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1. 发明申请

WO2011089099A1 4-PHENOXY-NICOTINAMIDE OR 4-PHENOXY-PYRIMIDINE-5-CARBOXAMIDE COMPOUNDS 审中-公开
标题翻译： 4-苯氧基-N-或4-苯氧基 - 吡咯烷-5-羧酰胺化合物
公开(公告)号：WO2011089099A1
公开(公告)日：2011-07-28
申请号：PCT/EP2011/050558
申请日：2011-01-18
申请人： F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , DEHMLOW, Henrietta , ERICKSON, Shawn, David , KIM, Kyungjin , MARTIN, Rainer, E. , OBST SANDER, Ulrike , PIETRANICO-COLE, Sherrie, Lynn , RICHTER, Hans , ULLMER, Christoph
发明人： BISSANTZ, Caterina , DEHMLOW, Henrietta , ERICKSON, Shawn, David , KIM, Kyungjin , MARTIN, Rainer, E. , OBST SANDER, Ulrike , PIETRANICO-COLE, Sherrie, Lynn , RICHTER, Hans , ULLMER, Christoph
IPC分类号： C07D401/06 , C07D401/12 , C07D401/14 , C07D417/12 , A61K31/44 , A61K31/4427 , A61K31/506 , A61P3/00
CPC分类号： C07D417/14 , C07D213/82 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D417/12
摘要： This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula (I), wherein A 1 , A 2 , B 1 , B 2 and R 1 to R 11 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.
摘要翻译：本发明涉及式（I）的新型苯基酰胺或吡啶基酰胺衍生物，其中A1，A2，B1，B2和R1至R11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。这些化合物是GPBAR1激动剂，可用作治疗II型糖尿病等疾病的药物。

2. 发明申请

WO2010034657A1 3-AMINO-INDAZOLE OR 3-AMINO-4,5,6,7-TETRAHYDRO-INDAZOLE DERIVATIVES 审中-公开
标题翻译： 3-氨基吲哚或3-氨基-4,5,6,7-四氢吲哚衍生物
公开(公告)号：WO2010034657A1
公开(公告)日：2010-04-01
申请号：PCT/EP2009/061966
申请日：2009-09-15
申请人： F. HOFFMANN-LA ROCHE AG , BENSON, Gregory, Martin , BLEICHER, Konrad , FENG, Song , GRETHER, Uwe , KUHN, Bernd , MARTIN, Rainer, E. , PLANCHER, Jean-Marc , RICHTER, Hans , MARKUS, Rudolph , TAYLOR, Sven
发明人： BENSON, Gregory, Martin , BLEICHER, Konrad , FENG, Song , GRETHER, Uwe , KUHN, Bernd , MARTIN, Rainer, E. , PLANCHER, Jean-Marc , RICHTER, Hans , MARKUS, Rudolph , TAYLOR, Sven
IPC分类号： C07D231/56 , A61K31/416 , A61P3/06 , A61P3/10 , C07D401/12 , C07D407/12
CPC分类号： C07D231/56 , C07D401/12 , C07D407/12
摘要： This invention relates to novel indazole derivatives of formula (I), wherein R 1 to R 7 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are FXR modulators and can be use as medicaments. The compounds are selective modulators of the farnesoid-X-receptor, preferably agonists u j[ιe farnesoid-X-receptor (FXR) is a member of the nuclear hormone receptor superfamily of transcription factors. Diseases which are affected by FXR modulators include increased lipid and cholesterol levels, particularly high LDL-cholesterol, high triglycerides, low HDL-cholesterol, dyslipidemia, diseases of cholesterol absorption, atherosclerotic disease, peripheral occlusive disease, ischemic, stroke, diabetes, particularly non-insulin dependent diabetes mellitus, metabolic syndrome, diabetic nephropathy, obesity, cholesterol gallstone disease, cholestasis/fibrosis of the liver, non alcoholic steatohepatitis (NASH), non-alcoholic fatty liver disease (NAFLD), psoriasis, cancer, particularly gastrointestinal cancer, osteoporosis, Parkinson's disease and Alzheimer's disease. Preferred diseases (and conditions) which are affected by FXR modulators are prevention or treatment of high LDL cholesterol levels high triglycerides, dyslipidemia, cholesterol gallstone disease, cancer, non-insulin dependent diabetes mellitus and metabolic syndrome. Particularly preferred diseases which arc affected by FXR modulators arc high LDL cholesterol, high triglyceride levels and dyslipidemia.
摘要翻译：本发明涉及式（I）的新的吲唑衍生物，其中R 1至R 7如说明书和权利要求书中所定义，以及其生理上可接受的盐。这些化合物是FXR调节剂，可用作药物。这些化合物是法呢基-X-受体的选择性调节剂，优选激动剂uj [法新颖-X-受体（FXR）是转录因子的核激素受体超家族的成员。受FXR调节剂影响的疾病包括增加脂质和胆固醇水平，特别是高LDL-胆固醇，高甘油三酸酯，低HDL-胆固醇，血脂异常，胆固醇吸收疾病，动脉粥样硬化疾病，外周性闭塞性疾病，缺血性，中风，糖尿病，特别是非 - 胰岛素依赖性糖尿病，代谢综合征，糖尿病肾病，肥胖症，胆固醇胆结石疾病，肝脏胆汁郁积/纤维化，非酒精性脂肪性肝炎（NASH），非酒精性脂肪性肝病（NAFLD），牛皮癣，癌症，特别是胃肠癌，骨质疏松症，帕金森病和阿尔茨海默病。受FXR调节剂影响的首选疾病（和病症）是预防或治疗高LDL胆固醇水平高甘油三酯，血脂异常，胆固醇胆结石疾病，癌症，非胰岛素依赖性糖尿病和代谢综合征。受FXR调节剂影响的特别优选的疾病具有高LDL胆固醇，高甘油三酯水平和血脂异常。

