JP2013501806A5 - - Google Patents
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- JP2013501806A5 JP2013501806A5 JP2012524868A JP2012524868A JP2013501806A5 JP 2013501806 A5 JP2013501806 A5 JP 2013501806A5 JP 2012524868 A JP2012524868 A JP 2012524868A JP 2012524868 A JP2012524868 A JP 2012524868A JP 2013501806 A5 JP2013501806 A5 JP 2013501806A5
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- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- composition
- compound
- formula
- pharmaceutically acceptable
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 239000000203 mixture Substances 0.000 claims description 118
- 239000008194 pharmaceutical composition Substances 0.000 claims description 101
- 150000001875 compounds Chemical class 0.000 claims description 71
- WWZKQHOCKIZLMA-UHFFFAOYSA-N octanoic acid Chemical compound CCCCCCCC(O)=O WWZKQHOCKIZLMA-UHFFFAOYSA-N 0.000 claims description 59
- 150000003839 salts Chemical class 0.000 claims description 49
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 claims description 43
- 238000000034 method Methods 0.000 claims description 36
- 239000005635 Caprylic acid (CAS 124-07-2) Substances 0.000 claims description 27
- 229960002446 octanoic acid Drugs 0.000 claims description 27
- 238000001990 intravenous administration Methods 0.000 claims description 24
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims description 22
- 229960003511 macrogol Drugs 0.000 claims description 22
- BKVAAWMQOQLENB-UHFFFAOYSA-N 15-hydroxy stearic acid Chemical compound CCCC(O)CCCCCCCCCCCCCC(O)=O BKVAAWMQOQLENB-UHFFFAOYSA-N 0.000 claims description 20
- 229940057917 medium chain triglycerides Drugs 0.000 claims description 20
- 238000009472 formulation Methods 0.000 claims description 19
- 206010028813 Nausea Diseases 0.000 claims description 17
- 230000008693 nausea Effects 0.000 claims description 17
- 150000003626 triacylglycerols Chemical class 0.000 claims description 17
- 206010047700 Vomiting Diseases 0.000 claims description 16
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 12
- 238000002512 chemotherapy Methods 0.000 claims description 12
- 239000000693 micelle Substances 0.000 claims description 12
- 150000003904 phospholipids Chemical class 0.000 claims description 12
- 239000003549 soybean oil Substances 0.000 claims description 12
- 235000012424 soybean oil Nutrition 0.000 claims description 12
- LADGBHLMCUINGV-UHFFFAOYSA-N tricaprin Chemical compound CCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCC)COC(=O)CCCCCCCCC LADGBHLMCUINGV-UHFFFAOYSA-N 0.000 claims description 12
- 150000004668 long chain fatty acids Chemical class 0.000 claims description 10
- 239000003981 vehicle Substances 0.000 claims description 10
- 241000288906 Primates Species 0.000 claims description 8
- 230000001154 acute effect Effects 0.000 claims description 8
- 239000000839 emulsion Substances 0.000 claims description 8
- 239000004530 micro-emulsion Substances 0.000 claims description 8
- 239000008363 phosphate buffer Substances 0.000 claims description 8
- VMPHSYLJUKZBJJ-UHFFFAOYSA-N trilaurin Chemical compound CCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCC)COC(=O)CCCCCCCCCCC VMPHSYLJUKZBJJ-UHFFFAOYSA-N 0.000 claims description 8
- 230000008673 vomiting Effects 0.000 claims description 7
- 206010028980 Neoplasm Diseases 0.000 claims description 6
- 239000000872 buffer Substances 0.000 claims description 6
