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
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • A61K31/33—Heterocyclic compounds
    • 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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    • A61K31/40—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
    • A61K31/4025—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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  • 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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Pyrrole Compounds (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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CN101977626A (zh) * 2008-01-21 2011-02-16 德莫迪斯公司 丝氨酸蛋白酶抑制剂在治疗皮肤病中的用途
WO2013055984A1 (en) 2011-10-14 2013-04-18 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
CN107922428B (zh) * 2015-06-25 2021-02-05 普洛麦格公司 噻吩并吡咯化合物及其作为刺虾源性荧光素酶的抑制剂的用途
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
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
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