[go: up one dir, main page]

PE20080708A1 - Compuestos 2-pirrolidincarboxamida sustituidos como inhibidores de la proteasa que activa el canal respiratorio - Google Patents

Compuestos 2-pirrolidincarboxamida sustituidos como inhibidores de la proteasa que activa el canal respiratorio

Info

Publication number
PE20080708A1
PE20080708A1 PE2007000642A PE2007000642A PE20080708A1 PE 20080708 A1 PE20080708 A1 PE 20080708A1 PE 2007000642 A PE2007000642 A PE 2007000642A PE 2007000642 A PE2007000642 A PE 2007000642A PE 20080708 A1 PE20080708 A1 PE 20080708A1
Authority
PE
Peru
Prior art keywords
pyrrolidinecarboxamide
protease
activates
alkyl
inhibitors
Prior art date
Application number
PE2007000642A
Other languages
English (en)
Inventor
David C Tully
Arnab K Chatterjee
Agnes Vidal
Hank Michael James Petrassi
Zhiwei Wang
Badry Bursulaya
Glen Spraggon
Original Assignee
Irm Llc
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
Application filed by Irm Llc filed Critical Irm Llc
Publication of PE20080708A1 publication Critical patent/PE20080708A1/es

Links

Classifications

    • 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
    • C07D207/08—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 hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • 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
    • C07D417/14—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 three or more hetero rings
    • A—HUMAN NECESSITIES
    • 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
    • A61K31/42—Oxazoles
    • A61K31/423—Oxazoles condensed with carbocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P11/06—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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0827—Tripeptides containing heteroatoms different from O, S, or N

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

SE REFIERE A COMPUESTOS DE 2-PIRROLIDINCARBOXAMIDA SUSTITUIDOS DE FORMULA (I), EN DONDE J ES CARBOCICLO MONOCICLICO O FUSIONADO DE 5 A 12 MIEMBROS, ARILO, HETEROARILO, HETEROCICLICO QUE COTIENE N, O Y/O S; R1 ES -(CH2)l-NHR2, -(CR2)l-NRC(=NR)-NR2, ENTRE OTROS; W-R2 ESTA EN CUALQUIER POSICION DEL ANILLO A; W ES -O(CR2)k-, -S(CR2)k-, -S(O)1-2(CR2)k-, ENTRE OTROS; R2 ES ALQUILO(C1-C6), ALQUENILO(C2-C6), R8, ENTRE OTROS; Y ES SO2R3, -(CO)-O-R3, ENTRE OTROS; R4 ES H, ALQUILO(C1-C6), R8, NR6R7, ENTRE OTROS; R5 ES HALO, ALQUILO(C1-C6), ALCOXI(C1-C6), ENTRE OTROS; X Y R8 SON INDEPENDIENTEMENTE UN CARBOCICLO, HETEROCICLICO, ARILO, HETEROARILO, ENTRE OTROS; i ES 0 A1; k, l y m SON INDEPENDIENTEMENTE DE 0 A 6; n ES 1- 6; p ES 0 A 3. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA Y UN PROCEDIMIENTO DE PREPARACION. ESTOS COMPUESTOS MODULAN LA ACTIVIDAD DE LA PROTEASA (PRSS2, TMPRSS11, TMPRSS2, TMPRSS3, CAP2, ENTRE OTRAS) QUE ACTIVA EL CANAL RESPIRATORIO Y SON UTILES EN EL TRATAMIENTO DE FIBROSIS CISTICA, BRONQUITIS CRONICA, ASMA, CARCINOMA PULMONAR Y RELACIONADAS
PE2007000642A 2006-05-23 2007-05-23 Compuestos 2-pirrolidincarboxamida sustituidos como inhibidores de la proteasa que activa el canal respiratorio PE20080708A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US80298306P 2006-05-23 2006-05-23
US86060406P 2006-11-22 2006-11-22

Publications (1)

Publication Number Publication Date
PE20080708A1 true PE20080708A1 (es) 2008-07-30

Family

ID=38565503

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2007000642A PE20080708A1 (es) 2006-05-23 2007-05-23 Compuestos 2-pirrolidincarboxamida sustituidos como inhibidores de la proteasa que activa el canal respiratorio

