AR068639A1 - Derivados de biarilo - Google Patents

Derivados de biarilo

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Publication number
AR068639A1
AR068639A1 ARP080104259A ARP080104259A AR068639A1 AR 068639 A1 AR068639 A1 AR 068639A1 AR P080104259 A ARP080104259 A AR P080104259A AR P080104259 A ARP080104259 A AR P080104259A AR 068639 A1 AR068639 A1 AR 068639A1
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AR
Argentina
Prior art keywords
alkyl
optionally substituted
alkynyl
alkenyl
hydroxy
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ARP080104259A
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English (en)
Inventor
Patrizi Mattei
Fabienne Rickin
Luke Green
Olivier Roche
Johannes Aebi
Alfred Binggeli
Hans P Maerki
Guido Hartmann
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Hoffmann La Roche
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Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR068639A1 publication Critical patent/AR068639A1/es

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    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56—Nitrogen atoms
    • C07D211/58—Nitrogen atoms attached in position 4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Se reivindica el compuesto, una composicion farmacéutica y el uso del compuesto para preparar medicamentos. Reivindicacion 1: Compuestos de formula (1) en los que R1 es halogeno, alquilo C1-6, alcoxi C1-6, haloalquilo C1-6, heteroalquilo, alquilsulfanilo C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1-6, cicloalquilo C3-7, cicloalquil C3-7alquilo C1-6; R2 es hidrogeno, alquilo C1-6, haloalquilo C1-6, trimetilsilanil-alquilo C1-6, heteroalquilo, alquenilo C2-6, alquinilo C2-6, hidroxi-alquenilo C3-6, hidroxi-alquinilo C3-6, alcoxi C1-6alquenilo C3-6, alcoxi C1-6alquinilo C3-6, trimetilsilanil-alquinilo C2-6, hidroxi, alcoxi C1-6, haloalcoxi C1-6, heteroalcoxi, cicloalquilo C3-7 opcionalmente sustituido, cicloalquil C3-7alquilo C1-6 opcionalmente sustituido, halogeno, ciano, fenilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, heterociclilo opcionalmente sustituido o fenilmetoxi alcoxi C1-6 opcionalmente sustituido, siempre que el fenilo opcionalmente sustituido no posea un nitro como. sustituyente; R3 es, cuando está unido a un átomo de carbono del anillo, independientemente hidrogeno, alquilo C1-6, haloalquilo C1-6, heteroalquilo, alquenilo C2-6, alquinilo C2-6, hidroxi-alquenilo C3-6, hidroxi-alquinilo C3-6, alcoxi C1-6alquenilo C3-6, alcoxi C1-6alquinilo C3-6, hidroxi, alcoxi C1-6, haloalcoxi C1-6, heteroalcoxi, halogeno, ciano, fenilo opcionalmente sustituido, cicloalquilo C3-7 opcionalmente sustituido, cicloalquil C3-7 alquilo C1-6 opcionalmente sustituido, heteroarilo opcionalmente sustituido, heterociclilo opcionalmente sustituido, fenilalquilo C1-6 opcionalmente sustituido, heteroarilalquilo C1-6 opcionalmente sustituido, heterociclilalquilo C1-6 opcionalmente sustituido, nitro, carboxi, formilo, acilo, alcoxicarbonilo C1-6, carbamoilo, aminocarbonilo sustituido por mono- o di-alquilo C1-6, tioalquilo C1-6, alquilsulfinilo C1-6 o alquilsulfonilo C1-6 o amino opcionalmente sustituido por uno o dos sustituyentes independientemente, seleccionados del grupo que consiste en alquilo C1-6, heteroalquilo, cicloalquilo C3-7 opcionalmente sustituido y heterociclilo opcionalmente sustituido; cuando está unido a un átomo de nitrogeno del anillo, independientemente