3. 发明申请

WO2009080555A3 CARBOXYL- OR HYDROXYL- SUBSTITUTED BENZIMIDAZOLE DERIVATIVES 审中-公开
公开(公告)号：WO2009080555A3
公开(公告)日：2009-07-02
申请号：PCT/EP2008/067399
申请日：2008-12-12
申请人： F. HOFFMANN-LA ROCHE AG , BENSON, Gregory Martin , BLEICHER, Konrad , GRETHER, Uwe , KUHN, Bernd , MARTIN, Rainer, E. , PLANCHER, Jean-Marc , RICHTER, Hans , TAYLOR, Sven , YANG, Minmin
发明人： BENSON, Gregory Martin , BLEICHER, Konrad , GRETHER, Uwe , KUHN, Bernd , MARTIN, Rainer, E. , PLANCHER, Jean-Marc , RICHTER, Hans , TAYLOR, Sven , YANG, Minmin
IPC分类号： C07D401/14 , C07D401/04 , C07D235/12 , C07D401/12 , A61K31/4184 , A61P3/10
摘要： This invention relates to novel carboxyl- or hydroxylsubstituted benzimidazole derivatives of formula (I) wherein R 1 to R 6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to FXR and can be used as medicaments.

4. 发明申请

WO2007025897A2 BENZOOXAZOLE, OXAZOLOPYRIDINE, BENZOTHIAZOLE AND THIAZOLOPYRIDINE DERIVATIVES 审中-公开
标题翻译：苯唑唑，氧杂吡咯烷，苯并噻唑和噻唑吡啶衍生物
公开(公告)号：WO2007025897A2
公开(公告)日：2007-03-08
申请号：PCT/EP2006/065522
申请日：2006-08-21
申请人： F. HOFFMANN-LA ROCHE AG , BINGGELI, Alfred , CHRIST, Andreas, D. , GREEN, Luke , GUBA, Wolfgang , MAERKI, Hans, P. , MARTIN, Rainer, E. , MOHR, Peter
发明人： BINGGELI, Alfred , CHRIST, Andreas, D. , GREEN, Luke , GUBA, Wolfgang , MAERKI, Hans, P. , MARTIN, Rainer, E. , MOHR, Peter
IPC分类号： C07D413/12 , C07D413/14 , C07D498/04 , C07D417/12 , C07D417/14 , A61P3/10
CPC分类号： C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： This invention is concerned with compounds of the formula (I) wherein X, A, B, R 1 , R 2 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to then- use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
摘要翻译：本发明涉及式（I）的化合物，其中X，A，B，R 1，R 2和G如说明书和权利要求中所定义，以及其药学上可接受的盐。本发明还涉及含有这些化合物的药物组合物，其制备方法，然后用于治疗和/或预防与调节SST受体亚型5有关的疾病。

5. 发明申请

WO2022049134A1 HETEROCYCLIC COMPOUNDS 审中-公开
公开(公告)号：WO2022049134A1
公开(公告)日：2022-03-10
申请号：PCT/EP2021/074150
申请日：2021-09-01
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BENZ, Joerg , GRETHER, Uwe , HORNSPERGER, Benoit , KROLL, Carsten , KUHN, Bernd , MARTIN, Rainer, E. , O'HARA, Fionn , PUELLMANN, Bernd , RICHTER, Hans , RITTER, Martin
IPC分类号： C07D403/06 , C07D403/14 , C07D413/04 , C07D413/14 , C07D487/04 , A61K31/4192 , A61K31/422 , A61P25/00
摘要： The invention provides new heterocyclic compounds having the general formula (I) wherein B, C, L, X, Y, RL and R3 to R5 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.

