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AR054830A1 - Derivados de indol -3-il-espiro-piperidina como antagonista del receptor v1a - Google Patents

Derivados de indol -3-il-espiro-piperidina como antagonista del receptor v1a

Info

Publication number
AR054830A1
AR054830A1 ARP060102988A ARP060102988A AR054830A1 AR 054830 A1 AR054830 A1 AR 054830A1 AR P060102988 A ARP060102988 A AR P060102988A AR P060102988 A ARP060102988 A AR P060102988A AR 054830 A1 AR054830 A1 AR 054830A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
halogen
nririi
aryl
Prior art date
Application number
ARP060102988A
Other languages
English (en)
Inventor
Caterina Bissantz
Christophe Grundschober
Hasane Ratni
Mark Rogers-Evans
Patrick Schnider
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR054830A1 publication Critical patent/AR054830A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10Spiro-condensed systems
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurology (AREA)
  • Reproductive Health (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Pregnancy & Childbirth (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Reivindicacion 1: Compuestos de la formula general (1), en la que: A se elige entre los grupos de formulas (2) a (9) en los que, en la formula (2) la línea de puntos es nula o es un doble enlace; R1 es H; o es alquilo C1-6 opcionalmente sustituido por CN; o es arilo, heteroarilo o sulfonilarilo de 5 o 6 eslabones, que están opcionalmente sustituidos por uno o varios B; o es -(CH2)m-Ra, en el que R4 es: CN; ORi; NRiRii; cicloalquilo C3-6, heterocicloalquilo de 3 a 7 eslabones, arilo, o heteroarilo de 5 o 6 eslabones, que están opcionalmente sustituidos por uno o varios B; o es -(CH2)n-C(O)-Rb o -(CH2)n-(SO2)-Rb, en el que Rb es: alquilo C1-6; alcoxi C1-6; cicloalquilo C3-6; -(CH2)m-RiiiRiv; NRiRii; cicloalquilo C3-6, heterocicloalquilo de 4 a 7 eslabones, arilo, o heteroarilo de 5 o 6 eslabones, que están opcionalmente sustituidos por uno o varios B; o R1 y R3 junto con el anillo indol al que están unidos forman un heterocicloalquilo de 5 o 6 eslabones, que puede estar sustituido por =O, C(O)O-alquiloC1-6 o alquilo C1-6; R2 es uno o varios de H, OH, halogeno, CN, nitro, alquilo C1-6 opcionalmente sustituido por -NRiiiRiv, alcoxi C1-6, -O-CH2-alqueniloC2-6, benciloxi; o dos R2 pueden formar un puente oxo o dioxo junto con el anillo indol, al que están unidos; R3 es H; o es halogeno; o es -(CO)-Rc, en el que Rc es: alquilo C1-6; -(CH2)n-NRiRii; -(CH2)n-NRiiiRiv; heterocicloalquilo de 5 o 6 eslabones, opcionalmente sustituido por alquilo C1-6; o es alquilo C1-6 o arilo, que están opcionalmente sustituido por: halogeno; -O(CO)-alquiloC1-6; o por -NH(CO)Rd, en el que Rd es alquilo C1-6 opcionalmente sustituido por halogeno o nitro, o Rd es arilo o un heteroarilo de 5 o 6 eslabones, que están opcionalmente sustituidos por halogeno, nitro, alquilo C1-6 o haloalquilo C1-6; R4 es uno o varios de H; halogeno, alquilo C1-6 o alcoxi C1-6 opcionalmente sustituido por OH, o dos R4 pueden formar un puente oxo o dioxo junto con el anillo fenilo, al que están unidos; R5 es H, alquilo C1-6 o arilo; R6 es H o alquilo C1-6; R7 es H o -SO2-Re en el que Re es alquilo C1-6 o arilo; R8 es H o alquilo C1-6; X es CH2 o C=O; B es halogeno, CN, NRiRii, alquilo C1-6 opcionalmente sustituido por CN, halogeno, o alcoxi C1-6, alcoxi C1-6, haloalcoxi C1-6, cicloalquilo C3-6, -C(O)O-alquiloC1-6, -C(O)-NRiRii, -C(O)-alquiloC1-6, -S(O)2-alquiloC1-6, -S(O)2-NRiRii, (CRiiiRiv)n-fenilo, o (CRiiiRiv)n-heteroarilo de 5 o 6 eslabones, en el que el resto fenilo o heteroarilo de 5 o 6 eslabones está opcionalmente sustituido por uno o varios sustituyentes elegidos entre el grupo formado por: halogeno, CN, NRiRii, alquilo C1-6 opcionalmente sustituido por CN, halogeno o alcoxi C1-6, alcoxi C1-6, haloalcoxi C1-6, cicloalquilo C3-6, -C(O)O-alquiloC1-6, -C(O)-NRiRii, -C(O)-alquiloC1-6, -S(O)2-alquiloC1-6, -S(O)2-NRiRii; Ri y Rii son H, alquilo C1-6, alquiloC1-6-NRiiiRiv, -(CO)O-alquiloC1-6, -C(O)-NRiiiRiv, -C(O)-alquiloC1-6, -S(O)2-alquiloC1- 6, -S(O)2-NRiiiRiv u OH; Riii y Riv son H o alquilo C1-6; m es un numero de 1 a 6; n es un numero de 0 a 4; así como a las sales farmacéuticamente aceptables de los mismos.
ARP060102988A 2005-07-14 2006-07-12 Derivados de indol -3-il-espiro-piperidina como antagonista del receptor v1a AR054830A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP05106443 2005-07-14
EP05109364 2005-10-07

