AR064841A1 - Compuestos y composiciones como como inhibidores de proteasa activadora de canal - Google Patents

Compuestos y composiciones como como inhibidores de proteasa activadora de canal

Info

Publication number
AR064841A1
AR064841A1 ARP080100104A ARP080100104A AR064841A1 AR 064841 A1 AR064841 A1 AR 064841A1 AR P080100104 A ARP080100104 A AR P080100104A AR P080100104 A ARP080100104 A AR P080100104A AR 064841 A1 AR064841 A1 AR 064841A1
Authority
AR
Argentina
Prior art keywords
ring
aryl
alkynyl
alkenyl
alkyl
Prior art date
Application number
ARP080100104A
Other languages
English (en)
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 AR064841A1 publication Critical patent/AR064841A1/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
    • 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
    • C07K5/06—Dipeptides
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • 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
    • A61K31/40—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
    • 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
    • A61K31/425—Thiazoles
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/10—Expectorants
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides 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
    • C07K5/06—Dipeptides
    • C07K5/06086—Dipeptides with the first amino acid being basic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Communicable Diseases (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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrrole Compounds (AREA)

Abstract

Composiciones farmacéuticas de los mismos, los cuales son utiles para modular las proteasas activadoras de canal, y utilizando estos compuestos, métodos para tratar, disminuir o prevenir una condicion asociada con una proteasa activadora de canal, incluyendo, pero no limitándose a, prostasina, PRSS22, TMPRSS 11 (por ejemplo, TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptasa (MTSP-1), CAP2, CAP3, tripsina, catepsina A, o elastasa de neutrofilos. Reivindicacion 1: Un compuesto de la formula (1), o sales farmacéuticamente aceptables del mismo, en donde O-(CR2)p-R2 es un sustituyente en cualquier posicion del anillo A; J es un anillo carbocíclico monocíclico o fusionado de 5 a 12 miembros, un anillo heterocíclico que comprende N, O y/o S; un anillo de arilo o hetero-arilo, en el entendido de que J no es triazolilo; B es como en formula (2) o (CR2)k-R5; Y es un enlace -SO2-, -NHCO- u -O-(CO)-; R1 es halogeno, -(CR2)l-NR6R7, -(CR2)l-NRC(=NR)-NR6R7, -(CR2)l- C(=NR)-R6R7, -C(O)-(CR2)l-NR6R7, -(CR2)l-NR-SO2R6, -(CR2)l-NR-C(O)-R6, -(CR2)l-SO2NR6R7, o -(CR2)l-OR6, o un alcoxilo C1-6 opcionalmente sustituido, alquilo C1-6, alquenilo C2-6, o alquinilo C2-6; o un anillo carbocíclico opcionalmente sustituido, un anillo heterocíclico, arilo o helero-arilo; R3 es alquilo C1-6, alquenilo C2-6, alquinilo C2-6, -(CR2)l-R5; de una manera alternativa, NH-Y-R3 forman juntos NH2; R2, R4 y R5 son independientemente un anillo carbocíclico de 5 a 12 miembros opcionalmente sustituido, un anillo heterocíclico, arilo o hetero-arilo; o R4 es H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, o formula (2), en donde P es C o N, y el anillo E junto con P forman un anillo monociclico o fusionado de 5 a 12 miembros opcionalmente sustituido; R6 y R7 son independientemente H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, o -(CR2)l-R5; cada R es H, o alquilo C1-6, alquenilo C2-6, o alquinilo C2-6; l es de 0 a 6; k, m, n, y p son independientemente de 1 a 6; x es de 0 a 4; en el entendido de que R4 es piperidinilo cuando NH-Y-R3 forman juntos NH2; y además en el entendido de que R5 es piperidinilo cuando B es (CR2)k-R5.
ARP080100104A 2007-01-10 2008-01-10 Compuestos y composiciones como como inhibidores de proteasa activadora de canal AR064841A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US88433407P 2007-01-10 2007-01-10
US89147407P 2007-02-23 2007-02-23

Publications (1)

Publication Number Publication Date
AR064841A1 true AR064841A1 (es) 2009-04-29

Family

ID=39148650

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP080100104A AR064841A1 (es) 2007-01-10 2008-01-10 Compuestos y composiciones como como inhibidores de proteasa activadora de canal

Country Status (33)

