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PE20010229A1 - PYRIMIDONES SUBSTITUTED FOR ARYLS AND POLYCYCLIC HETEROARYLS USEFUL FOR THE SELECTIVE INHIBITION OF THE COAGULATION CASCADE - Google Patents

PYRIMIDONES SUBSTITUTED FOR ARYLS AND POLYCYCLIC HETEROARYLS USEFUL FOR THE SELECTIVE INHIBITION OF THE COAGULATION CASCADE

Info

Publication number
PE20010229A1
PE20010229A1 PE2000000575A PE0005752000A PE20010229A1 PE 20010229 A1 PE20010229 A1 PE 20010229A1 PE 2000000575 A PE2000000575 A PE 2000000575A PE 0005752000 A PE0005752000 A PE 0005752000A PE 20010229 A1 PE20010229 A1 PE 20010229A1
Authority
PE
Peru
Prior art keywords
alkyl
aryls
coagulation cascade
substituted
group
Prior art date
Application number
PE2000000575A
Other languages
Spanish (es)
Inventor
Michael S South
Melvin L Rueppel
Hamme
William L Neumann
Darin E Jones
Original Assignee
Monsanto Co
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.)
Filing date
Publication date
Application filed by Monsanto Co filed Critical Monsanto Co
Publication of PE20010229A1 publication Critical patent/PE20010229A1/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/02Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D253/00Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
    • C07D253/02Heterocyclic 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
    • C07D253/061,2,4-Triazines
    • C07D253/0651,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
    • C07D253/071,2,4-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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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)
  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)

Abstract

SE REFIERE A PIRIMIDONAS SUSTITUIDAS DE ARILOS Y HETEROARILOS POLICICLICOS DE FORMULA I, DONDE: B ES UN GRUPO b; R9-R13, R32-R36 SON ACETAMIDO, HALOACETAMIDO, ENTRE OTROS; R9-R13 SON HETEROARILO, HETEROCICLILO SI R9-R13 NO SON SUSTITUYENTES DE B; R16, R19, R32-R36 SON Qb, UNO DE R16 Y R19 ES Qb Y Qb ES Qbe; B ES TRIALQUILSILILO, ALQUILO C2-C8, ENTRE OTROS; A ES UN ENLACE, (W7)rr-(CH(R15))pa, ENTRE OTROS; rr ES 0-1; pa ES 0-6; W7 ES O, S, C(O), (R7)NC(O), ENTRE OTROS; R7 ES OH, ALQUILO; R15 ES OH, HALO, ALQUILO, HALOALQUILO; ES NH, NOH; M ES N, R1-C; R1 ES ALQUILO, CIANO, ENTRE OTROS; R2 ES Z°-Q; Z° ES (CR41R42)q; q ES 1-3; R41 Y R42 SON AMIDINO, HIDROXIAMINO, ENTRE OTROS; Q ES UN GRUPO II; D1, D2, J1, J2, K1 SON C, N, O, S, UN ENLACE; K ES (CR4aRb)n; n ES 1-2; R4a Y R4b SON HALO, HIDROXIALQUILO, ALQUILO; E° ES E1; E1 ES CO, CS, CONR7, SO2, ENTRE OTROS; Y° ES GRUPO IV, ENTRE OTROS; D5, D6, J5, J6 SON C, N, O, S, ENTRE OTROS; Qb ES AMINOALQUILENILO, ENTRE OTROS; Qbe ES NR6CNR25NR23R24, ENTRE OTROS. NO MAS DE UNO DE R20 Y R21 o R23 Y R24 SON OH, AMINO, ENTRE OTROS; R20 A R26 SON ALQUILO, OH, ENTRE OTROS. LOS COMPUESTOS DE PIRIMIDONAS SUSTITUIDAS SON INHIBIDORES DE PROTEASAS DE SERINA DE LA CASCADA DE COAGULACION POR LO QUE PUEDEN SER UTILES PARA EL TRATAMIENTO DE ENFERMEDADES TROMBOTICAS, CORONARIAS, CEREBROVASCULARESREFERS TO PYRIMIDONES SUBSTITUTED FOR ARYLS AND POLYCYCLIC HETEROARYLS OF FORMULA I, WHERE: B IS A GROUP b; R9-R13, R32-R36 ARE ACETAMIDE, HALOACETAMIDE, AMONG OTHERS; R9-R13 ARE HETEROARYL, HETERO CYCLYL IF R9-R13 ARE NOT A SUBSTITUTE FOR B; R16, R19, R32-R36 ARE Qb, ONE OF R16 AND R19 IS Qb AND Qb IS Qbe; B IS TRIALKYSILYL, C2-C8 ALKYL, AMONG OTHERS; A IS A LINK, (W7) rr- (CH (R15)) pa, AMONG OTHERS; rr IS 0-1; pa IS 0-6; W7 IS O, S, C (O), (R7) NC (O), AMONG OTHERS; R7 IS OH, ALKYL; R15 IS OH, HALO, ALKYL, HALOALKYL; IS NH, NOH; M IS N, R1-C; R1 IS ALKYL, CYANO, AMONG OTHERS; R2 IS Z ° -Q; Z ° ES (CR41R42) q; q IS 1-3; R41 AND R42 ARE AMIDINE, HYDROXYAMINE, AMONG OTHERS; Q IS A GROUP II; D1, D2, J1, J2, K1 ARE C, N, O, S, A LINK; K IS (CR4aRb) n; n IS 1-2; R4a AND R4b ARE HALO, HYDROXYALKYL, ALKYL; E ° IS E1; E1 IS CO, CS, CONR7, SO2, AMONG OTHERS; Y ° IS GROUP IV, AMONG OTHERS; D5, D6, J5, J6 ARE C, N, O, S, AMONG OTHERS; Qb IS AMINOALKYLENYL, AMONG OTHERS; Qbe IS NR6CNR25NR23R24, AMONG OTHERS. NO MORE THAN ONE OF R20 AND R21 or R23 AND R24 ARE OH, AMINO, AMONG OTHERS; R20 TO R26 ARE ALKYL, OH, AMONG OTHERS. SUBSTITUTED PYRIMIDONE COMPOUNDS ARE INHIBITORS OF SERINE PROTEASES FROM THE COAGULATION CASCADE SO THEY MAY BE USEFUL FOR THE TREATMENT OF THROMBOTIC, CORONARY, CEREBROVASCULAR DISEASES

PE2000000575A 1999-05-19 2000-06-09 PYRIMIDONES SUBSTITUTED FOR ARYLS AND POLYCYCLIC HETEROARYLS USEFUL FOR THE SELECTIVE INHIBITION OF THE COAGULATION CASCADE PE20010229A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US13479499P 1999-05-19 1999-05-19

Publications (1)

Publication Number Publication Date
PE20010229A1 true PE20010229A1 (en) 2001-03-07

Family

ID=22465042

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2000000575A PE20010229A1 (en) 1999-05-19 2000-06-09 PYRIMIDONES SUBSTITUTED FOR ARYLS AND POLYCYCLIC HETEROARYLS USEFUL FOR THE SELECTIVE INHIBITION OF THE COAGULATION CASCADE

Country Status (22)

Country Link
EP (1) EP1178970A1 (en)
JP (1) JP2002544262A (en)
KR (1) KR20010114271A (en)
CN (1) CN1157380C (en)
AR (1) AR030021A1 (en)
AU (2) AU771718B2 (en)
BR (1) BR0010758A (en)
CA (1) CA2373614A1 (en)
CZ (1) CZ20014116A3 (en)
EA (1) EA004867B1 (en)
HU (1) HUP0201242A3 (en)
IL (1) IL146243A0 (en)
MX (1) MXPA01011804A (en)
NO (1) NO20015604L (en)
NZ (1) NZ514874A (en)
PE (1) PE20010229A1 (en)
PL (1) PL352827A1 (en)
SK (1) SK15852001A3 (en)
TW (1) TWI222445B (en)
UY (1) UY26156A1 (en)
WO (1) WO2000069832A1 (en)
ZA (2) ZA200109339B (en)

