ZA200308146B - Biguanide derivatives. - Google Patents

Biguanide derivatives. Download PDF

Info

Publication number: ZA200308146B
Authority: ZA; South Africa
Prior art keywords: composition; together form; nitrogen atom; represent; diabetes
Prior art date: 2001-03-21

Application number

ZA200308146A

Other languages

English (en)

Inventor

Gerard Moinet

Cravo Daniel

Original Assignee

Merck Patent Gmbh

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.)

2001-03-21

Filing date

2003-10-20

Publication date

2005-01-20

2003-10-20 Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh

2005-01-20 Publication of ZA200308146B publication Critical patent/ZA200308146B/en

Links

150000004283 biguanides Chemical class 0.000 title description 6
150000001875 compounds Chemical class 0.000 claims description 48
206010012601 diabetes mellitus Diseases 0.000 claims description 31
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208000016097 disease of metabolism Diseases 0.000 description 1
BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical compound [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 description 1
208000035475 disorder Diseases 0.000 description 1
MOTZDAYCYVMXPC-UHFFFAOYSA-N dodecyl hydrogen sulfate Chemical compound CCCCCCCCCCCCOS(O)(=O)=O MOTZDAYCYVMXPC-UHFFFAOYSA-N 0.000 description 1
239000008298 dragée Substances 0.000 description 1
230000007613 environmental effect Effects 0.000 description 1
AFAXGSQYZLGZPG-UHFFFAOYSA-N ethanedisulfonic acid Chemical compound OS(=O)(=O)CCS(O)(=O)=O AFAXGSQYZLGZPG-UHFFFAOYSA-N 0.000 description 1
CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical compound CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 description 1
238000001704 evaporation Methods 0.000 description 1
230000008020 evaporation Effects 0.000 description 1
239000003889 eye drop Substances 0.000 description 1
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230000037406 food intake Effects 0.000 description 1
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239000001530 fumaric acid Substances 0.000 description 1
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239000007903 gelatin capsule Substances 0.000 description 1
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MASNOZXLGMXCHN-ZLPAWPGGSA-N glucagon Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 MASNOZXLGMXCHN-ZLPAWPGGSA-N 0.000 description 1
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GVALZJMUIHGIMD-UHFFFAOYSA-H magnesium phosphate Chemical compound [Mg+2].[Mg+2].[Mg+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O GVALZJMUIHGIMD-UHFFFAOYSA-H 0.000 description 1
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229910000157 magnesium phosphate Inorganic materials 0.000 description 1
235000010994 magnesium phosphates Nutrition 0.000 description 1
235000019359 magnesium stearate Nutrition 0.000 description 1
VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
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239000011707 mineral Substances 0.000 description 1
150000007522 mineralic acids Chemical class 0.000 description 1
235000019426 modified starch Nutrition 0.000 description 1
LNOPIUAQISRISI-UHFFFAOYSA-N n'-hydroxy-2-propan-2-ylsulfonylethanimidamide Chemical compound CC(C)S(=O)(=O)CC(N)=NO LNOPIUAQISRISI-UHFFFAOYSA-N 0.000 description 1
OELFLUMRDSZNSF-BRWVUGGUSA-N nateglinide Chemical compound C1C[C@@H](C(C)C)CC[C@@H]1C(=O)N[C@@H](C(O)=O)CC1=CC=CC=C1 OELFLUMRDSZNSF-BRWVUGGUSA-N 0.000 description 1
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235000001968 nicotinic acid Nutrition 0.000 description 1
229960003512 nicotinic acid Drugs 0.000 description 1
229910017604 nitric acid Inorganic materials 0.000 description 1
235000020824 obesity Nutrition 0.000 description 1
239000002674 ointment Substances 0.000 description 1
239000003538 oral antidiabetic agent Substances 0.000 description 1
150000007524 organic acids Chemical class 0.000 description 1
235000005985 organic acids Nutrition 0.000 description 1
230000008520 organization Effects 0.000 description 1
230000003204 osmotic effect Effects 0.000 description 1
210000000496 pancreas Anatomy 0.000 description 1
229960001412 pentobarbital Drugs 0.000 description 1
229960002275 pentobarbital sodium Drugs 0.000 description 1
230000010412 perfusion Effects 0.000 description 1
208000033808 peripheral neuropathy Diseases 0.000 description 1
229940021222 peritoneal dialysis isotonic solution Drugs 0.000 description 1
235000019271 petrolatum Nutrition 0.000 description 1
239000000825 pharmaceutical preparation Substances 0.000 description 1
229960003243 phenformin Drugs 0.000 description 1
ICFJFFQQTFMIBG-UHFFFAOYSA-N phenformin Chemical compound NC(=N)NC(=N)NCCC1=CC=CC=C1 ICFJFFQQTFMIBG-UHFFFAOYSA-N 0.000 description 1
150000003016 phosphoric acids Chemical class 0.000 description 1
239000002504 physiological saline solution Substances 0.000 description 1
OXNIZHLAWKMVMX-UHFFFAOYSA-N picric acid Chemical class OC1=C([N+]([O-])=O)C=C([N+]([O-])=O)C=C1[N+]([O-])=O OXNIZHLAWKMVMX-UHFFFAOYSA-N 0.000 description 1
239000006187 pill Substances 0.000 description 1
229960005095 pioglitazone Drugs 0.000 description 1
IUGYQRQAERSCNH-UHFFFAOYSA-N pivalic acid Chemical compound CC(C)(C)C(O)=O IUGYQRQAERSCNH-UHFFFAOYSA-N 0.000 description 1
239000002798 polar solvent Substances 0.000 description 1
229920001223 polyethylene glycol Polymers 0.000 description 1
230000000291 postprandial effect Effects 0.000 description 1
239000000843 powder Substances 0.000 description 1
238000002360 preparation method Methods 0.000 description 1
235000019260 propionic acid Nutrition 0.000 description 1
238000000746 purification Methods 0.000 description 1
IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 description 1
102000005962 receptors Human genes 0.000 description 1
108020003175 receptors Proteins 0.000 description 1
230000004044 response Effects 0.000 description 1
229960004586 rosiglitazone Drugs 0.000 description 1
230000000276 sedentary effect Effects 0.000 description 1
230000035945 sensitivity Effects 0.000 description 1
231100000489 sensitizer Toxicity 0.000 description 1
239000011734 sodium Substances 0.000 description 1
239000002904 solvent Substances 0.000 description 1
239000008347 soybean phospholipid Substances 0.000 description 1
235000019698 starch Nutrition 0.000 description 1
238000003756 stirring Methods 0.000 description 1
239000005720 sucrose Substances 0.000 description 1
235000000346 sugar Nutrition 0.000 description 1
239000007940 sugar coated tablet Substances 0.000 description 1
125000000542 sulfonic acid group Chemical group 0.000 description 1
208000011580 syndromic disease Diseases 0.000 description 1
235000012222 talc Nutrition 0.000 description 1
239000011975 tartaric acid Substances 0.000 description 1
235000002906 tartaric acid Nutrition 0.000 description 1
235000010487 tragacanth Nutrition 0.000 description 1
239000000196 tragacanth Substances 0.000 description 1
229940116362 tragacanth Drugs 0.000 description 1
XOOUIPVCVHRTMJ-UHFFFAOYSA-L zinc stearate Chemical class [Zn+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O XOOUIPVCVHRTMJ-UHFFFAOYSA-L 0.000 description 1