Country Link
US (1) US20080176901A1 (es)
EP (2) EP2279777A2 (es)
JP (1) JP2010515729A (es)
KR (1) KR101084787B1 (es)
AR (1) AR064841A1 (es)
AT (1) ATE493174T1 (es)
AU (1) AU2007342223B2 (es)
BR (1) BRPI0720799A2 (es)
CA (1) CA2673803A1 (es)
CL (1) CL2008000060A1 (es)
CO (1) CO6190626A2 (es)
CU (1) CU23762B7 (es)
CY (1) CY1111340T1 (es)
DE (1) DE602007011670D1 (es)
DK (1) DK2104535T3 (es)
EA (1) EA016199B1 (es)
EC (1) ECSP099517A (es)
GT (1) GT200900196A (es)
HK (1) HK1129860A1 (es)
HN (1) HN2009001282A (es)
HR (1) HRP20110201T1 (es)
MA (1) MA31037B1 (es)
MX (1) MX2009007476A (es)
NO (1) NO20092817L (es)
NZ (1) NZ577939A (es)
PE (1) PE20081566A1 (es)
PL (1) PL2104535T3 (es)
PT (1) PT2104535E (es)
RS (1) RS51644B (es)
SV (1) SV2009003330A (es)
TN (1) TN2009000294A1 (es)
TW (1) TW200845981A (es)
WO (1) WO2008085608A1 (es)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0712021A2 (pt) 2006-05-23 2012-01-03 Irm Llc composto e composiÇÕes como inibidores da protease ativadora de canal
JP5208963B2 (ja) 2007-01-10 2013-06-12 エフ．ホフマン−ラ ロシュ アーゲー キマーゼ阻害剤としてのスルホンアミド誘導体
MX2009008518A (es) 2007-02-09 2009-08-20 Irm Llc Compuestos y composiciones como inhibidores de la proteasa activadora de canal.
KR20120058468A (ko) 2009-05-18 2012-06-07 오리온 코포레이션 프로테아제 억제제
GB201805174D0 (en) * 2018-03-29 2018-05-16 Univ Leeds Innovations Ltd Compounds
US11584714B2 (en) 2018-05-29 2023-02-21 Omeros Corporation MASP-2 inhibitors and methods of use
JP2022519924A (ja) * 2019-03-22 2022-03-25 アキリオン ファーマシューティカルズ， インコーポレーテッド 補体媒介性障害の治療のための医薬化合物
JP2023500182A (ja) 2019-09-17 2023-01-05 メレオ バイオファーマ ４ リミテッド 移植片拒絶反応、閉塞性細気管支炎症候群、及び移植片対宿主病の治療に使用するためのアルベレスタット
AU2020395306A1 (en) * 2019-12-04 2022-06-30 Omeros Corporation MASP-2 inhibitors and methods of use
EP4069678A1 (en) 2019-12-04 2022-10-12 Omeros Corporation Masp-2 inhibitors and methods of use
CA3159172A1 (en) 2019-12-04 2021-06-10 Michael Cicirelli Masp-2 inhibitors and methods of use
ES2962498T3 (es) 2020-04-16 2024-03-19 Mereo Biopharma 4 Ltd Métodos que implican el inhibidor de elastasa de neutrófilos alvelestat para el tratamiento de enfermedades respiratorias mediadas por deficiencia de alfa-1 antitripsina
TW202325294A (zh) 2021-10-20 2023-07-01 英商梅瑞奧生物製藥４有限公司 用於治療纖維化之嗜中性球彈性蛋白酶抑制劑
WO2023183405A2 (en) * 2022-03-22 2023-09-28 Alexion Pharmaceuticals, Inc. Pharmaceutical compounds for the treatment of complement mediated disorders

