BRPI0407082B8 - composto n-(4-(1-(2,6-difluorobenzil)-5-((dimetilamino)metil)-3-(6-metóxi-3-piridazinil)-2,4-dioxo-1,2,3,4-tetraidrotieno[2,3-d]pirimidina-6-il)fenil)-n’-metoxiuréia, ou um sal do mesmo, produto farmacêutico, e, uso do composto - Google Patents

composto n-(4-(1-(2,6-difluorobenzil)-5-((dimetilamino)metil)-3-(6-metóxi-3-piridazinil)-2,4-dioxo-1,2,3,4-tetraidrotieno[2,3-d]pirimidina-6-il)fenil)-n’-metoxiuréia, ou um sal do mesmo, produto farmacêutico, e, uso do composto

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Publication number
BRPI0407082B8
BRPI0407082B8 BRPI0407082A BRPI0407082A BRPI0407082B8 BR PI0407082 B8 BRPI0407082 B8 BR PI0407082B8 BR PI0407082 A BRPI0407082 A BR PI0407082A BR PI0407082 A BRPI0407082 A BR PI0407082A BR PI0407082 B8 BRPI0407082 B8 BR PI0407082B8
Authority
BR
Brazil
Prior art keywords
compound
alkoxy
alkyl
phenyl
pharmaceutical
Prior art date
Application number
BRPI0407082A
Other languages
English (en)
Inventor
Miwa Kazuhiro
Kusaka Masami
Suzuki Nobuhiro
Cho Nobuo
Imada Takashi
Hitaka Takenori
Original Assignee
Takeda Pharmaceuticals Co
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 Takeda Pharmaceuticals Co filed Critical Takeda Pharmaceuticals Co
Publication of BRPI0407082A publication Critical patent/BRPI0407082A/pt
Publication of BRPI0407082B1 publication Critical patent/BRPI0407082B1/pt
Publication of BRPI0407082B8 publication Critical patent/BRPI0407082B8/pt
Publication of BRPI0407082C1 publication Critical patent/BRPI0407082C1/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
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    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • 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
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16Masculine contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18Feminine contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
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    • 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
    • A61P5/00Drugs for disorders of the endocrine system
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P5/02Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
    • A61P5/04Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin for decreasing, blocking or antagonising the activity of the hypothalamic hormones
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    • A61P5/06Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones

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  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
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  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

"composto, pró-droga, produto farmacêutico, método de antagonizar hormônio liberador de gonadotropina, e, uso do composto". a presente invenção proporciona um composto representado pela fórmula sendo que r^ 1^ é um c~ 1-4~ alquila;r^ 2^ é (1) um grupo heterocíclico contendo nitrogênio com de 5 a 7 membros que pode apresentar um substituinte selecionado do grupo que consiste de (1<39>) halogênio, (2<39>) um grupo hidróxi, (3<39>) um c~ 1-4~ alquila e (4<39>) um c~ 1-4~ alcóxi, (2) um fenila que pode apresentar um substituinte selecionado do grupo que consiste de (1<39>) um halogênio, (2<39>) um c~ 1-4~ alcóxi-c~ 1-4~ alquila, (3<39>) um mono-c~ 1-4~ alquilcarbamoil-c~ 1-4~ alquila, (4<39>) um c~ 1-4~ alcóxi e (5<39>) um mono-c~ 1-4~ alquilcarbamoil-c~ 1-4~ alcóxi, ou análogos; r^ 3^ é um c~ 1-4~ alquila; r^ 4^ é um c~ 1-4~ alcóxi, ou análogos; n é um número inteiro de 1 a 4; ou um sal do mesmo, como um composto de tienopirimidina apresentando atividade antagonista de hormônio liberador de gonadotropina.
BRPI0407082A 2003-01-29 2004-01-28 composto n-(4-(1-(2,6-difluorobenzil)-5-((dimetilamino)metil)-3-(6-metóxi-3-piridazinil)-2,4-dioxo-1,2,3,4-tetraidrotieno[2,3-d]pirimidina-6-il)fenil)-n’-metoxiuréia, ou um sal do mesmo, produto farmacêutico, e, uso do composto BRPI0407082C1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2003-020854 2003-01-29
JP2003020854 2003-01-29
PCT/JP2004/000741 WO2004067535A1 (ja) 2003-01-29 2004-01-28 チエノピリミジン化合物およびその用途

Publications (4)

Publication Number Publication Date
BRPI0407082A BRPI0407082A (pt) 2006-01-24
BRPI0407082B1 BRPI0407082B1 (pt) 2019-06-04
BRPI0407082B8 true BRPI0407082B8 (pt) 2019-06-25
BRPI0407082C1 BRPI0407082C1 (pt) 2021-05-25

Family

ID=32820637

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0407082A BRPI0407082C1 (pt) 2003-01-29 2004-01-28 composto n-(4-(1-(2,6-difluorobenzil)-5-((dimetilamino)metil)-3-(6-metóxi-3-piridazinil)-2,4-dioxo-1,2,3,4-tetraidrotieno[2,3-d]pirimidina-6-il)fenil)-n’-metoxiuréia, ou um sal do mesmo, produto farmacêutico, e, uso do composto

Country Status (27)

Country Link
US (4) US7300935B2 (pt)
EP (1) EP1591446B1 (pt)
KR (1) KR101074462B1 (pt)
CN (2) CN101153042A (pt)
AU (1) AU2004207706B2 (pt)
BE (1) BE2022C501I2 (pt)
BR (1) BRPI0407082C1 (pt)
CA (1) CA2514407C (pt)
CO (1) CO5590921A2 (pt)
CY (2) CY1114008T1 (pt)
DK (1) DK1591446T3 (pt)
ES (1) ES2410814T3 (pt)
FR (1) FR21C1056I2 (pt)
HK (1) HK1084665A1 (pt)
HU (1) HUS2100052I1 (pt)
IL (1) IL169869A (pt)
LT (1) LTC1591446I2 (pt)
MX (1) MXPA05007990A (pt)
NL (1) NL301158I2 (pt)
NO (2) NO331981B1 (pt)
NZ (1) NZ541772A (pt)
PL (1) PL214756B1 (pt)
PT (1) PT1591446E (pt)
RU (1) RU2331648C2 (pt)
SI (1) SI1591446T1 (pt)
WO (1) WO2004067535A1 (pt)
ZA (1) ZA200506611B (pt)

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