ES2596434T3 - Moduladores de receptores opioides - Google Patents
Moduladores de receptores opioides Download PDFInfo
- Publication number
- ES2596434T3 ES2596434T3 ES13173454.3T ES13173454T ES2596434T3 ES 2596434 T3 ES2596434 T3 ES 2596434T3 ES 13173454 T ES13173454 T ES 13173454T ES 2596434 T3 ES2596434 T3 ES 2596434T3
- Authority
- ES
- Spain
- Prior art keywords
- opioid receptor
- receptor modulators
- compound
- ean
- control
- 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.)
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/417—Imidazole-alkylamines, e.g. histamine, phentolamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4174—Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/10—Laxatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/12—Antidiarrhoeals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/28—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
- C07C237/30—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to hydrogen atoms or to acyclic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D275/00—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
- C07D275/04—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems
- C07D275/06—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems with hetero atoms directly attached to the ring sulfur atom
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Peptides Or Proteins (AREA)
- Plural Heterocyclic Compounds (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Oscillators With Electromechanical Resonators (AREA)
- Eye Examination Apparatus (AREA)
- Steroid Compounds (AREA)
- Amplifiers (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Amplitude Modulation (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
Una formulación de dosificación farmacéutica adecuado para la administración oral que comprende el compuesto que tiene la estructura:**Fórmula** o una sal farmacéuticamente aceptable del mismo y un portador farmacéuticamente aceptable.
Description
Tabla IV
R3-1 R3-2 R41
5 284 3-Metoxicarbonil-4-metoxi-fenilmetilo metilo fenilo H H 4-aminocarbonilo H 3-Carboxi-4-metoxi-fenilmetilo metilo fenilo H H 4-aminocarbonilo H
Se divulgan los compuestos mostrados en la Tabla V:
Tabla V
15
25
35
45
55
- Comp.
- 4
- 6
- 8
25
15
25
35
45
55
- 12
- 18
- 20
- 75
- 227
26
(continuada)
- Producción Fecal (Nº de sedimentos)
- Nº de
- Dosis (mg/kg) control EAN compuesto % de EAN % de % de
- compuesto
- de control compuesto de compuesto de
- control
- EAN
- 143
- 10 3,7 13,6 9,1 367,6 245,9 66,9
- 143
- 30 7,5 9,2 5,2 122,7 69,3 56,5
- 144
- 30 3,7 13,6 11,5 367,6 310,8 84,6
- 178
- 30 3,2 8,8 5,5 275,0 171,9 62,5
- 192
- 10 5,4 12,5 10,5 231,5 194,4 84,0
- 194
- 10 5,4 12,5 11,8 231,5 218,5 94,4
- 194
- 30 8,1 11,0 4,2 135,8 51,9 38,2
- 194
- 30 3,1 4,8 4,9 154,3 157,5 102,1
- 194
- 30 3,7 14,0 6,2 378,4 167,6 44,3
- 196
- 10 3,7 14,0 9,2 378,4 248,6 65,7
- 196
- 30 1,1 9,5 4,3 863,6 390,9 45,3
- 199
- 10 2,7 10,5 9,1 388,9 337,0 86,7
- 199
- 10 3,8 13,1 10,8 344,7 284,2 82,4
- 205
- 30 3,3 9,5 2,3 287,9 70,7 24,6
- 206
- 10 3,8 13,1 8,6 344,7 226,3 65,6
- 207
- 10 5,6 9,4 8,3 167,9 148,2 88,3
- 207
- 10 7,7 13,0 5,0 168,8 64,9 38,5
- 207
- 10 5,7 12,8 6,6 225,9 116,5 51,6
- 207
- 10 2,9 12,8 5,3 441,4 182,8 41,4
- 207
- 30 3,5 3,2 91,4
- 207
- 30 3,5 13,0 6,4 371,4 184,1 49,6
- 216
- 10 3,6 10,3 4,9 286,1 136,1 47,6
- 218
- 30 2,7 10,5 3,7 388,9 137,6 35,4
- 223
- 30 3,1 4,8 5,0 154,3 160,7 104,2
- 224
- 10 3,6 6,9 3,5 191,7 97,2 50,7
- 225
- 30 3,1 4,8 7,3 154,3 234,7 152,1
Tabla XI: Ensayo de Producción de Sedimentos Fecales de Ratón dependiente de Dosis
- Nº de
- sedimentos
- Nº de comp.