Country Status (14)

Country Link
US (2) US7951823B2 (es)
EP (1) EP2027143A2 (es)
JP (1) JP2009538327A (es)
KR (1) KR101069051B1 (es)
AR (1) AR061109A1 (es)
AU (1) AU2007253819B2 (es)
BR (1) BRPI0712021A2 (es)
CA (1) CA2651762A1 (es)
CL (1) CL2007001481A1 (es)
MX (1) MX2008014839A (es)
PE (1) PE20080708A1 (es)
RU (1) RU2419626C2 (es)
TW (1) TW200813094A (es)
WO (1) WO2007137080A2 (es)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0507577D0 (en) * 2005-04-14 2005-05-18 Novartis Ag Organic compounds
JP2009538327A (ja) * 2006-05-23 2009-11-05 アイアールエム・リミテッド・ライアビリティ・カンパニー チャネル活性化プロテアーゼ阻害剤である化合物および組成物
KR101069089B1 (ko) * 2006-05-23 2011-09-30 아이알엠 엘엘씨 채널 활성화 프로테아제 억제제로서의 화합물 및 조성물
EA016327B1 (ru) * 2007-02-09 2012-04-30 Айрм Ллк Соединения и композиции в качестве ингибиторов протеазы, активирующей каналы
EA200901082A1 (ru) * 2007-02-09 2010-02-26 Айрм Ллк Соединения и композиции в качестве ингибиторов протеазы, активирующей каналы
IE20070935A1 (en) * 2007-12-21 2009-06-24 Trinity College Dublin Guanidine based compounds and their use in the treatment of mental and neurological disorders.
PL2421826T3 (pl) * 2009-04-20 2014-03-31 Hoffmann La Roche Pochodne proliny jako inhibitory katepsyn
KR20130028058A (ko) * 2010-02-03 2013-03-18 엠이에이치 어소시에이츠, 인코포레이티드 선택적 및 생활성 동배체로서의 다수 치환된 플루오로메탄류
CN103946213A (zh) * 2011-11-25 2014-07-23 霍夫曼-拉罗奇有限公司 作为组织蛋白酶抑制剂的新吡咯烷衍生物
CA2963305A1 (en) 2014-10-06 2016-04-14 Cortexyme, Inc. Inhibitors of lysine gingipain
CN105001131A (zh) * 2015-07-31 2015-10-28 吉尔生化（上海）有限公司 一种医药中间体nα-z-s-苄基-l-半胱氨酸-4-硝基苯酯的合成方法
CA3004095A1 (en) 2015-11-09 2017-05-18 Cortexyme, Inc. Inhibitors of arginine gingipain
CA3036862A1 (en) 2016-09-16 2018-03-22 Cortexyme, Inc. Ketone inhibitors of lysine gingipain
CN110483437B (zh) * 2018-05-14 2022-12-06 嘉兴维眸生物科技有限公司 一种含五元环的化合物及其制备和应用
WO2021053058A1 (en) 2019-09-17 2021-03-25 Mereo Biopharma 4 Limited Alvelestat for use in the treatment of graft rejection, bronchiolitis obliterans syndrome and graft versus host disease
DK4106757T3 (da) 2020-04-16 2023-10-23 Mereo Biopharma 4 Ltd Fremgangsmåder der involverer neutrofil elastase-inhibitor alvelestat til behandling af luftvejssygdom medieret af alpha-1-antitrypsin-mangel
AU2022373971A1 (en) 2021-10-20 2024-04-04 Mereo Biopharma 4 Limited Neutrophil elastase inhibitors for use in the treatment of fibrosis