hidrogeno, alquilo C1-6, haloalquilo C1-6, heteroalquilo, alquenilo C2-6, alquinilo C2-6, hidroxi-alquenilo C3-6, hidroxi-alquinilo C3-6, alcoxi C1-6alquenilo C3-6, alcoxi C1-6alquinilo C3-6, cicloalquilo C3-7 opcionalmente sustituido o cicloalquil C3-7alquilo C1-6 opcionalmente sustituido, heterociclilo opcionalmente sustituido, o opcionalmente sustituido heterociclil alquilo C1-6; m es 0, 1, 2, 3 o 4; la parte cíclica A en la formula (1) es heterociclilo, que es un radical mono-cíclico no aromático de cuatro. a ocho átomos en el anillo, en que uno o dos átomos en el anillo son átomos de nitrogeno, siendo el resto de átomos en el anillo, átomos de carbono; uno de X1, X2 y X3 es C-R4, los otros son independientemente N o C-R5; R4 es fenilo o heteroarilo, que es un radical monocíclico aromático de seis átomos en el anillo, en que uno o dos átomos en el anillo son átomos de nitrogeno, siendo el resto de átomos en el anillo, átomos de carbono, y dicho fenilo y dicho heteroarilo están sustituidos por uno, dos o tres sustituyentes independientemente seleccionados del grupo que consiste en alquilo C1-8, haloalquilo C1-6, alcoxi C1-6, haloalquiloxi C1-6, halogeno y ciano; R5 es hidrogeno, alquilo C1-6, alcoxi C1-6, haloalquilo C1-6 o halogeno; siempre que la parte cíclica A contenga al menos un átomo de nitrogeno, que no está unido directamente al grupo carbonilo o a un heteroátomo; y que la parte cíclica A no contenga un átomo de nitrogeno, que está unido directamente a un heteroátomo; y siempre que la parte cíclica A no sea 2-(pirrolidin-1-il alquil C1-6 opcionalmente sustituido)-pirrolidina-1-ilo; o profármacos o sales farmacéuticamente aceptables de los mismos, en los que, a no ser que se indique de otra manera, el término ôheterocicliloö indica radicales monocíclicos no aromáticos de cuatro a siete átomos en el anillo, en que uno a tres átomos en el anillo son heteroátomos independientemente seleccionados de N, O y S(O)n (en el que n es un numero entero de entre 0 y 2), siendo el resto de átomos en el anillo, átomos de C; el término ôheteroariloö indica un radical mono-cíclico aromático de 5 o 6 átomos en el anillo, con uno a tres heteroátomos en el anillo independientemente seleccionados de entre N, O, y S, siendo el resto de átomos en el anillo, átomos de C; el término ôcicloalquilo C3-7 opcionalmente sustituidoö indica un cicloalquilo C3-7 opcionalmente sustituido por uno a tres sustituyentes independientemente seleccionados del grupo que consiste en alquilo C1-6, haloalquilo C1-6, heteroalquilo, alquenilo C2-6, alquinilo C2-6, hidroxi-alquenilo C3-6, hidroxi-alquinilo C3-6, alcoxi C1-6alquenilo C3-6, alcoxi C1-6alquinilo C3-6, hidroxi, alcoxi C1-6, haloalcoxi C1-6, heteroalcoxi, cicloalquilo C3-7, cicloalquil C3-7 alquilo C1-6, halogeno, ciano, nitro, amino, amino sustituido por mono- o di-alquilo C1-6, carboxi, formilo, acilo, alcoxi-carbonilo C1-6, carbamoilo, aminocarbonilo sustituido por mono- o di-alquilo C1-6, tioalquilo C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1-6 y acilamino; el término ôfenilo opcionalmente sustituidoö indica un fenilo opcionalmente sustituido por uno a tres sustituyentes independientemente seleccionado del grupo que consiste en alquilo C1-6, haloalquilo C1-6, heteroalquilo, alquenilo C2-6, alquinilo C2-6, hidroxi-alquenilo C3-6, hidroxi-alquinilo C3-6, alcoxi C1-6alquenilo C3-6, alcoxi C1-6alquinilo C3-6, hidroxi, alcoxi C1-6, haloalcoxi C1-6, heteroalcoxi, cicloalquilo C3-7, cicloalquil C3-7 alquilo C1-6, halogeno, ciano, nitro, amino, amino sustituido por mono- o di-alquilo C1-6, carboxi, formilo, acilo, alcoxicarbonilo C1-6, carbamoilo, aminocarbonilo sustituido por mono- o di-alquilo C1-6, , tioalquilo C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1-6 y acilamino; el término ôheterociclilo opcionalmente sustituidoö indica un heterociclilo opcionalmente sustituido por uno a tres sustituyentes independientemente seleccionados del grupo que consiste en alquilo C1-6, haloalquilo C1-6, heteroalquilo, alquenilo C2-6, alquinilo C2-6, hidroxi-alquenilo C3-6, hidroxi-alquinilo C3-6, alcoxi C1-6alquenilo C3-6, alcoxi C1-6alquinilo C3-6, hidroxi, alcoxi C1-6, haloalcoxi C1-6, heteroalcoxi, cicloalquilo C3-7, cicloalquil C3-7 alquilo C1-6, halogeno, ciano, nitro, amino, amino sustituido por mono- o di-alquilo C1-6, carboxi, formilo, acilo, alcoxicarbonilo C1-6, carbamoilo, aminocarbonilo sustituido por mono- o di-alquilo C1-6, tioalquilo C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1-6 y acilamino; el término ôheteroarilo opcionalmente sustituidoö indica un heteroarilo opcionalmente sustituido por uno a tres sustituyentes independientemente seleccionados del grupo que consiste en alquilo C1-6, haloalquilo C1-6, heteroalquilo, alquenilo C2-6, alquinilo C2-6, hidroxi-alquenilo C3-6, hidroxi-alquinilo C3-6, alcoxi C1-6alquenilo C3-6, alcoxi C1-6alquinilo C3-6, hidroxi, alcoxi C1-6, haloalcoxi C1-6, heteroalcoxi, cicloalquilo C3-7, cicloalquil C3-7 alquilo C1-6, halogeno, ciano, nitro, amino, amino sustituido por mono- o di-alquilo C1-6, carboxi, formilo, acilo, alcoxicarbonilo C1-6, carbamoilo, aminocarbonilo sustituido por mono- o di-alquilo C1-6, tioalquilo C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1-6 y acilamino; el término ôheteroalquiloö indica alquilo C1-6 sustituido por uno o más sustituyentes seleccionados independientemente del grupo que consiste en nitro, hidroxi, ciano, alcoxi C1-6, formilo, acilo, carboxilo, tioalquilo C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1-6, carbamoilo, amino y amino sustituido por mono- o di-alquilo C1-6; el término ôheteroalcoxiö indica alcoxi C1-6 sustituido por uno o más sustituyentes seleccionados independientemente de entre el grupo que consiste en nitro, hidroxi, ciano, alcoxi C1-6, formilo, acilo, carboxilo, tioalquilo C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1-6, carbamoilo, amino y amino sustituido por mono- o di-alquilo C1-6; el término ôaciloö indica R-C(O)-, en el que R es alquilo C1-6, haloalquilo C1-6, cicloalquilo C3-7 o cicloalquil C3-7 alquilo C1-6; el término ôpirrolidin-1-ilo opcionalmente sustituidoö indica un pirrolidin-1-ilo opcionalmente sustituido por uno a tres sustituyentes independientemente seleccionados del grupo que consiste en alquilo C1-6, haloalquilo C1-6, heteroalquilo, alquenilo C2-6, alquinilo C2-6, hidroxi-alquenilo C3-6, hidroxi-alquinilo C3-6, alcoxi C1-6alquenilo C3-6, alcoxi C1-6alquinilo C3-6, hidroxi, alcoxi C1-6, haloalcoxi C1-6, heteroalcoxi, cicloalquilo C3-7, cicloalquil C3-7 alquilo C1-6, halogeno, ciano, nitro, amino, amino sustituido por mono- o di-alquilo C1-6, carboxi, formilo, acilo, alcoxicarbonilo C1-6, carbamoilo, aminocarbonilo sustituido por mono- o di-alquilo C1-6, tioalquilo C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1-6 y acilamino.
ARP080104259A 2007-10-01 2008-09-30 Derivados de biarilo AR068639A1 (es)

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US (1) US8153805B2 (es)
EP (1) EP2205583A2 (es)
JP (1) JP2010540584A (es)
KR (1) KR20100050570A (es)
CN (1) CN101801952A (es)
AR (1) AR068639A1 (es)
AU (1) AU2008307158A1 (es)
BR (1) BRPI0817935A2 (es)
CA (1) CA2700691A1 (es)
CL (1) CL2008002911A1 (es)
MX (1) MX2010003621A (es)
PE (1) PE20090775A1 (es)
RU (1) RU2010116821A (es)
TW (1) TW200920368A (es)
WO (1) WO2009043747A2 (es)

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CA2687931C (en) 2007-05-31 2016-05-24 Boehringer Ingelheim International Gmbh Ccr2 receptor antagonists and uses thereof
US8242145B2 (en) * 2008-02-14 2012-08-14 Panmira Pharmaceuticals, Llc Cyclic diaryl ether compounds as antagonists of prostaglandin D2 receptors
WO2009145989A2 (en) * 2008-04-02 2009-12-03 Amira Pharmaceuticals, Inc. Aminoalkylphenyl antagonists of prostaglandin d2 receptors
US8071807B2 (en) * 2008-07-03 2011-12-06 Panmira Pharmaceuticals, Llc Antagonists of prostaglandin D2 receptors
US8383654B2 (en) 2008-11-17 2013-02-26 Panmira Pharmaceuticals, Llc Heterocyclic antagonists of prostaglandin D2 receptors
EP2375904B1 (en) * 2008-12-09 2014-05-28 Merck Sharp & Dohme Corp. Biaryl carboxamides
EA020548B1 (ru) 2008-12-19 2014-12-30 Бёрингер Ингельхайм Интернациональ Гмбх Циклические пиримидин-4-карбоксамиды в качестве антагонистов рецептора ccr2, предназначенные для лечения воспаления, астмы и хозл
US8729095B2 (en) 2009-08-28 2014-05-20 Daiichi Sankyo Company, Limited 3-(biaryloxy)propionic acid derivatives for prevention and/or treatment of thromboembolic diseases
US8471004B2 (en) 2009-10-07 2013-06-25 Hoffman-La Roche Inc. Bicyclic compounds
NZ599770A (en) 2009-12-17 2014-06-27 Boehringer Ingelheim Int New ccr2 receptor antagonists and uses thereof
JP5658272B2 (ja) * 2009-12-17 2015-01-21 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 Ｃｃｒ２の新規アンタゴニスト及びこれらの使用
CA2782085A1 (en) 2010-01-06 2011-07-14 Panmira Pharmaceuticals, Llc Dp2 antagonist and uses thereof
WO2011141477A1 (en) 2010-05-12 2011-11-17 Boehringer Ingelheim International Gmbh New ccr2 receptor antagonists, method for producing the same, and use thereof as medicaments
WO2011141474A1 (en) 2010-05-12 2011-11-17 Boehringer Ingelheim International Gmbh Novel ccr2 receptor antagonists, method for producing the same, and use thereof as medicaments
US8841313B2 (en) 2010-05-17 2014-09-23 Boehringer Ingelheim International Gmbh CCR2 antagonists and uses thereof
WO2011147772A1 (en) 2010-05-25 2011-12-01 Boehringer Ingelheim International Gmbh Ccr2 receptor antagonists
US8962656B2 (en) 2010-06-01 2015-02-24 Boehringer Ingelheim International Gmbh CCR2 antagonists
JP5786258B2 (ja) * 2011-07-15 2015-09-30 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 新規かつ選択的なｃｃｒ２拮抗薬
WO2015175855A1 (en) * 2014-05-16 2015-11-19 Emory University Chemokine cxcr4 and ccr5 receptor modulators and used related thereto
US10758525B2 (en) 2015-01-22 2020-09-01 MyoKardia, Inc. 4-methylsulfonyl-substituted piperidine urea compounds
