公开(公告)号：EP1047678B1

公开(公告)日：2004-09-08

申请号：EP98957745.7

申请日：1998-11-10

Applicant: Warner-Lambert Company LLC

Inventor： BRYANS, Justin Stephen ,  CAPIRIS, Thomas ,  HORWELL, David Christopher ,  KNEEN, Clare Octavia ,  WUSTROW, David, Juergen

IPC: C07D257/04 ,  A61K31/41 ,  C07D271/06 ,  C07F9/38 ,  A61K31/66 ,  C07D291/04 ,  C07C311/10 ,  A61K31/18 ,  C07C311/07 ,  C07C239/14 ,  A61K31/16 ,  C07C309/25 ,  A61K31/255

CPC classification number: C07D257/04 ,  C07C233/36 ,  C07C239/14 ,  C07C259/06 ,  C07C309/25 ,  C07C311/05 ,  C07C311/09 ,  C07C311/33 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/46 ,  C07C2603/74 ,  C07D211/26 ,  C07D271/07 ,  C07D285/18 ,  C07D309/04 ,  C07D335/02 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06 ,  C07D419/06 ,  C07F9/3808 ,  C07F9/383 ,  C07F9/592 ,  C07F9/6552 ,  C07F9/655363

Abstract: Novel amines of formulas 1, 1C, 1F, 1G and 1H or a pharmaceutical acceptable salt thereof wherein n is an integer of from 0 to 2; m is an integer of from 0 to 3; R is sulfonamide, amide, heterocycle, sulfonic acid, or hydroxamic acid; A' is a bridged ring selected from wherein is the point of attachment; Z1 to Z4 are each independently selected from hydrogen and methyl; o is an integer of from 1 to 4; and p is an integer of from 0 to 2. In formula (1) above R cannot be sulfonic acid when m is 2 and n is 1 are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially irritable bowel syndrome.

Abstract translation: 式（1），（1C），（1F），（1G）和（1个H）或其药学上可接受的盐，其中n是从0至2的整数的新颖胺; m是从0至3的整数; R是磺酰胺，酰胺，膦酸基，杂环，磺酸，或异羟肟酸; A“是由式（1），（2），（3），（4），（5）是worin连接点中选择的桥连的环; Z1到Z4是选自氢和甲基中选择的每个unabhängig; o是1至4的整数; 且p是上述R为0〜2。在式（1）的整数不能磺酸当m为2和n为1的盘游离缺失和是有用的，如癫痫，昏厥发作，运动机能减退，颅异常的治疗剂 ，神经退行性疾病，抑郁症，焦虑，恐慌，疼痛，神经病理症状，特别是肠易激综合征。

公开(公告)号：EP1400526A2

公开(公告)日：2004-03-24

申请号：EP03027569.7

申请日：1998-11-10

Applicant: Warner-Lambert Company LLC

Inventor： Bellioti, Thomas Richard ,  Bryans, Justin Stephen ,  Capiris, Thomas ,  Horwell, David Christopher ,  Kneen, Clare Octavia ,  Wustrow, David Juergen

IPC: C07F9/38 ,  A61K31/41 ,  A61K31/66

CPC classification number: C07C311/32 ,  C07C233/36 ,  C07C239/14 ,  C07C259/06 ,  C07C309/25 ,  C07C311/05 ,  C07C311/09 ,  C07C311/33 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/46 ,  C07C2603/74 ,  C07D211/26 ,  C07D257/04 ,  C07D271/07 ,  C07D285/18 ,  C07D309/04 ,  C07D335/02 ,  C07D401/06 ,  C07D405/06 ,  C07D407/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06 ,  C07D419/06 ,  C07F9/3808 ,  C07F9/383 ,  C07F9/592 ,  C07F9/6552 ,  C07F9/655363

Abstract: Novel amines of formulas (1A) and (1B) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially IBS. Processes for the preparation and intermediates useful in the preparation are also disclosed.
R is sulfonamide,
amide,
sulfonic acid,
or phosphonic acid.

