COMPOUNDS CONTAINING AN ALICYCLIE STRUCTURE AND ANTI-TUMOR APPLICATION

This invention relates with anti-tumor activities of new compounds containing an adamantyl group or analogs thereof. The invention also relates with the medication applications of anti-tumor and other diseases by this kind of compounds with the combination of S, P, T structures containing adamantyl group and the formation of stereoisomer, tautomers, prodrug, pharmaceutically acceptable salts, complex salts or solvates to their anticancer application and anticancer agents, which have the following general formula: 2. The compound according to the S formula of claim 1 , wherein:{'sub': 1', '2', '3', '4', '2', '1-10, 'The dotted lines are optionally substituted single bonds, optionally substituted double bond or a optionally substituted heterocyclic group containing carbon, oxygen, sulfur or nitrogen element; said X, X, X, Xare, independently at each occurrence, C═O, C═S, C═NH, C═Rb—Ra, CHOH, CHORb, CHRb or substituent, where Rb contains, independently at each occurrence, one or combination of C, N or P element; Ra is H, H, optionally substituted straight-alkyl, optionally substituted branched-alkyl, Coptionally substituted saturated alkyl, optionally substituted 1-4 double bond, optionally substituted 1-4 triple bond, optionally substituted unsaturated alkyl, optionally substituted saturated or unsaturated alicyclic, optionally substituted arylcyclic, optionally substituted aryl or optionally substituted heterocyclic, optionally substituted arylheterocyclic, fused heterocyclic group where contains hydroxyl, halogen, oxygen, nitrogen, sulfur, phosphorus element or selenium element;'}{'sub': 1', '2', '3', '4', '5', '6', '7', '8, 'said A, A, A, A, A, A, Aor Ais, independently at each occurrence, optionally substituted independently cyclic, alkyl, aryl, alicyclic, heterocyclic, aliphatic, aromatic heterocyclic, heterocyclic, glycosyl, multi-hydroxyl, amino acid, phosphate, acyloxyl, phosphoric, sulfonyloxyl, alkoxy, aryloxyl, heterocyclic oxyl, aryl cyclic, aliphatic ...

MIXED CRYSTAL AGOMELATINE (FORM VIII), PREPARATION METHOD AND USE THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING SAME

The present invention provides a mixed crystalline form VIII of agomelatine, its method of preparation, application and pharmaceutical composition. The said mixed crystal consists mainly of crystalline form VI of agomelatine. The said mixed crystalline form is stable and has good reproducibility. Through stability tests, it has been found to be superior to the crystalline form VI in terms of stability. As a result, the crystalline form VIII of the present invention possesses advantages in pharmaceutical preparation. 114-. (canceled)17. The mixed crystalline form according to claim 15 , having the following DSC change-in-absorption diagram claim 15 , the onset value range being 97-98° C. claim 15 , the endothermic peak area being no lower than 90% claim 15 , with the preferable ratio being 95-99%.19. The preparation method according to claim 18 , wherein the molar ratio of agomelatine compounds of formula (II) and sodium acetate is from 1:1-1.5 claim 18 ,20. The preparation method according to claim 19 , wherein the molar ratio of agomelatine compounds of formula (II) and sodium acetate is from 1:1-1.1.21. The preparation method according to claim 18 , wherein the ratio of volume of acetic acid to water is 1:15-30.22. The preparation method according to claim 18 , wherein when the temperature of the resulting reaction mixture reaches 12-18° C. claim 18 , water is added dropwise in order to bring about crystallization.23. The preparation method according to claim 22 , wherein when the temperature of the resulting reaction mixture reaches 15° C. claim 22 , water is added dropwise in order to bring about crystallization.24. The preparation method according to claim 18 , wherein water is added dropwise to the resulting reaction mixture which is then agitated at a temperature of 10° C. in order to bring about crystallization.25. The preparation method according to claim 18 , wherein following the addition of the sodium acetate claim 18 , the reaction mixture is heated to ...

AMINE-BORANES AS BIFUNCTIONAL REAGENTS FOR DIRECT AMIDATION OF CARBOXYLIC ACIDS

The present invention generally relates to a process for selective and direct activation and subsequent amidation of aliphatic and aromatic carboxylic acids to afford an amide RCONRR. That the process is capable of delivering gaseous or low-boiling point amines provides a major advantage over existing methodologies, which involves an intermediate of triacyloxyborane-amine complex [(RCO)—B—NHRR]. This procedure readily produces primary, secondary, and tertiary amides, and is compatible with the chirality of the acid and amine involved. The preparation of known pharmaceutical molecules and intermediates has also been demonstrated. 1. A process for direct activation and subsequent amidation of an aliphatic or an aromatic carboxylic acid to manufacture an amide RCONRR , comprising the steps of{'sup': 1', '2', '1', '2', '1', '2', '1', '2, 'sub': '3', 'a. preparing an amine-borane RRNH—NHfrom an amine RRNH; wherein Rand Rare, independently, hydrogen, an alkyl, or an aryl, wherein said alkyl or aryl are optionally substituted and said Rand Rare not both an aryl or a hydrogen at the same time;'}{'sup': 3', '3, 'b. preparing a carboxylic acid RCOOH, wherein Ris an alkyl or an aryl, each of which is optionally substituted;'}c. dissolving one equivalent of said amine-borane and about three equivalents of said carboxylic acid in xylenes or a compatible solvent to afford a reaction mixture;d. first heating said reaction mixture to about 90-100° C. for about 1 hour, then raising the temperature to about 150° C. for about 12 hours; and{'sup': 3', '1', '2', '3, 'e. resolving said reaction mixture to afford said amide RCONRRtogether with recovered excess carboxylic acid RCOOH.'}2. The process according to claim 1 , wherein said optionally substituted alkyl or aryl may comprises one or more heteroatoms selected from the group consisting of B claim 1 , N claim 1 , O claim 1 , S claim 1 , Se claim 1 , Cl claim 1 , Br claim 1 , F claim 1 , I claim 1 , Si claim 1 , As claim 1 , Te claim ...

High mobility group b1 protein inhibitors

Compounds, pharmaceutically acceptable salts, and pharmaceutical compositions thereof are disclosed that are useful for inhibition of the biological activity of HMGB1, as well as methods of treatment for diseases involving the inflammation activity or cytokine activity of HMGB1.

INHIBITORS OF DEUBIQUITINATING PROTEASES

Disclosed are small molecule inhibitors of deubiquitinating enzymes (DUBs), and methods of using them. Certain compounds display a preference for specific ubiquitin specific proteases (USPs). 23-. (canceled)58-. (canceled)1012-. (canceled)14. (canceled)16. (canceled)17. The compound of claim 1 , wherein the compound is a compound of Formula I or a compound of Formula II; and n is 1.18. The compound of claim 1 , wherein the compound is a compound of Formula I or a compound of Formula II; and m is 1.19. (canceled)20. The compound of claim 1 , wherein the compound is a compound of Formula I or a compound of Formula II; and Ris —H.2127-. (canceled)28. The compound of claim 1 , wherein Ris —C(O)ORor an optionally substituted benzyl.2938-. (canceled)4046-. (canceled)4853-. (canceled)5669-. (canceled) This application claims the benefit of priority to U.S. Provisional Patent Application Ser. No. 61/813,328, filed Apr. 18, 2013; the contents of which are hereby incorporated by reference.This invention was made with government support under R01-GM100921 awarded by the National Institutes of Health. The government has certain rights in the invention.The ubiquitin system is the linchpin in maintenance of cellular fitness. While many studies have focused on ubiquitylation pathways, comparatively little is known about deubquitination proteins (DUBs). DUBs are a large group of proteases that regulate ubiquitin-dependent regulatory pathways by cleaving ubiquitin-protein bonds. DUBs can also cleave C-terminally modified ubiquitin. DUBs are also commonly referred to as deubiquinating proteases, deubiquitylating proteases, deubiquitylating proteinases, deubiquinating proteinases, deubiquitinating peptidases, deubiquitinating isopeptidases, deubiquitylating isozpeptidases, deubiquitinases, deubiquitylases, ubiquitin proteases, ubiquitin hydrolyases, ubiquitin isopeptidases, or DUbs. The human genome encodes in five gene families nearly 100 DUBs with specificity for ubiquitin. ...

Use of sarmentine and its analogs for controlling plant pests

Methods and compositions for controlling plant pests, particularly weeds and/or plant phytopathogens using sarmentine and/or analogs thereof are disclosed.

NOVEL COMPOUNDS ADVANTAGEOUS IN THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISEASES AND DISORDERS

A series of novel amides showing broad pharmaceutical activity. Compounds described herein are effective as anticonvulsants, chemical countermeasures, and analgesics. Such compounds also show, neuroprotective/neuroreparative effects and activity against spinal muscular atrophy. Such pharmaceutically active compounds show utility in the treatment of central nervous system (“CNS”) diseases and disorders, such as anxiety, depression, insomnia, migraine headaches, schizophrenia, neurodegenerative diseases (e.g., Parkinson's disease, Alzheimer's, ALS, and Huntington's disease) spasticity, and bipolar disorder. Furthermore, such compounds may additionally find utility as analgesics (e.g., for the treatment of chronic or neuropathic pain) and as neuroprotective agents useful in the treatment of stroke(s), and/or traumatic brain and/or spinal cord injuries. 2. A pharmaceutical composition claim 1 , comprising a therapeutically effective amount of at least one compound of Formula I of admixed with at least one of a pharmaceutically acceptable carrier or an excipient.3. The pharmaceutical composition as in claim 2 , wherein the excipient includes a carrier.4. A pharmaceutical composition for treating and/or preventing one or more neurodegenerative disease claim 1 , comprising a neuroprotective and/or neuroreparative effective amount of at least one compound of Formula I of admixed with at least one of a pharmaceutically acceptable carrier or an excipient.5. The pharmaceutical composition of claim 4 , wherein the neurodegenerative disease is at least one of Huntington's Disease claim 4 , Parkinson's Disease claim 4 , Alzheimer's Disease claim 4 , or amyotrophic lateral sclerosis (ALS).6. A pharmaceutical composition for treating and/or preventing spinal muscular atrophy claim 1 , comprising a therapeutically effective amount of at least one compound of Formula I of admixed with at least one of a pharmaceutically acceptable carrier or an excipient.7. A method for treating and/ ...

Method for producing 3-arylpropionamide compound and 3-arylpropionic acid ester compound

(wherein X represents a chlorine atom or a bromine atom; and Y represents an alkyl group optionally substituted with fluorine atom(s), a hydrogen atom, a fluorine atom, a cyano group, an alkylcarbonyl group, a dialkylamino group, or the like) with acrylamide or an acrylic acid ester in the presence of a metal catalyst and a reducing agent.

SMALL MOLECULES THAT SPECIFICALLY INHIBIT TNF-INDUCED NF-KB INFLAMMATION PATHWAY

Provided herein are small molecules that specifically inhibit TNF-induced nuclear factor kB (NF-kB) inflammation pathway. Also provided are methods of screening compounds to identify molecules that specifically inhibit a TNF-induced NF-kB inflammation pathway, methods of inhibiting TNF-induced NF-kB inflammation pathway, and methods of preventing formation of mature TNFR1 complex. 3. The compound of claim 1 , wherein X claim 1 , Xand Xare O.4. The compound of claim 1 , wherein Ris H.5. The compound of claim 1 , wherein Ris a cyclopentyl or cyclohexyl.6. A pharmaceutical composition comprising the compound of and at least one pharmaceutically acceptable carrier.7. The pharmaceutical composition of claim 6 , wherein the composition is suitable for administration to a human.8. The pharmaceutical composition of claim 6 , formulated into a dosage form:(a) selected from the group consisting of liquid dispersions, gels, aerosols, lyophilized formulations, tablets, and capsules;(b) selected from the group consisting of controlled release formulations, fast melt formulations, delayed release formulations, extended release formulations, pulsatile release formulations, and mixed immediate release and controlled release formulations; or(c) any combination of (a) and (b).9. The pharmaceutical composition of claim 6 , formulated for administration selected from the group consisting of oral claim 6 , pulmonary claim 6 , rectal claim 6 , colonic claim 6 , parenteral claim 6 , intracisternal claim 6 , intravaginal claim 6 , intraperitoneal claim 6 , intravenous claim 6 , subcutaneous claim 6 , intramuscular claim 6 , nebulization claim 6 , inhalation claim 6 , ocular claim 6 , otic claim 6 , local claim 6 , buccal claim 6 , nasal claim 6 , and topical administration.11. The method of claim 10 , wherein the cell is a human cell.12. The method of claim 10 , wherein the method is in vivo or in vitro.13. The method of claim 12 , wherein the contacting is in vivo in a subject suffering ...

含有脂环结构化合物的抗肿瘤作用与应用

本发明涉及一种含有脂环结构化合物的抗肿瘤作用与应用，目的是提供一种含有金刚烷基或金刚烷类似结构基形成的链状化合物、立体异构体、前药、药用盐、复盐或溶剂化的化合物具有下列结构通式I，

Hydrogen peroxide complexes and their use in the cure system of anaerobic adhesives

Provided is a complex of hydrogen peroxide and at least one compound represented by Formula (I): wherein X is (i), -C(R 3 ) 3 , -C=C(R 3 ), -O(R 3 ), -N(R 3 ) 2 , or -S(R 3 ); and R 1 , R 2 , and R 3 are each independently selected from H, alkyl, alkenyl, alkynyl, aralkyl, aryl, heteroaryl heteroarylalkyl, heterocyclyl, and cycloalkyl, or R 2 and an R 3 are optionally taken together to form an alicyclic ring. Also provided are anaerobic cure systems and curable compositions employing the complexes described herein.

