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AR069692A1 - Peptidilnitrilos y sus usos como inhibidores de la dipeptidil peptidasa - Google Patents

Peptidilnitrilos y sus usos como inhibidores de la dipeptidil peptidasa

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Publication number
AR069692A1
AR069692A1 ARP080105431A ARP080105431A AR069692A1 AR 069692 A1 AR069692 A1 AR 069692A1 AR P080105431 A ARP080105431 A AR P080105431A AR P080105431 A ARP080105431 A AR P080105431A AR 069692 A1 AR069692 A1 AR 069692A1
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AR
Argentina
Prior art keywords
alkyl
cycloalkyl
saturated
independently represent
attached form
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ARP080105431A
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English (en)
Inventor
Mark Furber
Christopher Andrew Luckhurst
Linda Anne Stein
Hitesh Jayantilal Sanganee
Peter Alan Cage
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Astrazeneca Ab
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Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR069692A1 publication Critical patent/AR069692A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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 two hetero rings
    • C07D417/12—Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—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
    • 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—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
    • 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—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
    • C07D409/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Otolaryngology (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)
  • Hydrogenated Pyridines (AREA)
  • Pyrrole Compounds (AREA)

Abstract

Un proceso para su preparacion, composiciones farmacéuticas que contienen a los mismos y su uso en el tratamiento del asma, enfermedad pulmonar obstructiva cronica o rinitis alérgica. Reivindicacion 1: Un compuesto caracterizado porque es de la formula (1) donde n representa de manera independiente 0, 1, 2, 3 o 4; X1 representa un grupo metileno; y representa 0, 1 o 2; cada R1 representa de manera independiente halogeno, hidroxilo, carboxilo, ciano, alquilo C1-6, alcoxi C1-6, trifluorometilo, NR6R7, C(O)NR6R7, NR6aC(O)R7a, SO2NR6R7, NR6aSO2R7a o S(O)mR8 y R1 se sustituye opcionalmente con hidroxi, halogeno o alcoxi C1-6; R2 representa un átomo de hidrogeno o un grupo alquilo C1-6 opcionalmente sustituido con por lo menos un sustituyente seleccionado entre halogeno, hidroxilo, carboxilo, ciano, trifluorometilo, alquilo C1-6, cicloalquilo C3-6, NR9R10, C(O)NR11R12, NR13C(O)R14, SO2NR15R16, NR17SO2R18 y S(O)pR19; R3 representa un átomo de hidrogeno o un grupo alquilo C1-6 opcionalmente sustituido con por lo menos un sustituyente seleccionado entre halogeno, hidroxilo, carboxilo, ciano, trifluorometilo, alquilo C1-6, cicloalquilo C3-6, NR20R21, C(O)NR22R23, NR24C(O)R25, SO2NR26R27, NR28SO2R29 y S(O)pR30; R4 representa un átomo de hidrogeno o un grupo alquilo C1-6 opcionalmente sustituido con por lo menos un sustituyente seleccionado entre halogeno, hidroxilo, carboxilo, ciano, trifluorometilo, alquilo C1-6, cicloalquilo C3-6, NR31R32, C(O)NR33R34, NR35C(O)R36, SO2NR37R38, NR39SO2R40 y S(O)rR41, R5 representa un átomo de hidrogeno o un grupo alquilo C1-6 opcionalmente sustituido con por