HUP0101172A1 - Orto-antranilsavamid-származékok és antikoagulánsokként történő alkalmazásuk - Google Patents

Orto-antranilsavamid-származékok és antikoagulánsokként történő alkalmazásuk

Info

Publication number
HUP0101172A1
HUP0101172A1 HU0101172A HUP0101172A HUP0101172A1 HU P0101172 A1 HUP0101172 A1 HU P0101172A1 HU 0101172 A HU0101172 A HU 0101172A HU P0101172 A HUP0101172 A HU P0101172A HU P0101172 A1 HUP0101172 A1 HU P0101172A1
Authority
HU
Hungary
Prior art keywords
aryl
group
haloalkyl
cyano
halogen
Prior art date
Application number
HU0101172A
Other languages
English (en)
Inventor
Damian O. Arnaiz
You-Ling Chou
Brian D. Griedel
Rushad E. Karanjawala
Monica J. Kochanny
Wheeseong Lee
Amy Mei Liang
Michael M. Morrissey
Gary B. Phillips
Karna Lyn Sacchi
Stephen T. Sakata
Kenneth J. Shaw
R. Michael Snider
Shung C. Wu
Bin Ye
Zuchun Zhao
Original Assignee
Schering Aktiengesellschaft
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
Priority claimed from US09/187,459 external-priority patent/US6140351A/en
Application filed by Schering Aktiengesellschaft filed Critical Schering Aktiengesellschaft
Publication of HUP0101172A1 publication Critical patent/HUP0101172A1/hu
Publication of HUP0101172A3 publication Critical patent/HUP0101172A3/hu

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom 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
    • C07D333/38—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
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes 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 carbon atoms of the hetero ring
    • C07D333/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D333/70—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D417/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • C07D473/06—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)

Abstract

A találmány olyan, egyedi sztereoizomer vagy sztereoizomer-keverékformájában lévő (I) általános képletű vegyületekre - amelynekképletében m 1, 2 vagy 3; n 1, 2, 3, 4 vagy 5; R2-vel és egy vagy többR1-gyel szubsztituált aril- vagy heterociklusos gyűrű; egy vagy többR4-gyel szubsztituált aril- vagy heterociklusos gyűrű; D és E -N (R5)-C(X)-; -R8-N (R5)-C(X)-; -N (R5)-C (X) -R8-; -R8-N (R5)-C(X)-R8-N(R5)-S(O)p-; R8-N(R5)-S(O)p; -N(R5)-S (O)p-R8- vagy -R8-N(R5)-S(O)p-R8-linkercsoport, p 0, 1 vagy 2, X oxigén-, kénatom vagy H2 csoport, ésahol D és E a linker egyik végével az R1 és R2 szubsztituenst hordozóB gyűrűhöz kapcsolódik; R1 hidrogén-, halogénatom, alkil-, aril-,aralkil-, halogén-alkil-, ciano-, -OR5, -S (O)p-R9, -C(O)OR5, -C(O)N(R5)R6, -N(R5) R6, -O-C(O)R5, -N(R5) -CH(R12) -C(O)OR5, adottesetben szubsztituált heterociklil- vagy heterociklil-alkilcsoport; R2hidrogén-, halogénatom, alkil-, aril-, aralkil-, halogén-alkil-,ciano-, -ORS, -S(O)p-R9, -C(O)OR5, -C(O)N(R5)R6, -N(R10)R11, -C(R7)H-N(R10)R11, -C(R7)H-R8-N(R10)R11, -C(R7) H-OR5, -C (R7)H-R8-OR5, -C(R7)H-S(O)p-R9, -C(R7)H-R8-S (O)p-R9-, -O-R8-S (O)p-R9, -C(R7)H-N(R5)R6, -C(R7)H-R8-, -N(R5)R6, -O-R8-CH(OH) -CH2-N(R10)R11, -O-R8-N(R10)R11, -O-R8-O-C(O)R5, -O-R8-CH(OH)-CH2-OR8, -O-(R8-O)t-R5csoport, -O-(R8-O)t-R19, -O-R8-C(O)R5, -O-R8-C(O)R19, -O-R8-C (O)OR5,-N(R5)-RB-N(R10)R11, -S(O)p-R8-N(R5)R6, -S(O)p-RB-C (O)OR5, -N(R5)-CH(R12)-C (O)OR5 csoport; R3 adott esetben egy vagy több R14-gyelszubsztituált aril- vagy heterociklilcsoport, ahol R4 hidrogén-,halogénatom, alkil-, halogén-alkil-, ciano-, nitro-, -OR5, -C(O)OR5, -N (R5) R6, -C(O)N(R5) R6 vagy -R8-N(R5)R6 csoport; és gyógyászatilagelfogadható sóikra vonatkozik, amelyek gátolják a Xa-faktor enzimet ésígy antikoagulánsokként hasznosíthatók. A találmány kiterjed atalálmány szerinti vegyületeket vagy gyógyászatilag elfogadható sóikattartalmazó gyógyszerkészítményekre, valamint a vegyületek vagygyógyászatilag elfogadható sóik alkalmazási eljárásaira is. Ó
HU0101172A 1997-12-19 1998-11-27 Ortho-anthranilamide derivatives and their use as anti-coagulants HUP0101172A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US99428497A 1997-12-19 1997-12-19
US09/187,459 US6140351A (en) 1997-12-19 1998-11-05 Ortho-anthranilamide derivatives as anti-coagulants