4-substituted-2-phenoxyphenylamine modulators of delta-opioid receptors

FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to novel compounds of formula I, possessing ability of binding with delta-opioid receptors. In formulaRis selected from the group, consisting of i) phenyl, optionally substituted with one-two substituents, independently selected from the group, consisting of Calkyl, Calcoxy, Calkylthio, hydroxyl, di(Calkyl), aminocarbonyl, chlorine and fluorine, in such a way that only one di(Calkyl)aminocarbonyl is present; ii) naphthyl; iii) pyridinyl, optionally substituted with one substituent, selected from the group, consisting of Calkyl, Calcoxy, Calkylthio, hydroxy, fluorine, chlorine and cyano; iv) pyrimidin-5-yl; v) furanyl; vi) thienyl; vii) 5-oxo-4,5-dihydro-[1,2,4]oxodiazol-3-yl; and viii) di(Calkyl)aminocarbonyl; Y represents ethyl, vinyl or bond; or Y represents O, when Rrepresents optionally substituted phenyl, where substituent represents Calcoxy; Rrepresents phenyl, optionally substituted with one-two substituents, independently selected from the group, consisting of Calkyl, Calcoxy, fluorine, chlorine and cyano, trifluoromethoxy and hydroxy; or Rrepresents phenyl, substituted with one aminocarbonyl, di(Calkyl)aminocarbonyl, Calcoxycarbonyl or carboxysubstituent; Ris selected from the group, consisting of i) 3-aminocyclohexyl; ii) 4-aminocyclohexyl; iii) piperidin-3-yl; iv) piperidin-4-yl; v) pyrrolodin-2-yl-methyl, in which pyrrolodin-2-yl is optionally substituted by 3-rd or 4-th position with one or two fluorine-substituents; vi) azetidin-3-yl; vii) 2-(N-methylamino)ethyl; viii) 3-hydroxy-2-aminopropyl; ix) piperidin-3-yl-methyl; x) 1-azabicyclo[2.2.2]octan-3-yl; and xi) 8-azabicyclo[3.2.1]octan-3-yl; or Rtogether with Rand nitrogen atom, which they both are bound to, form piperazinyl, optionally substituted with 4-Calkyl; Rrepresents hydrogen, 2-(N-methylamino)ethyl or Calkyl, optionally substituted with azetidin-3-yl.EFFECT: compounds can be used in treatment of pain in the range from medium to strong ...

Hydrogen peroxide complexes and their use in the cure system of anaerobic adhesives

본 발명은 과산화수소 및 화학식 Ⅰ로 표시되는 하나 이상의 화합물의 복합체를 제공한다. 그리고 본원에서 기술한 복합체를 사용하는 혐기성 경화 시스템 및 경화성 조성물을 제공한다. <화학식 Ⅰ> (상기 식에서, X는 , -C(R 3 ) 3 , -C≡C(R 3 ), -O(R 3 ), -N(R 3 ) 2 , 또는 -S(R 3 )이며; R 1 , R 2 , 및 R 3 는 수소, 알킬, 알케닐, 알키닐, 아르알킬, 아릴, 헤테로아릴, 헤테로아릴알킬, 헤테로시클릴, 및 시클로알킬로 이루어진 군으로부터 각각 독립적으로 선택되거나, 또는 R 2 및 R 3 는 임의적으로 함께 지환족 고리를 형성한다.)

New process for the synthesis of agomelatine

본 발명은 하기 화학식 (I)의 화합물의 산업적 합성 방법에 관한 것이다: The present invention relates to a process for the industrial synthesis of compounds of formula (I):

Compounds advantageous in the treatment of central nervous system diseases and disorders

A series of novel amides showing broad pharmaceutical activity. Compounds described herein are effective as anticonvulsants, chemical countermeasures, and analgesics. Such compounds also show, neuroprotective/neuroreparative effects and activity against spinal muscular atrophy. Such pharmaceutically active compounds show utility in the treatment of central nervous system (“CNS”) diseases and disorders, such as anxiety, depression, insomnia, migraine headaches, schizophrenia, neurodegenerative diseases (e.g., Parkinson's disease, Alzheimer's, ALS, and Huntington's disease) spasticity, and bipolar disorder. Furthermore, such compounds may additionally find utility as analgesics (e.g., for the treatment of chronic or neuropathic pain) and as neuroprotective agents useful in the treatment of stroke(s), and/or traumatic brain and/or spinal cord injuries.

Derivatives of adamantane, method of their synthesis, pharmaceutical composition based on thereof, method of its preparing and method of effect on immune suppression

FIELD: organic chemistry, chemical technology, pharmacy. SUBSTANCE: invention relates to novel compounds of the formula (I) where A means group CH 2 or oxygen atom; B means hydrogen or halogen atom; D means CH 2 , OCH 2 , NHCH 2 , CH 2 CH 2 ; R means phenyl, benzothiazolyl, indolyl, indazolyl, purinyl, pyridyl, pyrimidinyl, thiophenyl being each of these groups can be substituted or unsubstituted. Invention relates also to method of synthesis of these compounds that involves interaction of compound of the formula (II) where L means a removable group with compound of the formula Дуб с ПЧ сэ (19) 13) ВИ” 2197 477‘ (51) МПК? С2 С 07С 233/25, С 070 209/04, 231/54, 277/62, 221/22, Аб1 К 31/46, 31/40, 31/445, А 61Р 19/00 РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 2000117580/04, 01.12.1998 (71) Заявитель: АСТРАЗЕНЕКА Ю КЕЙ ЛИМИТЕД (СВ) (24) Дата начала действия патента: 01.12.1998 (72) Изобретатель: БЭКСТЕР Эндрю (СВ), БРАФ Стефен (СВ), МАКИНАЛЛИ Томас (СВ), МОРТИМОР Майкл (СВ), КЛЭДИНГБОЭЛЬ Дэвид (СВ) (30) Приоритет: 05.12.1997 ЗЕ 9704545-4 (46) Дата публикации: 21.01.2003 (56) Ссылки: М.1. Магауапап, оигпа! ог Мед!са! Спепизу, 1972, уо1.15, МЛЛ, р.1180-1182. ЕР 0395093 АЛ, 31.10.1990. ЗТМ |1егпаНопа!, Ее САРЦУ$, САРЕЦ$ ассеззюоп по. 1975:592744, Воситег по.83:192744. ЦЗ 3789072 АЛ, 29.01.1974. ЗТМ 1щегпаНопа!, Ее САРШИ$, САРШЦ$ ассеззюп по. 1974:26871, Воситет по.80:26871. ТМ |1егпаНопа!, Ее САРЦУ$, САРШЦ$ ассеззюоп по. 1968:402562, Воситег! по.69:2562. КО 2068840 СЛ, 10.11.1996. (73) Патентообладатель: АСТРАЗЕНЕКА Ю КЕЙ ЛИМИТЕД (СВ) (74) Патентный поверенный: Лебедева Наталья Георгиевна (85) Дата перевода заявки РСТ на национальную фазу: 05.07.2000 (86) Заявка РСТ: ЗЕ 9802189 (01.12.1998) (87) Публикация РСТ: М/О 99/29660 (17.06.1999) (98) Адрес для переписки: 129010, Москва, ул. Б. Спасская, 25, стр.3, ООО "Юридическая фирма Городисский и Партнеры", пат.пов. Н.Г. Лебедевой, рег.№ 0112 ( ...

