OA12665A - New anhydrous crystalline forms of gabapentin. - Google Patents

New anhydrous crystalline forms of gabapentin. Download PDF

Info

Publication number: OA12665A
Authority: OA; OAPI
Prior art keywords: gabapentin; dehydrate; crystalline; following; monohydrate
Prior art date: 2001-10-09

Application number

OA1200400095A

Other languages

English (en)

Inventor

Suresh R Babu

Claude Jeffrey Calvitt

Linna R Chen

Brian TOBIAS

Original Assignee

Warner Lambert Co

Priority date (The priority date 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 date listed.)

2001-10-09

Filing date

2002-10-03

Publication date

2006-06-19

2002-10-03 Application filed by Warner Lambert Co filed Critical Warner Lambert Co

2006-06-19 Publication of OA12665A publication Critical patent/OA12665A/en

Links

UGJMXCAKCUNAIE-UHFFFAOYSA-N Gabapentin Chemical compound OC(=O)CC1(CN)CCCCC1 UGJMXCAKCUNAIE-UHFFFAOYSA-N 0.000 title claims abstract description 85
229960002870 gabapentin Drugs 0.000 title claims abstract description 42
WRSFRDZQQUAKNA-UHFFFAOYSA-N 2-[1-(aminomethyl)cyclohexyl]acetic acid;hydrate Chemical compound O.OC(=O)CC1(CN)CCCCC1 WRSFRDZQQUAKNA-UHFFFAOYSA-N 0.000 claims abstract description 19
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 14
238000000034 method Methods 0.000 claims description 10
239000000126 substance Substances 0.000 claims description 10
238000000634 powder X-ray diffraction Methods 0.000 claims description 8
230000000694 effects Effects 0.000 claims description 7
239000002904 solvent Substances 0.000 claims description 6
239000011877 solvent mixture Substances 0.000 claims description 5
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 3
239000002274 desiccant Substances 0.000 claims description 2
230000005855 radiation Effects 0.000 claims 6
229910016523 CuKa Inorganic materials 0.000 claims 4
238000004519 manufacturing process Methods 0.000 abstract description 3
239000003814 drug Substances 0.000 abstract description 2
229940124597 therapeutic agent Drugs 0.000 abstract description 2
150000004682 monohydrates Chemical class 0.000 description 8
OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 6
239000000843 powder Substances 0.000 description 6
238000001144 powder X-ray diffraction data Methods 0.000 description 4
238000001228 spectrum Methods 0.000 description 4
VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 description 3
238000012856 packing Methods 0.000 description 3
238000006243 chemical reaction Methods 0.000 description 2
150000001875 compounds Chemical class 0.000 description 2
238000010438 heat treatment Methods 0.000 description 2
XBUDZAQEMFGLEU-UHFFFAOYSA-N 2-[1-(aminomethyl)cyclohexyl]acetic acid;hydron;chloride Chemical compound Cl.OC(=O)CC1(CN)CCCCC1 XBUDZAQEMFGLEU-UHFFFAOYSA-N 0.000 description 1
RYGMFSIKBFXOCR-UHFFFAOYSA-N Copper Chemical compound [Cu] RYGMFSIKBFXOCR-UHFFFAOYSA-N 0.000 description 1
LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
208000006083 Hypokinesia Diseases 0.000 description 1
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 description 1
238000005481 NMR spectroscopy Methods 0.000 description 1
229910052581 Si3N4 Inorganic materials 0.000 description 1
239000002253 acid Substances 0.000 description 1
238000004458 analytical method Methods 0.000 description 1
238000003556 assay Methods 0.000 description 1
238000001460 carbon-13 nuclear magnetic resonance spectrum Methods 0.000 description 1
229910052802 copper Inorganic materials 0.000 description 1
239000010949 copper Substances 0.000 description 1
238000005388 cross polarization Methods 0.000 description 1
230000008034 disappearance Effects 0.000 description 1
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
238000011549 displacement method Methods 0.000 description 1
208000002173 dizziness Diseases 0.000 description 1
238000001035 drying Methods 0.000 description 1
238000000921 elemental analysis Methods 0.000 description 1
206010015037 epilepsy Diseases 0.000 description 1
YUWFEBAXEOLKSG-UHFFFAOYSA-N hexamethylbenzene Chemical compound CC1=C(C)C(C)=C(C)C(C)=C1C YUWFEBAXEOLKSG-UHFFFAOYSA-N 0.000 description 1
238000004128 high performance liquid chromatography Methods 0.000 description 1
230000003483 hypokinetic effect Effects 0.000 description 1
208000014674 injury Diseases 0.000 description 1
238000002844 melting Methods 0.000 description 1
230000008018 melting Effects 0.000 description 1
239000000203 mixture Substances 0.000 description 1
239000003960 organic solvent Substances 0.000 description 1
239000002243 precursor Substances 0.000 description 1
238000001953 recrystallisation Methods 0.000 description 1
238000007790 scraping Methods 0.000 description 1
238000007789 sealing Methods 0.000 description 1
HQVNEWCFYHHQES-UHFFFAOYSA-N silicon nitride Chemical compound N12[Si]34N5[Si]62N3[Si]51N64 HQVNEWCFYHHQES-UHFFFAOYSA-N 0.000 description 1
229910052708 sodium Inorganic materials 0.000 description 1
239000011734 sodium Substances 0.000 description 1
239000007787 solid Substances 0.000 description 1
238000000279 solid-state nuclear magnetic resonance spectrum Methods 0.000 description 1
238000001179 sorption measurement Methods 0.000 description 1
238000009987 spinning Methods 0.000 description 1
238000000967 suction filtration Methods 0.000 description 1
238000002560 therapeutic procedure Methods 0.000 description 1
230000008733 trauma Effects 0.000 description 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C227/38—Separation; Purification; Stabilisation; Use of additives
- C07C227/40—Separation; Purification
- C07C227/42—Crystallisation
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C229/28—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and containing rings
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
- C07C2601/14—The ring being saturated