Family Cites Families (108)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1219606A (en) 1968-07-15 1971-01-20 Rech S Et D Applic Scient Soge Quinuclidinol derivatives and preparation thereof
JPS6235216A (ja) 1985-08-09 1987-02-16 Noritoshi Nakabachi 不均質物質層の層厚非破壊測定方法および装置
GB8923590D0 (en) 1989-10-19 1989-12-06 Pfizer Ltd Antimuscarinic bronchodilators
PT100441A (pt) 1991-05-02 1993-09-30 Smithkline Beecham Corp Pirrolidinonas, seu processo de preparacao, composicoes farmaceuticas que as contem e uso
WO1993018007A1 (en) 1992-03-13 1993-09-16 Tokyo Tanabe Company Limited Novel carbostyril derivative
MX9301943A (es) 1992-04-02 1994-08-31 Smithkline Beecham Corp Compuestos.
WO1993019750A1 (en) 1992-04-02 1993-10-14 Smithkline Beecham Corporation Compounds useful for treating allergic or inflammatory diseases
US5605923A (en) 1992-04-02 1997-02-25 Smithkline Beecham Corporation Compounds useful for treating inflammatory diseases and inhibiting production of tumor necrosis factor
US5707966A (en) * 1994-03-04 1998-01-13 Eli Lilly And Company Antithrombotic agents
US5705487A (en) * 1994-03-04 1998-01-06 Eli Lilly And Company Antithrombotic agents
IL112795A (en) * 1994-03-04 2001-01-28 Astrazeneca Ab Derivatives of peptides as antithrombotic drugs, their preparation, and pharmaceutical preparations containing them
US5726159A (en) * 1994-03-04 1998-03-10 Eli Lilly And Company Antithrombotic agents
US5914319A (en) * 1995-02-27 1999-06-22 Eli Lilly And Company Antithrombotic agents
GB2299455B (en) * 1995-03-31 1999-12-22 Motorola Inc Self phased antenna element with dielectric and associated method
US5863929A (en) * 1996-06-25 1999-01-26 Eli Lilly And Company Anticoagulant agents
GB9622386D0 (en) 1996-10-28 1997-01-08 Sandoz Ltd Organic compounds
US6166037A (en) 1997-08-28 2000-12-26 Merck & Co., Inc. Pyrrolidine and piperidine modulators of chemokine receptor activity
WO1999016766A1 (fr) 1997-10-01 1999-04-08 Kyowa Hakko Kogyo Co., Ltd. Derives de benzodioxole
US6541669B1 (en) 1998-06-08 2003-04-01 Theravance, Inc. β2-adrenergic receptor agonists
CA2335094C (en) 1998-06-30 2008-12-23 The Dow Chemical Company Polymer polyols and a process for the production thereof
GB9913083D0 (en) 1999-06-04 1999-08-04 Novartis Ag Organic compounds
PL203117B1 (pl) 1999-05-04 2009-08-31 Schering Corp Piperydynopiperydynowa pochodna użyteczna jako antagonista CCR5, zawierająca ją kompozycja farmaceutyczna i jej zastosowanie
PL203116B1 (pl) 1999-05-04 2009-08-31 Schering Corp Piperazynopiperydynowa pochodna użyteczna jako antagonista CCR5, zawierająca ją kompozycja farmaceutyczna i jej zastosowanie
US6683115B2 (en) 1999-06-02 2004-01-27 Theravance, Inc. β2-adrenergic receptor agonists
ES2165768B1 (es) 1999-07-14 2003-04-01 Almirall Prodesfarma Sa Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen.
NZ517166A (en) 1999-08-21 2004-01-30 Altana Pharma Ag Synergistic combination of PDE inhibitors and beta 2 adrenoceptor agonists
OA11558A (en) 1999-12-08 2004-06-03 Advanced Medicine Inc Beta 2-adrenergic receptor agonists.
CN1426401A (zh) 2000-04-27 2003-06-25 贝林格尔英格海姆法玛公司 新的长效倍他米美类药物(betamimetics)其制备方法,及其作为药物组合物的用途
