cas 18621-17-5, 1-(Diphenylmethyl)-3-hydroxyazetidine

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Indirect reduction of CO2and recycling of polymers by manganese-catalyzed transfer hydrogenation of amides, carbamates, urea derivatives, and polyurethanes
The reduction of polar bonds, in particular carbonyl groups, is of fundamental importance in organic chemistry and biology. Herein, we report a manganese pincer complex as a versatile catalyst for the transfer hydrogenation of amides, carbamates, urea derivatives, and even polyurethanes leading to the corresponding alcohols, amines, and methanol as products. Since these compound classes can be prepared using CO2as a C1 building block the reported reaction represents an approach to the indirect reduction of CO2. Notably, these are the first examples on the reduction of carbamates and urea derivatives as well as on the C-N bond cleavage in amides by transfer hydrogenation. The general applicability of this methodology is highlighted by the successful reduction of 12 urea derivatives, 26 carbamates and 11 amides. The corresponding amines, alcohols and methanol were obtained in good to excellent yields up to 97%. Furthermore, polyurethanes were successfully converted which represents a viable strategy towards a circular economy. Based on control experiments and the observed intermediates a feasible mechanism is proposed.
Liu, Xin,Werner, Thomas
p. 10590 - 10597
(2021/08/20)

Selective Deprotection of the Diphenylmethylsilyl (DPMS) Hydroxyl Protecting Group under Environmentally Responsible, Aqueous Conditions
Two new methods for selective deprotection of diphenylmethylsilyl (DPMS) ethers are described. Unmasking can be achieved with either catalytic amounts of perfluoro-1-butanesulfonyl fluoride (a SuFEx reagent) under mild, aqueous micellar conditions, or using stoichiometric amounts of 18-crown-6 ether in aqueous ethanol.
Akporji, Nnamdi,Lieberman, Josh,Maser, Michael,Yoshimura, Masahiko,Boskovic, Zarko,Lipshutz, Bruce H.
p. 5743 - 5747
(2019/11/11)

TAU-PROTEIN TARGETING PROTACS AND ASSOCIATED METHODS OF USE
The present disclosure relates to bifunctional compounds, which find utility as modulators of tau protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tau protein, such that tau protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tau. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tau protein. Diseases or disorders that result from aggregation or accumulation of tau protein are treated or prevented with compounds and compositions of the present disclosure.
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Paragraph 1022

(2018/05/24)

Synthesis of Novel Hybrid 4 H -Pyran-lipoic and 4 H -Pyran-azetidine Derivatives
In this study, a molecular hybridization strategy was used to design and synthesize two novel series of hybrid compounds: 4 H -pyran-lipoic and 4 H -pyran-azetidine, employing ammonium hydroxide and involving the participation of aldehydes, malononitrile, and compounds derived from β-ketoesters to obtain the products with good yields.
Hernández-Borja, Fernando,Contreras, Leticia,López, Julio,Alcaraz, Yolanda,Cruz, David,Estrada-Soto, Samuel,Delgado, Francisco,Vázquez, Miguel A.
p. 1020 - 1026
(2017/11/29)

Preparation method of N-diphenylmethyl-3-hydroxyazetidine
The invention relates to a preparation method of azelnidipine intermediate N-(diphenylmethyl)-3-hydroxyazetidine. The preparation method is disclosed based improvement of a conventional method. According to the preparation method, an alkali is added into a reaction system, so that reaction time is shortened from 48h to 16h or less, the reaction time is shortened greatly, and energy consumption is reduced; yield can be maintained to be 83 to 88%, and product purity is increased to be higher than 99.9% via effective adjustment of reaction temperature and appropriate postprocessing, and the preparation method is extremely suitable for industrialized production.
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Paragraph 0022; 0023; 0024; 0025; 0026

(2017/05/16)

JAK INHIBITOR
The present invention discloses a series of JAK inhibitors, and particularly discloses a compound of formula (I) or a pharmaceutically acceptable salt thereof and the use thereof in preparation of drugs for treating diseases related to JAK.
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Paragraph 0289; 0290; 0291

(2017/12/15)

9-AMINOMETHYL SUBSTITUTED TETRACYCLINE COMPOUND
The present invention relates to 9-aminomethyl substituted tetracycline compounds represented by formula (I), or pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, as well as a method for preparing these compounds and a pharmaceutical composition comprising the same. The present invention relates also to a use of these compounds in the preparation of a medicament for the treatment and/or prophylaxis of tetracycline drug-sensitive disease. wherein, R2a, R2b, R3, R4a, R4b, R5, R6a, R6b, R7, R8, R9a, R9b, R10, R11, R12, R13a and R13b are each independently as defined in the description.
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Paragraph 0160-0162

(2014/06/24)

PROCESSES AND INTERMEDIATES FOR MAKING A JAK INHIBITOR
This invention relates to processes and intermediates for making {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, useful in the treatment of diseases related to the activity of Janus kinases (JAK) including inflammatory disorders, autoimmune disorders, cancer, and other diseases.
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Paragraph 0155

(2014/09/29)

Acylazetine as a dienophile in bioorthogonal inverse electron-demand Diels-Alder ligation
A new bioorthogonal N-acylazetine tag, suitable for tetrazine mediated inverse electron-demand Diels-Alder conjugation, is developed. The tag is small and achiral. We demonstrate the usefulness of N-acylazetine-tetrazine based bioorthogonal chemistry in two-step activity-based protein profiling. The performance of the new tetrazinophile in the labeling of catalytically active proteasome subunits was comparable to that of the more sterically demanding norbornene tag.
Engelsma, Sander B.,Willems, Lianne I.,Van Paaschen, Claudia E.,Van Kasteren, Sander I.,Van Der Marel, Gijsbert A.,Overkleeft, Herman S.,Filippov, Dmitri V.
supporting information
p. 2744 - 2747
(2014/06/09)

9-AMINOMETHYL SUBSTITUTED TETRACYCLINE COMPOUNDS
The present invention relates to 9-aminomethyl substituted tetracycline compounds represented by formula (I), or pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, as well as a method for preparing these compounds and a pharmaceutical composition comprising the same. The present invention relates also to a use of these compounds in the preparation of a medicament for the treatment and/or prophylaxis of tetracycline drug-sensitive disease. wherein, R2a, R2b, R3, R4a, R4b, R5, R6a, R6b, R7, R8, R9a, R9b, R10, R11, R12, R13a and R13b are each independently as defined in the description.
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Page/Page column

(2014/07/08)

HETEROCYCLIC COMPOUND AND H1 RECEPTOR ANTAGONIST
A heterocyclic compound useful as an antiallergic agent is provided. A compound represented by the following formula (1) or a salt thereof: wherein the ring A is a homocyclic or heterocyclic ring; the ring B is a heterocyclic ring which contains G and nitrogen atom N as constituent atoms thereof, wherein G is CH or N; R1 is a carbonyl group or an alkylene group; R2a and R2b are an alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; X is an oxygen atom or a sulfur atom; Z is a hydroxyl group, an alkoxy group, a cycloalkyloxy group, an aryloxy group, an aralkyloxy group, an amino group, or an N-substituted amino group; and n is 0 or 1; with the proviso that when the ring A is a benzene ring or when the ring B is a piperazine ring, R1 is an alkylene group which may have a substituent.
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Paragraph 0373; 0374; 0375; 0376

(2013/04/13)