Classifications

- 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
- C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
- C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
- C07D295/215—Radicals derived from nitrogen analogues of carbonic acid
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
Diabetes (AREA)
Medicinal Chemistry (AREA)
Life Sciences & Earth Sciences (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Hematology (AREA)
Obesity (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Emergency Medicine (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Pharmacology & Pharmacy (AREA)
Endocrinology (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Lubricants (AREA)
Pyrrole Compounds (AREA)
Indole Compounds (AREA)

ZA200308146A 2001-03-21 2003-10-20 Biguanide derivatives. ZA200308146B (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
FR0103846A FR2822464B1 (fr)	2001-03-21	2001-03-21	Derives biguanides et leurs applications en therapeutique

Publications (1)

Publication Number	Publication Date
ZA200308146B true ZA200308146B (en)	2005-01-20

Family

ID=8861407

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
ZA200308146A ZA200308146B (en)	2001-03-21	2003-10-20	Biguanide derivatives.

Country Status (21)

Country	Link
US (1)	US7285681B2 (fr)
EP (1)	EP1370525B1 (fr)
JP (1)	JP4418157B2 (fr)
KR (1)	KR20030085558A (fr)
CN (1)	CN1228325C (fr)
AT (1)	ATE449066T1 (fr)
AU (1)	AU2002308178B2 (fr)
BR (1)	BR0208131A (fr)
CA (1)	CA2441309C (fr)
CZ (1)	CZ20032766A3 (fr)
DE (1)	DE60234424D1 (fr)
ES (1)	ES2336771T3 (fr)
FR (1)	FR2822464B1 (fr)
HU (1)	HUP0303593A3 (fr)
MX (1)	MXPA03008404A (fr)
NO (1)	NO20034171L (fr)
PL (1)	PL362528A1 (fr)
RU (1)	RU2276136C2 (fr)
SK (1)	SK12802003A3 (fr)
WO (1)	WO2002074740A1 (fr)
ZA (1)	ZA200308146B (fr)

