OA11956A - Polymorphs of a crystalline azabicyclo (2,2,2) octan-3-amine citrate and their pharmaceutical compositions. - Google Patents

Polymorphs of a crystalline azabicyclo (2,2,2) octan-3-amine citrate and their pharmaceutical compositions. Download PDF

Info

Publication number: OA11956A
Authority: OA; OAPI
Prior art keywords: citrate monohydrate; citrate; crystalline; hours; octan
Prior art date: 1999-06-01

Application number

OA1200100318A

Other languages

English (en)

Inventor

Michael James Castaldi

George Joseph Quallich

Lewin Theophilus Wint

Original Assignee

Pfizer Prod Inc

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.)

1999-06-01

Filing date

2000-05-18

Publication date

2006-04-13

2000-05-18 Application filed by Pfizer Prod Inc filed Critical Pfizer Prod Inc

2006-04-13 Publication of OA11956A publication Critical patent/OA11956A/en

Links

239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 6
WCQNEVLYWBFPSQ-UHFFFAOYSA-N 2-hydroxypropane-1,2,3-tricarboxylic acid;octan-3-amine Chemical compound CCCCCC(N)CC.OC(=O)CC(O)(C(O)=O)CC(O)=O WCQNEVLYWBFPSQ-UHFFFAOYSA-N 0.000 title claims description 4
YASYEJJMZJALEJ-UHFFFAOYSA-N Citric acid monohydrate Chemical compound O.OC(=O)CC(O)(C(O)=O)CC(O)=O YASYEJJMZJALEJ-UHFFFAOYSA-N 0.000 claims abstract description 15
206010047700 Vomiting Diseases 0.000 claims abstract description 6
239000000203 mixture Substances 0.000 claims abstract description 6
KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 16
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 12
CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 6
102000002002 Neurokinin-1 Receptors Human genes 0.000 claims description 4
108010040718 Neurokinin-1 Receptors Proteins 0.000 claims description 4
238000001914 filtration Methods 0.000 claims description 4
239000012458 free base Substances 0.000 claims description 4
238000000034 method Methods 0.000 claims description 4
150000001875 compounds Chemical class 0.000 claims description 3
238000002425 crystallisation Methods 0.000 claims description 3
230000008025 crystallization Effects 0.000 claims description 3
238000004519 manufacturing process Methods 0.000 claims description 3
238000000634 powder X-ray diffraction Methods 0.000 claims description 3
ZAFNJMIOTHYJRJ-UHFFFAOYSA-N Diisopropyl ether Chemical compound CC(C)OC(C)C ZAFNJMIOTHYJRJ-UHFFFAOYSA-N 0.000 claims description 2
238000001035 drying Methods 0.000 claims description 2
KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 3
238000003756 stirring Methods 0.000 claims 2
PEGOJNFMPFGHLY-UHFFFAOYSA-N 2-hydroxypropane-1,2,3-tricarboxylic acid;octan-3-amine;hydrate Chemical compound O.CCCCCC(N)CC.OC(=O)CC(O)(C(O)=O)CC(O)=O PEGOJNFMPFGHLY-UHFFFAOYSA-N 0.000 claims 1
230000001747 exhibiting effect Effects 0.000 claims 1
238000005469 granulation Methods 0.000 claims 1
230000003179 granulation Effects 0.000 claims 1
125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
JASMWYNKLTULAN-UHFFFAOYSA-N octan-3-amine Chemical compound CCCCCC(N)CC JASMWYNKLTULAN-UHFFFAOYSA-N 0.000 abstract description 2
239000002775 capsule Substances 0.000 abstract 1
238000009472 formulation Methods 0.000 abstract 1
239000012729 immediate-release (IR) formulation Substances 0.000 abstract 1
238000001990 intravenous administration Methods 0.000 abstract 1
239000006186 oral dosage form Substances 0.000 abstract 1
150000004682 monohydrates Chemical class 0.000 description 5
IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 4
KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 3
238000004458 analytical method Methods 0.000 description 3
229960004106 citric acid Drugs 0.000 description 3
235000015165 citric acid Nutrition 0.000 description 3
239000002002 slurry Substances 0.000 description 3
RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
239000000155 melt Substances 0.000 description 2
229910052757 nitrogen Inorganic materials 0.000 description 2
239000000843 powder Substances 0.000 description 2
238000010926 purge Methods 0.000 description 2
239000002464 receptor antagonist Substances 0.000 description 2
229940044551 receptor antagonist Drugs 0.000 description 2
239000007787 solid Substances 0.000 description 2
WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 1
238000006243 chemical reaction Methods 0.000 description 1
238000004090 dissolution Methods 0.000 description 1
239000002895 emetic Substances 0.000 description 1
238000005259 measurement Methods 0.000 description 1
239000006187 pill Substances 0.000 description 1
238000001907 polarising light microscopy Methods 0.000 description 1
238000000425 proton nuclear magnetic resonance spectrum Methods 0.000 description 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
- 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
- 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

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
General Health & Medical Sciences (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Bioinformatics & Cheminformatics (AREA)
Pharmacology & Pharmacy (AREA)
Engineering & Computer Science (AREA)
Animal Behavior & Ethology (AREA)
Chemical Kinetics & Catalysis (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Hospice & Palliative Care (AREA)
Otolaryngology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicinal Preparation (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

OA1200100318A 1999-06-01 2000-05-18 Polymorphs of a crystalline azabicyclo (2,2,2) octan-3-amine citrate and their pharmaceutical compositions. OA11956A (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US13699299P	1999-06-01	1999-06-01

Publications (1)

Publication Number	Publication Date
OA11956A true OA11956A (en)	2006-04-13

Family

ID=22475338

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
OA1200100318A OA11956A (en)	1999-06-01	2000-05-18	Polymorphs of a crystalline azabicyclo (2,2,2) octan-3-amine citrate and their pharmaceutical compositions.

Country Status (48)

Country	Link
US (1)	US6255320B1 (de)
EP (1)	EP1181290B1 (de)
JP (1)	JP3830816B2 (de)
KR (1)	KR100476606B1 (de)
CN (1)	CN1146565C (de)
AP (1)	AP2001002349A0 (de)
AR (1)	AR033331A1 (de)
AT (1)	ATE244239T1 (de)
AU (1)	AU767334B2 (de)
BG (1)	BG65240B1 (de)
BR (1)	BR0011094A (de)
CA (1)	CA2372238C (de)
CO (1)	CO5170463A1 (de)
CY (1)	CY2007011I1 (de)
CZ (1)	CZ295819B6 (de)
DE (1)	DE60003679T2 (de)
DK (1)	DK1181290T3 (de)
DZ (1)	DZ3050A1 (de)
EA (1)	EA003731B1 (de)
EC (1)	ECSP003508A (de)
EE (1)	EE200100656A (de)
ES (1)	ES2199825T3 (de)
GT (1)	GT200000087A (de)
HN (1)	HN2000000077A (de)
HR (1)	HRP20010904A2 (de)
HU (1)	HUP0201301A3 (de)
IL (1)	IL146406A0 (de)
MA (1)	MA26742A1 (de)
MX (1)	MXPA01012325A (de)
MY (1)	MY133508A (de)
NO (1)	NO20015848L (de)
NZ (1)	NZ515349A (de)
OA (1)	OA11956A (de)
PA (1)	PA8496101A1 (de)
PE (1)	PE20010209A1 (de)
PL (1)	PL196046B1 (de)
PT (1)	PT1181290E (de)
SI (1)	SI1181290T1 (de)
SK (1)	SK285820B6 (de)
SV (1)	SV2001000093A (de)
TN (1)	TNSN00120A1 (de)
TR (1)	TR200103473T2 (de)
TW (1)	TWI285204B (de)
UA (1)	UA66925C2 (de)
UY (1)	UY26176A1 (de)
WO (1)	WO2000073304A1 (de)
YU (1)	YU81101A (de)
ZA (1)	ZA200109775B (de)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
BRPI0507301A (pt) *	2004-01-30	2007-06-26	Pfizer Prod Inc	composições farmacêuticas de antagonistas do receptor de nuerocinina e ciclodextrina e métodos para melhor toleráncia no local de injeção
MXPA06007964A (es) *	2004-01-30	2007-01-26	Pfizer Prod Inc	Antagonistas del receptor nk-1 para mejorar la recuperacion de anestesia.
JP5021318B2 (ja) *	2004-01-30	2012-09-05	ファイザー・プロダクツ・インク	β−シクロデキストリンを液体投薬形態に用いて多用量製剤を達成するための抗菌性防腐剤
KR100812046B1 (ko) *	2004-02-02	2008-03-10	화이자 프로덕츠 인크.	1-(2ｓ,3ｓ)-2-벤즈히드릴-ｎ-(5-삼급-부틸-2-메톡시벤질)퀴누클리딘-3-아민의 제조 방법
SG11201507286QA (en) *	2013-03-15	2015-10-29	Pearl Therapeutics Inc	Methods and systems for conditioning of particulate crystalline materials
CN110577522B (zh) *	2018-06-07	2022-12-27	东莞市东阳光动物保健药品有限公司	马罗匹坦柠檬酸盐新晶型及其制备方法
CN112979639B (zh) *	2019-12-16	2025-08-08	凯默斯医药科技(上海)有限公司	一种马罗皮坦新晶型及其制备方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
UA27776C2 (uk) *	1991-05-31	2000-10-16	Пфайзер Інк.	Похідні хінуклідину та їх фармацевтично прийнятні солі, що є антагоністами речовини р у ссавців, фармацевтична композиція, що має антагоністичну дію на речовину р у ссавців
US5393762A (en) *	1993-06-04	1995-02-28	Pfizer Inc.	Pharmaceutical agents for treatment of emesis
US5576317A (en) *	1994-12-09	1996-11-19	Pfizer Inc.	NK-1 receptor antagonists and 5HT3 receptor antagonists for the treatment of emesis

2000
- 2000-05-08 US US09/566,307 patent/US6255320B1/en not_active Expired - Lifetime
- 2000-05-17 HN HN2000000077A patent/HN2000000077A/es unknown
- 2000-05-18 UA UA2001118214A patent/UA66925C2/uk unknown
- 2000-05-18 OA OA1200100318A patent/OA11956A/en unknown
- 2000-05-18 PL PL00352716A patent/PL196046B1/pl not_active IP Right Cessation
- 2000-05-18 EA EA200101108A patent/EA003731B1/ru active Protection Beyond IP Right Term
- 2000-05-18 DE DE60003679T patent/DE60003679T2/de not_active Expired - Lifetime
- 2000-05-18 ES ES00925528T patent/ES2199825T3/es not_active Expired - Lifetime
- 2000-05-18 AU AU44248/00A patent/AU767334B2/en not_active Expired
- 2000-05-18 NZ NZ515349A patent/NZ515349A/xx unknown
- 2000-05-18 TR TR2001/03473T patent/TR200103473T2/xx unknown
- 2000-05-18 WO PCT/IB2000/000665 patent/WO2000073304A1/en not_active Ceased
- 2000-05-18 PT PT00925528T patent/PT1181290E/pt unknown
- 2000-05-18 EP EP00925528A patent/EP1181290B1/de not_active Expired - Lifetime
- 2000-05-18 YU YU81101A patent/YU81101A/sh unknown
- 2000-05-18 HU HU0201301A patent/HUP0201301A3/hu unknown
- 2000-05-18 SI SI200030161T patent/SI1181290T1/xx unknown
- 2000-05-18 CZ CZ20014269A patent/CZ295819B6/cs not_active IP Right Cessation
- 2000-05-18 CN CNB008082782A patent/CN1146565C/zh not_active Expired - Lifetime
- 2000-05-18 IL IL14640600A patent/IL146406A0/xx not_active IP Right Cessation
- 2000-05-18 HR HR20010904A patent/HRP20010904A2/hr not_active Application Discontinuation
- 2000-05-18 MX MXPA01012325A patent/MXPA01012325A/es unknown
- 2000-05-18 CA CA002372238A patent/CA2372238C/en not_active Expired - Lifetime
- 2000-05-18 DK DK00925528T patent/DK1181290T3/da active
- 2000-05-18 AP APAP/P/2001/002349A patent/AP2001002349A0/en unknown
- 2000-05-18 AT AT00925528T patent/ATE244239T1/de not_active IP Right Cessation
- 2000-05-18 SK SK1733-2001A patent/SK285820B6/sk not_active IP Right Cessation
- 2000-05-18 JP JP2001500629A patent/JP3830816B2/ja not_active Expired - Lifetime
- 2000-05-18 BR BR0011094-9A patent/BR0011094A/pt not_active Application Discontinuation
- 2000-05-18 KR KR10-2001-7015494A patent/KR100476606B1/ko not_active Expired - Fee Related
- 2000-05-18 EE EEP200100656A patent/EE200100656A/xx unknown
- 2000-05-23 PA PA20008496101A patent/PA8496101A1/es unknown
- 2000-05-26 TW TW089110206A patent/TWI285204B/zh not_active IP Right Cessation
- 2000-05-26 CO CO00039195A patent/CO5170463A1/es not_active Application Discontinuation
- 2000-05-29 UY UY26176A patent/UY26176A1/es not_active Application Discontinuation
- 2000-05-30 MY MYPI20002409A patent/MY133508A/en unknown
- 2000-05-30 PE PE2000000520A patent/PE20010209A1/es not_active Application Discontinuation
- 2000-05-30 AR ARP000102663A patent/AR033331A1/es active IP Right Grant
- 2000-05-31 SV SV2000000093A patent/SV2001000093A/es unknown
- 2000-05-31 TN TNTNSN00120A patent/TNSN00120A1/fr unknown
- 2000-05-31 MA MA25997A patent/MA26742A1/fr unknown
- 2000-05-31 DZ DZ000101A patent/DZ3050A1/xx active
- 2000-05-31 GT GT200000087A patent/GT200000087A/es unknown
- 2000-06-01 EC EC2000003508A patent/ECSP003508A/es unknown
2001
- 2001-11-28 ZA ZA200109775A patent/ZA200109775B/en unknown
- 2001-11-30 NO NO20015848A patent/NO20015848L/no not_active Application Discontinuation
- 2001-12-10 BG BG106204A patent/BG65240B1/bg unknown
2007
- 2007-03-27 CY CY2007011C patent/CY2007011I1/el unknown

