163498-79-1Relevant articles and documents
Therapeutic agent pcnsl (by machine translation)
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Paragraph 0118, (2016/10/09)
The present invention provides a malignant lymphoma therapeutic or preventive agent that comprises as the active ingredient a compound represented by general formula [1] as defined by (I) or (II), or a pharmaceutically acceptable salt thereof. [1] (I) X is CH or N; R1 is a halogen; R2 is a halogen, H, a cyano, a group represented by general formula [9], [9] an optionally substituted heteroaryl, or the like; R3 is H or a hydroxyl; R4 is H or an alkyl; and R5 is H or an alkyl. (II) X is -CRA, RA is -CORB, RB is an optionally substituted amino, alkoxy, or saturated cyclic amino group; R1 is a halogen; R2 is H; R3is H or a hydroxy; R4 is H or an alkyl; and R5 is H or an alkyl.
AMINOPYRAZINE DERIVATIVE AND MEDICINE
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Page/Page column 38-39, (2011/12/12)
The present invention relates to a compound represented by general formula [1] satisfying the following (I) or (II), or a pharmaceutical acceptable salt of the compound. (I) X is CH or N; R1 is a halogen atom,; and R2 is H, a halogen atom, CN, [2], [3], [8], [9], an —O-alkyl, an —O-(saturated ring), etc. [2]: —C(RC)(RD)(RE) (RC to RE each are H, an alkyl, etc.) [3]: —N(RF)(RG) (RF and RG each are H, OH, amino, a (hetero)aryl, etc.) [8]: —C(═O)RL (RL is an alkyl, OH, an alkoxy, amino, etc.) [9]: a (substituted)phenyl; (II) X is >C—C(—O)R3 (R3 is a (substituted)amino, an alkoxy, OH, etc.); R1 is a halogen atom; R2 is H; R3 is H or OH; and R3 and R4 each are H or an alkyl.
Compounds and Uses Thereof - 848
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Page/Page column 74, (2009/01/24)
This invention relates to novel compounds having the structural formula I below: and their pharmaceutically acceptable salts, tautomers or in vivo-hydrolysable precursors, compositions and methods of use thereof, wherein R1, R2, Rsu
Indoline derivatives
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, (2008/06/13)
This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1and R2may be single substituents or fused to form spirocyclic rings.
CYCLIC REGIMENS UTILIZING INDOLINE DERIVATIVES
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, (2008/06/13)
This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: wherein R 1 and R 2 may be single substituents or fused to form spirocyclic rings, in combination with progestins, estrogens, or both. These methods of treatment may be used for contraception or for the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate, or minimization of side effects or cyclic menstrual bleeding. Additional uses of the invention include stimulation of food intake.
Thio-oxindole derivatives
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Page column 49, (2010/11/30)
This invention relates to compounds which are agonists of the progesterone receptor which have the general structures: wherein: R1and R2are H, alkyl, substituted alkyl; OH; O(alkyl); O(substituted alkyl); OAc; aryl; substituted aryl; heteroaryl; substituted heteroaryl; alkylaryl; alkylheteroaryl;1-propynyl; or3-propynyl; or R1and R2are joined to form an alkyl, alkenyl or heterocyclic ring; or R1and R2together comprise a double bond to CMe2; C(cycloalkyl), O, or C(cycloether); R3is H, OH, NH2, C1to C6alkyl, substituted C1to C6alkyl, C3to C6alkenyl, alkynyl, substituted alkynyl, or CORA; RAis H, C1to C3alkyl, substituted C1to C3alkyl, C1to C3alkoxy, substituted C1to C3alkoxy, C1to C3aminoalkyl, or substituted C1to C3aminoalkyl; R4is H, halogen, CN, NH2, NO2, C1to C6alkyl, or substituted C1to C6alkyl, C1to C6alkoxy, substituted C1to C6alkoxy, C1to C6aminoalkyl, or substituted C1to C6aminoalkyl; R5is optionally substituted and selected from a benzene ring, a five or six membered heterocyclic ring with 1, 2, or 3 heteroatoms selected from O, S, SO, SO2or NR6; or an indol-4-yl, indol-7-yl or benzo-2-thiophene moiety; Q1is S, NR7, CR8R9; or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds to induce contraception or treat progesterone-related carcinomas and adenocarcinomas.
Pyrazinyl-substituted naphthalene derivatives
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, (2008/06/13)
Compounds of the formula where R1 is of the formulae R2 is —R4, —O—R4, —O—S (O)2—R4, —NR4R5, R4—(CH2)b—NH(C═X)—(CH2)—, R4—(CH2)b—O(C═O)NH—(CH2)c—(C═O)NH—, R4(C═O)NH—(C═O)NH—, —(CH2)b—NH(C═X)—(CH2)c—R4, R4—(CH2)b—O(C═)—(CH2)c—, —(CH2)b—O(C═O)—(CH2)c—R4, —NH(C═X)NH—R4, R4—O(C═O)O—, —O(C═)NH—R4, R4—O(C═O)NH—, —(CH2)b—(C═0)—(CH2)c—R4, —NH—S(O)2—R4, —C(OH)R4R5, —CH(OH)—R4, —(C═O)—NR4R5, —CN, —NO2, substituted C1 to C6 alkyl, substituted or unsubstituted C1 to C6 alkenyl, or substituted or unsubstituted C1 to C6 alkynyl, said substituted moieties substituted with a moiety of the formulae —R4, —R4R5, —O—R4, or —S(O)d—R4. These compounds are useful psychotherapeutics and are potent serotonin (5-HT1) agonists and antagonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain and chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotranmission. The compounds can also be used as centrally acting antihypertensives and vasodilators.
