公开(公告)号：US4983607A

公开(公告)日：1991-01-08

申请号：US417970

申请日：1989-10-10

Applicant: Philippe Manoury ,  Daniel Obitz ,  Michel Peynot ,  Jonathan Frost

Inventor： Philippe Manoury ,  Daniel Obitz ,  Michel Peynot ,  Jonathan Frost

IPC: C07D215/22 ,  A61K31/495 ,  A61P43/00 ,  C07D215/227 ,  C07D401/12

CPC classification number: C07D215/227 ,  C07D401/12

Abstract: A quinolinone derivative which is a compound of formula (I): ##STR1## in which: R.sub.1 and R.sub.2 are each, independently of one another, a hydrogen or halogen atom or a (C.sub.1-4)alkyl radical;R.sub.3 is a hydrogen atom or a (C.sub.1-4)alkyl radical;R.sub.4 is an unsubstituted or substituted naphthyl, tetrahydronaphthyl, benzyl, phenyl, pyridyl, isoquinolyl or benzoyl radical; and X and Y are each a hydrogen atom or together form a bond; or a pharmaceutically acceptable acid addition salt thereof and, when X and Y are each a hydrogen atom, the diastereoisomers and enantiomers thereof.

Abstract translation: 作为式（I）化合物的喹啉酮衍生物：其中：R 1和R 2各自独立地为氢或卤素原子或（C 1-4）烷基; R3是氢原子或（C1-4）烷基; R4是未取代或取代的萘基，四氢萘基，苄基，苯基，吡啶基，异喹啉基或苯甲酰基; X和Y各自为氢原子或一起形成键; 或其药学上可接受的酸加成盐，当X和Y各自为氢原子时，其非对映异构体和对映异构体。

公开(公告)号：US4963680A

公开(公告)日：1990-10-16

申请号：US388374

申请日：1989-08-02

Applicant: Philippe Manoury ,  Jean Binet ,  Daniel Obitz ,  Gerard Defosse ,  Elisabeth Dewitte ,  Corinne Veronique

Inventor： Philippe Manoury ,  Jean Binet ,  Daniel Obitz ,  Gerard Defosse ,  Elisabeth Dewitte ,  Corinne Veronique

IPC: C07D295/08 ,  C07D295/096 ,  C07D295/20 ,  C07D295/205

CPC classification number: C07D295/096 ,  C07D295/205

Abstract: A piperazine derivative of formula (I) ##STR1## in which: R is hydrogen or a straight or branched (C.sub.1 -.sub.4) alkoxycarbonyl group; andA is a 7-methoxy-1-naphthalenyl, 6-methoxy-2,3-dihydro-1-(1H)-indenyl or 7-methoxy-1,2,3,4-tetrahydro-1-naphthalenyl group, or an optically active isomer thereof, or a salt thereof.

Abstract translation: 式（I）的哌嗪衍生物其中：R为氢或直链或支链（C1-4）烷氧基羰基; 和A是7-甲氧基-1-萘基，6-甲氧基-2,3-二氢-1-（1H） - 茚基或7-甲氧基-1,2,3,4-四氢-1-萘基，或 其光学活性异构体或其盐。

公开(公告)号：US5192763A

公开(公告)日：1993-03-09

申请号：US710711

申请日：1991-06-06

Applicant: Pascal George ,  Jacques Menin ,  Jean-Pierre Merly ,  Dennis Bigg ,  Daniel Obitz ,  Michel Peynot ,  Corinne Veronique

Inventor： Pascal George ,  Jacques Menin ,  Jean-Pierre Merly ,  Dennis Bigg ,  Daniel Obitz ,  Michel Peynot ,  Corinne Veronique

IPC: A61K31/495 ,  A61K31/40 ,  A61P9/10 ,  A61P25/08 ,  A61P25/18 ,  A61P25/28 ,  C07D207/09

CPC classification number: C07D207/09

Abstract: [(1-Arylpyrrolidin-2-yl)methyl]piperazine compounds corresponding to the formula ##STR1## in which Z denotes a group of formula N-R.sub.1 in which R.sub.1 is either a hydrogen atom or a C.sub.1-3 alkyl group or a group of formula Ar--C.sub.n H.sub.2n in which n denotes 0, 1 or 2 and Ar denotes a phenyl group optionally substituted by one or more halogen atoms and/or C.sub.1-3 alkyl or C.sub.1-3 alkoxy radicals, or a group of formula COR.sub.2 in which R.sub.2 denotes the CH.sub.3, C.sub.6 H.sub.5, CH.sub.2 C.sub.6 H.sub.5 or OC.sub.2 H.sub.5 group and their salts of addition to pharmaceutically acceptable acids. The compounds are useful for the treatment of neurological disorders.

