UA73348C2 - Sodium-hydrogen exchanger inhibitor of the type 1 (nhe-1) - Google Patents

Sodium-hydrogen exchanger inhibitor of the type 1 (nhe-1) Download PDF

Info

Publication number: UA73348C2
Authority: UA; Ukraine
Prior art keywords: compound; tissue; prodrug form; pharmaceutically acceptable; formula
Prior art date: 2000-04-28

Application number

UA2002108497A

Other languages

English (en)

Ukrainian (uk)

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.)

2000-04-28

Filing date

2001-02-28

Publication date

2005-07-15

2001-02-28 Application filed by Pfizer Prod Inc filed Critical Pfizer Prod Inc

2005-07-15 Publication of UA73348C2 publication Critical patent/UA73348C2/uk

Links

239000003112 inhibitor Substances 0.000 title abstract description 10
102000052126 Sodium-Hydrogen Exchangers Human genes 0.000 title 1
108091006672 Sodium–hydrogen antiporter Proteins 0.000 title 1
238000000034 method Methods 0.000 claims abstract description 78
208000028867 ischemia Diseases 0.000 claims abstract description 22
230000000451 tissue damage Effects 0.000 claims abstract description 16
231100000827 tissue damage Toxicity 0.000 claims abstract description 16
239000008194 pharmaceutical composition Substances 0.000 claims abstract description 10
150000001875 compounds Chemical class 0.000 claims description 205
239000000651 prodrug Substances 0.000 claims description 131
229940002612 prodrug Drugs 0.000 claims description 131
150000003839 salts Chemical class 0.000 claims description 82
210000001519 tissue Anatomy 0.000 claims description 38
210000002216 heart Anatomy 0.000 claims description 32
241000124008 Mammalia Species 0.000 claims description 30
239000002904 solvent Substances 0.000 claims description 26
ZRALSGWEFCBTJO-UHFFFAOYSA-N Guanidine Chemical compound NC(N)=N ZRALSGWEFCBTJO-UHFFFAOYSA-N 0.000 claims description 20
238000001356 surgical procedure Methods 0.000 claims description 18
230000000302 ischemic effect Effects 0.000 claims description 13
210000000056 organ Anatomy 0.000 claims description 11
CHJJGSNFBQVOTG-UHFFFAOYSA-N N-methyl-guanidine Natural products CNC(N)=N CHJJGSNFBQVOTG-UHFFFAOYSA-N 0.000 claims description 10
SWSQBOPZIKWTGO-UHFFFAOYSA-N dimethylaminoamidine Natural products CN(C)C(N)=N SWSQBOPZIKWTGO-UHFFFAOYSA-N 0.000 claims description 10
239000003085 diluting agent Substances 0.000 claims description 8
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-1 5-cyclopropyl-1-(quinolin-5-yl )-1H-pyrazole-4-carbonyl Chemical group 0.000 claims description 5
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102100030980 Sodium/hydrogen exchanger 1 Human genes 0.000 abstract 4
108010093115 growth factor-activatable Na-H exchanger NHE-1 Proteins 0.000 abstract 4
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VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical group Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 16
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HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 6
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IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 4
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LISFMEBWQUVKPJ-UHFFFAOYSA-N quinolin-2-ol Chemical class C1=CC=C2NC(=O)C=CC2=C1 LISFMEBWQUVKPJ-UHFFFAOYSA-N 0.000 description 4
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FWPIDFUJEMBDLS-UHFFFAOYSA-L tin(II) chloride dihydrate Chemical compound O.O.Cl[Sn]Cl FWPIDFUJEMBDLS-UHFFFAOYSA-L 0.000 description 4
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NGNBDVOYPDDBFK-UHFFFAOYSA-N 2-[2,4-di(pentan-2-yl)phenoxy]acetyl chloride Chemical compound CCCC(C)C1=CC=C(OCC(Cl)=O)C(C(C)CCC)=C1 NGNBDVOYPDDBFK-UHFFFAOYSA-N 0.000 description 3
QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 description 3
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QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
229910052722 tritium Inorganic materials 0.000 description 1
238000001665 trituration Methods 0.000 description 1
238000007738 vacuum evaporation Methods 0.000 description 1
210000004509 vascular smooth muscle cell Anatomy 0.000 description 1
230000025033 vasoconstriction Effects 0.000 description 1
235000008979 vitamin B4 Nutrition 0.000 description 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
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
- 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
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Veterinary Medicine (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Animal Behavior & Ethology (AREA)
Life Sciences & Earth Sciences (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
General Chemical & Material Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Chemical Kinetics & Catalysis (AREA)
Heart & Thoracic Surgery (AREA)
Cardiology (AREA)
Epidemiology (AREA)
Urology & Nephrology (AREA)
Vascular Medicine (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Preventing Corrosion Or Incrustation Of Metals (AREA)
Treatment Of Water By Ion Exchange (AREA)
Plural Heterocyclic Compounds (AREA)

UA2002108497A 2000-04-28 2001-02-28 Sodium-hydrogen exchanger inhibitor of the type 1 (nhe-1) UA73348C2 (en)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
US20043200P	2000-04-28	2000-04-28
PCT/IB2001/000277 WO2001083470A1 (en)	2000-04-28	2001-02-28	Sodium-hydrogen exchanger type 1 inhibitor (nhe-1)

Publications (1)

Publication Number	Publication Date
UA73348C2 true UA73348C2 (en)	2005-07-15

Family

ID=22741697

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
UA2002108497A UA73348C2 (en)	2000-04-28	2001-02-28	Sodium-hydrogen exchanger inhibitor of the type 1 (nhe-1)

Country Status (40)

Country	Link
EP (1)	EP1276737A1 (is)
JP (1)	JP2003531900A (is)
KR (1)	KR20020093079A (is)
CN (1)	CN1225466C (is)
AP (1)	AP2002002651A0 (is)
AR (1)	AR028375A1 (is)
AU (1)	AU2001235896A1 (is)
BG (1)	BG107139A (is)
BR (1)	BR0110268A (is)
CA (1)	CA2407535A1 (is)
CO (1)	CO5221125A1 (is)
CR (1)	CR6797A (is)
CZ (1)	CZ20023408A3 (is)
DZ (1)	DZ3310A1 (is)
EA (1)	EA004882B1 (is)
EE (1)	EE200200615A (is)
GT (1)	GT200100064A (is)
HN (1)	HN2001000042A (is)
HR (1)	HRP20020851A2 (is)
HU (1)	HUP0300651A2 (is)
IL (1)	IL152075A0 (is)
IS (2)	IS6567A (is)
MA (1)	MA26897A1 (is)
MX (1)	MXPA02010600A (is)
MY (1)	MY133842A (is)
NO (1)	NO20025132L (is)
NZ (1)	NZ521348A (is)
OA (1)	OA12256A (is)
PA (1)	PA8513301A1 (is)
PE (1)	PE20011270A1 (is)
PL (1)	PL357765A1 (is)
SK (1)	SK14872002A3 (is)
SV (1)	SV2002000418A (is)
TN (1)	TNSN01065A1 (is)
TR (1)	TR200202439T2 (is)
UA (1)	UA73348C2 (is)
UY (1)	UY26680A1 (is)
WO (1)	WO2001083470A1 (is)
YU (1)	YU79602A (is)
ZA (1)	ZA200208605B (is)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
WO2002060892A1 (en) *	2001-01-31	2002-08-08	Pfizer Products Inc.	Ethanolates of sodium-hydrogen exchanger type-1 inhibitor
MXPA04004685A (es) *	2001-12-19	2004-08-12	Pfizer Prod Inc	Procedimientos para preparar inhibidores de tipo-1 de intercambiador sodio-hidrogeno.
CA2483927A1 (en) *	2002-05-02	2003-11-13	Pfizer Products Inc.	Treatment of diabetes and diabetic complications with nhe-1 inhibitors
FR2840302B1 (fr) *	2002-06-03	2004-07-16	Aventis Pharma Sa	Derives d'isoindolones, procede de preparation et intermediaire de ce procede a titre de medicaments et compositions pharmaceutiques les renfermant
ES2220185B1 (es) *	2002-07-16	2006-04-01	Consejo Sup. De Investig. Cientificas	Nuevo peptido inhibidor del intercambiador na+/h+ (pinhe), y sus aplicaciones.
AU2004212957A1 (en) *	2003-02-14	2004-09-02	Smithkline Beecham Corporation	Novel compounds
RU2518741C1 (ru) *	2013-03-22	2014-06-10	Федеральное государственное автономное образовательное учреждение высшего профессионального образования "ЮЖНЫЙ ФЕДЕРАЛЬНЫЙ УНИВЕРСИТЕТ"	СРЕДСТВО, ИНГИБИРУЮЩЕЕ Na+/H+-ОБМЕН, И ГАЛОГЕНИДЫ 1-ДИАЛКИЛАМИНОЭТИЛ-3-[ЗАМЕЩЕННЫЙ(ДИЗАМЕЩЕННЫЙ) ФЕНАЦИЛ]-2-АМИНОБЕНЗИМИДАЗОЛИЯ

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
CA2321642A1 (en) *	1998-02-27	1999-09-02	Ronald T. Wester	N-¬(substituted five-membered di- or triaza diunsaturated ring)carbonyl\|guanidine derivatives for the treatment of ischemia

2001
- 2001-02-28 JP JP2001580898A patent/JP2003531900A/ja active Pending
- 2001-02-28 KR KR1020027014355A patent/KR20020093079A/ko not_active Abandoned
- 2001-02-28 YU YUP-796/02A patent/YU79602A/sh unknown
- 2001-02-28 PL PL01357765A patent/PL357765A1/xx not_active Application Discontinuation
- 2001-02-28 EP EP01908037A patent/EP1276737A1/en not_active Withdrawn
- 2001-02-28 NZ NZ521348A patent/NZ521348A/en unknown
- 2001-02-28 HU HU0300651A patent/HUP0300651A2/hu unknown
- 2001-02-28 OA OA1200200331A patent/OA12256A/en unknown
- 2001-02-28 WO PCT/IB2001/000277 patent/WO2001083470A1/en not_active Ceased
- 2001-02-28 EE EEP200200615A patent/EE200200615A/xx unknown
- 2001-02-28 CN CNB018087256A patent/CN1225466C/zh not_active Expired - Fee Related
- 2001-02-28 IL IL15207501A patent/IL152075A0/xx unknown
- 2001-02-28 MX MXPA02010600A patent/MXPA02010600A/es active IP Right Grant
- 2001-02-28 BR BR0110268-0A patent/BR0110268A/pt not_active IP Right Cessation
- 2001-02-28 EA EA200201023A patent/EA004882B1/ru not_active IP Right Cessation
- 2001-02-28 HR HR20020851A patent/HRP20020851A2/hr not_active Application Discontinuation
- 2001-02-28 CZ CZ20023408A patent/CZ20023408A3/cs unknown
- 2001-02-28 DZ DZ013310A patent/DZ3310A1/fr active
- 2001-02-28 AP APAP/P/2002/002651A patent/AP2002002651A0/en unknown
- 2001-02-28 SK SK1487-2002A patent/SK14872002A3/sk unknown
- 2001-02-28 AU AU2001235896A patent/AU2001235896A1/en not_active Abandoned
- 2001-02-28 UA UA2002108497A patent/UA73348C2/uk unknown
- 2001-02-28 CA CA002407535A patent/CA2407535A1/en not_active Abandoned
- 2001-02-28 TR TR2002/02439T patent/TR200202439T2/xx unknown
- 2001-03-06 HN HN2001000042A patent/HN2001000042A/es unknown
- 2001-03-12 PA PA20018513301A patent/PA8513301A1/es unknown
- 2001-04-20 GT GT200100064A patent/GT200100064A/es unknown
- 2001-04-24 UY UY26680A patent/UY26680A1/es not_active Application Discontinuation
- 2001-04-26 PE PE2001000376A patent/PE20011270A1/es not_active Application Discontinuation
- 2001-04-26 MY MYPI20011977A patent/MY133842A/en unknown
- 2001-04-26 AR ARP010101970A patent/AR028375A1/es unknown
- 2001-04-27 SV SV2001000418A patent/SV2002000418A/es not_active Application Discontinuation
- 2001-04-27 TN TNTNSN01065A patent/TNSN01065A1/fr unknown
- 2001-04-27 CO CO01032977A patent/CO5221125A1/es not_active Application Discontinuation
2002
- 2002-09-23 BG BG107139A patent/BG107139A/bg unknown
- 2002-09-24 IS IS6567A patent/IS6567A/is unknown
- 2002-10-18 MA MA26875A patent/MA26897A1/fr unknown
- 2002-10-18 CR CR6797A patent/CR6797A/es not_active Application Discontinuation
- 2002-10-21 IS IS6588A patent/IS6588A/is unknown
- 2002-10-24 ZA ZA200208605A patent/ZA200208605B/en unknown
- 2002-10-25 NO NO20025132A patent/NO20025132L/no not_active Application Discontinuation

Also Published As

Publication number	Publication date
DZ3310A1 (fr)	2001-11-07
EA200201023A1 (ru)	2003-02-27
ZA200208605B (en)	2003-10-24
HN2001000042A (es)	2001-07-09
YU79602A (en)	2006-05-25
WO2001083470A1 (en)	2001-11-08
PA8513301A1 (es)	2003-09-05
SK14872002A3 (sk)	2004-03-02
EE200200615A (et)	2004-04-15
AU2001235896A1 (en)	2001-11-12
NO20025132D0 (no)	2002-10-25
BR0110268A (pt)	2003-12-30
PE20011270A1 (es)	2001-12-12
TNSN01065A1 (fr)	2005-11-10
CA2407535A1 (en)	2001-11-08
IL152075A0 (en)	2003-05-29
MY133842A (en)	2007-11-30
EP1276737A1 (en)	2003-01-22
MA26897A1 (fr)	2004-12-20
KR20020093079A (ko)	2002-12-12
CN1225466C (zh)	2005-11-02
IS6567A (is)	2002-09-24
HRP20020851A2 (en)	2005-02-28
HUP0300651A2 (hu)	2003-07-28
NZ521348A (en)	2004-09-24
TR200202439T2 (tr)	2003-02-21
NO20025132L (no)	2002-12-12
IS6588A (is)	2002-10-21
CO5221125A1 (es)	2002-11-28
SV2002000418A (es)	2002-07-03
PL357765A1 (en)	2004-07-26
EA004882B1 (ru)	2004-08-26
AP2002002651A0 (en)	2002-12-31
JP2003531900A (ja)	2003-10-28
CN1426404A (zh)	2003-06-25
MXPA02010600A (es)	2003-03-10
CR6797A (es)	2004-05-17
GT200100064A (es)	2002-03-22
CZ20023408A3 (cs)	2004-01-14
UY26680A1 (es)	2001-12-28
AR028375A1 (es)	2003-05-07
OA12256A (en)	2003-11-06
BG107139A (bg)	2003-07-31

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