BR112017028492B1 (pt) 2015-07-02 2023-12-26 Centrexion Therapeutics Corporation Citrato de (4-((3r,4r)-3-metoxitetra-hidro-piran-4- ilamino)piperidin-1-il) (5- metil-6-(((2r, 6s)-6-(p-tolil) tetra-hidro-2h-piran-2-il)metilamino)pirimidin-4-il) metanona, seu uso e seu método de preparação, e composição farmacêutica
CN116731101A (zh) 2016-06-01 2023-09-12 雅斯娜 用于治疗多种疾病的n-己酸-l-酪氨酸-l-异亮氨酸-(6)-氨基己酰胺的衍生物
US20180206726A1 (en) 2016-12-07 2018-07-26 Progenity Inc. Gastrointestinal tract detection methods, devices and systems
CA3045310A1 (en) 2016-12-14 2018-06-21 Progenity, Inc. Treatment of a disease of the gastrointestinal tract with a chemokine/chemokine receptor inhibitor
WO2020106754A1 (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

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2538950A1 (de) 1975-09-02 1977-03-03 Basf Ag Verfahren zur herstellung von 2,6- dichlor-nicotinsaeuren
JPS5334790A (en) * 1976-09-13 1978-03-31 Yamanouchi Pharmaceut Co Ltd Novel nitrosourea derivatives and their preparation
WO1994022826A1 (en) * 1993-04-07 1994-10-13 Otsuka Pharmaceutical Co., Ltd. Peripheral vasodilating agent containing n-acylated 4-amino piperidine derivatives as active ingredients
RU2299206C9 (ru) * 1999-05-04 2007-11-20 Шеринг Корпорейшн Производные пиперазина, фармацевтические композиции, их содержащие, и применение в качестве антагонистов ccr5
US6689765B2 (en) * 1999-05-04 2004-02-10 Schering Corporation Piperazine derivatives useful as CCR5 antagonists
AR033517A1 (es) 2000-04-08 2003-12-26 Astrazeneca Ab Derivados de piperidina, proceso para su preparacion y uso de estos derivados en la fabricacion de medicamentos
US20020045613A1 (en) * 2000-04-27 2002-04-18 Heinz Pauls 1-aroyl-piperidinyl benzamidines
CN1182114C (zh) * 2000-05-01 2004-12-29 先灵公司 用作ccr5拮抗剂的哌嗪衍生物
US6670364B2 (en) * 2001-01-31 2003-12-30 Telik, Inc. Antagonists of MCP-1 function and methods of use thereof
ATE394371T1 (de) * 2001-03-20 2008-05-15 Serono Lab Pyrrolidinesterderivate mit oxytocinmodulierender wirkung
AR036366A1 (es) * 2001-08-29 2004-09-01 Schering Corp Derivados de piperidina utiles como antagonistas de ccr5, composiciones farmaceuticas, el uso de dichos derivados para la fabricación de un medicamento y un kit
GB0223223D0 (en) * 2002-10-07 2002-11-13 Novartis Ag Organic compounds
ATE552253T1 (de) 2002-11-08 2012-04-15 Novartis Int Pharm Ltd 3-substituierte-6-aryl- pyridin derivate als liganden für c5a-rezeptoren
US7498346B2 (en) 2003-12-11 2009-03-03 Genzyme Corporation Chemokine receptor binding compounds
PL1735278T3 (pl) * 2004-04-01 2010-06-30 Lilly Co Eli Związki receptora histaminowego H3, wytwarzanie i zastosowania terapeutyczne
GB0418830D0 (en) * 2004-08-24 2004-09-22 Astrazeneca Ab Novel compounds
US7820699B2 (en) * 2005-04-27 2010-10-26 Hoffmann-La Roche Inc. Cyclic amines
US20060258672A1 (en) * 2005-05-13 2006-11-16 Joseph Barbosa Multicyclic compounds and methods of their use
JP2009533416A (ja) * 2006-04-12 2009-09-17 ファイザー・リミテッド ケモカインｃｃｒ５受容体の調節剤としてのピロリジン誘導体
EP2099454A4 (en) * 2006-11-17 2010-11-10 Abbott Lab AMINOPYRROLIDINES AS CHEMOKINE RECEPTOR ANTAGONISTS
CN101255134A (zh) * 2008-04-08 2008-09-03 温州医学院 芳基吡啶类化合物及其药物用途

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