- control EAN EAN (% de control) Compuesto (mg)
- 0,3 0,5 1,0
- 3,0 5,0 6,0 10,0 30,0
- 75
- 235,7
- 93
- 2,7 8,3 307,4 6,2 5,5 3,2
- 97
- 6,1 11,6 190,2 14 7,5 3,5
- 97
- 4,8 10,1 210,4 9,1 10,4 2,3
- 102
- 5,3 10,7 201,9 6,9 4,5 2,22
- 114
- 3,4 10 294,1 9,6 7,7 5,4
- 200
- 3,556 8,8 247,5 8,1 8,2 5,8
- 207
- 5,2 11,4 219,2 11,4 12 4,9
- 207
- 4,8 8,6 179,2 9,4 8,6 6,7
- 207
- 3,4 10,8 317,6 7,5 5,5 3,5
- 207
- 3,6 6,5 180,6 7,3 4,8 3,4
- 224
- 2,2 9,6 436,4 7,6 7,2 4,2
74
Claims (1)
-
imagen1 imagen2 imagen3
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US55334204P | 2004-03-15 | 2004-03-15 | |
US553342P | 2004-03-15 |
Publications (1)
Publication Number | Publication Date |
---|---|
ES2596434T3 true ES2596434T3 (es) | 2017-01-09 |
Family
ID=34962827
Family Applications (5)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ES16178050T Active ES2705077T3 (es) | 2004-03-15 | 2005-03-14 | Moduladores de receptores opioides |
ES13173454.3T Active ES2596434T3 (es) | 2004-03-15 | 2005-03-14 | Moduladores de receptores opioides |
ES12194058.9T Active ES2533176T3 (es) | 2004-03-15 | 2005-03-14 | Proceso para preparar intermedios de compuestos útiles como moduladores de receptores opioides |
ES10182349T Active ES2428008T3 (es) | 2004-03-15 | 2005-03-14 | Moduladores de receptores opioides |
ES05728171T Active ES2367576T3 (es) | 2004-03-15 | 2005-03-14 | Nuevos compuestos como moduladores de receptores opioides. |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ES16178050T Active ES2705077T3 (es) | 2004-03-15 | 2005-03-14 | Moduladores de receptores opioides |
Family Applications After (3)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ES12194058.9T Active ES2533176T3 (es) | 2004-03-15 | 2005-03-14 | Proceso para preparar intermedios de compuestos útiles como moduladores de receptores opioides |
ES10182349T Active ES2428008T3 (es) | 2004-03-15 | 2005-03-14 | Moduladores de receptores opioides |
ES05728171T Active ES2367576T3 (es) | 2004-03-15 | 2005-03-14 | Nuevos compuestos como moduladores de receptores opioides. |
Country Status (36)
Country | Link |
---|---|
US (8) | US7741356B2 (es) |
EP (5) | EP2573068B9 (es) |
JP (1) | JP4778954B2 (es) |
KR (1) | KR101166342B1 (es) |
CN (2) | CN1950342B (es) |
AR (2) | AR048269A1 (es) |
AT (1) | ATE516274T1 (es) |
AU (1) | AU2005224091B2 (es) |
BR (1) | BRPI0508820B8 (es) |
CA (1) | CA2560047C (es) |
CR (1) | CR8655A (es) |
CY (3) | CY1111927T1 (es) |
DK (5) | DK2653465T3 (es) |
EC (1) | ECSP066856A (es) |
ES (5) | ES2705077T3 (es) |
HK (4) | HK1099016A1 (es) |
HR (4) | HRP20110694T1 (es) |
HU (2) | HUE029852T2 (es) |
IL (3) | IL178040A (es) |
LT (2) | LT2653465T (es) |
LU (1) | LUC00007I2 (es) |
ME (3) | ME01601B (es) |
MX (1) | MXPA06010642A (es) |
MY (1) | MY146972A (es) |
NL (1) | NL300865I2 (es) |
NO (3) | NO338203B1 (es) |
