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公开(公告)号:PT1035115E
公开(公告)日:2005-01-31
申请号:PT00102260
申请日:2000-02-15
Applicant: HOFFMANN LA ROCHE
Inventor: STADLER HEINZ , HUNKELER WALTER , GODEL THIERRY , HOFFMANN TORSTEN , SCHNIDER PATRICK , MICHAEL BOES , QUIRICO BRANCA , GUIDO GALLEY
IPC: A61K20060101 , A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/444 , A61K31/455 , A61K31/496 , A61P1/00 , A61P9/00 , A61P11/00 , A61P25/00 , A61P25/04 , A61P25/28 , A61P25/30 , A61P27/02 , A61P29/00 , A61P43/00 , C07D20060101 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/63 , C07D213/65 , C07D213/74 , C07D213/75 , C07D213/78 , C07D213/82 , C07D401/04 , C07D401/12 , C07D413/12 , C07D413/14
Abstract: The present invention relates to compounds of the general formula wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R is hydrogen or halogen; or R and R may be together -CH=CH-CH=CH-; R and R are independently from each other hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; or R and R may be together -CH=CH-CH=CH-, optionally substituted by one or two substituents selected from lower alkyl or lower alkoxy; R is hydrogen, lower alkyl or form a cycloalkyl group; R is hydrogen, -N(R )2, -N(R )(CH2)nOH, -N(R )S(O)2-lower alkyl, -N(R )S(O)2-phenyl, -N=CH-N(R )2, -N(R )C(O)R or a cyclic tertiary amine of the group R is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R is hydrogen, hydroxy, lower alkyl, -(CH2)nCOO-lower alkyl, -N(R )CO-lower alkyl, hydroxy-lower alkyl, cyano, -(CH2)nO(CH2)nOH, -CHO or a 5-or 6 membered heterocyclic group, optionally bonded via an alkylene group, X is -C(O)N(R )-, -(CH2)mO-, -(CH2)mN(R )-, -N(R )C(O)-, or -N(R )(CH2)m-; n is 0 - 4; and m is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I show a high affinity to the NK-1 receptor. They may be used for the treatment of diseases, which relate to NK-1 receptor antagonists.
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公开(公告)号:DK1035115T3
公开(公告)日:2005-01-24
申请号:DK00102260
申请日:2000-02-15
Applicant: HOFFMANN LA ROCHE
Inventor: BOES MICHAEL , BRANCA QUIRICO , GALLEY GUIDO , GODEL THIERRY , HOFFMANN TORSTEN , HUNKELER WALTER , SCHNIDER PATRICK , STADLER HEINZ
IPC: A61K20060101 , A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/444 , A61K31/455 , A61K31/496 , A61P1/00 , A61P9/00 , A61P11/00 , A61P25/00 , A61P25/04 , A61P25/28 , A61P25/30 , A61P27/02 , A61P29/00 , A61P43/00 , C07D20060101 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/63 , C07D213/65 , C07D213/74 , C07D213/75 , C07D213/78 , C07D213/82 , C07D401/04 , C07D401/12 , C07D413/12 , C07D413/14
Abstract: The present invention relates to compounds of the general formula wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R is hydrogen or halogen; or R and R may be together -CH=CH-CH=CH-; R and R are independently from each other hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; or R and R may be together -CH=CH-CH=CH-, optionally substituted by one or two substituents selected from lower alkyl or lower alkoxy; R is hydrogen, lower alkyl or form a cycloalkyl group; R is hydrogen, -N(R )2, -N(R )(CH2)nOH, -N(R )S(O)2-lower alkyl, -N(R )S(O)2-phenyl, -N=CH-N(R )2, -N(R )C(O)R or a cyclic tertiary amine of the group R is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R is hydrogen, hydroxy, lower alkyl, -(CH2)nCOO-lower alkyl, -N(R )CO-lower alkyl, hydroxy-lower alkyl, cyano, -(CH2)nO(CH2)nOH, -CHO or a 5-or 6 membered heterocyclic group, optionally bonded via an alkylene group, X is -C(O)N(R )-, -(CH2)mO-, -(CH2)mN(R )-, -N(R )C(O)-, or -N(R )(CH2)m-; n is 0 - 4; and m is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I show a high affinity to the NK-1 receptor. They may be used for the treatment of diseases, which relate to NK-1 receptor antagonists.
