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公开(公告)号:US20190134019A1
公开(公告)日:2019-05-09
申请号:US16239265
申请日:2019-01-03
IPC分类号: A61K31/4465 , C07D211/22 , C07D211/32
CPC分类号: A61K31/4465 , C07D211/22 , C07D211/32
摘要: The invention relates to compounds of formula I: where a, R1, and R3-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
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公开(公告)号:US20180289687A1
公开(公告)日:2018-10-11
申请号:US16007233
申请日:2018-06-13
IPC分类号: A61K31/4465 , C07D211/22 , C07D211/32
CPC分类号: A61K31/4465 , C07D211/22 , C07D211/32
摘要: The invention relates to compounds of formula I: where a, R1, and R3-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
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公开(公告)号:US10071099B2
公开(公告)日:2018-09-11
申请号:US15301438
申请日:2015-04-03
发明人: Kenji Kangawa , Hiroshi Hosoda , Takashi Nojiri
IPC分类号: A61K31/18 , A01N41/06 , C07C311/28 , C07C311/29 , A61K31/5375 , A61K9/00 , A61K31/197 , A61K31/216 , A61K31/277 , A61K31/341 , A61K31/357 , A61K31/381 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4184 , A61K31/4192 , A61K31/42 , A61K31/421 , A61K31/423 , A61K31/426 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/445 , A61K31/4465 , A61K31/454 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/505 , A61K31/517 , A61K31/519 , A61K45/06 , A61K31/192 , A61K31/27 , A61K31/36 , A61K31/40 , A61K31/403 , A61K31/428 , A61K31/438 , A61K31/44 , A61K31/4439 , A61K31/472 , A61K31/554
CPC分类号: A61K31/5375 , A61K9/0053 , A61K31/18 , A61K31/192 , A61K31/197 , A61K31/216 , A61K31/27 , A61K31/277 , A61K31/341 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4184 , A61K31/4192 , A61K31/42 , A61K31/421 , A61K31/423 , A61K31/426 , A61K31/428 , A61K31/438 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4439 , A61K31/445 , A61K31/4465 , A61K31/454 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/505 , A61K31/517 , A61K31/519 , A61K31/554 , A61K45/06
摘要: Provided are a novel medicament for suppressing or preventing the metastasis of a malignant tumor such as carcinoma, a novel treatment or prevention method for suppressing or preventing the metastasis of a malignant tumor, etc. The medicament comprises a non-peptidic angiotensin type 2 receptor agonist as an active ingredient. In the medicament, the non-peptidic angiotensin type 2 receptor agonist may be, for example, a sulfonyl malonamide compound. The medicament may be a medicament for use in combination with an anticancer agent and/or an antitumor agent.
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公开(公告)号:US10034870B2
公开(公告)日:2018-07-31
申请号:US15591419
申请日:2017-05-10
IPC分类号: A61K31/4465 , C07D211/32 , C07D211/22
CPC分类号: A61K31/4465 , C07D211/22 , C07D211/32
摘要: The invention relates to compounds of formula I: where a, R1, and R3-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
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公开(公告)号:US20180209956A1
公开(公告)日:2018-07-26
申请号:US15745587
申请日:2016-07-11
IPC分类号: G01N33/50 , A61K31/05 , A61P35/00 , A61K31/65 , A61K31/353 , A61K31/4468 , A61K31/122 , A61K31/341 , A61K31/19 , C40B30/02
CPC分类号: G01N33/502 , A61K31/05 , A61K31/122 , A61K31/135 , A61K31/164 , A61K31/165 , A61K31/167 , A61K31/19 , A61K31/191 , A61K31/192 , A61K31/341 , A61K31/352 , A61K31/353 , A61K31/381 , A61K31/40 , A61K31/404 , A61K31/4465 , A61K31/4468 , A61K31/4704 , A61K31/4709 , A61K31/52 , A61K31/553 , A61K31/58 , A61K31/65 , A61K31/7048 , A61P35/00 , G01N33/57415 , G01N2500/02 , G01N2500/04 , G16B35/00 , G16C20/60
摘要: Disclosed are methods, compositions, kits, and systems for identifying small-molecule drugs for treating cancer in a subject. The disclosed methods, compositions, kits, and systems may be utilized to identify small-molecule inhibitors of radiation sensitive protein 52 (RAD52) in order to treat cancer in a subject, such as breast cancer in a subject having a BRCA1-deficient, BRCA2-deficient, and/or PALB2-deficient phenotype by administering the identified small-molecule inhibitors to the subject.
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公开(公告)号:US20180125836A1
公开(公告)日:2018-05-10
申请号:US15692894
申请日:2017-08-31
IPC分类号: A61K31/4465 , A61K9/00 , A61K9/08
CPC分类号: A61K31/4465 , A61K9/0019 , A61K9/08
摘要: A method for inhibiting platelet aggregation in a patient in need thereof, comprising 1) administering to the patient a bolus injection of an active drug, in an amount of between about 25 μg/kg, and 2) administering to the patient, after the bolus injection, an intravenous infusion for a period of between about 12 hours and about 72 hours, of the active drug, in an amount of about 0.15 μg/kg/min, wherein the active drug is tirofiban or a salt thereof.
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公开(公告)号:US09884863B2
公开(公告)日:2018-02-06
申请号:US15380798
申请日:2016-12-15
发明人: Jia Zhou , Haijun Chen , Qiang Shen
IPC分类号: C07D471/04 , C07D409/12 , C07D333/64
CPC分类号: C07D471/04 , A61K9/0019 , A61K31/166 , A61K31/167 , A61K31/18 , A61K31/222 , A61K31/381 , A61K31/4245 , A61K31/4436 , A61K31/4465 , A61K31/4535 , A61K31/47 , A61K31/4709 , A61K31/473 , A61K31/495 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K45/06 , C07C235/60 , C07C235/64 , C07C311/08 , C07D211/40 , C07D211/46 , C07D215/52 , C07D265/30 , C07D295/155 , C07D295/24 , C07D333/54 , C07D333/64 , C07D409/12 , C07D413/04 , A61K2300/00
摘要: Provided are STAT3 inhibitors and methods of treating inflammation or a hyperproliferative disease such as, e.g., cancer. In some aspects, compounds may be used to treat breast cancer, a head/neck cancer, a lung cancer, a prostate cancer, or pancreatic cancer.
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公开(公告)号:US20180021322A1
公开(公告)日:2018-01-25
申请号:US15709394
申请日:2017-09-19
IPC分类号: A61K31/4465 , A61K31/451 , A61K31/16
CPC分类号: A61K31/4465 , A61K31/16 , A61K31/451 , C07D211/58 , C07D405/12 , C07D409/12
摘要: The present invention provides a compound of the formula: wherein ring Z is a 5-, 6- or 7-membered ring; R1 is C1-10 alkyl, C1-10 haloalkyl, optionally substituted aralkyl, optionally substituted aryl, optionally substituted heteroaryl or optionally substituted heteroaralkyl; R2 is C1-10 alkylene; and Y is optionally substituted aryl, optionally substituted heteroaryl, or a moiety of the formula —C(═O)-X1, wherein X1 is —OR3 or —NR4R5, where each of R3, R4 and R5 is H or C1-10 alkyl. The present invention also provides a method for using compound of Formula I to treat a wide variety of clinical conditions.
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公开(公告)号:US20170087142A1
公开(公告)日:2017-03-30
申请号:US15377344
申请日:2016-12-13
IPC分类号: A61K31/46 , A61K31/40 , A61K31/454 , A61K31/439 , A61K31/166 , A61K31/325 , A61K31/4465 , A61K31/4178
CPC分类号: A61K31/46 , A61K9/2063 , A61K9/4858 , A61K31/166 , A61K31/27 , A61K31/325 , A61K31/40 , A61K31/4178 , A61K31/439 , A61K31/445 , A61K31/4465 , A61K31/454 , A61K31/4709 , A61K31/55 , A61K45/06 , A61K2300/00
摘要: The present invention relates to a pharmaceutical composition comprising propiverine, trospium or glycopyrrolate; and a non-anticholinergic antiemetic agent. It is also related to a pharmaceutical composition comprising a high dose of solifenacin or a pharmaceutically acceptable salts thereof; and a non-anticholinergic antiemetic agent. Pharmaceutical compositions containing high dose of nsPAChA for use for increasing the AChEI blood concentrations and for combating neurodegeneration are also described. The invention also relates to a method for inducing neuroprotection and combating neurodegeneration in a patient suffering from Alzheimer type dementia as well as to a method for increasing the blood levels of an acetyl choline esterase inhibitor (AChEI) in a human subject treated with an AChEI dose.
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公开(公告)号:US20170014419A1
公开(公告)日:2017-01-19
申请号:US15301438
申请日:2015-04-03
发明人: Kenji KANGAWA , Hiroshi HOSODA , Takashi NOJIRI
IPC分类号: A61K31/5375 , A61K31/216 , A61K31/197 , A61K31/495 , A61K31/445 , A61K31/4465 , A61K31/277 , A61K31/4406 , A61K31/4402 , A61K31/4409 , A61K31/4965 , A61K31/505 , A61K31/415 , A61K31/42 , A61K31/341 , A61K31/381 , A61K31/421 , A61K31/426 , A61K31/47 , A61K31/4184 , A61K31/404 , A61K31/4164 , A61K31/423 , A61K31/4035 , A61K31/517 , A61K31/519 , A61K31/454 , A61K31/496 , A61K31/357 , A61K31/4192 , A61K31/41 , A61K45/06 , A61K9/00 , A61K31/18
CPC分类号: A61K31/5375 , A61K9/0053 , A61K31/18 , A61K31/192 , A61K31/197 , A61K31/216 , A61K31/27 , A61K31/277 , A61K31/341 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4184 , A61K31/4192 , A61K31/42 , A61K31/421 , A61K31/423 , A61K31/426 , A61K31/428 , A61K31/438 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4439 , A61K31/445 , A61K31/4465 , A61K31/454 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/505 , A61K31/517 , A61K31/519 , A61K31/554 , A61K45/06
摘要: Provided are a novel medicament for suppressing or preventing the metastasis of a malignant tumor such as carcinoma, a novel treatment or prevention method for suppressing or preventing the metastasis of a malignant tumor, etc. The medicament comprises a non-peptidic angiotensin type 2 receptor agonist as an active ingredient. In the medicament, the non-peptidic angiotensin type 2 receptor agonist may be, for example, a sulfonyl malonamide compound. The medicament may be a medicament for use in combination with an anticancer agent and/or an antitumor agent.
摘要翻译: 提供了用于抑制或预防恶性肿瘤如癌的转移的新型药物,用于抑制或预防恶性肿瘤转移的新型治疗或预防方法等。该药物包含非肽类血管紧张素2型受体激动剂 作为活性成分。 在药物中,非肽类血管紧张素2型受体激动剂可以是例如磺酰丙酰胺化合物。 药物可以是与抗癌剂和/或抗肿瘤剂组合使用的药物。
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