ATE304532T1 - Inhibitoren von serin proteasen - Google Patents

Inhibitoren von serin proteasen

Info

Publication number
ATE304532T1
ATE304532T1 AT01940716T AT01940716T ATE304532T1 AT E304532 T1 ATE304532 T1 AT E304532T1 AT 01940716 T AT01940716 T AT 01940716T AT 01940716 T AT01940716 T AT 01940716T AT E304532 T1 ATE304532 T1 AT E304532T1
Authority
AT
Austria
Prior art keywords
inhibitors
sub
serine proteases
factor
compounds
Prior art date
Application number
AT01940716T
Other languages
English (en)
Inventor
John Walter Liebeschuetz
Christopher William Murray
Stephen Clinton Young
Nicholas Paul Camp
Stuart Donald Jones
William Alexander Wylie
John Joseph Masters
Michael Robert Wiley
Scott Martin Sheehan
David Birenbaum Engel
Brian Morgan Watson
Original Assignee
Lilly Co Eli
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 PCT/GB2000/002302 external-priority patent/WO2000076971A2/en
Application filed by Lilly Co Eli filed Critical Lilly Co Eli
Application granted granted Critical
Publication of ATE304532T1 publication Critical patent/ATE304532T1/de

Links

Classifications

    • 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
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D207/12Oxygen or sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D211/40Oxygen atoms
    • C07D211/44Oxygen atoms attached in position 4
    • C07D211/46Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D211/56Nitrogen atoms
    • C07D211/58Nitrogen atoms attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D211/60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • 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
    • C07D401/06Heterocyclic 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 linked by a carbon chain containing only aliphatic 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
    • C07D401/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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
    • 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
    • C07D417/14Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
AT01940716T 2000-06-13 2001-06-12 Inhibitoren von serin proteasen ATE304532T1 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PCT/GB2000/002302 WO2000076971A2 (en) 1999-06-14 2000-06-13 Serine protease inhibitors
GBGB0030305.7A GB0030305D0 (en) 2000-12-13 2000-12-13 Compounds
PCT/GB2001/002551 WO2001096303A1 (en) 2000-06-13 2001-06-12 Serine protease inhibitors

Publications (1)

Publication Number Publication Date
ATE304532T1 true ATE304532T1 (de) 2005-09-15

Family

ID=9904938

Family Applications (1)

Application Number Title Priority Date Filing Date
AT01940716T ATE304532T1 (de) 2000-06-13 2001-06-12 Inhibitoren von serin proteasen

Country Status (8)

Country Link
US (2) US7053078B2 (de)
EP (1) EP1289954B1 (de)
AT (1) ATE304532T1 (de)
AU (1) AU2001274220A1 (de)
DE (1) DE60113412T2 (de)
ES (1) ES2248341T3 (de)
GB (1) GB0030305D0 (de)
WO (1) WO2001096303A1 (de)

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EP1409479B1 (de) 2001-07-26 2008-01-23 Eli Lilly And Company 1-glycinyl-4-(1-methylpiperidin-4-yl)piperazine und -piperidine als faktor-xa-antagonisten
MY130373A (en) * 2001-10-29 2007-06-29 Malesci Sas Linear basic compounds having nk-2 antagonist activity and formulations thereof
AU2002366563A1 (en) * 2001-12-12 2003-06-23 Eli Lilly And Company Certain glycine derivatives as factor xa inhibitors for use in the treatment of thrombotic disorders
EP2161254B1 (de) 2002-03-05 2014-08-13 Sumitomo Chemical Company, Limited Zwischenprodukt zur Herstellung Biarylverbindungen
CN1288135C (zh) 2002-04-01 2006-12-06 伊莱利利公司 某些作为丝氨酸蛋白酶xa因子抑制剂的1-(d-环丙基甘氨酰基)-4-(哌啶-4-基)哌嗪化合物
PE20040804A1 (es) 2002-12-19 2004-12-31 Boehringer Ingelheim Pharma DERIVADOS DE CARBOXAMIDAS COMO INHIBIDORES DEL FACTOR Xa
WO2004060872A1 (en) 2002-12-30 2004-07-22 Eli Lilly And Company Factor xa inhibitors
US7157471B2 (en) * 2003-08-25 2007-01-02 Boehringer Ingelheim International Gmbh Haloalkyl- and piperidine-substituted benzimidazole-derivatives
US7371743B2 (en) 2004-02-28 2008-05-13 Boehringer Ingelheim International Gmbh Carboxylic acid amides, the preparation thereof and their use as medicaments
KR20070012552A (ko) 2004-05-13 2007-01-25 베링거 인겔하임 인터내셔날 게엠베하 신규한 치환된 티오펜카복스아미드, 이의 제조방법 및약제로서의 이의 용도
WO2005111013A1 (de) * 2004-05-13 2005-11-24 Boehringer Ingelheim International Gmbh Substituierte thiophen-2-carbonsäureamide, deren herstellung und deren verwendung als arzneimittel
DE102004047840A1 (de) * 2004-09-29 2006-03-30 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue substituierte Thiophencarbonsäureamide, deren Herstellung und deren Verwendung als Arzneimittel
US20060079522A1 (en) * 2004-10-08 2006-04-13 Marzabadi Mohammad R Amino substituted aryloxybenzylpiperidine derivatives
EP1724269A1 (de) * 2005-05-20 2006-11-22 Sanofi-Aventis Deutschland GmbH Heteroarylcarbonsäure-sulfamoylalkylamidderivate als Faktor Xa-Inhibitoren
US20090012010A1 (en) * 2007-05-18 2009-01-08 Neuromed Phramaceuticals Ltd. Amino acid derivatives as calcium channel blockers
CA2722923C (en) 2008-04-29 2016-08-02 Boehringer Ingelheim International Gmbh Indazole compounds as ccr1 receptor antagonists
JP5411927B2 (ja) * 2008-05-06 2014-02-12 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ccr1アンタゴニストとしてのピラゾール化合物
EP2346868B1 (de) * 2008-09-26 2016-01-27 Boehringer Ingelheim International Gmbh Azaindazolverbindungen als ccr1-rezeptorantagonisten
EP2491028B1 (de) 2009-10-21 2013-12-11 Boehringer Ingelheim International GmbH Indazol- und pyrazolopyridin- verbindungen als ccr1 rezeptor antagonisten
EP2493875B1 (de) 2009-10-27 2014-08-06 Boehringer Ingelheim International GmbH Iheterozyklische verbindungen als ccr1-rezeptorantagonisten
CA2782384A1 (en) * 2009-12-08 2011-06-16 Boehringer Ingelheim International Gmbh Process for synthesis of intermediates useful for making substituted indazole and azaindazole compounds
WO2011137109A1 (en) 2010-04-30 2011-11-03 Boehringer Ingelheim International Gmbh Azaindazole amide compounds as ccr1 receptor antagonists
EP2655371B1 (de) 2010-12-23 2015-02-25 Boehringer Ingelheim International GmbH Pyrazolopiperidinverbindungen als ccr1-rezeptorantagonisten
EP3506983B1 (de) * 2016-09-01 2021-08-25 Mebias Discovery, Inc. Substituierte harnstoff-derivate zur behandlung von schmerz
AU2018211057B2 (en) 2017-01-17 2021-12-23 Mebias Discovery, Inc. Substituted 3-dialkylaminomethyl-piperidin-4-yl-benzamides and methods of making and using same
WO2021032933A1 (en) * 2019-08-21 2021-02-25 Kalvista Pharmaceuticals Limited Enzyme inhibitors
CN112409199B (zh) * 2020-11-26 2022-07-12 山东普洛汉兴医药有限公司 一种氨基酸甲酯连续化生产工艺及装置

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IE902295A1 (en) 1989-07-07 1991-01-16 Abbott Lab Amino acid analog cck antagonists
CA2200163A1 (en) 1996-03-22 1997-09-22 Michael Robert Wiley Antithrombotic diamides
CA2258915A1 (en) 1996-06-25 1997-12-31 Michael Robert Wiley Anticoagulant agents
IL123986A (en) 1997-04-24 2011-10-31 Organon Nv Medicinal compounds
US6372759B1 (en) 1997-06-26 2002-04-16 Eli Lilly And Company Antithrombotic agents
IL133627A0 (en) 1997-06-26 2001-04-30 Lilly Co Eli Antithrombotic agents
EP1014962A4 (de) 1997-06-26 2007-06-27 Lilly Co Eli Antitrombotische mitteln
IL133625A0 (en) 1997-06-26 2001-04-30 Lilly Co Eli Antithrombotic agents
WO1999011658A1 (en) * 1997-08-29 1999-03-11 Proteus Molecular Design Ltd. Meta-benzamidine derivatives as serin protease inhibitors
IL135488A0 (en) * 1997-11-18 2001-05-20 Teijin Ltd Cyclic amine derivatives
ATE272633T1 (de) 1998-12-23 2004-08-15 Lilly Co Eli Aromatische amiden
AU2054700A (en) 1998-12-23 2000-07-31 Eli Lilly And Company Antithrombotic amides
EP1140905B1 (de) 1998-12-23 2003-05-14 Eli Lilly And Company Heteroaromatische amide als inhibitoren von faktor xa
EP1140839B1 (de) 1998-12-24 2004-03-17 Eli Lilly And Company Heterocyclische amide als inhibitoren von faktor xa
JP2003500382A (ja) 1999-05-24 2003-01-07 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 Xa因子の阻害剤
EP1185509A2 (de) 1999-05-24 2002-03-13 Cor Therapeutics, Inc. Inhibitoren von faktor xa
DE60022508T2 (de) 1999-06-14 2006-06-08 Eli Lilly And Co., Indianapolis Inhibitoren von serin proteasen
EP1192135A2 (de) * 1999-06-14 2002-04-03 Eli Lilly And Company Inhibitoren von serin proteasen

Also Published As

Publication number Publication date
US20040259868A1 (en) 2004-12-23
WO2001096303A1 (en) 2001-12-20
ES2248341T3 (es) 2006-03-16
US20030109706A1 (en) 2003-06-12
GB0030305D0 (en) 2001-01-24
DE60113412D1 (de) 2005-10-20
US6900196B2 (en) 2005-05-31
DE60113412T2 (de) 2006-06-29
US7053078B2 (en) 2006-05-30
EP1289954A1 (de) 2003-03-12
AU2001274220A1 (en) 2001-12-24
EP1289954B1 (de) 2005-09-14

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