Novel compounds

The invention provides adamantane derivatives, a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.

Bridged lipoglycopeptides that potentiate the activity of beta-lactam antibacterials

본 발명은 제1형 신호 펩티다제 억제제 (SpsB)인 신규 리포글리코펩티드 화합물을 제공한다. 본 발명의 화합물은, 특히 β-락탐 항생제, 예컨대 이미페넴 및 에르타페넴의 강화제로서 사용되는 경우, 다양한 박테리아 관련 감염성 질환의 치료에 유용하다. 따라서, 본 발명은 본원에 기재된 화합물을 단독으로 또는 β-락탐 항생제와 조합으로 사용하여 박테리아 관련 감염을 치료하는 방법을 제공한다.

NEW PROCESS FOR THE SYNTHESIS OF AGOMELATIN

NEW PROCESS FOR THE SYNTHESIS OF AGOMELATIN

Procédé de synthèse industrielle du composé de formule (I) g id="ID2934857-3" he="" wi="" file="" img-format="tif"/> > Process for the industrial synthesis of the compound of formula (I) ## EQU1 ##

Patent FR2729147B1

Hydrogen peroxide complexes and their use in the cure system of anaerobic adhesives

Provided is a complex of hydrogen peroxide and at least one compound represented by Formula (I): wherein X is (i), -C(R3)3, -C=C(R3), -O(R3), -N(R3)3, or -S(R3); and R1, R2, and R3 are each independently selected from H, alkyl, alkenyl, alkynyl, aralkyl, aryl, heteroaryl heteroarylalkyl, heterocyclyl, and cycloalkyl, or R2 and an R3 are optionally taken together to form an alicyclic ring. Also provided are anaerobic cure systems and curable compositions employing the complexes described herein.

NEW PROCEDURE FOR THE SYNTHESIS OF AGOMELATIN

SE REFIERE A UN PROCESO PARA LA SINTESIS DE AGOMELATINA QUE COMPRENDE LA REACCION DE (7-METOXI-1-NAFTIL)ACETONITRILO QUE SE SOMETE A UNA REDUCCION POR HIDROGENO EN PRESENCIA DE NIQUEL DE RANEY EN UN MEDIO QUE CONTIENE ANHIDRIDO ACETICO EN UN MEDIO PROTICO POLAR QUE SE AISLA EN SOLIDO, A UNA PRESION COMPRENDIDA ENTRE 10 Y 50 BARES DE H Y UNA TEMPERATURA ENTRE 25 Y 90 ºC. DICHO COMPUESTO ES UTIL EN EL TRATAMIENTO DE TRASTORNOS DEL SISTEMA NERVIOSO CENTRAL IT REFERS TO A PROCESS FOR THE SYNTHESIS OF AGOMELATIN THAT INCLUDES THE REACTION OF (7-METOXY-1-NAPHTHYL) ACETONITRILE THAT IS SUBMITTED TO A REDUCTION BY HYDROGEN IN THE PRESENCE OF RANEY NICKEL IN A MEDIUM CONTAINING A MEDIUM PROTEIN IN ACE ANHYDRIDE POLAR THAT IS ISOLATED IN SOLID, AT A PRESSURE OF BETWEEN 10 AND 50 BARS OF H AND A TEMPERATURE BETWEEN 25 AND 90 ºC. SAID COMPOUND IS USEFUL IN THE TREATMENT OF DISORDERS OF THE CENTRAL NERVOUS SYSTEM

Use of sarmentine and its analogs for controlling plant pests

Methods and compositions for modulating phytopathogenic infection in a plant comprise applying to the plant and/or seeds thereof and/or substrate used for growing said plant an amount of a sarmentine and/or a sarmentine analog having substantially the same activity as sarmentine effective to modulate said phytopathogenic infection via virus, fungi, bacteria, nematode and insect.

New method for synthesizing agomelatine

NEW PROCESS FOR OBTAINING THE V-CRYSTALLINE FORM OF AGOMELATIN

Process for the synthesis of agomelatine

Способ промышленного синтеза соединения формулы (I):. (I)

2-adamantyl-butyramide derivatives as selective 11.beta.-hsd1 inhibitors

The present invention relates to 2-adamantyl-butyramide derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11.beta.-HSD-1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.

Improved inhibitors for the soluble epoxide hydrolase

Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.

Hydrophilic oil repellent agent and method for manufacturing same, and surface covering material, coating film, resin composition, oil-water separation filter medium, and porous body

The hydrophilic oil repellent includes one or more types of nitrogen-containing fluorine-based compounds. The nitrogen-containing fluorine-based compound includes any one hydrophilicity imparting group selected from the group consisting of anion type hydrophilicity imparting groups, cation type hydrophilicity imparting groups, and amphoteric type hydrophilicity imparting groups in the molecule.

New process for the synthesis of agomelatine.

Procedimiento de síntesis industrial del compuesto de fórmula (I). (ver fórmula I).

MIXED CRYSTALLINE AGOMELATIN (FORM VIII), ITS METHOD OF OBTAINING AND APPLICATION AND PHARMACEUTICAL COMPOSITION, CONTAINING THE SAME

Настоящее изобретение обеспечивает смешанную кристаллическую форму VIII агомелатина, его способ получения, применение и фармацевтическую композицию. Указанный смешанный кристалл включает главным образом кристаллическую форму VI агомелатина. Указанная смешанная кристаллическая форма является стабильной и имеет хорошую воспроизводимость. Посредством тестов стабильности было найдено превосходство по сравнению с кристаллической формой VI с точки зрения стабильности. Вследствие этого, кристаллическая форма VIII настоящего изобретения обладает преимуществами в фармацевтическом получении. The present invention provides a mixed crystalline form of agomelatine form VIII, its preparation method, use and pharmaceutical composition. The specified mixed crystal includes mainly crystalline form VI agomelatine. The specified mixed crystalline form is stable and has good reproducibility. Through stability tests, superiority was found over crystalline form VI in terms of stability. As a result, crystalline form VIII of the present invention has advantages in pharmaceutical preparation.

