JP2021088575A5 - - Google Patents
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- JP2021088575A5 JP2021088575A5 JP2021021155A JP2021021155A JP2021088575A5 JP 2021088575 A5 JP2021088575 A5 JP 2021088575A5 JP 2021021155 A JP2021021155 A JP 2021021155A JP 2021021155 A JP2021021155 A JP 2021021155A JP 2021088575 A5 JP2021088575 A5 JP 2021088575A5
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- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- composition according
- administered
- item
- methanesulfonate
- 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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- 239000008194 pharmaceutical composition Substances 0.000 claims description 29
- 206010021518 Impaired gastric emptying Diseases 0.000 claims description 10
- 239000003814 drug Substances 0.000 claims description 10
- 208000024891 symptom Diseases 0.000 claims description 8
- 208000001288 gastroparesis Diseases 0.000 claims description 7
- 201000006549 dyspepsia Diseases 0.000 claims description 6
- 238000007913 intrathecal administration Methods 0.000 claims description 6
- 206010028813 Nausea Diseases 0.000 claims description 5
- 206010047700 Vomiting Diseases 0.000 claims description 5
- BQDBKDMTIJBJLA-UHFFFAOYSA-N metopimazine Chemical compound C12=CC(S(=O)(=O)C)=CC=C2SC2=CC=CC=C2N1CCCN1CCC(C(N)=O)CC1 BQDBKDMTIJBJLA-UHFFFAOYSA-N 0.000 claims description 5
- 230000008693 nausea Effects 0.000 claims description 5
- 230000008673 vomiting Effects 0.000 claims description 5
- 208000021302 gastroesophageal reflux disease Diseases 0.000 claims description 4
- 208000004998 Abdominal Pain Diseases 0.000 claims description 3
- 206010000060 Abdominal distension Diseases 0.000 claims description 3
- 206010010774 Constipation Diseases 0.000 claims description 3
- 206010012735 Diarrhoea Diseases 0.000 claims description 3
- 241000792859 Enema Species 0.000 claims description 3
- 230000004596 appetite loss Effects 0.000 claims description 3
- 208000024330 bloating Diseases 0.000 claims description 3
- 239000002775 capsule Substances 0.000 claims description 3
- 239000007920 enema Substances 0.000 claims description 3
- 229940095399 enema Drugs 0.000 claims description 3
- 208000019017 loss of appetite Diseases 0.000 claims description 3
- 235000021266 loss of appetite Nutrition 0.000 claims description 3
- 239000000203 mixture Substances 0.000 claims description 3
- 238000002360 preparation method Methods 0.000 claims description 3
- 239000006188 syrup Substances 0.000 claims description 3
- 235000020357 syrup Nutrition 0.000 claims description 3
- 239000006071 cream Substances 0.000 claims description 2
- 239000000839 emulsion Substances 0.000 claims description 2
- 239000003889 eye drop Substances 0.000 claims description 2
- 229940012356 eye drops Drugs 0.000 claims description 2
- 238000001361 intraarterial administration Methods 0.000 claims description 2
- 238000007918 intramuscular administration Methods 0.000 claims description 2
- 238000001990 intravenous administration Methods 0.000 claims description 2
- 239000006210 lotion Substances 0.000 claims description 2
- 235000015927 pasta Nutrition 0.000 claims description 2
- 239000000843 powder Substances 0.000 claims description 2
- 239000000243 solution Substances 0.000 claims description 2
- 239000007921 spray Substances 0.000 claims description 2
- 239000000725 suspension Substances 0.000 claims description 2
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 6
- 229960000767 metopimazine Drugs 0.000 claims 4
- 239000003937 drug carrier Substances 0.000 claims 2
- 238000000034 method Methods 0.000 description 49
- 150000001875 compounds Chemical class 0.000 description 25
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 description 24
- 208000012902 Nervous system disease Diseases 0.000 description 14
- 210000000105 enteric nervous system Anatomy 0.000 description 14
- 229940123736 Decarboxylase inhibitor Drugs 0.000 description 12
- 239000003954 decarboxylase inhibitor Substances 0.000 description 12
- 229960003638 dopamine Drugs 0.000 description 12
- 125000000217 alkyl group Chemical group 0.000 description 10
- 125000000592 heterocycloalkyl group Chemical group 0.000 description 8
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 description 6
- 125000005843 halogen group Chemical group 0.000 description 6
- 229940124597 therapeutic agent Drugs 0.000 description 5
- 230000008499 blood brain barrier function Effects 0.000 description 4
- 210000001218 blood-brain barrier Anatomy 0.000 description 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 4
- 125000005842 heteroatom Chemical group 0.000 description 4
- 239000002207 metabolite Substances 0.000 description 4
- 229910052760 oxygen Inorganic materials 0.000 description 4
- 150000003839 salts Chemical class 0.000 description 4
- 239000012453 solvate Substances 0.000 description 4
- 229910052717 sulfur Inorganic materials 0.000 description 4
- 229940123603 Dopamine D2 receptor antagonist Drugs 0.000 description 3
- 229960004205 carbidopa Drugs 0.000 description 3
- TZFNLOMSOLWIDK-JTQLQIEISA-N carbidopa (anhydrous) Chemical group NN[C@@](C(O)=O)(C)CC1=CC=C(O)C(O)=C1 TZFNLOMSOLWIDK-JTQLQIEISA-N 0.000 description 3
- 239000000442 dopamine 2 receptor blocking agent Substances 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 125000001484 phenothiazinyl group Chemical group C1(=CC=CC=2SC3=CC=CC=C3NC12)* 0.000 description 3
- 239000003826 tablet Substances 0.000 description 3
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 description 2
- 241000124008 Mammalia Species 0.000 description 2
- 208000006876 Multiple Endocrine Neoplasia Type 2b Diseases 0.000 description 2
- UCTWMZQNUQWSLP-UHFFFAOYSA-N adrenaline Chemical compound CNCC(O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-UHFFFAOYSA-N 0.000 description 2
- 230000002411 adverse Effects 0.000 description 2
- 125000003118 aryl group Chemical group 0.000 description 2
- 125000004093 cyano group Chemical group *C#N 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- DYMRYCZRMAHYKE-UHFFFAOYSA-N n-diazonitramide Chemical compound [O-][N+](=O)N=[N+]=[N-] DYMRYCZRMAHYKE-UHFFFAOYSA-N 0.000 description 2
- 239000000018 receptor agonist Substances 0.000 description 2
- 229940044601 receptor agonist Drugs 0.000 description 2
- 229940044551 receptor antagonist Drugs 0.000 description 2
- 239000002464 receptor antagonist Substances 0.000 description 2
- 0 *c(cc1)cc2c1SC1=CC=CCC1N2I=* Chemical compound *c(cc1)cc2c1SC1=CC=CCC1N2I=* 0.000 description 1
- 229940127291 Calcium channel antagonist Drugs 0.000 description 1
- 208000017667 Chronic Disease Diseases 0.000 description 1
- 208000012661 Dyskinesia Diseases 0.000 description 1
- 208000003098 Ganglion Cysts Diseases 0.000 description 1
- 208000027601 Inner ear disease Diseases 0.000 description 1
- 206010073659 Intestinal neuronal dysplasia Diseases 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 208000005890 Neuroma Diseases 0.000 description 1
- 102000003840 Opioid Receptors Human genes 0.000 description 1
- 108090000137 Opioid Receptors Proteins 0.000 description 1