2 - (2, 4, 5 - SUBSTITUTED -ANILINO) PYRIMIDINE DERIVATIVES AS EGFR MODULATORS USEFUL FOR TREATING CANCER
The present invention relates to certain 2-(2,4,5-substituted-anilino) pyrimidine compounds and pharmaceutically acceptable salts thereof which may be useful in the treatment or prevention of a disease or medical condition mediated through certain mutated forms of epidermal growth factor receptor (for example the L858R activating mutant, the Exonl9 deletion activating mutant and the T790M resistance mutant). Such compounds and salts thereof may be useful in the treatment or prevention of a number of different cancers. The invention also relates to pharmaceutical compositions comprising said compounds and salts thereof, especially useful polymorphic forms of these compounds and salts, intermediates useful in the manufacture of said compounds and to methods of treatment of diseases mediated by various different forms of EGFR using said compounds and salts thereof.
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(2013/03/26)

Synthesis and biological evaluation of novel azetidine derivatives as dopamine antagonist
In this study, azetidine derivatives were evaluated for their potency as dopaminergic antagonist. The study comprised derivatives substituted in 3-position with amide moiety. Further, the phenyl moiety of amide was modified at 2, 3, or 4-position. The substituted compounds were biologically evaluated for their affinity for D2 and D4 receptors. The most potent D2 and D4 antagonist among these compounds appeared to be the N-(1-benzhydryl-azetidin-3yl)-2-bromo-benzamide and N-(1-benzhydryl-azetidin-3yl)-4-bromo-benzamide, respectively. Various docking interactions of CPPMA with the D4 receptor and the same for compound 5 i.e., N-(1-benzhydryl-azetidin-3yl)-4-bromo-benzamide were found to have good correlation with observed biological activity.
Metkar, Shashikant D.,Bhatia, Manish S.,Desai, Uday V.
p. 5982 - 5989
(2013/11/06)

NOVEL TRIAZINE COMPOUNDS
The present invention relates to novel triazine compounds of formula (1), methods of their preparation, pharmaceutical compositions containing these compounds and the use of these compounds to treat proliferative disorders such as tumors and cancers and also other conditions and disorders related to or associated with dysregulation of PI3 Kinases, PI3 Kinase pathway, mTOR and/ or the mTOR pathway.
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Page/Page column 63

(2012/08/08)

Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders
To try and generate broad spectrum human rhinovirus VP1 inhibitors with more attractive physicochemical, DMPK and safety profiles, we explored the current SAR of known VP1 compounds. This lead to the identification of specific structural regions where reduction in polarity can be achieved, so guiding chemistry to analogues with significantly superior profiles to previously reported inhibitors.
Morley, Andrew,Tomkinson, Nicholas,Cook, Andrew,MacDonald, Catherine,Weaver, Richard,King, Sarah,Jenkinson, Lesley,Unitt, John,McCrae, Christopher,Phillips, Tim
supporting information; experimental part
p. 6031 - 6035
(2011/11/06)

AZETIDINE AND CYCLOBUTANE DERIVATIVES AS JAK INHIBITORS
The present invention relates to azetidine and cyclobutane derivatives, as well as their compositions, methods of use, and processes for preparation, which are JAK inhibitors useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.
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Page/Page column 62

(2009/09/28)

ANTIMICROBIAL HETEROCYCLIC COMPOUNDS FOR TREATMENT OF BACTERIAL INFECTIONS
The present invention provides heterocyclic compounds of the following formula (I) : or pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof useful as antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
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Page/Page column 70

(2008/12/08)

Rearrangement of dialkyl-2-(azetidin-3-yl)propane-1,3-dioates-a structural revision
The rearrangement reaction of dialkyl 2-[1-diphenylmethyl)azetidin-3-yl]propane-1,3-dioates during saponification was studied. Contrary to a previous report postulating the formation of a 4-(hydroxy-methyl)-2-oxo-pyrrolidine-3-carboxylic acid derivative, our analytical data showed that the rearrangement reaction led to a lactone ring. This structural revision is based on elemental analysis, IR and two-dimensional NMR studies.
Faust, Mark R.,Hoesl, Cornelia E.,Wanner, Klaus T.
experimental part
p. 2981 - 2988
(2009/05/31)