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Crystallography & Structural Chemistry (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

OA1200400095A 2001-10-09 2002-10-03 New anhydrous crystalline forms of gabapentin. OA12665A (en)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
US32837501P	2001-10-09	2001-10-09
US10/256,155 US6800782B2 (en)	2001-10-09	2002-09-25	Anhydrous crystalline forms of gabapentin

Publications (1)

Publication Number	Publication Date
OA12665A true OA12665A (en)	2006-06-19

Family

ID=26945177

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
OA1200400095A OA12665A (en)	2001-10-09	2002-10-03	New anhydrous crystalline forms of gabapentin.

Country Status (27)

Country	Link
US (1)	US6800782B2 (sr)
EP (1)	EP1463712A1 (sr)
JP (1)	JP2005505594A (sr)
KR (1)	KR20050033525A (sr)
CN (1)	CN1568305A (sr)
AP (1)	AP2004003025A0 (sr)
BG (1)	BG108702A (sr)
BR (1)	BR0213156A (sr)
CA (1)	CA2462331A1 (sr)
CO (1)	CO5570697A2 (sr)
CZ (1)	CZ2004416A3 (sr)
EA (1)	EA006557B1 (sr)
GE (1)	GEP20063936B (sr)
HR (1)	HRP20040408A2 (sr)
HU (1)	HUP0401782A3 (sr)
IL (1)	IL161099A0 (sr)
IS (1)	IS7195A (sr)
MA (1)	MA27072A1 (sr)
MX (1)	MXPA04003301A (sr)
NO (1)	NO20041370L (sr)
NZ (1)	NZ531993A (sr)
OA (1)	OA12665A (sr)
PL (1)	PL368117A1 (sr)
RS (1)	RS28204A (sr)
SK (1)	SK1572004A3 (sr)
TN (1)	TNSN04055A1 (sr)
WO (1)	WO2003031391A1 (sr)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US20070043236A1 (en) *	2003-05-19	2007-02-22	Chandiran Thakashina M	Process for preparation of gabapentin
WO2004106281A1 (en) *	2003-05-30	2004-12-09	Ranbaxy Laboratories Limited	Crystalline gabapentin
WO2004110342A2 (en) *	2003-06-12	2004-12-23	Matrix Laboratories Ltd	Novel polymorph of gabapentin and its conversion to gabapentin form-ii
US7169812B2 (en) *	2003-07-01	2007-01-30	Medtronic, Inc.	Process for producing injectable gabapentin compositions
ITMI20040579A1 (it) *	2004-03-25	2004-06-25	Zambon Spa	Processo di preparazione di gabapentina
WO2010023694A2 (en) *	2008-09-01	2010-03-04	Hikal Ltd	Crystalline forms of gabapentin and process thereof
CN104649921B (zh) *	2015-01-14	2016-09-28	天津大学	一种加巴喷丁与己二酸共晶及其制备方法
CN116693410B (zh) *	2023-06-08	2024-06-07	浙江竹子制药有限公司	一种粒径可控的加巴喷丁制备方法

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
DE2460891C2 (de) *	1974-12-21	1982-09-23	Gödecke AG, 1000 Berlin	1-Aminomethyl-1-cycloalkanessigsäuren und deren Ester, Verfahren zu deren Herstellung und diese Verbindungen enthaltende Arzneimittel
US4087544A (en) *	1974-12-21	1978-05-02	Warner-Lambert Company	Treatment of cranial dysfunctions using novel cyclic amino acids
JPS62247160A (ja) *	1986-03-31	1987-10-28	Aisin Seiki Co Ltd	スタ−リングエンジンの始動装置
US4894476A (en) *	1988-05-02	1990-01-16	Warner-Lambert Company	Gabapentin monohydrate and a process for producing the same
US4960931A (en) *	1988-05-02	1990-10-02	Warner-Lambert Company	Gabapentin mohohydrate and a process for producing the same
DE3928184A1 (de) *	1989-08-25	1991-02-28	Goedecke Ag	Verfahren zur herstellung von cyclischen aminosaeurederivaten sowie zwischenprodukte
IL119890A (en)	1996-12-24	2002-03-10	Teva Pharma	Gabapentin form iii and preparation of gabapentin form ii
ES2137137B1 (es)	1998-05-25	2000-08-16	Medichem Sa	Nuevo polimorfo de gabapentina no hidratada, su procedimiento de obtencion y su utilizacion para la obtencion de gabapentina de calidad farmaceutica.

2002
- 2002-09-25 US US10/256,155 patent/US6800782B2/en not_active Expired - Fee Related
- 2002-10-03 EP EP02766485A patent/EP1463712A1/en not_active Withdrawn
- 2002-10-03 HU HU0401782A patent/HUP0401782A3/hu unknown
- 2002-10-03 OA OA1200400095A patent/OA12665A/en unknown
- 2002-10-03 CA CA002462331A patent/CA2462331A1/en not_active Abandoned
- 2002-10-03 CZ CZ2004416A patent/CZ2004416A3/cs unknown
- 2002-10-03 EA EA200400417A patent/EA006557B1/ru not_active IP Right Cessation
- 2002-10-03 AP APAP/P/2004/003025A patent/AP2004003025A0/en unknown
- 2002-10-03 WO PCT/US2002/031706 patent/WO2003031391A1/en not_active Ceased
- 2002-10-03 HR HR20040408A patent/HRP20040408A2/hr not_active Application Discontinuation
- 2002-10-03 JP JP2003534375A patent/JP2005505594A/ja active Pending
- 2002-10-03 BR BR0213156-0A patent/BR0213156A/pt not_active IP Right Cessation
- 2002-10-03 MX MXPA04003301A patent/MXPA04003301A/es active IP Right Grant
- 2002-10-03 KR KR1020047005149A patent/KR20050033525A/ko not_active Ceased
- 2002-10-03 SK SK157-2004A patent/SK1572004A3/sk not_active Application Discontinuation
- 2002-10-03 PL PL02368117A patent/PL368117A1/xx not_active Application Discontinuation
- 2002-10-03 RS YU28204A patent/RS28204A/sr unknown
- 2002-10-03 CN CNA02820056XA patent/CN1568305A/zh active Pending
- 2002-10-03 GE GE5594A patent/GEP20063936B/en unknown
- 2002-10-03 IL IL16109902A patent/IL161099A0/xx unknown
- 2002-10-03 NZ NZ531993A patent/NZ531993A/en unknown
2004
- 2004-03-23 IS IS7195A patent/IS7195A/is unknown
- 2004-04-01 NO NO20041370A patent/NO20041370L/no not_active Application Discontinuation
- 2004-04-05 MA MA27606A patent/MA27072A1/fr unknown
- 2004-04-06 CO CO04032599A patent/CO5570697A2/es not_active Application Discontinuation
- 2004-04-07 TN TNP2004000055A patent/TNSN04055A1/fr unknown
- 2004-04-28 BG BG108702A patent/BG108702A/xx unknown

Also Published As

Publication number	Publication date
BG108702A (en)	2005-05-31
HRP20040408A2 (en)	2004-10-31
GEP20063936B (en)	2006-10-10
HUP0401782A2 (hu)	2005-10-28
MXPA04003301A (es)	2004-07-23
HUP0401782A3 (en)	2006-01-30
EA200400417A1 (ru)	2004-10-28
EP1463712A1 (en)	2004-10-06
IL161099A0 (en)	2004-08-31
BR0213156A (pt)	2004-09-14
CO5570697A2 (es)	2005-10-31
US20030092933A1 (en)	2003-05-15
RS28204A (sr)	2006-12-15
NO20041370L (no)	2004-04-01
CZ2004416A3 (cs)	2005-03-16
CN1568305A (zh)	2005-01-19
TNSN04055A1 (fr)	2006-06-01
PL368117A1 (en)	2005-03-21
KR20050033525A (ko)	2005-04-12
SK1572004A3 (sk)	2005-03-04
AP2004003025A0 (en)	2004-06-30
MA27072A1 (fr)	2004-12-20
CA2462331A1 (en)	2003-04-17
US6800782B2 (en)	2004-10-05
WO2003031391A1 (en)	2003-04-17
NZ531993A (en)	2006-09-29
IS7195A (is)	2004-03-23
JP2005505594A (ja)	2005-02-24
EA006557B1 (ru)	2006-02-24

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