ES2616752T3 - Composición y cocristal de aprepitant L-prolina - Google Patents
Composición y cocristal de aprepitant L-prolina Download PDFInfo
- Publication number
- ES2616752T3 ES2616752T3 ES11779217.6T ES11779217T ES2616752T3 ES 2616752 T3 ES2616752 T3 ES 2616752T3 ES 11779217 T ES11779217 T ES 11779217T ES 2616752 T3 ES2616752 T3 ES 2616752T3
- Authority
- ES
- Spain
- Prior art keywords
- aprepitant
- proline
- crystal
- cocristal
- composition
- 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.)
- Active
Links
- ATALOFNDEOCMKK-OITMNORJSA-N aprepitant Chemical compound O([C@@H]([C@@H]1C=2C=CC(F)=CC=2)O[C@H](C)C=2C=C(C=C(C=2)C(F)(F)F)C(F)(F)F)CCN1CC1=NNC(=O)N1 ATALOFNDEOCMKK-OITMNORJSA-N 0.000 title abstract description 31
- 229960001372 aprepitant Drugs 0.000 title abstract description 31
- 239000013078 crystal Substances 0.000 title abstract description 28
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 title abstract description 27
- 229930182821 L-proline Natural products 0.000 title abstract description 27
- 229960002429 proline Drugs 0.000 title abstract description 27
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 29
- 238000000634 powder X-ray diffraction Methods 0.000 description 15
- 239000000523 sample Substances 0.000 description 8
- 238000012512 characterization method Methods 0.000 description 5
- 238000001460 carbon-13 nuclear magnetic resonance spectrum Methods 0.000 description 3
- 238000004090 dissolution Methods 0.000 description 3
- 238000002474 experimental method Methods 0.000 description 3
- 239000011521 glass Substances 0.000 description 3
- 230000005855 radiation Effects 0.000 description 3
- 238000002411 thermogravimetry Methods 0.000 description 3
- 238000004922 13C solid-state nuclear magnetic resonance spectroscopy Methods 0.000 description 2
- ORILYTVJVMAKLC-UHFFFAOYSA-N adamantane Chemical compound C1C(C2)CC3CC1CC2C3 ORILYTVJVMAKLC-UHFFFAOYSA-N 0.000 description 2
- 238000004458 analytical method Methods 0.000 description 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 2
- 238000000113 differential scanning calorimetry Methods 0.000 description 2
- 238000010494 dissociation reaction Methods 0.000 description 2
- 230000005593 dissociations Effects 0.000 description 2
- 239000012738 dissolution medium Substances 0.000 description 2
- 239000002609 medium Substances 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- 238000000425 proton nuclear magnetic resonance spectrum Methods 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 230000003595 spectral effect Effects 0.000 description 2
- 238000001228 spectrum Methods 0.000 description 2
- 239000007858 starting material Substances 0.000 description 2
- 238000005160 1H NMR spectroscopy Methods 0.000 description 1
- 239000005711 Benzoic acid Substances 0.000 description 1
- IAZDPXIOMUYVGZ-WFGJKAKNSA-N Dimethyl sulfoxide Chemical compound [2H]C([2H])([2H])S(=O)C([2H])([2H])[2H] IAZDPXIOMUYVGZ-WFGJKAKNSA-N 0.000 description 1
- 239000008186 active pharmaceutical agent Substances 0.000 description 1
- 125000003118 aryl group Chemical group 0.000 description 1
- 230000004888 barrier function Effects 0.000 description 1
- 235000010233 benzoic acid Nutrition 0.000 description 1
- 230000005540 biological transmission Effects 0.000 description 1
- 229910052799 carbon Inorganic materials 0.000 description 1
