LT2632921T - 6-(1h-indol-4-il)-4-(5-{[4-(1-metiletil)-1-piperazinil]metil}-1,3-oksazol-2-il)-1h-indazolo polimorfai ir druskos kaip pi3k inhibitoriai, skirti panaudoti pvz. kvėpavimo takų ligų gydymui - Google Patents

6-(1h-indol-4-il)-4-(5-{[4-(1-metiletil)-1-piperazinil]metil}-1,3-oksazol-2-il)-1h-indazolo polimorfai ir druskos kaip pi3k inhibitoriai, skirti panaudoti pvz. kvėpavimo takų ligų gydymui

Info

Publication number
LT2632921T
LT2632921T LTEP11776738.4T LT11776738T LT2632921T LT 2632921 T LT2632921 T LT 2632921T LT 11776738 T LT11776738 T LT 11776738T LT 2632921 T LT2632921 T LT 2632921T
Authority
LT
Lithuania
Prior art keywords
oxazol
indazole
polymorphs
indol
methylethyl
Prior art date
Application number
LTEP11776738.4T
Other languages
English (en)
Inventor
Julie Nicole Hamblin
Paul Spencer Jones
Suzanne Elaine Keeling
Joelle Le
Nigel James Parr
Robert David Willacy
Original Assignee
Glaxo Group Limited
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 Glaxo Group Limited filed Critical Glaxo Group Limited
Publication of LT2632921T publication Critical patent/LT2632921T/lt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
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  • Engineering & Computer Science (AREA)
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  • Reproductive Health (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Communicable Diseases (AREA)
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  • Virology (AREA)
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  • Vascular Medicine (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Otolaryngology (AREA)
LTEP11776738.4T 2010-10-27 2011-10-25 6-(1h-indol-4-il)-4-(5-{[4-(1-metiletil)-1-piperazinil]metil}-1,3-oksazol-2-il)-1h-indazolo polimorfai ir druskos kaip pi3k inhibitoriai, skirti panaudoti pvz. kvėpavimo takų ligų gydymui LT2632921T (lt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB1018124.6A GB201018124D0 (en) 2010-10-27 2010-10-27 Polymorphs and salts
PCT/EP2011/068604 WO2012055846A1 (en) 2010-10-27 2011-10-25 Polymorphs and salts of 6-(1h-indol-4-yl)-4-(5- { [4-(1-methylethyl)-1-pi perazinyl] methyl} -1,3-oxazol-2-yl)-1h-indazole as pi3k inhibitors for use in the treatment of e.g. respiratory disorders

Publications (1)

Publication Number Publication Date
LT2632921T true LT2632921T (lt) 2018-12-27

Family

ID=43365584

Family Applications (1)

Application Number Title Priority Date Filing Date
LTEP11776738.4T LT2632921T (lt) 2010-10-27 2011-10-25 6-(1h-indol-4-il)-4-(5-{[4-(1-metiletil)-1-piperazinil]metil}-1,3-oksazol-2-il)-1h-indazolo polimorfai ir druskos kaip pi3k inhibitoriai, skirti panaudoti pvz. kvėpavimo takų ligų gydymui

Country Status (26)