Family Cites Families (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8809316D0 (en) * 1987-05-11 1988-05-25 Ici America Inc Heterocyclic ketones
US5672582A (en) 1993-04-30 1997-09-30 Merck & Co., Inc. Thrombin inhibitors
IL112795A (en) 1994-03-04 2001-01-28 Astrazeneca Ab Peptide derivatives as antithrombic agents their preparation and pharmaceutical compositions containing them
ZA951618B (en) 1994-03-04 1996-08-27 Lilly Co Eli Antithrombotic agents
US5707966A (en) * 1994-03-04 1998-01-13 Eli Lilly And Company Antithrombotic agents
US5726159A (en) * 1994-03-04 1998-03-10 Eli Lilly And Company Antithrombotic agents
US5705487A (en) * 1994-03-04 1998-01-06 Eli Lilly And Company Antithrombotic agents
WO1995033763A1 (en) 1994-06-02 1995-12-14 Hoechst Marion Roussel, Inc. Novel elastase inhibitors
JPH0820597A (ja) 1994-07-07 1996-01-23 Meiji Seika Kaisha Ltd トロンビン阻害作用を有する複素環カルボニル化合物
US5618792A (en) * 1994-11-21 1997-04-08 Cortech, Inc. Substituted heterocyclic compounds useful as inhibitors of (serine proteases) human neutrophil elastase
US5710130A (en) * 1995-02-27 1998-01-20 Eli Lilly And Company Antithrombotic agents
US5914319A (en) * 1995-02-27 1999-06-22 Eli Lilly And Company Antithrombotic agents
CA2176414A1 (en) 1995-05-18 1996-11-19 S. David Kimball Acyl guanidine and amidine prodrugs
US5523308A (en) 1995-06-07 1996-06-04 Costanzo; Michael J. Peptidyl heterocycles useful in the treatment of thrombin related disorders
US6022861A (en) * 1995-06-07 2000-02-08 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
US6211154B1 (en) * 1995-06-07 2001-04-03 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
US5827866A (en) 1995-06-07 1998-10-27 Ortho Pharmaceutical Corporation Peptidyl heterocycles useful in the treatment of thrombin related disorders
US6069130A (en) 1995-06-07 2000-05-30 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
US5827860A (en) 1995-06-07 1998-10-27 Ortho Pharmaceutical Corporation Peptidyl heterocycles useful in the treatment of thrombin related disorders
IL119466A (en) 1995-11-03 2001-08-26 Akzo Nobel Nv Thrombin inhibitors, their preparation and pharmaceutical compositions containing them
TW523513B (en) 1996-03-01 2003-03-11 Akzo Nobel Nv Serine protease inhibitors
JP2000513354A (ja) 1996-06-18 2000-10-10 ワーナー―ランバート・コンパニー キラルな塩基性アミノ酸ケト―複素環化合物の製造方法
IL121474A0 (en) 1996-08-23 1998-02-08 Akzo Nobel Nv Thrombin inhibitors
UA79749C2 (en) 1996-10-18 2007-07-25 Vertex Pharma Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
AU734615B2 (en) 1996-12-06 2001-06-21 Cortech, Inc. Serine protease inhibitors
US6004933A (en) 1997-04-25 1999-12-21 Cortech Inc. Cysteine protease inhibitors
PL336589A1 (en) 1997-05-02 2000-07-03 Akzo Nobel Nv Serinic protease inhibitors
IL134233A0 (en) 1997-08-11 2001-04-30 Boehringer Ingelheim Ca Ltd Hepatitis c inhibitor peptide analogues
US6323219B1 (en) * 1998-04-02 2001-11-27 Ortho-Mcneil Pharmaceutical, Inc. Methods for treating immunomediated inflammatory disorders
EP1114822A3 (en) 1998-06-03 2002-11-13 Cortech Inc. Indoles and tetrahydroisoquinolines containing alpha-keto oxadiazoles as serine protease inhibitors
US6323180B1 (en) 1998-08-10 2001-11-27 Boehringer Ingelheim (Canada) Ltd Hepatitis C inhibitor tri-peptides
AR022061A1 (es) 1998-08-10 2002-09-04 Boehringer Ingelheim Ca Ltd Peptidos inhibidores de la hepatitis c, una composicion farmaceutica que los contiene, el uso de los mismos para preparar una composicion farmaceutica, el uso de un producto intermedio para la preparacion de estos peptidos y un procedimiento para la preparacion de un peptido analogo de los mismos.