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公开(公告)号:MA26793A1
公开(公告)日:2004-12-20
申请号:MA26424
申请日:2001-11-26
Applicant: HOFFMANN LA ROCHE
Inventor: BOES MICHAEL , GALLEY GUIDO , GODEL THIERRY , HOFFMANN TORSTEN , HUNKELER WALTER , SCHNIDER PATRICK , STADLER HEINZ
IPC: A61K31/496 , A61K31/505 , A61K31/506 , A61K31/5377 , A61P1/04 , A61P1/08 , A61P9/00 , A61P11/06 , A61P17/02 , A61P19/02 , A61P25/00 , A61P25/06 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/36 , A61P27/00 , A61P27/02 , A61P29/00 , A61P37/08 , A61P43/00 , C07D213/00 , C07D239/00 , C07D239/28 , C07D239/32 , C07D239/34 , C07D239/38 , C07D239/42 , C07D239/48 , C07D295/00 , C07D401/04 , C07D403/04
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公开(公告)号:DE60014216D1
公开(公告)日:2004-11-04
申请号:DE60014216
申请日:2000-02-15
Applicant: HOFFMANN LA ROCHE
Inventor: BOES MICHAEL , BRANCA QUIRICO , GALLEY GUIDO , GODEL THIERRY , HOFFMANN TORSTEN , HUNKELER WALTER , SCHNIDER PATRICK , STADLER HEINZ
IPC: A61K20060101 , A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/444 , A61K31/455 , A61K31/496 , A61P1/00 , A61P9/00 , A61P11/00 , A61P25/00 , A61P25/04 , A61P25/28 , A61P25/30 , A61P27/02 , A61P29/00 , A61P43/00 , C07D20060101 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/63 , C07D213/65 , C07D213/74 , C07D213/75 , C07D213/78 , C07D213/82 , C07D401/04 , C07D401/12 , C07D413/12 , C07D413/14
Abstract: The present invention relates to compounds of the general formula wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R is hydrogen or halogen; or R and R may be together -CH=CH-CH=CH-; R and R are independently from each other hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; or R and R may be together -CH=CH-CH=CH-, optionally substituted by one or two substituents selected from lower alkyl or lower alkoxy; R is hydrogen, lower alkyl or form a cycloalkyl group; R is hydrogen, -N(R )2, -N(R )(CH2)nOH, -N(R )S(O)2-lower alkyl, -N(R )S(O)2-phenyl, -N=CH-N(R )2, -N(R )C(O)R or a cyclic tertiary amine of the group R is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R is hydrogen, hydroxy, lower alkyl, -(CH2)nCOO-lower alkyl, -N(R )CO-lower alkyl, hydroxy-lower alkyl, cyano, -(CH2)nO(CH2)nOH, -CHO or a 5-or 6 membered heterocyclic group, optionally bonded via an alkylene group, X is -C(O)N(R )-, -(CH2)mO-, -(CH2)mN(R )-, -N(R )C(O)-, or -N(R )(CH2)m-; n is 0 - 4; and m is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I show a high affinity to the NK-1 receptor. They may be used for the treatment of diseases, which relate to NK-1 receptor antagonists.
