OA12414A - NMDA receptor agonist pharmaceutical compositions. - Google Patents

NMDA receptor agonist pharmaceutical compositions. Download PDF

Info

Publication number: OA12414A
Authority: OA; OAPI
Prior art keywords: pharmaceutical composition; composition; free; disease; percent
Prior art date: 2000-12-13

Application number

OA1200300145A

Other languages

English (en)

Inventor

Jinyang Hong

Yesook Kim

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.)

2000-12-13

Filing date

2001-12-05

Publication date

2006-04-18

2001-12-05 Application filed by Pfizer Prod Inc filed Critical Pfizer Prod Inc

2006-04-18 Publication of OA12414A publication Critical patent/OA12414A/en

Links

239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 28
239000003706 n methyl dextro aspartic acid receptor stimulating agent Substances 0.000 title abstract description 3
238000000034 method Methods 0.000 claims abstract description 15
QEMSVZNTSXPFJA-HNAYVOBHSA-N 1-[(1s,2s)-1-hydroxy-1-(4-hydroxyphenyl)propan-2-yl]-4-phenylpiperidin-4-ol Chemical compound C1([C@H](O)[C@H](C)N2CCC(O)(CC2)C=2C=CC=CC=2)=CC=C(O)C=C1 QEMSVZNTSXPFJA-HNAYVOBHSA-N 0.000 claims abstract description 11
238000001356 surgical procedure Methods 0.000 claims abstract description 10
210000003169 central nervous system Anatomy 0.000 claims abstract description 9
208000024827 Alzheimer disease Diseases 0.000 claims abstract description 8
208000006011 Stroke Diseases 0.000 claims abstract description 8
208000023105 Huntington disease Diseases 0.000 claims abstract description 6
208000019695 Migraine disease Diseases 0.000 claims abstract description 6
208000005314 Multi-Infarct Dementia Diseases 0.000 claims abstract description 6
208000002193 Pain Diseases 0.000 claims abstract description 6
208000028017 Psychotic disease Diseases 0.000 claims abstract description 6
208000030886 Traumatic Brain injury Diseases 0.000 claims abstract description 6
206010046543 Urinary incontinence Diseases 0.000 claims abstract description 6
201000004810 Vascular dementia Diseases 0.000 claims abstract description 6
206010015037 epilepsy Diseases 0.000 claims abstract description 6
206010027599 migraine Diseases 0.000 claims abstract description 6
208000015122 neurodegenerative disease Diseases 0.000 claims abstract description 6
230000009529 traumatic brain injury Effects 0.000 claims abstract description 6
208000030507 AIDS Diseases 0.000 claims abstract description 5
206010012289 Dementia Diseases 0.000 claims abstract description 5
208000013016 Hypoglycemia Diseases 0.000 claims abstract description 5
208000018737 Parkinson disease Diseases 0.000 claims abstract description 5
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239000002249 anxiolytic agent Substances 0.000 claims abstract description 5
230000000949 anxiolytic effect Effects 0.000 claims abstract description 5
206010013663 drug dependence Diseases 0.000 claims abstract description 5
230000002218 hypoglycaemic effect Effects 0.000 claims abstract description 5
208000014674 injury Diseases 0.000 claims abstract description 5
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208000011117 substance-related disease Diseases 0.000 claims abstract description 5
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239000000203 mixture Substances 0.000 claims description 54
150000002500 ions Chemical class 0.000 claims description 27
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XEEYBQQBJWHFJM-UHFFFAOYSA-N iron Substances [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims description 13
QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 12