US6242422B1 (en) 1998-10-22 2001-06-05 Idun Pharmacueticals, Inc. (Substituted)Acyl dipeptidyl inhibitors of the ice/ced-3 family of cysteine proteases
KR20000047461A (ko) 1998-12-29 2000-07-25 성재갑 트롬빈 억제제
CA2361479A1 (en) * 1999-01-27 2000-08-03 Ortho-Mcneil Pharmaceutical, Inc. Peptidyl heterocyclic ketones useful as tryptase inhibitors
JP2000256396A (ja) * 1999-03-03 2000-09-19 Dainippon Pharmaceut Co Ltd 複素環式化合物およびその中間体ならびにエラスターゼ阻害剤
GB9929552D0 (en) 1999-12-14 2000-02-09 Proteus Molecular Design Compounds
EP1196436A2 (en) 1999-07-07 2002-04-17 Bristol-Myers Squibb Pharma Company Peptide boronic acid inhibitors of hepatitis c virus protease
GB9923710D0 (en) 1999-10-08 1999-12-08 Proteus Molecular Design Chemical compounds
WO2001040262A1 (en) 1999-12-03 2001-06-07 Bristol-Myers Squibb Pharma Company Alpha-ketoamide inhibitors of hepatitis c virus ns3 protease
US7244721B2 (en) * 2000-07-21 2007-07-17 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
CN1498224A (zh) * 2000-07-21 2004-05-19 ���鹫˾ 用作丙型肝炎病毒ns3-丝氨酸蛋白酶抑制剂的新型肽
SV2003000617A (es) 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
JP2005511475A (ja) 2001-03-02 2005-04-28 ブリストル−マイヤーズ スクイブ カンパニー メラノコルチン受容体のモジュレーターとして有用な化合物及びそれを含む製薬組成物
JP4455056B2 (ja) 2001-07-11 2010-04-21 バーテックス ファーマシューティカルズ インコーポレイテッド 架橋二環式セリンプロテアーゼ阻害剤
EP1425029A4 (en) * 2001-08-10 2006-06-07 Palatin Technologies Inc PEPTIDOMIMETICS OF BIOLOGICALLY ACTIVE METALLOPEPTIDES
WO2003072528A2 (en) 2002-02-08 2003-09-04 Idun Pharmaceuticals, Inc. (substituted)acyl dipeptidyl inhibitors of the ice/ced-3 family of cysteine proteases
US7019019B2 (en) * 2002-12-23 2006-03-28 Dendreon Corporation Matriptase inhibitors and methods of use
US7205384B2 (en) * 2003-08-05 2007-04-17 Ortho-Mcneil Pharmaceutical Inc. Process for preparing peptidyl heterocyclic ketone derivatives
TWI359147B (en) 2003-09-05 2012-03-01 Vertex Pharma Inhibitors of serine proteases, particularly hcv n
MXPA06004006A (es) 2003-10-10 2006-06-28 Vertex Pharma Inhibidores de serina proteasas, especialmente de ns3-ns4a proteasa del virus de la hepatitis c.
CA2549167A1 (en) 2003-12-11 2005-06-30 Schering Corporation Inhibitors of hepatitis c virus ns3/ns4a serine protease
US20050222383A1 (en) * 2004-02-05 2005-10-06 Irm Llc Prostasin substrates and inhibitors
RU2006134005A (ru) 2004-02-27 2008-04-10 Шеринг Корпорейшн (US) Новые соединения, действующие как ингибиторы сериновой протеазы ns3 вируса гепатита с
RU2393154C2 (ru) 2004-03-24 2010-06-27 Йерини Аг Новые соединения для ингибирования ангиогенеза и их применение
MXPA06013404A (es) 2004-05-20 2007-01-23 Schering Corp Prolinas sustituidas como inhibidores de serina proteasa ns3 de virus de hepatitis c.
JPWO2006006644A1 (ja) 2004-07-14 2008-05-01 協和醗酵工業株式会社 複素環式化合物
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
US20060275366A1 (en) * 2005-06-02 2006-12-07 Schering Corporation Controlled-release formulation
KR101069089B1 (ko) 2006-05-23 2011-09-30 아이알엠 엘엘씨 채널 활성화 프로테아제 억제제로서의 화합물 및 조성물
JP2009538327A (ja) * 2006-05-23 2009-11-05 アイアールエム・リミテッド・ライアビリティ・カンパニー チャネル活性化プロテアーゼ阻害剤である化合物および組成物
US20080176901A1 (en) * 2007-01-10 2008-07-24 Irm Llc Compounds and compositions as channel activating protease inhibitors
EA016327B1 (ru) 2007-02-09 2012-04-30 Айрм Ллк Соединения и композиции в качестве ингибиторов протеазы, активирующей каналы
EA200901082A1 (ru) 2007-02-09 2010-02-26 Айрм Ллк Соединения и композиции в качестве ингибиторов протеазы, активирующей каналы

