公开(公告)号：EP2501231B1

公开(公告)日：2016-12-21

申请号：EP10832030.0

申请日：2010-11-15

Applicant: Merck Sharp & Dohme Corp.

Inventor： KUDUK, Scott, D. ,  CHANG, Ronald, K. ,  GRESHOCK, Thomas, J.

IPC: A01N43/42 ,  A61K31/44 ,  A61K31/47 ,  C07D471/04

CPC classification number: C07D221/02 ,  C07D241/02 ,  C07D471/04 ,  C07D519/00

公开(公告)号：EP2252299A1

公开(公告)日：2010-11-24

申请号：EP09711011.8

申请日：2009-02-04

Applicant: Merck Sharp & Dohme Corp.

Inventor： BESHORE, Douglas, C. ,  DIPARDO, Robert, M. ,  KUDUK, Scott, D.

IPC: A61K31/535

CPC classification number: C07D221/02 ,  C07D215/56 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D405/10 ,  C07D409/10 ,  C07D409/14 ,  C07D413/10

Abstract: The present invention is directed to fused pyridone compounds of formula (I) (I) that are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

公开(公告)号：EP4431612A1

公开(公告)日：2024-09-18

申请号：EP23162704.3

申请日：2023-03-17

Applicant: Universität Graz

Inventor： Kroutil, Wolfgang ,  Pletz, Jakob ,  Cigan, Emmanuel

IPC: C12P17/12 ,  C12P15/00 ,  C07C231/02 ,  C07C233/08 ,  C07D221/02

CPC classification number: C07C231/02 ,  C07D221/02 ,  C12P15/00 ,  C12P17/12

Abstract: Die Erfindung betrifft ein Verfahren zur Herstellung von Corytuberin und Salutaridin über Reticulin als Zwischenprodukt, wobei das Verfahren die folgenden Reaktionsschritte umfasst:
a) Amidierung von 2-(4-Hydroxy-3-methoxyphenyl)-N-methylethanamin (12) mit 3-Hydroxy-4-methoxyphenylessigsäure zum N-[2-(4-Hydroxy-3-methoxyphenyl)ethyl-N-methyl-3-hydroxy-4-methoxyphenylessigsäureamid (13):

b) Bischler-Napieralski-Zyklisierung des tertiären Amids (13) zu 1,2-Dehydroreticulin (14):

c) biokatalytische enantioselektive Hydrierung von 1,2-Dehydroreticulin (14) zu Reticulin (15) und zwar entweder
c1) unter Verwendung einer Imin-Reduktase zu (S)-Reticulin (S)-(15) oder
c2) unter Verwendung einer Dehydroreticulin-Reduktase zu (R)-Reticulin (R)-(15):


d) biokatalytische oxidative Phenol-Kupplung zwischen den beiden aromatischen Ringen des jeweiligen Reticulins und zwar entweder
d1) ortho-ortho-Kupplung von (S)-Reticulin in Gegenwart von Corytuberin-Synthase (CorSyn) zu Corytuberin (16) oder
d2) ortho-para-Kupplung von (R)-Reticulin in Gegenwart von Salutaridin-Synthase (SalSyn) zu Salutaridin (17):

公开(公告)号：EP2501231A4

公开(公告)日：2013-05-15

申请号：EP10832030

申请日：2010-11-15

Applicant: MERCK SHARP & DOHME

Inventor： KUDUK SCOTT D ,  CHANG RONALD K ,  GRESHOCK THOMAS J

IPC: A01N43/42 ,  A61K31/44 ,  A61K31/47 ,  C07D471/04

CPC classification number: C07D221/02 ,  C07D241/02 ,  C07D471/04 ,  C07D519/00

公开(公告)号：EP2252299A4

公开(公告)日：2013-01-09

申请号：EP09711011

申请日：2009-02-04

Applicant: MERCK SHARP & DOHME

Inventor： BESHORE DOUGLAS C ,  DIPARDO ROBERT M ,  KUDUK SCOTT D

IPC: A61K31/535 ,  A61P25/28 ,  C07D215/56 ,  C07D221/02 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D405/10 ,  C07D409/10 ,  C07D409/14 ,  C07D413/10

CPC classification number: C07D221/02 ,  C07D215/56 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D405/10 ,  C07D409/10 ,  C07D409/14 ,  C07D413/10

公开(公告)号：EP2501231A1

公开(公告)日：2012-09-26

申请号：EP10832030.0

申请日：2010-11-15

Applicant: Merck Sharp & Dohme Corp.