Publications (2)

Publication Number Publication Date
HUP0101172A1 true HUP0101172A1 (hu) 2002-05-29
HUP0101172A3 HUP0101172A3 (en) 2002-12-28

Family

ID=26883056

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0101172A HUP0101172A3 (en) 1997-12-19 1998-11-27 Ortho-anthranilamide derivatives and their use as anti-coagulants

Country Status (19)

Country Link
US (2) US6380221B1 (hu)
EP (1) EP1040108B1 (hu)
JP (1) JP3811006B2 (hu)
CN (1) CN1143855C (hu)
AT (1) ATE260103T1 (hu)
AU (1) AU751856B2 (hu)
CA (1) CA2315070A1 (hu)
DE (1) DE69821985T2 (hu)
DK (1) DK1040108T3 (hu)
ES (1) ES2215337T3 (hu)
HU (1) HUP0101172A3 (hu)
IL (1) IL135536A0 (hu)
NO (1) NO20003111L (hu)
NZ (1) NZ503809A (hu)
PL (1) PL341044A1 (hu)
PT (1) PT1040108E (hu)
RU (1) RU2226529C2 (hu)
SK (1) SK9432000A3 (hu)
WO (1) WO1999032477A1 (hu)

Families Citing this family (79)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU707323B2 (en) 1995-03-10 1999-07-08 Berlex Laboratories, Inc. Benzamidine derivatives and their use as anti-coagulants
SK29599A3 (en) 1996-09-12 1999-08-06 Schering Ag Benzamidine derivatives substituted by cyclic amino acid or cyclic hydroxy acid derivatives and their use as anti-coagulants
US6004985A (en) 1996-10-09 1999-12-21 Berlex Laboratories, Inc. Thio acid derived monocylic N-heterocyclics as anticoagulants
ATE306261T1 (de) 1997-06-26 2005-10-15 Lilly Co Eli Antithrombosemittel
EP1007037A4 (en) 1997-06-26 2004-10-06 Lilly Co Eli ANTITHROMBOTIC AGENTS
WO1999000128A1 (en) 1997-06-26 1999-01-07 Eli Lilly And Company Antithrombotic agents
JP2002512633A (ja) 1997-06-26 2002-04-23 イーライ・リリー・アンド・カンパニー 抗血栓剤
US6291514B1 (en) 1998-02-09 2001-09-18 3-Dimensional Pharmaceuticals, Inc. Heteroaryl amidines, methylamidines and guanidines, preparation thereof, and use thereof as protease inhibitors
GB9824579D0 (en) * 1998-11-10 1999-01-06 Novartis Ag Organic compounds
US6127376A (en) 1998-12-04 2000-10-03 Berlex Laboratories, Inc. Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants
EP1140881B1 (en) 1998-12-23 2006-05-17 Eli Lilly And Company Antithrombotic amides
US6689780B1 (en) 1998-12-23 2004-02-10 Eli Lilly And Company Heteroroaromatic amides as inhibitor of factor Xa
AU2055500A (en) 1998-12-23 2000-07-31 Eli Lilly And Company Aromatic amides
EP1161412A1 (en) * 1999-03-16 2001-12-12 Glaxo Group Limited Nuclear receptor arylating compounds
AU5414000A (en) 1999-06-14 2001-01-02 Eli Lilly And Company Compounds
US6844367B1 (en) 1999-09-17 2005-01-18 Millennium Pharmaceuticals, Inc. Benzamides and related inhibitors of factor Xa
US6720317B1 (en) 1999-09-17 2004-04-13 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
JP2003514897A (ja) * 1999-11-24 2003-04-22 シーオーアール セラピューティクス インコーポレイテッド ベータ−アミノ酸系、アスパラギン酸系およびジアミノプロピオン酸系Ｘａ因子阻害剤
WO2001064642A2 (en) 2000-02-29 2001-09-07 Cor Therapeutics, Inc. Benzamides and related inhibitors of factor xa
MY138097A (en) * 2000-03-22 2009-04-30 Du Pont Insecticidal anthranilamides
AU776053B2 (en) 2000-03-31 2004-08-26 Astellas Pharma Inc. Diazepan derivatives or salts thereof
US7160878B2 (en) 2000-07-27 2007-01-09 Eli Lilly And Company Substituted heterocyclic amides
US20040077690A1 (en) * 2000-09-29 2004-04-22 Bing-Yan Zhu Quaternary amidino based inhibitors of factor xa
WO2002026712A2 (en) * 2000-09-29 2002-04-04 Millennium Pharmaceuticals, Inc. Quaternary amines and related inhibitors of factor xa
US6710058B2 (en) 2000-11-06 2004-03-23 Bristol-Myers Squibb Pharma Company Monocyclic or bicyclic carbocycles and heterocycles as factor Xa inhibitors
DK1336605T3 (da) * 2000-11-22 2006-06-19 Astellas Pharma Inc Substituerede phenolderivater eller salte deraf som inhibitorer af koagulationsfaktor X
AU2001297648A1 (en) * 2000-11-28 2002-08-28 Eli Lilly And Company Substituted carboxamides as inhibitors of factor xa
DE10061876A1 (de) * 2000-12-12 2002-06-20 Aventis Pharma Gmbh Arylierte Furan- und Thiophencarbonsäureamide, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament sowie sie enthaltende pharmazeutische Zubereitungen
US6878714B2 (en) 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
US7105682B2 (en) 2001-01-12 2006-09-12 Amgen Inc. Substituted amine derivatives and methods of use
US7102009B2 (en) 2001-01-12 2006-09-05 Amgen Inc. Substituted amine derivatives and methods of use
US20030134836A1 (en) 2001-01-12 2003-07-17 Amgen Inc. Substituted arylamine derivatives and methods of use
US6995162B2 (en) * 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
US6998408B2 (en) 2001-03-23 2006-02-14 Bristol-Myers Squibb Pharma Company 6-5, 6-6, or 6-7 Heterobicycles as factor Xa inhibitors
US6864255B2 (en) 2001-04-11 2005-03-08 Amgen Inc. Substituted triazinyl amide derivatives and methods of use
DE10121003A1 (de) * 2001-04-28 2002-12-19 Aventis Pharma Gmbh Anthranilsäureamide, Verfahren zur Herstellung, ihrer Verwendung als Medikament sowie sie enthaltende pharmazeutische Zubereitungen
SE0102764D0 (sv) 2001-08-17 2001-08-17 Astrazeneca Ab Compounds
TWI320039B (en) 2001-09-21 2010-02-01 Lactam-containing compounds and derivatives thereof as factor xa inhibitors
UA78232C2 (uk) 2001-09-21 2007-03-15 Брістол-Майерс Сквібб Компані Лактамвмісні сполуки та їх похідні як інгібітори фактора ха
TW200302225A (en) 2001-12-04 2003-08-01 Bristol Myers Squibb Co Substituted amino methyl factor Xa inhibitors
AU2002350172A1 (en) 2001-12-07 2003-06-23 Eli Lilly And Company Substituted heterocyclic carboxamides with antithrombotic activity
TW200307667A (en) 2002-05-06 2003-12-16 Bristol Myers Squibb Co Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors
US7312214B2 (en) 2002-05-10 2007-12-25 Bristol-Myers Squibb Company 1, 1-disubstituted cycloalkyl derivatives as factor Xa inhibitors
ES2299702T3 (es) 2002-06-20 2008-06-01 Astrazeneca Ab Derivados de acido benzoico orto-sustituidos para el tratamiento de la resistencia a la insulina.
SE0201937D0 (sv) 2002-06-20 2002-06-20 Astrazeneca Ab Therapeutic agents
US7351858B2 (en) 2002-06-20 2008-04-01 Astrazeneca Ab Ortho-substituted benzoic acid derivatives for the treatment of insulin resistance
US7307088B2 (en) 2002-07-09 2007-12-11 Amgen Inc. Substituted anthranilic amide derivatives and methods of use
CN100513398C (zh) 2002-12-03 2009-07-15 Axys药物公司 作为因子viia抑制剂的2-(2-羟基联苯-3-基)-1h-苯并咪唑-5-甲脒衍生物
US7696225B2 (en) 2003-01-06 2010-04-13 Osi Pharmaceuticals, Inc. (2-carboxamido)(3-Amino) thiophene compounds
TWI299664B (en) 2003-01-06 2008-08-11 Osi Pharm Inc (2-carboxamido)(3-amino)thiophene compounds
US7122557B2 (en) 2003-03-18 2006-10-17 Bristol-Myers Squibb Company Sulfonyl-amidino-containing and tetrahydropyrimidino-containing compounds as factor Xa inhibitors