Country Link
US (1) US8993576B2 (lt)
EP (2) EP3447055A1 (lt)
JP (1) JP5894603B2 (lt)
KR (1) KR101774026B1 (lt)
CN (1) CN103270037B (lt)
AU (1) AU2011322649B2 (lt)
BR (1) BR112013010126B1 (lt)
CA (1) CA2814436C (lt)
CY (1) CY1121248T1 (lt)
DK (1) DK2632921T3 (lt)
EA (1) EA022872B1 (lt)
ES (1) ES2703716T3 (lt)
GB (1) GB201018124D0 (lt)
HR (1) HRP20182059T1 (lt)
HU (1) HUE042754T2 (lt)
IL (1) IL225704A (lt)
LT (1) LT2632921T (lt)
MX (1) MX347619B (lt)
PL (1) PL2632921T3 (lt)
PT (1) PT2632921T (lt)
RS (1) RS58072B1 (lt)
SG (1) SG189179A1 (lt)
SI (1) SI2632921T1 (lt)
TR (1) TR201819939T4 (lt)
WO (1) WO2012055846A1 (lt)
ZA (1) ZA201302480B (lt)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009147190A1 (en) 2008-06-05 2009-12-10 Glaxo Group Limited Novel compounds
US8536169B2 (en) 2008-06-05 2013-09-17 Glaxo Group Limited Compounds
ES2445199T3 (es) 2008-06-05 2014-02-28 Glaxo Group Limited Derivados de benzpirazol como inhibidores de PI3-quinasas
ES2542551T3 (es) 2009-03-09 2015-08-06 Glaxo Group Limited 4-Oxadiazol-2-il-indazoles como inhibidores de PI3 cinasas
SI2899191T1 (sl) 2009-04-30 2017-11-30 Glaxo Group Limited Z oksazolom substituirani indazoli kot PI3-kinazni inhibitorji
ES2602972T3 (es) * 2010-09-08 2017-02-23 Glaxosmithkline Intellectual Property Development Limited Derivados de indazol para su uso en el tratamiento de infección por virus de la gripe
GB201018124D0 (en) 2010-10-27 2010-12-08 Glaxo Group Ltd Polymorphs and salts
EP2878594B1 (en) * 2012-07-27 2018-11-28 Sato Pharmaceutical Co., Ltd. Difluoromethylene compound
KR20210010958A (ko) 2012-11-08 2021-01-28 리젠 파마슈티컬스 소시에떼 아노님 Pde4 억제제 및 pi3 델타 또는 이중 pi3 델타-감마 키나아제 억제제를 함유하는 약제학적 조성물
JP2016537327A (ja) * 2013-10-17 2016-12-01 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドGlaxosmithkline Intellectual Property Development Limited 呼吸器疾患の治療のためのpi3k阻害剤
WO2015055691A1 (en) 2013-10-17 2015-04-23 Glaxosmithkline Intellectual Property Development Limited Pi3k inhibitor for treatment of respiratory disease
GB201509492D0 (en) * 2015-06-02 2015-07-15 Glaxosmithkline Ip Dev Ltd Novel processes