Publications (1)

Publication Number Publication Date
AR054830A1 true AR054830A1 (es) 2007-07-18

Family

ID=37001896

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060102988A AR054830A1 (es) 2005-07-14 2006-07-12 Derivados de indol -3-il-espiro-piperidina como antagonista del receptor v1a

Country Status (25)

Country Link
US (2) US7332501B2 (es)
EP (1) EP1904477B1 (es)
JP (1) JP4927079B2 (es)
KR (1) KR100974967B1 (es)
CN (1) CN101253164B (es)
AR (1) AR054830A1 (es)
AT (1) ATE421511T1 (es)
AU (1) AU2006268724B2 (es)
BR (1) BRPI0612988A2 (es)
CA (1) CA2615726C (es)
CY (1) CY1108996T1 (es)
DE (1) DE602006004997D1 (es)
DK (1) DK1904477T3 (es)
ES (1) ES2317558T3 (es)
IL (1) IL188478A (es)
MX (1) MX2008000585A (es)
MY (1) MY144684A (es)
NO (1) NO20080059L (es)
PL (1) PL1904477T3 (es)
PT (1) PT1904477E (es)
RU (1) RU2414466C2 (es)
SI (1) SI1904477T1 (es)
TW (1) TWI312780B (es)
WO (1) WO2007006688A1 (es)
ZA (1) ZA200800320B (es)

