公开(公告)号：US20240109834A1

公开(公告)日：2024-04-04

申请号：US18368410

申请日：2023-09-14

申请人： Insmed Incorporated

发明人： Vladimir MALININ ,  Walter PERKINS ,  Franziska LEIFER ,  Donna M. KONICEK ,  Zhili LI ,  Adam PLAUNT

IPC分类号： C07C69/734 ,  A61K9/00 ,  A61K9/10 ,  A61K9/14 ,  A61K9/51 ,  A61K31/165 ,  A61K31/216 ,  A61K31/225 ,  A61K47/06 ,  A61K47/14 ,  A61K47/24 ,  A61K47/28 ,  A61K47/34 ,  A61K47/54 ,  A61K47/60 ,  A61M15/00 ,  A61M16/14 ,  A61P9/12 ,  A61P11/00 ,  C07C69/712 ,  C07C69/736 ,  C07C69/753 ,  C07C235/20 ,  C07C235/22

CPC分类号： C07C69/734 ,  A61K9/0019 ,  A61K9/0043 ,  A61K9/0053 ,  A61K9/0073 ,  A61K9/0075 ,  A61K9/0078 ,  A61K9/10 ,  A61K9/14 ,  A61K9/51 ,  A61K31/165 ,  A61K31/216 ,  A61K31/225 ,  A61K47/06 ,  A61K47/14 ,  A61K47/24 ,  A61K47/28 ,  A61K47/34 ,  A61K47/543 ,  A61K47/544 ,  A61K47/60 ,  A61M15/0085 ,  A61M15/009 ,  A61M16/14 ,  A61P9/12 ,  A61P11/00 ,  C07C69/712 ,  C07C69/736 ,  C07C69/753 ,  C07C235/20 ,  C07C235/22 ,  A61M2202/064 ,  C07C2601/18 ,  C07C2603/14

摘要： Prostacyclin compounds and compositions comprising the same are provided herein. Specifically, prostacyclin compounds comprising treprostinil covalently linked to a linear C5-C18 alkyl, branched C5-C18 alkyl, linear C2-C18 alkenyl, branched C3-C18 alkenyl, aryl, aryl-C1-C18 alkyl or an amino acid or a peptide (e.g., dipeptide, tripeptide, tetrapeptide) are described. The linkage, in one embodiment, is via a carbamate, amide or ester bond. Prostacyclin compounds provided herein can also include at least one hydrogen atom substituted with at least one deuterium atom. Methods for treating pulmonary hypertension (e.g., pulmonary arterial hypertension) and portopulmonary hypertension are also provided.

公开(公告)号：US09708247B2

公开(公告)日：2017-07-18

申请号：US14849428

申请日：2015-09-09

申请人： The Regents of the University of California

发明人： Peter Walter ,  Carmela Sidrauski ,  Diego Acosta Alvear ,  Michelle R. Arkin ,  Christopher G. Wilson ,  Kean Hooi Ang ,  Brian R. Hearn ,  Punitha Vedantham ,  Adam R. Renslo ,  Mervyn Maze ,  Susana Vacas

IPC分类号： C07C235/14 ,  A61K31/165 ,  A61K31/4192 ,  C07D403/12 ,  C07D495/04 ,  C07C255/54 ,  C07C257/14 ,  C07C271/24 ,  C07C271/52 ,  C07C211/29 ,  C07C317/22 ,  C07C317/44 ,  C07C323/60 ,  C07C235/20 ,  C07C235/22 ,  C07C235/24 ,  C07F7/08

CPC分类号： C07C235/14 ,  A61K31/165 ,  A61K31/4192 ,  C07C211/29 ,  C07C235/20 ,  C07C235/22 ,  C07C235/24 ,  C07C255/54 ,  C07C257/14 ,  C07C271/24 ,  C07C271/52 ,  C07C317/22 ,  C07C317/44 ,  C07C323/60 ,  C07C2601/04 ,  C07C2601/14 ,  C07D403/12 ,  C07D495/04 ,  C07F7/081

摘要： Provided herein, inter alia, are compounds and methods useful for modulating the translational effects of eIF2α phosphorylation, the Integrated Stress Response (ISR), and the unfolded protein response (UPR); for treating diseases; for increasing protein production, and for improving long-term memory.

公开(公告)号：US09255064B2

公开(公告)日：2016-02-09

申请号：US14641104

申请日：2015-03-06

申请人： Insmed Incorporated

发明人： Vladimir Malinin ,  Walter Perkins ,  Franziska Leifer ,  Donna Konicek ,  Zhili Li ,  Adam Plaunt

IPC分类号： C07C235/22 ,  C07C69/736 ,  C07C69/753 ,  C07C235/20 ,  C07C69/712

CPC分类号： A61K31/225 ,  A61K9/0075 ,  A61K9/0078 ,  A61K31/165 ,  A61K31/216 ,  A61K47/06 ,  A61K47/543 ,  A61K47/544 ,  A61K47/60 ,  C07C69/712 ,  C07C69/736 ,  C07C69/753 ,  C07C235/20 ,  C07C235/22 ,  C07C2601/18 ,  C07C2603/14

摘要： Prostacyclin compounds and compositions comprising the same are provided herein. Specifically, prostacyclin compounds comprising treprostinil covalently linked to a linear C5-C18 alkyl, branched C5-C18 alkyl, linear C2-C18 alkenyl, branched C3-C18 alkenyl, aryl, aryl-C1-C18 alkyl or an amino acid or a peptide (e.g., dipeptide, tripeptide, tetrapeptide) are described. The linkage, in one embodiment, is via a carbamate, amide or ester bond. Prostacyclin compounds provided herein can also include at least one hydrogen atom substituted with at least one deuterium atom. Methods for treating pulmonary hypertension (e.g., pulmonary arterial hypertension) and portopulmonary hypertension are also provided.

公开(公告)号：US08841347B2

公开(公告)日：2014-09-23

申请号：US13853542

申请日：2013-03-29

申请人： Anna Maria Waszkielewicz ,  Uniwersytet Jagiellonski

发明人： Henryk Marona ,  Anna Waszkielewicz ,  Katarzyna Kiec-Kononowicz

IPC分类号： A61K31/135 ,  C07C235/20 ,  C07C217/16 ,  C07C235/22 ,  C07C217/20 ,  C07C237/22 ,  C07C217/18

CPC分类号： C07C217/18 ,  C07B2200/07 ,  C07C217/16 ,  C07C217/20 ,  C07C235/20 ,  C07C235/22 ,  C07C237/22 ,  C07C2601/14

摘要： The subject of the invention is a group of new derivatives of aminoalkanols, more specifically [(phenoxy)alkyl]aminoalkanols and [(phenoxy)acyl] aminoalkanols, their method of obtaining and their use for production of a medicine which is used in the prophylaxis, prevention and/or treatment of diseases or symptoms having neurological background and for production a medicine with anticonvulsant activity, which is used in seizures of various origin, also in the limbic system, in myoclonic or sound-induced seizures, in psychomotor epilepsy, as well as relieving neuropathic or inflammatory pain.

摘要翻译： 本发明的主题是一组氨基链烷醇的新衍生物，更具体地是[（苯氧基）烷基]氨基链烷醇和[（苯氧基）酰基]氨基链烷醇的衍生物，它们的获得方法和它们用于生产用于预防的药物 ，预防和/或治疗具有神经背景的疾病或症状并用于生产具有抗惊厥活性的药物，其用于各种起源的缉获，也用于边缘系统，肌阵挛或声音诱发的癫痫发作，精神运动性癫痫中，作为 以及缓解神经性或炎性疼痛。

公开(公告)号：US20090192198A1

公开(公告)日：2009-07-30

申请号：US12390318

申请日：2009-02-20

申请人： R. Scott Bitner ,  Kaitlin E. Browman ,  Michael E. Brune ,  Steven Fung ,  Peer B. Jacobson ,  Lynne E. Rueter ,  Marina I. Strakhova ,  Jiahong Wang ,  Jyoti R. Patel ,  Qi Shuai ,  James T. Link ,  Jeffrey J. Rohde ,  Jurgen Dinges ,  Bryan K. Sorensen ,  Martin Winn ,  Hong Yong ,  Vince S. Yeh

发明人： R. Scott Bitner ,  Kaitlin E. Browman ,  Michael E. Brune ,  Steven Fung ,  Peer B. Jacobson ,  Lynne E. Rueter ,  Marina I. Strakhova ,  Jiahong Wang ,  Jyoti R. Patel ,  Qi Shuai ,  James T. Link ,  Jeffrey J. Rohde ,  Jurgen Dinges ,  Bryan K. Sorensen ,  Martin Winn ,  Hong Yong ,  Vince S. Yeh

IPC分类号： A61K31/4439 ,  A61K31/19 ,  A61P35/00 ,  A61K31/165

CPC分类号： C07C235/14 ,  A61K31/165 ,  A61K31/19 ,  A61K31/4439 ,  C07C235/22 ,  C07C237/24 ,  C07C271/28 ,  C07C311/46 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2603/74 ,  C07D207/48 ,  C07D257/04 ,  C07D261/08 ,  C07D295/088 ,  C07D401/04

摘要： The present invention relates to inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.

摘要翻译： 本发明涉及11-β-羟基类固醇脱氢酶1型酶的抑制剂及其在治疗非胰岛素依赖性2型糖尿病，胰岛素抵抗，肥胖症，脂质障碍，代谢综合征，中枢神经系统疾病和疾病中的用途，以及 与过量糖皮质激素有关的病症。

公开(公告)号：US20090043129A1

公开(公告)日：2009-02-12

申请号：US11814483

申请日：2006-01-24

申请人： Antonella Brizzi ,  Vittorio Brizzi ,  Rossella Sirianni ,  Vincenzo Di Marzo ,  Maria Grazia ,  Tiziana Bisogno

发明人： Antonella Brizzi ,  Vittorio Brizzi ,  Rossella Sirianni ,  Vincenzo Di Marzo ,  Maria Grazia ,  Tiziana Bisogno

IPC分类号： C07C233/11 ,  A61K31/165 ,  A61P29/00 ,  A61P3/00 ,  A61P35/00

CPC分类号： C07C235/22 ,  C07C235/20 ,  C07C235/24

摘要： The present invention relates to high affinity compounds, able to bind CB1 and CB2 endocannabinoid receptors. The compounds of the invention find particular application as agents for pain therapy and/or anti-inflammatory and/or anti-stress and/or anti-oxidising and/or hypotensive and/or immune suppressive therapy and/or anti-spastic activity in multiple sclerosis and/or anti-cancer.

摘要翻译： 本发明涉及能够结合CB1和CB2内源性大麻素受体的高亲和力化合物。 本发明的化合物特别用作多种用于疼痛治疗和/或抗炎和/或抗应激和/或抗氧化和/或降血压和/或免疫抑制治疗和/或抗痉挛活性的药剂。 硬化和/或抗癌。

公开(公告)号：US20080306084A1

公开(公告)日：2008-12-11

申请号：US12112406

申请日：2008-04-30

申请人： Stefan Oberboersch ,  Melanie Reich ,  Bernd Sundermann ,  Utz-Peter Jagusch ,  Beatrix Merla ,  Stefan Schunk ,  Werner Englberger ,  Timo Struenker ,  Hagen-Heinrich Hennies ,  Edward Bijsterveld ,  Fritz Theil ,  Heinz Graubaum

发明人： Stefan Oberboersch ,  Melanie Reich ,  Bernd Sundermann ,  Utz-Peter Jagusch ,  Beatrix Merla ,  Stefan Schunk ,  Werner Englberger ,  Timo Struenker ,  Hagen-Heinrich Hennies ,  Edward Bijsterveld ,  Fritz Theil ,  Heinz Graubaum

IPC分类号： A61K31/496 ,  C07D215/36 ,  A61K31/47 ,  C07D401/06

CPC分类号： C07D207/04 ,  C07C233/56 ,  C07C235/20 ,  C07C235/22 ,  C07C311/17 ,  C07C311/20 ,  C07C311/29 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07D211/08 ,  C07D333/20 ,  C07D409/04

摘要： Substituted amide compounds corresponding to formula I: processes for preparing them, pharmaceutical compositions containing these compounds, and the use of substituted amide derivatives for the preparation of medicaments for the treatment of pain and various other conditions.

摘要翻译： 对应于式I的取代的酰胺化合物：其制备方法，含有这些化合物的药物组合物，以及使用取代的酰胺衍生物制备用于治疗疼痛和各种其它病症的药物。

公开(公告)号：US20080064693A1

公开(公告)日：2008-03-13

申请号：US11661470

申请日：2005-08-26

申请人： Libuse Jaroskova ,  Joannes Linders ,  Louis Van Der Veken ,  Gustaaf Willemsens ,  Francois Bischoff

发明人： Libuse Jaroskova ,  Joannes Linders ,  Louis Van Der Veken ,  Gustaaf Willemsens ,  Francois Bischoff

IPC分类号： C07C235/32 ,  A61K31/165 ,  A61K31/195 ,  A61K31/216 ,  A61K31/341 ,  A61K31/343 ,  A61K31/35 ,  A61K31/40 ,  C07D207/00 ,  C07D319/14 ,  C07D317/00 ,  C07D307/77 ,  C07D307/02 ,  C07D307/00 ,  C07D265/36 ,  C07D265/30 ,  C07D211/56 ,  C07C321/00 ,  A61K31/42 ,  A61K31/445 ,  A61K31/536 ,  A61K31/5375 ,  A61P3/00 ,  C07C229/00

CPC分类号： A61K31/165 ,  C07C235/22 ,  C07C237/04 ,  C07C271/38 ,  C07C307/08 ,  C07C311/07 ,  C07C311/09 ,  C07C311/20 ,  C07C2603/74 ,  C07D207/27 ,  C07D263/20 ,  C07D265/36 ,  C07D295/32 ,  C07D307/85 ,  C07D311/66 ,  C07D319/20

摘要： The N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1, 2, 3, or 4; Z represents O, S, NR6, SO or SO2; R1 represent hydrogen, cyano, hydroxy, or C1-4alkyl optionally substituted with halo, R2 represents hydrogen, C1-4alkyl, or C1-4alkyloxy-; R3 represents hydrogen, C1-4alkyl, C1-4alkyloxy- or R3 combined with R2 form together a divalent radical selected from the group consisting of —O—CH2— (a), —NR7—CH2— (b), —(CR8R9)m— (c) and —CR10═ (d) wherein m represents 1 or 2 and R7, R8, R9 and R10 are each independently selected from hydrogen or C1-4alkyl; R4 represents hydrogen, halo, hydroxy, cyano, amino, NR11R12, C1-4alkyloxy-optionally substituted with one or where possible two or three substituents selected from hydroxy and halo or R4 represents C1-4alkyl optionally substituted with one or where possible two or three substituents selected from hydroxy and halo; R5 represents hydrogen, halo, cyano, amino, phenyl, hydroxy, C1-4alkyloxycarbonyl, hydroxycarbonyl, NR13R14 or C1-4alkyl substituted with one or more substituents selected from hydroxycarbonyl, phenyl, C1-4alkyloxy or NR15R16; R6 represents hydrogen; R11 and R12 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; R13 and R14 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; R15 and R16 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; R17 and R18 each independently represent hydrogen, C1-4 alkyl or C1-4alkylcarbonyl-.

公开(公告)号：US20070244198A1

公开(公告)日：2007-10-18

申请号：US11772474

申请日：2007-07-02

申请人： Lanna Li ,  Eva-Lotte Lindstedt Alstermark ,  Christina Olsson

发明人： Lanna Li ,  Eva-Lotte Lindstedt Alstermark ,  Christina Olsson

IPC分类号： A61K31/167 ,  C07C235/16

CPC分类号： C07C233/11 ,  C07B2200/07 ,  C07C233/51 ,  C07C235/20 ,  C07C235/22 ,  C07C235/24 ,  C07C255/46 ,  C07C309/66 ,  C07C323/41 ,  C07C323/56 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D209/14 ,  C07D295/135 ,  C07D295/185

摘要： The present invention provides a compound of formula I processes for preparing such compounds, their the utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance, methods for their therapeutic use and pharmaceutical compositions containing them.

摘要翻译： 本发明提供式I化合物的制备方法，它们可用于治疗包括脂质紊乱（血脂异常）在内的临床症状，不论是否与胰岛素抵抗有关，其治疗用途的方法和含有它们的药物组合物。

公开(公告)号：US20060111406A1

公开(公告)日：2006-05-25

申请号：US10517581

申请日：2003-06-11

申请人： Rafael Ferritto Crespo ,  Jose Martin ,  Maria Martinortega Finger ,  Isabel Rojo Garcia ,  Quanrong Shen ,  Alan Warshawsky ,  Yanping Xu

发明人： Rafael Ferritto Crespo ,  Jose Martin ,  Maria Martinortega Finger ,  Isabel Rojo Garcia ,  Quanrong Shen ,  Alan Warshawsky ,  Yanping Xu

IPC分类号： A61K31/44 ,  A61K31/433 ,  A61K31/428 ,  A61K31/42 ,  A61K31/195 ,  A61K31/381

CPC分类号： C07C235/06 ,  C07C69/734 ,  C07C233/18 ,  C07C235/08 ,  C07C235/14 ,  C07C235/20 ,  C07C235/22 ,  C07C235/24 ,  C07C235/26 ,  C07C235/34 ,  C07C323/41 ,  C07C2601/04 ,  C07C2601/14 ,  C07D211/32 ,  C07D213/40 ,  C07D217/06 ,  C07D277/46 ,  C07D277/82 ,  C07D285/12 ,  C07D285/135 ,  C07D295/18 ,  C07D295/185 ,  C07D317/58 ,  C07D317/60 ,  C07D333/20

摘要： The present invention is directed to compounds, compositions, and use of compounds the structural Formula (I).

摘要翻译： 本发明涉及结构式（I）的化合物，组合物和化合物的用途。