公开(公告)号：EP3728284B1

公开(公告)日：2024-08-21

申请号：EP18839991.9

申请日：2018-12-21

IPC分类号： C07J43/00 ,  C07J5/00 ,  C07J7/00 ,  C07J9/00 ,  C07J41/00 ,  A61K31/57 ,  A61K31/58 ,  A61K31/56 ,  A61K31/575 ,  A61P25/00 ,  C07J1/00 ,  C07J3/00 ,  C07J13/00 ,  C07J17/00 ,  C07J21/00 ,  C07J51/00 ,  C07J71/00

CPC分类号： C07J1/0011 ,  C07J3/005 ,  C07J5/0015 ,  C07J7/002 ,  C07J7/007 ,  C07J7/0085 ,  C07J9/00 ,  C07J13/007 ,  C07J17/00 ,  C07J21/00 ,  C07J21/008 ,  C07J41/005 ,  C07J41/0066 ,  C07J41/0094 ,  C07J43/003 ,  C07J51/00 ,  C07J71/0005

公开(公告)号：EP3309166A2

公开(公告)日：2018-04-18

申请号：EP17175566.3

申请日：2014-01-23

申请人： Sphaera Pharma Pvt. Ltd.

发明人： Dugar, Sundeep ,  Schreiner, Frederic George ,  Mahajan, Dinesh ,  Sharma, Amit ,  Patil, Ishwar Rakesh ,  Kuila, Bilash

IPC分类号： C07J71/00 ,  C07J5/00 ,  C07J1/00 ,  C07J3/00 ,  C07J7/00 ,  C07J9/00 ,  C07J11/00 ,  C07J17/00 ,  C07J21/00 ,  C07J31/00 ,  C07J41/00 ,  C07J43/00 ,  A61K31/56 ,  A61P21/00

CPC分类号： C07J17/00 ,  C07J1/0011 ,  C07J1/0022 ,  C07J3/005 ,  C07J5/0015 ,  C07J5/0053 ,  C07J7/0005 ,  C07J7/002 ,  C07J7/007 ,  C07J9/00 ,  C07J11/00 ,  C07J21/00 ,  C07J21/006 ,  C07J31/006 ,  C07J41/0011 ,  C07J41/0016 ,  C07J41/0038 ,  C07J41/005 ,  C07J43/003

摘要： The present invention provides novel compounds of 11β-hydroxy steroids and compositions and their application as pharmaceuticals for preventing or reversing injury to mitochondria, for treating or preventing diseases relating to mitochondrial dysfunction or depletion, and for inducing regeneration or restructuring of mitochondria as a means of treating diseases relating to abnormalities in mitochondrial structure and function in a human or animal subject. Also disclosed herein are methods for diagnosing injury to mitochondria and for diagnosing the success or failure of therapeutics designed to treat, prevent, or reverse injury to or depletion of mitochondria.

摘要翻译： 本发明提供了11β-羟基类固醇的新化合物及其组合物及其作为药物用于预防或逆转线粒体损伤，用于治疗或预防与线粒体功能障碍或耗竭有关的疾病，以及诱导线粒体再生或重建作为 治疗与人或动物受试者中线粒体结构和功能异常有关的疾病。 本文还公开了诊断线粒体损伤和诊断设计用于治疗，预防或逆转线粒体损伤或耗竭的治疗成功或失败的方法。

公开(公告)号：EP3243829A1

公开(公告)日：2017-11-15

申请号：EP16001932.9

申请日：2010-05-28

申请人： Ústav Organické Chemie A Biochemie Akademie Ved Ceské Republiky, v.v.i. ,  Fyziologický Ústav Akademie VÊD Ceské Republiky V.V.I. ,  Národní ústav dusevního zdraví

发明人： Chodounská, Hana ,  Stastná, Eva ,  Kapras, Vojtech ,  Kohout, Ladislav ,  Borovská, Jirna ,  Vyklicky, Ladislav ,  Vales, Karel ,  Cais, Ondrej ,  Rambousek, Lukás ,  Stuchlík, Ales ,  Bubeníková Valesová, Vera

IPC分类号： C07J7/00 ,  C07J41/00 ,  A61K31/57 ,  A61P25/02 ,  A61P25/08 ,  A61P25/24 ,  A61P25/18 ,  A61P25/04 ,  A61P25/30 ,  A61P25/28 ,  A61P35/00

CPC分类号： C07J41/005 ,  C07J7/002 ,  Y02P20/55

摘要： The presented invention applies to the compounds with general formula I, where R 1 stands for a group of the general formula R 3 OOC-R 2- C (R 4 )-R 5 -, where R 2 stands for alkyl or alkenyl group with 1 to 18 carbon in a straight or a branching carbon chain, which may be substituted by one or more halogen atoms; R 3 represents either a hydrogen atom or a protecting group of carboxyl groups, preferably benzyl group; R 4 represents oxygen atom, nitrogen atom or a sulfur atom bound by a double bond or R 4 represents two hydrogen atoms; R 5 represents any at least bivalent atom, preferably an oxygen atom, nitrogen, or carbon atom, except when R 2 represents the group -(CH 2 ) n - where n = 0-3 and simultaneously R 3 represents a hydrogen atom and R 4 and R 5 represent an oxygen atom. The present invention also relates to the production process of the compounds with general formula I, where R 1 stands for as mentioned previously, the compounds with general formula I for use in treatment of various diseases of central nervous system, in treatment of neuropsychiatric disorders related to imbalance of glutamatergic neurotransmitter system, ischemic damage of CNS, neurodegenerative changes and disorders of CNS, affective disorders, depression, PTSD and other diseases related to stress, anxiety, schizophrenia and psychotic disorders, pain, addictions, multiple sclerosis, epilepsy and gliomas.
This invention further applies to the compounds with general formula I for use in the production of veterinary and human pharmaceutical preparations for use in treatment of above mentioned diseases as well as in production of substances used in experimental research, analytic chemistry, dietary supplements or cosmetic preparations.

摘要翻译： 本发明适用于具有通式I的化合物，其中R 1代表通式R 3 OOC-R 2 -C（R 4）-R 5 - 的基团，其中R 2代表烷基或烯基，其中1-18碳 直链或支链碳链，其可以被一个或多个卤素原子取代; R 3表示氢原子或羧基的保护基，优选苄基; R4表示氧原子，氮原子或通过双键结合的硫原子或R4表示两个氢原子; 除了当R 2代表基团 - （CH 2）n - 时，其中n = 0〜3，同时R 3代表氢原子，R 4和R 5代表一个至少是二价原子，优选氧原子，氮或碳原子 氧原子。 本发明还涉及具有通式I的化合物的制备方法，其中R1如前所述，具有通式I的化合物用于治疗各种中枢神经系统疾病，用于治疗与神经精神病相关的神经精神障碍 谷氨酸能神经递质系统失衡，中枢神经系统缺血性损伤，中枢神经系统的神经退行性改变和障碍，情感障碍，抑郁症，创伤后应激障碍和其他与压力，焦虑，精神分裂症和精神病性障碍，疼痛，成瘾，多发性硬化症，癫痫和神经胶质瘤有关的疾病。 本发明进一步适用于具有通式I的化合物，用于生产用于治疗上述疾病以及用于实验研究，分析化学，膳食补充剂或化妆品制剂的物质的生产的兽药和人药物制剂 。

公开(公告)号：EP2435463B1

公开(公告)日：2016-10-12

申请号：EP10744655.1

申请日：2010-05-28

申请人： Ústav Organické Chemie Biochemie Akademie Ved Ceské Republiky, V.V.I. ,  Fyziologický Ústav Akademie VÊD Ceské Republiky V.V.I. ,  Národní ústav dusevního zdraví

发明人： CHODOUNSKÁ, Hana ,  STASTNÁ, Eva ,  KAPRAS, Vojtech ,  KOHOUT, Ladislav ,  BOROVSKÁ, Jirna ,  VYKLICKY, Ladislav ,  VALES, Karel ,  CAIS, Ondrej ,  RAMBOUSEK, Lukás ,  STUCHLÍK, Ales ,  BUBENÍKOVÁ VALESOVÁ, Vera

IPC分类号： C07J7/00 ,  C07J41/00 ,  A61K31/57 ,  A61P25/02 ,  A61P25/08 ,  A61P25/24 ,  A61P25/18 ,  A61P25/04 ,  A61P25/30 ,  A61P25/28 ,  A61P35/00

CPC分类号： C07J41/005 ,  C07J7/002 ,  Y02P20/55

摘要： The presented invention applies to the compounds with general formula I, where R 1 stands for a group of the general formula R 3 OOC-R 2- C (R 4 )-R 5 -, where R 2 stands for alkyl or alkenyl group with 1 to 18 carbon in a straight or a branching carbon chain, which may be substituted by one or more halogen atoms; R 3 represents either a hydrogen atom or a protecting group of carboxyl groups, preferably benzyl group; R 4 represents oxygen atom, nitrogen atom or a sulfur atom bound by a double bond or R 4 represents two hydrogen atoms; R 5 represents any at least bivalent atom, preferably an oxygen atom, nitrogen, or carbon atom, except when R 2 represents the group -(CH 2 ) n - where n = 0-3 and simultaneously R 3 represents a hydrogen atom and R 4 and R 5 represent an oxygen atom. The present invention also relates to the production process of the compounds with general formula I, where R 1 stands for as mentioned previously, the compounds with general formula I for use in treatment of various diseases of central nervous system, in treatment of neuropsychiatric disorders related to imbalance of glutamatergic neurotransmitter system, ischemic damage of CNS, neurodegenerative changes and disorders of CNS, affective disorders, depression, PTSD and other diseases related to stress, anxiety, schizophrenia and psychotic disorders, pain, addictions, multiple sclerosis, epilepsy and gliomas. This invention further applies to the compounds with general formula I for use in the production of veterinary and human pharmaceutical preparations for use in treatment of above mentioned diseases as well as in production of substances used in experimental research, analytic chemistry, dietary supplements or cosmetic preparations.

公开(公告)号：EP2675821A1

公开(公告)日：2013-12-25

申请号：EP12711108.6

申请日：2012-02-15

申请人： Ústav Organické Chemie A Biochemie Akademie Ved Ceské Republiky, v.v.i. ,  Fyziologicky Ústav Akademie VED Ceské Republiky, V.V.I.

发明人： CHODOUNSKÁ, Hana ,  KAPRAS, Vojtech ,  VYKLICKY, Ladislav ,  BOROVSKÁ, Jirina ,  VYKLICKY, Vojtech ,  VALES , Karel ,  STUCHLÍK, Ales ,  RAMBOUSEK, Lukás

IPC分类号： C07J41/00 ,  C07J75/00 ,  A61K31/57 ,  A61P25/00 ,  A61P25/24 ,  A61P25/28

CPC分类号： C07J41/0011 ,  C07J41/0005 ,  C07J41/005

摘要： Pregnanolone derivatives, substituted in 3 alpha-position with the cationic group, of general formula I, and a method of the production of these compounds and their utilization for treatment of neuropsychiatric disorders related to imbalance of glutamatergic neurotransmitter system, such as ischemic damage of CNS, neurodegenerative changes and disorders of CNS, affective disorders, depression, post traumatic stress disorder, and other diseases related to stress, anxiety, schizophrenia, and psychotic disorders, pain, addictions, multiple sclerosis, epilepsy, and gliomas. The compounds are also used for production of veterinary and human pharmaceutical preparation for treatment of above mentioned diseases and for production of pharmaceutical preparations containing these compounds.

摘要翻译： 孕衍生物，substituiertem与阳离子基团3α-位中，通式I，和生产合成化合物的方法及其在治疗与谷氨酸能神经递质系统，颜色的不平衡神经精神障碍的利用：例如CNS的缺血性损伤 ，神经退行性变化和中枢神经系统的障碍，情感障碍，抑郁症，创伤后应激障碍，以及与应激，焦虑症，精神分裂症，和精神障碍，疼痛，成瘾，多发性硬化，癫痫，神经胶质瘤和其他疾病。 因此，该化合物用于制造用于治疗上述疾病的兽医和人类药物制剂和生产含有合成化合物的药物制剂。

公开(公告)号：EP2318427B1

公开(公告)日：2013-10-23

申请号：EP09780232.6

申请日：2009-07-07

申请人： Nicox S.A.

发明人： BENEDINI, Francesca ,  BONFANTI, Annalisa ,  CHIROLI, Valerio ,  STEELE, Rebecca ,  ONGINI, Ennio ,  BIONDI, Stefano

IPC分类号： C07J41/00 ,  C07J71/00 ,  A61K31/573 ,  A61P5/44 ,  A61P27/02

CPC分类号： C07J71/0031 ,  C07J41/005

公开(公告)号：EP2625190A2

公开(公告)日：2013-08-14

申请号：EP11819158.4

申请日：2011-10-06

申请人： Justus-Liebig- Universitat Giessen

发明人： BECKER, Katja ,  KRIEG, Reimar ,  SCHÖNECKER, Bruno

IPC分类号： C07J41/00 ,  A61K31/56 ,  A61P31/04 ,  A61P31/10 ,  A61P31/12 ,  A61P33/00

CPC分类号： C07J11/00 ,  A61K31/56 ,  A61K45/06 ,  C07J41/005 ,  Y02A50/382 ,  Y02A50/385 ,  Y02A50/387 ,  Y02A50/389 ,  Y02A50/393 ,  Y02A50/406 ,  Y02A50/409 ,  Y02A50/411 ,  Y02A50/414 ,  Y02A50/423 ,  Y02A50/463 ,  Y02A50/465 ,  Y02A50/471 ,  Y02A50/491 ,  Y02A50/492

摘要： The invention relates to steroid-derived compounds of general formula (I) wherein L is a linker and R
# is a steroid group, and to the use of the compounds of general formula (I) in medicine and for the prophylaxis and/or treatment of infectious diseases. The invention also relates to pharmaceutical compositions containing at least one compound of general formula (I), and to the synthesis of the compounds of general formula (I).

公开(公告)号：EP2611821A2

公开(公告)日：2013-07-10

申请号：EP11805619.1

申请日：2011-09-02

申请人： Cadila Healthcare Limited

发明人： SOLANKI, Kirtipalsinh ,  BAVADIA, Ruchir Z ,  PATEL, Dhaval P ,  PATEL, Dhaval J ,  SHAH, Tejash C ,  SINGH, Manoj Kumar

IPC分类号： C07J31/00 ,  C07J41/00

CPC分类号： C07J31/00 ,  C07J31/006 ,  C07J41/005

摘要： The present invention relates to an improved process for the preparation of substituted Fluticasone derivatives. The invention also reveals the processes for the purification of Fluticasones and related intermediates to provide the highly pure product.

摘要翻译： 本发明涉及一种制备取代的氟替卡松衍生物的改进方法。 本发明还揭示了Fluticasones和相关中间体的纯化方法，以提供高纯度的产品。

公开(公告)号：EP2109618A1

公开(公告)日：2009-10-21

申请号：EP08708271.5

申请日：2008-01-28

申请人： Nicox S.A.

发明人： BENEDINI, Francesca ,  BIONDI, Stefano ,  ONGINI, Ennio

IPC分类号： C07J41/00 ,  A61K31/573 ,  A61P5/44

CPC分类号： C07J41/005

摘要： The invention relates to nitrooxyderivative of corticosteroids of general formula (I) and pharmaceutically acceptable salts or stereoisomers thereof wherein R is the corticosteroid residue of formula (II): The compounds are useful in the treatment of respiratory diseases, inflammatory diseases, dermatological diseases and oculardiseases.

公开(公告)号：EP1294402B1

公开(公告)日：2006-01-11

申请号：EP01943329.1

申请日：2001-05-08

申请人： Schering AG

发明人： ELGER, Walter ,  HILLISCH, Alexander ,  HEDDEN, Annemarie ,  SCHWARZ, Sigfrid ,  SCHÖLLKOPF, Klaus

IPC分类号： A61K47/20 ,  A61K31/565 ,  A61K31/566 ,  A61K31/568 ,  A61K31/49 ,  A61K31/4045 ,  A61P43/00

CPC分类号： C07J41/0044 ,  C07J41/0038 ,  C07J41/005

摘要： The invention relates to compounds which, acting as a prodrug and/or support, enable an active agent to be taken up by the erythrocytes and/or an active agent to bind to the erythrocytes. The uptake of these compounds by and/or the binding thereof to the erythrocytes is made possible by a group of formula -SO2NR R , wherein R and R , independently of each other, mean a hydrogen atom, an acyl group, an alkyl group, a cycloalkyl group, an aryl group, a cyano group or a hydroxy group. The inventive prodrugs enable active agents such as endogenic substances, natural substances and synthetic substances with therapeutically useful properties which have a high "first path" effect, to be administered orally effectively or significantly improve the oral activity thereof.