PT1300407E (pt) 2000-06-27 2004-05-31 S A L V A T Lab Sa Compostos carbamatos derivados de arilalquilaminas
GB0015876D0 (en) 2000-06-28 2000-08-23 Novartis Ag Organic compounds
DE10038639A1 (de) 2000-07-28 2002-02-21 Schering Ag Nichtsteroidale Entzündungshemmer
DZ3468A1 (fr) 2000-08-05 2002-02-14 Glaxo Group Ltd 6.alpha., 9.alpha.-difluoro-17.alpha.-`(2-furanylcarboxyle) oxy!-11.beta.-hydroxy-16.alpha.-methyle-3-oxo-androst-1,4,-diene-17-acide carbothioique s-fluoromethyle ester utilise comme agent anti inflammatoire
GB0028383D0 (en) 2000-11-21 2001-01-03 Novartis Ag Organic compounds
BR0116450A (pt) 2000-12-22 2003-09-30 Almirall Prodesfarma Ag Composto, processos para a preparação de um carbamato, e para produzir um sal, composição farmacêutica, uso de um composto ou de uma composição farmacêutica, e, produto de combinação
BR0116624A (pt) 2000-12-28 2003-12-23 Almirall Prodesfarma Ag Composto, processo para produzir o mesmo, composição farmacêutica, uso do composto ou da composição farmacêutica, e, produto de combinação
GB0103630D0 (en) 2001-02-14 2001-03-28 Glaxo Group Ltd Chemical compounds
EP1366025B1 (en) 2001-03-08 2007-06-27 Glaxo Group Limited Agonists of beta-adrenoreceptors
JP4143413B2 (ja) 2001-03-22 2008-09-03 グラクソ グループ リミテッド β２−アドレナリン受容体アゴニストとしてのホルムアニリド誘導体
CN1302007C (zh) 2001-04-30 2007-02-28 葛兰素集团有限公司 具有抗炎性的在17.α位上具有环酯基的雄甾烷的17.β.－硫代羧酸酯衍生物
ATE399174T1 (de) 2001-06-12 2008-07-15 Glaxo Group Ltd Neue anti inflammatorische 17.alpha.- heterozyklische ester von 17.beta.-carbothioat androstan derivativen
EP2319919B1 (en) 2001-06-21 2015-08-12 BASF Enzymes LLC Nitrilases
EP1425029A4 (en) * 2001-08-10 2006-06-07 Palatin Technologies Inc PEPTIDOMIMETICS OF BIOLOGICALLY ACTIVE METALLOPEPTIDES
CN103288793B (zh) 2001-09-14 2015-09-23 葛兰素集团有限公司 治疗呼吸疾病的苯乙醇胺衍生物
EP1438309A1 (en) 2001-10-17 2004-07-21 Ucb, S.A. Quinuclidine derivatives, processes for preparing them and their uses as m2 and/or m3 muscarinic receptor inhibitors
GB0125259D0 (en) 2001-10-20 2001-12-12 Glaxo Group Ltd Novel compounds
AR037517A1 (es) 2001-11-05 2004-11-17 Novartis Ag Derivados de naftiridinas, un proceso para su preparacion, composicion farmaceutica y el uso de los mismos para la preparacion de un medicamento para el tratamiento de una enfermedad inflamatoria
US6653323B2 (en) 2001-11-13 2003-11-25 Theravance, Inc. Aryl aniline β2 adrenergic receptor agonists
TWI249515B (en) 2001-11-13 2006-02-21 Theravance Inc Aryl aniline beta2 adrenergic receptor agonists
AU2002356759A1 (en) 2001-12-01 2003-06-17 Glaxo Group Limited 17.alpha. -cyclic esters of 16-methylpregnan-3,20-dione as anti-inflammatory agents
US7452904B2 (en) 2001-12-20 2008-11-18 Chiesi Farmaceutici S.P.A. 1-alkyl-1-azoniabicyclo' 2.2.2 octane carbamate derivatives and their use as muscarinic receptor antagonists
WO2003072592A1 (en) 2002-01-15 2003-09-04 Glaxo Group Limited 17.alpha-cycloalkyl/cycloylkenyl esters of alkyl-or haloalkyl-androst-4-en-3-on-11.beta.,17.alpha.-diol 17.beta.-carboxylates as anti-inflammatory agents
WO2003062259A2 (en) 2002-01-21 2003-07-31 Glaxo Group Limited Non-aromatic 17.alpha.-esters of androstane-17.beta.-carboxylate esters as anti-inflammatory agents
