CU23944B1 - Amidas del ácido pirrolidin-1,2-dicarboxílico sustituidas como moduladores de calicreína 7 - Google Patents

Amidas del ácido pirrolidin-1,2-dicarboxílico sustituidas como moduladores de calicreína 7

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Publication number
CU23944B1
CU23944B1 CU2009000229A CU20090229A CU23944B1 CU 23944 B1 CU23944 B1 CU 23944B1 CU 2009000229 A CU2009000229 A CU 2009000229A CU 20090229 A CU20090229 A CU 20090229A CU 23944 B1 CU23944 B1 CU 23944B1
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CU
Cuba
Prior art keywords
calicrein
pirrolidin
amidas
modulators
acid replaced
Prior art date
Application number
CU2009000229A
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English (en)
Other versions
CU20090229A7 (es
Inventor
Frederic Berst
Ursula Bodendorf
Claus Ehrhardt
Stefanie Flohr
Bernd Gerhartz
Ulrich Hassiepen
Andreas Marzinzik
Josef Gottfried Meingassner
Nils Ostermann
Stefan Andreas Randl
Original Assignee
Novartis Ag
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Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of CU20090229A7 publication Critical patent/CU20090229A7/es
Publication of CU23944B1 publication Critical patent/CU23944B1/es

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/04—Heterocyclic 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
    • C07D207/10—Heterocyclic 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
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/401—Proline; Derivatives thereof, e.g. captopril
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    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
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    • C07D211/36—Heterocyclic 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
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    • C07D405/12—Heterocyclic 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
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    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14—Hydrolases (3)
    • C12N9/48—Hydrolases (3) acting on peptide bonds (3.4)
    • C12N9/50—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
    • C12N9/64—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
    • C12N9/6421—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
    • C12N9/6424—Serine endopeptidases (3.4.21)
    • C12N9/6445—Kallikreins (3.4.21.34; 3.4.21.35)
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    • C12Y—ENZYMES
    • C12Y304/00—Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
    • C12Y304/21—Serine endopeptidases (3.4.21)
    • C12Y304/21034—Plasma kallikrein (3.4.21.34)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2299/00—Coordinates from 3D structures of peptides, e.g. proteins or enzymes

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  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Genetics & Genomics (AREA)
  • Dermatology (AREA)
  • General Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Toxicology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Peptides Or Proteins (AREA)
  • Pyrrole Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

La presente invención se refiere a la estructura de cristal de la proteasa de serina calicreína 7, y al uso de esta estructura de cristal en el descubrimiento de fármacos. La presente invención también se refiere a compuestos que se enlazan específicamente a este sitio activo de la calcreína 7.
CU2009000229A 2007-06-28 2009-12-24 Amidas del ácido pirrolidin-1,2-dicarboxílico sustituidas como moduladores de calicreína 7 CU23944B1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP07111316 2007-06-28
EP07115197 2007-08-29

Publications (2)

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CU20090229A7 CU20090229A7 (es) 2012-02-15
CU23944B1 true CU23944B1 (es) 2013-10-29