- 201000011510 cancer Diseases 0.000 claims description 6
- 235000011187 glycerol Nutrition 0.000 claims description 6
- SHBUUTHKGIVMJT-UHFFFAOYSA-N Hydroxystearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OO SHBUUTHKGIVMJT-UHFFFAOYSA-N 0.000 claims description 5
- 208000031649 Postoperative Nausea and Vomiting Diseases 0.000 claims description 5
- 229940072106 hydroxystearate Drugs 0.000 claims description 5
- 239000003921 oil Substances 0.000 claims description 5
- 235000019198 oils Nutrition 0.000 claims description 5
- LVGKNOAMLMIIKO-UHFFFAOYSA-N Elaidinsaeure-aethylester Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC LVGKNOAMLMIIKO-UHFFFAOYSA-N 0.000 claims description 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 4
- 206010018910 Haemolysis Diseases 0.000 claims description 4
- 241001465754 Metazoa Species 0.000 claims description 4
- 235000019483 Peanut oil Nutrition 0.000 claims description 4
- 235000019485 Safflower oil Nutrition 0.000 claims description 4
- -1 alkali metal salt Chemical class 0.000 claims description 4
- 125000000217 alkyl group Chemical group 0.000 claims description 4
- 150000001413 amino acids Chemical class 0.000 claims description 4
- 230000001430 anti-depressive effect Effects 0.000 claims description 4
- 239000000935 antidepressant agent Substances 0.000 claims description 4
- 229940005513 antidepressants Drugs 0.000 claims description 4
- 239000004359 castor oil Substances 0.000 claims description 4
- 235000019438 castor oil Nutrition 0.000 claims description 4
- 229960001777 castor oil Drugs 0.000 claims description 4
- 150000001768 cations Chemical class 0.000 claims description 4
- 235000005687 corn oil Nutrition 0.000 claims description 4
- 239000002285 corn oil Substances 0.000 claims description 4
- 235000012343 cottonseed oil Nutrition 0.000 claims description 4
- 239000002385 cottonseed oil Substances 0.000 claims description 4
- 230000000095 emetic effect Effects 0.000 claims description 4
- LVGKNOAMLMIIKO-QXMHVHEDSA-N ethyl oleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC LVGKNOAMLMIIKO-QXMHVHEDSA-N 0.000 claims description 4
- 229940093471 ethyl oleate Drugs 0.000 claims description 4
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims description 4
- 238000010438 heat treatment Methods 0.000 claims description 4
- 230000008588 hemolysis Effects 0.000 claims description 4
- HBOQXIRUPVQLKX-UHFFFAOYSA-N linoleic acid triglyceride Natural products CCCCCC=CCC=CCCCCCCCC(=O)OCC(OC(=O)CCCCCCCC=CCC=CCCCCC)COC(=O)CCCCCCCC=CCC=CCCCCC HBOQXIRUPVQLKX-UHFFFAOYSA-N 0.000 claims description 4
- 150000002632 lipids Chemical class 0.000 claims description 4
- 239000004006 olive oil Substances 0.000 claims description 4
- 235000008390 olive oil Nutrition 0.000 claims description 4
- 235000021315 omega 9 monounsaturated fatty acids Nutrition 0.000 claims description 4
- 239000000312 peanut oil Substances 0.000 claims description 4
- 235000005713 safflower oil Nutrition 0.000 claims description 4
- 239000003813 safflower oil Substances 0.000 claims description 4
- 239000008159 sesame oil Substances 0.000 claims description 4
- 235000011803 sesame oil Nutrition 0.000 claims description 4
- 239000010686 shark liver oil Substances 0.000 claims description 4
- 229940069764 shark liver oil Drugs 0.000 claims description 4