- 208000018737 Parkinson disease Diseases 0.000 description 1
- 206010039710 Scleroderma Diseases 0.000 description 1
- 208000005400 Synovial Cyst Diseases 0.000 description 1
- 238000009825 accumulation Methods 0.000 description 1
- 229940125681 anticonvulsant agent Drugs 0.000 description 1
- 239000001961 anticonvulsive agent Substances 0.000 description 1
- 229940082988 antihypertensives serotonin antagonists Drugs 0.000 description 1
- 239000003420 antiserotonin agent Substances 0.000 description 1
- 125000005605 benzo group Chemical group 0.000 description 1
- 229940049706 benzodiazepine Drugs 0.000 description 1
- 125000003310 benzodiazepinyl group Chemical class N1N=C(C=CC2=C1C=CC=C2)* 0.000 description 1
- 239000000480 calcium channel blocker Substances 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 230000000747 cardiac effect Effects 0.000 description 1
- 238000002512 chemotherapy Methods 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- FGXWKSZFVQUSTL-UHFFFAOYSA-N domperidone Chemical compound C12=CC=CC=C2NC(=O)N1CCCN(CC1)CCC1N1C2=CC=C(Cl)C=C2NC1=O FGXWKSZFVQUSTL-UHFFFAOYSA-N 0.000 description 1
- 229960001253 domperidone Drugs 0.000 description 1
- 239000007789 gas Substances 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 210000002149 gonad Anatomy 0.000 description 1
- 230000003054 hormonal effect Effects 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 230000000968 intestinal effect Effects 0.000 description 1
- 208000002551 irritable bowel syndrome Diseases 0.000 description 1
- 210000003712 lysosome Anatomy 0.000 description 1
- 230000001868 lysosomic effect Effects 0.000 description 1
- 201000001119 neuropathy Diseases 0.000 description 1
- 230000007823 neuropathy Effects 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 1
- 239000006191 orally-disintegrating tablet Substances 0.000 description 1
- 208000033808 peripheral neuropathy Diseases 0.000 description 1
- 239000012896 selective serotonin reuptake inhibitor Substances 0.000 description 1
- 229940124834 selective serotonin reuptake inhibitor Drugs 0.000 description 1
- 239000000952 serotonin receptor agonist Substances 0.000 description 1
- NHXLMOGPVYXJNR-ATOGVRKGSA-N somatostatin Chemical class C([C@H]1C(=O)N[C@H](C(N[C@@H](CO)C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N1)[C@@H](C)O)NC(=O)CNC(=O)[C@H](C)N)C(O)=O)=O)[C@H](O)C)C1=CC=CC=C1 NHXLMOGPVYXJNR-ATOGVRKGSA-N 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 208000027491 vestibular disease Diseases 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261745734P | 2012-12-24 | 2012-12-24 | |
| US61/745,734 | 2012-12-24 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018213361A Division JP2019048848A (ja) | 2012-12-24 | 2018-11-14 | Ｇｉ管障害を治療するための方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2021088575A JP2021088575A (ja) | 2021-06-10 |
| JP2021088575A5 true JP2021088575A5 (https=) | 2021-08-19 |
Family
ID=51021982
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015549742A Active JP6154025B2 (ja) | 2012-12-24 | 2013-12-19 | Ｇｉ管障害を治療するための方法 |
| JP2017108370A Active JP6437593B2 (ja) | 2012-12-24 | 2017-05-31 | Ｇｉ管障害を治療するための方法 |
| JP2018213361A Pending JP2019048848A (ja) | 2012-12-24 | 2018-11-14 | Ｇｉ管障害を治療するための方法 |
| JP2021021155A Pending JP2021088575A (ja) | 2012-12-24 | 2021-02-12 | Ｇｉ管障害を治療するための方法 |
Family Applications Before (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015549742A Active JP6154025B2 (ja) | 2012-12-24 | 2013-12-19 | Ｇｉ管障害を治療するための方法 |