Family Cites Families (138)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9127376D0 (en) 1991-12-24 1992-02-19 Wellcome Found Amidino derivatives
NZ251092A (en) 1992-04-02 1996-12-20 Smithkline Beecham Corp 4-cyano-cyclohexane derivatives; medicaments; used in treating asthma
ZA954940B (en) 1994-06-15 1996-12-17 Wellcome Found Enzyme inhibitors
DE69622166T2 (de) 1995-04-14 2003-04-03 Smithkline Beecham Corp Dosierinhalator für albuterol
MY117948A (en) 1997-01-13 2004-08-30 Glaxo Group Ltd Nitride oxide synthase inhibitors.
DE19723722A1 (de) 1997-05-30 1998-12-10 Schering Ag Nichtsteroidale Gestagene
TW533865U (en) 1997-06-10 2003-05-21 Glaxo Group Ltd Dispenser for dispensing medicament and actuation indicating device
AU9281298A (en) 1997-10-01 1999-04-23 Kyowa Hakko Kogyo Co. Ltd. Benzodioxole derivatives
US6506766B1 (en) 1998-02-13 2003-01-14 Abbott Laboratories Glucocortiocoid-selective antinflammatory agents
JP2002506856A (ja) 1998-03-14 2002-03-05 ビイク グルデン ロンベルク ヒエーミツシエ フアブリーク ゲゼルシヤフト ミツト ベシユレンクテル ハフツング フタラジノンpdeiii/iv阻害剤
GB9811599D0 (en) 1998-05-30 1998-07-29 Glaxo Group Ltd Nitric oxide synthase inhibitors
US6352152B1 (en) 1998-12-18 2002-03-05 Smithkline Beecham Corporation Method and package for storing a pressurized container containing a drug
US6390291B1 (en) 1998-12-18 2002-05-21 Smithkline Beecham Corporation Method and package for storing a pressurized container containing a drug
US6315112B1 (en) 1998-12-18 2001-11-13 Smithkline Beecham Corporation Method and package for storing a pressurized container containing a drug
US6119853A (en) 1998-12-18 2000-09-19 Glaxo Wellcome Inc. Method and package for storing a pressurized container containing a drug
EP1175422A2 (en) 1999-05-04 2002-01-30 Ligand Pharmaceuticals Incorporated Tetracyclic progesterone receptor modulator compounds and methods
ES2165768B1 (es) 1999-07-14 2003-04-01 Almirall Prodesfarma Sa Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen.
CO5180649A1 (es) 1999-09-01 2002-07-30 Abbott Lab Antagonistas de los receptores de los glucocorticoides para el tratamiento de la diabetes para el tratamiento de la diabetes
OA11558A (en) 1999-12-08 2004-06-03 Advanced Medicine Inc Beta 2-adrenergic receptor agonists.
SK287576B6 (sk) 2000-08-05 2011-03-04 Glaxo Group Limited S-fluórmetylester kyseliny 6alfa, 9alfa-difluór-17alfa-[(2- furanylkarboxyl)oxy]-11beta-hydroxy-16alfa-metyl-3-oxo-androsta- 1,4-dién-17beta-karbotiovej, spôsob jeho prípravy, farmaceutický prostriedok s jeho obsahom, jeho použitie a medziprodukty
CA2423251A1 (en) 2000-09-29 2002-04-04 Glaxo Group Limited Morpholin-acetamide derivatives for the treatment of inflammatory diseases
GB0031179D0 (en) 2000-12-21 2001-01-31 Glaxo Group Ltd Nitric oxide synthase inhibitors
US6484903B2 (en) 2001-01-09 2002-11-26 Riverwood International Corporation Carton with an improved dispensing feature in combination with a unique handle
GB0103630D0 (en) 2001-02-14 2001-03-28 Glaxo Group Ltd Chemical compounds
WO2002067683A1 (en) 2001-02-26 2002-09-06 Merck & Co., Inc. Hiv protease inhibitors supported on cation exchange resins for oral administration
WO2002070490A1 (en) 2001-03-08 2002-09-12 Glaxo Group Limited Agonists of beta-adrenoceptors