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PL1904477T3 (pl) * 2005-07-14 2009-07-31 Hoffmann La Roche Pochodne indolo-3-karbonylo-spiro-piperydyny jako antagoniści receptora V1a
ATE488519T1 (de) * 2005-09-28 2010-12-15 Hoffmann La Roche Indol-3-ylcarbonylazaspiroderivate als vasopressinrezeptorantagonisten
US7351706B2 (en) * 2006-01-05 2008-04-01 Hoffmann-La Roche Inc. Indol-3-yl-carbonyl-spiro-piperidine derivatives
WO2008068185A1 (en) 2006-12-07 2008-06-12 F. Hoffmann-La Roche Ag Spiro-piperidine derivatives as via receptor antagonists
CN101541786A (zh) 2006-12-08 2009-09-23 弗·哈夫曼-拉罗切有限公司 作为V1a受体拮抗剂的吲哚类化合物
KR20090082502A (ko) * 2006-12-22 2009-07-30 에프. 호프만-라 로슈 아게 스피로-피페리딘 유도체
ES2376378T3 (es) * 2007-01-12 2012-03-13 F. Hoffmann-La Roche Ag Derivados de espiropiperidina-glicinamida.
TW200940547A (en) * 2007-12-13 2009-10-01 Speedel Experimenta Ag Organic compounds
WO2011137024A1 (en) * 2010-04-26 2011-11-03 Merck Sharp & Dohme Corp. Novel spiropiperidine prolylcarboxypeptidase inhibitors
PT2683723T (pt) 2011-03-10 2016-08-05 Zoetis Services Llc Derivados espirocíclicos de isoxazolina como agentes antiparasitários
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CN104203950B (zh) 2012-03-16 2016-08-24 生命医药公司 肝x受体调节剂
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CA3037222C (en) 2016-09-21 2024-02-13 Vectus Biosystems Limited Compositions for the treatment of hypertension and/or fibrosis
HU231206B1 (hu) 2017-12-15 2021-10-28 Richter Gedeon Nyrt. Triazolobenzazepinek
TW201938171A (zh) 2017-12-15 2019-10-01 匈牙利商羅特格登公司 作為血管升壓素V1a受體拮抗劑之三環化合物
CN113563255B (zh) * 2020-04-29 2023-08-18 成都倍特药业股份有限公司 瑞芬沙星中间体的制备方法

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US5686624A (en) * 1992-01-30 1997-11-11 Sanofi 1-benzenesulfonyl-1,3-dihydro-indol-2-one derivatives, their preparation and pharmaceutical compositions in which they are present
RO115804B1 (ro) * 1992-12-11 2000-06-30 Merck & Co Inc Derivati de spiropiperidine, procedee de preparare si compozitii farmaceutice ale acestora
EP1410437A2 (en) * 2001-01-22 2004-04-21 Morgan Chemical Products, Inc. Cvd diamond enhanced microprocessor cooling system
PL1904477T3 (pl) * 2005-07-14 2009-07-31 Hoffmann La Roche Pochodne indolo-3-karbonylo-spiro-piperydyny jako antagoniści receptora V1a

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CA2615726C (en) 2014-05-27
ES2317558T3 (es) 2009-04-16
JP2009501185A (ja) 2009-01-15
AU2006268724B2 (en) 2011-06-02
NO20080059L (no) 2008-04-02
TWI312780B (en) 2009-08-01
SI1904477T1 (sl) 2009-06-30
CN101253164A (zh) 2008-08-27
US20070027173A1 (en) 2007-02-01
ZA200800320B (en) 2009-02-25
MY144684A (en) 2011-10-31
RU2008100082A (ru) 2009-08-20
CY1108996T1 (el) 2014-07-02
MX2008000585A (es) 2008-03-14
PL1904477T3 (pl) 2009-07-31
WO2007006688A1 (en) 2007-01-18
RU2414466C2 (ru) 2011-03-20
US20080146557A1 (en) 2008-06-19
IL188478A (en) 2012-01-31
JP4927079B2 (ja) 2012-05-09
ATE421511T1 (de) 2009-02-15
US7629353B2 (en) 2009-12-08
KR20080024231A (ko) 2008-03-17
IL188478A0 (en) 2008-04-13
US7332501B2 (en) 2008-02-19
KR100974967B1 (ko) 2010-08-09
DE602006004997D1 (de) 2009-03-12
CN101253164B (zh) 2012-05-16
BRPI0612988A2 (pt) 2010-12-14
AU2006268724A1 (en) 2007-01-18
PT1904477E (pt) 2009-03-12
DK1904477T3 (da) 2009-03-16
HK1123554A1 (en) 2009-06-19
CA2615726A1 (en) 2007-01-18
EP1904477B1 (en) 2009-01-21
EP1904477A1 (en) 2008-04-02
TW200726469A (en) 2007-07-16

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