US7205318B2 (en) 2003-03-18 2007-04-17 Bristol-Myers Squibb Company Lactam-containing cyclic diamines and derivatives as a factor Xa inhibitors
EP1479680A1 (en) * 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH Azaindole derivatives as Factor Xa inhibitors
KR101204247B1 (ko) 2003-07-22 2012-11-22 아스텍스 테라퓨틱스 리미티드 3,4-이치환된 1ｈ-피라졸 화합물 및 그의 시클린 의존성키나제 (ｃｄｋ) 및 글리코겐 합성효소 키나제-3(ｇｓｋ-3) 조정제로서 용도
TW200524915A (en) * 2003-09-26 2005-08-01 Tanabe Seiyaku Co Carbamoyl-type benzofuran derivatives
TW200512181A (en) * 2003-09-26 2005-04-01 Tanabe Seiyaku Co Amide-type carboxamide derivatives
US7199149B2 (en) 2003-10-01 2007-04-03 Bristol Myers Squibb Company Monocyclic and bicyclic lactams as factor Xa inhibitors
US7507748B2 (en) * 2004-07-22 2009-03-24 Amgen Inc. Substituted aryl-amine derivatives and methods of use
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
AR054425A1 (es) 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
ES2323244T3 (es) * 2005-05-13 2009-07-09 Qosmos Analisis del trafico en redes de alta velocidad.
US8247556B2 (en) 2005-10-21 2012-08-21 Amgen Inc. Method for preparing 6-substituted-7-aza-indoles
WO2008057972A1 (en) 2006-11-02 2008-05-15 Millennium Pharmaceuticals, Inc. Methods of synthesizing pharmaceutical salts of a factor xa inhibitor
JP2010120852A (ja) * 2007-03-09 2010-06-03 Daiichi Sankyo Co Ltd 新規なジアミド誘導体
WO2008135524A2 (en) * 2007-05-02 2008-11-13 Boehringer Ingelheim International Gmbh Substituted anthranilamides and analogues, manufacturing and use thereof as medicaments
EP2170058B1 (en) * 2007-06-20 2013-07-03 Merck Sharp & Dohme Corp. Cetp inhibitors derived from benzoxazole arylamides
AU2008271127C1 (en) 2007-06-29 2014-04-17 Gilead Sciences, Inc. Purine derivatives and their use as modulators of Toll-like receptor 7
SG172060A1 (en) 2008-12-09 2011-07-28 Gilead Sciences Inc Modulators of toll-like receptors
KR101793300B1 (ko) 2009-10-22 2017-11-02 길리애드 사이언시즈, 인코포레이티드 특히 바이러스성 감염의 치료에 유용한 퓨린 또는 데아자퓨린의 유도체
WO2012014109A1 (en) 2010-07-30 2012-02-02 Ranbaxy Laboratories Limited Heterocyclic sulfonamides as inhibitors of transfer rna synthetase for use as antibacterial agents
EP3470407B1 (en) 2010-11-05 2024-01-24 Firmenich Incorporated Compounds useful as modulators of trpm8
US8883819B2 (en) 2011-09-01 2014-11-11 Irm Llc Bicyclic heterocycle derivatives for the treatment of pulmonary arterial hypertension
US9073921B2 (en) 2013-03-01 2015-07-07 Novartis Ag Salt forms of bicyclic heterocyclic derivatives
WO2015054662A1 (en) 2013-10-10 2015-04-16 Eastern Virginia Medical School 4-((2-hydroxy-3-methoxybenzyl)amino) benzenesulfonamide derivatives as 12-lipoxygenase inhibitors
SG11201700070QA (en) 2014-07-11 2017-02-27 Gilead Sciences Inc Modulators of toll-like receptors for the treatment of hiv
SI3194401T1 (sl) 2014-09-16 2020-12-31 Gilead Sciences, Inc. Trdne oblike modulatorja toličnega receptorja
BR112018006471B1 (pt) 2015-10-01 2024-02-27 Senomyx, Inc Composto, composição, método de modular o membro de melastina do canal potencial do receptor transitório 8 (trpm8), método de modular a sensação de resfrescância de uma composição e método de induzir uma sensação de refrescância em um ser humano ou animal
AU2019339777B2 (en) 2018-09-12 2022-09-01 Novartis Ag Antiviral pyridopyrazinedione compounds
KR20220070005A (ko) 2019-09-26 2022-05-27 노파르티스 아게 항바이러스성 피라졸로피리디논 화합물

