SA98190653A - مثبطات بروتييز مساعدة - Google Patents

مثبطات بروتييز مساعدة Download PDF

Info

Publication number: SA98190653A
Authority: SA; Saudi Arabia
Prior art keywords: guanidine; hand; compound; phenyl; thiazole
Prior art date: 1997-09-04

Application number

SA98190653A

Other languages

Arabic (ar)

English (en)

Inventor

سيجفريد بينجامين كريستنسين ، أي في

ريني لويس ديسجارلايس

كورنيليا جوتا فورستير

Original Assignee

سميثكلآين بيتشام كوربوريشن

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.)

1997-09-04

Filing date

1998-10-17

Publication date

2005-12-03

1998-10-17 Application filed by سميثكلآين بيتشام كوربوريشن filed Critical سميثكلآين بيتشام كوربوريشن

2005-12-03 Publication of SA98190653A publication Critical patent/SA98190653A/ar

Links

239000004365 Protease Substances 0.000 title claims description 14
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210000001519 tissue Anatomy 0.000 claims abstract 2
ZRALSGWEFCBTJO-UHFFFAOYSA-N Guanidine Chemical compound NC(N)=N ZRALSGWEFCBTJO-UHFFFAOYSA-N 0.000 claims description 150
CHJJGSNFBQVOTG-UHFFFAOYSA-N N-methyl-guanidine Natural products CNC(N)=N CHJJGSNFBQVOTG-UHFFFAOYSA-N 0.000 claims description 73
SWSQBOPZIKWTGO-UHFFFAOYSA-N dimethylaminoamidine Natural products CN(C)C(N)=N SWSQBOPZIKWTGO-UHFFFAOYSA-N 0.000 claims description 73
-1 amino butoxy Chemical group 0.000 claims description 58
FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims description 46
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 45
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239000007927 intramuscular injection Substances 0.000 description 1
238000010253 intravenous injection Methods 0.000 description 1
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INQOMBQAUSQDDS-UHFFFAOYSA-N iodomethane Chemical compound IC INQOMBQAUSQDDS-UHFFFAOYSA-N 0.000 description 1
150000002500 ions Chemical class 0.000 description 1
125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 1
YDNLNVZZTACNJX-UHFFFAOYSA-N isocyanatomethylbenzene Chemical compound O=C=NCC1=CC=CC=C1 YDNLNVZZTACNJX-UHFFFAOYSA-N 0.000 description 1
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230000003137 locomotive effect Effects 0.000 description 1
239000011777 magnesium Substances 0.000 description 1
229910052749 magnesium Inorganic materials 0.000 description 1
235000019359 magnesium stearate Nutrition 0.000 description 1
239000000594 mannitol Substances 0.000 description 1
235000010355 mannitol Nutrition 0.000 description 1
238000004519 manufacturing process Methods 0.000 description 1
238000001819 mass spectrum Methods 0.000 description 1
239000012913 medium supplement Substances 0.000 description 1
238000002844 melting Methods 0.000 description 1
230000008018 melting Effects 0.000 description 1
239000012528 membrane Substances 0.000 description 1
229910052751 metal Inorganic materials 0.000 description 1
239000002184 metal Substances 0.000 description 1
229910052987 metal hydride Inorganic materials 0.000 description 1
150000004681 metal hydrides Chemical class 0.000 description 1
MYWUZJCMWCOHBA-VIFPVBQESA-N methamphetamine Chemical compound CN[C@@H](C)CC1=CC=CC=C1 MYWUZJCMWCOHBA-VIFPVBQESA-N 0.000 description 1
229930182817 methionine Natural products 0.000 description 1
125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 description 1
244000005700 microbiome Species 0.000 description 1
235000010755 mineral Nutrition 0.000 description 1
239000011707 mineral Substances 0.000 description 1
239000007758 minimum essential medium Substances 0.000 description 1
230000004048 modification Effects 0.000 description 1
238000012986 modification Methods 0.000 description 1
239000003607 modifier Substances 0.000 description 1
XONPDZSGENTBNJ-UHFFFAOYSA-N molecular hydrogen;sodium Chemical compound [Na].[H][H] XONPDZSGENTBNJ-UHFFFAOYSA-N 0.000 description 1
125000002757 morpholinyl group Chemical group 0.000 description 1
DADSZOFTIIETSV-UHFFFAOYSA-N n,n-dichloroaniline Chemical compound ClN(Cl)C1=CC=CC=C1 DADSZOFTIIETSV-UHFFFAOYSA-N 0.000 description 1
PSHKMPUSSFXUIA-UHFFFAOYSA-N n,n-dimethylpyridin-2-amine Chemical compound CN(C)C1=CC=CC=N1 PSHKMPUSSFXUIA-UHFFFAOYSA-N 0.000 description 1
SNMVRZFUUCLYTO-UHFFFAOYSA-N n-propyl chloride Chemical compound CCCCl SNMVRZFUUCLYTO-UHFFFAOYSA-N 0.000 description 1
230000017074 necrotic cell death Effects 0.000 description 1
229910052754 neon Inorganic materials 0.000 description 1
GKAOGPIIYCISHV-UHFFFAOYSA-N neon atom Chemical compound [Ne] GKAOGPIIYCISHV-UHFFFAOYSA-N 0.000 description 1
125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
230000003472 neutralizing effect Effects 0.000 description 1
150000002825 nitriles Chemical class 0.000 description 1
125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 1