6. 发明申请

WO2021086785A1 BIFUNCTIONAL COMPOUNDS 审中-公开
公开(公告)号：WO2021086785A1
公开(公告)日：2021-05-06
申请号：PCT/US2020/057356
申请日：2020-10-26
申请人： F. HOFFMANN-LA ROCHE AG , C4 THERAPEUTICS, INC. , HOFFMANN-LA ROCHE INC.
发明人： GAUFRETEAU, Delphine , HUTTER, Roman , JOVCHEVA, Eleonora , KUHN, Bernd , LUEBBERS, Thomas , MARTIN, Rainer, E. , MARTIN, Laetitia, Janine , MUELLER, Barbara, Johanna , NORCROSS, Roger , RICKLIN, Fabienne , SCHMID, Philipp , WACH, Jean-yves , WICHMANN, Juergen , DUPLESSIS, Martin , LAZARSKI, Kiel , LIANG, Yanke
IPC分类号： A61P35/00 , C07D487/04
摘要： The invention provides a bifunctional compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein said Targeting Ligand, Linker and Degron are as described herein.

7. 发明申请

WO2021083949A1 BIFUNCTIONAL COMPOUNDS FOR THE TREATMENT OF CANCER 审中-公开
公开(公告)号：WO2021083949A1
公开(公告)日：2021-05-06
申请号：PCT/EP2020/080265
申请日：2020-10-28
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC. , C4 THERAPEUTICS, INC.
发明人： DUPLESSIS, Martin , GAUFRETEAU, Delphine , HUTTER, Roman , JOVCHEVA, Eleonora , KUHN, Bernd , LAZARSKI, Kiel , LIANG, Yanke , LUEBBERS, Thomas , MARTIN, Laetitia, Janine , MARTIN, Rainer, E. , MUELLER, Barbara, Johanna , NORCROSS, Roger , SCHMID, Philipp , WACH, Jean-Yves
IPC分类号： C07D401/14 , C07D471/08 , C07D487/08 , C07D487/10 , C07D498/10 , C07D519/00 , A61P35/00 , A61K31/501 , A61K31/537
摘要： The invention provides bifunctional compounds of formula (I) or a pharmaceutically acceptable salt thereof. Formula (I). The compounds cause the degradation of SMARCA2 via the targeted ubiquination of SMARCA2 protein and subsequent proteasomal degradation and are thus useful for the treatment of cancer. The targeting ligand is of formula (TL).

