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公开(公告)号：TR201815872T4
公开(公告)日：2018-11-21
申请号：TR201815872
申请日：2015-08-04
Applicant: HOFFMANN LA ROCHE
Inventor： KONRAD BLEICHER , ANTON CUENI , KURT PUENTENER , JUNICHI SHIINA
Abstract: Mevcut buluş, formül I'in oksitosin analoglarının hazırlanması için yeni bir prosesi içermekte olup burada R1, hidrojen veya C1-7-alkil'dir ve R1, hidrojen veya C1-7-alkil'dir; veya R1 ve R2, eklendikleri nitrojen ve karbon atomu ile birlikte, tercihe göre hidroksi veya halojen ile ornatılan 5 üyeli bir heterosikl oluşturur; R3, C1-7-alkil'dir. Formül I'in oksitosin analogları, reseptör agonistleri olarak hareket eder ve nörolojik bozuklukların tedavisinde kullanılmak üzere potansiyele sahiptir.
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公开(公告)号：MX2018005236A
公开(公告)日：2018-08-15
申请号：MX2018005236
申请日：2016-10-24
Applicant: HOFFMANN LA ROCHE
Inventor： HANS HILPERT , HONG SHEN , TAISHAN HU , SABINE KOLCZEWSKI , THEODOR STOLL , KONRAD BLEICHER , BERNHARD FASCHING , ALEXANDER ALANINE , JULIEN BEIGNET , DWIGHT MACDONALD , STEPHEN JACKSON , CARSTEN KROLL , ADRIAN SCHAEUBLIN , HELMUT THOMAS , AMAL WAHHAB , CLAUDIA ZAMPALONI
Abstract: La presente invención proporciona compuestos de fórmula (I) (ver formula) (I) en donde de X1 a X8 y de R1 a R8 son tal como se definen en el presente documento, así como sales farmacéuticamente aceptables de los mismos. Además, la presente invención se refiere a la fabricación de compuestos de fórmula (I), composiciones farmacéuticas que los comprenden y su uso como medicamentos para el tratamiento de enfermedades e infecciones causadas por Acinetobacter baumannii.
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公开(公告)号：MY126586A
公开(公告)日：2006-10-31
申请号：MYPI20001650
申请日：2000-04-18
Applicant: HOFFMANN LA ROCHE
Inventor： THOMAS JOHANNES WOLTERING , JURGEN WICHMANN , VINCENT MUTEL , ERIC VIEIRA , KONRAD BLEICHER
IPC: C07D295/08 , C07D335/14 , A61K31/325 , A61K31/352 , A61K31/381 , A61K31/382 , A61K31/421 , A61K31/422 , A61K31/4245 , A61K31/4409 , A61K31/5375 , A61P25/00 , A61P25/06 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/34 , A61P27/02 , C07C233/90 , C07C233/91 , C07C271/64 , C07C333/10 , C07C333/16 , C07D213/00 , C07D213/30 , C07D213/60 , C07D213/61 , C07D263/48 , C07D271/00 , C07D271/06 , C07D271/07 , C07D271/10 , C07D271/113 , C07D295/088 , C07D311/84 , C07D333/16 , C07D335/12 , C07D409/12 , C07D413/12
