AU2023232536A1 - Polymorph forms of aticaprant for use in treating major depressive disorder - Google Patents
Polymorph forms of aticaprant for use in treating major depressive disorder Download PDFInfo
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- AU2023232536A1 AU2023232536A1 AU2023232536A AU2023232536A AU2023232536A1 AU 2023232536 A1 AU2023232536 A1 AU 2023232536A1 AU 2023232536 A AU2023232536 A AU 2023232536A AU 2023232536 A AU2023232536 A AU 2023232536A AU 2023232536 A1 AU2023232536 A1 AU 2023232536A1
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- Australia
- Prior art keywords
- aticaprant
- crystalline form
- amorphous
- treatment
- anhedonia
- 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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- JXKPEJDQGNYQSM-UHFFFAOYSA-M sodium propionate Chemical compound [Na+].CCC([O-])=O JXKPEJDQGNYQSM-UHFFFAOYSA-M 0.000 description 1
- 235000010334 sodium propionate Nutrition 0.000 description 1
- 239000004324 sodium propionate Substances 0.000 description 1
- 229960003212 sodium propionate Drugs 0.000 description 1
- 229960004025 sodium salicylate Drugs 0.000 description 1
- 235000010339 sodium tetraborate Nutrition 0.000 description 1
- PPASLZSBLFJQEF-RXSVEWSESA-M sodium-L-ascorbate Chemical compound [Na+].OC[C@H](O)[C@H]1OC(=O)C(O)=C1[O-] PPASLZSBLFJQEF-RXSVEWSESA-M 0.000 description 1
- 238000000371 solid-state nuclear magnetic resonance spectroscopy Methods 0.000 description 1
- 238000000935 solvent evaporation Methods 0.000 description 1
- 239000011877 solvent mixture Substances 0.000 description 1
- 229950001013 sonepiprazole Drugs 0.000 description 1
- WNUQCGWXPNGORO-NRFANRHFSA-N sonepiprazole Chemical compound C1=CC(S(=O)(=O)N)=CC=C1N1CCN(CC[C@H]2C3=CC=CC=C3CCO2)CC1 WNUQCGWXPNGORO-NRFANRHFSA-N 0.000 description 1
- 235000010199 sorbic acid Nutrition 0.000 description 1
- 239000004334 sorbic acid Substances 0.000 description 1
- 229940075582 sorbic acid Drugs 0.000 description 1
- 229960002920 sorbitol Drugs 0.000 description 1
- 238000010561 standard procedure Methods 0.000 description 1
- 239000012086 standard solution Substances 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 201000009032 substance abuse Diseases 0.000 description 1
- 231100000736 substance abuse Toxicity 0.000 description 1
- 208000011117 substance-related disease Diseases 0.000 description 1
- LSNNMFCWUKXFEE-UHFFFAOYSA-L sulfite Chemical class [O-]S([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-L 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 230000008685 targeting Effects 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 230000009967 tasteless effect Effects 0.000 description 1
- BHTRKEVKTKCXOH-LBSADWJPSA-N tauroursodeoxycholic acid Chemical compound C([C@H]1C[C@@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(=O)NCCS(O)(=O)=O)C)[C@@]2(C)CC1 BHTRKEVKTKCXOH-LBSADWJPSA-N 0.000 description 1
- 230000002123 temporal effect Effects 0.000 description 1