8. 发明申请

WO2014079787A1 SUBSTITUTED 1,6-NAPHTHYRIDINES 审中-公开
标题翻译：取代的1,6-萘啶
公开(公告)号：WO2014079787A1
公开(公告)日：2014-05-30
申请号：PCT/EP2013/074012
申请日：2013-11-18
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： CECCARELLI, Simona, M. , JAGASIA, Ravi , JAKOB-ROETNE, Roland , MARTIN, Rainer, E. , PETERS, Jens-Uwe , WICHMANN, Juergen
IPC分类号： A61K31/4375 , A61P25/24 , A61P25/28 , A61P25/30
CPC分类号： C07D471/04 , A61K31/4375 , A61K31/444 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/541
摘要： The present invention relates to the use of compounds of general formula (I) wherein R' is hydrogen or lower alkyl; R 1 is halogen, lower alkyl, cycloalkyl or cyano; or is phenyl, optionally substituted by one to three substituents, selected from lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, halogen, cyano, hydroxy, C(O)-NH-lower alkyl, CH 2 -C(O)-NH-lower alkyl, CH 2 -NH-C(O)-lower alkyl, CH 2 NH 2 , S(O) 2 CH 3 , S(O) 2 N(CH 3 ) 2 , or by heterocycloalkyl groups; or is pyrazol-1, 4 or 5-yl, optionally substituted by lower alkyl; or is thiazol-5-yl, optionally substituted by one or two lower alkyl groups; or is pyridine 2, 3 or 4-yl, optionally substituted by lower alkyl, lower alkoxy, halogen or N(CH 3 ) 2 ; or is 3,6-dihydro-2H-pyran; or is benzo[d][1,3]dioxol-5-yl; or is 2,3-dihydrobenzo[b][1,4]dioxin-6-yl; R 2 is hydrogen, lower alkyl or lower alkyl substituted by alkoxy; R 3 is hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, NH-S(O) 2 -CH 3 , -(CH 2 ) m -O-lower alkyl or -(CH 2 ) n -S(O) 2 -CH 3 ; or is -(CR 2 ) n -phenyl, optionally substituted by -S(O) 2 CH 3 or lower alkoxy; or is -(CH 2 ) n -heterocycloalkyl, optionally substituted by lower alkyl and =O; or is -(CH 2 ) n -heteroaryl, optionally substituted by one or two lower alkyl groups; or is -(CH 2 ) n -cycloalkyl, optionally substituted by cyano; or R 2 and R 3 form together with the N atom to which they are attached a heterocyclic ring, selected from morpholine, piperidine, 1, 1-dioxo-thiomorpholine or piperazine which may be substituted by lower alkyl or C(O)O-lower alkyl, or may form a pyrrolidine ring, optionally substituted by hydroxy; R is independently from n hydrogen or lower alkyl; n is 0, 1, 2, 3; m is 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof, for the treatment of schizophrenia, obsessive-compulsive personality disorder, depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson's disease, dementia, Alzheimer's disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction ("chemobrain"), Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, and disturbances due to radiation therapy, chronic stress, optic neuropathy or macular degeneration, or abuse of neuro-active drugs selected from alcohol, opiates, methamphetamine, phencyclidine or cocaine.
摘要翻译：本发明涉及通式（I）的化合物，其中R'是氢或低级烷基; R1是卤素，低级烷基，环烷基或氰基; 或者是被选自低级烷基，被卤素取代的低级烷基，低级烷氧基，被卤素取代的低级烷氧基，卤素，氰基，羟基，C（O）-NH-低级烷基，CH 2 - C（O）-NH-低级烷基，CH 2 -NH-C（O） - 低级烷基，CH 2 NH 2，S（O）2 CH 3，S（O）2 N（CH 3）2或杂环烷基; 或是任选被低级烷基取代的吡唑-1,4或5-基; 或是任选被一个或两个低级烷基取代的噻唑-5-基; 或任选被低级烷基，低级烷氧基，卤素或N（CH 3）2取代的吡啶2,3或4-基; 或者是3,6-二氢-2H-吡喃; 或者是苯并[d] [1,3]二氧杂环戊烯-5-基; 或是2,3-二氢苯并[b] [1,4]二恶英-6-基; R2是氢，被烷氧基取代的低级烷基或低级烷基; R 3是氢，低级烷基，被卤素取代的低级烷基，被羟基取代的低级烷基，NH-S（O）2 -CH 3， - （CH 2）m -O-低级烷基或 - （CH 2）n -S（O）2 -CH 3; 或为 - （CR 2）n - 苯基，任选被-S（O）2 CH 3或低级烷氧基取代; 或是 - （CH 2）n - 杂环烷基，任选被低级烷基和= O取代; 或是 - （CH 2）n - 杂芳基，任选被一个或两个低级烷基取代; 或为 - （CH 2）n - 环烷基，任选被氰基取代; 或者R 2和R 3与它们所连接的N原子一起形成杂环，该杂环选自吗啉，哌啶，1,1-二氧代硫代吗啉或哌嗪，其可被低级烷基或C（O）O-低级烷基取代，或可以形成任选被羟基取代的吡咯烷环; R独立地为氢或低级烷基; n为0,1,2,3; m为2; 或其药学上可接受的酸加成盐与外消旋混合物或其相应的对映体和/或光学异构体反应，用于治疗精神分裂症，强迫症人格障碍，抑郁症，双相性精神障碍，焦虑症，正常老化，癫痫，视网膜变性，创伤性脑损伤，脊髓损伤，创伤后应激障碍，恐慌症，帕金森病，痴呆，阿尔茨海默病，轻度认知障碍，化学疗法诱发的认知功能障碍（“chemobrain”），唐氏综合征，自闭症谱系障碍，听力损失，耳鸣，脊髓小脑性共济失调，肌萎缩性侧索硬化，多发性硬化，亨廷顿舞蹈病，中风以及由于放射治疗引起的干扰，慢性应激，视神经病变或黄斑变性，或滥用选自酒精，阿片剂，甲基苯丙胺的神经活性药物，苯环利定或可卡因。

10. 发明公开

EP4208456A1 HETEROCYCLIC COMPOUNDS 审中-实审
公开(公告)号：EP4208456A1
公开(公告)日：2023-07-12
申请号：EP21772763.5
申请日：2021-09-01
申请人： F. Hoffmann-La Roche AG
发明人： BENZ, Joerg , GRETHER, Uwe , HORNSPERGER, Benoit , KROLL, Carsten , KUHN, Bernd , MARTIN, Rainer, E. , O'HARA, Fionn , PUELLMANN, Bernd , RICHTER, Hans , RITTER, Martin
IPC分类号： C07D403/06 , C07D403/14 , C07D413/04 , C07D413/14 , C07D487/04 , A61K31/4192 , A61K31/422 , A61P25/00

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