NEW PROCEDURE FOR OBTAINING THE CRYSTAL V FORM OF AGOMELATIN

REFERIDA A UNA FORMA CRISTALINA V DE AGOMELATINA DE FORMULA (I) QUE PRESENTA UN DIAGRAMA DE DIFRACCION X SOBRE POLVO CON VALORES DE ANGULOS DE BRAGG 2 THETA TALES COMO 9,84, 12,40, 13,31, 15,14, 15,98, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UN PROCEDIMIENTO DE OBTENCION DE LA AGOMELATINA CRISTALINA V MEDIANTE LA ATOMIZACION DE UNA DISOLUCION DE AGOMELATINA EN UNA CONCENTRACION DE 5 g/l, EN UN DISOLVENTE TAL COMO ETANOL Y ETER ISOPROPILICO, A UNA TEMPERATURA DE EBULLICION INFERIOR A 120 ºC REFERRED TO A CRYSTALLINE V FORM OF AGOMELATIN OF FORMULA (I) THAT PRESENTS AN X DIFFRACTION DIAGRAM ON POWDER WITH ANGLE VALUES OF BRAGG 2 THETA SUCH AS 9.84, 12.40, 13.31, 15.14, 15, 98, AMONG OTHERS. IT ALSO REFERS TO A PROCEDURE FOR OBTAINING CRYSTALLINE AGOMELATIN V BY ATOMIZING A SOLUTION OF AGOMELATIN IN A CONCENTRATION OF 5 g / l, IN A SOLVENT SUCH AS ETHANOL AND ISOPROPYL ETHER, AT A BOILING TEMPERATURE LESS THAN 120ºC.

Method of producing acetate salt of methyl ester of (2r,3s)-3-phenylisoserine

FIELD: chemistry. SUBSTANCE: invention relates to a method for anantioselective production of an acetate salt of methyl ester of (2R,3S)-3-phenylisoserine of formula (I), which is a structural element suitable for use in synthesis of taxane derivatives. The method involves the following steps: a) treating racemic treo-3-phenylisoserine amide (VI) with an enantiomerically pure acid to obtain the corresponding salt formed from (2R,3S)-3-phenylisoserine amide and acid; b) treating the salt formed from (2R,3S)-3-phenylisoserine amide and acid with a strong inorganic acid in a protonic solvent to obtain a salt formed from (2R,3S)-3-phenylisoserine amide and inorganic acid; c) treating the salt formed from (2R,3S)-3-phenylisoserine amide and inorganic acid with hydrochloric acid in a protonic solvent with subsequent treatment with acetic acid to crystallise an acetate salt of methyl ester of (2R,3S)-3-phenylisoserine amide. The invention also relates to an intermediate compound, specifically (2R,3S)-3-phenylisoserine amide in form of a salt of (-) dibenzoyl tartaric acid. EFFECT: method for enantioselective production of an acetate salt of methyl ester of (2R,3S)-3-phenylisoserine amide of formula (I). 4 cl, 6 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 459 802 (13) C2 (51) МПК C07C 227/18 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21)(22) Заявка: 2009131595/04, 11.02.2008 (24) Дата начала отсчета срока действия патента: 11.02.2008 (43) Дата публикации заявки: 27.02.2011 Бюл. № 6 (73) Патентообладатель(и): ИНДЕНА С.П.А. (IT) 2 4 5 9 8 0 2 (45) Опубликовано: 27.08.2012 Бюл. № 24 (56) Список документов, цитированных в отчете о поиске: US 6025516 А 15.02.2000. Peter G.M.Wuts et al, Tetrahedron: Asymmetry, 2000, 11, p.21172123. Kearns J. et al, Tetrahedron Letters, 1984, v.35, no.18, p.2845-2848. RU 2103258 C1 27.01.1998. 2 4 5 9 8 0 2 R U (86) Заявка PCT: EP 2008/001015 (11.02.2008) C 2 C 2 (85) Дата начала рассмотрения ...

New process for synthesizing agomelatine

La présente invention vise un procédé de synthèse industrielle de l'agomélatine de formule (I) (voir formule I) à partir du 3-méthoxyacénaphtoquinone de formule (II): (voir formule II)

Alkyl (hetero) cyclic derivatives, processes for their preparation and pharmaceutical compositions containing them

Use of sarmentine and its analogs for controlling weeds

New method for obtaining the crystalline form v of agomelatine

New alkylated (hetero)cyclic compounds; process for preparing the same and pharmaceutical compositions containing them

L'invention concerne les composés de formule (I): (See formula I) et leur procédé de préparation. Ces composés sont particulièrement utiles pour le traitement des troubles du système mélatoninergique. The invention relates to the compounds of formula (I): (See formula I) and their preparation process. These compounds are particularly useful for the treatment of disorders of the melatoninergic system.

Process for the production of 2- [4 - ( 3- and 2-fluorobenzyloxy) benzylamino] propan amides

Mixed crystal of agomelatine (form-VIII), preparation method and application thereof and pharmaceutical composition containing the same

本发明提供了阿戈美拉汀混晶(形式-VIII)、其制备方法、应用和包含其的药物组合物，其中所述混晶主要含阿戈美拉汀VI晶型。该混晶晶型稳定且重现性好，通过稳定性实验发现在稳定性方面优于VI晶型。因此，本发明的形式-VIII在制剂方面具有优势。

