILLER, Duane, D. , LI, Wei , WANG, Zhao , LU, Yan , CHEN, Jianjun , DALTON, James, T. , LI, Chien-Ming
IPC分类号： A61K31/425 , C12N5/02 , C07D263/34 , A61K31/421 , C07D233/22 , A61K31/415
CPC分类号： C07D403/04 , A61K31/421 , A61K31/426
摘要： Compounds according to formula (I) are disclosed, (I), where Q is S, N, or O; X is optional, and can be O=, S=, =N-NH 2 , =N-OH, or -OH; Y is optional and can be -N(H)-, O, or C 1 to C 20 hydrocarbon; and R 1 and R 2 are each independently substituted or unsubstituted single-, fused- or multiple-ring aryl or (hetero)cyclic ring systems. Methods of making these compounds, pharmaceutical compositions containing the compounds, and their use, particularly for treating or preventing cancer, are also disclosed.
摘要翻译：公开了式（I）的化合物，其中Q为S，N或O;（I） X是任选的，并且可以是O =，S =，= N-NH 2，= N-OH或-OH; Y是任选的，可以是-N（H） - ，O或C 1 -C 20烃; 且R 1和R 2各自独立地为取代或未取代的单，稠环或多环芳基或（杂）环系。还公开了制备这些化合物的方法，含有这些化合物的药物组合物及其用途，特别是用于治疗或预防癌症的方法。

9. 发明申请

WO2010016844A1 LOFEXIDINE ENANTIOMERS FOR USE AS A TREATMENT FOR CNS DISEASE AND PATHOLOGIES AND ITS CHIRAL SYNTHESIS 审中-公开
标题翻译：用于治疗CNS疾病和病理学及其合成的LOFEXIDINE ENANTIMERS
公开(公告)号：WO2010016844A1
公开(公告)日：2010-02-11
申请号：PCT/US2008/072570
申请日：2008-08-08
申请人： AGEAN LLC , DIGENIS, George, A. , CROOKS, Peter , ALGHANANEEM, Abeer
发明人： DIGENIS, George, A. , CROOKS, Peter , ALGHANANEEM, Abeer
IPC分类号： A61K31/4164 , C07D233/22 , A61P25/00
CPC分类号： C07D233/22
摘要： The invention relates to methods for treatment of CNS disease and pathologies using non-racemic mixtures of lofexidine enantiomers. The invention also relates to processes for the manufacture of chirally pure enantiomers of lofexidine.
摘要翻译：本发明涉及使用非夫洛西定对映异构体的非外消旋混合物治疗CNS疾病和病理的方法。本发明还涉及制备洛哌啶的手性纯的对映异构体的方法。

10. 发明申请

WO2009003867A1 4-IMIDAZOLINES AND THEIR USE AS ANTIDEPRESSANTS 审中-公开
标题翻译： 4-咪唑啉及其作为抗生素的用途
公开(公告)号：WO2009003867A1
公开(公告)日：2009-01-08
申请号：PCT/EP2008/057980
申请日：2008-06-24
申请人： F. HOFFMANN-LA ROCHE AG , GALLEY, Guido , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
发明人： GALLEY, Guido , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
IPC分类号： C07D233/06 , C07D233/12 , C07D233/22 , C07D233/24 , A61K31/4174 , A61P25/24
CPC分类号： C07D233/06 , C07D233/12 , C07D233/22 , C07D233/24
摘要： The present invention relates to compounds of formula (I) wherein R 1 is hydrogen, halogen or lower alkyl; R 2 is hydrogen or amino; X-Y is -(CH 2 ) n -, N(R)-CH 2 -, -O-CH 2 - or -S-CH 2 -; Ar is phenyl or naphthyl; n is 1 or 2; R is hydrogen or lower alkyl; and to their pharmaceutically active salts, with the exclusion of the racemic compound 4-benzyl-4,5-dihydro-lH-imidazole or its tautomer (CAS 131548-83-9). It has been found that the compounds of formula (I) have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
摘要翻译：本发明涉及式（I）化合物，其中R 1是氢，卤素或低级烷基; R2是氢或氨基; X-Y是 - （CH 2）n - ，N（R）-CH 2 - ， - O-CH 2 - 或-S-CH 2 - ; Ar是苯基或萘基; n为1或2; R是氢或低级烷基; 和其药物活性盐，排除外消旋化合物4-苄基-4,5-二氢-1H-咪唑或其互变异构体（CAS 131548-83-9）。已经发现式（I）化合物对微量胺相关受体（TAAR）具有良好的亲和力，特别是对于TAAR1。这些化合物可用于治疗抑郁症，焦虑障碍，双相情感障碍，注意力缺陷多动障碍（ADHD），应激相关疾病，精神病性精神障碍如精神分裂症，神经系统疾病如帕金森病，神经变性疾病如阿尔茨海默病，癫痫，偏头痛，高血压，药物滥用和代谢障碍如进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和同化障碍，体温平衡紊乱和失调，睡眠和昼夜节律紊乱以及心血管疾病。

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