NZ (1) | NZ549842A (es) |
PH (1) | PH12012501640A1 (es) |
PL (4) | PL2573068T3 (es) |
PT (4) | PT2653465T (es) |
RS (4) | RS52933B (es) |
SI (4) | SI2653465T1 (es) |
TW (1) | TWI361069B (es) |
UA (1) | UA86053C2 (es) |
WO (1) | WO2005090315A1 (es) |
ZA (1) | ZA200608587B (es) |
Families Citing this family (63)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20080050367A1 (en) | 1998-04-07 | 2008-02-28 | Guriq Basi | Humanized antibodies that recognize beta amyloid peptide |
TWI239847B (en) | 1997-12-02 | 2005-09-21 | Elan Pharm Inc | N-terminal fragment of Abeta peptide and an adjuvant for preventing and treating amyloidogenic disease |
UA86053C2 (ru) | 2004-03-15 | 2009-03-25 | Янссен Фармацевтика Н.В. | Соединения как модуляторы опиоидных рецепторов |
US7244866B2 (en) | 2004-05-14 | 2007-07-17 | Janssen Pharmaceutical N.V. | Carboxamido opioid compounds |
PE20061329A1 (es) | 2004-12-15 | 2006-12-08 | Neuralab Ltd | Anticuerpos ab humanizados para mejorar la cognicion |
CA2601674A1 (en) * | 2005-03-14 | 2006-09-21 | Janssen Pharmaceutica N.V. | Process for the preparation of opioid modulators |
EA014245B1 (ru) * | 2005-12-14 | 2010-10-29 | Бристол-Маерс Сквибб Компани | Аналоги арилпропионамида, арилакриламида, арилпропинамида или арилметилмочевины в качестве ингибиторов фактора xia |
CA2634743C (en) * | 2005-12-23 | 2014-07-29 | Zealand Pharma A/S | Modified lysine-mimetic compounds |
KR20110122881A (ko) | 2006-04-07 | 2011-11-11 | 워너 칠콧 컴퍼니 엘엘씨 | 인간 단백질 타이로신 포스파타아제 베타(hptp베타)에 결합하는 항체 및 그의 용도 |
US8784810B2 (en) | 2006-04-18 | 2014-07-22 | Janssen Alzheimer Immunotherapy | Treatment of amyloidogenic diseases |
US7622593B2 (en) | 2006-06-27 | 2009-11-24 | The Procter & Gamble Company | Human protein tyrosine phosphatase inhibitors and methods of use |
EP2468724B1 (en) * | 2006-12-21 | 2015-11-18 | Zealand Pharma A/S | Synthesis of pyrrolidine compounds |
SG185941A1 (en) * | 2007-07-09 | 2012-12-28 | Janssen Pharmaceutica Nv | Novel crystals and process of making 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy- benzoic acid |
PL2182983T3 (pl) | 2007-07-27 | 2014-10-31 | Janssen Alzheimer Immunotherap | Leczenie chorób amyloidowych z wykorzystaniem humanizowanych przeciwciał specyficznych względem Abeta |
JO3076B1 (ar) | 2007-10-17 | 2017-03-15 | Janssen Alzheimer Immunotherap | نظم العلاج المناعي المعتمد على حالة apoe |
TWI468375B (zh) * | 2008-10-27 | 2015-01-11 | Janssen Pharmaceutica Nv | 製備經保護之l-丙胺酸衍生物之方法 |
US9067981B1 (en) | 2008-10-30 | 2015-06-30 | Janssen Sciences Ireland Uc | Hybrid amyloid-beta antibodies |
JP5198220B2 (ja) * | 2008-11-13 | 2013-05-15 | 東ソ−・エフテック株式会社 | アミノ酸誘導体の製造方法 |
JP5536113B2 (ja) | 2009-07-06 | 2014-07-02 | アケビア セラピューティクス インコーポレイテッド | がん細胞の転移を予防するための化合物、組成物および方法 |
EP2524912A1 (en) | 2011-05-16 | 2012-11-21 | Bionomics Limited | Amine derivatives |
