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1. (CN1768065) Thienopyrimidine compound and use of the same

Office : China
Application Number: 200480008798.9 Application Date: 28.01.2004
Publication Number: 1768065 Publication Date: 03.05.2006
Grant Number: 100360538 Grant Date: 09.01.2008
Publication Kind : C
Prior PCT appl.: Application Number:PCTJP2004000741 ; Publication Number:2004067535 Click to see the data
IPC:
C07D 495/04
A61K 31/519
A61P 1/04
A61P 5/04
A61P 5/24
A61P 13/08
A61P 15/00
A61P 15/08
A61P 15/18
A61P 17/10
A61P 17/14
A61P 25/28
A61P 35/00
A61P 43/00
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
495
Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519
ortho- or peri-condensed with heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1
Drugs for disorders of the alimentary tract or the digestive system
04
for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
5
Drugs for disorders of the endocrine system
02
of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
04
for decreasing, blocking or antagonising the activity of the hypothalamic hormones
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
5
Drugs for disorders of the endocrine system
24
of the sex hormones
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13
Drugs for disorders of the urinary system
08
of the prostate
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15
Drugs for genital or sexual disorders; Contraceptives
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15
Drugs for genital or sexual disorders; Contraceptives
08
for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15
Drugs for genital or sexual disorders; Contraceptives
18
Feminine contraceptives
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17
Drugs for dermatological disorders
10
Anti-acne agents
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17
Drugs for dermatological disorders
14
for baldness or alopecia
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25
Drugs for disorders of the nervous system
28
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
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43
Drugs for specific purposes, not provided for in groups A61P1/-A61P41/108
CPC:
A61K 31/519
Applicants: Takeda Chemical Industries Ltd.
武田药品工业株式会社
Inventors: Cho Nobuo
长展生
Imada Michi
今田岐
Tobitaka Takenori
飞高武宪
Miwa Norihiro
三轮宪弘
Kusaka Masami
日下雅美
Suzuki Nobuhiro
铃木伸宏
Agents: bian xinqin wu xiaonan
北京市柳沈律师事务所
北京市柳沈律师事务所
Priority Data: 020854/2003 29.01.2003 JP
Title: (EN) Thienopyrimidine compound and use of the same
(ZH) 噻吩并嘧啶化合物及其用途
Abstract: front page image
(EN) It is intended to provide a compound represented by the following general formula or its salt: wherein R<1> represents C1-4 alkyl; R<2> represents (1) a nitrogen-containing 5- to 7-membered heterocyclic group optionally having a substituent selected from among (1') halogeno, (2') hydroxy, (3') C1-4 alkyl and (4') C1-4 alkoxy, (2) phenyl optionally having a substituent selected from among (1') halogeno, (2') C1-4 alkoxy-C1-4 alkyl, (3') mono C1-4 alkyl-carbamoyl-C1-4 alkyl, (4') C1-4 alkoxy and (5') mono C1-4 alkylcarbamoyl-C1-4 alkoxy, etc.; R<3> represents C1-4 alkyl; R<4> represents C1-4 alkoxy, etc.; and n is an integer of from 1 to 4; as a thienopyrimidine compound having antagonism to gonadotropin-releasing hormone.
(ZH)

本发明披露具有下述通式的化合物或其盐:式中R1为C1-4烷基;R2为(1)取代或未取代的5-至7-元含氮的杂环基,取代基选自:(1’)卤素,(2’)羟基,(3’)C1-4烷基和(4’)C1-4烷氧基;(2)任选具有取代基的苯基,取代基选自:(1’)卤素,(2’)C1-4烷氧基-C1-4烷基,(3’)单-C1-4烷基-氨基甲酰基-C1-4烷基,(4’)C1-4烷氧基和(5’)单-C1-4烷基氨基甲酰基-C1-4烷氧基等;R3为C1-4烷基;R4为C1-4烷氧基等;n为1-4的整数;所述化合物为具有促性腺素释放激素拮抗活性的噻吩并嘧啶化合物。


Also published as:
NO20053974PL378002PLP.378002MXPA/a/2005/007990KR1020050096171ZA2005/06611
IL169869BRPI0407082CO5590921EP1591446JP2004250439JP2008094846
RU02331648US20060160829US20080108623US20120071486CA2514407ES2410814
US20140221381PT1591446NZ541772DK1591446AU2004207706BNRE/2013/0034
ID047.1556BRPI0407082WO/2004/067535