Abstract translation: 公开了式（1A）和（1B）的新型胺并且可用作治疗癫痫，晕厥发作，运动机能减退，颅脑疾病，神经变性疾病，抑郁症，焦虑症，恐慌症，疼痛，神经病理性疾病，炎性疾病和 胃肠疾病，特别是IBS。 还公开了用于制备的制备方法和中间体。 R是磺酰胺，酰胺，磺酸或膦酸。

公开(公告)号：EP1475371A1

公开(公告)日：2004-11-10

申请号：EP04006036.0

申请日：1998-11-10

Applicant: Warner-Lambert Company LLC

Inventor： Bryans, Justin Stephen ,  Capiris, Thomas ,  Horwell, David Christopher ,  Kneen, Clare Octavia ,  Wustrow, David Juergen

IPC: C07D257/04 ,  A61K31/41 ,  C07D271/06 ,  C07F9/38 ,  A61K31/66 ,  C07D291/04 ,  C07C311/10 ,  A61K31/18 ,  C07C311/07 ,  C07C239/14 ,  A61K31/16 ,  C07C309/25 ,  A61K31/255

CPC classification number: C07D257/04 ,  C07C233/36 ,  C07C239/14 ,  C07C259/06 ,  C07C309/25 ,  C07C311/05 ,  C07C311/09 ,  C07C311/33 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/46 ,  C07C2603/74 ,  C07D211/26 ,  C07D271/07 ,  C07D285/18 ,  C07D309/04 ,  C07D335/02 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06 ,  C07D419/06 ,  C07F9/3808 ,  C07F9/383 ,  C07F9/592 ,  C07F9/6552 ,  C07F9/655363

Abstract: Novel amines of formulas 1, 1C, 1F, 1G and 1H
or a pharmaceutical acceptable salt thereof wherein
n is an integer of from 0 to 2;
m is an integer of from 0 to 3;
R is sulfonamide,
amide,
heterocycle,
sulfonic acid, or
hydroxamic acid;
A' is a bridged ring selected from
wherein
is the point of attachment;
Z 1 to Z 4 are each independently selected from hydrogen and methyl;
o is an integer of from 1 to 4; and
p is an integer of from 0 to 2.
In formula (1) above R cannot be sulfonic acid when m is 2 and n is 1 are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially irritable bowel syndrome.

Abstract translation: 式1的新颖cardamines，1C，1F，1G和1H 或其worin n中的药物上可接受的盐是从0到2的整数; m是从0至3的整数; R是磺酰胺，酰胺，杂环，磺酸，或异羟肟酸; A“是从中选择的桥环worin是连接点; Z1到Z4是选自氢和甲基中选择的每个unabhängig; o是1至4的整数; 且p是上述R为0〜2。在式（1）的整数不能磺酸当m为2和n为1的盘游离缺失和是有用的，如癫痫，昏厥发作，运动机能减退，颅异常的治疗剂 ，神经退行性疾病，抑郁症，焦虑，恐慌，疼痛，神经病理疾病，炎性疾病和胃肠功能紊乱，尤其是爱情肠易激综合征。

公开(公告)号：EP1045834A1

公开(公告)日：2000-10-25

申请号：EP98958528.6

申请日：1998-11-10

Applicant: WARNER-LAMBERT COMPANY

Inventor： BRYANS, Justin Stephen ,  HORWELL, David Christopher ,  KNEEN, Clare Octavia ,  WUSTROW, David, Juergen

IPC: C07D211/26 ,  A61K31/445 ,  C07D211/34 ,  C07F9/38 ,  A61K31/66 ,  C07D413/06 ,  C07D401/06 ,  C07D417/06 ,  C07D419/06 ,  C07D309/04 ,  A61K31/35 ,  A61K31/41 ,  C07D407/06 ,  C07D335/02 ,  A61K31/38

CPC classification number: C07F9/655363 ,  C07C233/36 ,  C07C239/14 ,  C07C259/06 ,  C07C309/25 ,  C07C311/05 ,  C07C311/09 ,  C07C311/33 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/46 ,  C07C2603/74 ,  C07D211/26 ,  C07D257/04 ,  C07D271/07 ,  C07D285/18 ,  C07D309/04 ,  C07D335/02 ,  C07D401/06 ,  C07D405/06 ,  C07D407/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06 ,  C07D419/06 ,  C07F9/3808 ,  C07F9/383 ,  C07F9/592 ,  C07F9/6552

Abstract: Novel amines of formulas 1D and 1Eare disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially IBS. Processes for the preparation and intermediates useful in the preparation are also disclosed.

Abstract translation: 公式一维和1Eare盘的新cardamines游离缺失的，且与癫痫，昏厥发作，运动机能减退，颅异常，神经退行性疾病，抑郁症，焦虑，恐慌，疼痛，神经病理疾病，炎性疾病和胃肠功能紊乱，爱尤其是肠易激综合征的治疗剂 ， 因此用于制备和中间体在制备有用的方法是游离缺失盘。

公开(公告)号：EP2234961A2

公开(公告)日：2010-10-06

申请号：EP08851324.7

申请日：2008-11-20

Applicant: LEO PHARMA A/S

Inventor： FENSHOLDT, Jef ,  HAVEZ, Sophie Elisabeth ,  NØRREMARK, Bjarne

IPC: C07C211/35 ,  C07C211/36 ,  C07C211/48 ,  C07C215/28 ,  C07C217/52 ,  C07C217/74 ,  C07C233/05 ,  C07C233/41 ,  C07C237/24 ,  C07C237/30 ,  C07C237/32 ,  C07C237/34 ,  C07C237/36 ,  C07C237/40 ,  C07C239/14

CPC classification number: C07D295/182 ,  C07C211/35 ,  C07C211/36 ,  C07C211/48 ,  C07C215/28 ,  C07C217/52 ,  C07C217/74 ,  C07C233/05 ,  C07C233/41 ,  C07C237/24 ,  C07C237/30 ,  C07C237/32 ,  C07C237/34 ,  C07C237/36 ,  C07C237/40 ,  C07C239/14 ,  C07C255/03 ,  C07C255/32 ,  C07C255/50 ,  C07C257/18 ,  C07C259/10 ,  C07C259/18 ,  C07C271/44 ,  C07C309/15 ,  C07C311/05 ,  C07C311/08 ,  C07C311/37 ,  C07C311/51 ,  C07C317/32 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07D205/04 ,  C07D207/08 ,  C07D207/12 ,  C07D207/16 ,  C07D207/27 ,  C07D209/08 ,  C07D209/12 ,  C07D209/20 ,  C07D211/46 ,  C07D211/60 ,  C07D211/62 ,  C07D213/30 ,  C07D213/38 ,  C07D213/40 ,  C07D213/80 ,  C07D231/12 ,  C07D231/40 ,  C07D233/61 ,  C07D233/90 ,  C07D263/22 ,  C07D271/06 ,  C07D295/088 ,  C07D295/13 ,  C07D295/135 ,  C07D295/192 ,  C07D295/195 ,  C07D295/26 ,  C07D305/08 ,  C07D307/12 ,  C07D307/52 ,  C07D307/68 ,  C07D307/79 ,  C07D309/10 ,  C07D319/18 ,  C07D333/38 ,  C07D333/40 ,  C07D333/58 ,  C07D413/04 ,  C07D413/06 ,  C07D417/06

Abstract: The invention relates to novel cyclic hydrocarbon compounds and derivatives thereof, processes for the preparation thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.

Abstract translation: 本发明涉及新型环状烃化合物及其衍生物，其制备方法，用作药物的所述化合物，用于治疗的所述化合物，包含所述化合物的药物组合物，涉及用所述化合物治疗疾病的方法 ，以及所述化合物在制备药物中的用途。

公开(公告)号：EP1400526A3

公开(公告)日：2004-03-31

申请号：EP03027569.7

申请日：1998-11-10

Applicant: Warner-Lambert Company LLC

Inventor： Bellioti, Thomas Richard ,  Bryans, Justin Stephen ,  Capiris, Thomas ,  Horwell, David Christopher ,  Kneen, Clare Octavia ,  Wustrow, David Juergen

IPC: C07F9/38 ,  A61K31/41 ,  A61K31/66

CPC classification number: C07C311/32 ,  C07C233/36 ,  C07C239/14 ,  C07C259/06 ,  C07C309/25 ,  C07C311/05 ,  C07C311/09 ,  C07C311/33 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/46 ,  C07C2603/74 ,  C07D211/26 ,  C07D257/04 ,  C07D271/07 ,  C07D285/18 ,  C07D309/04 ,  C07D335/02 ,  C07D401/06 ,  C07D405/06 ,  C07D407/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06 ,  C07D419/06 ,  C07F9/3808 ,  C07F9/383 ,  C07F9/592 ,  C07F9/6552 ,  C07F9/655363

Abstract: Novel amines of formulas (1A) and (1B) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially IBS. Processes for the preparation and intermediates useful in the preparation are also disclosed. R is sulfonamide, amide, sulfonic acid, or phosphonic acid.