NEW AGOMELATINE SYNTHESIS PROCEDURE

New fluoro:cyclopropane derivs. - useful as insecticides and acaricides

Fluorocyclopropane derivs. of formula (I) are news, where R1 is H, f or Cl; A is COOR2, CONR2R3, CH2OR4 or COOCH2CONR2R3; R2 and R3 are H, 1-20C alkyl, 2-20C alkenyl, 2-20C alkynyl, (1-10C)alkoxy(1-10C)alkyl, 1-10C haloalkyl, halocyclopropyl(1-9C)alkylcarboxy(2-10C)alkyl (sic), halocyclopropyl(1-9C)alkylcarboxy(2-6C)alkoxy(2-6C)alkyl (sic), aryl(1-3C)alkyl, aryl(2-4C)alkenyl, aryl(2-4C)alkynyl, haloaryl(1-3C)alkyl, haloaryl(2-4C)alkenyl, aryloxyaryl(1-3C)alkyl, aryloxyaryl(2-4C)alkenyl, (1-10C)alkylaryl(1-3C)alkyl, (1-10C)alkylaryl(2-4C)alkenyl, (1-10C)alkoxyaryl(1-3C)alkyl, (1-10C)alkoxyaryl(2-4C)alkenyl, (2-6C)alkenyloxyaryl(2-4C)alkenyl, (2-6C)alkynyloxyaryl(2-4C)alkenyl, halocyclopropyl(1-4C)alkylcarboxyaryl (sic), halocyclopropyl(1-4C)alkylcarboxyaryl(2-4C)alkenyl, Ar or Het; or NR2R3 is a satd. or unsatd., branched or unbranched (sic) heterocyclic ring; or R2 in COOR2 is alkali metal, 1 equiv. of a divalent metal, or ammonium opt. substd. by one or more 1-10C alkyl gps.; Ar is aryl opt. substd. by one or more of 1-20C alkyl, 1-6C haloalkyl, 1-16C alkoxy, 1-6C haloalkoxy, phenyl(1-6C)alkyl, phenyl(1-6C)alkoxy, 3-10C cycloalkoxy, 3-10C halocycloalkenyloxy, 2-6C haloalkenyloxy, 2-6C alkynyloxy, 2-6C haloalkynyloxy, aryl(1-6C)alkoxy, halogen, NH2, CN, OH, NO2, aryloxy, heteroaryloxy, haloaryloxy, arylamino, haloarylamino, 2-7C alkoxycarbonyl, 3-8C alkoxycarbonylmethyl, 2-7C haloalkoxycarbonyl, 1-2C alkyldioxy (sic), 1-6C alkylthio, 1-6C alkylamino and di(1-6C alkyl)amino; Het is heteroaryl opt. substd. by halogen, 1-3C alkyl or 1-3C haloalkyl; R4 is H or COR2; and n is 2-20. USE - (I) are insecticides and acaricides useful for controlling crop pests and animal and human ectoparasites, e.g. aphio, Nilaparvata, Tetranychuo, Diabrotica and Heliothio spp

Mixed crystal agomelatine (form-viii), preparation method and use thereof and pharmaceutical composition containing same.

La presente invención proporciona un cristal mixto de agomelatina (forma VIII), sus métodos de preparación, su aplicación y sus composiciones farmacéuticas en las que el cristal mixto es principalmente agomelatina de forma VI. La estabilidad del tipo mixto y la buena reproducibilidad y su método de preparación son mejores que en la mayoría de los informes existentes respecto de estabilidad y solubilidad del polimorfo VI. Por lo tanto, la presente invención proporciona una forma VIII que resulta ventajosa en la preparación.

New alkylated (hetero) cyclic compounds, process of their preparation and pharmaceutical compositions containing them

Bridged lipoglycopeptides that potentiate the activity of beta-lactam antibacterials

The present invention provides novel lipoglycopeptide compounds which are Type 1 signal peptidase inhibitors (SpsB). Compounds of the present invention are useful for the treatment of various bacterial related infectious diseases, particularly when used as a potentiator of a ß-lactam antibiotic such as imipenem and ertapenem. Accordingly, the present invention provides a method for the treatment of bacterial related infections using the compounds described herein, either alone or in combination with a ß-lactam antibiotic.

New process for synthesizing agomelatine

Procédé de synthèse industrielle du composé de formule (I) (voir formule I) Process for the industrial synthesis of the compound of formula (I) (see formula I)

Crystalline form VIII of agomelatine, preparation method, use thereof and pharmaceutical composition containing the same

The invention provides a mixed crystalline form VIII of agomelatine, the preparation method, use thereof, and a pharmaceutical composition containing the same.The said crystalline form of agomelatine is stable and has good reproducibility. It is found through a stability test to be superior to a crystal form VI in terms of stability. Therefore, the crystalline form VIII of the present invention has an advantage in terms of preparation. The preparation method, according to the invention, involves the dissolution of agomelatine compound in acetic acid, to which sodium acetate is then added, followed by the dropwise addition of water to this reaction mixture, which is then agitated at a temperature of 7…13°C in order to bring about crystallization, with the crystals then being separated from the solution.

Process for the preparation of (2r,3s)-3-phenylisoserine methyl ester acetate salt.

Un procedimiento para la preparación enantioselectiva de la sal acetato de metil éster de (2R,3S)-3-fenilisoserina de fórmula (I) (ver fórmula (I)) que es un bloque constructor útil para la síntesis y derivados de taxano; el procedimiento involucra la resolución de la amida de treo-fenilisoserina racémica y su conversión a (I).

NEW PROCESS FOR THE SYNTHESIS OF AGOMELATIN

Improved inhibitors for the soluble epoxide hydrolase

Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.

Alkyl (hetero) cyclic compounds process for their preparation and pharmaceutical compositions containing them

New process for obtaining crystalline form v of agomelatine

La présente invention prise un procédé d'obtention de la forme cristalline V de l'agomélatine de formule (I) par atomisation: (voir formule I)

Process for the synthesis of agomelatine

Synthesis of agomelatine comprises reaction of 3-methoxyacenaphthoquinone (II) in the presence of strong base to obtain (7-methoxy-naphthalen-1-yl)-oxo-acetic acid (III); placing (III) under amination conditions to obtain 1-(7-methoxy-naphthalen-1- yl)-propane-1,2-dione (IV); reacting (IV) with a reducing system to obtain 2-(7-methoxy-naphthalen-1-yl)-ethylamine (V); and reacting (V) with sodium acetate and acetic anhydride to obtain agomelatine, which is isolated in the form of a solid. An independent claim is included for 1-(7-methoxy-naphthalen-1-yl)-pr opane-1,2-dione (IV) as intermediate for the synthesis of agomelatine. - ACTIVITY : Antidepressant; Hypnotic; Cardiovascular-Gen.; Gastrointestinal-Gen.; CNS-Gen.; Eating-Disorders-Gen.; Anorectic; Muscular-Gen. - MECHANISM OF ACTION : 5-Hydroxytryptamine 2C receptor antagonist.

Process for the preparation of (2r,3s)-3-phenylisoserine methyl ester acetate salt

A process for the enantioselective preparation of (2R,3S)-3-phenylisoserine methyl ester acetate salt of formula (I) which is an useful building block for the synthesis of taxane derivatives. The process involves the resolution of racemic threo-phenylisoserine amide and its conversion into (I).

NEW PROCESS FOR THE SYNTHESIS OF AGOMELATIN

NEW PROCEDURE FOR THE SYNTHESIS OF AGOMELATIN.

Procedimiento de síntesis industrial del compuesto de fórmula (I):

N-alkylcarbonyl-amino acid ester and n-alkylcarbonyl-amino lactone compounds and their use

一般而言，本发明涉及影响感觉过程的清爽、安抚和清凉化合物。更具体而言，本发明涉及本文所述的某些N-烷基羰基-氨基酸酯和N-烷基羰基-氨基内酯化合物；包含该类化合物的组合物和物品；和治疗方法，例如，缓解皮肤以及口腔和上呼吸道的内层的刺激、痒和疼痛不适的方法，例如治疗咳嗽和/或哮喘的方法。

N-alkylcarbonyl-amino acid ester and n-alkylcarbonyl-amino lactone compounds and their use

一般而言，本发明涉及影响感觉过程的清爽、安抚和清凉化合物。更具体而言，本发明涉及本文所述的某些N－烷基羰基－氨基酸酯和N－烷基羰基－氨基内酯化合物；包含该类化合物的组合物和物品；和治疗方法，例如，缓解皮肤以及口腔和上呼吸道的内层的刺激、痒和疼痛不适的方法，例如治疗咳嗽和/或哮喘的方法。

The method producing 2-[4-(3-and 2-fluorine benzyloxy) benzyl amino] Propionamides

获得具有高纯度，特别是具有低于0.03%，优选低于0.01%重量的二苄基衍生物杂质含量的治疗活性2?[4?(3?和2?(氟苄氧基)苄氨基)丙酰胺类及其与药学上可接受的酸形成的盐的方法。该方法通过在有多相催化剂存在下的质子有机溶剂中使希夫碱中间体2?[4?(3?和2?氟苄氧基)亚苄氨基]丙酰胺类催化加氢来进行。

Use of sarmentine and its analogs for controlling plant pests

Methods and compositions for controlling plant pests, particularly weeds and/or plant phytopathogens using sarmentine and/or analogs thereof are disclosed.

New process for the synthesis of agomelatine

NEW PROCEDURE FOR OBTAINING THE CRYSTALLINE V FORM OF AGOMELATINE

Procedimiento de obtencion de la forma cristalina V del compuesto de formula (I).

process for agomelatine synthesis

A presente invenção refere-se a um processo para a síntese industrial do composto da fórmula (I): The present invention relates to a process for the industrial synthesis of the compound of formula (I):

Process for the preparation of (2r,3s)-3-phenylisoserine methyl ester acetate salt

Cyclic Bisamides Useful in Formulating Inks for Phase-Change Printing

Cyclic bisamides may be used to formulate inks for jet ink printing. The cyclic bisamide may be prepared from a cyclic diamine and acylic monocarboxylic acids. Conversely, the cyclic bisamide may be prepared from a cyclic diacid and acylic monoamines. The performance properties of the product may be enhanced by adding some additional difunctional reactant(s), e.g., diacid or diamine. A blend of bisamides may provide better performance properties than either of the component bisamides alone, where the blend includes at least one cyclic bisamide. The bisamides, in combination with an image-forming material, and optionally in combination with other materials, is taken to a molten form and then applied to a substrate to provide a printed substrate.

N-alkylcarbonyl-amino acid ester and N-alkylcarbonyl-amino lactone compounds and their use

The present invention generally relates to refreshing, soothing, and cooling compounds that affect sensory processes. More particularly, the present invention pertains to certain -alkylcarbonyl-amino acid ester and -alkylcarbonyl-amino lactone compounds as described herein; compositions and articles comprising such compounds; and methods of treatment, for example, methods of alleviating the discomforts of irritation, itch, and pain in the skin and in the linings of the oral cavity and upper respiratory tract, for example, in methods of treatment of cough and/or asthma.

METHOD TO CONTROL WEED HERBS

“método para controlar ervas daninhas.” são divulgados neste documento métodos e composições para controlar pragas de plantas, particularmente ervas daninhas e/ou fitopatógenos de plantas, usando sarmentina e/ou análogos 5 da mesma. "Method for controlling weeds." Disclosed herein are methods and compositions for controlling plant pests, particularly weeds and / or plant phytopathogens, using sarmentin and / or analogues thereof.

Process for the preparation of (2r, 3s) -3-phenylisoserine methyl ester acetate salt

Cyclic bisamides useful in formulating inks for phase-change printing

环状双酰胺可以用来配制喷墨印刷的油墨。所述环状双酰胺可以由环状双胺和非环状的一元羧酸制备。反过来，所述环状双酰胺也可以由环状二酸和非环状的一元胺制备。通过添加附加的双官能团反应物，例如二酸或二胺可以提高产品的性能。双酰胺的掺合物可以提供比任一单组分的双酰胺更好的性能，其中掺合物包括至少一种环状双酰胺。使双酰胺采取熔融形态，与成像材料组合，并且任选与其它材料组合，然后施加到衬底上，从而提供印刷的衬底。

New process for synthesizing agomelatine

本发明涉及合成阿戈美拉汀的新方法，工业合成式(I)化合物的方法。

NEW AGOMELATINE SYNTHESIS PROCEDURE

Procedimeinto de sintesis industrial del compuesto de formula (I).

Adamantane derivatives

本发明提供式(Ⅰ)所代表的金刚烷衍生物、其制备方法、含有该衍生物的药物组合物及其在治疗中的用途。所说的式(Ⅰ)中,A代表基团CH 2 或O原子,B代表H或卤原子,D代表基团CH 2 、OCH 2 、NHCH 2 或CH 2 CH 2 ,R代表苯基、苯并噻唑基、吲哚基、吲唑基、嘌呤基、吡啶基、嘧啶基或噻吩基,各基团可以选择性地被一个或多个取代基取代。

New process for the synthesis of agomelatine

본 발명은 하기 화학식 (I)의 산업적 합성 방법에 관한 것이다: The present invention relates to a process for the industrial synthesis of formula (I):

Use of sarmentine and its analogs for controlling weeds

process for obtaining the crystalline form of agomelatine

PROCESSO PARA A OBTENçãO DA FORMA CRISTALINA DA AGOMELATINA. Processo para a obtenção da forma cristalina V do composto de formula (I): PROCESS FOR OBTAINING THE CRYSTALLINE FORM OF AGOMELATIN. Process for obtaining crystalline form V of the compound of formula (I):

Derivatives of carboxymethylcyclopropane

Novel 2-(2-chloro-2-fluorocyclopropyl)acetic acid derivatives of the formula I <IMAGE> in which X is oxygen or -NR-, Y is hydrogen or in each case unsubstituted or substituted C1-C20-alkyl, C3-C7-cycloalkyl, C3-C20-alkenyl, C3-C20-alkynyl, benzyl or aryl, and R is hydrogen or C1-C6-alkyl, can be used as pesticides, preferably for controlling insects and arachnids.