Abstract translation: 对应于式（I）的[（1-芳基吡咯烷-2-基）甲基]哌嗪化合物，其中Z表示式为N-R 1的基团，其中R 1为氢原子或C 1-3烷基 或其中n表示0,1或2且Ar表示任选被一个或多个卤素原子和/或C 1-3烷基或C 1-3烷氧基取代的苯基的式Ar-C n H 2n的基团，或式 COR2，其中R2表示CH 3，C 6 H 5，CH 2 C 6 H 5或OC 2 H 5基团，以及它们与药学上可接受的酸的加成盐。 该化合物可用于治疗神经障碍。

公开(公告)号：US4530843A

公开(公告)日：1985-07-23

申请号：US545159

申请日：1983-10-25

Applicant: Daniel Obitz

Inventor： Daniel Obitz

IPC: A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/47 ,  A61K31/472 ,  A61P25/24 ,  A61P25/26 ,  C07D209/08 ,  C07D209/46 ,  C07D209/48 ,  C07D215/22 ,  C07D215/227 ,  C07D217/24 ,  C07D235/26

CPC classification number: C07D209/48 ,  C07D209/08 ,  C07D209/46 ,  C07D215/227 ,  C07D217/24 ,  C07D235/26

Abstract: Heterocyclic amidoxime derivatives of the general formula: ##STR1## wherein R' represents hydrogen or the methyl radical, and R represents the 1-oxo-1H-isoquinolin-2-yl, 2-oxo-2H-quinolin-1-yl, 2,3-dihydro-1H-indol-1-yl, 1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl, 1H-indol-1-yl, 1-oxo-1,3-dihydro-2H-isoindol-2-yl, 2-oxo-3,4-dihydro-2H-quinolin-1-yl, 5-chloro-3-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl, 5-chloro-2-oxo-3-phenyl-2,3-dihydro-1H-benzimidazol-1-yl, 4-chloro-1-oxo-1H-isoquinolin-2-yl or 3-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl radical, and--when R' represents the methyl radical--racemates and enantiomers of such compounds, are new compounds useful in therapy, and especially for the treatment of complaints of the central nervous system and for the treatment of depression.

Abstract translation: 其中R'表示氢或甲基，R表示1-氧代-1H-异喹啉-2-基，2-氧代-2H-喹啉-1-基，2-氧代-2H-异喹啉-2-基， ，3-二氢-1H-异吲哚-1-基，1,3-二氧代-1,3-二氢-2H-异吲哚-2-基，1H-吲哚-1-基，1-氧代-1,3-二氢 -2H-异吲哚-2-基，2-氧代-3,4-二氢-2H-喹啉-1-基，5-氯-3-甲基-2-氧代-2,3-二氢-1H-苯并咪唑-1-基 - 基，5-氯-2-氧代-3-苯基-2,3-二氢-1H-苯并咪唑-1-基，4-氯-1-氧代-1H-异喹啉-2-基或3-甲基-2 - 氧代-2,3-二氢-1H-苯并咪唑-1-基，当R'表示这些化合物的甲基自由基 - 外消旋体和对映异构体时，可用于治疗，特别是治疗投诉的新化合物 中枢神经系统和治疗抑郁症。

公开(公告)号：US4438121A

公开(公告)日：1984-03-20

申请号：US381749

申请日：1982-05-25

Applicant: Daniel Obitz

Inventor： Daniel Obitz

IPC: A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/47 ,  A61K31/472 ,  A61P25/24 ,  A61P25/26 ,  C07D209/08 ,  C07D209/46 ,  C07D209/48 ,  C07D215/22 ,  C07D215/227 ,  C07D217/24 ,  C07D235/26 ,  C07D217/02

CPC classification number: C07D209/48 ,  C07D209/08 ,  C07D209/46 ,  C07D215/227 ,  C07D217/24 ,  C07D235/26

Abstract: Heterocyclic amidoxime derivatives of the general formula: ##STR1## wherein R' represents hydrogen or the methyl radical, and R represents the 1-oxo-1H-isoquinolin-2-yl, 2-oxo-2H-quinolin-1-yl, 2,3-dihydro-1H-indol-1-yl, 1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl, 1H-indol-1-yl, 1-oxo-1,3-dihydro-2H-isoindol-2-yl, 2-oxo-3,4-dihydro-2H-quinolin-1-yl, 5-chloro-3-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl, 5-chloro-2-oxo-3-phenyl-2,3-dihydro-1H-benzimidazol-1-yl, 4-chloro-1-oxo-1H-isoquinolin-2-yl or 3-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl radical, and - when R' represents the methyl radical - racemates and enantiomers of such compounds, are new compounds useful in therapy, and especially for the treatment of complaints of the central nervous system and for the treatment of depression.