Abstract translation: 式（1A）和（1B）的新颖cardamines是圆盘游离缺失和是有用的，如癫痫，昏厥发作，运动机能减退，颅异常，神经变性疾病，抑郁症，焦虑，恐慌，疼痛，神经病理疾病，炎性疾病的治疗剂，以及 胃肠功能紊乱，肠易激综合征爱情更是如此。 因此用于制备和中间体在制备有用的方法是游离缺失盘。 R是磺酰胺，酰胺，磺酸，或膦酸。

公开(公告)号：EP1045839A2

公开(公告)日：2000-10-25

申请号：EP98962805.2

申请日：1998-11-10

Applicant: WARNER-LAMBERT COMPANY

Inventor： BELLIOTTI, Thomas, Richard ,  BRYANS, Justin Stephen ,  CAPIRIS, Thomas ,  HORWELL, David Christopher ,  KNEEN, Clare Octavia ,  WUSTROW, David, Juergen

IPC: C07D257/04

CPC classification number: C07C311/32 ,  C07C233/36 ,  C07C239/14 ,  C07C259/06 ,  C07C309/25 ,  C07C311/05 ,  C07C311/09 ,  C07C311/33 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/46 ,  C07C2603/74 ,  C07D211/26 ,  C07D257/04 ,  C07D271/07 ,  C07D285/18 ,  C07D309/04 ,  C07D335/02 ,  C07D401/06 ,  C07D405/06 ,  C07D407/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06 ,  C07D419/06 ,  C07F9/3808 ,  C07F9/383 ,  C07F9/592 ,  C07F9/6552 ,  C07F9/655363

Abstract: Novel amines of formulas (1A) and (1B) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially IBS. Processes for the preparation and intermediates useful in the preparation are also disclosed. R is sulfonamide, amide, sulfonic acid, or phosphonic acid.

公开(公告)号：EP3366669A2

公开(公告)日：2018-08-29

申请号：EP16856928.3

申请日：2016-10-21

Applicant: Technical Institute of Physics and Chemistry of the Chinese Academy of Sciences

Inventor： WANG, Pengfei ,  WU, Jiasheng ,  LIU, Weimin ,  GU, Ying ,  GE, Jiechao ,  ZHENG, Xiuli ,  ZHANG, Hongyan

IPC: C07C221/00 ,  C07C225/32 ,  C07C249/02 ,  C07C251/24 ,  C07C319/18 ,  C07C323/25 ,  C07C213/06 ,  C07C217/12 ,  A61K41/00 ,  A61P35/00

CPC classification number: A61K31/473 ,  A61K31/122 ,  A61K31/135 ,  A61K41/0057 ,  A61K47/54 ,  A61K47/543 ,  A61K47/60 ,  A61P35/00 ,  C07C50/36 ,  C07C217/12 ,  C07C221/00 ,  C07C225/22 ,  C07C225/32 ,  C07C229/18 ,  C07C237/08 ,  C07C239/14 ,  C07C243/22 ,  C07C249/02 ,  C07C251/24 ,  C07C251/56 ,  C07C251/86 ,  C07C309/69 ,  C07C319/18 ,  C07C323/25 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07D213/00 ,  C07D221/02

Abstract: The invention discloses a monosubstituted or polysubstituted amphiphilic hypocrellin derivative, and a preparation method and application thereof. The amphiphilic hypocrellin derivative substituted by a group containing PEG, a quaternary ammonium salt or the like prepared according to the invention has an obvious red shift in its absorption spectrum and a significantly enhanced molar extinction coefficient, compared with the parent hypocrellin, can efficiently produce singlet state oxygen and other reactive oxygen species under photosensitive conditions; has different amphiphilicities and increased biocompatibility with cells or tissues by regulating its hydrophilicity and hydrophobicity; can meet the requirements of different clinical drugs, and solves the requirements of different drug delivery methods for different drug hydrophilicity and lipophilicity. Under identical conditions, the amphiphilic hypocrellin derivative photosensitizer according to the invention has higher ability to photodynamically inactivate tumor cells than the first and second generation commercial photosensitizers.

公开(公告)号：EP1049662B1

公开(公告)日：2006-06-21

申请号：EP99904115.5

申请日：1999-01-19

Applicant: TANABE SEIYAKU CO., LTD.