Also Published As

Publication number	Publication date
PL196046B1 (pl)	2007-11-30
EP1181290B1 (de)	2003-07-02
JP2003501354A (ja)	2003-01-14
ATE244239T1 (de)	2003-07-15
IL146406A0 (en)	2002-07-25
CZ20014269A3 (cs)	2002-04-17
TWI285204B (en)	2007-08-11
DE60003679T2 (de)	2004-05-27
EA200101108A1 (ru)	2002-04-25
BR0011094A (pt)	2002-03-19
CY2007011I2 (el)	2010-07-28
DZ3050A1 (fr)	2004-03-27
PA8496101A1 (es)	2002-07-30
SK17332001A3 (sk)	2002-07-02
HUP0201301A3 (en)	2002-10-28
UY26176A1 (es)	2000-12-29
HK1046284A1 (en)	2003-01-03
NO20015848L (no)	2001-12-18
US6255320B1 (en)	2001-07-03
DE60003679D1 (de)	2003-08-07
CN1146565C (zh)	2004-04-21
AU767334B2 (en)	2003-11-06
SK285820B6 (sk)	2007-09-06
EE200100656A (et)	2003-02-17
ES2199825T3 (es)	2004-03-01
WO2000073304A1 (en)	2000-12-07
SV2001000093A (es)	2001-11-08
PT1181290E (pt)	2003-09-30
AR033331A1 (es)	2003-12-17
CN1353711A (zh)	2002-06-12
NO20015848D0 (no)	2001-11-30
DK1181290T3 (da)	2003-09-29
ECSP003508A (es)	2002-02-25
TR200103473T2 (tr)	2002-04-22
MY133508A (en)	2007-11-30
KR20020010688A (ko)	2002-02-04
CA2372238C (en)	2006-12-19
CY2007011I1 (el)	2010-07-28
HRP20010904A2 (en)	2003-02-28
HUP0201301A2 (en)	2002-08-28
NZ515349A (en)	2004-03-26
YU81101A (sh)	2004-07-15
HN2000000077A (es)	2001-02-02
KR100476606B1 (ko)	2005-03-18
CA2372238A1 (en)	2000-12-07
CZ295819B6 (cs)	2005-11-16
BG106204A (en)	2002-07-31
PL352716A1 (en)	2003-09-08
JP3830816B2 (ja)	2006-10-11
TNSN00120A1 (fr)	2005-11-10
MXPA01012325A (es)	2002-07-22
MA26742A1 (fr)	2004-12-20
AU4424800A (en)	2000-12-18
SI1181290T1 (en)	2003-12-31
GT200000087A (es)	2001-11-22
EP1181290A1 (de)	2002-02-27
UA66925C2 (uk)	2004-06-15
AP2001002349A0 (en)	2001-12-31
PE20010209A1 (es)	2001-03-01
EA003731B1 (ru)	2003-08-28
BG65240B1 (bg)	2007-09-28
ZA200109775B (en)	2002-11-28
CO5170463A1 (es)	2002-06-27

Publication	Publication Date	Title
US6939856B2 (en)	2005-09-06	Method for preparing dexchlor tannate
OA11956A (en)	2006-04-13	Polymorphs of a crystalline azabicyclo (2,2,2) octan-3-amine citrate and their pharmaceutical compositions.
US6262067B1 (en)	2001-07-17	Polymorphs of a crystalline azo-bicyclo 2,2,2 OCT-3-yl amine dihydrochloride and their pharmaceutical compositions
EP0703915B1 (de)	2000-09-27	Xamonelin-Tartrat
EP0009608B1 (de)	1982-04-21	N-Phenyläthylacetamide, Verfahren zu ihrer Herstellung und sie enthaltende therapeutische Zusammensetzungen
US6387925B1 (en)	2002-05-14	Polymorphs of a crystalline azo-bicyclo (2.2.2) oct-3-yl amine citrate and their pharmaceutical compositions
US7001886B2 (en)	2006-02-21	Hot melt method for preparing diphenhydramine tannate
HK1046284B (en)	2005-02-08	Polymorphs of crystalline azabicyclo(2,2,2) octan-3-aminecitrate and their pharmaceutical compositions