- VLPFTAMPNXLGLX-UHFFFAOYSA-N trioctanoin Chemical group CCCCCCCC(=O)OCC(OC(=O)CCCCCCC)COC(=O)CCCCCCC VLPFTAMPNXLGLX-UHFFFAOYSA-N 0.000 claims description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 4
- 239000003795 chemical substances by application Substances 0.000 claims description 3
- 238000001802 infusion Methods 0.000 claims description 3
- DCXXMTOCNZCJGO-UHFFFAOYSA-N tristearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCCCCCC)COC(=O)CCCCCCCCCCCCCCCCC DCXXMTOCNZCJGO-UHFFFAOYSA-N 0.000 claims description 3
- 239000004475 Arginine Substances 0.000 claims description 2
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims description 2
- XBPCUCUWBYBCDP-UHFFFAOYSA-N Dicyclohexylamine Chemical compound C1CCCCC1NC1CCCCC1 XBPCUCUWBYBCDP-UHFFFAOYSA-N 0.000 claims description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical group Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 2
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 2
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims description 2
- 239000004472 Lysine Substances 0.000 claims description 2
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims description 2
- MBBZMMPHUWSWHV-BDVNFPICSA-N N-methylglucamine Chemical compound CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO MBBZMMPHUWSWHV-BDVNFPICSA-N 0.000 claims description 2
- 239000002202 Polyethylene glycol Substances 0.000 claims description 2
- 206010066962 Procedural nausea Diseases 0.000 claims description 2
- 206010066963 Procedural vomiting Diseases 0.000 claims description 2
- 239000004480 active ingredient Substances 0.000 claims description 2
- 239000008186 active pharmaceutical agent Substances 0.000 claims description 2
- 229910052783 alkali metal Inorganic materials 0.000 claims description 2
- 229910052784 alkaline earth metal Inorganic materials 0.000 claims description 2
- 150000003863 ammonium salts Chemical class 0.000 claims description 2
- 239000002260 anti-inflammatory agent Substances 0.000 claims description 2
- 229940121363 anti-inflammatory agent Drugs 0.000 claims description 2
- 239000002246 antineoplastic agent Substances 0.000 claims description 2
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims description 2
- 239000008280 blood Substances 0.000 claims description 2
- 210000004369 blood Anatomy 0.000 claims description 2
- 230000037396 body weight Effects 0.000 claims description 2
- 229910052791 calcium Inorganic materials 0.000 claims description 2
- 239000011575 calcium Substances 0.000 claims description 2
- 230000000973 chemotherapeutic effect Effects 0.000 claims description 2
- 229940127089 cytotoxic agent Drugs 0.000 claims description 2
- 235000014113 dietary fatty acids Nutrition 0.000 claims description 2
- 229930195729 fatty acid Natural products 0.000 claims description 2
- 239000000194 fatty acid Substances 0.000 claims description 2
- 150000004665 fatty acids Chemical class 0.000 claims description 2
- 229940028435 intralipid Drugs 0.000 claims description 2
- 239000002502 liposome Substances 0.000 claims description 2
- 229910052749 magnesium Inorganic materials 0.000 claims description 2
- 239000011777 magnesium Substances 0.000 claims description 2
- 239000002736 nonionic surfactant Substances 0.000 claims description 2
- 150000007530 organic bases Chemical class 0.000 claims description 2
- 239000003960 organic solvent Substances 0.000 claims description 2
- 239000003002 pH adjusting agent Substances 0.000 claims description 2
