DE60133823T2 - Somatostatin analoge verbindungen - Google Patents
Somatostatin analoge verbindungen Download PDFInfo
- Publication number
- DE60133823T2 DE60133823T2 DE60133823T DE60133823T DE60133823T2 DE 60133823 T2 DE60133823 T2 DE 60133823T2 DE 60133823 T DE60133823 T DE 60133823T DE 60133823 T DE60133823 T DE 60133823T DE 60133823 T2 DE60133823 T2 DE 60133823T2
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- Prior art keywords
- compound
- salt
- compound according
- agent
- insulin
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
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- Y02P20/50—Improvements relating to the production of bulk chemicals
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Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
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- Pharmacology & Pharmacy (AREA)
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- Communicable Diseases (AREA)
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- Oncology (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0018891 | 2000-08-01 | ||
| GBGB0018891.2A GB0018891D0 (en) | 2000-08-01 | 2000-08-01 | Organic compounds |
| PCT/EP2001/008824 WO2002010192A2 (en) | 2000-08-01 | 2001-07-30 | Somatostatin analogues |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE60133823D1 DE60133823D1 (de) | 2008-06-12 |
| DE60133823T2 true DE60133823T2 (de) | 2009-05-20 |
Family
ID=9896782
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE60133823T Expired - Lifetime DE60133823T2 (de) | 2000-08-01 | 2001-07-30 | Somatostatin analoge verbindungen |
Country Status (35)
Families Citing this family (160)
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| GB0018891D0 (en) * | 2000-08-01 | 2000-09-20 | Novartis Ag | Organic compounds |
| WO2003057214A1 (en) | 2001-12-28 | 2003-07-17 | Somatocor Pharmaceuticals, Inc. | Imidazolidin-2,4-dione derivatives as non-peptide somatostatin receptor ligands |
| SI1572615T1 (sl) | 2002-12-12 | 2010-06-30 | Novartis Ag | Postopek za sintezo peptidov ki vsebujejo hidroksi prolinsko substrukturo |
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| GB0300095D0 (en) * | 2003-01-03 | 2003-02-05 | Novartis Ag | Organic compounds |
| GB0314695D0 (en) * | 2003-06-24 | 2003-07-30 | Novartis Ag | Organic compounds |
| PE20050285A1 (es) * | 2003-06-24 | 2005-06-09 | Novartis Ag | Composicion farmaceutica que comprende analogos ciclicos de somatostatina |
| GB0318682D0 (en) * | 2003-08-08 | 2003-09-10 | Novartis Ag | Organic compounds |
| EP1522311A1 (fr) * | 2003-10-10 | 2005-04-13 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | Utilisation de la somatostine ou d'un de ses analogues pour préparer un médicament destiné à réguler la réserve folliculaire ovarienne chez la femme non ménopausée |
| MY158342A (en) | 2003-11-14 | 2016-09-30 | Novartis Ag | Pharmaceutical composition |
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| GB0602639D0 (en) * | 2006-02-09 | 2006-03-22 | Novartis Ag | Organic compounds |
| AU2007255416A1 (en) * | 2006-06-08 | 2007-12-13 | Novartis Ag | Combination of somatostatin-analogs with dopamine- or growth hormone receptor antagonist |
| US7697338B2 (en) * | 2006-11-16 | 2010-04-13 | Sandisk Corporation | Systems for controlled boosting in non-volatile memory soft programming |
| WO2008064570A1 (en) * | 2006-11-28 | 2008-06-05 | The University Of Hong Kong | The use of granulin-epithelin precursor (gep) antibodies for detection and suppression of hepatocellular carcinoma (hcc) |
| EP1941902A1 (en) * | 2007-01-02 | 2008-07-09 | Novartis AG | Use of Somatostatin analogs in cluster headache |
| EP2118123B1 (en) | 2007-01-31 | 2015-10-14 | Dana-Farber Cancer Institute, Inc. | Stabilized p53 peptides and uses thereof |
| EP3159352B1 (en) | 2007-03-28 | 2023-08-02 | President and Fellows of Harvard College | Stitched polypeptides |
| PE20090387A1 (es) | 2007-05-24 | 2009-04-28 | Novartis Ag | Formulacion de pasireotida |
| WO2009009035A1 (en) * | 2007-07-06 | 2009-01-15 | Ipsen Pharma S.A.S. | Somatostatin analog and uses thereof |
| GB0719818D0 (en) * | 2007-10-11 | 2007-11-21 | Asterion Ltd | Growth hormone fusion polypeptides |
| MX2010005936A (es) | 2007-11-28 | 2010-06-15 | Novartis Ag | Uso de analogos de somatostatina en meningioma. |
| EP2067786A1 (en) | 2007-12-07 | 2009-06-10 | ITALFARMACO S.p.A. | Novel non selective analogs of somatostatin |
| ES2431573T3 (es) | 2007-12-03 | 2013-11-27 | Italfarmaco S.P.A. | Nuevos análogos no selectivos de somatostatina |
| US20090325863A1 (en) * | 2008-06-13 | 2009-12-31 | Kleinberg David L | Somatostatin analogs and IGF-I inhibition for breast cancer prevention |
| JP5721624B2 (ja) | 2008-07-08 | 2015-05-20 | ノバルティス アーゲー | 内因性高インスリン血症性低血糖症の治療のためのパシレオチドの使用 |
| EP2213307A1 (en) | 2009-02-03 | 2010-08-04 | Novartis AG | Injectable depot formulations |
| EP2172189A1 (en) | 2008-10-01 | 2010-04-07 | Novartis AG | Pharmaceutical Compositions |
| HRP20170929T1 (hr) | 2008-09-17 | 2017-09-22 | Chiasma Inc. | Farmaceutski pripravci i odgovarajući postupci za isporuku |
| UY33236A (es) | 2010-02-25 | 2011-09-30 | Novartis Ag | Inhibidores dimericos de las iap |
| KR102104762B1 (ko) | 2010-08-13 | 2020-04-24 | 에일러론 테라퓨틱스 인코포레이티드 | 펩티도미메틱 거대고리 |
| US8629103B2 (en) | 2010-12-02 | 2014-01-14 | New York University | Treatment of non-proliferative cystic disease of the breast |
| UY33794A (es) | 2010-12-13 | 2012-07-31 | Novartis Ag | Inhibidores diméricos de las iap |
| CN103261186A (zh) | 2010-12-13 | 2013-08-21 | 诺瓦提斯公司 | 二聚化iap抑制剂 |
| US20130035054A1 (en) * | 2011-07-14 | 2013-02-07 | Faceon Mobile | Phone with multi-portal access for display during incoming and outgoing call |
| WO2013019923A2 (en) | 2011-08-02 | 2013-02-07 | New York University | Methods for detecting progenitor cells and uses thereof |
| JP6026544B2 (ja) | 2011-09-27 | 2016-11-16 | ノバルティス アーゲー | 変異体ｉｄｈの阻害剤としての３−ピリミジン−４−イル−オキサゾリジン−２−オン類 |
| TW201806968A (zh) | 2011-10-18 | 2018-03-01 | 艾利倫治療公司 | 擬肽巨環化合物 |
| AU2012348640B2 (en) | 2011-12-05 | 2016-07-21 | Camurus Ab | Robust controlled-release peptide formulations |
| WO2013084138A1 (en) | 2011-12-05 | 2013-06-13 | Novartis Ag | Cyclic urea derivatives as androgen receptor antagonists |
| BR112014016870A2 (pt) | 2012-01-09 | 2017-06-27 | Huesken Dieter | composições orgânicas para tratar doenças relacionadas com beta-catenina |
| US8815926B2 (en) | 2012-01-26 | 2014-08-26 | Novartis Ag | Substituted pyrrolo[3,4-D]imidazoles for the treatment of MDM2/4 mediated diseases |
| CA2864120A1 (en) | 2012-02-15 | 2013-08-22 | Aileron Therapeutics, Inc. | Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles |
| NZ627528A (en) | 2012-02-15 | 2016-05-27 | Aileron Therapeutics Inc | Peptidomimetic macrocycles |
| IN2014DN09831A (enExample) * | 2012-05-25 | 2015-08-07 | Camurus Ab | |
| TWI633887B (zh) | 2012-05-31 | 2018-09-01 | 大塚製藥股份有限公司 | 用於預防及／或治療多囊性腎臟病之藥物 |
| BR112015009470A2 (pt) | 2012-11-01 | 2019-12-17 | Aileron Therapeutics Inc | aminoácidos dissubstituídos e seus métodos de preparação e uso |
| US9480759B2 (en) | 2012-11-21 | 2016-11-01 | Serene, Llc | Tin-117m somatostatin receptor binding compounds and methods |
| DK2958907T3 (en) | 2013-02-19 | 2018-06-06 | Novartis Ag | Thus, benzothiophene derivatives and compositions as selective estrogen receptor degraders |
| KR20150127197A (ko) | 2013-03-14 | 2015-11-16 | 노파르티스 아게 | 돌연변이 idh의 억제제로서의 3-피리미딘-4-일-옥사졸리딘-2-온 |
| HK1213251A1 (zh) | 2013-03-14 | 2016-06-30 | Novartis Ag | 作为突变idh抑制剂的3-嘧啶-4-基-恶唑烷-2-酮化合物 |
| WO2014147586A1 (en) | 2013-03-22 | 2014-09-25 | Novartis Ag | 1-(2-(ethylamino)pyrimidin-4-yl)pyrrolidin-2-ones as inhibitors of mutant idh |
| CN103467575B (zh) * | 2013-08-22 | 2016-03-02 | 深圳翰宇药业股份有限公司 | 一种帕西瑞肽的制备方法 |
| CN103641894B (zh) * | 2013-12-06 | 2015-10-28 | 深圳翰宇药业股份有限公司 | 一种治疗库欣病的多肽药物的制备方法 |
| WO2015092634A1 (en) | 2013-12-16 | 2015-06-25 | Novartis Ag | 1,2,3,4-tetrahydroisoquinoline compounds and compositions as selective estrogen receptor antagonists and degraders |
| KR20160098258A (ko) | 2013-12-19 | 2016-08-18 | 노파르티스 아게 | 약물 전달 시스템 |
| CN105899491B (zh) | 2014-01-17 | 2019-04-02 | 诺华股份有限公司 | 用于抑制shp2活性的1-哒嗪-/三嗪-3-基-哌(-嗪)/啶/吡咯烷衍生物及其组合物 |
| CN105899493B (zh) | 2014-01-17 | 2019-03-29 | 诺华股份有限公司 | 用于抑制shp2活性的1-(三嗪-3-基/哒嗪-3-基)-哌(-嗪)啶衍生物及其组合物 |
| JO3517B1 (ar) | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| JOP20200094A1 (ar) | 2014-01-24 | 2017-06-16 | Dana Farber Cancer Inst Inc | جزيئات جسم مضاد لـ pd-1 واستخداماتها |
| JOP20200096A1 (ar) | 2014-01-31 | 2017-06-16 | Children’S Medical Center Corp | جزيئات جسم مضاد لـ tim-3 واستخداماتها |
| ME03558B (me) | 2014-03-14 | 2020-07-20 | Novartis Ag | Molekuli anti-lag-3 antiтela i njihove upotrebe |
| AU2015265607A1 (en) | 2014-05-28 | 2016-11-17 | Idenix Pharmaceuticals Llc | Nucleoside derivatives for the treatment of cancer |
| KR20170058424A (ko) | 2014-09-24 | 2017-05-26 | 에일러론 테라퓨틱스 인코포레이티드 | 펩티드모방 거대고리 및 이의 용도 |
| MA41044A (fr) | 2014-10-08 | 2017-08-15 | Novartis Ag | Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer |
| MX389663B (es) | 2014-10-14 | 2025-03-20 | Novartis Ag | Moleculas de anticuerpo que se unen a pd-l1 y usos de las mismas. |
| EP3226689B1 (en) | 2014-12-05 | 2020-01-15 | Merck Sharp & Dohme Corp. | Novel tricyclic compounds as inhibitors of mutant idh enzymes |
| EP3226688B1 (en) | 2014-12-05 | 2020-07-01 | Merck Sharp & Dohme Corp. | Tricyclic compounds as inhibitors of mutant idh enzymes |
| WO2016089833A1 (en) | 2014-12-05 | 2016-06-09 | Merck Sharp & Dohme Corp. | Novel tricyclic compounds as inhibitors of mutant idh enzymes |
| AU2015360485B2 (en) | 2014-12-10 | 2020-06-25 | Amryt Endo, Inc. | Oral octreotide administered in combination with other therapeutic agents |
| US20210317161A1 (en) | 2014-12-19 | 2021-10-14 | Auro Peptides Ltd | A process for the preparation of pasireotide |
| WO2016100882A1 (en) | 2014-12-19 | 2016-06-23 | Novartis Ag | Combination therapies |
| AU2016215350B2 (en) | 2015-02-03 | 2021-11-25 | Amryt Endo, Inc. | Method of treating diseases |
| US10449211B2 (en) | 2015-03-10 | 2019-10-22 | Aduro Biotech, Inc. | Compositions and methods for activating “stimulator of interferon gene”—dependent signalling |
| SG11201707750YA (en) | 2015-03-20 | 2017-10-30 | Aileron Therapeutics Inc | Peptidomimetic macrocycles and uses thereof |
| US10730911B2 (en) | 2015-04-08 | 2020-08-04 | Universitat Zurich | Backbone-cyclized peptidomimetics with GLP-1R modulating activity |
| CN108368147A (zh) | 2015-05-27 | 2018-08-03 | 南方研究院 | 用于治疗癌症的核苷酸 |
| EP3310779B1 (en) | 2015-06-19 | 2019-05-08 | Novartis AG | Compounds and compositions for inhibiting the activity of shp2 |
| CN112625028B (zh) | 2015-06-19 | 2024-10-29 | 诺华股份有限公司 | 用于抑制shp2活性的化合物和组合物 |
| EP3310771B1 (en) | 2015-06-19 | 2020-07-22 | Novartis AG | Compounds and compositions for inhibiting the activity of shp2 |
| US10556924B2 (en) | 2015-06-22 | 2020-02-11 | Biophore India Pharmaceuticals Pvt. Ltd. | Process for the preparation of pasireotide |
| GB201511790D0 (en) | 2015-07-06 | 2015-08-19 | Iomet Pharma Ltd | Pharmaceutical compound |
| DK3317301T3 (da) | 2015-07-29 | 2021-06-28 | Immutep Sas | Kombinationsterapier omfattende antistofmolekyler mod lag-3 |
| US20180222982A1 (en) | 2015-07-29 | 2018-08-09 | Novartis Ag | Combination therapies comprising antibody molecules to pd-1 |
| EP3878465A1 (en) | 2015-07-29 | 2021-09-15 | Novartis AG | Combination therapies comprising antibody molecules to tim-3 |
| US11453697B1 (en) | 2015-08-13 | 2022-09-27 | Merck Sharp & Dohme Llc | Cyclic di-nucleotide compounds as sting agonists |
| EA034786B1 (ru) | 2015-08-13 | 2020-03-20 | Мерк Шарп И Доум Корп. | Циклические динуклеотидные соединения в качестве агонистов sting |
| SI3370768T1 (sl) | 2015-11-03 | 2022-04-29 | Janssen Biotech, Inc. | Protitelesa, ki se specifično vežejo na PD-1, in njihove uporabe |
| US10538497B2 (en) | 2015-12-15 | 2020-01-21 | Merck Sharp & Dohme Corp. | Compounds as indoleamine 2,3-dioxygenase inhibitors |
| EP3389712B1 (en) | 2015-12-17 | 2024-04-10 | Novartis AG | Antibody molecules to pd-1 and uses thereof |
| US10577362B2 (en) | 2016-05-04 | 2020-03-03 | Genoscience Pharma | Substituted 2, 4-diamino-quinoline derivatives for use in the treatment of proliferative diseases |
| WO2017216706A1 (en) | 2016-06-14 | 2017-12-21 | Novartis Ag | Compounds and compositions for inhibiting the activity of shp2 |
| US11098077B2 (en) | 2016-07-05 | 2021-08-24 | Chinook Therapeutics, Inc. | Locked nucleic acid cyclic dinucleotide compounds and uses thereof |
| TN2020000158A1 (en) | 2016-10-04 | 2022-04-04 | Merck Sharp & Dohme | BENZO[b]THIOPHENE COMPOUNDS AS STING AGONISTS |
| WO2018091542A1 (en) | 2016-11-21 | 2018-05-24 | Idenix Pharmaceuticals Llc | Cyclic phosphate substituted nucleoside derivatives for the treatment of liver diseases |
| AU2018212788A1 (en) | 2017-01-27 | 2019-07-25 | Janssen Biotech, Inc. | Cyclic dinucleotides as STING agonists |
| WO2018138684A1 (en) | 2017-01-27 | 2018-08-02 | Janssen Biotech, Inc. | Cyclic dinucleotides as sting agonists |
| UY37695A (es) | 2017-04-28 | 2018-11-30 | Novartis Ag | Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo |
| EP3621624B1 (en) | 2017-05-12 | 2023-08-30 | Merck Sharp & Dohme LLC | Cyclic di-nucleotide compounds as sting agonists |
| WO2018237173A1 (en) | 2017-06-22 | 2018-12-27 | Novartis Ag | Antibody molecules to cd73 and uses thereof |
| RU2020109328A (ru) | 2017-08-04 | 2021-09-06 | Мерк Шарп И Доум Корп. | Комбинации антагонистов pd-1 и бензо[b]тиофеновых агонистов sting для лечения рака |
| US11285131B2 (en) | 2017-08-04 | 2022-03-29 | Merck Sharp & Dohme Corp. | Benzo[b]thiophene STING agonists for cancer treatment |
| TWI851542B (zh) | 2017-09-11 | 2024-08-11 | 美商克魯松藥物公司 | Ｓｈｐ２之八氫環戊烷并[c]吡咯別構抑制劑 |
| WO2019067332A1 (en) | 2017-09-27 | 2019-04-04 | Merck Sharp & Dohme Corp. | COMPOSITIONS AND METHODS FOR TREATING CANCER THROUGH A COMBINATION OF PROGRAMMED DEATH ANTIBODY ANTIBODIES (PD-1) AND A CXCR2 ANTAGONIST |
| WO2019078968A2 (en) * | 2017-10-18 | 2019-04-25 | Angex Pharmaceutical, Inc. | CYCLIC COMPOUNDS AS IMMUNOMODULATORS |
| WO2019089412A1 (en) | 2017-11-01 | 2019-05-09 | Merck Sharp & Dohme Corp. | Novel substituted tetrahydroquinolin compounds as indoleamine 2,3-dioxygenase (ido) inhibitors |
| CA3082108A1 (en) | 2017-11-14 | 2019-05-23 | Merck Sharp & Dohme Corp. | Novel substituted biaryl compounds as indoleamine 2,3-dioxygenase (ido) inhibitors |
| WO2019099294A1 (en) | 2017-11-14 | 2019-05-23 | Merck Sharp & Dohme Corp. | Novel substituted biaryl compounds as indoleamine 2,3-dioxygenase (ido) inhibitors |
| AU2018386222B2 (en) | 2017-12-15 | 2023-04-20 | Janssen Biotech, Inc. | Cyclic dinucleotides as sting agonists |
| WO2019125974A1 (en) | 2017-12-20 | 2019-06-27 | Merck Sharp & Dohme Corp. | Cyclic di-nucleotide compounds as sting agonists |
| US12398209B2 (en) | 2018-01-22 | 2025-08-26 | Janssen Biotech, Inc. | Methods of treating cancers with antagonistic anti-PD-1 antibodies |
| US12215116B2 (en) | 2018-03-13 | 2025-02-04 | Merck Sharp & Dohme Llc | Arginase inhibitors and methods of use |
