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1. 发明申请

US20210000818A1 METHODS FOR TREATING DEPRESSIVE SYMPTOMS 有权
公开(公告)号：US20210000818A1
公开(公告)日：2021-01-07
申请号：US16913404
申请日：2020-06-26
申请人： Alkermes Pharma Ireland Limited
发明人： Laura Cook Blumberg , Daniel R. Deaver , David J. Eyerman , Thomas Andrew Wynn
IPC分类号： A61K31/485 , C07D211/62 , C07D217/04 , C07D221/22 , C07D221/28 , C07D223/04 , C07D401/12 , C07D405/12 , C07D489/00 , C07D489/09
摘要： The present application relates methods for treating a depressive symptom comprising administering an effective amount of a μ opioid receptor agonist or a pharmaceutically acceptable salt thereof to a subject in need thereof. Non-limiting examples of such agonist include the compounds of Formulas I, II, III, and IV, as well as the compounds of Table A.

2. 发明授权

US06887998B2 Process for 8-carboxamido-2,6-methano-3-benzazocines 有权
标题翻译： 8-甲酰胺基-2,6-亚甲基-3-苯并吖嗪的方法
公开(公告)号：US06887998B2
公开(公告)日：2005-05-03
申请号：US10409803
申请日：2003-04-09
申请人： Mark P. Wentland
发明人： Mark P. Wentland
IPC分类号： A61K31/4748 , A61K31/485 , A61P1/00 , A61P1/06 , A61P1/12 , A61P3/04 , A61P9/10 , A61P11/00 , A61P11/14 , A61P13/02 , A61P17/04 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/08 , A61P25/28 , A61P25/30 , A61P25/36 , A61P29/00 , A61P37/06 , A61P43/00 , C07B61/00 , C07D221/26 , C07D401/04 , C07D405/06 , C07D489/00 , C07D489/08 , C07D489/09 , C07D489/10 , C07D491/20 , C07D491/22 , C07D515/08 , C07D489/02
CPC分类号： C07D489/12 , A61K31/485 , C07D221/22 , C07D221/26 , C07D401/04 , C07D405/06 , C07D489/00 , C07D489/02 , C07D489/08 , C07D489/10 , C07D491/18
摘要： 8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH2—OH, —CH2NH2, —NHSO2CH3, and Y is O, S or NOH are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications. 8-Carboxamides, thiocarboxamides, hydroxyamidines and formamides are preferred.
摘要翻译：一般结构I的8-取代的2,6-亚甲基-3-苯并吖嗪，其中A是-CH 2 -OH，-CH 2 NH 2， / SO 2，NHSO 2 CH 3，Y为O，S或NOH可用作止痛剂，抗腹泻剂，抗惊厥药，镇咳药和抗瘾药物。 8-羧酰胺，硫代甲酰胺，羟脒和甲酰胺是优选的。

3. 发明申请

US20050038061A1 6-Aminomorphinane derivatives, method for production and use thereof 失效
标题翻译： 6-氨基吗啡烷衍生物，其制备方法和用途
公开(公告)号：US20050038061A1
公开(公告)日：2005-02-17
申请号：US10499133
申请日：2002-12-16
申请人： Johannes Schutz , Helmut Schmidhammer
发明人： Johannes Schutz , Helmut Schmidhammer
IPC分类号： A61K31/485 , A61P1/04 , A61P1/10 , A61P1/12 , A61P1/16 , A61P3/04 , A61P5/40 , A61P7/10 , A61P9/00 , A61P9/08 , A61P9/10 , A61P11/00 , A61P13/12 , A61P15/00 , A61P19/00 , A61P19/02 , A61P21/00 , A61P23/00 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/32 , A61P25/36 , A61P29/00 , A61P29/02 , A61P35/00 , A61P37/02 , A61P37/04 , A61P37/06 , C07D489/08 , C07D489/09
CPC分类号： C07D489/08 , A61K31/485
摘要： This invention relates to compounds of the formula (I).
摘要翻译：本发明涉及式（I）化合物。

