ATE355101T1 - Inhibitoren von serin proteasen - Google Patents

Inhibitoren von serin proteasen

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Publication number
ATE355101T1
ATE355101T1 AT01270360T AT01270360T ATE355101T1 AT E355101 T1 ATE355101 T1 AT E355101T1 AT 01270360 T AT01270360 T AT 01270360T AT 01270360 T AT01270360 T AT 01270360T AT E355101 T1 ATE355101 T1 AT E355101T1
Authority
AT
Austria
Prior art keywords
inhibitors
serine proteases
sub
compounds
formula
Prior art date
Application number
AT01270360T
Other languages
English (en)
Inventor
Sarah Elizabeth Lively
Martin James Harrison
Neil Jason Naylor
Christopher Neil Farthing
Bohdan Waszkowycz
Original Assignee
Tularik Ltd
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/GB2000/004764 external-priority patent/WO2001044226A1/en
Application filed by Tularik Ltd filed Critical Tularik Ltd
Application granted granted Critical
Publication of ATE355101T1 publication Critical patent/ATE355101T1/de

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    • C07D273/00—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic rings
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • C07C237/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
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    • C07D211/40—Oxygen atoms
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    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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    • 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
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    • C07D333/78—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
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    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
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    • C07D409/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
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US7074934B2 (en) * 2000-06-13 2006-07-11 Tularik Limited Serine protease inhibitors
US7138529B2 (en) * 2003-04-16 2006-11-21 Hoffmann-La Roche Inc. Substituted 3-cyanothiophene acetamides as glucagon receptor antagonists
US20050085531A1 (en) * 2003-10-03 2005-04-21 Hodge Carl N. Thiophene-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions, and uses thereof
DE102004006808A1 (de) * 2004-02-11 2005-09-01 Grünenthal GmbH Substituierte 4,5,6,7-Tetrahydro-benzothiazol-2-ylamin-Verbindungen
PL1753512T3 (pl) 2004-05-28 2009-03-31 4Sc Ag Tetrahydropirydotiofeny
WO2005120642A2 (en) 2004-06-11 2005-12-22 Altana Pharma Ag Tetrahydropyridothiophenes for treating hyperproliferative disorders
JP2008510726A (ja) * 2004-08-20 2008-04-10 エントレメッド インコーポレイテッド プロテイナーゼ活性化受容体アンタゴニストを含む組成物および方法
CA2596202A1 (en) 2005-02-09 2006-08-17 Altana Pharma Ag Tetrahydropyridothiophenes for the treatment of proliferative diseases such as cancer
US7741488B2 (en) 2005-02-11 2010-06-22 4Sc Ag Tetrahydropyridothiophenes as antiproliferative agents for the treatment of cancer
US7714136B2 (en) 2005-05-25 2010-05-11 4Sc Ag Tetrahydropyridothiophenes
US7763728B2 (en) 2005-05-25 2010-07-27 4Sc Ag Tetrahydropyridothiophenes
CN101421265A (zh) * 2006-01-18 2009-04-29 安姆根有限公司 作为蛋白激酶b(pkb)抑制剂的噻唑化合物
AU2008276521B2 (en) 2007-07-17 2011-11-03 Amgen Inc. Heterocyclic modulators of PKB
WO2009011871A2 (en) * 2007-07-17 2009-01-22 Amgen Inc. Thiadiazole modulators of pkb
AR075899A1 (es) * 2009-03-20 2011-05-04 Onyx Therapeutics Inc Tripeptidos epoxicetonas cristalinos inhibidores de proteasa
MY162557A (en) 2010-02-26 2017-06-15 Oral Health Australia Pty Ltd Treatment or prevention of infection
CN103408541B (zh) * 2013-07-16 2015-04-01 浙江医药高等专科学校 吲哚取代的噻唑并环己烷类化合物、及其抗肿瘤用途
CN103435573B (zh) * 2013-07-16 2015-04-01 浙江医药高等专科学校 苄基取代的噻唑并环己烷类化合物、其制备方法和用途
JP6425724B2 (ja) 2013-08-08 2018-11-21 ガラパゴス・ナムローゼ・フェンノートシャップＧａｌａｐａｇｏｓ Ｎ．Ｖ． Ｃｆｔｒモジュレーターとしてのチエノ［２，３−ｃ］ピラン
EA202190046A1 (ru) 2018-06-19 2021-03-24 Новартис Аг N-замещенные производные тетрагидротиенопиридина и их применение
AU2019291111B9 (en) * 2018-06-21 2023-08-24 UCB Biopharma SRL Thiophene derivatives for the treatment of disorders caused by IgE
CA3120388A1 (en) * 2018-11-19 2020-05-28 11949098 Canada Inc. Modulators of rar related orphan receptors (rors)

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WO2000077027A2 (en) 1999-06-14 2000-12-21 Tularik Limited Serine protease inhibitors
US6262069B1 (en) 1997-08-29 2001-07-17 Protherics Molecular Design Limited 1-amino-7-isoquinoline derivatives as serine protease inhibitors
EP1073624A1 (de) * 1998-04-24 2001-02-07 Proteus Molecular Design Limited Aminomethylbenzoesäureesterderivate als tryptase inhibitore
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US6855715B1 (en) 1999-06-14 2005-02-15 Eli Lilly And Company Serine protease inhibitors
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AU2002222207B2 (en) 2006-09-21
MXPA03005254A (es) 2004-10-14
US7067516B2 (en) 2006-06-27
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BR0116166A (pt) 2003-12-23
AU2220702A (en) 2002-06-24
GB0114185D0 (en) 2001-08-01
CA2436935A1 (en) 2002-06-20
US20040116439A1 (en) 2004-06-17
EP1343561B1 (de) 2007-02-28
DE60126978D1 (de) 2007-04-12
DE60126978T2 (de) 2007-10-31
CA2436935C (en) 2011-05-10
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