GB0202216D0 (en) 2002-01-31 2002-03-20 Glaxo Group Ltd Novel compounds
GB0204719D0 (en) 2002-02-28 2002-04-17 Glaxo Group Ltd Medicinal compounds
RS51097B (sr) 2002-03-26 2010-10-31 Boehringer Ingelheim Pharmaceuticals Inc. Glukokortikoidni mimetici,postupci za njihovo dobijanje, farmaceutski preparati i njihova primena
JP2005521717A (ja) 2002-03-26 2005-07-21 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド グルココルチコイドミメチックス、その製造方法、その医薬組成物、及び使用
WO2003086294A2 (en) 2002-04-11 2003-10-23 Merck & Co., Inc. 1h-benzo[f]indazol-5-yl derivatives as selective glucocorticoid receptor modulators
ES2206021B1 (es) 2002-04-16 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de pirrolidinio.
WO2003091204A1 (en) 2002-04-25 2003-11-06 Glaxo Group Limited Phenethanolamine derivatives
JP2005527618A (ja) 2002-05-28 2005-09-15 セラヴァンス インコーポレーテッド アルコキシアリールβ２アドレナリン作動性レセプターアゴニスト
US7186864B2 (en) 2002-05-29 2007-03-06 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
ES2201907B1 (es) 2002-05-29 2005-06-01 Almirall Prodesfarma, S.A. Nuevos derivados de indolilpiperidina como potentes agentes antihistaminicos y antialergicos.
DE10224888A1 (de) 2002-06-05 2003-12-24 Merck Patent Gmbh Pyridazinderivate
US7074806B2 (en) 2002-06-06 2006-07-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
DE10225574A1 (de) 2002-06-10 2003-12-18 Merck Patent Gmbh Aryloxime
DE10227269A1 (de) 2002-06-19 2004-01-08 Merck Patent Gmbh Thiazolderivate
JP2006502104A (ja) 2002-06-25 2006-01-19 メルク フロスト カナダ アンド カンパニー ８−（ビアリール）キノリンｐｄｅ４阻害剤
ES2204295B1 (es) 2002-07-02 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de quinuclidina-amida.
JP2005538972A (ja) 2002-07-02 2005-12-22 メルク フロスト カナダ アンド カンパニー ジアリール置換エタンピリドンｐｄｅ４阻害剤
PT1521733E (pt) 2002-07-08 2014-10-29 Pfizer Prod Inc Moduladores do recetor de glucocorticoides
GB0217225D0 (en) 2002-07-25 2002-09-04 Glaxo Group Ltd Medicinal compounds
AR040962A1 (es) 2002-08-09 2005-04-27 Novartis Ag Compuestos derivados de tiazol 1,3-2-ona, composicion farmaceutica y proceso de preparacion del compuesto
WO2004018449A1 (en) 2002-08-10 2004-03-04 Altana Pharma Ag Piperidine-derivatives as pde4 inhibitors
EP1556049A1 (en) 2002-08-10 2005-07-27 ALTANA Pharma AG Piperidine-pyridazones and phthalazones as pde4 inhibitors
EP1542987A1 (en) 2002-08-10 2005-06-22 ALTANA Pharma AG Piperidine-n-oxide-derivatives
EP1556369A1 (en) 2002-08-10 2005-07-27 ALTANA Pharma AG Pyridazinone-derivatives as pde4 inhibitors
PL374014A1 (en) 2002-08-17 2005-09-19 Altana Pharma Ag Novel phenanthridines having pde 3/4 inhibiting properties
US20060113968A1 (en) 2002-08-17 2006-06-01 Altana Pharma Ag Novel benzonaphthyridines
AU2003259747A1 (en) 2002-08-21 2004-03-11 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted hihydroquinolines as glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
SE0202483D0 (sv) 2002-08-21 2002-08-21 Astrazeneca Ab Chemical compounds
EP1534675B1 (en) 2002-08-23 2009-02-25 Ranbaxy Laboratories, Ltd. Fluoro and sulphonylamino containing 3,6-disubstituted azabicyclo¬3.1.0 hexane derivatives as muscarinic receptor antagonists
WO2004019945A1 (en) 2002-08-29 2004-03-11 Altana Pharma Ag 3-hydroxy-6-phenylphenanthridines as pde-4 inhibitors