230000036963 noncompetitive effect Effects 0.000 description 1
230000000269 nucleophilic effect Effects 0.000 description 1
QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
239000012053 oil suspension Substances 0.000 description 1
239000004006 olive oil Substances 0.000 description 1
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239000001814 pectin Substances 0.000 description 1
235000010987 pectin Nutrition 0.000 description 1
229920001277 pectin Polymers 0.000 description 1
125000001147 pentyl group Chemical group C(CCCC)* 0.000 description 1
239000000825 pharmaceutical preparation Substances 0.000 description 1
239000008196 pharmacological composition Substances 0.000 description 1
239000012071 phase Substances 0.000 description 1
COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 description 1
229910052698 phosphorus Inorganic materials 0.000 description 1
239000004033 plastic Substances 0.000 description 1
229920003023 plastic Polymers 0.000 description 1
230000010287 polarization Effects 0.000 description 1
229920000767 polyaniline Polymers 0.000 description 1
229920001223 polyethylene glycol Polymers 0.000 description 1
239000001267 polyvinylpyrrolidone Substances 0.000 description 1
235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
239000011591 potassium Substances 0.000 description 1
CHWRSCGUEQEHOH-UHFFFAOYSA-N potassium oxide Chemical compound [O-2].[K+].[K+] CHWRSCGUEQEHOH-UHFFFAOYSA-N 0.000 description 1
229910001950 potassium oxide Inorganic materials 0.000 description 1
239000003755 preservative agent Substances 0.000 description 1
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238000003825 pressing Methods 0.000 description 1
102000004196 processed proteins & peptides Human genes 0.000 description 1
125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
229940024999 proteolytic enzymes for treatment of wounds and ulcers Drugs 0.000 description 1
125000003373 pyrazinyl group Chemical group 0.000 description 1
UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 1
125000004076 pyridyl group Chemical group 0.000 description 1
230000005855 radiation Effects 0.000 description 1
235000008001 rakum palm Nutrition 0.000 description 1
230000009467 reduction Effects 0.000 description 1
238000005067 remediation Methods 0.000 description 1
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230000002441 reversible effect Effects 0.000 description 1
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238000007086 side reaction Methods 0.000 description 1
239000011780 sodium chloride Substances 0.000 description 1
239000001509 sodium citrate Substances 0.000 description 1
NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
238000007614 solvation Methods 0.000 description 1
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239000008107 starch Substances 0.000 description 1
235000019698 starch Nutrition 0.000 description 1
239000008117 stearic acid Substances 0.000 description 1
238000003860 storage Methods 0.000 description 1
125000001424 substituent group Chemical group 0.000 description 1
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150000003467 sulfuric acid derivatives Chemical class 0.000 description 1
239000003765 sweetening agent Substances 0.000 description 1
238000010189 synthetic method Methods 0.000 description 1
CWXPZXBSDSIRCS-UHFFFAOYSA-N tert-butyl piperazine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCNCC1 CWXPZXBSDSIRCS-UHFFFAOYSA-N 0.000 description 1
229940124597 therapeutic agent Drugs 0.000 description 1
238000002560 therapeutic procedure Methods 0.000 description 1
125000001984 thiazolidinyl group Chemical group 0.000 description 1
238000004809 thin layer chromatography Methods 0.000 description 1
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230000008733 trauma Effects 0.000 description 1
239000013638 trimer Substances 0.000 description 1
PRXNKYBFWAWBNZ-UHFFFAOYSA-N trimethylphenylammonium tribromide Chemical compound Br[Br-]Br.C[N+](C)(C)C1=CC=CC=C1 PRXNKYBFWAWBNZ-UHFFFAOYSA-N 0.000 description 1
OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 description 1
239000004474 valine Substances 0.000 description 1
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125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
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Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
- C07D277/38—Nitrogen atoms
- C07D277/44—Acylated amino or imino radicals
- C07D277/48—Acylated amino or imino radicals by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof, e.g. carbonylguanidines
- 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
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- 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