239000001301 oxygen Substances 0.000 claims description 12
229910052760 oxygen Inorganic materials 0.000 claims description 12
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 12
150000003839 salts Chemical class 0.000 claims description 11
JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 claims description 10
BDERNNFJNOPAEC-UHFFFAOYSA-N 1-propanol Substances CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 claims description 9
FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims description 9
229910052742 iron Inorganic materials 0.000 claims description 9
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229940044613 1-propanol Drugs 0.000 claims description 8
RGHHSNMVTDWUBI-UHFFFAOYSA-N 4-hydroxybenzaldehyde Chemical compound OC1=CC=C(C=O)C=C1 RGHHSNMVTDWUBI-UHFFFAOYSA-N 0.000 claims description 8
229940123150 Chelating agent Drugs 0.000 claims description 8
JPVYNHNXODAKFH-UHFFFAOYSA-N Cu2+ Chemical compound [Cu+2] JPVYNHNXODAKFH-UHFFFAOYSA-N 0.000 claims description 8
239000007864 aqueous solution Substances 0.000 claims description 8
239000002738 chelating agent Substances 0.000 claims description 8
229910001431 copper ion Inorganic materials 0.000 claims description 8
KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims description 7
-1 iron ion Chemical class 0.000 claims description 7
239000002253 acid Substances 0.000 claims 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 6
BDAGIHXWWSANSR-UHFFFAOYSA-M Formate Chemical compound [O-]C=O BDAGIHXWWSANSR-UHFFFAOYSA-M 0.000 claims description 5
241000124008 Mammalia Species 0.000 claims description 5
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QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical group CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims description 4
KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical group OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 claims description 4
KDYFGRWQOYBRFD-UHFFFAOYSA-N succinic acid Chemical compound OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 claims description 4
150000001450 anions Chemical class 0.000 claims description 2
239000013522 chelant Substances 0.000 claims description 2
239000001384 succinic acid Substances 0.000 claims description 2
SGPGESCZOCHFCL-UHFFFAOYSA-N Tilisolol hydrochloride Chemical group [Cl-].C1=CC=C2C(=O)N(C)C=C(OCC(O)C[NH2+]C(C)(C)C)C2=C1 SGPGESCZOCHFCL-UHFFFAOYSA-N 0.000 claims 1
150000003893 lactate salts Chemical group 0.000 claims 1
238000004519 manufacturing process Methods 0.000 claims 1
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FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 14
230000000694 effects Effects 0.000 description 7
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XKRFYHLGVUSROY-UHFFFAOYSA-N Argon Chemical compound [Ar] XKRFYHLGVUSROY-UHFFFAOYSA-N 0.000 description 4
IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 4
OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 4
VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 4
HOKKHZGPKSLGJE-GSVOUGTGSA-N N-Methyl-D-aspartic acid Chemical group CN[C@@H](C(O)=O)CC(O)=O HOKKHZGPKSLGJE-GSVOUGTGSA-N 0.000 description 4
239000003795 chemical substances by application Substances 0.000 description 4
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102000004868 N-Methyl-D-Aspartate Receptors Human genes 0.000 description 3
108090001041 N-Methyl-D-Aspartate Receptors Proteins 0.000 description 3
HOKKHZGPKSLGJE-UHFFFAOYSA-N N-methyl-D-aspartic acid Natural products CNC(C(O)=O)CC(O)=O HOKKHZGPKSLGJE-UHFFFAOYSA-N 0.000 description 3