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US (2) US8309596B2 (es)
EP (1) EP2170939A1 (es)
JP (2) JP2010532162A (es)
KR (1) KR20100027159A (es)
CN (1) CN101687913B (es)
AR (1) AR067336A1 (es)
AU (1) AU2008267167C1 (es)
BR (1) BRPI0813230A2 (es)
CA (1) CA2691849A1 (es)
CL (1) CL2008001906A1 (es)
CO (1) CO6251242A2 (es)
CR (1) CR11134A (es)
CU (1) CU23944B1 (es)
EA (1) EA018050B1 (es)
EC (1) ECSP099829A (es)
GT (1) GT200900326A (es)
HN (1) HN2009003484A (es)
IL (1) IL202284A0 (es)
MA (1) MA31454B1 (es)
MX (1) MX2009013952A (es)
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NZ (1) NZ581438A (es)
PE (1) PE20090484A1 (es)
SG (1) SG182961A1 (es)
TN (1) TN2009000520A1 (es)
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UA (1) UA98647C2 (es)
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Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20110130338A1 (en) * 2008-01-21 2011-06-02 Dermadis Sa Use of serine protease inhibitors in the treatment of skin diseases
EP2899183B1 (en) 2011-10-14 2018-09-19 Bristol-Myers Squibb Company Substituted Tetrahydroisoquinoline Compounds as Factor Xia Inhibitors
US20140179727A1 (en) 2012-12-14 2014-06-26 Trevi Therapeutics, Inc. Methods for treating pruritus
US8987289B2 (en) * 2012-12-14 2015-03-24 Trevi Therapeutics, Inc. Methods for treating pruritus
EP3097084B1 (en) 2014-01-23 2020-09-30 Sixera Pharma AB New kallikrein 7 inhibitors
US10513694B2 (en) 2015-06-25 2019-12-24 Promega Corporation Thienopyrrole compounds and uses thereof
CN105218545A (zh) * 2015-11-04 2016-01-06 衡阳师范学院 激肽释放酶7小分子抑制剂及其制备方法、用途
CN105330665B (zh) * 2015-11-04 2017-10-03 衡阳师范学院 一种抑制激肽释放酶klk7的化合物、制备方法和用途
CN106518868B (zh) * 2015-11-04 2018-02-23 衡阳师范学院 激肽释放酶7小分子抑制剂及其制备方法、用途
CN106243058B (zh) * 2016-07-28 2018-06-29 三峡大学 一种化合物在制备抑制激肽释放酶klk7的药物上的应用及其合成方法
US20200040103A1 (en) 2018-03-14 2020-02-06 Genentech, Inc. Anti-klk5 antibodies and methods of use
CN108421034A (zh) * 2018-04-24 2018-08-21 济南磐升生物技术有限公司 激肽释放酶7在皮肤创伤愈合中的应用
IL318587A (en) 2018-07-23 2025-03-01 Trevi Therapeutics Inc Treatment of chronic cough, shortness of breath and wheezing
CN110256417A (zh) * 2019-07-05 2019-09-20 衡阳师范学院 一种激肽释放酶klk7抑制物、制备方法和用途
US12312414B2 (en) 2019-09-18 2025-05-27 Genentech, Inc. Anti-KLK7 antibodies, anti-KLK5 antibodies, multispecific anti-KLK5/KLK7 antibodies, and methods of use
CA3166928A1 (en) 2020-01-10 2021-07-15 Trevi Therapeutics, Inc. Methods of administering nalbuphine

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3905870A (en) * 1972-11-03 1975-09-16 Bayer Ag Purification of kallikrein
DE3843226A1 (de) 1988-12-22 1990-06-28 Boehringer Ingelheim Kg Chromatographieplatten und verfahren zur duennschicht-chromatographischen trennung von enantiomeren
AU4296897A (en) * 1996-07-24 1998-02-10 Novartis Ag Complex crystal form
JPH11292840A (ja) * 1998-04-06 1999-10-26 Soyaku Gijutsu Kenkyusho:Kk ノルスタチン誘導体又はその塩
KR100468254B1 (ko) * 1999-12-24 2005-01-27 에프. 호프만-라 로슈 아게 카텝신 ｋ 억제제로서의 니트릴 유도체
AU2001273040A1 (en) 2000-06-27 2002-01-08 Du Pont Pharmaceuticals Company Factor xa inhibitors
DE10110750A1 (de) 2001-03-07 2002-09-12 Bayer Ag Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften
GB0115515D0 (en) * 2001-06-25 2001-08-15 Ferring Bv Oxytocin agonisys
JP2003185650A (ja) * 2001-12-18 2003-07-03 National Institute Of Advanced Industrial & Technology 薬剤のスクリーニング方法
JP2005519915A (ja) 2002-01-18 2005-07-07 セレテック・リミテッド・ライアビリティ・カンパニー Ｅｄｇ受容体に関連する症状の処置方法
AU2002953533A0 (en) 2002-12-24 2003-01-16 Arthron Limited Fc receptor modulating compounds and compositions
US7129264B2 (en) * 2003-04-16 2006-10-31 Bristol-Myers Squibb Company Biarylmethyl indolines and indoles as antithromboembolic agents
KR20060023154A (ko) * 2003-06-18 2006-03-13 메르크 파텐트 게엠베하 혈전증 치료용 응고 인자 ｘａ 및 ｖｉｉａ의 저해제로서의피롤리딘-１,２-디카르복실산-１-[(４-에티닐-페닐)-아미드]-２-[(페닐)-아미드] 유도체
DE10358814A1 (de) * 2003-12-16 2005-07-21 Merck Patent Gmbh Prolinylarylacetamide
WO2005075667A1 (en) 2004-02-03 2005-08-18 Bayer Healthcare Ag Diagnostics and therapeutics for diseases associated with kallikrein 7 (klk7)
DE102004014945A1 (de) * 2004-03-26 2005-10-13 Merck Patent Gmbh Prolinylderivate
PL1781639T3 (pl) 2004-07-28 2012-07-31 Janssen Pharmaceutica Nv Podstawione pochodne indolilo-alkiloaminowe jako nowe inhibitory deacetylazy histonowej

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