BR9813938A - Compostos terapeuticamente ativos baseados na substituição bioisóstera de indazol por catecol em inibidores de pde4 - Google Patents

Compostos terapeuticamente ativos baseados na substituição bioisóstera de indazol por catecol em inibidores de pde4

Info

Publication number
BR9813938A
BR9813938A BR9813938-0A BR9813938A BR9813938A BR 9813938 A BR9813938 A BR 9813938A BR 9813938 A BR9813938 A BR 9813938A BR 9813938 A BR9813938 A BR 9813938A
Authority
BR
Brazil
Prior art keywords
diseases
catechol
indazole
therapeutically active
compound
Prior art date
Application number
BR9813938-0A
Other languages
English (en)
Inventor
Anthony Marfat
Original Assignee
Pfizer Prod Inc
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 Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of BR9813938A publication Critical patent/BR9813938A/pt

Links

Classifications

    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/525—Isoalloxazines, e.g. riboflavins, vitamin B2
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P11/04—Drugs for disorders of the respiratory system for throat disorders
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P27/16—Otologicals
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Communicable Diseases (AREA)
  • Otolaryngology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Patente de Invenção: <B>"COMPOSTOS TERAPEUTICAMENTE ATIVOS BASEADOS NA SUBSTITUIçãO BIOISóSTERA DE INDAZOL POR CATECOL EM INIBIDORES DE PDE4"<D>. São descritas composições de matéria terapeuticamente ativas que são úteis no tratamento ou prevenção de doenças e condições compreendendo doenças inflamatórias, incluindo inflamação das articulações, doença de Crohn, e doença inflamatória do intestino; doenças respiratórias tais como doença pulmonar crónica obstrutiva (COPD) incluindo asma, bronquite crónica, e enfisema pulmonar; doenças infecciosas incluindo choque endotóxico e síndrome do choque tóxico; doenças imonológicas incluindo lúpus eritematoso sistêmico e psoríase; e outras doenças incluindo doenças de reabsorção dos ossos e danos de reperfusão; onde a referida composição de matéria compreende um composto que é um inibidor de fosfodiesterase isozima 4 (PDE4) e em que um componente essencial da estrutura química global do referido composto é um indazol, e em que o referido indazol constitui uma substituição bioisostérica de um componente catecol ou derivado funcional do mesmo em um composto conhecido possuindo a mesma referida atividade terapêutica e os mesmos restantes referidos componentes da sua estrutura química global. Incluídos estão compostos de Fórmula (IA) ou (IB): onde R²~ a~ e R²~ b~ são selecionados independentemente do grupo consistindo essencialmente em hidrogênio e dos substituintes seguidamente enumerados, contanto que um, mas não ambos R²~ a~ e R²~ b~ sejam selecionados independentemente como hidrogênio, onde os referidos substituintes compreendem porções incluindo as seguintes: (IC), (ID), (IE), (IF), (IIA), (IIB), (IIC), (IID), (IIE), (IIF), (IIG), (IIH), (III), (IIIA), (IIIB), (IIIC), (IIID), (IIIE), (IIIF), (IIIG), (IIIH), (IIII), (IIIJ), (IIIK), (IIIL), (IIIM), (IIIN), (IIIO), (IIIP), (IIIQ), (IIIR), (IIIS), (IIIT), (IV), (VA), (VB); (VC), (VD), (VE~ a~), (VE), (VF), (VG), (VH), (VI), (VJ), (VK), (VL), (VM).
BR9813938-0A 1997-11-04 1998-10-09 Compostos terapeuticamente ativos baseados na substituição bioisóstera de indazol por catecol em inibidores de pde4 BR9813938A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US6416097P 1997-11-04 1997-11-04
PCT/IB1998/001579 WO1999023076A1 (en) 1997-11-04 1998-10-09 Therapeutically active compounds based on indazole bioisostere replacement of catechol in pde4 inhibitors

Publications (1)

Publication Number Publication Date
BR9813938A true BR9813938A (pt) 2000-09-26

Family

ID=22053970

Family Applications (1)

Application Number Title Priority Date Filing Date
BR9813938-0A BR9813938A (pt) 1997-11-04 1998-10-09 Compostos terapeuticamente ativos baseados na substituição bioisóstera de indazol por catecol em inibidores de pde4