- 239000008389 polyethoxylated castor oil Substances 0.000 claims description 2
- 229920001223 polyethylene glycol Polymers 0.000 claims description 2
- 239000012896 selective serotonin reuptake inhibitor Substances 0.000 claims description 2
- 229940124834 selective serotonin reuptake inhibitor Drugs 0.000 claims description 2
- 239000003369 serotonin 5-HT3 receptor antagonist Substances 0.000 claims description 2
- 229910052708 sodium Inorganic materials 0.000 claims description 2
- 239000011734 sodium Substances 0.000 claims description 2
- 239000012064 sodium phosphate buffer Substances 0.000 claims description 2
- 239000007787 solid Substances 0.000 claims description 2
- 239000002904 solvent Substances 0.000 claims description 2
- 239000008181 tonicity modifier Substances 0.000 claims description 2
- 230000003111 delayed effect Effects 0.000 claims 4
- 239000003240 coconut oil Substances 0.000 claims 2
- 235000019864 coconut oil Nutrition 0.000 claims 2
- 238000002347 injection Methods 0.000 claims 1
- 239000007924 injection Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 description 4
- 239000003814 drug Substances 0.000 description 4
- 230000001062 anti-nausea Effects 0.000 description 3
- 235000019482 Palm oil Nutrition 0.000 description 2
- 239000002895 emetic Substances 0.000 description 2
- 239000002540 palm oil Substances 0.000 description 2
- 230000001568 sexual effect Effects 0.000 description 2
- FELGMEQIXOGIFQ-CYBMUJFWSA-N (3r)-9-methyl-3-[(2-methylimidazol-1-yl)methyl]-2,3-dihydro-1h-carbazol-4-one Chemical compound CC1=NC=CN1C[C@@H]1C(=O)C(C=2C(=CC=CC=2)N2C)=C2CC1 FELGMEQIXOGIFQ-CYBMUJFWSA-N 0.000 description 1
- 239000002111 antiemetic agent Substances 0.000 description 1
- 229940000425 combination drug Drugs 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- 229960005343 ondansetron Drugs 0.000 description 1
- 239000002464 receptor antagonist Substances 0.000 description 1
- 229940044551 receptor antagonist Drugs 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US23412909P | 2009-08-14 | 2009-08-14 | |
| US61/234,129 | 2009-08-14 | ||
| PCT/US2010/045317 WO2011019911A1 (en) | 2009-08-14 | 2010-08-12 | Intravenous formulations of neurokinin-1 antagonists |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015216374A Division JP6308991B2 (ja) | 2009-08-14 | 2015-11-04 | ニューロキニン−１アンタゴニストの静脈内用製剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013501806A JP2013501806A (ja) | 2013-01-17 |
| JP2013501806A5 true JP2013501806A5 (enExample) | 2013-09-19 |
| JP5860399B2 JP5860399B2 (ja) | 2016-02-16 |
Family
ID=43586486
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012524868A Expired - Fee Related JP5860399B2 (ja) | 2009-08-14 | 2010-08-12 | ニューロキニン−１アンタゴニストの静脈内用製剤 |
| JP2015216374A Expired - Fee Related JP6308991B2 (ja) | 2009-08-14 | 2015-11-04 | ニューロキニン−１アンタゴニストの静脈内用製剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015216374A Expired - Fee Related JP6308991B2 (ja) | 2009-08-14 | 2015-11-04 | ニューロキニン−１アンタゴニストの静脈内用製剤 |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US9101615B2 (enExample) |
| EP (2) | EP2464230B1 (enExample) |
| JP (2) | JP5860399B2 (enExample) |
| KR (1) | KR101834577B1 (enExample) |
| CN (2) | CN105503870A (enExample) |
| AU (1) | AU2010282483B2 (enExample) |
| BR (1) | BR112012003263A2 (enExample) |
| CA (1) | CA2770403C (enExample) |
| ES (1) | ES2609640T3 (enExample) |
| IL (1) | IL217942A0 (enExample) |