Inventor： KUDUK, Scott, D. ,  CHANG, Ronald, K. ,  GRESHOCK, Thomas, J.

IPC: A01N43/42 ,  A61K31/44 ,  A61K31/47

CPC classification number: C07D221/02 ,  C07D241/02 ,  C07D471/04 ,  C07D519/00

Abstract: The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

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：EP3228616A4

公开(公告)日：2018-04-25

申请号：EP15865019

申请日：2015-12-04

Applicant: ASTELLAS PHARMA INC ,  KOTOBUKI PHARMACEUTICAL CO LTD

Inventor： KAWAGUCHI KENICHI ,  ISHIHATA AKIHIRO ,  KANAI AKIRA ,  TSUCHIYA KAZUYUKI ,  INAGAKI YUSUKE ,  KAZAMI JUNICHI ,  MORIKAWA HIROSHI ,  HIRAMOTO MASASHI ,  ENJO KENTARO ,  TAKAMATSU HAJIME

IPC: C07D213/55 ,  A61K31/435 ,  A61K31/438 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/4433 ,  A61K31/444 ,  A61K31/472 ,  A61K31/4747 ,  A61P7/12 ,  A61P13/00 ,  A61P43/00 ,  C07D213/63 ,  C07D217/16 ,  C07D221/02 ,  C07D221/04 ,  C07D221/20 ,  C07D401/04 ,  C07D405/04

CPC classification number: C07D405/04 ,  A61K31/435 ,  A61K31/438 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/4433 ,  A61K31/444 ,  A61K31/472 ,  A61K31/4747 ,  A61P7/12 ,  C07D213/55 ,  C07D213/63 ,  C07D217/16 ,  C07D217/24 ,  C07D221/02 ,  C07D221/04 ,  C07D221/20 ,  C07D401/04

Abstract: The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically an agent for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-(pyridylmethyl)-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.

公开(公告)号：EP3277680A1

公开(公告)日：2018-02-07

申请号：EP16711288.7

申请日：2016-03-23

Applicant: BASF SE

Inventor： GRAMMENOS, Wassilios ,  BOUDET, Nadege ,  MUELLER, Bernd ,  WOLF, Antje ,  ESCRIBANO CUESTA, Ana ,  CAMBEIS, Erica ,  LOHMANN, Jan Klaas ,  GROTE, Thomas ,  KRETSCHMER, Manuel ,  HADEN, Egon ,  FEHR, Marcus

IPC: C07D471/04 ,  A01N43/00 ,  C07D491/048 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

CPC classification number: C07D221/02 ,  A01N43/42 ,  A01N43/90 ,  C07D213/04 ,  C07D401/04 ,  C07D471/04 ,  C07D491/048 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

Abstract: wherein the variables are defined as given in the description and claims. The invention further relates to uses, processes and intermediates for compounds I.

公开(公告)号：EP2018165B1

公开(公告)日：2011-04-13

申请号：EP07717861.4

申请日：2007-01-12

Applicant: Sanofi-Aventis

Inventor： BONO, Françoise ,  GUILLO, Nathalie ,  MAFFRAND, Jean-Pierre ,  FONS, Pierre ,  OLSEN, Jacob-Alsboek ,  ANNE-ARCHARD, Gilles

IPC: A61K31/435 ,  A61P9/00 ,  A61P11/00 ,  C07D519/00

CPC classification number: C07D519/00 ,  A61K31/435 ,  A61K47/55 ,  C07D209/02 ,  C07D221/02

Abstract: FGF receptor agonist compounds corresponding to the general formula: M1-L-M2 in which M1 and M2, which may be identical or different, each represent, independently of one another, a monomer unit M, and L represents a linker group which covalently links M1 and M2, wherein said monomer unit corresponds to the general formula M which follows: (I). Preparation process and therapeutic use.