PE20010217A1 - URACILS SUBSTITUTED FOR ARYLS AND POLYCYCLIC HETEROARYLS USEFUL FOR THE SELECTIVE INHIBITION OF THE COAGULATION CASCADE - Google Patents
URACILS SUBSTITUTED FOR ARYLS AND POLYCYCLIC HETEROARYLS USEFUL FOR THE SELECTIVE INHIBITION OF THE COAGULATION CASCADEInfo
- Publication number
- PE20010217A1 PE20010217A1 PE2000000543A PE0005432000A PE20010217A1 PE 20010217 A1 PE20010217 A1 PE 20010217A1 PE 2000000543 A PE2000000543 A PE 2000000543A PE 0005432000 A PE0005432000 A PE 0005432000A PE 20010217 A1 PE20010217 A1 PE 20010217A1
- Authority
- PE
- Peru
- Prior art keywords
- hydride
- aryls
- alkyl
- coagulation cascade
- selective inhibition
- Prior art date
Links
- 230000015271 coagulation Effects 0.000 title 1
- 238000005345 coagulation Methods 0.000 title 1
- 230000005764 inhibitory process Effects 0.000 title 1
- 150000004678 hydrides Chemical class 0.000 abstract 5
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 abstract 4
- 229910052799 carbon Inorganic materials 0.000 abstract 4
- 229910052760 oxygen Inorganic materials 0.000 abstract 4
- 229910052717 sulfur Inorganic materials 0.000 abstract 4
- RHUYHJGZWVXEHW-UHFFFAOYSA-N 1,1-Dimethyhydrazine Chemical compound CN(C)N RHUYHJGZWVXEHW-UHFFFAOYSA-N 0.000 abstract 2
- YBYIRNPNPLQARY-UHFFFAOYSA-N 1H-indene Natural products C1=CC=C2CC=CC2=C1 YBYIRNPNPLQARY-UHFFFAOYSA-N 0.000 abstract 2
- -1 INDENYL Chemical class 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- LJGHYPLBDBRCRZ-UHFFFAOYSA-N 3-(3-aminophenyl)sulfonylaniline Chemical compound NC1=CC=CC(S(=O)(=O)C=2C=C(N)C=CC=2)=C1 LJGHYPLBDBRCRZ-UHFFFAOYSA-N 0.000 abstract 1
- AVXURJPOCDRRFD-UHFFFAOYSA-N Hydroxylamine Chemical compound ON AVXURJPOCDRRFD-UHFFFAOYSA-N 0.000 abstract 1
- 208000007536 Thrombosis Diseases 0.000 abstract 1
- 150000001409 amidines Chemical class 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- ZZUFCTLCJUWOSV-UHFFFAOYSA-N furosemide Chemical group C1=C(Cl)C(S(=O)(=O)N)=CC(C(O)=O)=C1NCC1=CC=CO1 ZZUFCTLCJUWOSV-UHFFFAOYSA-N 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical class [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 abstract 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/52—Two oxygen atoms
- C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
- C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D253/00—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
- C07D253/02—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 not condensed with other rings
- C07D253/06—1,2,4-Triazines
- C07D253/065—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
- C07D253/07—1,2,4-Triazines having 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
- C07D253/075—Two hetero atoms, in positions 3 and 5
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
SE REFIERE A URACILOS SUSTITUIDOS CON ARILOS Y HETEROARILOS POLICICLICOS I, DONDE: B ES EL GRUPO a; D1, D2, J1, J2, K1 SON C, N, O, S, ENLACE, NO MAS DE UNO DE D1, D2, J1, J2, K1 ES O, S, ENTRE OTRAS CONDICIONES; R9, R10, R11, R12, R13, R32, R33, R34, R35, R36 SON HIDRURO, ACETAMIDO, HALOACETAMIDO, ENTRE OTROS; R16, R19, R32, R33, R34, R35, R36 SON Qb, NO MAS DE UNO DE R16 Y R19 ES Qb; Qb ES Qbc; B ES HIDRURO, TRIALQUILSILILO, ALQUILO C2-C8, ENTRE OTROS; A ES UN ENLACE, (W7)rr-(CH(R15)pa Y (CH(R15))pa-(W7)rr; rr ES 0-1; pa ES 0-6; W7 ES O, S, C(O), (R7)NC(S), N(R7); R7 ES HIDRURO, OH, ALQUILO; R15 ES HIDRURO, OH, ES NH, NOH; M ES N, R1-C; R1 ES HIDRURO, ALQUILO, ALQUENILO, ENTRE OTROS; R2 ES Z°-Q; Z° ES (CR41R42)q, q ES 1-3, ENTRE OTROS; W° ES O, S, C(O), S(O), N(R41), ENTRE OTROS; R41 Y R42 SON AMIDINO, HIDROXIAMINO, ENTRE OTROS; Q ES HIDRURO; K ES (CR4aR4b)n, n ES 1-2; R4a Y R4b SON HALO, HIDRURO, ENTRE OTROS; E° ES E1 CUANDO K ES (CR4aR4b); E1 ES CO, C(S), CONR7, ENTRE OTROS; Y° ES Qb-Qssss, ENTRE OTROS; Qssss ES (CH(R38))r-W5; r ES 1-2; W5 ES 1,4 INDENILO; 1,5 INDENILO, ENTRE OTROS; R38 ES ARILO, HETEROARILO. UN COMPUESTO PREFERIDO 2-[3-[1-[3-AMINOFENIL]-N-[[4-IMINOMETILFENIL]METIL]-5-[N,N-DIMETILHIDRAZINA]-2,4-DIOXO-2(2H,4H)-PIRIMIDINIL]]ACETAMIDA, ENTRE OTROS. EL COMPUESTO I INHIBE LA TROMBOSIS, FORMACION DE PLAQUETASREFERS TO URACILS REPLACED WITH ARYLS AND POLYCYCLIC HETEROARYLS I, WHERE: B IS GROUP a; D1, D2, J1, J2, K1 ARE C, N, O, S, LINK, NO MORE THAN ONE OF D1, D2, J1, J2, K1 IS O, S, AMONG OTHER CONDITIONS; R9, R10, R11, R12, R13, R32, R33, R34, R35, R36 ARE HYDRIDE, ACETAMIDE, HALOACETAMIDE, AMONG OTHERS; R16, R19, R32, R33, R34, R35, R36 ARE Qb, NO MORE THAN ONE OF R16 AND R19 IS Qb; Qb IS Qbc; B IS HYDRIDE, TRIALKYLSILIL, C2-C8 ALKYL, AMONG OTHERS; A IS A LINK, (W7) rr- (CH (R15) pa Y (CH (R15)) pa- (W7) rr; rr ES 0-1; pa ES 0-6; W7 ES O, S, C ( O), (R7) NC (S), N (R7); R7 IS HYDRIDE, OH, ALKYL; R15 IS HYDRO, OH, IS NH, NOH; M IS N, R1-C; R1 IS HYDRIDE, ALKYL, ALKYL , AMONG OTHERS; R2 IS Z ° -Q; Z ° ES (CR41R42) q, q IS 1-3, AMONG OTHERS; W ° IS O, S, C (O), S (O), N (R41), AMONG OTHERS; R41 AND R42 ARE AMIDINE, HYDROXYAMINE, AMONG OTHERS; Q IS HYDRIDE; K IS (CR4aR4b) n, n IS 1-2; R4a AND R4b ARE HALO, HYDROXY, AMONG OTHERS; E ° IS E1 WHEN K IS ( CR4aR4b); E1 IS CO, C (S), CONR7, AMONG OTHERS; Y ° IS Qb-Qssss, AMONG OTHERS; Qssss ES (CH (R38)) r-W5; r ES 1-2; W5 ES 1.4 INDENYL; 1,5 INDENYL, AMONG OTHERS; R38 IS ARYL, HETEROARYL A PREFERRED COMPOUND 2- [3- [1- [3-AMINOPHENYL] -N - [[4-IMINOMETILPHENYL] METHYL] -5- [N, N -DIMETHYLHYDRAZINE] -2,4-DIOXO-2 (2H, 4H) -PYRIMIDINYL]] ACETAMIDE, AMONG OTHERS COMPOUND I INHIBITS THROMBOSIS, PLATELET FORMATION
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US13495799P | 1999-05-19 | 1999-05-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20010217A1 true PE20010217A1 (en) | 2001-03-07 |
Family
ID=22465795
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2000000543A PE20010217A1 (en) | 1999-05-19 | 2000-06-02 | URACILS SUBSTITUTED FOR ARYLS AND POLYCYCLIC HETEROARYLS USEFUL FOR THE SELECTIVE INHIBITION OF THE COAGULATION CASCADE |
Country Status (14)
| Country | Link |
|---|---|
| EP (1) | EP1178971A1 (en) |
| JP (1) | JP2002544263A (en) |
| KR (1) | KR20010113969A (en) |
| CN (1) | CN1152023C (en) |
| AR (1) | AR043677A1 (en) |
| AU (1) | AU771740B2 (en) |
| BR (1) | BR0011273A (en) |
| CA (1) | CA2373610A1 (en) |
| MX (1) | MXPA01011806A (en) |
| NZ (1) | NZ514877A (en) |
| PE (1) | PE20010217A1 (en) |
| UY (1) | UY26157A1 (en) |
| WO (1) | WO2000069833A1 (en) |
| ZA (2) | ZA200109338B (en) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6716838B1 (en) | 1999-05-19 | 2004-04-06 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl uracils as anticoagulative agents |
| US6867217B1 (en) | 1999-05-19 | 2005-03-15 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade |
| US6653316B1 (en) | 1999-05-19 | 2003-11-25 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade |
| US7015230B1 (en) | 1999-05-19 | 2006-03-21 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade |
| US6458952B1 (en) * | 1999-05-19 | 2002-10-01 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade |
| US6664255B1 (en) | 1999-05-19 | 2003-12-16 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade |
| US6750342B1 (en) | 1999-05-19 | 2004-06-15 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade |
| AU2004200664B2 (en) * | 2000-01-25 | 2007-08-16 | Neurocrine Biosciences, Inc. | Gonadotropin-releasing hormone receptor antagonists and methods relating thereto |
| JP4931314B2 (en) | 2000-01-25 | 2012-05-16 | ニューロクライン バイオサイエンシーズ，インコーポレイテッド | Gonadotropin releasing hormone receptor antagonist and related methods |
| US6852761B2 (en) | 2000-03-13 | 2005-02-08 | Pharmacia Corporation | Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade |
| CA2405561A1 (en) | 2000-04-05 | 2001-10-18 | Pharmacia Corporation | Polycyclic aryl and heteroaryl substituted 4-pyrones useful for selective inhibition of the coagulation cascade |
| EP1268428A2 (en) | 2000-04-05 | 2003-01-02 | Pharmacia Corporation | Polycyclic aryl and heteroaryl substituted 4-pyridones useful for selective inhibition of the coagulation cascade |
| US6686484B2 (en) | 2000-04-17 | 2004-02-03 | Pharmacia Corporation | Polycyclic aryl and heteroaryl substituted 1,4-quinones useful for selective inhibition of the coagulation cascade |
| US6710058B2 (en) | 2000-11-06 | 2004-03-23 | Bristol-Myers Squibb Pharma Company | Monocyclic or bicyclic carbocycles and heterocycles as factor Xa inhibitors |
| MXPA03004458A (en) | 2000-11-20 | 2005-01-25 | Pharmacia Corp | Substituted polycyclic aryl and heteroaryl pyridines useful for selective inhibition of the coagulation cascade. |
| US7015223B1 (en) | 2000-11-20 | 2006-03-21 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl 1,2,4-triazinones useful for selective inhibition of the coagulation cascade |
| US7119094B1 (en) | 2000-11-20 | 2006-10-10 | Warner-Lambert Company | Substituted polycyclic aryl and heteroarpyl pyrazinones useful for selective inhibition of the coagulation cascade |
| WO2003029216A1 (en) | 2001-10-03 | 2003-04-10 | Pharmacia Corporation | 6-membered heterocyclic compounds useful for selective inhibition of the coagulation cascade |
| AU2002367752A1 (en) | 2001-10-03 | 2003-11-17 | Pharmacia Corporation | Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade |
| TW200307667A (en) | 2002-05-06 | 2003-12-16 | Bristol Myers Squibb Co | Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors |
| GB0622472D0 (en) * | 2006-11-10 | 2006-12-20 | Addex Pharmaceuticals Sa | Novel heterocyclic derivatives |
| EP2785700B1 (en) | 2011-11-29 | 2016-03-09 | Perosphere, Inc. | Anticoagulant reversal agents |
| AU2020396565C1 (en) * | 2019-12-04 | 2025-05-15 | Omeros Corporation | MASP-2 inhibitors and methods of use |
| CN116410143A (en) * | 2021-12-29 | 2023-07-11 | 杭州奥默医药股份有限公司 | A kind of multi-substituted uracil derivative and its preparation method and application |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR9509994A (en) * | 1994-12-13 | 1997-12-30 | Corvas Int Inc | Aromatic heterocyclic derivatives as enzyme inhibitors |
| JP2002544262A (en) * | 1999-05-19 | 2002-12-24 | ファルマシア・コーポレイション | Substituted polycyclic aryl and heteroaryl pyrimidinones as useful anticoagulants |
-
2000
- 2000-05-18 KR KR1020017014750A patent/KR20010113969A/en not_active Withdrawn
- 2000-05-18 MX MXPA01011806A patent/MXPA01011806A/en unknown
- 2000-05-18 NZ NZ514877A patent/NZ514877A/en unknown
- 2000-05-18 CN CNB008077533A patent/CN1152023C/en not_active Expired - Fee Related
- 2000-05-18 CA CA002373610A patent/CA2373610A1/en not_active Abandoned
- 2000-05-18 EP EP00931917A patent/EP1178971A1/en not_active Withdrawn
- 2000-05-18 JP JP2000618250A patent/JP2002544263A/en active Pending
- 2000-05-18 AU AU49724/00A patent/AU771740B2/en not_active Ceased
- 2000-05-18 BR BR0011273-9A patent/BR0011273A/en not_active IP Right Cessation
- 2000-05-18 WO PCT/US2000/008226 patent/WO2000069833A1/en not_active Ceased
- 2000-05-19 AR ARP000102449A patent/AR043677A1/en unknown
- 2000-05-19 UY UY26157A patent/UY26157A1/en unknown
- 2000-06-02 PE PE2000000543A patent/PE20010217A1/en not_active Application Discontinuation
-
2001
- 2001-11-13 ZA ZA200109338A patent/ZA200109338B/en unknown
-
2004
- 2004-01-21 ZA ZA200400450A patent/ZA200400450B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2373610A1 (en) | 2000-11-23 |
| NZ514877A (en) | 2004-10-29 |
| EP1178971A1 (en) | 2002-02-13 |
| MXPA01011806A (en) | 2003-09-04 |
| WO2000069833A1 (en) | 2000-11-23 |
| BR0011273A (en) | 2002-06-18 |
| AU771740B2 (en) | 2004-04-01 |
| ZA200400450B (en) | 2004-09-29 |
| JP2002544263A (en) | 2002-12-24 |
| ZA200109338B (en) | 2004-05-26 |
| AU4972400A (en) | 2000-12-05 |
| CN1351594A (en) | 2002-05-29 |
| KR20010113969A (en) | 2001-12-28 |
| UY26157A1 (en) | 2000-12-29 |
| CN1152023C (en) | 2004-06-02 |
| AR043677A1 (en) | 2005-08-10 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Refusal |