Benzofused heterozryl amide derivatives of thienopyridines useful as therapeutic agents, pharmaceutical compositions including the same, and methods for their use
The invention relates to compounds represented by the formula I and to prodrugs or metabolites thereof, or pharmaceutically acceptable salts or solvates of said compounds, said prodrugs, and said metabolites, wherein Z, Y, R11 and R14, R15, R16, and R17 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula I and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formula I.
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(2008/06/13)

GUANIDINO-SUBSTITUTED QUINAZOLINONE COMPOUNDS AS MC4-R AGONISTS
A variety of small molecule, guanidine-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases when administered to subjects. The compounds have the structure IA, IB, and IC where the values of the variables are defined herein.
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Page/Page column 126

(2008/06/13)

AZETIDINECARBOXAMIDE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CB1 RECEPTOR MEDIATED DISORDERS
Compounds of formula (I) and their use in therapy, particularly for the treatment of a disorder mediated by CB1 receptors such as obesity: Formuila (I) wherein: R1 and R2 are independently selected from aryl; and R3 is hydrogen or alkyl; or a pharmaceutically acceptable salt or prodrug thereof, wherein at least one of R1 and R2 has a non-hydrogen substituent in the ortho-position(s) thereof relative to the point of attachment to the [-CH-0-] group.
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Page 27

(2008/06/13)

BENZOFUSED HETEROARYL AMIDE DERIVATIVES OF THIENOPYRIDINES USEFUL AS THERAPEUTIC AGENTS, PHARMACEUTICAL COMPOSITIONS INCLUDING THE SAME, AND METHODS FOR THEIR USE
The invention relates to compounds represented by the formula I and to prodrugs or metabolites thereof, or pharmaceutically acceptable salts or solvates of said compounds, said prodrugs, and said metabolites, wherein Z, Y, R11 and R14, R15, R16, and R17 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula I and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formula I.
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Page 45

(2010/02/04)

Facile Syntheses of Azetidin-3-ols by Rearrangement of 2,3-Epoxypropylamines
The N-alkyl-2,3-epoxypropylamines (2) formed from primary alkylamines (1) and epichlorohydrin were chemoselectively rearranged to the four-membered rings, N-alkylazetidin-3-ols (3), upon treatment of triethylamine in refluxing acetonitrile.
Oh, Chang Ho,Rhim, Chul Yun,You, Choong Ho,Cho, Jin Rai
p. 4297 - 4302
(2007/10/03)

Cathepsin cysteine protease inhibitors
This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of Cathepsins K and L. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
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Page 21-22

(2010/02/06)

Azetidinecarboxamide derivatives for the treatment of CNS disorders
A compound of formula (1): wherein R1is aryl; and R2, R3, R4, R5and R6which may be the same or different are selected from H, alkyl and aryl; pharmaceutically acceptable addition compounds thereof and the use of the compounds in therapy, particularly for CNS disorders such as anxiety and epilepsy.
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(2008/06/13)

N-benzenesulfonyl L-proline compounds as bradykinin antagonists
This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof wherein X1 and X2 are halo; R1 andR2 are independently hydrogen or C1-4 alkyl; R3 and R4 are each hydrogen or halo; andR5 is(a) -C3-9 diazacycloalkyl optionally substituted with C5-11 azabicycloalkyl;(b) -C3-9 azacycloalkyl-NH-(C5-11 azabicycloalkyl optionally substituted with C1-4 alkyl);(c) -NH-C1-3 alkyl-C(O)-C5-11 diazabicycloalkyl;(d) -NH-C1-3 alkyl-C(O)-NH-C5-11 azabicycloalkyl, the C5-11 azabicycloalkyl being optionally substituted with C1-4 alkyl;(e) -C3-9 azacycloalkyl optionally substituted with C3-9 azacycloalkyl; or(f) -NH-C1-5 alkyl-NH-C(O)-C4-9 cycloalkyl-NH2. These compounds are useful for the treatment of medical conditions mediated by bradykinin such as inflammation, allergic rhinitis, pain, etc. This invention also provides a pharmaceutical composition comprising the above compound.
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Page 11