| JP2017108370A Active JP6437593B2 (ja) | 2012-12-24 | 2017-05-31 | Ｇｉ管障害を治療するための方法 |
| JP2018213361A Pending JP2019048848A (ja) | 2012-12-24 | 2018-11-14 | Ｇｉ管障害を治療するための方法 |
Country Status (9)
| Country | Link |
|---|---|
| US (7) | US9132134B2 (https=) |
| EP (1) | EP2934540B1 (https=) |
| JP (4) | JP6154025B2 (https=) |
| CN (1) | CN104884064A (https=) |
| AU (1) | AU2013370966A1 (https=) |
| BR (1) | BR112015015258A2 (https=) |
| CA (2) | CA3178035A1 (https=) |
| ES (1) | ES2955693T3 (https=) |
| WO (1) | WO2014105655A1 (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9107815B2 (en) * | 2008-02-22 | 2015-08-18 | Allergan, Inc. | Sustained release poloxamer containing pharmaceutical compositions |
| JP6154025B2 (ja) * | 2012-12-24 | 2017-06-28 | ニューロガストルクス，インコーポレイテッド | Ｇｉ管障害を治療するための方法 |
| WO2015200369A1 (en) | 2014-06-24 | 2015-12-30 | Neurogastrx, Inc. | Prodrugs of metopimazine |
| US9695138B1 (en) | 2016-10-17 | 2017-07-04 | Acenda Pharma, Inc. | Phenothiazine derivatives and methods of use thereof |
| CN109053716B (zh) * | 2018-09-26 | 2021-01-08 | 暨明医药科技（苏州）有限公司 | 一种制备美托哌丙嗪的新工艺 |
| US10836757B1 (en) * | 2020-04-02 | 2020-11-17 | Neurogastrx, Inc. | Polymorphic forms of metopimazine |
| WO2022146970A1 (en) * | 2020-12-29 | 2022-07-07 | Neurogastrx, Inc. | Methods of metabolizing metopimazine and its salts |
| CN116940361A (zh) * | 2020-12-29 | 2023-10-24 | 纽洛佳斯特拉斯公司 | 美托哌丙嗪及其盐的代谢方法 |
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| JP6154025B2 (ja) * | 2012-12-24 | 2017-06-28 | ニューロガストルクス，インコーポレイテッド | Ｇｉ管障害を治療するための方法 |
| IN2013MU02528A (https=) | 2013-07-31 | 2015-06-26 | Centaur Pharmaceuticals Private Ltd | |
| WO2015200369A1 (en) | 2014-06-24 | 2015-12-30 | Neurogastrx, Inc. | Prodrugs of metopimazine |
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2013
- 2013-12-19 JP JP2015549742A patent/JP6154025B2/ja active Active
- 2013-12-19 BR BR112015015258A patent/BR112015015258A2/pt not_active IP Right Cessation
- 2013-12-19 WO PCT/US2013/076733 patent/WO2014105655A1/en not_active Ceased
- 2013-12-19 CA CA3178035A patent/CA3178035A1/en active Pending
- 2013-12-19 CN CN201380067866.8A patent/CN104884064A/zh active Pending
- 2013-12-19 ES ES13869541T patent/ES2955693T3/es active Active
- 2013-12-19 EP EP13869541.6A patent/EP2934540B1/en active Active
- 2013-12-19 AU AU2013370966A patent/AU2013370966A1/en not_active Abandoned
- 2013-12-19 CA CA2893427A patent/CA2893427C/en active Active
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2014
- 2014-11-26 US US14/555,455 patent/US9132134B2/en active Active
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2015
- 2015-08-07 US US14/820,885 patent/US9808467B2/en active Active
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2017
- 2017-05-31 JP JP2017108370A patent/JP6437593B2/ja active Active
- 2017-09-27 US US15/717,765 patent/US20180200258A1/en not_active Abandoned
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2018
- 2018-11-14 JP JP2018213361A patent/JP2019048848A/ja active Pending
- 2018-12-11 US US16/216,257 patent/US20190314384A1/en not_active Abandoned
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2020
- 2020-04-30 US US16/862,762 patent/US11147820B2/en active Active
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2021
- 2021-02-12 JP JP2021021155A patent/JP2021088575A/ja active Pending
- 2021-09-17 US US17/477,830 patent/US20220202826A1/en not_active Abandoned
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2023
- 2023-06-05 US US18/205,634 patent/US20240058353A1/en not_active Abandoned
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