ATE473740T1 (de) 2002-08-29 2010-07-15 Boehringer Ingelheim Pharma 3-(sulfonamidoethyl)-indol-derivate zur verwendung als glucocorticoid-mimetika bei der behandlung von entzündlichen, allergischen und proliferativen erkrankungen
EP1539164B1 (en) 2002-08-29 2006-12-20 ALTANA Pharma AG 2-hydroxy-6-phenylphenanthridines as pde-4 inhibitors
GB0220730D0 (en) 2002-09-06 2002-10-16 Glaxo Group Ltd Medicinal compounds
JP2006096662A (ja) 2002-09-18 2006-04-13 Sumitomo Pharmaceut Co Ltd 新規６−置換ウラシル誘導体及びアレルギー性疾患の治療剤
CA2497903A1 (en) 2002-09-18 2004-04-01 Ono Pharmaceutical Co., Ltd. Triazaspiro[5.5]undecane derivatives and drugs comprising the same as the active ingredient
US20050245588A1 (en) 2002-09-20 2005-11-03 Amjad Ali Octahydro-2-h-naphtho[1,2-f]indole-4-carboxamide derivatives as selective glucocorticoid receptor modulators
JP2004107299A (ja) 2002-09-20 2004-04-08 Japan Energy Corp 新規１−置換ウラシル誘導体及びアレルギー性疾患の治療剤
DE10246374A1 (de) 2002-10-04 2004-04-15 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Betamimetika mit verlängerter Wirkungsdauer, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
ATE392206T1 (de) 2002-10-11 2008-05-15 Pfizer Indolderivate als beta-2 agonisten
EP1440966A1 (en) 2003-01-10 2004-07-28 Pfizer Limited Indole derivatives useful for the treatment of diseases
US20060205790A1 (en) 2002-10-22 2006-09-14 Coe Diane M Medicinal arylethanolamine compounds
KR20050065624A (ko) 2002-10-23 2005-06-29 그렌마크 파머수티칼스 엘티디. 염증성 및 알레르기 질환의 치료에 유용한 신규한트리사이클릭 화합물, 이의 제조 방법 및 이를 함유하는약제 조성물
GB0225030D0 (en) 2002-10-28 2002-12-04 Glaxo Group Ltd Medicinal compounds
WO2004037773A1 (en) 2002-10-28 2004-05-06 Glaxo Group Limited Phenethanolamine derivative for the treatment of respiratory diseases
GB0225287D0 (en) 2002-10-30 2002-12-11 Glaxo Group Ltd Novel compounds
GB0225540D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
GB0225535D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
DE10253426B4 (de) 2002-11-15 2005-09-22 Elbion Ag Neue Hydroxyindole, deren Verwendung als Inhibitoren der Phosphodiesterase 4 und Verfahren zu deren Herstellung
DE10253220A1 (de) 2002-11-15 2004-05-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Dihydroxy-Methyl-Phenyl-Derivate, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
DE10253282A1 (de) 2002-11-15 2004-05-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Arzneimittel zur Behandlung von chronisch obstruktiver Lungenerkrankung
DE10261874A1 (de) 2002-12-20 2004-07-08 Schering Ag Nichtsteroidale Entzündungshemmer
US7019019B2 (en) 2002-12-23 2006-03-28 Dendreon Corporation Matriptase inhibitors and methods of use
CA2512987C (en) 2003-01-21 2011-06-14 Merck & Co., Inc. 17-carbamoyloxy cortisol derivatives as selective glucocorticoid receptor modulators
PE20040950A1 (es) 2003-02-14 2005-01-01 Theravance Inc DERIVADOS DE BIFENILO COMO AGONISTAS DE LOS RECEPTORES ADRENERGICOS ß2 Y COMO ANTAGONISTAS DE LOS RECEPTORES MUSCARINICOS
EP1460064A1 (en) 2003-03-14 2004-09-22 Pfizer Limited Indole-2-carboxamide derivatives useful as beta-2 agonists
GB0507577D0 (en) * 2005-04-14 2005-05-18 Novartis Ag Organic compounds