Family Cites Families (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB824908A (en) 1958-06-03 1959-12-09 May & Baker Ltd Improvements in or relating to triazine derivatives
JPS5922697B2 (ja) 1976-01-13 1984-05-28 エーザイ株式会社 ビス−（メタ−アミジノフエノキシ）−化合物
DE69129611T2 (de) * 1990-08-20 1998-12-17 Eisai Co Ltd Sulfonamid-Derivate
EP0518818A3 (en) 1991-06-11 1993-04-28 Ciba-Geigy Ag Arylethers, their manufacture and use as medicament
US5451700A (en) 1991-06-11 1995-09-19 Ciba-Geigy Corporation Amidino compounds, their manufacture and methods of treatment
ZA928276B (en) * 1991-10-31 1993-05-06 Daiichi Seiyaku Co Aromatic amidine derivates and salts thereof.
CA2129339C (en) 1992-02-14 2002-09-10 George P. Vlasuk Inhibitors of thrombosis
DE4213919A1 (de) 1992-04-28 1993-11-04 Thomae Gmbh Dr K Cyclische iminoderivate, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel
AU675981B2 (en) 1992-12-02 1997-02-27 Bristol-Myers Squibb Company Guanidinyl-substituted heterocyclic thrombin inhibitors
WO1994013693A1 (en) 1992-12-15 1994-06-23 Corvas International, Inc. NOVEL INHIBITORS OF FACTOR Xa
US5332822A (en) 1992-12-24 1994-07-26 Bristol-Myers Squibb Company Heteroaromatic and thioheteroaromatic substituted sulfonamide thrombin inhibitors
EP0684830B1 (en) 1993-02-12 1999-06-16 Corvas International, Inc. Inhibitors of thrombosis
US5633381A (en) 1994-07-05 1997-05-27 Berlex Laboratories, Inc. (Z,Z), (Z,E) and (E,Z) isomers of substituted bis(phenylmethylene)cycloketones
IL115420A0 (en) 1994-09-26 1995-12-31 Zeneca Ltd Aminoheterocyclic derivatives
AU707323B2 (en) * 1995-03-10 1999-07-08 Berlex Laboratories, Inc. Benzamidine derivatives and their use as anti-coagulants
US5691364A (en) 1995-03-10 1997-11-25 Berlex Laboratories, Inc. Benzamidine derivatives and their use as anti-coagulants
US5612363A (en) 1995-06-02 1997-03-18 Berlex Laboratories, Inc. N,N-di(aryl) cyclic urea derivatives as anti-coagulants
US5721214A (en) 1995-06-07 1998-02-24 Cor Therapeutics, Inc. Inhibitors of factor Xa
US5849759A (en) 1995-12-08 1998-12-15 Berlex Laboratories, Inc. Naphthyl-substituted benzimidazole derivatives as anti-coagulants
US5994375A (en) * 1996-02-12 1999-11-30 Berlex Laboratories, Inc. Benzamidine derivatives substituted by amino acid and hydroxy acid derivatives and their use as anti-coagulants
US5753635A (en) 1996-08-16 1998-05-19 Berlex Laboratories, Inc. Purine derivatives and their use as anti-coagulants
US5693641A (en) 1996-08-16 1997-12-02 Berlex Laboratories Inc. Bicyclic pyrimidine derivatives and their use as anti-coagulants
SK29599A3 (en) 1996-09-12 1999-08-06 Schering Ag Benzamidine derivatives substituted by cyclic amino acid or cyclic hydroxy acid derivatives and their use as anti-coagulants
US6004985A (en) 1996-10-09 1999-12-21 Berlex Laboratories, Inc. Thio acid derived monocylic N-heterocyclics as anticoagulants
JP2002512633A (ja) * 1997-06-26 2002-04-23 イーライ・リリー・アンド・カンパニー 抗血栓剤
WO1999000128A1 (en) 1997-06-26 1999-01-07 Eli Lilly And Company Antithrombotic agents
EP1007037A4 (en) 1997-06-26 2004-10-06 Lilly Co Eli ANTITHROMBOTIC AGENTS
US6140351A (en) * 1997-12-19 2000-10-31 Berlex Laboratories, Inc. Ortho-anthranilamide derivatives as anti-coagulants
CA2358095A1 (en) 1998-12-23 2000-07-06 Eli Lilly And Company Heteroroaromatic amides as inhibitor of factor xa