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US6750342B1 (en) 1999-05-19 2004-06-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
US6716838B1 (en) 1999-05-19 2004-04-06 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils as anticoagulative agents
US6653316B1 (en) 1999-05-19 2003-11-25 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
KR20010113969A (en) * 1999-05-19 2001-12-28 추후보정 Substituted polycyclic aryl and heteroaryl uracils as anticoagulative agents
US7015230B1 (en) 1999-05-19 2006-03-21 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
US6458952B1 (en) 1999-05-19 2002-10-01 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
US6867217B1 (en) 1999-05-19 2005-03-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade
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
WO2001087851A1 (en) * 2000-05-18 2001-11-22 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones 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
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
MXPA03004458A (en) 2000-11-20 2005-01-25 Pharmacia Corp Substituted polycyclic aryl and heteroaryl pyridines 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
WO2003029224A1 (en) * 2001-10-03 2003-04-10 Pharmacia Corporation 6-membered unsaturated 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
JP2005532268A (en) 2002-02-22 2005-10-27 ファルマシア・アンド・アップジョン・カンパニー・エルエルシー Substituted pyrimidinones and pyrimidinethiones
TW200307667A (en) 2002-05-06 2003-12-16 Bristol Myers Squibb Co Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors
US7217794B2 (en) 2003-04-02 2007-05-15 Daiamed, Inc. Compounds and methods for treatment of thrombosis
US7182738B2 (en) 2003-04-23 2007-02-27 Marctec, Llc Patient monitoring apparatus and method for orthosis and other devices
CA2610400A1 (en) * 2005-06-07 2006-12-14 Pharmacopeia, Inc. Azinone and diazinone v3 inhibitors for depression and stress disorders
CN104311537B (en) * 2014-09-19 2016-08-24 广东东阳光药业有限公司 Containing pyrimidone acetyl substituents pyrazole compound and combinations thereof thing and purposes
AU2020396565C1 (en) * 2019-12-04 2025-05-15 Omeros Corporation MASP-2 inhibitors and methods of use
CN115779953B (en) * 2022-12-19 2024-06-21 中南大学 Copper-loaded carbon-based monoatomic material, and preparation method and application thereof

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US5441960A (en) * 1992-04-16 1995-08-15 Zeneca Limited 1-pyrimidinylacetamide human leukocyte elastate inhibitors
US5948785A (en) * 1995-04-27 1999-09-07 The Green Cross Corporation Heterocyclic amide compounds and pharmaceutical use of the same

Also Published As

Publication number Publication date
AU771718B2 (en) 2004-04-01
AR030021A1 (en) 2003-08-13
UY26156A1 (en) 2000-12-29
BR0010758A (en) 2003-06-10
HUP0201242A2 (en) 2002-12-28
TWI222445B (en) 2004-10-21
EA200101214A1 (en) 2002-06-27
KR20010114271A (en) 2001-12-31
NZ514874A (en) 2004-11-26
AU2004202375A1 (en) 2004-06-24
AU4973400A (en) 2000-12-05
ZA200400448B (en) 2004-09-29
EP1178970A1 (en) 2002-02-13
EA004867B1 (en) 2004-08-26
SK15852001A3 (en) 2003-06-03
HUP0201242A3 (en) 2003-02-28
WO2000069832A1 (en) 2000-11-23
PL352827A1 (en) 2003-09-08
NO20015604L (en) 2002-01-11
IL146243A0 (en) 2002-07-25
ZA200109339B (en) 2004-05-26
CN1351593A (en) 2002-05-29
NO20015604D0 (en) 2001-11-16
CZ20014116A3 (en) 2002-06-12
CN1157380C (en) 2004-07-14
CA2373614A1 (en) 2000-11-23
JP2002544262A (en) 2002-12-24
MXPA01011804A (en) 2003-09-04

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