Also Published As

Publication number Publication date
CA2651762A1 (en) 2007-11-29
WO2007137080A3 (en) 2008-01-24
MX2008014839A (es) 2008-12-05
AU2007253819B2 (en) 2011-02-17
AU2007253819A1 (en) 2007-11-29
CL2007001481A1 (es) 2008-05-09
US7951823B2 (en) 2011-05-31
BRPI0712021A2 (pt) 2012-01-03
TW200813094A (en) 2008-03-16
RU2008150615A (ru) 2010-06-27
US20070275906A1 (en) 2007-11-29
US20110257077A1 (en) 2011-10-20
JP2009538327A (ja) 2009-11-05
KR20090014217A (ko) 2009-02-06
RU2419626C2 (ru) 2011-05-27
EP2027143A2 (en) 2009-02-25
WO2007137080A2 (en) 2007-11-29
US8338469B2 (en) 2012-12-25
AR061109A1 (es) 2008-08-06
KR101069051B1 (ko) 2011-09-29

Similar Documents

Publication Publication Date Title
PE20080708A1 (es) Compuestos 2-pirrolidincarboxamida sustituidos como inhibidores de la proteasa que activa el canal respiratorio
PE20081566A1 (es) Compuestos y composiciones como inhibidores de proteasa activadora de canal
PE20080101A1 (es) Derivados de pirrolidina como inhibidores de la proteasa que activa el conducto respiratorio
PE20081532A1 (es) Compuestos novedosos
PE20190705A1 (es) COMPUESTOS DE BENZO[b] TIOFENO COMO AGONISTAS DE STING
PE20090813A1 (es) Inhibidores de la 11b-hidroxiesteroide-deshidrogenasa
PE20181045A1 (es) Compuestos utiles como inmunomoduladores
MX2009000531A (es) Derivados heterociclicos fusionados y metodos de uso.
PE20121010A1 (es) Derivados de bencimidazol
PE20121031A1 (es) Nuevos conjugados, su preparacion y su aplicacion terapeutica
PE20110547A1 (es) Compuestos de isoindolina con actividad anticancerigena
PE20080768A1 (es) Compuestos de isoindolina 5-sustituidos
PE20061436A1 (es) Derivados de amida sustituida como inhibidores de proteina quinasa
CY1112495T1 (el) Κυτταροτοξικοι παραγοντες που περιλαμβανουν νεα παραγωγα τομαϋμυκινης
CY1113395T1 (el) Σταθερη φαρμακευτικη συνθεση που περιεχει πυριμιδινη-σουλφαμιδη
PE20120632A1 (es) Inhibidores de bace
PE20091376A1 (es) Derivados de fenilamino como moduladores de beta-amiloide
MY142018A (en) Thiophene derivatives as chk 1 inihibitors
PE20121526A1 (es) Compuestos policiclicos heterociclicos como inhibidores del virus de la hepatitis c
AR063788A1 (es) Derivados de 5-hidroximetil-oxazolidin -2-ona
EA200970585A1 (ru) Бензамидные производные как агонисты ер-рецепторов
PE20081831A1 (es) Derivados de heteroaril-pirrolidinil- y -piperidinil-cetona
PE20080889A1 (es) Aminometil-4-imidazoles
MX2010003942A (es) Nuevos inhibidores de epoxido hidrolasa soluble y su uso.
PE20081662A1 (es) DERIVADOS DE 6-OXO-6,7-DIHIDRO-5H-DIBENZO[b,d]AZEPIN-7-ILO

Legal Events

Date Code Title Description
FA Abandonment or withdrawal