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公开(公告)号:JO2254B1
公开(公告)日:2004-10-07
申请号:JOP20000015
申请日:2000-02-22
Applicant: HOFFMANN LA ROCHE
Inventor: BOES MICHAEL , GALLEY GUIDO , GODEL THIERRY , HOFFMANN TORSTEN , HUNKELER WALTER , SCHNIDER PATRICK , STADLER HEINZ
IPC: A61K31/44 , A61P25/00 , A61P29/00 , C07D213/30 , C07D213/38 , C07D213/75 , C07D213/81 , C07D401/04
Abstract: The invention relates to compounds of the formulawhereinR is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R1 is hydrogen or halogen; orR and R1 may be together -CH=CH-CH=CH-; R2 is hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; R3 is hydrogen, lower alkyl or form a cycloalkyl group; R4 is hydrogen, -N(R5)2, -N(R5)S(O)2-lower alkyl, -N(R5)C(O)R5 or a cyclic tertiary amine of the groupR5 is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R6 is hydrogen, hydroxy, lower alkyl, -N(R5)CO-lower alkyl, hydroxy-lower alkyl, cyano, -CHO or a 5- or 6 membered heterocyclic group, optionally bonded via an alkylene group,X is -C(O)N(R5)-, -(CH2)mO-, -(CH2)mN(R5)-, -N(R5)C(O)-, or -N(R5)(CH2)m-; n is 0-4; andm is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof.It has been shown that the above mentioned compounds have a good affinity to the NK-1 receptor
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公开(公告)号:JO2244B
公开(公告)日:2004-10-07
申请号:JO200012
申请日:2000-02-22
Applicant: HOFFMANN LA ROCHE
Inventor: BOES MICHAEL , GALLEY GUIDO , GODEL THIERRY , HOFFMANN TORSTEN , HUNKELER WALTER , SCHNIDER PATRICK , STADLER HEINZ
IPC: C07C211/44 , A61K31/167 , A61K31/44 , A61P25/00 , A61P29/00 , C07C211/54 , C07C233/29 , C07C233/33 , C07C233/44 , C07C317/14 , C07C317/40 , C07C323/41 , C07D213/75 , C07D213/79 , C07D213/81 , C07D295/12 , C07D295/135 , C07D401/04
CPC classification number: C07D213/75 , C07C233/29 , C07C233/33 , C07C233/44 , C07C317/40 , C07C323/41 , C07D295/135
Abstract: The invention relates to compounds of the general formula Wherein R is hydrogen, lower alkyl, lower alkyl, lower alkoxy , halogen or trifluoromethyl: R1 is hydrogen or halogen R and R1 may be together - CH = CH- CH = CH R2 is hydrogen, halogen, trifluoromethyl, lower aIkoxy or cyano; R3 is independently from each other hydrogen, lower alkyl or form a cycloalkyl group; R4 is hydrogen, halogen, lower alkyl, lower alkoxy,- N(R5)2, - N (R5) S (O)2 - lower alkyl, - N (R5) C (O) R5 or a cyclic tertiary amine of the group R5 is, independently from each other, hydrogen, C3-6 cycloalkyl, benzol or lower alkyl; R6 is hydrogen, hydroxy, lower alkyl, - N (R5) Co - lower alkyl, hydroxy-lower alkyl.cyano, CHO or a 5 – or 6 membered heterocyclic group optionally bonded via an alkylene group. X is - C(O)N(R5),-(CH2)mO-,-(CH2)mN(R5)C(O)-,-C (O)O-or- N(R5)(CH2)m’; Y is(CH2)n- O-,- S-,SO2-,-C(O)or N (R5) Z is = N-, -CH= or -C ( CL) = n is O - 4 ; and m is 1 or2 And to pharmaceutical acceptable acid addition salts thereof. It has been shown that the compounds of formula I have a high affinity to the NK -1 receptor.