Inventor： SIRCAR, Ila ,  GUDMUNDSSON, Kristjan, S. ,  MARTIN, Richard

IPC: C07C233/87 ,  C07C237/30 ,  C07C271/28 ,  C07C311/09 ,  C07D295/14 ,  C07D333/34 ,  A61K31/245 ,  A61K31/33

CPC classification number: C07D207/08 ,  C07C31/44 ,  C07C233/51 ,  C07C233/87 ,  C07C235/84 ,  C07C237/30 ,  C07C237/32 ,  C07C237/36 ,  C07C237/42 ,  C07C239/14 ,  C07C251/40 ,  C07C255/16 ,  C07C255/57 ,  C07C255/60 ,  C07C271/28 ,  C07C275/54 ,  C07C311/08 ,  C07C311/09 ,  C07C311/16 ,  C07C311/21 ,  C07C311/29 ,  C07C311/46 ,  C07C311/51 ,  C07C335/22 ,  C07D207/27 ,  C07D207/327 ,  C07D207/33 ,  C07D207/333 ,  C07D207/337 ,  C07D207/34 ,  C07D207/404 ,  C07D211/22 ,  C07D213/26 ,  C07D213/30 ,  C07D213/54 ,  C07D213/74 ,  C07D213/81 ,  C07D213/82 ,  C07D231/12 ,  C07D233/72 ,  C07D239/52 ,  C07D241/12 ,  C07D241/24 ,  C07D257/04 ,  C07D261/08 ,  C07D277/18 ,  C07D277/22 ,  C07D277/24 ,  C07D295/13 ,  C07D295/155 ,  C07D295/185 ,  C07D295/192 ,  C07D307/79 ,  C07D311/58 ,  C07D317/60 ,  C07D319/18 ,  C07D333/12 ,  C07D333/16 ,  C07D333/22 ,  C07D333/24 ,  C07D333/32 ,  C07D333/34 ,  C07D333/38 ,  C07D491/10

Abstract: The present invention relates to a pharmaceutical composition comprising as an active ingredient a compound of formula (I), wherein Ring A is an aromatic or a heterocyclic ring; Q is a bond, carbonyl, lower alkylene, lower alkenylene, -O-(lower alkylene)-, etc.; n is 0, 1 or 2; Z is oxygen or sulfur; W is oxygen, sulfur, -CH=CH-, -NH- or -N=CH-; R?1, R2 and R3¿ are the same or different and are hydrogen, halogen, hydroxyl, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkoxy group, a substituted or unsubstituted amino group, etc.; R4 is tetrazolyl, carboxyl group, amide or ester; R5 is hydrogen, nitro, amino, hydroxyl, lower alkanoyl, lower alkyl, etc.; R6 is selected from (a) a substituted or unsubstituted phenyl group, (b) a substituted or unsubstituted pyridyl group, (c) a substituted or unsubstituted thienyl group, (d) a substituted or unsubstituted benzofuranyl group, etc.; or a pharmaceutically acceptable salt thereof.

公开(公告)号：EP1052984B1

公开(公告)日：2004-05-12

申请号：EP99904977.8

申请日：1999-02-05

Applicant: Vernalis (Oxford) Ltd

Inventor： HUNTER, Michael George ,  BECKETT, Raymond Paul ,  CLEMENTS, John Martin ,  WHITTAKER, Mark ,  DAVIES, Stephen John ,  PRATT, Lisa Marie ,  SPAVOLD, Zoe Marie ,  LAUNCHBURY, Steven

IPC: A61K31/16 ,  A61K31/535 ,  A61K31/165 ,  A61K31/44 ,  A61K31/40 ,  A61K31/195 ,  A61K31/47 ,  A61K31/495 ,  A61K31/445 ,  A61K31/00 ,  A61P31/04

CPC classification number: C07C259/06 ,  A61K31/00 ,  A61K31/16 ,  A61K31/164 ,  A61K31/165 ,  A61K31/198 ,  A61K31/40 ,  A61K31/401 ,  A61K31/4402 ,  A61K31/445 ,  A61K31/4453 ,  A61K31/47 ,  A61K31/472 ,  A61K31/495 ,  A61K31/5375 ,  C07C239/14 ,  C07C323/60 ,  C07C2601/08 ,  C07C2601/14 ,  C07D213/75 ,  C07D217/26 ,  C07D263/26 ,  C07D295/185 ,  C07K5/0202