239000007853 buffer solution Substances 0.000 description 3
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239000012086 standard solution Substances 0.000 description 3
238000005160 1H NMR spectroscopy Methods 0.000 description 2
JLVSRWOIZZXQAD-UHFFFAOYSA-N 2,3-disulfanylpropane-1-sulfonic acid Chemical compound OS(=O)(=O)CC(S)CS JLVSRWOIZZXQAD-UHFFFAOYSA-N 0.000 description 2
LXAHHHIGZXPRKQ-UHFFFAOYSA-N 5-fluoro-2-methylpyridine Chemical compound CC1=CC=C(F)C=N1 LXAHHHIGZXPRKQ-UHFFFAOYSA-N 0.000 description 2
DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 2
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DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 description 2
239000013011 aqueous formulation Substances 0.000 description 2
229910052786 argon Inorganic materials 0.000 description 2
WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 2
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239000003153 chemical reaction reagent Substances 0.000 description 2
239000003085 diluting agent Substances 0.000 description 2
238000002474 experimental method Methods 0.000 description 2
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239000003703 n methyl dextro aspartic acid receptor blocking agent Substances 0.000 description 2
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238000004806 packaging method and process Methods 0.000 description 2
239000011780 sodium chloride Substances 0.000 description 2
238000002560 therapeutic procedure Methods 0.000 description 2
150000004684 trihydrates Chemical class 0.000 description 2
MBYLVOKEDDQJDY-UHFFFAOYSA-N tris(2-aminoethyl)amine Chemical compound NCCN(CCN)CCN MBYLVOKEDDQJDY-UHFFFAOYSA-N 0.000 description 2
229940006190 2,3-dimercapto-1-propanesulfonic acid Drugs 0.000 description 1
KQKFQBTWXOGINC-UHFFFAOYSA-N 4-phenylpiperidin-4-ol Chemical compound C=1C=CC=CC=1C1(O)CCNCC1 KQKFQBTWXOGINC-UHFFFAOYSA-N 0.000 description 1
UTBULQCHEUWJNV-UHFFFAOYSA-N 4-phenylpiperidine Chemical compound C1CNCCC1C1=CC=CC=C1 UTBULQCHEUWJNV-UHFFFAOYSA-N 0.000 description 1
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QXNVGIXVLWOKEQ-UHFFFAOYSA-N Disodium Chemical compound [Na][Na] QXNVGIXVLWOKEQ-UHFFFAOYSA-N 0.000 description 1
PIICEJLVQHRZGT-UHFFFAOYSA-N Ethylenediamine Chemical compound NCCN PIICEJLVQHRZGT-UHFFFAOYSA-N 0.000 description 1
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239000004471 Glycine Substances 0.000 description 1
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WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 1
HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 description 1
AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 1
QPCDCPDFJACHGM-UHFFFAOYSA-N N,N-bis{2-[bis(carboxymethyl)amino]ethyl}glycine Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(=O)O)CCN(CC(O)=O)CC(O)=O QPCDCPDFJACHGM-UHFFFAOYSA-N 0.000 description 1
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XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
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HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 description 1
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JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 1
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GXHMMDRXHUIUMN-UHFFFAOYSA-N methanesulfonic acid Chemical compound CS(O)(=O)=O.CS(O)(=O)=O GXHMMDRXHUIUMN-UHFFFAOYSA-N 0.000 description 1
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YWAKXRMUMFPDSH-UHFFFAOYSA-N pentene Chemical compound CCCC=C YWAKXRMUMFPDSH-UHFFFAOYSA-N 0.000 description 1
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Classifications

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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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Medicinal Chemistry (AREA)
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Life Sciences & Earth Sciences (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
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Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Biomedical Technology (AREA)
Neurosurgery (AREA)
Neurology (AREA)
Epidemiology (AREA)
Cardiology (AREA)
Heart & Thoracic Surgery (AREA)
Psychiatry (AREA)
Pain & Pain Management (AREA)
Diabetes (AREA)
Oil, Petroleum & Natural Gas (AREA)
Dermatology (AREA)
Urology & Nephrology (AREA)
Inorganic Chemistry (AREA)
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Emergency Medicine (AREA)
Addiction (AREA)
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Endocrinology (AREA)
Obesity (AREA)
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Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Hydrogenated Pyridines (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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OA1200300145A 2000-12-13 2001-12-05 NMDA receptor agonist pharmaceutical compositions. OA12414A (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US25537200P	2000-12-13	2000-12-13

Publications (1)

Publication Number	Publication Date
OA12414A true OA12414A (en)	2006-04-18

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ID=22968017

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
OA1200300145A OA12414A (en)	2000-12-13	2001-12-05	NMDA receptor agonist pharmaceutical compositions.

Country Status (41)

Country	Link
US (2)	US6635270B2 (de)
EP (1)	EP1347760B1 (de)
JP (1)	JP2004515529A (de)
KR (1)	KR100533407B1 (de)
CN (1)	CN1273135C (de)
AP (1)	AP1235A (de)
AR (1)	AR035607A1 (de)
AT (1)	ATE296629T1 (de)
AU (2)	AU1845402A (de)
BG (1)	BG107788A (de)
BR (1)	BR0116085A (de)
CA (1)	CA2431172A1 (de)
CZ (1)	CZ20031543A3 (de)
DE (1)	DE60111265T2 (de)
DO (1)	DOP2001000300A (de)
DZ (1)	DZ3484A1 (de)
EA (1)	EA006489B1 (de)
EC (1)	ECSP034655A (de)
EE (1)	EE200300284A (de)
ES (1)	ES2239648T3 (de)
GE (1)	GEP20053568B (de)
HR (1)	HRP20030473A2 (de)
HU (1)	HUP0400645A2 (de)
IL (1)	IL155810A0 (de)
IS (1)	IS6811A (de)
MA (1)	MA26970A1 (de)
MX (1)	MXPA03005257A (de)
NO (1)	NO20032678L (de)
NZ (1)	NZ525742A (de)
OA (1)	OA12414A (de)
PA (1)	PA8534901A1 (de)
PE (1)	PE20020710A1 (de)
PL (1)	PL362080A1 (de)
PT (1)	PT1347760E (de)
SK (1)	SK6982003A3 (de)
TN (1)	TNSN01173A1 (de)
UA (1)	UA73619C2 (de)
UY (1)	UY27068A1 (de)
WO (1)	WO2002047685A2 (de)
YU (1)	YU41103A (de)
ZA (1)	ZA200303892B (de)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
CA2811272C (en)	2003-04-08	2016-12-20	Progenics Pharmaceuticals, Inc.	Pharmaceutical formulations containing methylnaltrexone
TW200800959A (en) *	2005-06-10	2008-01-01	Wyeth Corp	Piperazine-piperidine antagonists and agonists of the 5-HT1a receptor
TW200808740A (en) *	2006-06-09	2008-02-16	Wyeth Corp	Succinate salts of 6-methoxy-8-[4-(1-(5-fluoro)-quinolin-8-yl-piperidin-4-yl)-piperazin-1-yl]-quinoline and crystalline forms thereof
TW200808741A (en) *	2006-06-09	2008-02-16	Wyeth Corp	6-methoxy-8-[4-(1-(5-fluoro)-quinolin-8-yl-piperidin-4-yl)-piperazin-1-yl]-quinoline hydrochloric acid salts
TW200811144A (en) *	2006-06-09	2008-03-01	Wyeth Corp	Crystalline forms of 6-methoxy-8-[4-(1-(5-fluoro)-quinolin-8-yl-piperidin-4-yl)-piperazin-1-yl]-quinoline
TWI489984B (zh)	2006-08-04	2015-07-01	Wyeth Corp	用於非經腸道傳輸化合物之配方及其用途
CL2007003410A1 (es) *	2006-11-28	2008-04-11	Wyeth Corp	Compuestos derivados de 5-fluoro-8-{4-[4-(6-metoxiquinolin-8-il)piperazin-1-il]piperidin-1-il}quinolina; procedimiento de preparacion; compuestos intermediarios; procedimiento de preparacion; composicion farmaceutica; y uso en el tratamiento de trast
TW200901974A (en) *	2007-01-16	2009-01-16	Wyeth Corp	Compounds, compositions, and methods of making and using them
CN101317844B (zh) *	2007-06-08	2010-11-17	章劲夫	化合物(+)-5-甲基-10，11-二氢-5H-二苯并〔a，d〕环庚烯-5，10-亚胺在制备避孕药物中的应用
BRPI0918868B8 (pt)	2008-09-18	2021-05-25	Naurex Inc	compostos moduladores do receptor de nmda e composições compreendendo os mesmos
US8951968B2 (en)	2009-10-05	2015-02-10	Northwestern University	Methods of treating depression and other related diseases
KR101692275B1 (ko)	2010-02-11	2017-01-04	노오쓰웨스턴 유니버시티	２차 구조 안정화된 ｎｍｄａ 수용체 조절제 및 그의 용도
WO2011100585A1 (en)	2010-02-11	2011-08-18	Joseph Moskal	Secondary structure stabilized nmda receptor modulators and uses thereof
CN102586243A (zh) *	2012-03-08	2012-07-18	中国人民解放军军事医学科学院放射与辐射医学研究所	一种预防电磁辐射致脑损伤的标志物
US20140206667A1 (en)	2012-11-14	2014-07-24	Michela Gallagher	Methods and compositions for treating schizophrenia
US9758525B2 (en)	2013-01-29	2017-09-12	Aptinyx Inc.	Spiro-lactam NMDA receptor modulators and uses thereof
EP2951186B1 (de)	2013-01-29	2018-07-25	Aptinyx Inc.	Spiro-lactam-nmda-rezeptormodulatoren und verwendungen davon
PE20151416A1 (es)	2013-01-29	2015-10-10	Naurex Inc	Moduladores de receptores nmda de espiro-lactama y sus usos
KR102410989B1 (ko)	2013-01-29	2022-06-17	앱티닉스 인크.	스피로-락탐 nmda 수용체 조절인자 및 그의 용도
JP2016506962A (ja)	2013-01-29	2016-03-07	ノーレックス, インコーポレイテッドNaurex, Inc.	スピロラクタム系ｎｍｄａ受容体モジュレーターおよびその使用
CN105934247A (zh)	2013-12-23	2016-09-07	株式会社三养生物制药	包含帕洛诺司琼的药物组合物
WO2017201285A1 (en)	2016-05-19	2017-11-23	Aptinyx Inc.	Spiro-lactam nmda receptor modulators and uses thereof
PE20190174A1 (es)	2016-05-19	2019-02-01	Aptinyx Inc	Moduladores del receptor espiro-lactama n-metil-d-aspartato y usos de los mismos
AU2017306158B2 (en)	2016-08-01	2021-10-14	Aptinyx Inc.	Spiro-lactam and bis-spiro-lactam NMDA receptor modulators and uses thereof
IL286107B2 (en)	2016-08-01	2024-09-01	Aptinyx Inc	Spiro-lactam nmda receptor modulators and usesthereof
JP7036792B2 (ja)	2016-08-01	2022-03-15	アプティニックスインコーポレイテッド	スピロ－ラクタムｎｍｄａ受容体修飾因子およびその使用
WO2018026798A1 (en)	2016-08-01	2018-02-08	Aptinyx Inc.	Spiro-lactam nmda modulators and methods of using same
KR102465758B1 (ko)	2016-08-01	2022-11-09	앱티닉스 인크.	스피로-락탐 nmda 수용체 조정제 및 그의 용도
PE20210455A1 (es)	2018-01-31	2021-03-08	Aptinyx Inc	Moduladores del receptor nmda espiro-lactama y usos de los mismos
US12012413B2 (en)	2019-11-11	2024-06-18	Tenacia Biotechnology (Hong Kong) Co., Limited	Methods of treating painful diabetic peripheral neuropathy

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US5272160A (en)	1989-05-17	1993-12-21	Pfizer Inc	2-piperidino-1-alkanol derivatives as antiischemic agents
US5710168A (en) *	1991-10-23	1998-01-20	Pfizer Inc.	2-piperidino-1-alkanol derivatives as neuroprotective agents
DK0843661T3 (da) *	1995-08-11	2002-07-22	Pfizer	(1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidin-1-yl)-1-propanolmethansulfonat-trihydrat
TW450807B (en) *	1995-09-15	2001-08-21	Pfizer	Pharmaceutical compositions for treating tinnitus comprising neuroprotective agents

2001
- 2001-05-12 UA UA2003065485A patent/UA73619C2/uk unknown
- 2001-12-05 US US10/010,827 patent/US6635270B2/en not_active Expired - Fee Related
- 2001-12-05 PL PL01362080A patent/PL362080A1/xx not_active Application Discontinuation
- 2001-12-05 EE EEP200300284A patent/EE200300284A/xx unknown
- 2001-12-05 HR HR20030473A patent/HRP20030473A2/hr not_active Application Discontinuation
- 2001-12-05 DE DE60111265T patent/DE60111265T2/de not_active Expired - Fee Related
- 2001-12-05 YU YU41103A patent/YU41103A/sh unknown
- 2001-12-05 CZ CZ20031543A patent/CZ20031543A3/cs unknown
- 2001-12-05 CN CNB018203922A patent/CN1273135C/zh not_active Expired - Fee Related
- 2001-12-05 KR KR10-2003-7007874A patent/KR100533407B1/ko not_active Expired - Fee Related
- 2001-12-05 EA EA200300514A patent/EA006489B1/ru not_active IP Right Cessation
- 2001-12-05 IL IL15581001A patent/IL155810A0/xx unknown
- 2001-12-05 EP EP01270205A patent/EP1347760B1/de not_active Expired - Lifetime
- 2001-12-05 WO PCT/IB2001/002359 patent/WO2002047685A2/en not_active Ceased
- 2001-12-05 BR BR0116085-0A patent/BR0116085A/pt not_active IP Right Cessation
- 2001-12-05 CA CA002431172A patent/CA2431172A1/en not_active Abandoned
- 2001-12-05 AU AU1845402A patent/AU1845402A/xx active Pending
- 2001-12-05 HU HU0400645A patent/HUP0400645A2/hu unknown
- 2001-12-05 AU AU2002218454A patent/AU2002218454B2/en not_active Ceased
- 2001-12-05 ES ES01270205T patent/ES2239648T3/es not_active Expired - Lifetime
- 2001-12-05 DZ DZ013484A patent/DZ3484A1/fr active
- 2001-12-05 JP JP2002549256A patent/JP2004515529A/ja active Pending
- 2001-12-05 NZ NZ525742A patent/NZ525742A/en unknown
- 2001-12-05 OA OA1200300145A patent/OA12414A/en unknown
- 2001-12-05 AT AT01270205T patent/ATE296629T1/de not_active IP Right Cessation
- 2001-12-05 SK SK698-2003A patent/SK6982003A3/sk unknown
- 2001-12-05 PT PT01270205T patent/PT1347760E/pt unknown
- 2001-12-05 GE GE5171A patent/GEP20053568B/en unknown
- 2001-12-05 MX MXPA03005257A patent/MXPA03005257A/es active IP Right Grant
- 2001-12-10 DO DO2001000300A patent/DOP2001000300A/es unknown
- 2001-12-11 PE PE2001001235A patent/PE20020710A1/es not_active Application Discontinuation
- 2001-12-11 AR ARP010105748A patent/AR035607A1/es unknown
- 2001-12-12 TN TNTNSN01173A patent/TNSN01173A1/fr unknown
- 2001-12-12 UY UY27068A patent/UY27068A1/es not_active Application Discontinuation
- 2001-12-13 AP APAP/P/2001/002376A patent/AP1235A/en active
- 2001-12-13 PA PA20018534901A patent/PA8534901A1/es unknown
2003
- 2003-05-08 IS IS6811A patent/IS6811A/is unknown
- 2003-05-09 BG BG107788A patent/BG107788A/bg unknown
- 2003-05-20 ZA ZA200303892A patent/ZA200303892B/en unknown
- 2003-06-03 MA MA27191A patent/MA26970A1/fr unknown
- 2003-06-12 NO NO20032678A patent/NO20032678L/no not_active Application Discontinuation
- 2003-06-13 EC EC2003004655A patent/ECSP034655A/es unknown
- 2003-08-19 US US10/643,441 patent/US20040039022A1/en not_active Abandoned

Also Published As

Publication number	Publication date
KR100533407B1 (ko)	2005-12-02
CZ20031543A3 (cs)	2004-06-16
DZ3484A1 (fr)	2002-06-20
JP2004515529A (ja)	2004-05-27
US20020111366A1 (en)	2002-08-15
DOP2001000300A (es)	2002-05-30
WO2002047685A3 (en)	2002-08-15
HUP0400645A2 (hu)	2004-06-28
AP2001002376A0 (en)	2001-12-31
ZA200303892B (en)	2004-05-20
MA26970A1 (fr)	2004-12-20
PA8534901A1 (es)	2002-08-26
AR035607A1 (es)	2004-06-16
UY27068A1 (es)	2002-07-31
US6635270B2 (en)	2003-10-21
NO20032678D0 (no)	2003-06-12
PL362080A1 (en)	2004-10-18
DE60111265T2 (de)	2006-05-04
HK1059575A1 (en)	2004-07-09
EP1347760A2 (de)	2003-10-01
ECSP034655A (es)	2003-07-25
EA006489B1 (ru)	2005-12-29
TNSN01173A1 (fr)	2005-11-10
AP1235A (en)	2004-01-06
WO2002047685A2 (en)	2002-06-20
IL155810A0 (en)	2003-12-23
UA73619C2 (en)	2005-08-15
IS6811A (is)	2003-05-08
KR20030070060A (ko)	2003-08-27
DE60111265D1 (de)	2005-07-07
ATE296629T1 (de)	2005-06-15
YU41103A (sh)	2006-05-25
NO20032678L (no)	2003-06-12
CN1479617A (zh)	2004-03-03
BR0116085A (pt)	2003-12-23
SK6982003A3 (en)	2004-08-03
CN1273135C (zh)	2006-09-06
PT1347760E (pt)	2005-09-30
EA200300514A1 (ru)	2003-10-30
US20040039022A1 (en)	2004-02-26
AU2002218454B2 (en)	2005-10-27
ES2239648T3 (es)	2005-10-01
CA2431172A1 (en)	2002-06-20
AU1845402A (en)	2002-06-24
GEP20053568B (en)	2005-07-11
NZ525742A (en)	2005-07-29
EP1347760B1 (de)	2005-06-01
BG107788A (bg)	2004-01-30
HRP20030473A2 (en)	2005-04-30
MXPA03005257A (es)	2003-09-25
PE20020710A1 (es)	2002-08-09
EE200300284A (et)	2003-10-15

Publication	Publication Date	Title
OA12414A (en)	2006-04-18	NMDA receptor agonist pharmaceutical compositions.
AU2002218454A1 (en)	2002-08-29	NMDA receptor agonist pharmaceutical compositions
MXPA05010817A (es)	2006-03-30	Formulaciones farmaceuticas que contienen metilnaltrexona.
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EP1662875A2 (de)	2006-06-07	Chelerythrin, seine analoge und ihre verwendung bei der behandlung der manisch-depressiven psychose sowie von anderen kognitiven störungen
WO2007040535A1 (en)	2007-04-12	Use of polyamine analogs for treatment and prevention of intestinal polyps
RU2038080C1 (ru)	1995-06-27	Лекарственное средство для парентерального введения
AU2020345320B2 (en)	2025-09-04	Method for preventing precipitation of injectable solution containing p-boronophenylalanine
CN114423458A (zh)	2022-04-29	含有对二羟硼基苯丙氨酸的注射液剂
IE63292B1 (en)	1995-04-05	Parenteral formulations of 1-diphenylmethyl-4-((2-(4-methylphenyl)-5-methyl-1h-imidazol-4-yl) methyl)piperazine
HK1059575B (en)	2006-12-08	Nmda receptor agonist pharmaceutical compositions
RU2851166C1 (ru)	2025-11-19	Фармацевтическая композиция и ее применение
KR900002745B1 (ko)	1990-04-28	안정 주사용 진토제 조성물의 제조방법
HK40063208A (en)	2022-06-17	Method for preventing precipitation of injectable solution containing p-boronophenylalanine
CN107028968B (zh)	2020-12-04	一种含有葡萄糖醛酸吗啡或其可药用盐的药物组合物
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