WO2002076933A1 (en) 2001-03-22 2002-10-03 Glaxo Group Limited Formailide derivatives as beta2-adrenoreceptor agonists
IL158168A0 (en) 2001-04-16 2004-03-28 Tanabe Seiyaku Co 5-membered, nitrogen-containing heterocyclic compounds and pharmaceutical compositions containing the same
AR033290A1 (es) 2001-04-30 2003-12-10 Glaxo Group Ltd Derivados antiinflamatorios de androstano
WO2002100879A1 (en) 2001-06-12 2002-12-19 Glaxo Group Limited Novel anti-inflammatory 17.alpha.-heterocyclic-esters of 17.beta.carbothioate androstane derivatives
CA2452114C (en) 2001-06-26 2010-11-16 Takeda Chemical Industries, Ltd. Tgf-.beta. superfamily production/secretion promoter
ES2438985T3 (es) 2001-09-14 2014-01-21 Glaxo Group Limited Formulación de inhalación que comprende derivados de fenetanolamina para el tratamiento de enfermedades respiratorias
US6653323B2 (en) 2001-11-13 2003-11-25 Theravance, Inc. Aryl aniline β2 adrenergic receptor agonists
WO2003051847A1 (en) 2001-12-19 2003-06-26 Smithkline Beecham P.L.C. (1-h-indazol-3-yl) -amide derivatives as gsk-3 inhibitors
ES2276038T3 (es) 2002-01-14 2007-06-16 Boehringer Ingelheim Pharmaceuticals Inc. Mimeticos de glucocorticoides, metodos para su obtencion, formulaciones farmaceuticas que los contienen y usos de los mismos.
EP1467730A4 (en) 2002-01-22 2010-03-10 Univ California Non-steroid ligands for the glucocorticoid receptor, compositions and uses thereof
TW200306819A (en) 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
GB0204719D0 (en) 2002-02-28 2002-04-17 Glaxo Group Ltd Medicinal compounds
US6903215B2 (en) 2002-03-26 2005-06-07 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
AU2003230700A1 (en) 2002-03-26 2003-10-13 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
DE10215316C1 (de) 2002-04-02 2003-12-18 Schering Ag Chinolin- und Isochinolin-Derivate, ein pharmazeutisches Mittel und ihre Verwendung als Entzündungshemmer
DE60335869D1 (de) 2002-04-11 2011-03-10 Merck Sharp & Dohme 1h-benzo(f)indazol-5-yl-derivate als selektive glucocorticoid-rezeptor-modulatoren
AU2003222841A1 (en) 2002-04-25 2003-11-10 Glaxo Group Limited Phenethanolamine derivatives
US7186864B2 (en) 2002-05-29 2007-03-06 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
US7074806B2 (en) 2002-06-06 2006-07-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
WO2004002480A1 (en) 2002-06-27 2004-01-08 Novo Nordisk A/S Novel glucagon antagonists/inverse agonists
JP4503436B2 (ja) 2002-07-08 2010-07-14 ファイザー・プロダクツ・インク 糖質コルチコイド受容体のモジュレーター
JP2006508042A (ja) 2002-07-18 2006-03-09 ブリストル−マイヤーズ スクイブ カンパニー グルココルチコイド受容体の修飾物質および方法
GB0217225D0 (en) 2002-07-25 2002-09-04 Glaxo Group Ltd Medicinal compounds
US7074809B2 (en) 2002-08-09 2006-07-11 Astrazeneca Ab Compounds
WO2004014370A2 (en) 2002-08-09 2004-02-19 Astrazeneca Ab Oxadiazoles as modulators of metabotropic glutamate receptor-5
KR20050033070A (ko) 2002-08-09 2005-04-08 아스트라제네카 에이비이 메타보트로픽 글루타메이트 수용체-5의 조절제로서[1,2,4]옥사디아졸
US20040224986A1 (en) 2002-08-16 2004-11-11 Bart De Corte Piperidinyl targeting compounds that selectively bind integrins
ATE403648T1 (de) 2002-08-21 2008-08-15 Boehringer Ingelheim Pharma Substituierte dihydrochinoline als glucocorticoid-mmimetika,verfahren zu deren herstellung, pharmazeutische zubereitungen und deren verwendung
GB0220730D0 (en) 2002-09-06 2002-10-16 Glaxo Group Ltd Medicinal compounds
GB0230045D0 (en) 2002-12-23 2003-01-29 Glaxo Group Ltd Compounds
CN100387598C (zh) 2002-09-16 2008-05-14 葛兰素集团有限公司 吡唑并[3,4-b]吡啶化合物及其作为磷酸二酯酶抑制剂的用途
EP1542996A4 (en) 2002-09-20 2009-11-18 Merck & Co Inc OCTAHYDRO-2H-NAPHTOc1,2-F INDOL-4-CARBONSUUREAMIDE DERIVATIVES AS SELECTIVE MODULATORS OF THE GLUCOCORTICOID RECEPTOR
GB0224084D0 (en) 2002-10-16 2002-11-27 Glaxo Group Ltd Novel compounds
US20060205790A1 (en) 2002-10-22 2006-09-14 Coe Diane M Medicinal arylethanolamine compounds
GB0225030D0 (en) 2002-10-28 2002-12-04 Glaxo Group Ltd Medicinal compounds
JP2006503888A (ja) 2002-10-28 2006-02-02 グラクソ グループ リミテッド 呼吸器疾患を治療するためのフェネタノールアミン誘導体
GB0225535D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
GB0225540D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
US7202257B2 (en) 2003-12-24 2007-04-10 Deciphera Pharmaceuticals, Llc Anti-inflammatory medicaments
TWI328009B (en) 2003-05-21 2010-08-01 Glaxo Group Ltd Quinoline derivatives as phosphodiesterase inhibitors
KR20060070486A (ko) 2003-06-13 2006-06-23 젠타리스 게엠베하 포스파티딜이노시톨 3-키나제의 억제 활성을 갖는 화합물및 이의 사용 방법
GB0316290D0 (en) 2003-07-11 2003-08-13 Glaxo Group Ltd Novel compounds
US20050090529A1 (en) 2003-07-31 2005-04-28 Pfizer Inc 3,5 Disubstituted indazole compounds with nitrogen-bearing 5-membered heterocycles, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation
GB0320197D0 (en) 2003-08-28 2003-10-01 Novartis Ag Organic compounds
SI1677795T1 (sl) 2003-10-14 2011-04-29 Glaxo Group Ltd Antagonisti muskarinskega acetilholinskega receptorja
US7563906B2 (en) 2003-10-15 2009-07-21 Ube Industries, Ltd. Indazole derivatives
DK1699512T3 (da) 2003-11-03 2012-09-17 Glaxo Group Ltd Fluiddispenseringsindretning
AR046225A1 (es) 2003-11-04 2005-11-30 Glaxo Group Ltd Compuesto de 8-azoniabiciclo(3.2.1)octano, composicion farmaceutica para el tratamiento de enfermedades mediadas por receptores de acetilcolina muscarinicos que lo comprende y uso del compuesto para preparar dicha composicion
CA2557004A1 (en) 2003-12-19 2005-06-30 Glaxo Group Limited Pyrazolo [3,4-b] pyridine compounds, and their use as phosphodiesterase inhibitors
WO2005077345A1 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Compounds for the treatment of gastro-esophageal reflux disease
WO2005077373A2 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Treatment of gastro-esophageal reflux disease (gerd)
WO2005077368A2 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Treatment of gastro-esophageal reflux disease (gerd)
EP1713810B1 (en) 2004-02-04 2010-12-29 NeuroSearch A/S Diazabicyclic aryl derivatives as nicotinic acetylcholine receptor ligands
WO2005090352A1 (en) 2004-03-16 2005-09-29 Glaxo Group Limited Pyrazolo[3,4-b]pyridine compound, and its use as a pde4 inhibitor
GB0405937D0 (en) 2004-03-16 2004-04-21 Glaxo Group Ltd Compounds
GB0405933D0 (en) 2004-03-16 2004-04-21 Glaxo Group Ltd Compounds
MY144753A (en) 2004-04-27 2011-10-31 Glaxo Group Ltd Muscarinic acetylcholine receptor antagonists
EA200700117A1 (ru) 2004-06-24 2007-06-29 Инсайт Корпорейшн N-замещенные пиперидины и их применение в качестве фармацевтических препаратов
WO2006000401A1 (en) 2004-06-28 2006-01-05 Glaxo Group Limited Substituted oxazines as glucocorticoid receptor modulators
