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AR044650A1 - Derivados de tiofeno - pirimidinona y su uso en la terapia de enfermedades que requieren la inhibicion de la enzima 17b-hidroxiesteroide-dehidrogenasa. - Google Patents

Derivados de tiofeno - pirimidinona y su uso en la terapia de enfermedades que requieren la inhibicion de la enzima 17b-hidroxiesteroide-dehidrogenasa.

Info

Publication number
AR044650A1
AR044650A1 ARP040101983A ARP040101983A AR044650A1 AR 044650 A1 AR044650 A1 AR 044650A1 AR P040101983 A ARP040101983 A AR P040101983A AR P040101983 A ARP040101983 A AR P040101983A AR 044650 A1 AR044650 A1 AR 044650A1
Authority
AR
Argentina
Prior art keywords
alkyl
substituted
aryl
therapy
hydrogen
Prior art date
Application number
ARP040101983A
Other languages
English (en)
Inventor
Leena Hirvela
Nina Johansson
Pasi Koskimies
Olli Pentikainen
Tommi Nyronen
Tina Salminen
Mark Johnson
Original Assignee
Solvay Pharm Bv
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 Solvay Pharm Bv filed Critical Solvay Pharm Bv
Publication of AR044650A1 publication Critical patent/AR044650A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic 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
    • C07D495/04—Ortho-condensed systems
    • 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
    • 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
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P17/08—Antiseborrheics
    • 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
    • A61P17/10—Anti-acne agents
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • 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
    • 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
    • A61P25/28—Drugs 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
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • 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
    • A61P27/02—Ophthalmic agents
    • A61P27/12—Ophthalmic agents for cataracts
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/18—Drugs for disorders of the endocrine system of the parathyroid hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biomedical Technology (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hospice & Palliative Care (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Addiction (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (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)
  • Joining Of Glass To Other Materials (AREA)

Abstract

Derivados de tiofenpirimidinona y su uso en terapia especialmente para uso en el tratamiento y/o prevención de una enfermedad o desorden dependiente de una hormona esteroide, tal como enfermedades o desórdenes dependientes de la hormona esteroide que requiere la inhibición de enzimas 17beta-hidroxiesteroide-dehidrogenasas. Reivindicación 3: Un compuesto de la fórmula (1), en la cual: X representa S, SO o SO2; R1 y R2 están seleccionados individualmente del grupo que comprende alquilo, alquilo sustituido, arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, cicloheteroalquilo, cicloheteroalquilo sustituido, aril-alquilo, aril-alquilo sustituido, heteroarilalquilo, heteroarilalquilo sustituido, cicloheteteroalquil-alquilo, cicloheteroalquil-alquilo sustituido; o R2 puede estar seleccionado independientemente entre acilo, carboxilo o amido, mientras R1 y R2 no pueden representar simultáneamente alquilo no sustituido, y R2 debe ser distinto de metilo si todos los sustituyentes R3, R5 y R6 simultáneamente representan hidrógeno y R4 representa hidrógeno o metilo; R3 y R4 están individualmente seleccionados del grupo que comprende hidrógeno, oxo, halógeno o dihalógeno, acilo, alquilo, alquilo sustituido, hidroxilo, carboxilo, amido, amino, nitrilo, tio, alcoxi, aciloxi, ariloxi, alquiltio y ariltio; R5 representa hidrógeno; R6 representa hidrógeno o halógeno, y la cadena de hidrocarburos -C(R3)-C(R4)-C(R5)-C(R6)- del ciclo de seis miembros es saturada o contiene una o dos dobles ligaduras entre los átomos de carbono; el ciclo de seis miembros que comprende la cadena de hidrocarburos -C(R3)-C(R4)-C(R5)-C(R6)- debe ser un ciclo aromático si todos los sustituyentes R3, R4, R5 y R6 simultáneamente representan hidrógeno, para uso en terapia.
ARP040101983A 2003-06-10 2004-06-08 Derivados de tiofeno - pirimidinona y su uso en la terapia de enfermedades que requieren la inhibicion de la enzima 17b-hidroxiesteroide-dehidrogenasa. AR044650A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US47704703P 2003-06-10 2003-06-10

Publications (1)

Publication Number Publication Date
AR044650A1 true AR044650A1 (es) 2005-09-21

Family

ID=34421462

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP040101983A AR044650A1 (es) 2003-06-10 2004-06-08 Derivados de tiofeno - pirimidinona y su uso en la terapia de enfermedades que requieren la inhibicion de la enzima 17b-hidroxiesteroide-dehidrogenasa.

Country Status (24)

Country Link
US (1) US7465739B2 (es)
EP (1) EP1635839B1 (es)
JP (1) JP4605800B2 (es)
KR (1) KR20060054189A (es)
CN (1) CN1791412A (es)
AR (1) AR044650A1 (es)
AT (1) ATE479437T1 (es)
AU (1) AU2004277311B8 (es)
BR (1) BRPI0411295A (es)
CA (1) CA2527617A1 (es)
DE (1) DE602004028934D1 (es)
DK (1) DK1635839T3 (es)
ES (2) ES2352552T3 (es)
IL (1) IL172316A0 (es)
MX (1) MXPA05012745A (es)
NO (1) NO20060123L (es)
PL (1) PL1635839T3 (es)
PT (1) PT1635839E (es)
RU (1) RU2412190C2 (es)
SA (1) SA04250159B1 (es)
SI (1) SI1635839T1 (es)
TW (1) TWI349551B (es)
WO (1) WO2005032527A2 (es)
ZA (1) ZA200508296B (es)

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US7465739B2 (en) 2008-12-16
TWI349551B (en) 2011-10-01
AU2004277311B2 (en) 2010-04-29
JP4605800B2 (ja) 2011-01-05
CA2527617A1 (en) 2005-04-14
EP1635839B1 (en) 2010-09-01
ATE479437T1 (de) 2010-09-15
NO20060123L (no) 2006-03-09
US20050038053A1 (en) 2005-02-17
AU2004277311A1 (en) 2005-04-14
WO2005032527A2 (en) 2005-04-14
TW200509937A (en) 2005-03-16
ES2352554T3 (es) 2011-02-21
EP1635839A2 (en) 2006-03-22
AU2004277311B8 (en) 2010-05-27
SI1635839T1 (sl) 2010-12-31
JP2006527226A (ja) 2006-11-30
RU2412190C2 (ru) 2011-02-20
KR20060054189A (ko) 2006-05-22
WO2005032527B1 (en) 2005-09-22
DK1635839T3 (da) 2011-01-03
WO2005032527A3 (en) 2005-08-04
ZA200508296B (en) 2007-01-31
PT1635839E (pt) 2010-10-12
PL1635839T3 (pl) 2011-02-28
ES2352552T3 (es) 2011-02-21
CN1791412A (zh) 2006-06-21
IL172316A0 (en) 2011-08-01
BRPI0411295A (pt) 2006-08-01
MXPA05012745A (es) 2006-05-17
DE602004028934D1 (de) 2010-10-14
SA04250159B1 (ar) 2008-06-21
RU2006100033A (ru) 2007-07-20

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