| WO2019195124A1 (en) | 2018-04-03 | 2019-10-10 | Merck Sharp & Dohme Corp. | Benzothiophenes and related compounds as sting agonists |
| WO2019195063A1 (en) | 2018-04-03 | 2019-10-10 | Merck Sharp & Dohme Corp. | Aza-benzothiophene compounds as sting agonists |
| WO2019204179A1 (en) | 2018-04-20 | 2019-10-24 | Merck Sharp & Dohme Corp. | Novel substituted rig-i agonists: compositions and methods thereof |
| TWI869346B (zh) | 2018-05-30 | 2025-01-11 | 瑞士商諾華公司 | Ｅｎｔｐｄ２抗體、組合療法、及使用該等抗體和組合療法之方法 |
| WO2019231870A1 (en) | 2018-05-31 | 2019-12-05 | Merck Sharp & Dohme Corp. | Novel substituted [1.1.1] bicyclo compounds as indoleamine 2,3-dioxygenase inhibitors |
| WO2019245890A1 (en) | 2018-06-20 | 2019-12-26 | Merck Sharp & Dohme Corp. | Arginase inhibitors and methods of use |
| US10596276B2 (en) | 2018-07-25 | 2020-03-24 | Advanced Accelerator Applications (Italy) S.R.L. | Stable, concentrated radionuclide complex solutions |
| US10596278B2 (en) | 2018-07-25 | 2020-03-24 | Advanced Accelerator Applications (Italy) S.R.L. | Stable, concentrated radionuclide complex solutions |
| TW202517303A (zh) | 2018-07-25 | 2025-05-01 | 法商高級催化劑應用品有限公司 | 穩定的、濃縮的放射性核種錯合物溶液 |
| AU2019344897B2 (en) | 2018-09-18 | 2024-01-18 | Nikang Therapeutics, Inc. | Tri-substituted heteroaryl derivatives AS SRC homology-2 phosphatase inhibitors |
| CN113382986A (zh) | 2018-09-25 | 2021-09-10 | 黑钻治疗公司 | 酪氨酸激酶抑制剂组合物、其制备方法和使用方法 |
| JP2022502496A (ja) | 2018-09-25 | 2022-01-11 | ブラック ダイアモンド セラピューティクス，インコーポレイティド | チロシンキナーゼ阻害剤組成物、作製方法、および使用方法 |
| CA3113379A1 (en) | 2018-09-29 | 2020-04-02 | Novartis Ag | Process of manufacture of a compound for inhibiting the activity of shp2 |
| EP3873464B1 (en) | 2018-11-01 | 2025-07-30 | Merck Sharp & Dohme LLC | Novel substituted pyrazole compounds as indoleamine 2,3-dioxygenase inhibitors |
| EP3877366A4 (en) | 2018-11-06 | 2022-08-24 | Merck Sharp & Dohme Corp. | NOVEL SUBSTITUTED TRICYCLIC COMPOUNDS AS INDOLAMINE-2,3-DIOXYGENASE INHIBITORS |
| EP3886845B1 (en) | 2018-11-28 | 2024-09-04 | Merck Sharp & Dohme LLC | Novel substituted piperazine amide compounds as indoleamine 2, 3-dioxygenase (ido) inhibitors |
| US12240867B2 (en) | 2018-12-18 | 2025-03-04 | Merck Sharp & Dohme Llc | Arginase inhibitors and methods of use |
| EP3946324B1 (en) | 2019-04-04 | 2025-07-30 | Merck Sharp & Dohme LLC | Inhibitors of histone deacetylase-3 useful for the treatment of cancer, inflammation, neurodegeneration diseases and diabetes |
| EP3990635A1 (en) | 2019-06-27 | 2022-05-04 | Rigontec GmbH | Design method for optimized rig-i ligands |
| KR20220056176A (ko) | 2019-08-02 | 2022-05-04 | 메르사나 테라퓨틱스, 인코포레이티드 | 암 치료를 위한 sting(인터페론 유전자의 자극인자) 작용제로서의 비스-[n-((5-카바모일)-1h-벤조[d]이미다졸-2-일)-피라졸-5-카복사미드] 유도체 및 관련 화합물 |
| CN114787150A (zh) | 2019-08-15 | 2022-07-22 | 黑钻治疗公司 | 炔基喹唑啉化合物 |
| US20220348651A1 (en) | 2019-09-18 | 2022-11-03 | Novartis Ag | Entpd2 antibodies, combination therapies, and methods of using the antibodies and combination therapies |
| AU2020373913B2 (en) | 2019-10-28 | 2024-04-18 | Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences | Five-membered heterocyclic oxocarboxylic acid compound and medical use thereof |
| EP4069683A1 (en) | 2019-12-06 | 2022-10-12 | Mersana Therapeutics, Inc. | Dimeric compounds as sting agonists |
| EP4076443B1 (en) | 2019-12-17 | 2025-09-10 | Merck Sharp & Dohme LLC | Substituted 1,3,8-triazaspiro[4,5]decane-2,4-dione compound as indoleamine 2,3-dioxygenase (ido) and/or tryptophan 2,3-dioxygenase (tdo) inhibitors |
| EP4087583A4 (en) | 2020-01-07 | 2024-01-24 | Merck Sharp & Dohme LLC | Arginase inhibitors and methods of use |
| WO2021195206A1 (en) | 2020-03-24 | 2021-09-30 | Black Diamond Therapeutics, Inc. | Polymorphic forms and related uses |
| MY210304A (en) | 2020-04-02 | 2025-09-10 | Mersana Therapeutics Inc | Antibody drug conjugates comprising sting agonists |
| CN115836054B (zh) | 2020-05-06 | 2024-12-10 | 默沙东有限责任公司 | Il4i1抑制剂和使用方法 |
| WO2022140472A1 (en) | 2020-12-22 | 2022-06-30 | Nikang Therapeutics, Inc. | Compounds for degrading cyclin-dependent kinase 2 via ubiquitin proteosome pathway |
| US11141457B1 (en) | 2020-12-28 | 2021-10-12 | Amryt Endo, Inc. | Oral octreotide therapy and contraceptive methods |
| WO2022152821A1 (en) | 2021-01-13 | 2022-07-21 | Monte Rosa Therapeutics Ag | Isoindolinone compounds |
| WO2022170052A1 (en) | 2021-02-05 | 2022-08-11 | Black Diamond Therapeutics, Inc. | Quinazoline derivatives, pyridopyrimidine derivatives, pyrimidopyrimidine derivatives, and uses thereof |
| EP4323350A1 (en) | 2021-04-14 | 2024-02-21 | Monte Rosa Therapeutics AG | Isoindolinone compounds |
| EP4323349A1 (en) | 2021-04-14 | 2024-02-21 | Monte Rosa Therapeutics AG | Isoindolinone amide compounds useful to treat diseases associated with gspt1 |
| WO2022227015A1 (en) | 2021-04-30 | 2022-11-03 | Merck Sharp & Dohme Corp. | Il4i1 inhibitors and methods of use |
| WO2023284730A1 (en) | 2021-07-14 | 2023-01-19 | Nikang Therapeutics, Inc. | Alkylidene derivatives as kras inhibitors |
| US12331026B2 (en) | 2022-03-28 | 2025-06-17 | Nikang Therapeutics, Inc. | Sulfonamido derivatives as cyclin-dependent kinase 2 inhibitors |
| WO2023240024A1 (en) | 2022-06-08 | 2023-12-14 | Nikang Therapeutics, Inc. | Sulfamide derivatives as cyclin-dependent kinase 2 inhibitors |
| WO2024047112A1 (en) * | 2022-08-30 | 2024-03-07 | Somtheranostics Sarl | Halogenated somatostatin analogs with multiple somatostatin receptor subtype selectivity |
| AU2023375457A1 (en) | 2022-11-11 | 2025-05-01 | Nikang Therapeutics, Inc. | Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 via ubiquitin proteasome pathway |
| TW202502311A (zh) | 2023-03-29 | 2025-01-16 | 美商默沙東有限責任公司 | Il4i1抑制劑及其使用方法 |
| WO2025072462A1 (en) | 2023-09-27 | 2025-04-03 | Nikang Therapeutics, Inc. | Sulfonamide derivatives as cyclin-dependent kinase 2 inhibitors |
| TW202527955A (zh) | 2023-11-27 | 2025-07-16 | 美商尼坎醫療公司 | 用於經由泛素蛋白酶體途徑降解週期蛋白依賴性激酶２和週期蛋白依賴性激酶４的含有２，５－取代的嘧啶衍生物的雙功能化合物 |
| WO2025117981A1 (en) | 2023-12-02 | 2025-06-05 | Nikang Therapeutics, Inc. | Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 via ubiquitin proteasome pathway |
| WO2025212828A1 (en) | 2024-04-03 | 2025-10-09 | Nikang Therapeutics, Inc. | Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 and cyclin-dependent kinase 4 via ubiquitin proteasome pathway |
| WO2025240536A1 (en) | 2024-05-15 | 2025-11-20 | Nikang Therapeutics, Inc. | Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 and/or cyclin-dependent kinase 4 via ubiquitin proteasome pathway |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3863008A (en) | 1973-06-11 | 1975-01-28 | American Home Prod | Somatostatin as stimulant of luteinizing hormone secretion |
| NZ195303A (en) | 1979-10-31 | 1984-10-19 | Merck & Co Inc | Cyclic hexapeptide somatostatin analogues,and pharmaceutical compositions |
| US4292972A (en) | 1980-07-09 | 1981-10-06 | E. R. Squibb & Sons, Inc. | Lyophilized hydrocolloio foam |
| US4612386A (en) * | 1980-09-16 | 1986-09-16 | The Dow Chemical Company | Process for making esters |
| US4505897A (en) | 1983-04-18 | 1985-03-19 | The Administrators Of The Tulane Educational Fund | Cyclic pentapeptides displaying somatostatin antagonism and method of treatment of mammals therewith |
| US4612366A (en) | 1985-06-17 | 1986-09-16 | Merck & Co., Inc. | Cyclic hexapeptide somatostatin analogs |
| CA2012115C (en) | 1989-03-15 | 2001-07-03 | Biomeasure, Inc. | Iodinated somatostatins |
| HU217636B (hu) | 1989-04-26 | 2000-03-28 | Administrators Of The Tulane Educational Fund | Szomatosztatin analógok, ezeket tartalmazó gyógyszerkészítmények és eljárás előállításukra |
| US5620675A (en) | 1992-06-23 | 1997-04-15 | Diatech, Inc. | Radioactive peptides |
| US5716596A (en) | 1992-06-23 | 1998-02-10 | Diatide, Inc. | Radioactively labeled somatostatin-derived peptides for imaging and therapeutic uses |
| CA2167281C (en) | 1993-07-15 | 2001-09-04 | Richard T. Dean | Radiolabeled somatostatin-derived peptides for imaging and therapeutic uses |
| SG75092A1 (en) | 1993-08-09 | 2000-09-19 | Biomeasure Inc | Therapeutic peptide derivatives |
| US5770687A (en) | 1995-06-07 | 1998-06-23 | Peptor Limited | Comformationally constrained backbone cyclized somatostatin analogs |
| MY147327A (en) * | 1995-06-29 | 2012-11-30 | Novartis Ag | Somatostatin peptides |
| GB9513224D0 (en) * | 1995-06-29 | 1995-09-06 | Sandoz Ltd | Organic compounds |
| IT1277391B1 (it) | 1995-07-28 | 1997-11-10 | Romano Deghenghi | Peptidi ciclici analoghi della somatostatina ad attivita' inibitrice dell'ormone della crescita |
| WO1997043278A1 (en) | 1996-05-14 | 1997-11-20 | Novo Nordisk A/S | Somatostatin agonists and antagonists |
| US6355613B1 (en) | 1996-07-31 | 2002-03-12 | Peptor Limited | Conformationally constrained backbone cyclized somatostatin analogs |
| CA2246791A1 (en) | 1998-09-01 | 2000-03-01 | Alison Buchan | Treatment of endothelium with somatostatin analogues |
| GB0018891D0 (en) * | 2000-08-01 | 2000-09-20 | Novartis Ag | Organic compounds |
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2000
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