Abstract translation: 具有以下通式的杂环偕胺肟衍生物：其中R'表示氢或甲基，R表示1-氧代-1H-异喹啉-2-基，2-氧代-2H-喹啉-1-基，2 ，3-二氢-1H-吲哚-1-基，1,3-二氧代-1,3-二氢-2H-异吲哚-2-基，1H-吲哚-1-基，1-氧代-1,3-二氢 -2H-异吲哚-2-基，2-氧代-3,4-二氢-2H-喹啉-1-基，5-氯-3-甲基-2-氧代-2,3-二氢-1H-苯并咪唑-1-基 - 基，5-氯-2-氧代-3-苯基-2,3-二氢-1H-苯并咪唑-1-基，4-氯-1-氧代-1H-异喹啉-2-基或3-甲基-2 - 氧代-2,3-二氢-1H-苯并咪唑-1-基，和 - 当R'代表这些化合物的甲基自由基 - 外消旋体和对映异构体时，可用于治疗，特别是用于治疗 中枢神经系统和治疗抑郁症。

公开(公告)号：US4711892A

公开(公告)日：1987-12-08

申请号：US851113

申请日：1986-04-10

Applicant: Philippe Manoury ,  Daniel Obitz ,  Michel Peynot

Inventor： Philippe Manoury ,  Daniel Obitz ,  Michel Peynot

IPC: A61K31/44 ,  A61K31/443 ,  A61P31/04 ,  A61P33/02 ,  C07D405/12

CPC classification number: C07D405/12

Abstract: Nitrofuran derivatives corresponding to the formula (I). ##STR1## in which m is 0 or 1R is H or (C.sub.1-4)alkoxy are useful in treating bacterial, fungal, parasitic or protozan infections.

Abstract translation: 对应于式（I）的硝基呋喃衍生物。 其中m为0或1，R为H或（C1-4）烷氧基，可用于治疗细菌，真菌，寄生虫或原生动物感染。

公开(公告)号：US5010079A

公开(公告)日：1991-04-23

申请号：US388373

申请日：1989-08-02

Applicant: Philippe Manoury ,  Jean Binet ,  Daniel Obitz ,  Gerard Defosse ,  Elisabeth Dewitte ,  Corinne Veronique

Inventor： Philippe Manoury ,  Jean Binet ,  Daniel Obitz ,  Gerard Defosse ,  Elisabeth Dewitte ,  Corinne Veronique

IPC: A61K31/495 ,  A61P43/00 ,  C07D209/34 ,  C07D401/12

CPC classification number: C07D401/12 ,  C07D209/34

Abstract: An indolone derivative is useful for the treatment of anxiety, depression and schizophrenia and is a 5HT.sub.1A agonist and 5HT.sub.2 antagonist, which is a compound of formula (I): ##STR1## in which R.sub.1 is a hydrogen or halogen atom or a (C.sub.1-4)alkyl radical,R.sub.2 is a hydrogen atom or a (C.sub.1-4)alkyl radical,R.sub.3 is a hydrogen atom, a (C.sub.1-4)alkyl radical or an S-(C.sub.1-4) alkyl radical; andR.sub.4 is a phenyl, chlorophenyl, naphthyl, 7-methoxy-1-naphthyl, 6-methoxy-1-indanyl, 2-methoxy-6-pyridyl, 3-methoxy-2-pyridyl, isoquinolyl, 7-methoxy-1-isoquinolyl, 7-methoxy-1,2,3,4-tetrahydro-1-naphthyl or 7-fluoro-1-naphthyl radical;or a pharmaceutically acceptable acid addition salt thereof.

Abstract translation: 吲哚酮衍生物可用于治疗焦虑，抑郁和精神分裂症，并且是5HT1A激动剂和5HT2拮抗剂，其为式（I）的化合物：其中R 1为氢或卤素原子或（C1- 4）烷基，R 2是氢原子或（C 1-4）烷基，R 3是氢原子，（C 1-4）烷基或S-（C 1-4）烷基; 并且R 4是苯基，氯苯基，萘基，7-甲氧基-1-萘基，6-甲氧基-1-二氢化茚基，2-甲氧基-6-吡啶基，3-甲氧基-2-吡啶基，异喹啉基，7-甲氧基-1- 异喹啉基，7-甲氧基-1,2,3,4-四氢-1-萘基或7-氟-1-萘基; 或其药学上可接受的酸加成盐。

公开(公告)号：US4265911A

公开(公告)日：1981-05-05

申请号：US82656

申请日：1979-10-09

Applicant: Henry Najer ,  Daniel Obitz

Inventor： Henry Najer ,  Daniel Obitz

IPC: A61K31/155 ,  C07C123/00

CPC classification number: A61K31/155 ,  C07C259/14

Abstract: Propionamidoxime derivatives which are compounds of formula (I) ##STR1## in which A is a tetrahydronaphthyl or dihydronaphthyl radical and their pharmaceutically acceptable salts are valuable for treatment of the central nervous system and depression.The above compounds are prepared by reacting the nitrile (II) ##STR2## with hydroxylamine hydrochloride.

Abstract translation: 作为其中A为四氢萘基或二氢萘基的式（I）化合物的丙酰胺肟衍生物及其药学上可接受的盐对于治疗中枢神经系统和抑郁症是有价值的。 上述化合物通过使腈（II）与盐酸羟胺反应来制备。

公开(公告)号：US5530002A

公开(公告)日：1996-06-25

申请号：US385927

申请日：1995-02-09

Applicant: Phillip Manoury ,  Daniel Obitz ,  Michel Peynot ,  Mireille Sevrin ,  Pascal George

Inventor： Phillip Manoury ,  Daniel Obitz ,  Michel Peynot ,  Mireille Sevrin ,  Pascal George

IPC: C07D295/02 ,  A61K31/495 ,  A61P9/00 ,  A61P25/00 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/30 ,  C07D241/04 ,  C07D295/033 ,  C07D295/08 ,  C07D295/096

CPC classification number: C07D295/033 ,  C07D295/096

Abstract: Compounds of formula: ##STR1## in which X represents a hydrogen atom, a C.sub.1 -C.sub.3 alkoxy group or a cyclopropylmethoxy group and Y represents a hydrogen atom or a methoxy group, are useful in the therapy of conditions.

Abstract translation: 其中X表示氢原子，C1-C3烷氧基或环丙基甲氧基，Y表示氢原子或甲氧基的式（Ⅰ）化合物可用于条件治疗。

公开(公告)号：US4950670A

公开(公告)日：1990-08-21

申请号：US352342

申请日：1989-05-16

Applicant: Jonathan Frost ,  Bernard Gaudilliere ,  Jean Rousseau ,  Regis Dupont ,  Philippe Manoury ,  Daniel Obitz

Inventor： Jonathan Frost ,  Bernard Gaudilliere ,  Jean Rousseau ,  Regis Dupont ,  Philippe Manoury ,  Daniel Obitz

IPC: A61K31/505 ,  A61P9/12 ,  A61P25/04 ,  A61P25/06 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07D217/22 ,  C07D239/54 ,  C07D401/12

CPC classification number: C07D239/54 ,  C07D401/12

Abstract: A pyrimidinedione derivative which is a compound of formula (I): ##STR1## in which: R1 denotes hydrogen, a halogen, a methyl group or a methoxy group,R2 denotes hydrogen, a C.sub.1 -C.sub.4 alkyl group or a benzyl group,n denotes 2, 3 or 4,X denotes a CH group or nitrogen, andR3 denotes hydrogen, a halogen or a methoxy group when X denotes a CH group, with the proviso that R3 denotes hydrogen when X denotes nitrogen,or a pharmacologically acceptable acid addition salt thereof.

Abstract translation: 作为式（I）的化合物的嘧啶二酮衍生物：其中：R1表示氢，卤素，甲基或甲氧基，R2表示氢，C1-C4烷基或苄基，n 表示2,3或4，X表示CH基或氮，当X表示CH基时，R 3表示氢，卤素或甲氧基，条件是当X表示氮时，R3表示氢，或药理学上可接受的酸 加成盐。