Country Status (34)

Country Link
US (2) US6716978B2 (pt)
EP (1) EP1040100A1 (pt)
JP (1) JP2001521925A (pt)
KR (1) KR20010031783A (pt)
CN (1) CN1281441A (pt)
AP (1) AP1122A (pt)
AR (1) AR016413A1 (pt)
AU (1) AU754184B2 (pt)
BG (1) BG104391A (pt)
BR (1) BR9813938A (pt)
CA (1) CA2309175A1 (pt)
CZ (1) CZ20001623A3 (pt)
DZ (1) DZ2639A1 (pt)
EA (1) EA200000385A1 (pt)
HN (1) HN1998000172A (pt)
HR (1) HRP20000262A2 (pt)
HU (1) HUP0100330A3 (pt)
ID (1) ID24942A (pt)
IL (1) IL135714A0 (pt)
IS (1) IS5452A (pt)
MA (1) MA26562A1 (pt)
NO (1) NO20002127L (pt)
NZ (1) NZ503995A (pt)
OA (1) OA11353A (pt)
PA (1) PA8462601A1 (pt)
PE (1) PE131099A1 (pt)
PL (1) PL340799A1 (pt)
SK (1) SK6262000A3 (pt)
TN (1) TNSN98199A1 (pt)
TR (1) TR200001256T2 (pt)
UY (1) UY25232A1 (pt)
WO (1) WO1999023076A1 (pt)
YU (1) YU25400A (pt)
ZA (1) ZA9810042B (pt)

Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU754734B2 (en) * 1997-11-04 2002-11-21 Pfizer Products Inc. Indazole bioisostere replacement of catechol in therapeutically active compounds
IL126745A (en) * 1997-11-04 2003-09-17 Pfizer Prod Inc Methods of preparing 4-cyano-4- (substituted indazole) cyclohexanecarboxylic acids useful as pde4 inhibitors
UA71971C2 (en) 1999-06-04 2005-01-17 Agoron Pharmaceuticals Inc Diaminothiazoles, composition based thereon, a method for modulation of protein kinases activity, a method for the treatment of diseases mediated by protein kinases
US7141581B2 (en) 1999-07-02 2006-11-28 Agouron Pharmaceuticals, Inc. Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use
TWI262914B (en) 1999-07-02 2006-10-01 Agouron Pharma Compounds and pharmaceutical compositions for inhibiting protein kinases
PE20010306A1 (es) * 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
YU54202A (sh) 2000-01-18 2006-01-16 Agouron Pharmaceuticals Inc. Jedinjenja indazola, farmaceutske smeše i postupci za stimulisanje i inhibiranje ćelijske proliferacije
MXPA02010222A (es) 2000-04-18 2003-05-23 Agouron Pharma Pirazoles para inhibir proteina cinasa.
US6897231B2 (en) * 2000-07-31 2005-05-24 Signal Pharmaceuticals, Inc. Indazole derivatives as JNK inhibitors and compositions and methods related thereto
US7211594B2 (en) * 2000-07-31 2007-05-01 Signal Pharmaceuticals, Llc Indazole compounds and compositions thereof as JNK inhibitors and for the treatment of diseases associated therewith
ES2427930T3 (es) * 2001-05-23 2013-11-04 Mitsubishi Tanabe Pharma Corporation Composición terapéutica para el tratamiento regenerativo de enfermedades de los cartílagos
JP2006508996A (ja) * 2002-11-27 2006-03-16 アルタナ　ファルマ　アクチエンゲゼルシャフト 悪液質の治療における使用のための、ｐｄｅ４及びｐｄｅ３／４インヒビター
US7135575B2 (en) 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
JP2005089457A (ja) * 2003-09-03 2005-04-07 Yung Shin Pharmaceutical Industry Co Ltd 骨成長を促進するまたは骨吸収を阻害するための薬剤組成物
US6984652B2 (en) 2003-09-05 2006-01-10 Warner-Lambert Company Llc Gyrase inhibitors
RS53543B1 (en) * 2004-03-03 2015-02-27 Takeda Gmbh NEW HYDROXY-6-HETEROARYLPHENANTRIDINES AND THEIR USE AS PDE4 INHIBITORS
US7432266B2 (en) * 2004-10-15 2008-10-07 Memory Pharmaceuticals Corporation Phosphodiesterase 4 inhibitors
US7601847B2 (en) 2004-10-26 2009-10-13 Wyeth Preparation and purification of 4-(indazol-3-yl)phenols
US20070004777A1 (en) * 2005-03-23 2007-01-04 Bhagwat Shripad S Methods for treating or preventing acute myelogenous leukemia
EP1928866A1 (en) 2005-09-05 2008-06-11 Ranbaxy Laboratories Limited Substituted indazoles as inhibitors of phosphodiesterase type-iv
US7915286B2 (en) 2005-09-16 2011-03-29 Ranbaxy Laboratories Limited Substituted pyrazolo [3,4-b] pyridines as phosphodiesterase inhibitors
US7645752B2 (en) 2006-01-13 2010-01-12 Wyeth Llc Sulfonyl substituted 1H-indoles as ligands for the 5-hydroxytryptamine receptors
JP5131990B2 (ja) 2006-01-31 2013-01-30 アレイ バイオファーマ、インコーポレイテッド キナーゼ阻害剤およびその使用方法
AU2008224541B2 (en) 2007-03-14 2013-08-22 Sun Pharmaceutical Industries Limited Pyrazolo (3, 4-b) pyridine derivatives as phosphodiesterase inhibitors
US8877816B2 (en) * 2007-11-21 2014-11-04 Decode Genetics Ehf 4-(or 5-) substituted catechol derivatives
JP5216912B2 (ja) 2008-04-29 2013-06-19 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｃｃｒ１受容体拮抗薬としてのインダゾール化合物
WO2009137338A1 (en) 2008-05-06 2009-11-12 Boehringer Ingelheim International Gmbh Pyrazole compounds as ccr1 antagonists
JP5507567B2 (ja) 2008-09-26 2014-05-28 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｃｃｒ１受容体拮抗薬としてのアザインダゾール化合物
CA2778060A1 (en) 2009-10-21 2011-04-28 Boehringer Ingelheim International Gmbh Indazole and pyrazolopyridine compounds as ccr1 receptor antagonists
WO2011056440A1 (en) 2009-10-27 2011-05-12 Boehringer Ingelheim International Gmbh Heterocyclic compounds as ccr1 receptor antagonists
EP2509952A1 (en) * 2009-12-08 2012-10-17 Boehringer Ingelheim International GmbH Process for synthesis of intermediates useful for making substituted indazole and azaindazole compounds
WO2011076878A1 (en) * 2009-12-23 2011-06-30 Palau Pharma, S.A. Aminoalkylpyrimidine derivatives as histamine h4 receptor antagonists
EP2563787B1 (en) 2010-04-30 2014-11-26 Boehringer Ingelheim International GmbH Azaindazole amide compounds as ccr1 receptor antagonists
CN102958927A (zh) 2010-05-12 2013-03-06 Abbvie公司 激酶的吲唑抑制剂
JP5684406B2 (ja) 2010-12-23 2015-03-11 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｃｃｒ１受容体アンタゴニストとしてのピラゾロピペリジン化合物
TW201607923A (zh) 2014-07-15 2016-03-01 歌林達有限公司 被取代之氮螺環（４．５）癸烷衍生物
SI3169666T1 (en) 2014-07-15 2018-08-31 Gruenenthal Gmbh SUBSTITUTED DERIVATIVES AZASPIRO (4.5) DECAN
WO2019147824A1 (en) 2018-01-26 2019-08-01 Progenity, Inc. Treatment of a disease of the gastrointestinal tract with a pde4 inhibitor
WO2020106750A1 (en) 2018-11-19 2020-05-28 Progenity, Inc. Methods and devices for treating a disease with biotherapeutics
WO2021119482A1 (en) 2019-12-13 2021-06-17 Progenity, Inc. Ingestible device for delivery of therapeutic agent to the gastrointestinal tract
US11457370B2 (en) 2020-12-11 2022-09-27 Hewlett Packard Enterprise Development Lp System and method for seamless live upgrade of access points using neighbor data
IL304014A (en) 2020-12-30 2023-08-01 Tyra Biosciences Inc Indazole compounds as kinase inhibitors

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2064304A1 (de) * 1970-12-29 1972-07-20 Agfa-Gevaert Ag, 5090 Leverkusen Lichtempfindliches farbfotografisches Material
AU649421B2 (en) * 1990-05-18 1994-05-26 Sanofi-Aventis Deutschland Gmbh Isoxazole-4-carboxamides and hydroxyalkylidene-cyanoacetamides, drugs containing these compounds and use of such drugs
US5440038A (en) * 1993-12-07 1995-08-08 Miles Inc. Process for the purification of substituted 4-amino-1,2,4-triazine-5-ones
US6005118A (en) * 1996-05-03 1999-12-21 Caron; Stephane Methods of preparing 4-cyano-4 (substituted indazole) cyclohexane-carboxylic acids useful as PDE4 inhibitors
AP1147A (en) * 1996-05-03 2003-02-25 Pfizer Substituted indazole derivatives and related compounds.
IL127036A (en) * 1996-06-25 2001-06-14 Pfizer History of Inverted Indazol and Phdephodesterase (PDE) IV and TNF-Containing Pharmaceuticals Containing Them
EP0816357B1 (en) * 1996-06-27 2002-01-09 Pfizer Inc. Substituted indazole derivatives
EA002113B1 (ru) * 1996-09-04 2001-12-24 Пфайзер Инк. Производные индазола и их использование в качестве ингибиторов фосфодиэстеразы (фдэ) типа iv и продуцирования фактора некроза опухоли (фно)
ES2172882T3 (es) * 1997-05-08 2002-10-01 Pfizer Prod Inc Procedimientos y productos intermedios para la preparacion de derivados indazol sustituidos.
AU754734B2 (en) * 1997-11-04 2002-11-21 Pfizer Products Inc. Indazole bioisostere replacement of catechol in therapeutically active compounds

Also Published As

Publication number Publication date
JP2001521925A (ja) 2001-11-13
NZ503995A (en) 2003-02-28
TR200001256T2 (tr) 2000-11-21
ZA9810042B (en) 2000-05-03
NO20002127L (no) 2000-07-03
DZ2639A1 (fr) 2003-03-08
MA26562A1 (fr) 2004-12-20
PL340799A1 (en) 2001-02-26
AU9277798A (en) 1999-05-24
NO20002127D0 (no) 2000-04-26
AR016413A1 (es) 2001-07-04
HN1998000172A (es) 1999-01-08
US6716978B2 (en) 2004-04-06
PE131099A1 (es) 1999-12-17
OA11353A (en) 2003-12-19
UY25232A1 (es) 2000-12-29
KR20010031783A (ko) 2001-04-16
AU754184B2 (en) 2002-11-07
EP1040100A1 (en) 2000-10-04
US20030158189A1 (en) 2003-08-21
AP1122A (en) 2002-11-29
BG104391A (en) 2000-12-29
IS5452A (is) 2000-04-14
SK6262000A3 (en) 2002-03-05
YU25400A (sh) 2003-07-07
WO1999023076A1 (en) 1999-05-14
HUP0100330A2 (hu) 2002-02-28
CZ20001623A3 (cs) 2001-08-15
TNSN98199A1 (fr) 2005-03-15
US20020058687A1 (en) 2002-05-16
CN1281441A (zh) 2001-01-24
EA200000385A1 (ru) 2000-10-30
AP9801376A0 (en) 1998-12-31
PA8462601A1 (es) 2000-05-24
HUP0100330A3 (en) 2002-03-28
HRP20000262A2 (en) 2000-10-31
ID24942A (id) 2000-08-31
IL135714A0 (en) 2001-05-20
CA2309175A1 (en) 1999-05-14

Similar Documents

Publication Publication Date Title
BR9813938A (pt) Compostos terapeuticamente ativos baseados na substituição bioisóstera de indazol por catecol em inibidores de pde4
BR0307409A (pt) Compostos de hidrazida de ácido 2-furanocarboxìlico, composições farmacêuticas contendo os mesmos e uso dos mesmos para preparação de um agente preventivo ou terapêutico
BRPI0409227B8 (pt) &#34;composto, composição farmacêutica, uso de um composto e processo para a preparação de um composto de fórmula (i)&#34;
BR9812176A (pt) Antagonista de receptor il-8
ME00195B (me) 4&#39;-supstituisani nukleozidi
DK1487829T3 (da) Thiadizolylpiperazinderivater, der er nyttige til behandling eller forebyggelse af smerte
BR9910849A (pt) Composto, processo para a profilaxia ou tratamento de uma condição clìnica em um mamìfero, tal como um humano, formulação farmacêutica, uso de um composto, processo para preparação do composto, e, derivado protegido.
BRPI0507877A (pt) derivados de formamida, composição farmacêutica, uso dos mesmos e combinação
BR9813926A (pt) Substituição de bioisóstero de catecol por indazol em compostos terapeuticamente ativos
BR0307429A (pt) Composto, uso do mesmo, composição farmacêutica, e, método para o tratamento de distúrbios ou doenças relacionadas com receptor de histamina h3
BRPI0516825A (pt) inibição da protease ns3-ns4a do vìrus da hepatite c (vhc)
BR9913592A (pt) Compostos, processo de preparação dos compostos, e, composições farmacêuticas
BR0212378A (pt) Inibidores de 17beta-hidroxiesteróide desidrogenase tipo 3 para o tratamento de doenças dependentes de androgênio
BRPI0417687A (pt) derivados de benzenossulfonilamino-piridin-2-ila e compostos relacionados como inibidores de 11-beta-hidroxiesteróide desidrogenase tipo 1 (11-beta-hsd-1) para o tratamento de diabetes e obesidade
BR9814340A (pt) Derivados de indol como inibidores de fator xa
BR9806060A (pt) Composto, composição farmacêutica e processos para tratar um paciente sofrendo de um estado doentio, para inibir o fator xa, e, para inibir a formação de trombina.
BRPI0408369A (pt) derivados de indol úteis para o tratamento de doenças
BR9809648A (pt) Derivados de piperazinil-benzil-tetrazol antiinflamatórios e intermediários dos mesmos
BR0015821A (pt) Derivados de pirimidina
BR0308144A (pt) Composto, composição farmacêutica, uso de um composto, e, processo para a preparação de um composto
BR0012478A (pt) Derivados de aminotiazóis, sua preparação e composição farmacêuticas contendo os mesmos
BR9814376A (pt) Composto ou um pró-medicamento correspondente, ou um sal farmaceuticamente aceitável ou solvato de um tal composto ou um pró-medicamento deste, uso destes, composição farmacêutica, processo para o tratamento de um paciente humano ou animal não humano sofrendo de, ou sujeito a, condições que podem ser melhoradas pela admnistração de um inibidor da adesão celular mediada por &amp;4ß1, e, resina
PE45195A1 (es) Derivado de aminoacido, procedimiento para su preparacion y composicion farmaceutica que lo contiene
BR0105787A (pt) Composição farmacêutica, uso de um composto farmacêutico, método para tratamento de distúrbios, composto farmacêutico e método para confeccionar um composto farmacêutico
ITMI20042475A1 (it) Uso di derivati tiazolidinonici come agenti terapeutici

Legal Events

Date Code Title Description
B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B15K Others concerning applications: alteration of classification

Free format text: ALTERADA DE INT.CL.8: C07D 231/56, A61K 31/416, A61P 1/04, A61P 3/10, A61P 11/00, A61P 11/06 A61P 13/12, A61P 17/00, A61P 17/06, A61P 19/00, A61P 19/02, A61P 19/08, A61P 19/10, A61P 29/00, A61P 31/04, A61P 31/12, A61P 31/16, A61P 31/18, A61P 35/02, A61P 37/06, A61P 37/08

Ipc: C07D 231/56 (2007.01), A61K 31/416 (2007.01), A61P

B09B Patent application refused [chapter 9.2 patent gazette]

Free format text: INDEFIRO O PRESENTE PEDIDO DE PATENTE DE ACORDO COM ART. 8O DA LPI.