- 238000005119 centrifugation Methods 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 238000005384 cross polarization magic-angle spinning Methods 0.000 description 1
- 238000013480 data collection Methods 0.000 description 1
- 239000012153 distilled water Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 229910052739 hydrogen Inorganic materials 0.000 description 1
- 239000001257 hydrogen Substances 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 230000010354 integration Effects 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- LYGJENNIWJXYER-UHFFFAOYSA-N nitromethane Chemical compound C[N+]([O-])=O LYGJENNIWJXYER-UHFFFAOYSA-N 0.000 description 1
- 238000000655 nuclear magnetic resonance spectrum Methods 0.000 description 1
- 239000004033 plastic Substances 0.000 description 1
- 229920003223 poly(pyromellitimide-1,4-diphenyl ether) Polymers 0.000 description 1
- 229920001721 polyimide Polymers 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 239000008213 purified water Substances 0.000 description 1
- HDWRBQIOWXIBAB-WCCKRBBISA-N pyrrolidine;(2s)-pyrrolidine-2-carboxylic acid Chemical group C1CCNC1.OC(=O)[C@@H]1CCCN1 HDWRBQIOWXIBAB-WCCKRBBISA-N 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 229910052710 silicon Inorganic materials 0.000 description 1
- 239000010703 silicon Substances 0.000 description 1
- 229910000679 solder Inorganic materials 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- CZDYPVPMEAXLPK-UHFFFAOYSA-N tetramethylsilane Chemical compound C[Si](C)(C)C CZDYPVPMEAXLPK-UHFFFAOYSA-N 0.000 description 1
- 238000004448 titration Methods 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 230000004580 weight loss Effects 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P39/00—General protective or antinoxious agents
- A61P39/02—Antidotes
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Toxicology (AREA)
- Psychiatry (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38574410P | 2010-09-23 | 2010-09-23 | |
| US385744P | 2010-09-23 | ||
| US201161439654P | 2011-02-04 | 2011-02-04 | |
| US201161439654P | 2011-02-04 | ||
| US201161498214P | 2011-06-17 | 2011-06-17 | |
| US201161498214P | 2011-06-17 | ||
| PCT/IB2011/054210 WO2012038937A1 (en) | 2010-09-23 | 2011-09-23 | Aprepitant l-proline composition and cocrystal |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2616752T3 true ES2616752T3 (es) | 2017-06-14 |
Family
ID=44907915
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES11779217.6T Active ES2616752T3 (es) | 2010-09-23 | 2011-09-23 | Composición y cocristal de aprepitant L-prolina |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US9029369B2 (enExample) |
| EP (1) | EP2618828B1 (enExample) |
| JP (1) | JP5997162B2 (enExample) |
| KR (1) | KR101833578B1 (enExample) |
| CN (1) | CN103221049B (enExample) |
| AR (1) | AR083095A1 (enExample) |
| AU (1) | AU2011306391B2 (enExample) |
| BR (1) | BR112013006651A2 (enExample) |
| CA (1) | CA2846460C (enExample) |
| ES (1) | ES2616752T3 (enExample) |
| IL (1) | IL225443A0 (enExample) |
| TW (1) | TWI540131B (enExample) |
| WO (1) | WO2012038937A1 (enExample) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101833578B1 (ko) | 2010-09-23 | 2018-02-28 | 누포믹스 리미티드 | 아프레피탄트 l-프롤린 조성물 및 공결정 |
| US9532993B2 (en) | 2011-11-25 | 2017-01-03 | Nuformix Limited | Aprepitant L-proline solvates—compositions and cocrystals |
| US10098859B2 (en) | 2012-09-05 | 2018-10-16 | Amri Ssci, Llc | Cocrystals of p-coumaric acid |
| JP2017502973A (ja) * | 2013-12-30 | 2017-01-26 | オンコプレフェント ゲゼルシャフト ミット ベシュレンクテル ハフツング | 癌を予防する方法において使用するためのニューロキニン−１受容体アンタゴニスト |
| US10717755B2 (en) | 2018-02-07 | 2020-07-21 | Reata Pharmaceuticals, Inc. | Co-crystal forms of a novobiocin analog and proline |
| CN116283947A (zh) * | 2023-02-07 | 2023-06-23 | 成都医学院 | 一种阿瑞匹坦共晶及其制备方法和用途 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5145684A (en) | 1991-01-25 | 1992-09-08 | Sterling Drug Inc. | Surface modified drug nanoparticles |
| US5719147A (en) | 1992-06-29 | 1998-02-17 | Merck & Co., Inc. | Morpholine and thiomorpholine tachykinin receptor antagonists |
| US6048859A (en) | 1992-06-29 | 2000-04-11 | Merck & Co., Inc. | Morpholine and thiomorpholine tachykinin receptor antagonists |
| IL111960A (en) | 1993-12-17 | 1999-12-22 | Merck & Co Inc | Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them |
| ZA985765B (en) | 1997-07-02 | 1999-08-04 | Merck & Co Inc | Polymorphic form of a tachykinin receptor antagonist. |
| AU2003243699B2 (en) | 2002-06-21 | 2009-01-15 | Transform Pharmaceuticals, Inc. | Pharmaceutical compositions with improved dissolution |
| AU2003272270A1 (en) * | 2003-02-28 | 2004-09-28 | The Regents Of The University Of Michigan | Pharmaceutical co-crystal compositions of drugs such as carbamazeptine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen |
| WO2007147160A2 (en) * | 2006-06-16 | 2007-12-21 | Dr. Reddy's Laboratories Ltd. | Aprepitant compositions |
| EP2254555A4 (en) * | 2008-02-27 | 2013-10-09 | Reddys Lab Ltd Dr | APREPITANT FORMS WITH INCREASED SOLUBILITY AND PHARMACEUTICAL COMPOSITIONS FROM THEREOF |
| KR101833578B1 (ko) | 2010-09-23 | 2018-02-28 | 누포믹스 리미티드 | 아프레피탄트 l-프롤린 조성물 및 공결정 |
-
2011
- 2011-09-23 KR KR1020137010228A patent/KR101833578B1/ko active Active
- 2011-09-23 BR BR112013006651A patent/BR112013006651A2/pt not_active Application Discontinuation
- 2011-09-23 JP JP2013529758A patent/JP5997162B2/ja active Active
- 2011-09-23 TW TW100134362A patent/TWI540131B/zh active
- 2011-09-23 EP EP11779217.6A patent/EP2618828B1/en active Active
- 2011-09-23 WO PCT/IB2011/054210 patent/WO2012038937A1/en not_active Ceased
- 2011-09-23 US US13/825,380 patent/US9029369B2/en active Active
- 2011-09-23 CA CA2846460A patent/CA2846460C/en active Active
- 2011-09-23 CN CN201180055997.5A patent/CN103221049B/zh active Active
- 2011-09-23 AU AU2011306391A patent/AU2011306391B2/en active Active
- 2011-09-23 AR ARP110103486 patent/AR083095A1/es unknown
- 2011-09-23 ES ES11779217.6T patent/ES2616752T3/es active Active
-
2013
- 2013-03-21 IL IL225443A patent/IL225443A0/en active IP Right Grant
Also Published As
| Publication number | Publication date |
|---|---|
| TW201217366A (en) | 2012-05-01 |
| TWI540131B (zh) | 2016-07-01 |
| AU2011306391A1 (en) | 2013-04-11 |
| AU2011306391B2 (en) | 2016-12-15 |
| CA2846460C (en) | 2019-01-08 |
| CN103221049B (zh) | 2015-11-25 |
| JP5997162B2 (ja) | 2016-09-28 |
| EP2618828A1 (en) | 2013-07-31 |
| WO2012038937A1 (en) | 2012-03-29 |
| US20130252949A1 (en) | 2013-09-26 |
| CA2846460A1 (en) | 2012-03-29 |
| US9029369B2 (en) | 2015-05-12 |
| EP2618828B1 (en) | 2016-11-23 |
| BR112013006651A2 (pt) | 2017-07-18 |
| KR101833578B1 (ko) | 2018-02-28 |
| JP2013537901A (ja) | 2013-10-07 |
| KR20140040671A (ko) | 2014-04-03 |
| CN103221049A (zh) | 2013-07-24 |
| AR083095A1 (es) | 2013-01-30 |
| HK1187554A1 (zh) | 2014-04-11 |
| IL225443A0 (en) | 2013-06-27 |
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