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
General Health & Medical Sciences (AREA)
Veterinary Medicine (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Physical Education & Sports Medicine (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
Chemical Kinetics & Catalysis (AREA)
Public Health (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Rheumatology (AREA)
Orthopedic Medicine & Surgery (AREA)
Pain & Pain Management (AREA)
Immunology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Thiazole And Isothizaole Compounds (AREA)
Plural Heterocyclic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

SA98190653A 1997-09-04 1998-10-17 مثبطات بروتييز مساعدة SA98190653A (ar)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US5752797P	1997-09-04	1997-09-04

Publications (1)

Publication Number	Publication Date
SA98190653A true SA98190653A (ar)	2005-12-03

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ID=22011125

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
SA98190653A SA98190653A (ar)	1997-09-04	1998-10-17	مثبطات بروتييز مساعدة

Country Status (10)

Country	Link
EP (1)	EP1015438A4 (fr)
JP (1)	JP2001514257A (fr)
AU (1)	AU9300298A (fr)
CA (1)	CA2302361A1 (fr)
CO (1)	CO4970736A1 (fr)
MA (1)	MA26540A1 (fr)
PE (1)	PE115699A1 (fr)
SA (1)	SA98190653A (fr)
WO (1)	WO1999011637A1 (fr)
ZA (1)	ZA988064B (fr)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US20030144175A1 (en)	1998-12-23	2003-07-31	Smithkline Beecham Corporation	Protease inhibitors
WO2001034599A1 (fr)	1999-11-10	2001-05-17	Smithkline Beecham Corporation	Inhibiteurs de protease
US6583137B1 (en)	1999-11-10	2003-06-24	Smithkline Beecham Corporation	Protease inhibitors
AU1474801A (en)	1999-11-10	2001-06-06	Smithkline Beecham Corporation	Protease inhibitors
HUP0300068A2 (en)	2000-03-21	2003-05-28	Smithkline Beecham Corp	Protease inhibitors, their preparation, their use and pharmaceutical compositions containing them
US6699866B2 (en)	2001-04-17	2004-03-02	Sepracor Inc.	Thiazole and other heterocyclic ligands for mammalian dopamine, muscarinic and serotonin receptors and transporters, and methods of use thereof
JP2005515254A (ja)	2002-01-17	2005-05-26	スミスクラインビーチャムコーポレーション	カテプシンｋ阻害剤として有用なシクロアルキルケトアミド誘導体
KR100962972B1 (ko)	2002-07-26	2010-06-09	주식회사유한양행	1-페닐피페리딘-3-온 유도체 및 그의 제조방법
DE102004008141A1 (de)	2004-02-19	2005-09-01	Abbott Gmbh & Co. Kg	Guanidinverbindungen und ihre Verwendung als Bindungspartner für 5-HT5-Rezeptoren

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
JPS59225172A (ja) *	1983-06-03	1984-12-18	Yamanouchi Pharmaceut Co Ltd	新規グアニジノチアゾ−ル誘導体及びその製法

1998
- 1998-09-01 MA MA25238A patent/MA26540A1/fr unknown
- 1998-09-03 WO PCT/US1998/018289 patent/WO1999011637A1/fr not_active Ceased
- 1998-09-03 CA CA002302361A patent/CA2302361A1/fr not_active Abandoned
- 1998-09-03 JP JP2000508676A patent/JP2001514257A/ja not_active Withdrawn
- 1998-09-03 EP EP98945850A patent/EP1015438A4/fr not_active Withdrawn
- 1998-09-03 ZA ZA988064A patent/ZA988064B/xx unknown
- 1998-09-03 CO CO98050517A patent/CO4970736A1/es unknown
- 1998-09-03 AU AU93002/98A patent/AU9300298A/en not_active Abandoned
- 1998-09-04 PE PE1998000830A patent/PE115699A1/es not_active Application Discontinuation
- 1998-10-17 SA SA98190653A patent/SA98190653A/ar unknown

Also Published As

Publication number	Publication date
JP2001514257A (ja)	2001-09-11
CO4970736A1 (es)	2000-11-07
AU9300298A (en)	1999-03-22
CA2302361A1 (fr)	1999-03-11
EP1015438A4 (fr)	2000-11-08
ZA988064B (en)	1999-05-28
MA26540A1 (fr)	2004-12-20
PE115699A1 (es)	2000-01-13
WO1999011637A1 (fr)	1999-03-11
EP1015438A1 (fr)	2000-07-05

Publication	Publication Date	Title
JPH03118357A (ja)	1991-05-20	新規なペプチダーゼとイソメラーゼの阻害剤
PT100234B (pt)	1999-06-30	Novos esteres de alcoois aminados biciclicos e triciclicos, processo para a sua preparacao
HUE025553T2 (en)	2016-02-29	CFTR modulators
UA128374C2 (uk)	2024-06-26	Гетероароматичні сполуки як інгібітори ваніну
WO2019211585A1 (fr)	2019-11-07	Inhibiteurs du facteur xiia
UA82093C2 (uk)	2008-03-11	Фтор- та трифторалкіловмісні гетероциклічні сульфонамідні інгібітори утворення бета-амілоїду та їх похідні
CN1326870C (zh)	2007-07-18	抗菌的酰胺大环类物质
TW200538112A (en)	2005-12-01	Novel compounds
SA98190653A (ar)	2005-12-03	مثبطات بروتييز مساعدة
UA58589C2 (uk)	2003-08-15	Тієнілазолілалкоксіетанаміни, спосіб їх одержання, проміжні продукти для їх одержання та фармацевтична композиція
CZ293825B6 (cs)	2004-08-18	ChinoxalinyŹ způsob jejich výroby a jejich použití a farmaceutické prostředky tyto látky obsahující
AU592838B2 (en)	1990-01-25	Novel pyrrolidinylamide ester derivative having anti-prolyl endopeptidase activity and synthesis and use thereof
US8324202B2 (en)	2012-12-04	5-phenyl-1H-benzo [E] [1,4] diazepine compounds substituted with an hydroxamic acid group as histone deacetylase inhibitors
US6815214B2 (en)	2004-11-09	Pharmaceutical uses and synthesis of diketopiperazines
US6660832B1 (en)	2003-12-09	Macrocyclic compounds and preparation methods thereof
CZ20011152A3 (cs)	2001-07-11	Substituované 1,3-diaryl-2-pyridin-2-yl-3-(pyridin-2-ylamino)propanolové deriváty, způsob jejich přípravy, léčiva obsahující tyto sloučeniny a jejich použití
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Panjla et al.	2023	Targeting multidrug resistant Staphylococcus aureus with cationic chlorpromazine‐peptide conjugates
TW206224B (fr)	1993-05-21
CA2368733C (fr)	2014-10-07	Derives de phenylalanine
AU2002309420B2 (en)	2007-11-08	New compounds useful in reflux disease
IE46838B1 (en)	1983-10-05	Novel substituted phenylacetic acid amide compounds and processes for their preparation
WO2016144830A1 (fr)	2016-09-15	Emricasan deutéré
CN115322120B (zh)	2024-04-30	一类小分子化合物及在制备治疗dhodh介导疾病药物中的用途
US3960833A (en)	1976-06-01	Butirosin A 3",5"-O-isopropylidene derivatives