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公开(公告)号:JO2235B1
公开(公告)日:2004-10-07
申请号:JOP20000017
申请日:2000-03-02
Applicant: HOFFMANN LA ROCHE
Inventor: BOES MICHAEL , GALLEY GUIDO , GODEL THIERRY , HOFFMANN TORSTEN , HUNKELER WALTER , SCHNIDER PATRICK , STADLER HEINZ
IPC: C07D295/14 , A61K31/166 , A61K31/167 , A61K31/495 , A61K31/496 , A61P1/04 , A61P1/08 , A61P11/06 , A61P25/24 , A61P25/28 , A61P29/00 , A61P37/08 , A61P43/00 , C07C41/01 , C07C43/174 , C07C209/06 , C07C209/50 , C07C211/29 , C07C211/45 , C07C217/54 , C07C231/02 , C07C231/08 , C07C233/11 , C07C233/15 , C07C233/44 , C07C233/66 , C07C235/42 , C07D295/155
Abstract: The present invention relates to compounds of the general formula Wherein R is hydrogen, lower alkyl, lower alkoxy, halogen, amino, N(R6)2 or trifluoromethyl R1 hydroeng, lower alkoxy or halogen R and R1 may be together CH=CH-CH=CH R2 is halogen, lower alkyl or trifluoromethyl R3 is hydrogen or lower alkyl R4 is hydrogen or a cyclic tertiary amine, optionally substituted by lower alkyl R5 is hydrogen, nitro, amino or N(R6)2 R6 is hydrogen or lower alkyl X is C(O)N(R6)(CH2)and N is 1-2 And to pharmaceutical acceptable acid addition salts thereof The compounds of formula and their salts are characterized by valuable therapeutic properties.
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公开(公告)号:DE69906397T2
公开(公告)日:2004-02-19
申请号:DE69906397
申请日:1999-01-08
Applicant: HOFFMANN LA ROCHE
Inventor: BOES MICHAEL , HUNKELER WALTER , RIEMER CLAUS
IPC: C07C309/30 , A61K31/00 , A61K31/10 , A61K31/135 , A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/4433 , A61K31/4436 , A61K31/505 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P43/00 , C07C315/04 , C07C317/22 , C07C317/32 , C07C317/36 , C07D213/61 , C07D213/62 , C07D213/71 , C07D213/73 , C07D213/74 , C07D213/84 , C07D239/38 , C07D401/04 , C07D401/14 , C07D409/04
Abstract: The present invention relates to novel compounds of the general formula wherein R is hydrogen; R is hydrogen, trifluoromethyl or lower alkyl; R is hydrogen or amino; or R and R or R and R taken together are -CH=CH-CH=CH-; Z is pyrimidin-4-yl, pyridin-4-yl, pyridin-2-yl or phenyl; R R are each independently hydrogen, lower alkyl, trifluoromethyl, halogen, lower alkoxy, nitrilo, amino, lower alkyl-amino, di-lower alkyl-amino, piperazinyl, morpholinyl, pyrrolidinyl, vinyl, C3-C6 cycloalkyl, C3-C6 cycloalkenyl, t-buthylethinyl, hydroxyalkylethinyl, phenylethinyl, naphthyl, thiophenyl, or phenyl, which may be substituted by halogen, lower alkoxy, lower alkyl, trifluoromethyl or nitro, or a group -NH(CH2)nNR R , -N(CH3)(CH2)nNR R , -NH(CH2)n-morpholin-4-yl or -NH(CH2)nOH; n is 2-4 R and R are each independently hydrogen or lower alkyl, and to their pharmaceutically acceptable salts. It has been found that the compounds of formula I possess a selective affinity to 5HT-6 receptors.
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公开(公告)号:FI112487B
公开(公告)日:2003-12-15
申请号:FI951251
申请日:1995-03-16
Applicant: HOFFMANN LA ROCHE
Inventor: GODEL THIERRY , HUNKELER WALTER , STADLER HEINZ , WIDMER ULRICH
IPC: A61K31/41 , A61K31/55 , A61K31/5517 , A61P21/02 , A61P25/08 , A61P25/20 , A61P43/00 , C07D487/02 , C07D487/04 , C07D495/12 , C07D495/14 , C07D498/14 , C07D487/14
Abstract: Aminomethyl-substd. oxadiazolyl-imidazodiazepines of formula (I) and their addn salts are new: A and C atoms alpha and beta form a gp of formula e.g. (A ):Q = a gp. of formula e.g. (Q ):R , R = H; lower alkyl,etc.;or NR R = 5-8 membered heterocycle opt. contg. a further hetero atom or carrying a fused benzene ring; R = H and R = lower alkyl; or R +R = H; halo;etc.; and C atom gamma has the S configuration when R is other than H.