Abstract: THE PRESENT INVENTION RELATES TO COMPOUNDS OF FORMULA WHEREIN R1 SIGNIFIES HYDROGEN OR LOWER ALKYL; R2, R2' SIGNIFY, INDEPENDENTLY FROM EACH OTHER, HYDROGEN, LOWER ALKYL, LOWER ALKOXY, HALOGEN OR TRIFLUOROMETHYL; X SIGNIFIES O, S OR TWO HYDROGEN ATOMS NOT FORMING A BRIDGE; A1/A2 SIGNIFY, INDEPENDENTLY FROM EACH OTHER, PHENYL OR A 6-MEMBERED HETEROCYCLE CONTAINING 1 OR 2 NITROGEN ATOMS; B IS A GROUP OF FORMULA WHEREIN R3 SIGNIFIES LOWER ALKYL, LOWER ALKENYL, LOWER ALKINYL, BENZYL, LOWER ALKYL-CYCLOALKYL, LOWER ALKYL-CYANO, LOWER ALKYL-PYRIDINYL, LOWER ALKYL-LOWER ALKONYL-PHENYL, LOWER ALKYL-PHENYL, WHICH IS OPTIONALLY SUBSTITUTED BY LOWER ALKOXY, OR PHENYL, WHICH IS OPTIONALLY SUBSTITUTED BY LOWER ALKOXY, OR LOWER ALKYL-THIENYL, CYCLOALKYL, LOWER ALKYLTRIFIUOROMETHYL OR LOWER ALKYL-MORPHOLINYL, Y SIGNIFIES -O-, -S- OR A BOND; Z SIGNIFIES -O- OR -S-; OR B IS A 5-MEMBERED HETEROCYCLIC GROUP OF FORMULAS WHEREIN R4 AND R5 SIGNIFIES HYDROGEN, LOWER ALKYL, LOWER ALKOXY, CYCLOHEXYL, LOWER ALKYL-CYCLOHEXYL OR TRIFLUOROMETHYL, WITH THE PROVISO THAT AT LEAST ONE OF R4 OR R5 HAS TO BE HYDROGEN; AS WELL AS TO THEIR PHARMACEUTICALLY ACCEPTABLE SALTS.THESE COMPOUNDS MAY BE USED IN THE CONTROL OR PREVENTION OF ACUTE AND/OR CHRONIC NEUROLOGICAL DISORDERS SUCH AS RESTRICTED BRAIN FUNCTION CAUSED BY BYPASS OPERATIONS OR TRANSPLANTS, POOR BLOOD SUPPLY TO THE BRAIN, SPINAL CORD INJURIES, HEAD INJURIES, HYPOXIA CAUSED BY PREGNANCY, CARDIAC ARREST, HYPOGLYCAEMIA, ALZHEIMER'S DISEASE, HUNTINGTON'S CHOREA, ALS, DEMENTIA CAUSED BY AIDS, EYE INJURIES, RETINOPATHY, COGNITIVE DISORDERS, MEMORY DEFICITS, SCHIZOPHRENIA, IDIOPATHIC PARKINSONISM OR PARKINSONISM CAUSED BY MEDICAMENTS AS WELL AS CONDITIONS WHICH LEAD TO GLUTAMATE DEFICIENCY FUNCTIONS, SUCH AS E.G. MUSCLE SPASMS, CONVULSIONS, MIGRAINE, URINARY INCONTINENCE, NICOTINE ADDICTION, PSYCHOSES, OPIATE ADDICTION, ANXIETY, VOMITING, ACUTE AND CHRONIC PAIN, DYSKINESIA AND DEPRESSION.
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公开(公告)号：BRPI0919248A2
公开(公告)日：2019-09-24
申请号：BRPI0919248
申请日：2009-09-15
Applicant: HOFFMANN LA ROCHE
Inventor： BERND KUHN , GREGORY MARTIN BENSON , HANS RICHTER , JEAN-MARC PLANCHER , KONRAD BLEICHER , MARKUS RUDOLPH , RAINER E MARTIN , SONG FENG , SVEN TAYLOR , UWE GRETHER
IPC: C07D231/56 , A61K31/416 , A61P3/06 , A61P3/10 , C07D401/12 , C07D407/12
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公开(公告)号：ZA200806510B
公开(公告)日：2009-11-25
申请号：ZA200806510
申请日：2008-07-25
Applicant: HOFFMANN LA ROCHE
Inventor： JEAN ACKERMANN , KONRAD BLEICHER , CECCARELLI SIMONA M , ODILE CHOMIENNE , PATRIZIO MATTEI , ULRIKE OBST SANDER
IPC: A61K20100101 , A61P20100101 , C07D20100101
Abstract: The invention is concerned with novel heterobicyclic derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, V, W, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
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Patent Agency Ranking
公开(公告)号：ZA200804393B
公开(公告)日：2009-04-29
申请号：ZA200804393
申请日：2008-05-21
Applicant: HOFFMANN LA ROCHE
Inventor： JEAN ACKERMANN , KONRAD BLEICHER , CECCARELLI GRENZ SIMONA M , ODILE CHOMIENNE , PATRIZIO MATTEI , TANJA SCHULZ-GASCH
IPC: A61K20090101 , A61P20090101 , C07D20090101
Abstract: The invention is concerned with novel substituted piperidine derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
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公开(公告)号：BR112020021729A2
公开(公告)日：2021-01-26
申请号：BR112020021729
申请日：2019-04-23
Applicant: HOFFMANN LA ROCHE
Inventor： CHRISTIAN JENNY , DANIELLA CHEANG , KONRAD BLEICHER , PATRICK DI GIORGIO , PATRIZIO MATTEI , PETRA SCHMITZ , TAISHAN HU , THEODOR STOLL
Abstract: a presente invenção proporciona compostos de fórmula (i), em que x1, x2, r1 a r6 e a são como descritos neste documento, bem como seus sais farmaceuticamente aceitáveis. além disso, a presente invenção refere-se à fabricação dos compostos de fórmula (i), às composições farmacêuticas compreendendo-os e ao seu uso como medicamentos para o tratamento de doenças e infecções causadas por bactérias.
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公开(公告)号：BR112019021049A2
公开(公告)日：2020-05-12
申请号：BR112019021049
申请日：2018-04-09
Applicant: HOFFMANN LA ROCHE
Inventor： ADRIAN SCHAEUBLIN , ALEXANDER ALANINE , BERNHARD FASCHING , CARSTEN KROLL , CLAUDIA ZAMPALONI , HANS HILPERT , KONRAD BLEICHER , KURT AMREIN , SABINE KOLCZEWSKI
Abstract: a presente invenção refere-se aos compostos da fórmula (i) em que x1 a x8 e r1 a r8 são tais como descritos no presente caso, bem como os seus sais farmaceuticamente aceitáveis para o uso no tratamento ou prevenção de infecções e enfermidades resultantes causadas pela pseudomonas aeruginosa.
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公开(公告)号：BRPI0920198A2
公开(公告)日：2018-05-22
申请号：BRPI0920198
申请日：2009-10-06
Applicant: HOFFMANN LA ROCHE
Inventor： BERND KUHN , GREGORY MARTIN BENSON , HANS RICHTER , JEAN-MARC PLANCHER , KONRAD BLEICHER , RAINER E MARTIN , SONG FENG , SVEN TAYLOR , UWE GRETHER
IPC: C07D235/18 , A61K31/4184 , A61P3/00
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公开(公告)号：MX2016016050A
公开(公告)日：2017-02-28
申请号：MX2016016050
申请日：2015-08-04
Applicant: HOFFMANN LA ROCHE
Inventor： KURT PUENTENER , KONRAD BLEICHER , ANTON CUENI , JUNICHI SHIINA
Abstract: La invención comprende un nuevo proceso para la preparación de análogos de oxitocina de la fórmula (I), en la que R1 es hidrógeno o alquilo-C1-7 y R2 es hidrógeno o alquilo-C1-7; o R1 y R2 junto con el nitrógeno y el átomo de carbono al que están unidos forman un heterociclo de 5 miembros que está opcionalmente sustituido con hidroxi o halógeno; R3 es alquilo-C1-7. Análogos de oxitocina de la fórmula I actúan como agonistas del receptor de oxitocina y tienen el potencial de ser utilizados para el tratamiento de trastornos neurológicos.
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