lo menos un sustituyente seleccionado entre halogeno, hidroxilo, carboxilo, ciano, trifluorometilo, alquilo C1-6, cicloalquilo C3-6, NR42R43, C(O)NR44R45, NR46C(O)R47, SO2NR48R49, NR50SO2R51 y S(O)tR52, o R3 y R4 junto con los átomos de carbono a los cuales están unidos representan un anillo ciclopropilo, o R4 y R5 junto con el átomo de carbono al cual están unidos forman un anillo carbocíclico o heterocíclico saturado o insaturado, de 3 a 6 miembros cuyo anillo se puede sustituir opcionalmente con por lo menos un sustituyente seleccionado entre halogeno, hidroxilo, carboxilo y alquilo C1-6; A y B representan, cada uno de manera independiente, un sistema de anillos aromático de 5 a 10 miembros que comprende opcionalmente por lo menos un heteroátomo del anillo seleccionado entre nitrogeno, oxígeno y azufre, el sistema de anillos está sustituido opcionalmente con por lo menos un sustituyente seleccionado entre halogeno, carboxilo, hidroxilo, oxo, nitro, ciano, mercapto, cicloalquilo C3-6, alquenilo C2-6, trifluorometilo, alcoxi C1-6, alquilcarbonilo C1-6, alquilcarboniloxi C1-6, alcoxicarbonilo C1-6, -NR53R54, -C(O)NR55R56, NR57C(O)R58, SO2NR59R60, NR61SO2R62, S(O)vR63, heterocicliloxi de 4 a 7 miembros saturado, benciloxi, alquilpiperazinilo C1-6y un grupo alquilo C1-6 (el mismo sustituido opcionalmente con hidroxilo, NR64R65, fenilo o morfolinilo); m, p, q, r, t y v representan, cada uno de manera independiente, 0, 1 o 2; X2 representa una union, un átomo de oxígeno o azufre, SO, SO2, NR66, C(O)NR66, NR66C(O), SO2NR66, NR66SO2, alquilo C1-3, etenilo o etinilo; R6 y R7 representan, cada uno de manera independiente, hidrogeno, alquilo C1-6 o cicloalquilo C3-6, o R6 y R7 junto con el átomo de nitrogeno al cual están unidos forman un anillo heterocíclico saturado de 4 a 7 miembros; R9 y R10 representan, cada uno de manera independiente, hidrogeno, alquilo C1-6 o cicloalquilo C3-6, o R9 y R10 junto con el átomo de nitrogeno al cual están unidos forman un anillo heterocíclico saturado de 4 a 7 miembros; R11 y R12 representan, cada uno de manera independiente, hidrogeno, alquilo C1-6 o cicloalquilo C3-6, o R11 y R12 junto con el átomo de nitrogeno al cual están unidos forman un anillo heterocíclico saturado de 4 a 7 miembros; R15 y R16 representan, cada uno de manera independiente, hidrogeno, alquilo C1-6 o cicloalquilo C3-6, o R15 y R16 junto con el átomo de nitrogeno al cual están unidos forman un anillo heterocíclico saturado de 4 a 7 miembros; R20 y R21 representan, cada uno de manera independiente, hidrogeno, alquilo C1-6 o cicloalquilo C3-6, o R20 y R21 junto con el átomo de nitrogeno al cual están unidos forman un anillo heterocíclico saturado de 4 a 7 miembros; R22 y R23 representan, cada uno de manera independiente, hidrogeno, alquilo C1-6 o cicloalquilo C3-6, o R22 y R23 junto con el átomo de nitrogeno al cual están unidos forman un anillo heterocíclico saturado de 4 a 7 miembros; R26 y R27 representan, cada uno de manera independiente, hidrogeno, alquilo C1-6 o cicloalquilo C3-6, o R26 y R27 junto con el átomo de nitrogeno al cual están unidos forman un anillo heterocíclico saturado de 4 a 7 miembros; R31 y R32 representan, cada uno de manera independiente, hidrogeno, alquilo C1-6 o cicloalquilo C3-6, o R31 y R32 junto con el átomo de nitrogeno al cual están unidos forman un anillo heterocíclico saturado de 4 a 7 miembros; R33 y R34 representan, cada uno de manera independiente, hidrogeno, alquilo C1-6 o cicloalquilo C3-6, o R33 y R34 junto con el átomo de nitrogeno al cual están unidos forman un anillo heterocíclico saturado de 4 a 7 miembros; R37 y R38 representan, cada uno de manera independiente, hidrogeno, alquilo C1-6 o cicloalquilo C3-6, o R37 y R38 junto con el átomo de nitrogeno al cual están unidos forman un anillo heterocíclico saturado de 4 a 7 miembros; R42 y R43 representan, cada uno de manera independiente, hidrogeno, alquilo C1-6 o cicloalquilo C3-6, o R42 y R43 junto con el átomo de nitrogeno al cual están unidos forman un anillo heterocíclico saturado de 4 a 7 miembros; R44 y R45 representan, cada uno de manera independiente, hidrogeno, alquilo C1-6 o cicloalquilo C3-6, o R44 y R45 junto con el átomo de nitrogeno al cual están unidos forman un anillo heterocíclico saturado de 4 a 7 miembros; R48 y R49 representan, cada uno de manera independiente, hidrogeno, alquilo C1-6 o cicloalquilo C3-6, o R48 y R49 junto con el átomo de nitrogeno al cual están unidos forman un anillo heterocíclico saturado de 4 a 7 miembros; R53 y R54 representan, cada uno de manera independiente, hidrogeno, alquilo C1-6 o cicloalquilo C3-6, o R53 y R54 junto con el átomo de nitrogeno al cual están unidos forman un anillo heterocíclico saturado de 4 a 7 miembros; R55 y R56 representan, cada uno de manera independiente, hidrogeno, alquilo C1-6 o cicloalquilo C3-6, o R55 y R56 junto con el átomo de nitrogeno al cual están unidos forman un anillo heterocíclico saturado de 4 a 7 miembros; R59 y R60 representan, cada uno de manera independiente, hidrogeno, alquilo C1-6 o cicloalquilo C3-6, o R59 y R60 junto con el átomo de nitrogeno al cual están unidos forman un anillo heterocíclico saturado de 4 a 7 miembros; R64 y R65 representan, cada uno de manera independiente, hidrogeno, alquilo C1-6 o cicloalquilo C3-6, o R64 y R65 junto con el átomo de nitrogeno al cual están unidos forman un anillo heterocíclico saturado de 4 a 7 miembros; cada grupo R6a, R7a, R8, R13, R14, R17, R18, R19, R24, R25, R28, R29, R30, R35, R36, R39, R40, R41, R46, R47, R50, R51, R52, R57, R58, R61, R62 y R63 representa de manera independiente un átomo de hidrogeno o un grupo alquilo C1-6 o cicloalquilo C3-6; y R66 representa un átomo de hidrogeno o un grupo alquilo C1-6; o una sal aceptable para uso farmacéutico del mismo.
ARP080105431A 2007-12-12 2008-12-12 Peptidilnitrilos y sus usos como inhibidores de la dipeptidil peptidasa AR069692A1 (es)

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US (2) US7902181B2 (es)
EP (1) EP2231597A1 (es)
JP (1) JP2011506421A (es)
KR (1) KR20100098683A (es)
CN (1) CN101945851B (es)
AR (1) AR069692A1 (es)
AU (1) AU2008334444B2 (es)
BR (1) BRPI0820665A2 (es)
CA (1) CA2706679A1 (es)
CL (1) CL2008003694A1 (es)
CO (1) CO6280399A2 (es)
CR (1) CR11492A (es)
DO (1) DOP2010000178A (es)
EA (1) EA201000958A1 (es)
EC (1) ECSP10010245A (es)
IL (1) IL205873A0 (es)
MX (1) MX2010006110A (es)
PE (1) PE20091100A1 (es)
TW (1) TW200932725A (es)
UY (1) UY31524A1 (es)
WO (1) WO2009074829A1 (es)
ZA (1) ZA201004091B (es)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7737145B2 (en) 2005-12-29 2010-06-15 Estrellita Pharmaceuticals, Llc Diamine derivatives as inhibitors of leukotriene A4 hydrolase
BRPI0820665A2 (pt) * 2007-12-12 2018-05-29 Astrazeneca Ab compostos de peptidil nitrilas, processos para fabricação dos mesmos, composição farmacêutica, combinação e uso de ditos compostos
WO2010142985A1 (en) * 2009-06-10 2010-12-16 Astrazeneca Ab Substituted n-[1-cyano-2-(phenyl)ethyl]piperidin-2-ylcarboxmide compounds 761
US8633322B2 (en) 2009-10-29 2014-01-21 Janssen Pharmaceutica Nv Alkynyl derivatives useful as DPP-1 inhibitors
US8481547B2 (en) 2009-12-18 2013-07-09 Janssen Pharmaceutica Nv Substituted benzothiazole and benzoxazole derivatives useful as inhibitors of DPP-1
US8552032B2 (en) 2009-12-18 2013-10-08 Janssen Pharmaceutica Nv Bicyclic derivatives useful as inhibitors of DPP-1
US8686152B2 (en) 2010-03-10 2014-04-01 Janssen Pharmaceutica Nv 4,4-disubstituted piperidine derivatives useful as inhibitors of dipeptidyl peptidase-1 (DPP-1)
JP5764148B2 (ja) * 2010-03-10 2015-08-12 ヤンセン ファーマシューティカ エヌ．ベー． ジペプチジルペプチダーゼ−１（ｄｐｐ−１）の阻害剤として有用な４，４−二置換されたピペリジン誘導体
EP3159331A1 (en) 2010-05-05 2017-04-26 Infinity Pharmaceuticals, Inc. Tetrazolones as inhibitors of fatty acid synthase
WO2011154677A1 (en) 2010-06-09 2011-12-15 Astrazeneca Ab Substituted n-[1-cyano-2-(phenyl)ethyl] 1-aminocycloalk-1-ylcarboxamide compounds - 760
WO2012061926A1 (en) * 2010-11-08 2012-05-18 Zalicus Pharmaceuticals Ltd. Bisarylsulfone and dialkylarylsulfone compounds as calcium channel blockers
WO2012119941A1 (en) 2011-03-04 2012-09-13 Prozymex A/S Peptidyl nitrilcompounds as peptidase inhibitors
WO2012130299A1 (en) * 2011-03-30 2012-10-04 Prozymex A/S Peptidase inhibitors
US8999975B2 (en) * 2011-09-19 2015-04-07 Boehringer Ingelheim International Gmbh Substituted N- [1-cyano-2- (phenyl) ethyl] -2-azabicyclo [2.2.1] heptane-3-carboxamide inhibitors of cathepsin C
CA2905340C (en) 2013-03-12 2022-05-31 Celtaxsys, Inc. Low dose oral formulations of acebilustat
US8871783B2 (en) 2013-03-14 2014-10-28 Boehringer Ingelheim International Gmbh Substituted 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid (cyano-methyl)-amides inhibitors of cathepsin C
DK2970283T3 (da) * 2013-03-14 2021-01-25 Boehringer Ingelheim Int Substituerede 2-aza-bicyclo[2.2.1]heptan-3-carboxylsyre-(benzyl-cyano-methyl)-amider som inhibitorer af cathepsin-c
MX2015011677A (es) 2013-03-14 2016-07-08 Celtaxsys Inc Inhibidores de leucotrieno a4 hidrolasa.
JP6534650B2 (ja) 2013-03-14 2019-06-26 セルタクシス，インコーポレイテッド ロイコトリエンａ４加水分解酵素の阻害剤
EP2968265A4 (en) 2013-03-14 2016-12-28 Celtaxsys Inc INHIBITORS OF THE LEUKOTRIEN A4 HYDROLASE
EP2970230B1 (en) * 2013-03-14 2019-05-22 Boehringer Ingelheim International GmbH Substituted bicyclic 1-carboxylic-acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin c
US8877775B2 (en) 2013-03-14 2014-11-04 Boehringer Ingelheim International Gmbh Substituted 2-aza-bicyclo[2.2.2]octane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin C
SG11201601150WA (en) * 2013-09-09 2016-03-30 Prozymex As Peptidyl nitril compounds as dipeptidyl peptidase i inhibitors
NO2699580T3 (es) * 2014-01-24 2018-02-24
WO2016016242A1 (en) 2014-08-01 2016-02-04 Boehringer Ingelheim International Gmbh Substituted oxetanes and their use as inhibitors of cathepsin c
KR102510588B1 (ko) 2014-09-12 2023-03-17 베링거 인겔하임 인터내셔날 게엠베하 카텝신 c의 스피로사이클릭 억제제
PH12017501029B1 (en) 2014-12-24 2022-04-27 Lg Chemical Ltd Biaryl derivative as gpr120 agonist
DK3265452T3 (en) 2015-03-05 2020-06-08 Neuprozyme Therapeutics ApS Peptidyl nitril compounds as dipeptidyl peptidase i inhibitors
WO2016139355A1 (en) 2015-03-05 2016-09-09 Prozymex A/S N-substituted 3,3'-(biphenyl-4,4'-diyl)bis-2-aminopropanenitriles as dppi inhibitors
TWI691486B (zh) * 2016-01-29 2020-04-21 日商東麗股份有限公司 環狀胺衍生物及其醫藥用途
PL3758708T3 (pl) 2018-03-01 2025-03-31 Astrazeneca Ab Kompozycje farmaceutyczne zawierające (2s)-{(1s)-1-cyjano-2-[4-(3-metylo-2-okso-2,3-dihydro-1,3-benzoksazol-5-ilo)fenylo]etylo}-1,4-oksazepano-2-karboksyamid
WO2019232306A1 (en) 2018-05-31 2019-12-05 Celtaxsys, Inc. Method of reducing pulmonary exacerbations in respiratory disease patients
EP3823627A4 (en) 2018-07-17 2022-04-20 Insmed Incorporated CERTAIN (2S)-N-[(1S)-1-CYANO-2-PHENYLETHYL]-1,4-OXAZEPANE-2-CARBOXAMIDES FOR THE TREATMENT OF LUPUS ENEHROPATHY
EP4497473A3 (en) 2020-08-26 2025-04-23 Haisco Pharmaceuticals Pte. Ltd. Nitrile derivative that acts as inhibitor of dipeptidyl peptidase 1 and use thereof
CN114591315A (zh) * 2020-12-04 2022-06-07 瑞石生物医药有限公司 一种组织蛋白酶c小分子抑制剂
JP2023551488A (ja) 2020-12-04 2023-12-08 瑞石生物医薬有限公司 カテプシンｃの小分子阻害剤及びその医薬的使用
EP4289827A4 (en) * 2021-02-05 2025-01-22 Medshine Discovery Inc. CONDENSED RING DERIVATIVES CONTAINING 1,4-OXAZEPANE
CN115925696A (zh) * 2021-10-29 2023-04-07 瑞石生物医药有限公司 一种1-氰基-2-苯基乙基甲酰胺衍生物及其用途
JP2025506307A (ja) * 2022-02-22 2025-03-07 ハイスコ ファーマスーティカル プライベート リミテッド 含窒素複素環化合物の調製方法
JP2025508792A (ja) * 2022-02-22 2025-04-10 ハイスコ ファーマスーティカル プライベート リミテッド ジペプチジルペプチダーゼ阻害化合物の塩及び結晶形態
JP2025518345A (ja) 2022-06-07 2025-06-12 瑞石生物医薬有限公司 ベンゾ［ｃ］クロマン化合物の薬学的に許容される塩、ならびに薬学的に許容される塩の多形及び使用
WO2023236879A1 (zh) 2022-06-07 2023-12-14 瑞石生物医药有限公司 苯并[c]色满化合物的多晶型及其制备方法和用途
US20250250232A1 (en) * 2022-07-06 2025-08-07 Chiesi Farmaceutici S.P.A. Azetidine derivatives and use thereof as dipeptidyl peptidase 1 inhibitors
EP4561565A2 (en) * 2022-07-28 2025-06-04 Insmed Incorporated Novel dpp1 inhibitors and uses thereof
CN115785083A (zh) * 2022-12-27 2023-03-14 瑞石生物医药有限公司 一种组织蛋白酶c小分子抑制剂及其制备方法
EP4646265A1 (en) 2023-01-06 2025-11-12 Insmed Incorporated Novel, reversible dpp1 inhibitors and uses thereof

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CO5150173A1 (es) 1998-12-10 2002-04-29 Novartis Ag Compuestos n-(glicilo sustituido)-2-cianopirrolidinas inhibidores de peptidasa de dipeptidilo-iv (dpp-iv) los cuales son efectivos en el tratamiento de condiciones mediadas por la inhibicion de dpp-iv
DE60028045T2 (de) 1999-07-30 2007-02-15 Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield Neue bernsteinsäure derivative als cysteine-protease-inhibitoren
KR100468254B1 (ko) 1999-12-24 2005-01-27 에프. 호프만-라 로슈 아게 카텝신 ｋ 억제제로서의 니트릴 유도체
US7183290B2 (en) * 2001-06-27 2007-02-27 Smithkline Beecham Corporation Fluoropyrrolidines as dipeptidyl peptidase inhibitors
DE60222667T2 (de) * 2001-06-27 2008-07-17 Smithkline Beecham Corp. Fluorpyrrolidine als dipeptidylpeptidaseinhibitoren
EP1870402A1 (en) * 2002-04-30 2007-12-26 UCB Pharma, S.A. 2,6-quinolinyl and 2,6-naphthyl derivatives, processes for preparing them and their uses as VLA-4 inhibitors
JP2006527704A (ja) 2003-06-18 2006-12-07 プロザイメックス・アクティーゼルスカブ プロテアーゼ阻害剤
EP1720839A1 (en) * 2004-02-10 2006-11-15 Janssen Pharmaceutica N.V. Pyridazinones as antagonists of a4 integrins
US7504413B2 (en) * 2004-05-06 2009-03-17 Cytokinetics, Inc. N-(4-(imidazo[1,2A]pyridin-YL)phenethyl)benzamide inhibitors of the mitotic kinesin CENP-E for treating certain cellular proliferation diseases
BRPI0820665A2 (pt) * 2007-12-12 2018-05-29 Astrazeneca Ab compostos de peptidil nitrilas, processos para fabricação dos mesmos, composição farmacêutica, combinação e uso de ditos compostos

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