- RTKIYNMVFMVABJ-UHFFFAOYSA-L thimerosal Chemical compound [Na+].CC[Hg]SC1=CC=CC=C1C([O-])=O RTKIYNMVFMVABJ-UHFFFAOYSA-L 0.000 description 1
- 229940033663 thimerosal Drugs 0.000 description 1
- 229960002784 thioridazine Drugs 0.000 description 1
- 150000005075 thioxanthenes Chemical class 0.000 description 1
- 229940034199 thyrotropin-releasing hormone Drugs 0.000 description 1
- 229960005013 tiotixene Drugs 0.000 description 1
- 235000010384 tocopherol Nutrition 0.000 description 1
- 229930003799 tocopherol Natural products 0.000 description 1
- 229960001295 tocopherol Drugs 0.000 description 1
- 239000011732 tocopherol Substances 0.000 description 1
- 235000010487 tragacanth Nutrition 0.000 description 1
- 239000000196 tragacanth Substances 0.000 description 1
- 229940116362 tragacanth Drugs 0.000 description 1
- 238000011491 transcranial magnetic stimulation Methods 0.000 description 1
- 229960003741 tranylcypromine Drugs 0.000 description 1
- 229960003991 trazodone Drugs 0.000 description 1
- PHLBKPHSAVXXEF-UHFFFAOYSA-N trazodone Chemical compound ClC1=CC=CC(N2CCN(CCCN3C(N4C=CC=CC4=N3)=O)CC2)=C1 PHLBKPHSAVXXEF-UHFFFAOYSA-N 0.000 description 1
- ZEWQUBUPAILYHI-UHFFFAOYSA-N trifluoperazine Chemical compound C1CN(C)CCN1CCCN1C2=CC(C(F)(F)F)=CC=C2SC2=CC=CC=C21 ZEWQUBUPAILYHI-UHFFFAOYSA-N 0.000 description 1
- 229960002324 trifluoperazine Drugs 0.000 description 1
- 229940035722 triiodothyronine Drugs 0.000 description 1
- 229960002431 trimipramine Drugs 0.000 description 1
- ZSCDBOWYZJWBIY-UHFFFAOYSA-N trimipramine Chemical compound C1CC2=CC=CC=C2N(CC(CN(C)C)C)C2=CC=CC=C21 ZSCDBOWYZJWBIY-UHFFFAOYSA-N 0.000 description 1
- BSVBQGMMJUBVOD-UHFFFAOYSA-N trisodium borate Chemical compound [Na+].[Na+].[Na+].[O-]B([O-])[O-] BSVBQGMMJUBVOD-UHFFFAOYSA-N 0.000 description 1
- 238000002562 urinalysis Methods 0.000 description 1
- 238000001291 vacuum drying Methods 0.000 description 1
- MSRILKIQRXUYCT-UHFFFAOYSA-M valproate semisodium Chemical compound [Na+].CCCC(C(O)=O)CCC.CCCC(C([O-])=O)CCC MSRILKIQRXUYCT-UHFFFAOYSA-M 0.000 description 1
- 210000004515 ventral tegmental area Anatomy 0.000 description 1
- 238000000196 viscometry Methods 0.000 description 1
- 238000012800 visualization Methods 0.000 description 1
- 235000019165 vitamin E Nutrition 0.000 description 1
- 229940046009 vitamin E Drugs 0.000 description 1
- 239000011709 vitamin E Substances 0.000 description 1
- 230000001755 vocal effect Effects 0.000 description 1
- 230000008673 vomiting Effects 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- 229960000607 ziprasidone Drugs 0.000 description 1
- MVWVFYHBGMAFLY-UHFFFAOYSA-N ziprasidone Chemical compound C1=CC=C2C(N3CCN(CC3)CCC3=CC=4CC(=O)NC=4C=C3Cl)=NSC2=C1 MVWVFYHBGMAFLY-UHFFFAOYSA-N 0.000 description 1
- 229960004496 zotepine Drugs 0.000 description 1
- HDOZVRUNCMBHFH-UHFFFAOYSA-N zotepine Chemical compound CN(C)CCOC1=CC2=CC=CC=C2SC2=CC=C(Cl)C=C12 HDOZVRUNCMBHFH-UHFFFAOYSA-N 0.000 description 1