WO2012155199A1 (en) | 2011-05-16 | 2012-11-22 | Bionomics Limited | Amine derivatives as potassium channel blockers |
AU2012323856B2 (en) | 2011-10-13 | 2017-05-25 | EyePoint Pharmaceuticals, Inc. | Methods for treating Vascular Leak Syndrome and cancer |
US9447079B2 (en) * | 2013-03-14 | 2016-09-20 | Epizyme, Inc. | PRMT1 inhibitors and uses thereof |
BR112015022785A2 (pt) | 2013-03-14 | 2017-07-18 | Epizyme Inc | composto; composição farmacêutica; kit ou artigo farmacêutico embalado; método de inibição de uma arginina metil transferase (rmt); método de modulação da expressão genética; método de modulação da transcrição; e método de tratamento de um distúrbio mediado por rmt |
US9023883B2 (en) | 2013-03-14 | 2015-05-05 | Epizyme, Inc. | PRMT1 inhibitors and uses thereof |
US9120757B2 (en) | 2013-03-14 | 2015-09-01 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
US9675587B2 (en) | 2013-03-14 | 2017-06-13 | Allergan Holdings Unlimited Company | Opioid receptor modulator dosage formulations |
US20150050277A1 (en) | 2013-03-15 | 2015-02-19 | Aerpio Therapeutics Inc. | Compositions and methods for treating ocular diseases |
JP6483148B2 (ja) | 2014-03-14 | 2019-03-13 | エアーピオ セラピューティクス インコーポレイテッド | HPTP−β阻害剤 |
IS2977B (is) | 2015-02-23 | 2017-07-15 | Actavis Group Ptc Ehf. | Aðferð til framleiðslu á milliefnum sem eru nytsamleg við nýsmíði á elúxadólíni |
EP3319444B1 (en) | 2015-07-09 | 2022-03-09 | The Regents of the University of California | Mu opioid receptor modulators |
WO2017015606A1 (en) * | 2015-07-23 | 2017-01-26 | Teva Pharmaceuticals International Gmbh | Solid state forms of eluxadoline |
WO2017043626A1 (ja) * | 2015-09-11 | 2017-03-16 | 株式会社カネカ | 光学活性4-カルバモイル-2,6-ジメチルフェニルアラニン誘導体の製造法 |
CN108290057A (zh) | 2015-09-23 | 2018-07-17 | 爱尔皮奥治疗有限公司 | 用tie-2的激活剂治疗眼内压的方法 |
CN105250232B (zh) * | 2015-09-29 | 2018-08-14 | 江苏汇智知识产权服务有限公司 | 一种伊卢多啉肠溶片及其制备方法 |
WO2017114446A1 (zh) * | 2015-12-31 | 2017-07-06 | 苏州晶云药物科技有限公司 | 艾沙度林的新晶型及其制备方法 |
CN107129444B (zh) * | 2016-02-29 | 2018-08-31 | 尚科生物医药(上海)有限公司 | (s)-2-叔丁氧羰基氨基-3-(4-氨甲酰基-2,6-二甲基苯基)丙酸制备方法 |
EP3272741A1 (en) | 2016-07-21 | 2018-01-24 | Euticals S.P.A. | New stable solvate crystalline forms of eluxadoline |
CN105777584B (zh) * | 2016-03-28 | 2018-01-02 | 成都伊诺达博医药科技有限公司 | 丙氨酸衍生物的制备方法 |
CN105693554B (zh) * | 2016-04-06 | 2017-08-08 | 成都伊诺达博医药科技有限公司 | 丙氨酸衍生物的制备方法 |
WO2017191650A1 (en) * | 2016-05-03 | 2017-11-09 | Msn Laboratories Private Limited | Process for the preparation of 5-[[[(2s)-2-amino-3-[4-(aminocarbonyl)-2,6-dimethylphenyl]-1-oxopropyl][(1s)-1-(4-phenyl-1h-imidazol-2-yl)ethyl]amino]methyl-2-methoxybenzoic acid and its polymorphs thereof |
US20190177282A1 (en) * | 2016-05-30 | 2019-06-13 | Sun Pharmaceutical Industries Limited | A process for the preparation of eluxadoline |
EP3474847B1 (en) * | 2016-06-23 | 2022-09-07 | Sun Pharmaceutical Industries Limited | Processes for the preparation of eluxadoline |
WO2018020450A2 (en) | 2016-07-28 | 2018-02-01 | Lupin Limited | Process for the preparation of eluxadoline |
CZ2016548A3 (cs) | 2016-09-07 | 2018-03-14 | Zentiva, K.S. | Pevné formy eluxadolinu |
WO2018047131A1 (en) * | 2016-09-09 | 2018-03-15 | Sun Pharmaceutical Industries Limited | Amorphous eluxadoline |
WO2018055528A2 (en) * | 2016-09-20 | 2018-03-29 | Sun Pharmaceutical Industries Limited | Processes for the preparation of eluxadoline |
WO2018138272A1 (en) | 2017-01-27 | 2018-08-02 | Quimica Sintetica, S. A. | Eluxadoline crystalline form and process for the preparation thereof |
WO2018138274A1 (en) | 2017-01-27 | 2018-08-02 | Quimica Sintetica, S. A. | Eluxadoline crystalline forms and processes for their preparation |
DK3618847T3 (da) | 2017-05-05 | 2021-05-25 | Boston Medical Ct Corp | GAP-junction-modulatorer af intercellulær kommunikation og deres anvendelse til behandling af diabetisk øjensygdom |
WO2019008604A1 (en) | 2017-07-07 | 2019-01-10 | Cipla Limited | NEW FORMS OF MU-OPIOID RECEPTOR AGONIST |
WO2019144805A1 (zh) * | 2018-01-25 | 2019-08-01 | 四川科伦博泰生物医药股份有限公司 | 取代的苯乙胺化合物及其制备方法和用途 |
WO2019197274A1 (en) | 2018-04-09 | 2019-10-17 | Quimica Sintetica, S. A. | Process for the preparation of opioid modulators |
CA3109557A1 (en) | 2018-08-20 | 2020-02-27 | Allergan Holdings Unlimited Company | Polymorphs of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid |
US10894824B2 (en) | 2018-09-24 | 2021-01-19 | Aerpio Pharmaceuticals, Inc. | Multispecific antibodies that target HPTP-β (VE-PTP) and VEGF |
ES2867895T3 (es) * | 2018-11-30 | 2021-10-21 | Phytobiotics Futterzusatzstoffe Gmbh | Sistema para el análisis de imágenes de excrementos de animales |
CN111377832A (zh) * | 2018-12-27 | 2020-07-07 | 江苏联昇化学有限公司 | 一种伊卢多啉中间体制备的新方法 |
JP2022530657A (ja) | 2019-04-29 | 2022-06-30 | アイポイント ファーマシューティカルズ, インコーポレイテッド | シュレム管を標的とするTie-2活性化物質 |
WO2021198780A1 (en) | 2020-03-30 | 2021-10-07 | Allergan Holdings Unlimited Company | Forms of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid |
AU2021318923A1 (en) * | 2020-07-28 | 2023-03-09 | Jazz Pharmaceuticals Ireland Limited | Chiral synthesis of fused bicyclic Raf inhibitors |
US20220096676A1 (en) | 2020-09-29 | 2022-03-31 | Abl Ip Holding Llc | Techniques for Directing Ultraviolet Energy Towards a Moving Surface |
US11850319B2 (en) | 2020-09-29 | 2023-12-26 | Abl Ip Holding Llc | Techniques for directing ultraviolet energy towards a moving surface |
CN114163348A (zh) * | 2020-11-27 | 2022-03-11 | 成都泰蓉生物科技有限公司 | 一种氨酰基取代的l-苯丙氨酸的合成方法 |
Family Cites Families (20)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DD142804A3 (de) * | 1977-11-07 | 1980-07-16 | Wagner Guenter | Verfahren zur herstellung von na-alkyl-bzw.na-aryl-sulfonylierten omega-amidinophenyl-alpha-aminoalkylcarbonsaeureamiden |
US4879398A (en) * | 1987-12-31 | 1989-11-07 | Monsanto Company | Process for producing 2,6-disubstituted tyrosine |
SE9402880D0 (sv) | 1994-08-30 | 1994-08-30 | Astra Ab | New peptide derivatives |
AR003108A1 (es) * | 1995-01-27 | 1998-07-08 | Novo Nordisk As | Compuestos con propiedades de liberacion de la hormona del crecimiento, composicion farmaceutica que los contienen, el uso de los mismos para la preparación de un medicamento. |
US5565568A (en) | 1995-04-06 | 1996-10-15 | Eli Lilly And Company | 2-acylaminopropanamides as tachykinin receptor antagonists |
CA2217006C (en) | 1995-04-13 | 2001-05-22 | Hoechst Marion Roussel, Inc. | Novel substituted piperazine derivatives having tachykinin receptor antagonists activity |
CA2203428A1 (en) | 1995-08-21 | 1997-02-27 | Philip Arthur Hipskind | 2-acylaminopropanamides as growth hormone secretagogues |
AU7710596A (en) | 1995-11-29 | 1997-06-19 | Nihon Nohyaku Co., Ltd. | Phenylalanine derivatives, optically active substances, salts or coordination compounds thereof, and their use as fungicides |
US5792760A (en) | 1997-04-23 | 1998-08-11 | Eli Lilly And Company | Bisindoles as tachykinin receptor antagonists |
IT1304898B1 (it) | 1998-09-08 | 2001-04-05 | Menarini Ricerche Spa | Prodotti con caratteristiche basiche aventi attivita' antagonista sulrecettore nk-1 e loro impiego in preparazioni farmaceutiche |
EP1055665B1 (en) * | 1999-05-28 | 2003-10-22 | Pfizer Products Inc. | 3-(3-Hydroxyphenyl)-3-amino-propionamide derivatives |
FR2796643B1 (fr) | 1999-07-22 | 2005-04-29 | Sod Conseils Rech Applic | Derives de 2-arylimino-2, 3-dihydrothiazoles, leurs procedes de preparation et leur utilisation therapeutique |
GB0021419D0 (en) | 2000-08-31 | 2000-10-18 | Oxford Glycosciences Uk Ltd | Compounds |
US20020072017A1 (en) * | 2000-10-19 | 2002-06-13 | Hudnall Phillip Montgomery | Stabilized p-phenylenediamine-type photographic color developers in free base form |
SK6282003A3 (en) | 2000-10-30 | 2004-02-03 | Janssen Pharmaceutica Nv | Tripeptidyl peptidase inhibitors |
KR100898562B1 (ko) * | 2001-10-15 | 2009-05-20 | 얀센 파마슈티카 엔.브이. | 신규 치환된 4-페닐-4-[1h-이미다졸-2-일]-피페리딘유도체 및 선택적인 비펩타이드 델타 아편유사작용제로서의 그의 용도 |
US7041681B2 (en) * | 2002-04-29 | 2006-05-09 | Janssen Pharmaceutica N.V. | Compounds as opioid receptor modulators |
UA86053C2 (ru) * | 2004-03-15 | 2009-03-25 | Янссен Фармацевтика Н.В. | Соединения как модуляторы опиоидных рецепторов |
US7282507B2 (en) | 2004-05-03 | 2007-10-16 | Janssen Pharmaceutica N.V. | Indole derivatives as selective androgen receptor modulators (SARMS) |
CA2601674A1 (en) * | 2005-03-14 | 2006-09-21 | Janssen Pharmaceutica N.V. | Process for the preparation of opioid modulators |
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