WO2006000398A1 (en) 2004-06-28 2006-01-05 Glaxo Group Limited 2,3-benzoxazin derivatives as non-steroidal glucocorticoid receptor modulators
GB0418045D0 (en) 2004-08-12 2004-09-15 Glaxo Group Ltd Compounds
MX2007004465A (es) 2004-10-19 2007-05-07 Hoffmann La Roche Derivados de quinolina.
MX2007005820A (es) 2004-11-18 2007-07-18 Incyte Corp Inhibidores de deshidrogenasa esteroide hidroxilo 11-beta tipo 1 y metodos de uso de los mismos.
AU2005311826A1 (en) 2004-11-30 2006-06-08 Plexxikon, Inc. Indole derivatives for use as PPAR active compounds
ATE517908T1 (de) 2005-01-10 2011-08-15 Glaxo Group Ltd Androstan-17-alpha-carbonat-derivate zur verwendung bei der behandlung allergischer und entzündlicher zustände
US20090124588A1 (en) 2005-01-10 2009-05-14 Glaxo Group Limited Androstane 17-Alpha-Carbonate for Use in the Treatment of Inflammatory and Allergic Conditions
WO2006089076A2 (en) 2005-02-18 2006-08-24 Neurogen Corporation Thiazole amides, imidazole amides and related analogues
US20060264433A1 (en) 2005-05-23 2006-11-23 Backes Bradley J Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
WO2007011759A2 (en) 2005-07-15 2007-01-25 Kalypsys, Inc. Inhibitors of mitotic kinesin
TW200800946A (en) 2005-08-15 2008-01-01 Astrazeneca Ab Substituted piperazines as metabotropic glutamate receptor antagonists
CA2619881A1 (en) 2005-08-16 2007-02-22 Genzyme Corporation Chemokine receptor binding compounds
AU2007225836A1 (en) 2006-03-10 2007-09-20 Ono Pharmaceutical Co., Ltd. Nitrogenated heterocyclic derivative, and pharmaceutical agent comprising the derivative as active ingredient
EP2007373A4 (en) 2006-03-29 2012-12-19 Foldrx Pharmaceuticals Inc INHIBITION OF ALPHA SYNUCLEINE TOXICITY
US20080032960A1 (en) 2006-04-04 2008-02-07 Regents Of The University Of California PI3 kinase antagonists
GB0608820D0 (en) 2006-05-04 2006-06-14 Piramed Ltd Pharmaceutical compounds
US8492378B2 (en) 2006-08-03 2013-07-23 Takeda Pharmaceutical Company Limited GSK-3β inhibitor
WO2008020229A2 (en) 2006-08-17 2008-02-21 Astrazeneca Ab Antibacterial pyrrolecarboxamides
CN101541758A (zh) 2006-08-25 2009-09-23 艾博特公司 抑制trpv1的吲唑衍生物及其用途
WO2008038136A2 (en) 2006-09-25 2008-04-03 Mutabilis Sa Substituted heterocyclylcarbonylamino-acetic-acid-derivatives as inhibitors of bacterial heptose synthesis, methods for their preparation and biological applications of said inhibitors
AU2007302263A1 (en) 2006-09-29 2008-04-03 Novartis Ag Pyrazolopyrimidines as P13K lipid kinase inhibitors
TWI454262B (zh) 2006-11-02 2014-10-01 Targacept Inc 菸鹼乙醯膽鹼受體亞型選擇性之二氮雜雙環烷類醯胺
GB0701426D0 (en) 2007-01-25 2007-03-07 Univ Sheffield Compounds and their use
US8450348B2 (en) 2007-02-21 2013-05-28 Forma Tm, Llc Derivatives of squaric acid with anti-proliferative activity
JP2010116389A (ja) 2008-10-17 2010-05-27 Bayer Cropscience Ag 殺虫性アリールピロリジン類
US8648069B2 (en) 2007-06-08 2014-02-11 Abbvie Inc. 5-substituted indazoles as kinase inhibitors
EP2170884A2 (en) 2007-06-25 2010-04-07 Boehringer Ingelheim International GmbH Chemical compounds
AR067673A1 (es) 2007-07-26 2009-10-21 Vitae Pharmaceuticals Inc Derivados de 1,3 oxazinan - 2 - ona como inhibidores ciclicos de la 11 beta -hidroxiesteroide deshidrogenasa 1. composiciones farmaceuticas.
US8569292B2 (en) 2008-05-01 2013-10-29 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11β-hydroxysteroid dehydrogenase 1
ES2421537T3 (es) 2008-05-01 2013-09-03 Vitae Pharmaceuticals Inc Inhibidores cíclicos de la 11beta-hidroxiesteroide deshidrogenasa 1
CA2723034A1 (en) 2008-05-01 2009-11-05 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
EP2291373B1 (en) 2008-05-01 2013-09-11 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
ES2445199T3 (es) 2008-06-05 2014-02-28 Glaxo Group Limited Derivados de benzpirazol como inhibidores de PI3-quinasas
US8536169B2 (en) 2008-06-05 2013-09-17 Glaxo Group Limited Compounds
US8163743B2 (en) 2008-06-05 2012-04-24 GlaxoGroupLimited 4-carboxamide indazole derivatives useful as inhibitors of PI3-kinases
WO2009147190A1 (en) 2008-06-05 2009-12-10 Glaxo Group Limited Novel compounds
DE112009001347T5 (de) 2008-06-11 2011-04-21 Hamamatsu Photonics K.K., Hamamatsu Schmelzverbindungsprozess für Glas
PL2324018T3 (pl) 2008-07-25 2014-02-28 Boehringer Ingelheim Int Cykliczne inhibitory dehydrogenazy 11 beta-hydroksysteroidowej typu 1
WO2010127237A2 (en) 2009-04-30 2010-11-04 Boehringer Ingelheim International Gmbh Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
WO2010068287A2 (en) 2008-12-11 2010-06-17 Angion Biomedica Corp. Small molecule modulators of hepatocyte growth factor (scatter factor) activity
WO2010102058A2 (en) 2009-03-04 2010-09-10 Curna, Inc. Treatment of sirtuin 1 (sirt1) related diseases by inhibition of natural antisense transcript to sirt 1
ES2542551T3 (es) * 2009-03-09 2015-08-06 Glaxo Group Limited 4-Oxadiazol-2-il-indazoles como inhibidores de PI3 cinasas
US8680093B2 (en) 2009-04-30 2014-03-25 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
US8343959B2 (en) 2009-04-30 2013-01-01 Abbott Gmbh & Co. Kg N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds suitable for treating disorders that respond to modulation of the serotonin 5-HT6 receptor
UA107080C2 (uk) 2009-04-30 2014-11-25 Сполуки n-феніл(піперазиніл або гомопіперазиніл)бензолсульфонаміду або бензолсульфонілфеніл(піперазину або гомопіперазину), придатні для лікування захворювань, які реагують на модулювання рецептора 5-ht6 серотоніну
WO2010124845A1 (en) 2009-04-30 2010-11-04 Bayer Cropscience Ag Pesticidal arylpyrrolidines
SI2899191T1 (sl) 2009-04-30 2017-11-30 Glaxo Group Limited Z oksazolom substituirani indazoli kot PI3-kinazni inhibitorji
JP2013512878A (ja) 2009-12-03 2013-04-18 グラクソ グループ リミテッド 新規化合物
US20120238571A1 (en) 2009-12-03 2012-09-20 Glaxo Group Limited Indazole derivatives as pi 3-kinase
EP2507223A1 (en) 2009-12-03 2012-10-10 Glaxo Group Limited Benzpyrazole derivatives as inhibitors of p13 kinases
EP2614058B1 (en) 2010-09-08 2015-07-08 GlaxoSmithKline Intellectual Property Development Limited POLYMORPHS AND SALTS OF N-[5-[4-(5-{[(2R,6S)-2,6-DIMETHYL-4-MORPHOLINYL]METHYL}-& xA;1,3-OXAZOL-2-YL)-1H-INDAZOL-6-YL]-2-(METHYLOXY)-3-PYRIDINYL]METHANESULFONAMIDE
ES2602972T3 (es) * 2010-09-08 2017-02-23 Glaxosmithkline Intellectual Property Development Limited Derivados de indazol para su uso en el tratamiento de infección por virus de la gripe
GB201018124D0 (en) 2010-10-27 2010-12-08 Glaxo Group Ltd Polymorphs and salts

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