(2010/01/31)

Azetidinecarboxamide derivatives for treating CNS disorders
A compound of formula (1), wherein: R1is aryl; R2is H, alkyl or aryl; and R3is hydrogen or alkyl; pharmaceutically acceptable addition compounds thereof; and the use of the compounds in therapy, particularly for the treatment and prophylaxis of CNS disorders such as anxiety and epilepsy.
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(2008/06/13)

3-Azetidinylalkylpiperidines or -pyrrolidines as tachykinin antagonists
The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof. Such compounds and salts are tachykinin antagonists.
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(2008/06/13)

Piperidone tachykinin antagonists
The present invention provides compounds of formula (I) and the pharmaceutically acceptable acid addition salts thereof, wherein X is a direct link or C1-C4alkylene; and R is C3-C7cycloalkyl optionally substituted by 1 or 2 substituents each independently selected from fluoro and C3-C7cycloalkyl: with the proviso that X is not methylene when R is cyclopropyl, together with processes for the preparation of, intermediates used in the preparation of, compositions containing and uses of, such compounds. These compounds are useful as tachykinin antagonists.
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(2008/06/13)

Derivatives of azetidine and pyrrolidine
The invention relates to a compound having formula (I) wherein A is an optionally unsaturated 5- or 6-membered ring, which may comprise a heteroatom selected from N, O and S and which may be substituted with oxo or (1-6C)alkyl; R1, R2and R3are independently H, (1-6C)alkyl, (1-6C)alkoxy, (1-6C)alkoxy(1-6C)-alkyl, carbo(1-6C)alkoxy or halogen; X is O or S; and n is 1 or 2; or a pharmaceutically acceptable salt thereof, with the exception of 3-(naphth-1-yl-oxy)-pyrolidin and 3-(5,6,7,8-tetmhydro-naphth-1-yl-oxy)-pyrolidin. The compounds of the invention have antidepressant activity and can be used in treating or preventing serotonin-related diseases.
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(2008/06/13)

(Azetidin-1-ylalkyl) lactams as tachykinin antagonists
The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein R is C3 -C7 cycloalkyl, aryl or C1 -C6 alkyl, said C1 -C6 alkyl, said C1 -C6 alkyl being optionally substituted by fluoro, COOH, --COO(C1 -C4 alkyl), C3 -C7 cycloalkyl, adamantyl, aryl or het1, and said C3 -C7 cycloalkyl being optionally substituted by 1 or 2 substituents each independently selected from C1 -C4 alkyl, C3 -C7 cycloalkyl, C1 -C4 alkoxy, hydroxy, fluoro, fluoro (C1 -C4) alkyl and fluoro (C1 -C4) Alkoxy; R1 is phenyl, naphthyl, thienyl, benzothienyl or indolyl, each optionally substituted by 1 or 2 substituents each independently selected from C1 -C4 alkyl, C1 -C4 alkoxy, halo and trifluormethyl; R2 is --CO2 H, --CONR3 R4, --CONR5 (C3 -C7 cycloalkyl), --NR5 (C2 -C5 alkanoyl), --NR3 R4, --NR5 CONR5 R6, (C3 -C7 cycloalkyl-C1 -C4 alkyl)R5 N--, --NR5 COCF3, --NR5 SO2 CF3, --NR5 (SO2 C1 -C4 alkyl), --NR5 SO2 NR5 R6, --NR5 (SO2 aryl), --N(aryl) (SO2 C1 -C4 alkyl), --OR5, --O(C3 -C7 cycloalkyl), --SO2 NR5 R6, het3 or a group of formulas: (a), (b), (c), (d), (e), (f), (g) or (h); X is C1 -C4 alkylene; X1 is a direct link or C1 -C6 alkylene; X2 is a direct link, CO, SO2, or NR5 CO; and m is 0, 1 or 2; together with intermediates used in the preparation of compositions containing and the use as tachykinin angatonists of such derivatives. STR1
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(2008/06/13)

Azetidines
The present invention provides compounds of the formula (I): STR1 and the pharmaceutically acceptable salts thereof, wherein R is C3 -C7 cycloalkyl, aryl or C1 -C6 alkyl, said C1 -C6 alkyl being optionally substituted by fluoro, --COOH, --COO(C1 -C4) alkyl, C3 -C7 cycloalkyl, adamantyl, aryl or het1, and said C3 -C7 cycloalkyl being optionally substituted by 1 or 2 substituents each independently selected from C1 -C4 alkyl, C3 -C7 cycloalkyl, C1 -C4 alkoxy, hydroxy, fluoro, fluoro(C1 -C4) alkyl and fluoro(C1 -C4)alkoxy; R1 is phenyl, benzyl, naphthyl, thienyl, benzothienyl or indolyl, each optionally substituted by 1 or 2 substituents each independently selected from C1 -C4 alkyl, C1 -C4 alkoxy, halo and trifluoromethyl; R2 represents various groups; X is C1 -C4 alkylene; and X1 is a direct link or C1 -C6 alkylene. Such compounds and salts are useful as tachykinin antagonists.
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(2008/06/13)

3-aza and 3-oxa piperidone tachykinin antagonists
Compounds of the formula: STR1 wherein: X is O, NH or NR1 ; R1 is C1 -C6 alkyl, C3 -C7 cycloalkyl, C3 -C7 cycloalkyl(C1 -C4)alkyl, aryl or aryl (C1 -C4)alkyl; wherein the C1 -C6 alkyl group is optionally substituted by fluorine and the C3 -C7 cycloalkyl or C3 -C7 cycloalkyl(C1 -C4 )alkyl group is optionally substituted in the cycloalkyl ring by up to two substituents each independently selected from halo, C1 -C4 alkoxy or halo(C1 -C4)alkoxy; R2 is phenyl optionally substituted with one or two halo substituents, indolyl or thienyl; R3 is NH2, --NR4 SO2 (C1 -C6 alkyl), --NR4 SO2 aryl, --NR4 CO(C1 -C6 alkyl), --NR4 CO aryl or a 5 to 7-membered N-linked cyclic group incorporating W in the ring wherein W is O, NR5, CH(OH), CHCO2 H, CHN(R4)2, CHF, CF2, C=O or CH2 ; R4 is H or C1 -C6 alkyl; R5 is H, C1 -C6 alkyl, C3 -C7 cycloalkyl, C3 -C7 cycloalkyl(C1 -C6)alkyl, C2 -C6 alkanoyl, C4 -C8 cycloalkanoyl, C3 -C7 cycloalkyl(C2 -C6)alkanoyl, aryl CO--, C1 -C6 alkyl SO2 --, C3 -C7 cycloalkyl SO2 --, C3 -C7 cycloalkyl(C1 -C6)alkyl SO2 --, aryl-SO2 -- or (R6)2 NSO2 --, wherein each R6 is independently H or C1 -C4 alkyl or the two groups may be joined to form with the nitrogen atom to which they are attached, a pyrrolidinyl, piperidino, morphlino or piperazinyl group; m is 0, 1 or 2 with the proviso that m is not 0 when W is NR5, C=O, or O; and n is an integer of from 1 to 4; are neurokinin receptor antagonists of utility in the treatment of a variety of medical conditions including urinary incontinence, asthma and related conditions.
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(2008/06/13)

Derivatives of azetidine and pyrrolidine
The invention relates to a compound having the formula I wherein A is an optionally unsaturated 5- or 6-membered ring, which may comprise a heteroatom selected from N, O and S and which may be substituted with oxo or (1-6C)alkyl; R1, R2and R3are independently H, (1-6C)alkyl, (1-6C)alkoxy, (1-6C)alkoxy-(1-6C)alkyl, carbo(1-6C)alkoxy or halogen; X is O or S; and n is 1 or 2; or a pharmaceutically acceptable salt thereof, with the exception of 3-(naphth-1-yl-oxy)-pyrrolidin and 3-(5,6,7,8-tetrahydro-naphth-1-yl-oxy)-pyrrolidin., The compounds of the invention have antidepressant activity and can be used in treating or preventing serotonin-related diseases.
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(2008/06/13)

Imidazole, triazole and tetrazole derivatives
A class of substituted imidazole, triazole and tetrazole derivatives of formula (I), wherein the broken circle represents two non-adjacent double bonds in any position in the five-membered ring; two, three or four of V,W,X,Y and Z represent nitrogen and the remainder represent carbon provided that, when two of V,W,X,Y and Z represent nitrogen and the remainder represent carbon, then the said nitrogen atoms are in non-adjacent positions within the five-membered ring; E represents a bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms; F represents a group of formula (lI); U represents nitrogen or C--R2 ; B represents oxygen, sulphur or N--R3 ; are selective agonists of 5--HT1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.
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(2008/06/13)

Imidazole, Triazole and tetrazole derivatives
Imidazole, triazole and tetrazole derivatives of formula (I) are selective agonists of 5-HT1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated, wherein the broken circle represents two non-adjacent double bonds in any position in the five-membered ring; two, three or four of V, W, X, Y and Z represent nitrogen and the remainder represent carbon provided that, when two of V, W, X, Y and Z represent nitrogen and the remainder represent carbon, then the said nitrogen atoms are in non-adjacent positions within the five-membered ring; E represents a bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms; F represents a group of formula (a); U represents nitrogen or C--R2 ; B represents oxygen, sulphur or N--R3 ; R1 represents a group of formula (i), (ii) or (iii).
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(2008/06/13)

Novel 2-amino-1,4-dihydropyridine calcium antagonists. II. Synthesis and antihypertensive effects of 2-amino-1,4-dihydropyridine derivatives having N,N-dialkylaminoalkoxycarbonyl groups at 3- and/or 5-positions
Novel 2-amino-1,4-dihydropyridine derivatives I, which contain N,N-dialkylaminoalkoxycarbonyl groups at the 3- and/or 5-position, were synthesized and their antihypertensive effects were evaluated in spontaneously hypertensive rats. Remarkably prolonged duration of antihypertensive action was observed when a tertiary amino group was introduced into either the 3- or 5-ester side-chain of the 1,4-dihydropyridine ring. In particular, the compounds containing cyclic amino moieties at the 3-position showed greater potency than those with acyclic amino moieties. Chemical modification studies indicated that the two ester side-chains of 1,4-dihydropyridine at the 3- and 5-position might function in a different manner in relation to the antihypertensive activities. 3-(1-Benzhydrylazetidin-3-yl) 5-isopropyl 2-amino-1,4-dihydro-6-methyl-4-(3-nitrophenyl)-3,5-pyridine-dicarboxyl ate, I-43 (CS-905), exhibited potent and long-lasting antihypertensive effects with gradual onset of action, and is a promising candidate as an antihypertensive drug.
Kobayashi,Inoue,Nishino,Fujihara,Oizumi,Kimura
p. 797 - 817
(2007/10/02)

New synthesis of 2- azetines and 1-azabutadienes and the use of the latter in Diels-Alder reactions: Total synthesis of (±)-δ-coniceine
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Jung,Mi Choi
p. 6729 - 6730
(2007/10/02)

Antipsoriatic compositions
Disclosed herein are compositions containing 1-substituted-3-alkanesulfonyloxyazetidines, useful in the treatment of psoriasis.
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(2008/06/13)