Also Published As

Publication number Publication date
DK2104535T3 (da) 2011-04-04
EA200900920A1 (ru) 2010-02-26
MA31037B1 (fr) 2009-12-01
PL2104535T3 (pl) 2011-05-31
BRPI0720799A2 (pt) 2014-03-11
ECSP099517A (es) 2009-08-28
MX2009007476A (es) 2009-07-22
EA016199B1 (ru) 2012-03-30
CL2008000060A1 (es) 2008-07-18
SV2009003330A (es) 2011-07-28
JP2010515729A (ja) 2010-05-13
NZ577939A (en) 2011-03-31
PE20081566A1 (es) 2008-12-14
US20080176901A1 (en) 2008-07-24
RS51644B (en) 2011-10-31
HN2009001282A (es) 2012-04-16
NO20092817L (no) 2009-10-08
CY1111340T1 (el) 2015-08-05
TW200845981A (en) 2008-12-01
WO2008085608A1 (en) 2008-07-17
CA2673803A1 (en) 2008-07-17
HK1129860A1 (en) 2009-12-11
CU20090122A7 (es) 2011-07-11
EP2104535B9 (en) 2011-06-15
EP2104535A1 (en) 2009-09-30
KR101084787B1 (ko) 2011-11-21
EP2104535B1 (en) 2010-12-29
HRP20110201T1 (hr) 2011-08-31
AU2007342223B2 (en) 2011-02-24
PT2104535E (pt) 2011-03-31
ATE493174T1 (de) 2011-01-15
TN2009000294A1 (en) 2010-12-31
DE602007011670D1 (de) 2011-02-10
EP2279777A2 (en) 2011-02-02
GT200900196A (es) 2010-03-15
KR20090087511A (ko) 2009-08-17
CO6190626A2 (es) 2010-08-19
AU2007342223A1 (en) 2008-07-17
CU23762B7 (es) 2012-01-31

Similar Documents

Publication Publication Date Title
AR064841A1 (es) Compuestos y composiciones como como inhibidores de proteasa activadora de canal
AR061110A1 (es) Derivados de pirrolidin-2-carboxamida con accion inhibitoria de cap, composiciones farmaceuticas que los comprenden y su utilizacion en el tratamiento de afecciones respiratorias.
AR061109A1 (es) Compuestos y composiciones como inhibidores de la proteasa activadora de canal
CY1123025T1 (el) Αναστολεις βρωμοεπικρατειας
DOP2002000525A (es) Inhibidores del factor xa y de otras proteasas de serina implicadas en la cascada de la coagulacion.
PE20170127A1 (es) Indazol-3-carboxamidas 5-sustituidas y preparacion y uso de las mismas
SE0302486D0 (sv) Novel compounds
AR049956A1 (es) DERIVADOS DE 1,3 - OXAZOLIDIN - 2 - ONA COMO INHIBIDORES DE CETP Y ELEVADORES DEL NIVEL DE LAD-C; COMPOSICIONES FARMACÉUTICAS QUE LOS CONTIENEN Y SU USO EN LA FABRICACIoN DE UN MEDICAMENTO PARA EL TRATAMIENTO DE LA ATEROSCLEROSIS.
NO20091892L (no) Krystallinsk form av (3S)-3-(N-(N`-(2-tert-butylfenyl)oksamyl) alaninyl)amino-5-(2`,3`,5`,6`-tetrafluorfenoksy)-4 oksopentanoisk syre
DE60132975D1 (de) Neue substanzen und verbindungen als protease-inhibitoren
SE0302487D0 (sv) Novel compounds
EA200500289A1 (ru) Арилзамещенные бензимидазолы и их использование в качестве блокаторов натриевых каналов
ECSP045253A (es) Derivados de 5-feniltiazol y uso como inhibidores de pi3 cinasa
ECSP099371A (es) INHIBIDORES ESPIRO CETONA DE ACETIL-CoA CARBOXILASA
ECSP088677A (es) Piperazinas y piperidinas como potenciadores 157 del mglur5
UY29420A1 (es) Derivados de 2-piridona,composiciones que los contienen, procesos de preparación y aplicación
AR087309A1 (es) Compuesto heterociclico de anillos condensados sustituido, composicion farmaceutica que lo comprende y su uso para la fabricacion de un medicamento para el tratamiento de enfermedades neurogenerativas y aterosclerosis
EA202192669A1 (ru) Твердые формы ингибитора бета-лактамазы для пероральной доставки и их применения
ECSP055844A (es) Nuevos compuestos triciclicos
AR053169A1 (es) Metabolitos de n-2 (cloro-6-metilfenil)-2-[[6-[4-(2-hidroxietil)-1-piperazinil) -2-metil -4-pi rimidinil] amino]-5-tiazol carboxamidas
HRP20050775A2 (en) Quinolinone/benzoxazinone derivatives and uses thereof
DE602005010744D1 (de) Piperazinylpyridinderivate als mittel gegen adipositas
DE602004008959D1 (de) Benzoäbüä1,4üdioxepinderivate
DE602005009839D1 (de) Alkyl-und piperidin-substitutierte benzimidazol-derivate
UY26846A1 (es) Derivados de la pirrolidina

Legal Events

Date Code Title Description
FA Abandonment or withdrawal