4-SUBSTITUTED-2-PHENOXYPHENYLAMINE MODULATORS OF DELTA-OPIOID RECEPTORS

1. Соединение формулы IгдеRвыбран из группы, состоящей изi) фенила, необязательно замещенного одним-двумя заместителями, независимо выбранными из группы, состоящей из Cалкила, Cалкокси, Cалкилтио, гидрокси, ди(Cалкил)аминокарбонила, хлора и фтора; таким образом, чтобы присутствовал только один ди(Cалкил)аминокарбонил;ii) нафтила;iii) пиридинила, необязательно замещенного одним заместителем, выбранным из группы, состоящей из Cалкила, Cалкокси, Cалкилтио, гидрокси, фтора, хлора и циано;iv) пиримидин-5-ила;v) фуранила;vi) тиенила;vii) 5-оксо-4,5-дигидро-[1,2,4]оксодиазол-3-ила; иviii) ди(Cалкил)аминокарбонила;при условии что, когда Rпредставляет собой 5-оксо-4,5-дигидро-[1,2,4]оксадиазол-3-ил, Y представляет собой связь;Y представляет собой этил, винил или связь;или Y представляет собой O, когда Rпредставляет собой необязательно замещенный фенил;Rпредставляет собой фенил, необязательно замещенный одним-двумя заместителями, независимо выбранными из группы, состоящей из Cалкила, Cалкокси, фтора, хлора, циано, трифторметокси и гидрокси;или Rпредставляет собой фенил, замещенный одним аминокарбонилом, ди(Cалкил)аминокарбонилом, Cалкоксикарбонилом или карбоксизаместителем;Rвыбран из группы, состоящей изi) 3-аминоциклогексила;ii) 4-аминоциклогексила;iii) пиперидин-3-ила;iv) пиперидин-4-ила;v) пирролидин-2-ил-метила, в котором пирролидин-2-ил необязательно замещен по 3-му или 4-му положению одним или двумя фторзаместителями;vi) азетидин-3-ил-метила;vii) 2-(N-метиламино)этила;viii) 3-гидрокси-2-аминопропила;ix) пиперидин-3-ил-метила;x) 1-азабицикло[2.2.2]октан-3-ила; иxi) 8-азабицикло[3.2.1]октан-3-ила;или Rвместе с Rи атомом азота, к которому они оба присоединены, образуют пиперазинил, необяз�

New process for the synthesis of agomelatine

Inhibitors for the Soluble Epoxide Hydrolase

Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.

New process for obtaining the crystalline form v of agomelatine

New process for the synthesis of agomelatine

Process for the preparation of 2- [4- (3- and 2-fluorobenzyloxy) benzylamino] propanamides

En fremgangsmåte for å oppnå terapeutisk aktive 2-[4-(3- og 2. (fluorbenzyloksy)benzylamino]propanamider og deres salter med farmasøytisk akseptable syrer med høy renhetsgrad, særlig med et innhold av dibenzyl derivat urenheter lavere enn 0,03 %, foretrukket lavere enn 0.01 % i forhold til vekt. Fremgangsmåten utføres ved å underkaste Schiff base intermediatene 2-[4-(3- og 2-fluorbenzyloksy)benzylidenamino]propanamider for katalytisk hydrogenering under nærvær av en heterogen katalysator i et protisk organisk løsemiddel.

New process for the synthesis of agomelatine

본 발명은 하기 화학식 (I)의 산업적 합성 방법에 관한 것이다: The present invention relates to a process for the industrial synthesis of formula (I):

Mixed crystal agomelatine (form-viii), preparation method and use thereof and pharmaceutical composition containing same

Bridged lipoglycopeptides that potentiate the activity of beta-lactam antibacterials

The present invention provides novel lipoglycopeptide compounds which are Type 1 signal peptidase inhibitors (SpsB). Compounds of the present invention are useful for the treatment of various bacterial related infectious diseases, particularly when used as a potentiator of a β-lactam antibiotic such as imipenem and ertapenem. Accordingly, the present invention provides a method for the treatment of bacterial related infections using the compounds described herein, either alone or in combination with a β-lactam antibiotic.

Use of sarmentine and its analogs for controlling plant pests

Methods and compositions for modulating phytopathogenic infection in a plant comprise applying to the plant and/or seeds thereof and/or substrate used for growing said plant an amount of a sarmentine and/or a sarmentine analog having substantially the same activity as sarmentine effective to modulate said phytopathogenic infection via virus, fungi, bacteria, nematode and insect.

New process for the synthesis of agomelatine

Cycloalkylamides and their therapeutic use as antiepileptic and anticonvulsant

The present invention relates to the use of compounds of formula (I)for the treatment of a variety of disorders including, bu t not limited to, epilepsy, bipolar disorder, psychiatric disorders, migraine, pain, neuroprotection, and movement disorders.

NEW AGOMELATINE SYNTHESIS PROCEDURE

Procedimiento de sintesis industrial del compuesto de formula (I).

mixed crystalline agomelatine (forma-viii), method of preparation and use thereof and pharmaceutical composition containing same

resumo patente de invenção: "agomelatina cristalina misturada (forma-viii), método de preparação e uso da mesma e composição farmacêutica contendo a mesma". a presente invenção refere-se a uma forma viii cristalina misturada da agomelatina, o seu método de preparação, aplicação e composição farmacêutica. o cristal misturado citado acima consiste principalmente na forma cristalina vi da agomelatina. a forma cristalina misturada citada acima é estável e tem a boa reprodutibilidade. através de testes de estabilidade, foi encontrado para ser superior à forma cristalina vi quanto a estabilidade. por conseguinte, a forma cristalina viii da presente invenção possui vantagens na preparação farmacêutica. 1/1 Patent Summary: "Mixed crystalline agomelatine (forma-viii), method of preparation and use thereof and pharmaceutical composition containing same". The present invention relates to a mixed crystalline form of agomelatine, its method of preparation, application and pharmaceutical composition. The above mixed crystal consists mainly of the crystalline form vi of agomelatine. The above mixed crystalline form is stable and has good reproducibility. through stability testing, was found to be superior to the crystalline form vi for stability. therefore, the crystalline form viii of the present invention has advantages in the pharmaceutical preparation. 1/1

New process for the synthesis of agomelatine

2-adamantyl-butyramide derivatives as selective 11 beta-hsd1 inhibitors

Carboxymethylcyclopropane derivatives

NEW AGOMELATINE SYNTHESIS PROCEDURE

Procedimiento de síntesis industrial del compuesto de fórmula: ESPACIO PARA LA FÓRMULA Industrial synthesis procedure of the compound of formula: SPACE FOR FORMULA

New process for the synthesis of agomelatine

New alkylated (hetero)cyclic compounds; process for preparing the same and pharmaceutical compositions containing them

L'invention concerne les composés de formule (I): (See formula I) et leur procédé de préparation. Ces composés sont particulièrement utiles pour le traitement des troubles du système mélatoninergique.

Carboxymethylcyclopropane derivatives

Process for the production of 2-[4-(3- and 2-fluorobenzyloxy) benzylamino) propan amides

A process for obtaining therapeutically active 2-[4-(3- and 2- (fluorobenzyloxy)benzylamino]propanamides and their salts with pharmaceutically acceptable acids with high purity degree, in particular, with a content of dibenzyl derivatives impurities lower than 0.03%, preferably lower than 0.01% by weight. The process is carried out by submitting the Schiff bases intermediates 2- [4-(3- and 2-fluorobenzyloxy)benzylideneamino]propanamides to catalytic hydrogenation in the presence of a heterogeneous catalyst in a protic organic solvent.

Use of sarmentine and its analogs for controlling plant pests