Also Published As

Publication number Publication date
JP3811006B2 (ja) 2006-08-16
NZ503809A (en) 2002-04-26
PT1040108E (pt) 2004-06-30
HUP0101172A3 (en) 2002-12-28
JP2001526283A (ja) 2001-12-18
US6380221B1 (en) 2002-04-30
PL341044A1 (en) 2001-03-26
ES2215337T3 (es) 2004-10-01
RU2226529C2 (ru) 2004-04-10
WO1999032477A1 (en) 1999-07-01
NO20003111D0 (no) 2000-06-16
DE69821985D1 (de) 2004-04-01
CN1282329A (zh) 2001-01-31
CN1143855C (zh) 2004-03-31
WO1999032477B1 (en) 1999-09-10
NO20003111L (no) 2000-08-18
DK1040108T3 (da) 2004-05-24
IL135536A0 (en) 2001-05-20
CA2315070A1 (en) 1999-07-01
EP1040108A1 (en) 2000-10-04
US6498185B1 (en) 2002-12-24
ATE260103T1 (de) 2004-03-15
DE69821985T2 (de) 2005-05-04
SK9432000A3 (en) 2001-02-12
AU751856B2 (en) 2002-08-29
EP1040108B1 (en) 2004-02-25
AU1875999A (en) 1999-07-12

Similar Documents

Publication Publication Date Title
HUP0101172A1 (hu) Orto-antranilsavamid-származékok és antikoagulánsokként történő alkalmazásuk
HUP9802859A2 (hu) Acil-amino-szalicilsav-amid-származékok és alkalmazásuk peszticidként
DE69722027D1 (de) Kristalle von benzimidazolderivate und verfahren zu ihrer herstellung
HUP9700126A2 (hu) 2-Oxo- és 2-tio-1,2-dihidrokinolinil-oxazolidinon-származékok és ezeket tartalmazó gyógyszerkészítmények, eljárás előállításukra és intermedierjeik
TW326447B (en) Substituted 2-phenylpyridines, intermediates and process for their preparation and application thereof
HUP0001098A2 (hu) Xa faktort gátló hatású heterociklusos vegyületek
HUP0004529A2 (hu) VLA-4 által mediált leukocita adhéziót gátló szulfonilezett dipeptid-származékok, ezeket tartalmazó gyógyászati készítmények, valamint alkalmazásuk
HUP0202799A2 (hu) Herbicid hatású izoxazolinszármazékok és azt tartalmazó készítmény
HUP9900616A2 (hu) Triciklusos vegyületek, eljárás előállításukra, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
HUP0001192A2 (hu) Topiramát és származékainak alkalmazása elhízás kezelésére használható gyógyszerkészítmények előállítására
HUP0204399A2 (en) Pteridine compounds for the treatment of psoriasis, process for their preparation, pharmaceutical compositions containing them and their use
ATE282614T1 (de) Phenylharnstoff und phenylthioharnstoffderivate
HUP0002528A2 (hu) Xa faktort gátló hatású heterociklusos vegyületek
HUP0104452A2 (hu) Triciklusos vegyületeket tartalmazó gyógyászati kompozíció
HUP9903707A2 (hu) 17Béta-karboxi-,-tio-karboxi-vagy -amido-androsztánszármazékok laktonszármazékai, előállításuk, alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények
HUP9802937A2 (hu) Benzo[g]kinolin-származékok, e vegyületeket tartalmazó gyógyászati készítmények, eljárás előállításukra és alkalmazásuk
PE20020750A1 (es) Derivados de pirazol
DE3876813D1 (de) 3(2h)pyridazinon, verfahren zu dessen herstellung und dieses enthaltendes mittel gegen srs-a.
BR9801778A (hu)
HUP9904367A2 (hu) Benzamidinszármazékok és LTB4-antagonista hatású gyógyszerek hatóanyagaként való alkalmazásuk
HUP9904682A2 (hu) Fenil-oxazol- és -tiazol-származékok, alkalmazásuk és az ezeket tartalmazó gyógyszerkészítmények
KR940014384A (ko) 항바이러스제로서의 페녹시- 및 페녹시알킬-피페리딘
IE872588L (en) Compounds
FI894061A0 (fi) Menetelmä lääkeaineina käyttökelpoisten , -disubstituoitujen N-sykloalkyylialkyylibentsyyliamiinien valmistamiseksi ja niiden synteesivälituotteita
HUP0204354A2 (hu) Új heterociklusos vegyületek, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk