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
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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
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Novartis Ag
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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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    • 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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    • A61K31/40—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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    • A61K31/40—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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    • A61K31/435—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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    • A61K31/44—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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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
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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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    • 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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    • C07D405/02—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
    • 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)
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • 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

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)

Publication Number Publication Date
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)
MY (1) MY183252A (es)
NZ (1) NZ581438A (es)
PE (1) PE20090484A1 (es)
SG (1) SG182961A1 (es)
TN (1) TN2009000520A1 (es)
TW (1) TWI411433B (es)
UA (1) UA98647C2 (es)
WO (1) WO2009000878A1 (es)
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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
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
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
MX2021000908A (es) 2018-07-23 2021-06-08 Trevi Therapeutics Inc Tratamiento de la tos cronica, la dificultad respiratoria y la disnea.
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ZA200908159B (en) 2010-12-29
IL202284A0 (en) 2010-06-16
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TN2009000520A1 (en) 2011-03-31
CO6251242A2 (es) 2011-02-21
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PE20090484A1 (es) 2009-05-27
EP2170939A1 (en) 2010-04-07
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MA31454B1 (fr) 2010-06-01
MY183252A (en) 2021-02-18
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AU2008267167C1 (en) 2012-11-01
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AU2008267167B2 (en) 2011-10-27
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