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202263317475P | 2022-03-07 | 2022-03-07 | |
| US63/317,475 | 2022-03-07 | ||
| PCT/IB2023/052088 WO2023170550A1 (en) | 2022-03-07 | 2023-03-06 | Polymorph forms of aticaprant for use in treating major depressive disorder |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AU2023232536A1 true AU2023232536A1 (en) | 2024-10-24 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2023232536A Pending AU2023232536A1 (en) | 2022-03-07 | 2023-03-06 | Polymorph forms of aticaprant for use in treating major depressive disorder |
Country Status (14)
| Country | Link |
|---|---|
| US (3) | US11998524B2 (https=) |
| EP (1) | EP4489747A1 (https=) |
| JP (1) | JP2025508051A (https=) |
| KR (1) | KR20240156409A (https=) |
| CN (1) | CN119156211A (https=) |
| AU (1) | AU2023232536A1 (https=) |
| CA (1) | CA3254365A1 (https=) |
| CL (1) | CL2024002627A1 (https=) |
| CO (1) | CO2024012158A2 (https=) |
| IL (1) | IL315409A (https=) |
| JO (1) | JOP20240197A1 (https=) |
| MX (1) | MX2024010980A (https=) |
| TW (1) | TW202345796A (https=) |
| WO (1) | WO2023170550A1 (https=) |
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| US12161622B2 (en) | 2021-05-04 | 2024-12-10 | Janssen Pharmaceuticals, Inc. | Compositions and methods for the treatment of depression |
| EP4489730B1 (en) | 2022-03-07 | 2026-01-21 | Janssen Pharmaceuticals, Inc. | Compositions comprising aticaprant |
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| US5457208A (en) | 1993-06-21 | 1995-10-10 | Regents Of The University Of Minnesota | Kappa opioid receptor antagonists |
| WO2000069858A1 (en) | 1999-05-12 | 2000-11-23 | F. Hoffmann-La Roche Ag | Imidazodiazepine derivative |
| JP2004510789A (ja) | 2000-10-05 | 2004-04-08 | モーラー，ハンス | 選択的抗不安治療薬 |
| JP2004518654A (ja) | 2000-12-21 | 2004-06-24 | ザ マクレーン ホスピタル コーポレーション | 鬱病の治療法 |
| US6974824B2 (en) | 2001-01-08 | 2005-12-13 | Research Triangle Institute | Kappa opioid receptor ligands |
| DE60319812T2 (de) | 2002-03-28 | 2009-04-23 | Wisys Technology Foundation, Inc., Madison | Angstlösende wirkstoffe mit verminderten beruhigenden und ataktischen nebenwirkungen |
| KR101025633B1 (ko) | 2002-09-19 | 2011-03-30 | 일라이 릴리 앤드 캄파니 | 오피오이드 수용체 안타고니스트로서의 디아릴 에테르 |
| US7396943B2 (en) | 2003-03-07 | 2008-07-08 | Eli Lilly And Company | Opioid receptor antagonists |
| CN1756746A (zh) | 2003-03-07 | 2006-04-05 | 伊莱利利公司 | 作为阿片样物质受体拮抗剂的6－取代的烟酰胺衍生物 |
| BRPI0417156A (pt) | 2003-12-12 | 2007-03-06 | Lilly Co Eli | composto, composição farmacêutica, e, métodos para bloquear receptor mu, capa, delta ou combinação (heterodìmero) dos mesmos em mamìferos, para tratar e/ou prevenir doenças relacionadas com obesidade e obesidade, para suprimir apetite em um paciente, para efetuar perda de peso em um paciente obeso |
| CN1894240A (zh) | 2003-12-22 | 2007-01-10 | 伊莱利利公司 | 阿片受体拮抗剂 |
| EP1730140B1 (en) | 2004-03-12 | 2008-06-25 | Eli Lilly And Company | Opioid receptor antagonists |
| EP1727788B1 (en) | 2004-03-12 | 2010-07-28 | Eli Lilly And Company | Opioid receptor antagonists |
| AU2005222640A1 (en) | 2004-03-12 | 2005-09-29 | The Mclean Hospital Corporation | Salvinorin derivatives and uses thereof |
| CA2557794A1 (en) | 2004-03-15 | 2005-10-06 | Eli Lilly And Company | Opioid receptor antagonists |
| JP2007529523A (ja) | 2004-03-15 | 2007-10-25 | イーライ リリー アンド カンパニー | 肥満症を治療するためのオピオイド受容体拮抗物質としての４−（５−アミノメチル）−インドール−１−イルメチル）−ベンズアミド誘導体および関連化合物 |
| US8551986B2 (en) | 2005-12-08 | 2013-10-08 | The Mclean Hospital Corporation | Treatment of sequelae of psychiatric disorders |
| DK2001456T3 (da) | 2006-04-04 | 2010-04-12 | Emodys Gmbh | Anvendelse af kappa-opiodreceptorantagonistholde sammensætninger til behandling af dissociative forstyrrelser |
| US20100222345A1 (en) | 2006-08-09 | 2010-09-02 | Caroline Jean Diaz | Novel compounds as antagonists or inverse agonists for opioid receptors |
| WO2008021849A2 (en) | 2006-08-09 | 2008-02-21 | Smithkline Beecham Corporation | Novel compounds as antagonists or inverse agonists at opioid receptors |
| CN101511808A (zh) | 2006-09-08 | 2009-08-19 | 辉瑞产品公司 | 二芳基醚衍生物及其用途 |
| WO2009094260A1 (en) | 2008-01-22 | 2009-07-30 | Eli Lilly And Company | Kappa selective opioid receptor antagonist |
| BR112013002846A2 (pt) | 2010-08-05 | 2016-06-07 | Conrig Pharma Aps | derivados de tandospirona deuterada como agonista do receptor de 5-ht1a |
| EP2773352B1 (en) | 2011-12-09 | 2017-06-28 | Research Triangle Institute | 1-substituted 4-arylpiperazine as kappa opioid receptor antagonists |
| MX368870B (es) | 2013-12-20 | 2019-10-21 | H Lundbeck As | Uso de un antagonista de receptores de opioides con actividad kappa y vortioxetina para el tratamiento de trastorno depresivo con características melancólicas. |
| US10377698B2 (en) | 2015-03-30 | 2019-08-13 | University Of Innsbruck | Diphenethylamine derivatives which are inter alia useful as analgesics and method for their production |
| US10709685B2 (en) | 2015-05-28 | 2020-07-14 | Georgetown University | Use of methadone metabolites for treatment of anxiety and depression |
| WO2017218518A1 (en) | 2016-06-13 | 2017-12-21 | Board Of Regents Of The University Of Texas System | Pharmaceutical compositions and methods for treatment of pain |
| EP3490542A4 (en) | 2016-07-26 | 2020-07-08 | Flagship Pioneering Innovations V, Inc. | NEUROMODULATION COMPOSITIONS AND RELATED THERAPEUTIC METHODS FOR THE TREATMENT OF CANCER BY MODULATION OF AN ANTI-CANCER RESPONSE |
| JP7048572B6 (ja) | 2016-09-16 | 2023-12-20 | リサーチ トライアングル インスティテュート | テトラヒドロイソキノリンカッパーオピオイドアンタゴニスト |
| US10316021B2 (en) | 2016-11-28 | 2019-06-11 | Pfizer Inc. | Heteroarylphenoxy benzamide kappa opioid ligands |
| ES2926533T3 (es) | 2017-03-17 | 2022-10-26 | Scripps Research Inst | Antagonistas del receptor opioideo kappa y productos y métodos relacionados con los mismos |
| PH12018000077B1 (en) | 2017-07-05 | 2021-07-09 | Frimline Private Ltd | A pharmaceutical composition for neuropathic pain |
| US20190255036A1 (en) | 2018-02-16 | 2019-08-22 | Alexander Kariman | Compound and method for reducing neuropathic pain and depression |
| WO2019183556A1 (en) | 2018-03-23 | 2019-09-26 | University Of Kansas | Cyclic tetrapeptide analogs |
| US11491144B2 (en) | 2018-03-30 | 2022-11-08 | The Florida State University Research Foundation, Incorporated | Methods of treating fragile X mental retardation syndrome |
| JP2022505676A (ja) | 2018-10-23 | 2022-01-14 | ブラックソーン セラピューティクス インコーポレイテッド | 患者のスクリーニング、診断、及び層別化のためのシステム及び方法 |
| US20200171025A1 (en) | 2018-11-29 | 2020-06-04 | Srinivasa Rao Parella | Pharmaceutical composition comprising brexpiprazole and process for preparation thereof |
| US11266627B1 (en) * | 2021-05-04 | 2022-03-08 | Janssen Pharmaceuticals, Inc. | Compositions and methods for the treatment of depression |
| CN114195693A (zh) * | 2020-09-17 | 2022-03-18 | 广东东阳光药业有限公司 | 一种酰胺化合物的晶型及其制备方法 |
| US12161622B2 (en) | 2021-05-04 | 2024-12-10 | Janssen Pharmaceuticals, Inc. | Compositions and methods for the treatment of depression |
| AU2022268720A1 (en) | 2021-05-04 | 2023-12-21 | Janssen Pharmaceuticals, Inc. | Compositions and methods for the treatment of depression |
| EP4489730B1 (en) | 2022-03-07 | 2026-01-21 | Janssen Pharmaceuticals, Inc. | Compositions comprising aticaprant |
| WO2023170547A1 (en) | 2022-03-07 | 2023-09-14 | Janssen Pharmaceuticals, Inc. | Pure forms of crystalline aticaprant |
-
2023
- 2023-03-06 CN CN202380038808.6A patent/CN119156211A/zh active Pending
- 2023-03-06 CA CA3254365A patent/CA3254365A1/en active Pending
- 2023-03-06 TW TW112108148A patent/TW202345796A/zh unknown
- 2023-03-06 EP EP23712343.5A patent/EP4489747A1/en active Pending
- 2023-03-06 KR KR1020247033176A patent/KR20240156409A/ko active Pending
- 2023-03-06 AU AU2023232536A patent/AU2023232536A1/en active Pending
- 2023-03-06 WO PCT/IB2023/052088 patent/WO2023170550A1/en not_active Ceased
- 2023-03-06 IL IL315409A patent/IL315409A/en unknown
- 2023-03-06 US US18/178,961 patent/US11998524B2/en active Active
- 2023-03-06 JP JP2024553358A patent/JP2025508051A/ja active Pending
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- 2024-09-06 CO CONC2024/0012158A patent/CO2024012158A2/es unknown
- 2024-12-23 US US18/991,891 patent/US20250325515A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| US20250325515A1 (en) | 2025-10-23 |
| US20230277499A1 (en) | 2023-09-07 |
| CO2024012158A2 (es) | 2024-09-30 |
| US11998524B2 (en) | 2024-06-04 |
| JOP20240197A1 (ar) | 2024-09-05 |
| CL2024002627A1 (es) | 2025-01-24 |
| IL315409A (en) | 2024-11-01 |
| CN119156211A (zh) | 2024-12-17 |
| MX2024010980A (es) | 2024-12-06 |
| JP2025508051A (ja) | 2025-03-21 |
| TW202345796A (zh) | 2023-12-01 |
| US20240316003A1 (en) | 2024-09-26 |
| CA3254365A1 (en) | 2023-09-14 |
| KR20240156409A (ko) | 2024-10-29 |
| US12171743B2 (en) | 2024-12-24 |
| WO2023170550A1 (en) | 2023-09-14 |
| EP4489747A1 (en) | 2025-01-15 |
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