| MX (1) | MX336071B (enExample) |
| RU (2) | RU2642234C2 (enExample) |
| SG (2) | SG178403A1 (enExample) |
| TW (2) | TWI498329B (enExample) |
| WO (1) | WO2011019911A1 (enExample) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG170838A1 (en) * | 2006-04-05 | 2011-05-30 | Opko Health Inc | Hydrochloride salts of 8-[{1-(3,5-bis-(trifluoromethyl) phenyl) -ethoxy}- methyl] -8-phenyl-1,7-diaza-spiro[4.5] decan-2-one and preparation process therefor |
| NZ571693A (en) | 2006-04-05 | 2011-12-22 | Opko Health Inc | Pharmaceutical formulations: salts of 8-[{ 1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy} -methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one and treatment methods using the same |
| AR066191A1 (es) | 2007-03-22 | 2009-08-05 | Schering Corp | Proceso e intermediarios para la sintesis de compuestos 8- [ ( 1- (3,5- bis- ( trifluorometil) fenil) - etoxi ) - metil]- 8 fenil - 1,7- diaza - espiro (4, 5) decan -2 ona |
| HUE026148T2 (en) | 2008-09-05 | 2016-05-30 | Opko Health Inc | 8 - ({1- [3,5-bis (trifluoromethyl) phenyl] ethoxy} methyl) -8-phenyl-1,7-diaza-spiro [4,5] decane-on-compounds intermediates |
| CN105503870A (zh) | 2009-08-14 | 2016-04-20 | 欧科生医股份有限公司 | 神经激肽-1拮抗剂的静脉内制剂 |
| TW201605852A (zh) * | 2013-09-26 | 2016-02-16 | 美國禮來大藥廠 | 新穎化合物及其製備ｔａｕ造影劑及ｔａｕ造影調配物之用途 |
| JP6741655B2 (ja) | 2014-09-19 | 2020-08-19 | ヘロン セラピューティクス， インコーポレイテッドＨｅｒｏｎ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． | アプレピタントのエマルジョン製剤 |
| BR112017018620A2 (pt) | 2015-03-04 | 2018-04-17 | Vanda Pharmaceuticals Inc. | método de administração de tradipitanto, e, tradipitanto. |
| US20180250270A1 (en) | 2015-09-11 | 2018-09-06 | Chase Pharmaceuticals Corporation | Muscarinic combination and its use for combating hypocholinergic disorders of the central nervous system |
| US9974742B2 (en) | 2016-02-01 | 2018-05-22 | Heron Therapeutics, Inc. | Emulsion formulations of an NK-1 receptor antagonist and uses thereof |
| EP3411013A1 (en) * | 2016-02-01 | 2018-12-12 | Heron Therapeutics, Inc. | Emulsion comprising an nk-1 receptor antagonist |
| US20190175702A1 (en) * | 2016-08-03 | 2019-06-13 | Zhuhai Beihai Biotech Co., Ltd. | Formulations of fosaprepitant and aprepitant |
| CN109963583B (zh) * | 2016-11-21 | 2023-06-09 | 珠海贝海生物技术有限公司 | 罗拉吡坦制剂 |
| IL312486B2 (en) | 2017-04-10 | 2025-05-01 | Chase Therapeutics Corp | NK1 antagonist combination and method for treating synucleinopathies |
| CN110996911B (zh) * | 2017-06-26 | 2023-01-17 | 福多兹制药公司 | 阿瑞匹坦的纳米微脂囊配制品及其方法和应用 |
| KR20250069704A (ko) | 2017-06-30 | 2025-05-19 | 체이스 테라퓨틱스 코포레이션 | 우울증을 치료하기 위한 nk-1 길항제 조성물 및 우울증 치료에 사용하는 방법 |
| CN109200018A (zh) * | 2017-07-04 | 2019-01-15 | 南京诺瑞特医药科技有限公司 | 含有奈妥吡坦的微乳制剂 |
| CN108703950B (zh) * | 2018-08-27 | 2021-04-20 | 辅必成（上海）医药科技有限公司 | 一种罗拉吡坦的乳剂注射液 |
| CN109394693A (zh) * | 2018-12-25 | 2019-03-01 | 广州白云山汉方现代药业有限公司 | 一种罗拉匹坦乳剂及其制备方法和应用 |
| CN109453115A (zh) * | 2018-12-25 | 2019-03-12 | 广州白云山汉方现代药业有限公司 | 一种罗拉匹坦静脉注射乳剂及其制备方法和应用 |
| US12421260B2 (en) * | 2019-06-28 | 2025-09-23 | Shanghai Shengdi Pharmaceutical Co., Ltd | Neurokinin-1 antagonist |
| EP4125875A1 (en) | 2020-04-03 | 2023-02-08 | NeRRe Therapeutics Limited | An nk-1 receptor antagonist for treating a disease selecting from sepsis, septic shock,, acute respiratory distress syndrome (ards) or multiple organ dysfunction syndrome (mods) |
| KR20230018485A (ko) | 2020-06-02 | 2023-02-07 | 네르 쎄라퓨틱스 리미티드 | 폐에 대한 기계적 손상에 의해 촉진된 폐 섬유증 상태의 치료에 사용하기 위한 뉴로키닌 (nk)-1 수용체 길항제 |
| CN116472048B (zh) * | 2020-12-25 | 2025-02-18 | 上海盛迪医药有限公司 | Nk1拮抗剂前药化合物与5-ht3受体拮抗剂的联用用途 |
| CN118510509A (zh) * | 2022-01-12 | 2024-08-16 | 江苏恒瑞医药股份有限公司 | 一种包含神经激肽-1拮抗剂前药化合物的药物组合物 |
| EP4464712A4 (en) * | 2022-01-12 | 2025-07-23 | Jiangsu Hengrui Pharmaceuticals Co Ltd | CRYSTALLINE FORM OF A NEUROKININ-1 ANTAGONIST PRODRUG COMPOUND |
| CN119528985A (zh) * | 2023-08-28 | 2025-02-28 | 科睿迪(南京)医药科技有限公司 | 神经激肽-1受体拮抗剂化合物 |
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| US5661162A (en) | 1992-12-14 | 1997-08-26 | Merck Sharp & Dohme Limited | 4-aminomethyl/thiomethyl/sulfonylmethyl-4-phenylpiperdines as tachykinin receptor antagonists |
| GB9305718D0 (en) * | 1993-03-19 | 1993-05-05 | Glaxo Group Ltd | Medicaments |
| WO1995019344A1 (en) | 1994-01-13 | 1995-07-20 | Merck Sharp & Dohme Limited | Gem-disubstituted azacyclic tachykinin antagonists |
| NZ302926A (en) | 1995-02-28 | 1998-10-28 | Hoechst Marion Roussel Inc | Composition for use as antihistamines comprising piperidinoalkanol derivatives and inert ingredients |
| SE9503143D0 (sv) * | 1995-09-12 | 1995-09-12 | Astra Ab | New preparation |
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| CA2260269A1 (en) | 1996-07-17 | 1998-01-22 | Merck & Co., Inc. | Alteration of circadian rhythmicity with a tachykinin antagonist |
| AU735760B2 (en) | 1997-04-24 | 2001-07-12 | Merck Sharp & Dohme Limited | Use of a NK-1 receptor antagonist and an SSRI for treating obesity |
| JP3571511B2 (ja) * | 1997-11-11 | 2004-09-29 | トーアエイヨー株式会社 | 経皮吸収製剤 |
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2010
- 2010-08-12 CN CN201510830177.9A patent/CN105503870A/zh active Pending
- 2010-08-12 EP EP10808756.0A patent/EP2464230B1/en not_active Not-in-force
- 2010-08-12 WO PCT/US2010/045317 patent/WO2011019911A1/en not_active Ceased
- 2010-08-12 MX MX2012001872A patent/MX336071B/es unknown
- 2010-08-12 KR KR1020127006576A patent/KR101834577B1/ko not_active Expired - Fee Related
- 2010-08-12 ES ES10808756.0T patent/ES2609640T3/es active Active
- 2010-08-12 JP JP2012524868A patent/JP5860399B2/ja not_active Expired - Fee Related
- 2010-08-12 SG SG2012010146A patent/SG178403A1/en unknown
- 2010-08-12 BR BR112012003263A patent/BR112012003263A2/pt not_active Application Discontinuation
- 2010-08-12 SG SG10201407538WA patent/SG10201407538WA/en unknown
- 2010-08-12 CA CA2770403A patent/CA2770403C/en active Active
- 2010-08-12 AU AU2010282483A patent/AU2010282483B2/en not_active Ceased
- 2010-08-12 RU RU2012109405A patent/RU2642234C2/ru not_active IP Right Cessation
- 2010-08-12 EP EP16181864.6A patent/EP3143996A1/en not_active Withdrawn
- 2010-08-12 RU RU2017145628A patent/RU2017145628A/ru not_active Application Discontinuation
- 2010-08-12 CN CN201080046905.2A patent/CN102573475B/zh not_active Expired - Fee Related
- 2010-08-13 TW TW099127158A patent/TWI498329B/zh not_active IP Right Cessation
- 2010-08-13 TW TW104121014A patent/TW201604195A/zh unknown
- 2010-08-13 US US12/855,889 patent/US9101615B2/en active Active
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2012
- 2012-02-05 IL IL217942A patent/IL217942A0/en unknown
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2015
- 2015-07-28 US US14/811,342 patent/US20160024092A1/en not_active Abandoned
- 2015-11-04 JP JP2015216374A patent/JP6308991B2/ja not_active Expired - Fee Related
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