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CN101417988B (zh) *	2007-10-24	2011-04-27	山东轩竹医药科技有限公司	双胍哌嗪类二肽酰肽酶ⅳ抑制剂
KR101041428B1 (ko) *	2008-10-13	2011-06-14	한국화학연구원	Ｎ1-2-티오펜-2-일에틸-ｎ2-치환된 바이구아나이드 유도체,이의 제조방법 및 이를 유효성분으로 함유하는 약학 조성물
WO2010103040A1 (fr)	2009-03-10	2010-09-16	INSERM (Institut National de la Santé et de la Recherche Médicale)	Activateurs de protéine kinases activées par le 5'-adénosine monophosphate (ampk), destinés au traitement de l'hypertension pulmonaire
KR101136045B1 (ko) *	2009-11-16	2012-04-18	한국화학연구원	Ｎ1-(펜에틸)-ｎ2-치환된 바이구아나이드 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 약학 조성물
NL1037643C2 (en) *	2010-01-22	2011-07-25	Karel Paul Bouter	Nutritional product comprising a biguanide.
KR101324283B1 (ko) *	2010-04-27	2013-11-01	한올바이오파마주식회사	바이구아나이드 화합물의 신규 염, 그의 제조방법, 그를 포함하는 약제학적 조성물
WO2013188452A1 (fr) *	2012-06-11	2013-12-19	The Regents Of The University Of California	Composés et procédés de traitement du cancer
KR102216701B1 (ko)	2014-11-20	2021-02-18	이뮤노메트테라퓨틱스 인코포레이티드	바이구아나이드 화합물 및 이의 용도
CN107635963B (zh)	2015-04-30	2020-11-20	伊谬诺米特医疗有限公司	胍化合物及其用途
CN105125689B (zh) *	2015-09-21	2018-01-19	株洲千金药业股份有限公司	一种含有妇科千金片药渣的足浴粉及其制备方法
WO2018058109A1 (fr) *	2016-09-26	2018-03-29	Nusirt Sciences, Inc.	Compositions et méthodes pour le traitement de troubles métaboliques
CN113354561B (zh) *	2021-04-17	2023-03-28	中山大学	双胍衍生物及其应用与制剂

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GB852584A (en) *	1956-05-31	1960-10-26	Us Vitamin Corp	Biguanide compositions
US2937173A (en) *	1959-05-06	1960-05-17	Us Vitamin Pharm Corp	Indolino and tetrahydroquinolino triazines
US3879541A (en)	1970-03-03	1975-04-22	Bayer Ag	Antihyperglycemic methods and compositions
DE2009743A1 (de) *	1970-03-03	1971-09-16	Farbenfabriken Bayer Ag, 5090 Leverkusen	Substituierte Biguanide mit antihyperglykämischer Wirkung
US3960949A (en)	1971-04-02	1976-06-01	Schering Aktiengesellschaft	1,2-Biguanides
EP0034002A3 (fr)	1980-01-22	1981-09-23	Beecham Group Plc	Dérivés de carboxamidine
JPS6141367A (ja) *	1984-08-02	1986-02-27	三菱瓦斯化学株式会社	繊維または繊維製品の過酸化水素による漂白法
FR2696740B1 (fr) *	1992-10-13	1994-12-30	Dospharma Sa	Dérivés prodrogués de la diméthylbiguanide et applications comme médicaments.

2001
- 2001-03-21 FR FR0103846A patent/FR2822464B1/fr not_active Expired - Fee Related
2002
- 2002-03-20 BR BR0208131-8A patent/BR0208131A/pt not_active IP Right Cessation
- 2002-03-20 KR KR10-2003-7012150A patent/KR20030085558A/ko not_active Ceased
- 2002-03-20 RU RU2003130070/04A patent/RU2276136C2/ru not_active IP Right Cessation
- 2002-03-20 JP JP2002573749A patent/JP4418157B2/ja not_active Expired - Fee Related
- 2002-03-20 SK SK1280-2003A patent/SK12802003A3/sk unknown
- 2002-03-20 WO PCT/EP2002/003119 patent/WO2002074740A1/fr not_active Ceased
- 2002-03-20 CA CA2441309A patent/CA2441309C/fr not_active Expired - Fee Related
- 2002-03-20 DE DE60234424T patent/DE60234424D1/de not_active Expired - Lifetime
- 2002-03-20 AU AU2002308178A patent/AU2002308178B2/en not_active Ceased
- 2002-03-20 HU HU0303593A patent/HUP0303593A3/hu unknown
- 2002-03-20 US US10/472,229 patent/US7285681B2/en not_active Expired - Fee Related
- 2002-03-20 CN CNB02806254XA patent/CN1228325C/zh not_active Expired - Fee Related
- 2002-03-20 ES ES02753575T patent/ES2336771T3/es not_active Expired - Lifetime
- 2002-03-20 PL PL02362528A patent/PL362528A1/xx unknown
- 2002-03-20 EP EP02753575A patent/EP1370525B1/fr not_active Expired - Lifetime
- 2002-03-20 CZ CZ20032766A patent/CZ20032766A3/cs unknown
- 2002-03-20 AT AT02753575T patent/ATE449066T1/de not_active IP Right Cessation
- 2002-03-20 MX MXPA03008404A patent/MXPA03008404A/es not_active Application Discontinuation
2003
- 2003-09-19 NO NO20034171A patent/NO20034171L/no not_active Application Discontinuation
- 2003-10-20 ZA ZA200308146A patent/ZA200308146B/en unknown

Also Published As

Publication number	Publication date
ATE449066T1 (de)	2009-12-15
RU2003130070A (ru)	2005-04-10
WO2002074740A1 (fr)	2002-09-26
NO20034171D0 (no)	2003-09-19
KR20030085558A (ko)	2003-11-05
CN1228325C (zh)	2005-11-23
ES2336771T3 (es)	2010-04-16
FR2822464B1 (fr)	2004-08-06
CA2441309C (fr)	2010-06-15
HUP0303593A2 (hu)	2004-03-01
SK12802003A3 (sk)	2004-02-03
CZ20032766A3 (cs)	2004-01-14
FR2822464A1 (fr)	2002-09-27
HUP0303593A3 (en)	2007-03-28
US20040092495A1 (en)	2004-05-13
BR0208131A (pt)	2004-03-02
US7285681B2 (en)	2007-10-23
EP1370525B1 (fr)	2009-11-18
RU2276136C2 (ru)	2006-05-10
NO20034171L (no)	2003-09-19
AU2002308178B2 (en)	2007-03-01
JP2004523580A (ja)	2004-08-05
CA2441309A1 (fr)	2002-09-26
PL362528A1 (en)	2004-11-02
DE60234424D1 (en)	2009-12-31
CN1496347A (zh)	2004-05-12
HK1062172A1 (en)	2004-10-21
MXPA03008404A (es)	2004-01-29
JP4418157B2 (ja)	2010-02-17
EP1370525A1 (fr)	2003-12-17

Publication	Publication Date	Title
CA2441309C (fr)	2010-06-15	Derives de biguanide
AU2002308178A1 (en)	2003-03-27	Biguanide derivatives
HK1052708A1 (en)	2003-09-26	Glutamine-thiazolidide and - pyrrolidide and their use as dipeptidylpeptidase iv inhibitors
EP1189889B1 (fr)	2003-12-17	Compositions et methodes permettant d'inhiber la mort cellulaire
SK6822003A3 (en)	2003-11-04	Substituted 2-anilino-benzimidazoles and the use thereof as NHE-inhibitors
KR100717488B1 (ko)	2007-05-14	이미다조피리딘 유도체, 이의 제조 방법 및 이를 함유하는약제 조성물
US5032593A (en)	1991-07-16	Method of treating bronchoconstriction with 1,3-unsymmetrical straight chain alkyl-substituted 8-phenylxanthines
CA2504213A1 (fr)	2004-05-13	Nouveaux agonistes beta, leurs procedes de preparation et leur utilisation comme compositions pharmaceutiques
EP0362645A2 (fr)	1990-04-11	Utilisation de ptéridines pour la prévention de la résistance primaire et secondaire pendant la chimiothérapie et les mécaments contenant ces substances
DE10161767A1 (de)	2003-06-26	2-Guanidino-4-heterocyclyl-chinazoline
EP1513834B1 (fr)	2006-03-15	Thiophenes substitues, procedes de fabrication, utilisation en tant que medicament ou agent diagnostique et medicament contenant ces thiophenes
HU176481B (en)	1981-03-28	Process for preparing 9-/3-/4-phenoxy-methyl-piperidino/-propyl/-anenine derivatives
EA004687B1 (ru)	2004-06-24	Новые производные бензоилгуанидина с эффективными свойствами, способ их получения и их применение при изготовлении лекарственных средств
US4174402A (en)	1979-11-13	Method for the prophylaxis of SRS-A-induced symptoms
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