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公开(公告)号:ZA200201055B
公开(公告)日:2003-07-30
申请号:ZA200201055
申请日:2002-02-06
Applicant: HOFFMANN LA ROCHE
Inventor: TROTTMANN GERDA HUBER , HUNKELER WALTER , JAKOB-ROETNE ROLAND , KILPATRICK GAVIN JOHN , NETTEKOVEN MATTHIAS HEINRICH , RIEMER CLAUS
IPC: C07D213/73 , A61K31/437 , A61K31/4418 , A61K31/444 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/551 , A61K31/635 , A61P9/10 , A61P11/06 , A61P11/16 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/28 , A61P25/30 , A61P37/08 , A61P43/00 , C07D409/04 , C07D471/04 , C07D519/00 , C07D , A61K , A61P
Abstract: The invention relates to compounds of formulawhereinR1 is a 5 or 6 membered heteroaryl group, containing 1 to 3 heteroatoms, selected from N, O or S, and which groups are optionally substituted by one or two substituents, which are lower alkyl, -(CH2)nOH, halogen or lower alkoxy, and wherein the heteroaryl groups may be optionally linked to the pyrazole ring via an alkylene or alkenyl group, or isphenyl, optionally substituted by one or two substituents being lower alkyl, hydroxy-lower alkyl, halogen, hydroxy or lower alkoxy or is-O(CH2)n,phenyl, benzofuryl, indolyl or benzothiophenyl, or is-S-lower alkyl;R2 and R4 are independently from each other hydrogen, cyano or -S(O)2-phenyl;R3 is hydrogen, halogen or isa 5 or 6 membered heteroaryl group, containing 1 to 3 heteroatoms, selected from N, O or S, and which groups are optionally substituted by one or two substituents, which are lower alkyl, -(CH2)n-aryl, hydroxy, halogen, lower alkoxy, morpholinyl, amino, lower alkylamino or -C(O)NR'2, and wherein R' is lower alkyl or hydrogen, or isphenyl, optionally substituted by one or two substituents being halogen, lower alkyl, lower alkoxy, amino, di-lower alkyl amino, CF3, -OCF3, -NHC(O)lower alkyl, cyano, -C(O)-lower alkyl, -C(O)O-lower alkyl, -S-lower alkyl, -S(O)2NH-phenyl, -S(O)2-methylpiperazinyl; or is-NR'R'', wherein R' and R'' are independently from each other hydrogen, -(CH2)nphenyl, which phenyl ring is optionally substituted by halogen or lower alkoxy, -CH(lower alkyl)-phenyl, indan-1-yl, 1,2,3,4-tetrahydro-naphthalen, or cycloalkyl; or is-O-phenyl, which phenyl ring is optionally substituted by halogen, lower alkyl or lower alkoxy, -O-tetrahydronaphthalenyl or -O-CH2-6-methyl-pyridin-2-yl; or is-benzo[1,3]dioxolyl, -1H-indol-5-yl, naphthyl, benzofuran-2-yl, 1,3,4,9-tetrahydro-b-carbolin-2-yl, piperidin-1-yl, pyrrolidin-1-yl, piperazin-4-yl-methyl or morpholinyl;R5 is -NR2, wherein R may be the same or different and is hydrogen, lower alkyl, phenyl, benzyl, -CO-lower alkyl, -CO-lower alkoxy, -lower alkenyl, -CO(CH2)n-phenyl or -COO(CH2)n-phenyl, wherein the phenyl ring is optionally substituted by CF3, lower alkoxy, halogen or lower alkyl, -CO(CH2)3-NHCO-lower alkoxy, -(CH2)n-phenyl, wherein the phenyl ring is optionally substituted by lower alkoxy, CF3 or halogen, or is 4,5-dihydro-1H-imidazol-2-yl-benzoic acid, 1,4,5,6-tetrahydro-pyrimidin-2-yl-benzoic acid or 4,5,6,7-tetrahydro-1H-[1,3]diazepin-2-yl-benzoic acid;n is 0-4and their pharmaceutically acceptable salts
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