TW201613888A - Crystalline forms of an NK-1 antagonist - Google Patents
Crystalline forms of an NK-1 antagonistInfo
- Publication number
- TW201613888A TW201613888A TW104129368A TW104129368A TW201613888A TW 201613888 A TW201613888 A TW 201613888A TW 104129368 A TW104129368 A TW 104129368A TW 104129368 A TW104129368 A TW 104129368A TW 201613888 A TW201613888 A TW 201613888A
- Authority
- TW
- Taiwan
- Prior art keywords
- crystalline forms
- antagonist
- propanamide
- methylpiperazin
- pyridin
- Prior art date
Links
- 239000002742 neurokinin 1 receptor antagonist Substances 0.000 title abstract 2
- 206010047700 Vomiting Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- WAXQNWCZJDTGBU-UHFFFAOYSA-N netupitant Chemical compound C=1N=C(N2CCN(C)CC2)C=C(C=2C(=CC=CC=2)C)C=1N(C)C(=O)C(C)(C)C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1 WAXQNWCZJDTGBU-UHFFFAOYSA-N 0.000 abstract 1
- 230000008673 vomiting Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462055836P | 2014-09-26 | 2014-09-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TW201613888A true TW201613888A (en) | 2016-04-16 |
Family
ID=54601836
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW104129368A TW201613888A (en) | 2014-09-26 | 2015-09-04 | Crystalline forms of an NK-1 antagonist |
Country Status (9)
| Country | Link |
|---|---|
| US (5) | US9951016B2 (zh) |
| EP (1) | EP3197871A2 (zh) |
| JP (1) | JP2017529380A (zh) |
| KR (1) | KR20170063768A (zh) |
| CN (1) | CN107001275A (zh) |
| AU (1) | AU2015323515A1 (zh) |
| CA (1) | CA2960599A1 (zh) |
| TW (1) | TW201613888A (zh) |
| WO (1) | WO2016046638A2 (zh) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20150315149A1 (en) * | 2014-05-05 | 2015-11-05 | Apicore Us Llc | Methods of making netupitant and intermediates thereof |
| TW201613888A (en) | 2014-09-26 | 2016-04-16 | Helsinn Healthcare Sa | Crystalline forms of an NK-1 antagonist |
| WO2021202286A1 (en) * | 2020-03-30 | 2021-10-07 | Dignify Therapeutics, Llc | Compositions and methods for treating autonomic dysreflexia |
| US12097197B2 (en) | 2021-12-21 | 2024-09-24 | Slayback Pharma Llc | Stable liquid compositions of netupitant and palonosetron |
| EP4385497A1 (en) | 2022-12-12 | 2024-06-19 | Alfred E. Tiefenbacher (GmbH & Co. KG) | Antioxidant-free fixed dose combination of netupitant and palonosetron |
| WO2024126408A1 (en) | 2022-12-12 | 2024-06-20 | Alfred E. Tiefenbacher (Gmbh & Co. Kg) | Antioxidant-free fixed dose combination of netupitant and palonosetron |
| WO2024126398A1 (en) | 2022-12-12 | 2024-06-20 | Alfred E. Tiefenbacher (Gmbh & Co. Kg) | Fixed dose combination comprising netupitant and palonosetron |
| EP4385500A1 (en) | 2022-12-12 | 2024-06-19 | Alfred E. Tiefenbacher (GmbH & Co. KG) | Fixed dose combination comprising netupitant and palonosetron |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3720493A1 (de) * | 1987-06-20 | 1989-01-26 | Nattermann A & Cie | Arzneizubereitungen mit mikronisierten ebselen-kristallen |
| US5271944A (en) * | 1991-04-05 | 1993-12-21 | Biofor, Ltd. | Pharmacologically enhanced formulations |
| IL111960A (en) | 1993-12-17 | 1999-12-22 | Merck & Co Inc | Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them |
| EP0737192B1 (en) | 1993-12-29 | 2001-10-31 | Merck Sharp & Dohme Ltd. | Substituted morpholine derivatives and their use as therapeutic agents |
| TW385308B (en) | 1994-03-04 | 2000-03-21 | Merck & Co Inc | Prodrugs of morpholine tachykinin receptor antagonists |
| HU226608B1 (hu) * | 1996-08-22 | 2009-04-28 | Rtp Pharma Corp | Vízoldhatalan anyagok mikrorészecskéit tartalmazó készítmények és ezek elõállítására szolgáló eljárások |
| US5972938A (en) | 1997-12-01 | 1999-10-26 | Merck & Co., Inc. | Method for treating or preventing psychoimmunological disorders |
| SE1035115T5 (sv) * | 1999-02-24 | 2015-08-04 | Hoffmann La Roche | 4-fenylpyridin-derivat och deras anvaendning som NK-1 receptor-antagonister |
| JP3849428B2 (ja) * | 1999-04-23 | 2006-11-22 | 日本新薬株式会社 | 微粉化法 |
| US7655800B2 (en) * | 2005-02-02 | 2010-02-02 | Eisai R & D Management Co., Ltd. | Crystalline 1H-imidazo[4,5-b]pyridin-5-amine, 7-[5-[(cyclohexylmethylamino)-methyl]-1H-indol-2-yl]-2-methyl, sulfate (1:1), trihydrate and its pharmaceutical uses |
| CA3240562A1 (en) * | 2007-12-04 | 2009-06-11 | Remedy Pharmaceuticals, Inc. | Improved formulations and methods for lyophilization and lyophilates provided thereby |
| KR20130137595A (ko) * | 2010-08-10 | 2013-12-17 | 루핀 리미티드 | 블로난세린을 함유하는 경구용 서방성 약학 조성물 |
| US8426450B1 (en) * | 2011-11-29 | 2013-04-23 | Helsinn Healthcare Sa | Substituted 4-phenyl pyridines having anti-emetic effect |
| CN103897026A (zh) * | 2012-12-29 | 2014-07-02 | 朱继东 | 硼替佐米关键中间体的晶型，制备方法及其运用 |
| TW201613888A (en) * | 2014-09-26 | 2016-04-16 | Helsinn Healthcare Sa | Crystalline forms of an NK-1 antagonist |
-
2015
- 2015-09-04 TW TW104129368A patent/TW201613888A/zh unknown
- 2015-09-24 AU AU2015323515A patent/AU2015323515A1/en not_active Abandoned
- 2015-09-24 WO PCT/IB2015/002031 patent/WO2016046638A2/en active Application Filing
- 2015-09-24 CA CA2960599A patent/CA2960599A1/en active Pending
- 2015-09-24 CN CN201580062289.2A patent/CN107001275A/zh active Pending
- 2015-09-24 EP EP15797399.1A patent/EP3197871A2/en not_active Withdrawn
- 2015-09-24 KR KR1020177010823A patent/KR20170063768A/ko unknown
- 2015-09-24 JP JP2017516719A patent/JP2017529380A/ja active Pending
- 2015-09-25 US US14/865,370 patent/US9951016B2/en active Active
-
2018
- 2018-03-12 US US15/918,868 patent/US10233154B2/en active Active
-
2019
- 2019-01-28 US US16/259,913 patent/US10676440B2/en active Active
-
2020
- 2020-04-30 US US16/863,038 patent/US10961195B2/en active Active
-
2021
- 2021-02-25 US US17/185,206 patent/US12071406B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US20200255381A1 (en) | 2020-08-13 |
| CA2960599A1 (en) | 2016-03-31 |
| AU2015323515A1 (en) | 2017-03-16 |
| US9951016B2 (en) | 2018-04-24 |
| US20180201581A1 (en) | 2018-07-19 |
| US20210269401A1 (en) | 2021-09-02 |
| JP2017529380A (ja) | 2017-10-05 |
| US10676440B2 (en) | 2020-06-09 |
| WO2016046638A2 (en) | 2016-03-31 |
| US10233154B2 (en) | 2019-03-19 |
| WO2016046638A3 (en) | 2016-06-09 |
| US20190152915A1 (en) | 2019-05-23 |
| EP3197871A2 (en) | 2017-08-02 |
| CN107001275A (zh) | 2017-08-01 |
| US20160090359A1 (en) | 2016-03-31 |
| US12071406B2 (en) | 2024-08-27 |
| KR20170063768A (ko) | 2017-06-08 |
| US10961195B2 (en) | 2021-03-30 |
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