NZ502876A - Fused bicyclic lactam selective factor Xa inhibitors for treating thrombosis related diseases - Google Patents

Fused bicyclic lactam selective factor Xa inhibitors for treating thrombosis related diseases

Info

Publication number: NZ502876A
Authority: NZ; New Zealand
Prior art keywords: group; compound; aryl; 6alkyl; alkyl
Prior art date: 1997-08-11

Application number

NZ502876A

Other languages

English (en)

Inventor

Bing-Yan Zhu

Robert M Scarborough

Original Assignee

Cor Therapeutics 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.)

1997-08-11

Filing date

1998-08-11

Publication date

2001-11-30

1998-08-11 Application filed by Cor Therapeutics Inc filed Critical Cor Therapeutics Inc

2001-11-30 Publication of NZ502876A publication Critical patent/NZ502876A/en

Links

208000007536 Thrombosis Diseases 0.000 title claims abstract description 20
-1 bicyclic lactam Chemical class 0.000 title description 36
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title description 9
201000010099 disease Diseases 0.000 title description 8
229940123583 Factor Xa inhibitor Drugs 0.000 title description 7
150000001875 compounds Chemical class 0.000 claims abstract description 242
229910052739 hydrogen Inorganic materials 0.000 claims abstract description 125
125000003118 aryl group Chemical group 0.000 claims abstract description 121
125000000623 heterocyclic group Chemical group 0.000 claims abstract description 29
125000005842 heteroatom Chemical group 0.000 claims abstract description 27
125000006340 pentafluoro ethyl group Chemical group FC(F)(F)C(F)(F)* 0.000 claims abstract description 16
125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims abstract description 12
206010047249 Venous thrombosis Diseases 0.000 claims abstract description 9
125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims abstract description 7
206010051055 Deep vein thrombosis Diseases 0.000 claims abstract description 7
208000010125 myocardial infarction Diseases 0.000 claims abstract description 7
125000000882 C2-C6 alkenyl group Chemical group 0.000 claims abstract description 6
208000010378 Pulmonary Embolism Diseases 0.000 claims abstract description 6
206010002383 Angina Pectoris Diseases 0.000 claims abstract description 5
206010038563 Reocclusion Diseases 0.000 claims abstract description 5
210000004351 coronary vessel Anatomy 0.000 claims abstract description 5
206010014498 Embolic stroke Diseases 0.000 claims abstract description 4
206010040070 Septic Shock Diseases 0.000 claims abstract description 4
206010043647 Thrombotic Stroke Diseases 0.000 claims abstract description 4
208000032109 Transient ischaemic attack Diseases 0.000 claims abstract description 4
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229960002317 succinimide Drugs 0.000 description 1
239000005720 sucrose Substances 0.000 description 1
150000005846 sugar alcohols Chemical class 0.000 description 1
PXQLVRUNWNTZOS-UHFFFAOYSA-N sulfanyl Chemical class [SH] PXQLVRUNWNTZOS-UHFFFAOYSA-N 0.000 description 1
230000004083 survival effect Effects 0.000 description 1
238000013268 sustained release Methods 0.000 description 1
239000012730 sustained-release form Substances 0.000 description 1
239000003765 sweetening agent Substances 0.000 description 1
230000002195 synergetic effect Effects 0.000 description 1
239000012622 synthetic inhibitor Substances 0.000 description 1
230000009885 systemic effect Effects 0.000 description 1
230000008685 targeting Effects 0.000 description 1
235000002906 tartaric acid Nutrition 0.000 description 1
239000011975 tartaric acid Substances 0.000 description 1
VQADGGIIRBPDPH-UHFFFAOYSA-N tert-butyl n-[(2-methylpropan-2-yl)oxycarbonyl]-n-[[3-[(z)-n'-phenylmethoxycarbonylcarbamimidoyl]phenyl]methyl]carbamate Chemical compound CC(C)(C)OC(=O)N(C(=O)OC(C)(C)C)CC1=CC=CC(C(=N)NC(=O)OCC=2C=CC=CC=2)=C1 VQADGGIIRBPDPH-UHFFFAOYSA-N 0.000 description 1
WYOYHYCGFCPUGC-UHFFFAOYSA-N tert-butyl n-[(2-methylpropan-2-yl)oxycarbonyl]-n-[[4-[(e)-n'-phenylmethoxycarbonylcarbamimidoyl]phenyl]methyl]carbamate Chemical compound C1=CC(CN(C(=O)OC(C)(C)C)C(=O)OC(C)(C)C)=CC=C1C(=N)NC(=O)OCC1=CC=CC=C1 WYOYHYCGFCPUGC-UHFFFAOYSA-N 0.000 description 1
LCKJQFJCUDSKES-UHFFFAOYSA-N tert-butyl n-[(3-carbamimidoylphenyl)methyl]-n-[(2-methylpropan-2-yl)oxycarbonyl]carbamate Chemical compound CC(C)(C)OC(=O)N(C(=O)OC(C)(C)C)CC1=CC=CC(C(N)=N)=C1 LCKJQFJCUDSKES-UHFFFAOYSA-N 0.000 description 1
CQVIJSNGOULZTD-UHFFFAOYSA-N tert-butyl n-[[3-[(z)-n'-hydroxycarbamimidoyl]phenyl]methyl]-n-[(2-methylpropan-2-yl)oxycarbonyl]carbamate Chemical compound CC(C)(C)OC(=O)N(C(=O)OC(C)(C)C)CC1=CC=CC(C(=N)NO)=C1 CQVIJSNGOULZTD-UHFFFAOYSA-N 0.000 description 1
125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
150000003512 tertiary amines Chemical class 0.000 description 1
125000001935 tetracenyl group Chemical group C1(=CC=CC2=CC3=CC4=CC=CC=C4C=C3C=C12)* 0.000 description 1
YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
229960004559 theobromine Drugs 0.000 description 1
125000000335 thiazolyl group Chemical group 0.000 description 1
125000005309 thioalkoxy group Chemical group 0.000 description 1
239000003868 thrombin inhibitor Substances 0.000 description 1
230000002885 thrombogenetic effect Effects 0.000 description 1
230000036964 tight binding Effects 0.000 description 1
230000036962 time dependent Effects 0.000 description 1
239000012049 topical pharmaceutical composition Substances 0.000 description 1
125000002088 tosyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1C([H])([H])[H])S(*)(=O)=O 0.000 description 1
YFTHZRPMJXBUME-UHFFFAOYSA-N tripropylamine Chemical compound CCCN(CCC)CCC YFTHZRPMJXBUME-UHFFFAOYSA-N 0.000 description 1
LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
239000012588 trypsin Substances 0.000 description 1
229960005356 urokinase Drugs 0.000 description 1
231100000216 vascular lesion Toxicity 0.000 description 1
210000003462 vein Anatomy 0.000 description 1
239000002435 venom Substances 0.000 description 1
210000001048 venom Anatomy 0.000 description 1
231100000611 venom Toxicity 0.000 description 1
229940088594 vitamin Drugs 0.000 description 1
239000011782 vitamin Substances 0.000 description 1
235000013343 vitamin Nutrition 0.000 description 1
229930003231 vitamin Natural products 0.000 description 1
150000003722 vitamin derivatives Chemical class 0.000 description 1
PJVWKTKQMONHTI-UHFFFAOYSA-N warfarin Chemical compound OC=1C2=CC=CC=C2OC(=O)C=1C(CC(=O)C)C1=CC=CC=C1 PJVWKTKQMONHTI-UHFFFAOYSA-N 0.000 description 1
229960005080 warfarin Drugs 0.000 description 1
BPICBUSOMSTKRF-UHFFFAOYSA-N xylazine Chemical compound CC1=CC=CC(C)=C1NC1=NCCCS1 BPICBUSOMSTKRF-UHFFFAOYSA-N 0.000 description 1
229960001600 xylazine Drugs 0.000 description 1
239000011701 zinc Substances 0.000 description 1
229910052725 zinc Inorganic materials 0.000 description 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06139—Dipeptides with the first amino acid being heterocyclic
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
General Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Medicinal Chemistry (AREA)
Chemical Kinetics & Catalysis (AREA)
Public Health (AREA)
Hematology (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Diabetes (AREA)
Pharmacology & Pharmacy (AREA)
Bioinformatics & Cheminformatics (AREA)
Animal Behavior & Ethology (AREA)
Engineering & Computer Science (AREA)
General Chemical & Material Sciences (AREA)
Veterinary Medicine (AREA)
Biochemistry (AREA)
Biophysics (AREA)
Genetics & Genomics (AREA)
Molecular Biology (AREA)
Proteomics, Peptides & Aminoacids (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Peptides Or Proteins (AREA)

NZ502876A 1997-08-11 1998-08-11 Fused bicyclic lactam selective factor Xa inhibitors for treating thrombosis related diseases NZ502876A (en)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
US8418497P	1997-08-11	1997-08-11
US90803197A	1997-08-11	1997-08-11
PCT/US1998/016705 WO1999007731A1 (fr)	1997-08-11	1998-08-11	INHIBITEURS SELECTIFS DU FACTEUR Xa

Publications (1)

Publication Number	Publication Date
NZ502876A true NZ502876A (en)	2001-11-30

Family

ID=26770690

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
NZ502876A NZ502876A (en)	1997-08-11	1998-08-11	Fused bicyclic lactam selective factor Xa inhibitors for treating thrombosis related diseases

Country Status (5)

Country	Link
EP (1)	EP0994894A1 (fr)
JP (1)	JP2001515842A (fr)
CA (1)	CA2299610A1 (fr)
NZ (1)	NZ502876A (fr)
WO (1)	WO1999007731A1 (fr)

Families Citing this family (32)

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US6194435B1 (en)	1996-10-11	2001-02-27	Cor Therapeutics, Inc.	Lactams as selective factor Xa inhibitors
US6262047B1 (en)	1996-10-11	2001-07-17	Cor Therapeutics, Inc.	Selective factor Xa inhibitors
US6063794A (en)	1996-10-11	2000-05-16	Cor Therapeutics Inc.	Selective factor Xa inhibitors
US6369080B2 (en)	1996-10-11	2002-04-09	Cor Therapeutics, Inc.	Selective factor Xa inhibitors
NZ500353A (en)	1997-04-14	2002-02-01	Cor Therapeutics Inc	Cyclic diaza compounds that are selective inhibitors of factor Xa
AU747531B2 (en)	1997-04-14	2002-05-16	Millennium Pharmaceuticals, Inc.	Selective factor Xa inhibitors
AU6896398A (en)	1997-04-14	1998-11-11	Cor Therapeutics, Inc.	Selective factor xa inhibitors
AU741099B2 (en) *	1997-04-14	2001-11-22	Millennium Pharmaceuticals, Inc.	Selective factor Xa inhibitors
US6333321B1 (en)	1997-08-11	2001-12-25	Cor Therapeutics, Inc.	Selective factor Xa inhibitors
US6218382B1 (en)	1997-08-11	2001-04-17	Cor Therapeutics, Inc	Selective factor Xa inhibitors
US6228854B1 (en)	1997-08-11	2001-05-08	Cor Therapeutics, Inc.	Selective factor Xa inhibitors
NZ525513A (en)	1998-08-07	2004-09-24	Pont Pharmaceuticals Du	Succinoylamino lactams as inhibitors of Abeta protein production
HRP990246A2 (en)	1998-08-07	2000-06-30	Du Pont Pharm Co	Succinoylamino benzodiazepines as inhibitors of a beta protein production
WO2000038618A2 (fr)	1998-12-24	2000-07-06	Du Pont Pharmaceuticals Company	BENZODIAZEPINES SUCCINOYLAMINO UTILISEES COMME INHIBITEURS DE LA PRODUCTION DE PROTEINE A$g(b)
US6297233B1 (en)	1999-02-09	2001-10-02	Bristol-Myers Squibb Company	Lactam inhibitors of FXa and method
US6960576B2 (en)	1999-09-13	2005-11-01	Bristol-Myers Squibb Pharma Company	Hydroxyalkanoylaminolactams and related structures as inhibitors of Aβ protein production
HK1050005A1 (zh)	1999-09-13	2003-06-06	三维药物公司	氮杂环烷酮丝氨酸蛋白酶抑制剂
US6503902B2 (en)	1999-09-13	2003-01-07	Bristol-Myers Squibb Pharma Company	Hydroxyalkanoylaminolactams and related structures as inhibitors of a β protein production
WO2001027108A1 (fr)	1999-10-08	2001-04-19	Bristol-Myers Squibb Pharma Company	AMINO SULFONAMIDES DE LACTAME UTILISES COMME INHIBITEURS DE LA PRODUCTION DE PROTEINE A$g(b)
JP2003523345A (ja)	2000-02-17	2003-08-05	ブリストル−マイヤーズスクイブファーマカンパニー	Ａβタンパク質産生の阻害剤としてのスクシノイルアミノ炭素環および複素環
US6495540B2 (en)	2000-03-28	2002-12-17	Bristol - Myers Squibb Pharma Company	Lactams as inhibitors of A-β protein production
EP1268434A1 (fr)	2000-04-03	2003-01-02	Bristol-Myers Squibb Pharma Company	Lactames cycliques utiles en tant qu'inhibiteurs de la production de proteine a-beta
EP1268433A1 (fr)	2000-04-03	2003-01-02	Bristol-Myers Squibb Pharma Company	Lactames cycliques utilises comme inhibiteurs de la production de la proteine beta-amyloide
CA2404273A1 (fr)	2000-04-11	2001-10-18	Bristol-Myers Squibb Pharma Company	Lactames substitues utilises en tant qu'inhibiteurs de production de proteine a.beta.
AU2001255408A1 (en) *	2000-04-14	2001-10-30	Corvas International, Inc.	Tetrahydro-azepinone derivatives as thrombin inhibitors
CN1386118A (zh)	2000-06-01	2002-12-18	布里斯托尔-迈尔斯斯奎布药品公司	作为Aβ蛋白产生抑制剂的被环状琥珀酸酯取代的内酰胺类化合物
US6511973B2 (en)	2000-08-02	2003-01-28	Bristol-Myers Squibb Co.	Lactam inhibitors of FXa and method
EP1569912B1 (fr)	2002-12-03	2015-04-29	Pharmacyclics, Inc.	Derives de 2-(2-hydroxybiphenyl-3-yl)-1h-benzoimidazole-5-carboxamidine utilises en tant qu'inhibiteurs du facteur viia
CA2533824A1 (fr) *	2003-07-31	2005-02-10	Irm, Llc	Composes bicycliques et compositions utilisees comme inhibiteurs pdf
SG10201913587WA (en)	2016-02-05	2020-02-27	Denali Therapeutics Inc	Inhibitors of receptor-interacting protein kinase 1
DK3552017T3 (da)	2016-12-09	2022-05-16	Denali Therapeutics Inc	Forbindelser, der er anvendelige som ripk1-inhibitorer
WO2023137035A1 (fr)	2022-01-12	2023-07-20	Denali Therapeutics Inc.	Formes cristallines de ((s)-5-benzyl-n-(5-méthyl-4-oxo-2, 3,4,5- tétrahydropyrido [3,2-b] [l,4]oxazépin-3-yl)-4h-l,2,4-triazole-3-carboxamide

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
JPH10503176A (ja) *	1994-06-17	1998-03-24	コーバスインターナショナル，インコーポレイテッド	酵素インヒビターとしての３−アミノ−２−オキソ−１−ピペリジン酢酸誘導体
JPH10513151A (ja) *	1994-12-22	1998-12-15	バイオケムファーマインコーポレイテッド	トロンビン阻害剤としての複素環式ケトアルギニンペプチド
WO1998016523A2 (fr) *	1996-10-11	1998-04-23	Cor Therapeutics, Inc.	Inhibiteurs competitifs du facteur xa

1998
- 1998-08-11 WO PCT/US1998/016705 patent/WO1999007731A1/fr not_active Ceased
- 1998-08-11 EP EP98939912A patent/EP0994894A1/fr not_active Withdrawn
- 1998-08-11 CA CA002299610A patent/CA2299610A1/fr not_active Abandoned
- 1998-08-11 NZ NZ502876A patent/NZ502876A/en unknown
- 1998-08-11 JP JP2000506233A patent/JP2001515842A/ja active Pending

Also Published As

Publication number	Publication date
EP0994894A1 (fr)	2000-04-26
JP2001515842A (ja)	2001-09-25
WO1999007731A1 (fr)	1999-02-18
CA2299610A1 (fr)	1999-02-18

Legal Events

Date	Code	Title	Description
2002-03-28	PSEA	Patent sealed