4. 发明授权

US5578725A Delta opioid receptor antagonists 失效
标题翻译： Delta阿片受体拮抗剂
公开(公告)号：US5578725A
公开(公告)日：1996-11-26
申请号：US380091
申请日：1995-01-30
申请人： Philip S. Portoghese , Francine S. Farouz-Grant
发明人： Philip S. Portoghese , Francine S. Farouz-Grant
IPC分类号： C07D489/09 , C07D491/20 , C07D489/10
CPC分类号： C07D491/20
摘要： Compounds are provided of the formula: ##STR1## wherein R.sup.1 is (C.sub.1 -C.sub.5)alkyl, C.sub.3 -C.sub.6 (cycloalkyl)alkyl, C.sub.5 -C.sub.7 (cycloalkenyl)alkyl, (C.sub.6 -C.sub.12)aryl, (C.sub.6 -C.sub.12)aralkyl, trans(C.sub.4 -C.sub.5)alkenyl, allyl or furan-2-ylalkyl, R.sup.2 is H, OH or O.sub.2 C(C.sub.1 -C.sub.5)alkyl; R.sup.3 is H, (C.sub.6 -C.sub.10)aralkyl, (C.sub.1 -C.sub.5)alky or (C.sub.1 -C.sub.5)alkylCO; X is O, S or NY, wherein Y is H, benzyl or (C.sub.1 -C.sub.5)alkyl; R is CH(Z)CO.sub.2 Y, wherein Z is H, CH.sub.2 CO.sub.2 Y or (CH.sub.2).sub.n N(R.sup.4)(R.sup.5), wherein n is 1-5 and R.sup.4 and R.sup.5 are individually H, (C.sub.1 -C.sub.4)alkyl, phenyl, (C.dbd.NH)NH.sub.2, benzyloxycarbonyl or (C.dbd.NHNO.sub.2); and the pharmaceutically acceptable salts thereof.
摘要翻译：化合物由下式提供：其中R1是（C1-C5）烷基，C3-C6（环烷基）烷基，C5-C7（环烯基）烷基，（C6-C12）芳基，（C6-C12）芳烷基，反式（C 4 -C 5）烯基，烯丙基或呋喃-2-基烷基，R 2是H，OH或O 2 C（C 1 -C 5）烷基; R3是H，（C6-C10）芳烷基，（C1-C5）烷基或（C1-C5）烷基CO; X是O，S或NY，其中Y是H，苄基或（C1-C5）烷基; R是CH（Z）CO 2 Y，其中Z是H，CH 2 CO 2 Y或（CH 2）n N（R 4）（R 5），其中n是1-5，R 4和R 5分别是H，（C 1 -C 4）烷基，苯基，（ C = NH）NH 2，苄氧羰基或（C = NHNO 2）; 及其药学上可接受的盐。

5. 发明授权

US5436249A Opioid agonist compounds 失效
标题翻译：阿片样物质激动剂化合物
公开(公告)号：US5436249A
公开(公告)日：1995-07-25
申请号：US243661
申请日：1994-05-16
申请人： Michael S. Dappen , Barnett S. Pitzele , Michael F. Rafferty
发明人： Michael S. Dappen , Barnett S. Pitzele , Michael F. Rafferty
IPC分类号： C07D489/09 , C07D491/20 , C07D495/20 , A61K31/44 , C07D491/12
CPC分类号： C07D491/20 , C07D495/20
摘要： The present invention provides novel substituted opioid analgesic compounds of Formula I: ##STR1## which are opioid agonists, and which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
摘要翻译：本发明提供式I的新颖的取代的阿片样物质镇痛化合物：作为阿片样物质激动剂的式I化合物，其可用作治疗疼痛的止痛剂，药物组合物包含治疗有效量的式I化合物与药学上可接受的载体组合，以及用于消除或改善动物疼痛的方法，包括向动物施用治疗有效量的式I化合物。

6. 发明授权

US11534436B2 Methods for treating depressive symptoms 有权
公开(公告)号：US11534436B2
公开(公告)日：2022-12-27
申请号：US16913404
申请日：2020-06-26
申请人： Alkermes Pharma Ireland Limited
发明人： Laura Cook Blumberg , Daniel R. Deaver , David J. Eyerman , Thomas Andrew Wynn
IPC分类号： A61K31/485 , C07D211/62 , C07D217/04 , C07D221/22 , C07D221/28 , C07D223/04 , C07D401/12 , C07D405/12 , C07D489/00 , C07D489/09
摘要： The present application relates methods for treating a depressive symptom comprising administering an effective amount of a μ opioid receptor agonist or a pharmaceutically acceptable salt thereof to a subject in need thereof. Non-limiting examples of such agonist include the compounds of Formulas I, II, III, and IV, as well as the compounds of Table A.

7. 发明申请

US20200325146A1 OPIOID KETAL COMPOUNDS AND USES THEREOF 审中-公开
公开(公告)号：US20200325146A1
公开(公告)日：2020-10-15
申请号：US16860316
申请日：2020-04-28
申请人： Rhodes Technologies
发明人： Robert J. KUPPER , Raymond C. GLOWAKY
IPC分类号： C07D489/08 , C07D491/20 , C07D489/09 , A61K9/00 , A61K31/485 , A61K45/06 , C07D489/02
摘要： This invention relates to opioid ketal compounds of Formula (I), Formula (II), or Formula (III): or a pharmaceutically acceptable salts thereof, wherein R1 is H or CH3, R2 is H or OH, n is 0, 1, 2 or 3, R3 and R4 are independently H or optionally substituted C1-C4 alkyl, or when n is 0, then R3 and R4 and the carbon atoms to which they are attached together form six, or seven membered ring, which is optionally mono or disubstituted by C1-C4 alkyl. The invention also relates to oxycodone ketal compounds of Formula (IV) or (V): or a pharmaceutically acceptable salts thereof. The invention also relates to the use of such compounds for the treatment, prevention, or amelioration of pain.

8. 发明申请

US20100081815A1 Recycling process for increasing the yield of opiate alkaloid derivatives 有权
标题翻译：提高阿片类生物碱衍生物产量的回收方法
公开(公告)号：US20100081815A1
公开(公告)日：2010-04-01
申请号：US12586856
申请日：2009-09-29
申请人： Dennis J. Kalota
发明人： Dennis J. Kalota
IPC分类号： C07D221/22 , C07D489/09
CPC分类号： C07D489/12 , Y02P20/582
摘要： The present invention provides processes for the production of opiate alkaloids. In particular, the present invention provides processes for increasing the yield of opiate alkaloids by introducing at least one recycling step.
摘要翻译：本发明提供了生产阿片碱生物碱的方法。特别地，本发明提供通过引入至少一个回收步骤来提高阿片碱生物碱的产量的方法。

9. 发明授权

US6136817A Opioid receptor antagonist compounds 失效
标题翻译：阿片受体拮抗剂化合物
公开(公告)号：US6136817A
公开(公告)日：2000-10-24
申请号：US507369
申请日：1995-08-22
申请人： Helmut Schmidhammer
发明人： Helmut Schmidhammer
IPC分类号： A61K31/445 , A61P25/02 , A61P25/04 , A61P29/00 , A61P37/06 , C07D489/09 , C07D491/18 , C07D495/16 , A61K31/485
CPC分类号： C07D491/18
摘要： New morphinane derivatives of the formula ##STR1## their pharmaceutically acceptable salts, a process for their preparation and their use in the manufacture of pharmaceutical preparations.
摘要翻译： PCT No.PCT / SE95 / 00503 Sec。 371日期：1995年8月22日 102（e）日期1995年8月22日PCT提交1995年5月9日PCT公布。 WO95 / 31463 PCT出版物日期1995年11月23日公式的新型吗啡衍生物其药学上可接受的盐，其制备方法及其在制备药物制剂中的用途。

10. 发明授权

US5332818A Immunosuppressive agent and process of producing the same 失效
标题翻译：免疫抑制剂及其制备方法
公开(公告)号：US5332818A
公开(公告)日：1994-07-26
申请号：US34669
申请日：1993-03-22
申请人： Hiroshi Nagase , Koji Kawai , Shu Matsumoto , Takashi Endoh , Yoshiaki Katsura , Kohei Arakawa
发明人： Hiroshi Nagase , Koji Kawai , Shu Matsumoto , Takashi Endoh , Yoshiaki Katsura , Kohei Arakawa
IPC分类号： C07D489/09 , A61K20060101 , A61K31/485 , A61P25/04 , A61P37/06 , C07D491/18 , C07D491/20 , C07D721/72
CPC分类号： C07D491/18 , A61K31/485 , C07D491/20
摘要： An immunosuppressive agent which has low toxicity and which exhibits excellent effectiveness even if it is orally administered is presented. The immunosuppressive agent of the present invention is characterized in that it contains .delta.-opioid antagonist having high selectivity to .delta.-opioid receptor. The present invention also provides a process of producing a naltrindole derivative characterized by reacting naltrexone or a salt thereof with a phenylhydrazine derivative in a solvent in the presence of methanesulfonic acid.
摘要翻译：本发明提供一种毒性低，即使口服给药也具有优异效果的免疫抑制剂。本发明的免疫抑制剂的特征在于其含有对δ-阿片受体具有高选择性的δ-阿片样物质拮抗剂。本发明还提供一种制备纳吲哚衍生物的方法，其特征在于在甲磺酸存在下，在溶剂中使纳曲酮或其盐与苯肼衍生物反应。

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