5-ARYLINDOLE DERIVATIVES
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, (2008/06/13)
Compounds of the formula STR1 wherein A, B, D, E, and F are each independently nitrogen or carbon; R 1 is hydrogen, C 1 to C. sub. 6 alkyl,--(CH 2) n R 7, or C 1 to C 3 alkyl-aryl; R. sub.2, R 3, R 4, R 5 and R 6 are each independently hydrogen, C 1 to C 6 alkyl, aryl, C 1 to C 3 alkyl-aryl, halogen, cyano, nitro,--(CH 2) m NR 8 R 9,--(CH 2). sub.m OR 9,--SR 9,--SO 2 NR 8 R 9,--(CH 2). sub.m NR 8 SO 2 R 9,--(CH 2) m NR 8 CO 2 R. sub.9,--(CH 2) m NR 8 COR 9,--(CH 2). sub.m CONR. sub.7 R 9, or--(CH 2) m CO 2 R 9 ; R 2 and R. sub.3, R 3 and R 4, R 4 and R 5, and R 5 and R 6 may be taken together to form a five-to seven-membered alkyl ring, a six-membered ary ring, a five-to seven-membered heteroalkyl ring, having 1 heteroatom of N, O, or S, or a five-to six-membered heteroaryl ring having 1 or 2 heteroatoms of N, O, or S; R 7 is--OR. sub.10,--SR0. sub.10,--SO 2 NR 10 R 11,--NR 10 SO 2 R 11,--NR 10 CO 2 R 11,--NR 10 COR 11,--CONR 10 R 11, or--CO 2 R 10 ; R 8, R 9, R 10 and R 11 are each independently hydrogen, C 1 to C 6 alkyl, or C 1 to C. sub.3 alkyl-aryl; m is 0, 1, or 2; n is 2, 3, or 4; and the above aryl groups and the aryl moieties of the above alkyl-aryl groups are each independently phenyl or substituted phenyl, wherein said substituted phenyl may be substituted with one to three of C 1 to C. sub.4 alkyl, halogen, hydroxy, cyano, carboxamido, nitro, or C 1 to C 4 alkoxy, and the pharmaceutically acceptable salts thereof. These compounds are useful in treating migraine and other disorders and are new. These compounds are useful psychotherapeutics and are potent serotonin (5-HT 1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, and chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators.
5-ARYLINDOLE DERIVATIVES
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, (2008/06/13)
Compounds of formula (I), wherein A, B, D, E, and F are each independently nitrogen or carbon; R 1 is hydrogen, C 1 to C 6 alky,--(CH 2) n R 7, or C 1 to C 3 alkyl-aryl; R. sub.2, R 3, R 4, R 5 and R 6 are each independently hydrogen, C. sub.1 to C 6 alkyl, aryl, C 1 to C 3 alkyl-aryl, halogen, cyano, nitro,--(CH 2) m NR 8 R 9,--(CH 2). sub.m OR 9,--SR. sub.9,--SO 2 NR 8 R 9,--(CH 2). sub.m NR 8 SO 2 R 9,--(CH 2) m NR 8 CO 2 R. sub.9,--(CH 2 m NR 8 COR 9,--(CH 2) m CONR. sub.7 R 9, or--(CH 2) m CO 2 R 9 ; R 2 and R. sub.3, R 3 and R 4, R 4 and R 5, and R 5 and R 6 may be taken together to form a 5-to 7-membered alkyl ring, a 6-membered aryl ring, a 5-to 7-membered heteroalkyl ring, having 1 heteroatom of N, O, or S, or a 5-to 6-membered heteroaryl ring having 1 or 2 heteroatoms of N, O, or S; R 7 is--OR 10 ,--SR. sub.10,--SO 2 NR 10 R 11,--NR 10 SO 2 R 11,--NR 10 CO 2 R 11,--NR 10 COR 11,--CONR 10 R 11, or--CO 2 R 10 ; R 8, R 9, R 10 and R 11 are each independently hydrogen, C 1 to C 6 alkyl, or C 1 to C 3 alkyl-aryl; m is 0, 1, or 2; n is 2, 3, or 4; and the above aryl groups and the aryl moieties of the above alkyl-aryl groups are each independently phenyl or substituted phenyl, where said substituted phenyl may be substituted with 1 to 3 of C 1 to C 4 alkyl, halogen, hydroxy, cyano, carboxamido, nitro, or C 1 to C 4 alkoxy, and the pharmaceutically acceptable salts thereof. These compounds are useful in treating migraine and other disorders and are new. These compounds are useful psychotherapeutics and are potent serotonin (5-HT 1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, and chronic paroxysmal hermicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators.