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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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Classifications

    • 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)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Reproductive Health (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (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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DE602006004997D1 (de) * 2005-07-14 2009-03-12 Hoffmann La Roche Indol-3-carbonyl-spiro-piperidinderivate als antagonisten des v1a-rezeptors
CN101273046B (zh) * 2005-09-28 2011-05-25 弗·哈夫曼-拉罗切有限公司 作为加压素受体拮抗剂的吲哚-3-基-羰基氮杂螺环衍生物
US7351706B2 (en) * 2006-01-05 2008-04-01 Hoffmann-La Roche Inc. Indol-3-yl-carbonyl-spiro-piperidine derivatives
ATE469900T1 (de) 2006-12-07 2010-06-15 Hoffmann La Roche Spiropiperidinderivate als antagonisten des via- rezeptors
ES2345132T3 (es) 2006-12-08 2010-09-15 F. Hoffmann-La Roche Ag Indoles que actuan como agonistas del receptor v1a.
WO2008077810A2 (en) * 2006-12-22 2008-07-03 F. Hoffmann-La Roche Ag Spiro-piperidine derivatives
ATE536356T1 (de) * 2007-01-12 2011-12-15 Hoffmann La Roche Spiropiperidin-glycinamid-derivate
TW200940547A (en) * 2007-12-13 2009-10-01 Speedel Experimenta Ag Organic compounds
US8785634B2 (en) * 2010-04-26 2014-07-22 Merck Sharp & Dohme Corp Spiropiperidine prolylcarboxypeptidase inhibitors
PL2683723T3 (pl) 2011-03-10 2017-07-31 Zoetis Services Llc Spirocykliczne pochodne izoksazoliny jako środki przeciwpasożytnicze
RU2475489C1 (ru) * 2011-10-07 2013-02-20 Федеральное государственное бюджетное образовательное учреждение высшего профессионального образования "Чувашский государственный университет имени И.Н. Ульянова" Способ получения 8-амино-1-имино-6-морфолин-4-ил-2-окса-7-азаспиро[4,4]нона-3,6,8-триен-9-карбонитрилов
DK2825542T3 (en) 2012-03-16 2017-01-09 Vitae Pharmaceuticals Inc LIVER-X-receptor modulators
SI2825541T1 (sl) 2012-03-16 2016-10-28 Vitae Pharmaceuticals, Inc. Modulatorji jetrnega receptorja X
JO3109B1 (ar) * 2012-05-10 2017-09-20 Ferring Bv منبهات لمستقبلات v1a
KR101698124B1 (ko) * 2015-05-29 2017-01-19 한국외국어대학교 연구산학협력단 3-(메틸아미노)-3-((r)-피롤리딘-3-일)프로판니트릴 또는 이의 염의 제조방법
EP3414247B1 (en) * 2016-02-08 2021-04-21 F. Hoffmann-La Roche AG Spiroindolinones as ddr1 inhibitors
US20180002344A1 (en) 2016-06-16 2018-01-04 Genentech, Inc. Heteroaryl estrogen receptor modulators and uses thereof
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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
HU231206B1 (hu) 2017-12-15 2021-10-28 Richter Gedeon Nyrt. Triazolobenzazepinek
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
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DE602006004997D1 (de) * 2005-07-14 2009-03-12 Hoffmann La Roche Indol-3-carbonyl-spiro-piperidinderivate als antagonisten des v1a-rezeptors

Also Published As

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

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